PHAR 6020 Drug List

DHEA

..Dehydroepiandrosterone (DHEA; brand name Fidelin), also known as androstenolone or prasterone (INN), as well as 3β-hydroxyandrost-5-en-17-one or 5-androsten-3β-ol-17-one, is an important endogenous steroid hormone.[1] It is the most abundant circulating steroid in humans,[2] in whom it is produced in the adrenal glands,[3] the gonads, and the brain,[4] where it functions predominantly as a metabolic intermediate in the biosynthesis of the androgen and estrogen sex steroids.[1][5] However, DHEA also has a variety of potential biological effects in its own right, binding to an array of nuclear and cell surface receptors,[6] and acting as a neurosteroid.[7]

Armour

..Desiccated thyroid or thyroid extract, refers to porcine (or mixed beef and pork) thyroid glands, dried and powdered for therapeutic use. Pork (or mixed beef and pork) thyroid preparations were developed in the late 19th century, and are still used today to treat hypothyroidism, the condition of having an underactive thyroid gland. This product is sometimes referred to as "natural thyroid", "natural thyroid hormones", "pork thyroid", thyroid USP, thyroid BP, or by the name of a commercial brand, such as "Armour Thyroid" or "Nature-Throid" & "Westhroid". Desiccated thyroid has been described in the United States Pharmacopoeia for nearly a century as the cleaned, dried, and powdered thyroid gland previously deprived of connective tissue and fat... obtained from domesticated animals that are used for food by man (USP XVI). In the last few decades, pork alone is the usual source. Historically, before modern assays, the potency was specified only by iodine content ("not less than 0.17% and not more than 0.23%"), rather than hormonal content or activity. Brands include Forest Lab's Armour, and Naturethroid & Westhroid by RLC Labs. Also available is a new generic NP thyroid by Acella Pharmaceuticals. Canada's desiccated thyroid is made by Erfa and is called Thyroid. All consist of desiccated porcine thyroid powder, differing only in the binders and fillers. Nature-Throid and Westhroid are available in the following strengths: 1/4(16.25 mg), 1/2(32.5 mg), 3/4(48.75 mg), 1(65 mg), 1.25(81.25 mg), 1.5(97.5 mg), 1.75(113.75), 2(130 mg), 2.25(146.25 mg), 2.5(162.5 mg), 3(195 mg), 4(260 mg), & 5(325 mg) grain. Each one grain (65 mg) contains 9 mcg of T3, and 38 mcg of T4. All brands contain a mixture of thyroid hormones: T4 (thyroxine), T3 (triiodothyronine) in the proportions usually present in pig thyroids (approximately 80% T4 and 20% T3). Armour is made in the following strengths: 1/4, 1/2, 1, 2, and 3 grain as well as 4 and 5 grain tablets. One grain (about 60 mg) of desiccated thyroid contains about 38 mcg of T4 and 9 mcg of T3.[1] Because the preparation is whole thyroid gland, each 60 mg tablet also contains over 59 mg of all of the other constituents of pork thyroid glands.

Exenatide

..Exenatide (INN, marketed as Byetta, Bydureon) is a glucagon-like peptide-1 agonist (GLP-1 agonist) medication approved in April 2005 for the treatment of diabetes mellitus type 2. It belongs to the group of incretin mimetics and is manufactured by Amylin Pharmaceuticals. Exenatide in its Byetta form is administered as a subcutaneous injection (under the skin) of the abdomen, thigh, or arm, any time within the 60 minutes before the first and last meal of the day.[1] A once-weekly injection has been approved as of January 27, 2012 under the trademark Bydureon.[2]

Finasteride

..Finasteride (brand names Proscar and Propecia by Merck, among other generic names) is a synthetic drug approved by the FDA for the treatment of benign prostatic hyperplasia (BPH) and male pattern baldness (MPB). It is a type II 5α-reductase inhibitor. 5α-reductase is an enzyme that converts testosterone to dihydrotestosterone (DHT).

Lispro

..Insulin lispro (marketed by Eli Lilly and Company as "Humalog") is a fast acting insulin analogue. It was first approved for use in the United States in 1996, making it the first insulin analogue to enter the market.[1] Engineered through recombinant DNA technology, the penultimate lysine and proline residues on the C-terminal end of the B-chain are reversed. This modification does not alter receptor binding, but blocks the formation of insulin dimers and hexamers. This allowed larger amounts of active monomeric insulin to be immediately available for postprandial injections.[2] Insulin lispro has one primary advantage over regular insulin for postprandial glucose control. It has a shortened delay of onset, allowing slightly more flexibility than regular insulin, which requires a longer waiting period before starting a meal after injection. Both preparations should be coupled with a longer acting insulin for good glycemic control.

regular

..Medical preparations of insulin (from the major suppliers - Eli Lilly, Novo Nordisk, and Sanofi Aventis - or from any other) are never just 'insulin in water'. Clinical insulins are specially prepared mixtures of insulin plus other substances including preservatives. These delay absorption of the insulin, adjust the pH of the solution to reduce reactions at the injection site, and so on. Slight variations of the human insulin molecule are called insulin analogues, (technically "insulin receptor ligands") so named because they are not technically insulin, rather they are analogues which retain the hormone's glucose management functionality. They have absorption and activity characteristics not currently possible with subcutaneously injected insulin proper. They are either absorbed rapidly in an attempt to mimic real beta cell insulin (as with Lilly's lispro, Novo Nordisk's aspart and Sanofi Aventis' glulisine), or steadily absorbed after injection instead of having a 'peak' followed by a more or less rapid decline in insulin action (as with Novo Nordisk's version Insulin detemir and Sanofi Aventis's Insulin glargine), all while retaining insulin's glucose-lowering action in the human body. However, a number of meta-analyses, including those done by the Cochrane Collaboration in the United Kingdom in 2002,[9] Germany's Institute for Quality and Cost Effectiveness in the Health Care Sector [IQWiG] released in 2007,[10] and the Canadian Agency for Drugs and Technology in Health (CADTH)[11] also released in 2007 have shown no unequivocal advantages in clinical use of insulin analogues over more conventional insulin types. Choosing insulin type and dosage/timing should be done by an experienced medical professional working closely with the diabetic patient. The commonly used types of insulin are: Fast-acting: Includes the insulin analogues aspart, lispro, and glulisine. These begin to work within 5 to 15 minutes and are active for 3 to 4 hours. Most insulins form hexamers which delay entry into the blood in active form; these analog insulins do not, but have normal insulin activity. Newer varieties are now pending regulatory approval in the U.S. which are designed to work rapidly, but retain the same genetic structure as regular human insulin.[12][13] Short-acting: Includes regular insulin which begins working within 30 minutes and is active about 5 to 8 hours. Intermediate-acting: Includes NPH insulin which begins working in 1 to 3 hours and is active 16 to 24 hours. Long acting: Includes the analogues glargine and detemir, each of which begins working within 1 to 2 hours and continue to be active, without major peaks or dips, for about 24 hours, although this varies in many individuals. Ultra-long acting: Currently only includes the analogue degludec, which begins working within 30-90 minutes, and continues to be active for greater than 24 hours.[2] Combination insulin products - Includes a combination of either fast-acting or short-acting insulin with a longer acting insulin, typically an NPH insulin. The combination products begin to work with the shorter acting insulin (5-15 minutes for fast-acting, and 30 minutes for short acting), and remain active for 16 to 24 hours. There are several variations with different proportions of the mixed insulins (e.g. Novolog Mix 70/30 contains 70% aspart protamine [akin to NPH], and 30% aspart.)

medroxyprogesterone acetate

..Medroxyprogesterone acetate (INN, USAN, BAN), also known as 17α-hydroxy-6α-methylprogesterone acetate, and commonly abbreviated as MPA, is a steroidal progestin, a synthetic variant of the human hormone progesterone.[2][3] It is used as a contraceptive, in hormone replacement therapy and for the treatment of endometriosis as well as several other indications. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate,[3] what is normally being administered is MPA and not MP.[4]

Metoprolol

..Metoprolol (pron.: /mɛˈtoʊproʊlɑːl/) is a selective β1 receptor blocker used in treatment of several diseases of the cardiovascular system, especially hypertension. The active substance metoprolol is employed either as metoprolol succinate or metoprolol tartrate (where 100 mg metoprolol tartrate corresponds to 95 mg metoprolol succinate). The tartrate is an immediate-release and the succinate is an extended-release formulation.[1]

Misoprostal

..Misoprostol is a synthetic prostaglandin E1 (PGE1) analog that is used for the prevention of nonsteroidal anti-inflammatory drug (NSAID) induced gastric ulcers, to treat missed miscarriage, to induce labor, and as an abortifacient. The latter use is controversial in the United States. Misoprostol was invented and marketed by G.D. Searle & Company (now Pfizer) under the trade name Cytotec, but other brand-name and generic formulations are now available as well.

CEE

..Premarin is the commercial name for a medication consisting primarily of conjugated estrogens. Isolated from mares' urine (pregnant mares' urine), it is manufactured by Wyeth Pharmaceuticals (part of Pfizer since January 2009) and has been marketed since 1942. It is available in oral (0.3/​0.45/​0.625/​0.9/​1.25 mg), IV, and topical (vaginal) form.[1 The major forms of estrogen in Premarin are estrone (>50%), equilin (15-25%) and equilenin. The estrogens in Premarin are often called "conjugated equine estrogens" (CEE) because the estrogen molecules are generally present with hydrophilic side-groups attached such as sulfate. Thus, estrone sulfate is actually the major active constituent in Premarin. Estrone sulfate is easily absorbed into the blood after Premarin pills are taken by women. Estrone sulfate is converted to estradiol, an active estrogen normally found in women. It is not clear if estrogens such as equilin that are foreign to the human body have effects in women that are significantly different from the estrogens like estradiol that are normally made in the human body.

Propranolol

..Propranolol (INN) is a sympatholytic non-selective beta blocker. Sympatholytics are used to treat hypertension, anxiety and panic. It was the first successful beta blocker developed.[1] Propranolol is available in generic form as propranolol hydrochloride, Marketed in India under brand names like Ciplar and Ciplar LA Cipla ltd also other brands from AstraZeneca and Wyeth under the brand names Inderal, Inderal LA, Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum, Bedranol SR (Sandoz)Propranolol is a non-selective beta blocker, that is, it blocks the action of epinephrine and norepinephrine on both β1- and β2-adrenergic receptors. It has little intrinsic sympathomimetic activity (ISA) but has strong membrane stabilizing activity (only at high blood concentrations, e.g. overdosage). Research has also shown that propranolol has inhibitory effects on the norepinephrine transporter and/or stimulates norepinephrine release (present experiments have shown that the concentration of norepinephrine is increased in the synapse but do not have the ability to discern which effect is taking place).[31] Since propranolol blocks β-adrenoceptors, the increase in synaptic norepinephrine only results in α-adrenergic activation, with the α1-adrenoceptor being particularly important for effects observed in animal models. Therefore, some have suggested that it be looked upon as an indirect α1 agonist as well as a β antagonist. Probably owing to the effect at the α1-adrenoceptor, the racemic and the individual enantiomers of propranolol have been shown to substitute for cocaine in rats, with the most potent enantiomer being S-(-)-propranolol. In addition, some evidence suggests that propranolol may function as a partial agonist at one or more serotonin receptors (possibly 5-HT1B). Both enantiomers of the drug have a local anesthetic (topical) effect, which is normally mediated by blockade of voltage-gated sodium channels. Few studies have demonstrated propranolol's ability to block cardiac, neuronal, and skeletal voltage-gated sodium channels, accounting for its known "membrane stabilizing effect" and anti-arrhythmic and other central nervous system effects.[32][33][34]

Repaglinide

..Repaglinide is an antidiabetic drug in the class of medications known as meglitinides, and was invented in 1983. It is sold by Novo Nordisk under the name of Prandin in the U.S., GlucoNorm in Canada, Surepost in Japan,Repaglinide in Egypt by EIPICO, and NovoNorm elsewhere. In Japan it is produced by Dainippon Sumitomo Pharma.

Testosterone

..Testosterone is a steroid hormone from the androgen group and is found in mammals, reptiles,[1] birds,[2] and other vertebrates. In mammals, testosterone is primarily secreted in the testicles of males and the ovaries of females, although small amounts are also secreted by the adrenal glands. It is the principal male sex hormone and an anabolic steroid. In men, testosterone plays a key role in the development of male reproductive tissues such as the testis and prostate as well as promoting secondary sexual characteristics such as increased muscle, bone mass, and the growth of body hair.[3] In addition, testosterone is essential for health and well-being[4] as well as the prevention of osteoporosis.[5] Testosterone levels decline gradually with age in human beings. The clinical significance of this decrease is debated (see andropause). There is disagreement about when to treat aging men with testosterone replacement therapy. The American Society of Andrology's position is that "testosterone replacement therapy in aging men is indicated when both clinical symptoms and signs suggestive of androgen deficiency and decreased testosterone levels are present."[83] The American Association of Clinical Endocrinologists says "Hypogonadism is defined as a free testosterone level that is below the lower limit of normal for young adult control subjects. Previously, age-related decreases in free testosterone were once accepted as normal. Currently, they are not considered normal. Patients with borderline testosterone levels warrant a clinical trial of testosterone."[84] There is not total agreement on the threshold of testosterone value below which a man would be considered hypogonadal. (Currently there are no standards as to when to treat women.) Testosterone can be measured as "free" (that is, bioavailable and unbound) or more commonly, "total" (including the percentage which is chemically bound and unavailable). In the United States, male total testosterone levels below 300 ng/dL from a morning serum sample are generally considered low.[85] Identification of inadequate testosterone in an aging male by symptoms alone can be difficult. Adverse effects of testosterone supplementation include minor side effects such as acne and oily skin, and more significant complications such as increased hematocrit which can require venipuncture in order to treat, exacerbation of sleep apnea and acceleration of pre-existing prostate cancer growth in individuals who have undergone androgen deprivation. Another adverse effect may be significant hair loss and/or thinning of the hair. This may be prevented with Propecia (Finasteride), which blocks DHT (a byproduct of testosterone in the body), during treatment. Exogenous testosterone also causes suppression of spermatogenesis and can lead to infertility.[86] It is recommended that physicians screen for prostate cancer with a digital rectal exam and PSA (prostate specific antigen) level before starting therapy, and monitor hematocrit and PSA levels closely during therapy.

Rosiglitazone

.Rosiglitazone (trade name Avandia, GlaxoSmithKline) is an antidiabetic drug in the thiazolidinedione class of drugs. It works as an insulin sensitizer, by binding to the PPAR receptors in fat cells and making the cells more responsive to insulin. It is marketed by the pharmaceutical company GlaxoSmithKline (GSK) as a stand-alone drug or in combination with metformin (trade name Avandamet) or with glimepiride (trade name Avandaryl). First released in 1999, annual sales peaked at approximately $2.5bn in 2006, but declined after the drug was found to increase risk of heart attacks. The drug's patent expired in 2012.[1] Concerns about rosiglitazone's adverse effects has reduced its use despite the benefits it offers in treating diabetes.[2] Adverse effects caused by rosiglitazone are currently the subject of over 13,000 lawsuits against GSK.[3] As of July 2010, GSK has agreed to settlements on more than 11,500 of these suits. The drug is controversial and is estimated to have caused 83,000 heart attacks in the United States alone. Some reviewers have recommended rosiglitazone be taken off the market, but a Food and Drug Administration panel disagreed, and it remains available in the U.S., subject to significant restrictions.[4] From November 18, 2011, the federal government will not allow Avandia to be sold without a prescription from certified doctors. Patients will be required to be informed of the risks associated with its use, and the drug will be required to be purchased by mail order through specified pharmacies.[5] In Europe, the European Medicines Agency (EMA) recommended in September 2010 that the drug be suspended from the European market. However, patients currently taking rosiglitazone are advised to discuss alternative options during their next physician appointment.[6][7] In New Zealand, rosiglitazone was withdrawn from the market in April 2011.[8].

Aspart

A fast acting insulin analog (marketed by Novo Nordisk as "NovoLog/NovoRapid") is a man-made form of human insulin. A single amino acid has been slightly changed in its molecular structure. This change helps the fast-acting insulin analog absorb quickly into the bloodstream. As a result, it starts working in minutes, which allows you to take insulin and eat right away. Fast-acting insulin analogs are considered to act similar to the way insulin is released in people without diabetes mellitus. Novolog allows for a flexible dosing schedule, which allows the patient to adjust their insulin according to any changes in their eating habits.[1] The safety and efficacy of Insulin aspart (NovoLog/NovoRapid) in real life clinical practice was evaluated in the A1chieve study. It was created through recombinant DNA technology so that the amino acid, B28, which is normally proline, is substituted with an aspartic acid residue. This analogue has increased charge repulsion, which prevents the formation of hexamers, to create a faster acting insulin. The sequence was inserted into the yeast genome, and the yeast expressed the insulin analogue, which was then harvested from a bioreactor. According to JDRF, insulin aspart was approved for marketing in the United States by the Food and Drug Administration in June 2000.[citation needed]

Acarbose

Acarbose is an anti-diabetic drug used to treat type 2 diabetes mellitus and, in some countries, prediabetes. It is a generic sold in Europe and China as Glucobay (Bayer AG), in North America as Precose (Bayer Pharmaceuticals), and in Canada as Prandase (Bayer AG). It is cheap and popular in China, but not in the U.S., because it is not potent enough to justify the side effects of diarrhea and flatulation.[1] It is a starch blocker, and inhibits alpha glucosidase, an intestinal enzyme that releases glucose from larger carbohydrates. It is composed of an acarviosin moiety with a maltose at the reducing terminus.

Alendronate

Alendronic acid (INN) or alendronate sodium (USAN) — sold as Fosamax by Merck — is a bisphosphonate drug used for osteoporosis and several other bone diseases. It is marketed alone as well as in combination with vitamin D (2,800 IU and 5600 IU, under the name Fosamax+D). Merck's U.S. patent on alendronate expired in 2008 and Merck lost a series of appeals to block a generic version of the drug from being certified by the U.S. Food and Drug Administration (FDA). On February 6, 2008, the US FDA approved the first generic versions of alendronate, which were marketed by Barr Pharmaceuticals and Teva Pharmaceuticals USA. Teva Pharmaceuticals manufactures generic alendronate in 5-milligram, 10-milligram, and 40-milligram daily doses, and in 35-milligram and 70-milligram weekly doses, while Barr made generic alendronate in 70-milligram tablets, which were taken once weekly.[1] Barr pharmaceuticals were subsequently acquired by Teva in July 2008.

Diethylproprion

Amfepramone (INN, other names diethylcathinone and diethylpropion, trade names Anorex, Linea, Nobesine, Prefamone, Regenon, Tepanil, Tenuate), is a stimulant drug of the phenethylamine, amphetamine, and cathinone chemical classes that is used as an appetite suppressant.Amfepramone itself lacks any affinity for the monoamine transporters and instead functions as a prodrug to ethcathinone.[1] Ethcathinone (and therefore amfepramone as well) is a very weak dopaminergic and serotonergic, and is approximately 10x and 20x stronger on norepinephrine in comparison, respectively.[1] As a result, ethcathinone and amfepramone can essentially be considered selective norepinephrine releasing agents (NRAs).

Amiodarone

Amiodarone (sold under the brand name Nexterone by Baxter Healthcare Corporation) is an antiarrhythmic agent used for various types of cardiac dysrhythmias, both ventricular and atrial. It was discovered in 1961. Despite relatively common side-effects, it is used in arrhythmias that are otherwise difficult to treat with medication.Amiodarone is categorized as a class III antiarrhythmic agent, and prolongs phase 3 of the cardiac action potential, the repolarization phase where there is normally decreased calcium permeability and increased potassium permeability. It has numerous other effects however, including actions that are similar to those of antiarrhythmic classes Ia, II, and IV. Amiodarone shows beta blocker-like and potassium channel blocker-like actions on the SA and AV nodes, increases the refractory period via sodium- and potassium-channel effects, and slows intra-cardiac conduction of the cardiac action potential, via sodium-channel effects. Amiodarone chemically resembles thyroxine (thyroid hormone), and its binding to the nuclear thyroid receptor might contribute to some of its pharmacologic and toxic actions[8

Anastrozole

Anastrozole (INN) (marketed under the trade name Arimidex by AstraZeneca) is an aromatase-inhibiting drug approved for treatment of breast cancer after surgery, as well as for metastasis in both pre and post-menopausal women. The severity of breast cancer is increased by estrogen, as sex hormones cause hyperplasia, and differentiation at estrogen receptor sites.[3] Anastrozole works by inhibiting the synthesis of estrogen. The patent on Arimidex by AstraZeneca expired June 2010.

ASA (aspirin)

Aspirin (USAN), also known as acetylsalicylic acid (/əˌsɛtəlˌsælɨˈsɪlɨk/ ə-set-əl-sal-i-sil-ik; abbreviated ASA), is a salicylate drug, often used as an analgesic to relieve minor aches and pains, as an antipyretic to reduce fever, and as an anti-inflammatory medication. Aspirin was first isolated by Felix Hoffmann, a chemist with the German company Bayer in 1897.[1][2] Salicylic acid, the main metabolite of aspirin, is an integral part of human and animal metabolism. While in humans much of it is attributable to diet, a substantial part is synthesized endogenously.[3] Aspirin also has an antiplatelet effect by inhibiting the production of thromboxane, which under normal circumstances binds platelet molecules together to create a patch over damaged walls of blood vessels. Because the platelet patch can become too large and also block blood flow, locally and downstream, aspirin is also used long-term, at low doses, to help prevent heart attacks, strokes, and blood clot formation in people at high risk of developing blood clots.[4] It has also been established that low doses of aspirin may be given immediately after a heart attack to reduce the risk of another heart attack or of the death of cardiac tissue.[5][6] Aspirin may be effective at preventing certain types of cancer, particularly colorectal cancer.[7][7][8][9] The main undesirable side effects of aspirin taken by mouth are gastrointestinal ulcers, stomach bleeding, and tinnitus, especially in higher doses. In children and adolescents, aspirin is no longer indicated to control flu-like symptoms or the symptoms of chickenpox or other viral illnesses, because of the risk of Reye's syndrome.[10] Aspirin is part of a group of medications called nonsteroidal anti-inflammatory drugs (NSAIDs), but differs from most other NSAIDs in the mechanism of action. Though it, and others in its group called the salicylates, have similar effects (antipyretic, anti-inflammatory, analgesic) to the other NSAIDs and inhibit the same enzyme cyclooxygenase, aspirin (but not the other salicylates) does so in an irreversible manner and, unlike others, affects more the COX-1 variant than the COX-2 variant of the enzyme.[11] Today, aspirin is one of the most widely used medications in the world, with an estimated 40,000 tonnes of it being consumed each year.[12] In countries where Aspirin is a registered trademark owned by Bayer, the generic term is acetylsalicylic acid (ASA).[13Aspirin's ability to suppress the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the cyclooxygenase (PTGS) enzyme required for prostaglandin and thromboxane synthesis. Aspirin acts as an acetylating agent where an acetyl group is covalently attached to a serine residue in the active site of the PTGS enzyme. This makes aspirin different from other NSAIDs (such as diclofenac and ibuprofen), which are reversible inhibitors. Low-dose, long-term aspirin use irreversibly blocks the formation of thromboxane A2 in platelets, producing an inhibitory effect on platelet aggregation. This antithrombotic property makes aspirin useful for reducing the incidence of heart attacks.[110] 40 mg of aspirin a day is able to inhibit a large proportion of maximum thromboxane A2 release provoked acutely, with the prostaglandin I2 synthesis being little affected; however, higher doses of aspirin are required to attain further inhibition.[111] Prostaglandins, local hormones produced in the body, have diverse effects, including the transmission of pain information to the brain, modulation of the hypothalamic thermostat, and inflammation. Thromboxanes are responsible for the aggregation of platelets that form blood clots. Heart attacks are caused primarily by blood clots, and low doses of aspirin are seen as an effective medical intervention for acute myocardial infarction. An unwanted side effect of the effective anticlotting action of aspirin is that it may cause excessive bleeding. [edit]COX-1 and COX-2 inhibition There are at least two different types of cyclooxygenase: COX-1 and COX-2. Aspirin irreversibly inhibits COX-1 and modifies the enzymatic activity of COX-2. COX-2 normally produces prostanoids, most of which are proinflammatory. Aspirin-modified PTGS2 produces lipoxins, most of which are anti-inflammatory.[112] Newer NSAID drugs, COX-2 inhibitors (coxibs), have been developed to inhibit only PTGS2, with the intent to reduce the incidence of gastrointestinal side effects.[12] However, several of the new COX-2 inhibitors, such as rofecoxib (Vioxx), have been withdrawn recently, after evidence emerged that PTGS2 inhibitors increase the risk of heart attack and stroke.[113][114] Endothelial cells lining the microvasculature in the body are proposed to express PTGS2, and, by selectively inhibiting PTGS2, prostaglandin production (specifically, PGI2; prostacyclin) is downregulated with respect to thromboxane levels, as PTGS1 in platelets is unaffected. Thus, the protective anticoagulative effect of PGI2 is removed, increasing the risk of thrombus and associated heart attacks and other circulatory problems. Since platelets have no DNA, they are unable to synthesize new PTGS once aspirin has irreversibly inhibited the enzyme, an important difference with reversible inhibitors. [edit]Additional mechanisms Aspirin has been shown to have at least three additional modes of action. It uncouples oxidative phosphorylation in cartilaginous (and hepatic) mitochondria, by diffusing from the inner membrane space as a proton carrier back into the mitochondrial matrix, where it ionizes once again to release protons.[115] In short, aspirin buffers and transports the protons. When high doses of aspirin are given, it may actually cause fever, owing to the heat released from the electron transport chain, as opposed to the antipyretic action of aspirin seen with lower doses. In addition, aspirin induces the formation of NO-radicals in the body, which have been shown in mice to have an independent mechanism of reducing inflammation. This reduced leukocyte adhesion, which is an important step in immune response to infection; however, there is currently insufficient evidence to show that aspirin helps to fight infection.[116] More recent data also suggest salicylic acid and its derivatives modulate signaling through NF-κB.[117] NF-κB, a transcription factor complex, plays a central role in many biological processes, including inflammation. Aspirin is readily broken down in the body to salicylic acid, which itself has anti-inflammatory, antipyretic, and analgesic effects. In 2012, salicylic acid was found to activate AMP-activated protein kinase, and this has been suggested as a possible explanation for some of the effects of both salicylic acid and aspirin.[118][119] The acetyl portion of the aspirin molecule is not without its own targets. Acetylation of cellular proteins is a well-established phenomenon in the regulation of protein function at the posttranslational level. Recent studies have reported aspirin is able to acetylate several other targets in addition to COX isoenzymes.[120][121] These acetylation reactions may explain many hitherto unexplained effects of aspirin.

Enoxaparin (LMWH)

Bemiparin is an antithrombotic and belongs to the group of low molecular weight heparins (LMWH).[1] Like semuloparin, bemiparin is classified as an ultra-LMWH because of its low molecular mass of 3600 Daltons on average.[2] (Enoxaparin has 4500 Daltons.) These heparins have lower anti-thrombin activity than classical LMWHs and act mainly on factor Xa, reducing the risk of bleeding.[3] [edit]

Calcitonin

Calcitonin (also known as thyrocalcitonin) is a 32-amino acid linear polypeptide hormone that is produced in humans primarily by the parafollicular cells (also known as C-cells) of the thyroid, and in many other animals in the ultimobranchial body.[2] It acts to reduce blood calcium (Ca2+), opposing the effects of parathyroid hormone (PTH).[3] Calcitonin has been found in fish, reptiles, birds, and mammals. Its importance in humans has not been as well established as its importance in other animals, as its function is usually not significant in the regulation of normal calcium homeostasis.[4] It belongs to calcitonin-like protein family.

Captopril

Captopril (rINN) (pron.: /ˈkæptəprɪl/) is an angiotensin-converting enzyme (ACE) inhibitor used for the treatment of hypertension and some types of congestive heart failure. Captopril was the first ACE inhibitor developed and was considered a breakthrough both because of its novel mechanism of action and also because of the revolutionary development process. Captopril is commonly marketed by Bristol-Myers Squibb under the trade name Capoten. Captopril's main uses are based on its vasodilation and inhibition of some renal function activities. These benefits are most clearly seen in the following conditions: 1) Hypertension 2) Cardiac conditions such as congestive heart failure and after myocardial infarction 3) Preservation of kidney function in diabetic nephropathy Additionally, it has shown mood-elevating properties in some patients. This is consistent with the observation that animal screening models indicate putative antidepressant activity for this compound, although there has been one negative study. Formal clinical trials in depressed patients have not been reported.[2] It has also been investigated for use in the treatment of cancer.[3]

Cholestyramine

Cholestyramine or colestyramine (Questran, Questran Light, Cholybar) is a bile acid sequestrant, which binds bile in the gastrointestinal tract to prevent its reabsorption. It is a strong ion exchange resin, which means that it can exchange its chloride anions with anionic bile acids in the gastrointestinal tract and bind them strongly in the resin matrix. The functional group of the anion exchange resin is a quaternary ammonium group attached to an inert styrene-divinylbenzene copolymer. Cholestyramine removes bile acids from the body by forming insoluble complexes with bile acids in the intestine, which are then excreted in the feces. When bile acids are excreted, plasma cholesterol is converted to bile acid to normalize bile acid levels. This conversion of cholesterol into bile acids lowers plasma cholesterol concentrations.

Clomiphene

Clomifene (INN) or clomiphene (USAN) (trademarked as Clomid and Omifin) is a selective estrogen receptor modulator (SERM) that increases production of gonadotropins by inhibiting negative feedback on the hypothalamus. This synthetic drug comes supplied as white, round tablets in 50 mg strength only. It has become the most widely prescribed of all fertility drugs. It is used in the form of its citrate to induce ovulation. It is used mainly in female infertility, in turn mainly as ovulation induction to reverse oligoovulation or anovulation such as in infertility in polycystic ovary syndrome, as well as being used for ovarian hyperstimulation, such as part of an in vitro fertilization procedure.

Clonidine

Clonidine (trade name Kapvay or Nexiclon) is a sympatholytic medication used to treat medical conditions, such as high blood pressure, ADHD, anxiety/panic disorder, and certain pain conditions. It is classified as a centrally acting α2 adrenergic agonist. An alternative hypothesis that has been proposed is that clonidine acts centrally as an imidazoline receptor agonist.Clonidine treats high blood pressure by stimulating α2 receptors in the brain, which decreases cardiac output and peripheral vascular resistance, lowering blood pressure. It has specificity towards the presynaptic α2 receptors in the vasomotor center in the brainstem. This binding decreases presynaptic calcium levels, and inhibits the release of norepinephrine (NE). The net effect is a decrease in sympathetic tone.[21] It has also been proposed that the antihypertensive effect of clonidine is due to agonism on the I1-receptor (imidazoline receptor), which mediates the sympatho-inhibitory actions of imidazolines to lower blood pressure.[22]

Clopidogrel

Clopidogrel (INN) is an oral, thienopyridine class antiplatelet agent used to inhibit blood clots in coronary artery disease, peripheral vascular disease, and cerebrovascular disease. It is marketed by Bristol-Myers Squibb and Sanofi under the trade name Plavix. The drug works by irreversibly inhibiting a receptor called P2Y12, an adenosine diphosphate (ADP) chemoreceptor on platelet cell membranes. Adverse effects include hemorrhage, severe neutropenia, and thrombotic thrombocytopenic purpura (TTP).Clopidogrel is a prodrug, the action of which may be related to an ADP receptor on platelet cell membranes. The drug specifically and irreversibly inhibits the P2Y12 subtype of ADP receptor, which is important in activation of platelets and eventual cross-linking by the protein fibrin.[1] Platelet inhibition can be demonstrated two hours after a single dose of oral clopidogrel, but the onset of action is slow, so that a loading-dose of 300 mg is usually administered. [edit]

Chromolyn sodium

Cromoglicic acid (INN) (also referred to as cromolyn (USAN), cromoglycate (former BAN), or cromoglicate) is traditionally described as a mast cell stabilizer, and is commonly marketed as the sodium salt sodium cromoglicate or cromolyn sodium. This drug prevents the release of inflammatory chemicals such as histamine from mast cells. Because of their convenience (and perceived safety), leukotriene receptor antagonists have largely replaced it as the non-corticosteroid treatment of choice in the treatment of asthma. Cromoglicic acid requires administration four times daily, and does not provide additive benefit in combination with inhaled corticosteroids.[1]"Cromolyn works because it prevents the release of mediators that would normally attract inflammatory cells and because it stabilizes the inflammatory cells."[6] Nedocromil is another mast cell stabilizer that also works in controlling asthma. The underlying mechanism of action is not fully understood; for while cromoglicate stabilizes mast cells, this mechanism is probably not why it works in asthma.[7] Pharmaceutical companies have produced 20 related compounds that are equally or more potent at stabilising mast cells and none of them have shown any anti-asthmatic effect.[7] It is more likely that these work by inhibiting the response of sensory C fibers to the irritant capsaicin, inhibiting local axon reflexes involved in asthma, and may inhibit the release of preformed T cell cytokines and mediators involved in asthma. (see review by Garland, 1991) It is known to somewhat inhibit chloride channels (37% +/- 7%) [8] and thus may inhibit the: exaggerated neuronal reflexes triggered by stimulation of irritant receptors on sensory nerve endings (e.g. exercise-induced asthma) release of preformed cytokines from several type of inflammatory cells (T cells, eosinophils) in allergen-induced asthma Note: Another chemical (NPPB: 5-nitro-2(3-phenyl) propylamino-benzoic acid) was shown, in the same study, to be a more effective chloride channel blocker. Finally it may act by inhibiting calcium influx. Cromoglicate is classified as a chromone. [edit]

Erythropoietin (darbopoietin)

Darbepoetin alfa (rINN) (pron.: /dɑrbəˈpɔɪtɨn/) is a synthetic form of erythropoietin. It stimulates erythropoiesis (increases red blood cell levels) and is used to treat anemia, commonly associated with chronic renal failure and cancer chemotherapy. Darbepoetin is marketed by Amgen under the trade name Aranesp. The drug was approved in September 2001 by the Food and Drug Administration for treatment of anemia in patients with chronic renal failure by intravenous or subcutaneous injection.[1] In June 2001, it had been approved by the European Medicines Agency for this indication as well as the treatment of anemia in cancer patients undergoing chemotherapy.[2] Dr. Reddy's Laboratories launched darbepoetin alfa in India under the brand name 'Cresp' in August 2010. This is the world's first generic darbepoetin alfa. Cresp has been approved in India. Darbepoetin is produced by recombinant DNA technology in modified Chinese hamster ovary cells.[citation needed] It differs from endogenous erythropoietin (EPO) by containing two more N-linked oligosaccharide chains. It is an erythropoiesis-stimulating 165-amino acid protein. Like EPO, its use increases the risk of cardiovascular problems, including cardiac arrest, arrhythmia, hypertension and hypertensive encephalopathy, congestive heart failure, vascular thrombosis or ischemia, myocardial infarction, edema, and stroke. It can also increase risk of seizures. A recent study has extended these findings to treatment of patients exhibiting cancer-related anemia (distinct from anemia resulting from chemotherapy).[3] Pre-existing untreated hypertension is a contra-indication for darbepoetin, as well as some hematologic diseases. Other reported adverse reactions include hypotension, fever, chest pains, nausea and myalgia. Like EPO, it has the potential to be abused by athletes seeking a competitive advantage. Its use during the 2002 Winter Olympic Games to improve performance led to the disqualification of cross-country skiers Larisa Lazutina and Olga Danilova of Russia and Johann Mühlegg of Spain from their final races. Nevertheless, recent publication in professional literature indicate that the detection of prohibited substances at the 2002 Olympics may have been false as a result of less-than-perfect detection methodology, and the Olympic champions could therefore wrongly suffer IOC sanctions.[4]

Denosumab

Denosumab[1] is a fully human monoclonal antibody for the treatment of osteoporosis, treatment-induced bone loss, bone metastases, rheumatoid arthritis, multiple myeloma, and giant cell tumor of bone.[2][3] It was developed by the biotechnology company Amgen.[4] Denosumab is designed to inhibit RANKL (RANK ligand), a protein that acts as the primary signal for bone removal. In many bone loss conditions, RANKL overwhelms the body's natural defenses against bone destruction. In June 2010, denosumab was approved by the U.S. Food and Drug Administration (FDA) for use in postmenopausal women with risk of osteoporosis under the trade name Prolia,[5] and in November 2010, as Xgeva, for the prevention of skeleton-related events in patients with bone metastases from solid tumors.[6] Denosumab is the first RANKL inhibitor to be approved by the FDA.[7] In the summer of 2011 clinical trials were investigating denosumab in giant cell tumors, multiple myeloma with bone metastases, and hypercalcemia of malignancy, and further investigating its dosing and safety.[8]

Westhroid

Desiccated thyroid or thyroid extract, refers to porcine (or mixed beef and pork) thyroid glands, dried and powdered for therapeutic use. Pork (or mixed beef and pork) thyroid preparations were developed in the late 19th century, and are still used today to treat hypothyroidism, the condition of having an underactive thyroid gland. This product is sometimes referred to as "natural thyroid", "natural thyroid hormones", "pork thyroid", thyroid USP, thyroid BP, or by the name of a commercial brand, such as "Armour Thyroid" or "Nature-Throid" & "Westhroid". Desiccated thyroid has been described in the United States Pharmacopoeia for nearly a century as the cleaned, dried, and powdered thyroid gland previously deprived of connective tissue and fat... obtained from domesticated animals that are used for food by man (USP XVI). In the last few decades, pork alone is the usual source. Historically, before modern assays, the potency was specified only by iodine content ("not less than 0.17% and not more than 0.23%"), rather than hormonal content or activity. Brands include Forest Lab's Armour, and Naturethroid & Westhroid by RLC Labs. Also available is a new generic NP thyroid by Acella Pharmaceuticals. Canada's desiccated thyroid is made by Erfa and is called Thyroid. All consist of desiccated porcine thyroid powder, differing only in the binders and fillers. Nature-Throid and Westhroid are available in the following strengths: 1/4(16.25 mg), 1/2(32.5 mg), 3/4(48.75 mg), 1(65 mg), 1.25(81.25 mg), 1.5(97.5 mg), 1.75(113.75), 2(130 mg), 2.25(146.25 mg), 2.5(162.5 mg), 3(195 mg), 4(260 mg), & 5(325 mg) grain. Each one grain (65 mg) contains 9 mcg of T3, and 38 mcg of T4. All brands contain a mixture of thyroid hormones: T4 (thyroxine), T3 (triiodothyronine) in the proportions usually present in pig thyroids (approximately 80% T4 and 20% T3). Armour is made in the following strengths: 1/4, 1/2, 1, 2, and 3 grain as well as 4 and 5 grain tablets. One grain (about 60 mg) of desiccated thyroid contains about 38 mcg of T4 and 9 mcg of T3.[1] Because the preparation is whole thyroid gland, each 60 mg tablet also contains over 59 mg of all of the other constituents of pork thyroid glands.

Desogestrel

Desogestrel is a molecule used in hormonal contraceptives. Most combined oral contraceptive pills (COCPs, or simply OCs) on the market today contain both an estrogen compound (ethinyl estradiol is common) plus a progestin (a progesterone-like compound) such as desogestrel. Desogestrel-containing birth control pills are sometimes referred to as "third generation" oral contraceptives. In contrast, birth control pills that are considered "second generation" (Tri-Levlen, for example) contain an estrogen and a progestin, but the progestin is different, such as levonorgestrel.

Digoxin

Digoxin INN (/dɨˈdʒɒksɨn/[1]) is a purified cardiac glycoside extracted from the foxglove plant, Digitalis lanata.[2] Its corresponding aglycone is digoxigenin, and its acetyl derivative is acetyldigoxin. Digoxin is widely used in the treatment of various heart conditions, namely atrial fibrillation, atrial flutter and sometimes heart failure that cannot be controlled by other medication. Digoxin preparations are commonly marketed under the trade names Lanoxin, Digitek, and Lanoxicaps. It is also available as a 0.05 mg/ml oral solution and 0.25 mg/ml or 0.5 mg/ml injectable solution. It is marketed by GlaxoSmithKline and many other pharmaceutic manufacturers.Today, the most common indications for digoxin are atrial fibrillation and atrial flutter with rapid ventricular response. Beta blockers and/or calcium channel blockers should be the first choice.[3][4] High ventricular rate leads to insufficient diastolic filling time. By slowing down the conduction in the AV node and increasing its refractory period, digoxin can reduce the ventricular rate. The arrhythmia itself is not affected, but the pumping function of the heart improves owing to improved filling. The use of digoxin in heart problems during sinus rhythm was once standard, but is now controversial. In theory, the increased force of contraction should lead to improved pumping function of the heart, but its effect on prognosis is disputable, and other effective treatments are now available. Digoxin is no longer the first choice for congestive heart failure, but can still be useful in patients who remain symptomatic despite proper diuretic and ACE inhibitor treatment. Digitalis/digoxin has recently fallen out of favor because it did not demonstrate a mortality benefit in patients with congestive heart failure; however, it did demonstrate a reduction in hospitalizations for this condition.[5] Because other therapies have shown a mortality benefit in congestive heart failure, maximizing other therapies (e.g., beta blockers) first is recommended before using digoxin.

Diltiazem

Diltiazem is a nondihydropyridine (non-DHP) member of the class of drugs known as calcium channel blockers, used in the treatment of hypertension, angina pectoris, and some types of arrhythmia. It is also an effective preventive medication for migraine. It is a class 3 antianginal drug, and a class IV antiarrhythmic. It is a common adulterant of cocaine seized in the UK,[1] and has been found to reduce cocaine cravings in rats, indicating it may prolong the "high" (see below). It incites minimal reflex sympathetic changes. It is based upon a 1,4-thiazepine ring. Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

Drosperinone

Drospirenone (INN, USAN), also known as 1,2-dihydrospirorenone, is a synthetic hormone used in birth control pills.[1] It is sold under the brand names Yasmin, Yasminelle, Yaz, Beyaz, Ocella, Zarah, and Angeliq, all of which are combination products of drospirenone with an estrogen such as ethinylestradiol.

enalapril

Enalapril (marketed as Vasotec in the USA, Enaladex in some other countries, and Enacard for veterinary use[1]) is an angiotensin converting enzyme (ACE) inhibitor used in the treatment of hypertension and some types of chronic heart failure. ACE converts the peptide hormone angiotensin I to angiotensin II. One of the actions of angiotensin II is the vasoconstriction of blood vessels resulting in an increase in blood pressure. ACE inhibitors such as enalapril prevent this effect. Enalapril has been shown to lower the death rate in systolic heart failure.[2] Enalapril was the first member of the group known as the dicarboxylate-containing ACE inhibitors.

Estrogens

Estrogens (AmE), Oestrogens (BE), are a group of compounds named for their importance in both menstrual and estrous reproductive cycles. They are the primary female sex hormones. Natural estrogens are steroid hormones, while some synthetic ones are non-steroidal. The name comes from the Greek οἶστρος (oistros), literally meaning "gadfly" but figuratively sexual passion or desire,[1] and the suffix -gen, meaning "producer of". Estrogens are synthesized in all vertebrates[2] as well as some insects.[3] Their presence in both vertebrates and insects suggests that estrogenic sex hormones have an ancient evolutionary history. Estrogens are used as part of some oral contraceptives, in estrogen replacement therapy for postmenopausal women, and in hormone replacement therapy for trans women. Like all steroid hormones, estrogens readily diffuse across the cell membrane. Once inside the cell, they bind to and activate estrogen receptors which in turn modulate the expression of many genes.[4] Additionally, estrogens have been shown to activate a G protein-coupled receptor, GPR30.[5]

Ethinyl estradiol

Ethinyl estradiol (EE) (pron.: /ˌɛθɨnɨlˌiːstrəˈdaɪ.əl/), also sometimes written as ethinylestradiol, ethynyl estradiol, or ethinyl oestradiol, is a derivative of 17β-estradiol (E2), the major endogenous estrogen in humans. EE is an orally bioactive estrogen used in many formulations of combined oral contraceptive pills. It is one of the most commonly used medications for this purpose. Transdermal ethinyl estradiol carries a greater risk of clot formation and venous thromboembolism than 17 beta estradiol, which some have theorized to be related to different amounts of hepatic metabolism after absorption. The same contraindications and precautions apply for EE as with other estrogen medications. Estinyl was a preparation of EE alone that was used for the management of menopausal symptoms and female hypogonadism.[1] EE is released into the environment as a xenoestrogen from the urine and feces of people who take it as a medication. The major concern with unopposed estrogen is of endometrial cancer. As such, the medication is generally prescribed with progesterone in the setting of birth control.

Ethynodiol diacetate

Ethynodiol diacetate (INN; sold as Continuin, Femulen, Luteonorm, Luto-Metrodiol, and Metrodiol), or ethynodiol diacetate (USAN, BAN), is a steroidal progestin which is used as a hormonal contraceptive.[1][2] Relative to other 19-nortestosterone derivatives, it has relatively little or no potency as an androgen,[3][4] and also unlike most progestins in general, has significant estrogenic effects.[5][3] [edit]

Ezetimibe

Ezetimibe (pron.: /ɛˈzɛtɨmɪb/) is a drug that lowers plasma cholesterol levels. It acts by decreasing cholesterol absorption in the intestine. It may be used alone (marketed as Zetia or Ezetrol), when other cholesterol-lowering medications are not tolerated, or together with statins (e.g., ezetimibe/simvastatin, marketed as Vytorin and Inegy) when statins alone do not control cholesterol. Ezetimibe decreases cholesterol levels, but has not been shown to improve outcomes in cardiovascular disease patients by decreasing atherosclerotic or vascular events compared to placebo. Ezetimibe is endorsed in the Canadian Lipid Guidelines and is considered a well-tolerated option for an add-on agent to statin, to help patients achieve their LDL (or bad cholesterol) targets. [1] Ezetimibe is the only add-on to statin therapy that has successfully shown cardiovascular benefit when combined with statin, but has not been proven to have an incremental benefit compared to statins alone. [2] Britain's NICE statement, published in 2007, endorses its use for monotherapy if statins are not tolerated or as add-on therapy.[3]

Folic acid and B12

Folic acid (also known as folate, vitamin M, vitamin B9,[3] vitamin Bc[4] (or folacin), pteroyl-L-glutamic acid, pteroyl-L-glutamate, and pteroylmonoglutamic acid[5]) are forms of the water-soluble vitamin B9. Folate is composed of the aromatic pteridine ring linked to para-aminobenzoic acid and one or more glutamate residues. Folic acid is itself not biologically active, but its biological importance is due to tetrahydrofolate and other derivatives after its conversion to dihydrofolic acid in the liver.[6] Vitamin B9 (folic acid and folate) is essential for numerous bodily functions. Humans cannot synthesize folate de novo; therefore, folate has to be supplied through the diet to meet their daily requirments. The human body needs folate to synthesize DNA, repair DNA, and methylate DNA as well as to act as a cofactor in certain biological reactions.[7] It is especially important in aiding rapid cell division and growth, such as in infancy and pregnancy. Children and adults both require folic acid to produce healthy red blood cells and prevent anemia.[8] Folate and folic acid derive their names from the Latin word folium (which means "leaf"). Leafy vegetables are principal sources of folic acid, although in Western diets fortified cereals and bread may be a larger dietary source.[citation needed] A lack of dietary folates leads to folate deficiency, which is uncommon in normal Western diets.[citation needed] A complete lack of dietary folate takes months before deficiency develops as normal individuals have about 500-20,000 µg[9] of folate in body stores.[10] This deficiency can result in many health problems, the most notable one being neural tube defects in developing embryos. Common symptoms of folate deficiency include diarrhea, macrocytic anemia with weakness or shortness of breath, nerve damage with weakness and limb numbness (peripheral neuropathy),[11] pregnancy complications, mental confusion, forgetfulness or other cognitive declines, mental depression, sore or swollen tongue, peptic or mouth ulcers, headaches, heart palpitations, irritability, and behavioral disorders. Low levels of folate can also lead to homocysteine accumulation.[7] DNA synthesis and repair are impaired and this could lead to cancer development.[7]

Furosemide

Furosemide (INN/BAN[1]) or frusemide (former BAN) is a loop diuretic used in the treatment of congestive heart failure and edema. It is most commonly marketed by Sanofi-Aventis under the brand name Lasix, and also under the brand name Frumex.[2] It has also been used to prevent Thoroughbred and Standardbred race horses from bleeding through the nose during races. Along with some other diuretics, furosemide is also included on the World Anti-Doping Agency's banned drug list due to its alleged use as a masking agent for other drugs.Furosemide is primarily used for the treatment of hypertension and edema.[3] It is the first-line agent in most people with edema due to congestive heart failure.[3] It is also used for hepatic cirrhosis, renal impairment, nephrotic syndrome, in adjunct therapy for cerebral/pulmonary edema where rapid diuresis is required (IV injection), and in the management of severe hypercalcemia in combination with adequate rehydration.[4]

Gemfibrazole

Gemfibrozil is the generic name for an oral drug used to lower lipid levels. It belongs to a group of drugs known as fibrates. It is most commonly sold as the brand name, Lopid. Other brand names include Jezil and Gen-Fibro.[citation neededIs an activator of Peroxisome proliferator-activated receptor-alpha (PPARα), a nuclear receptor that is involved in metabolism of carbohydrates and fats, as well as adipose tissue differentiation. This increase in the synthesis of lipoprotein lipase thereby increases the clearance of triglycerides.[citation needed] [edit]

Glyburide

Glibenclamide (INN), also known as glyburide (USAN), is an antidiabetic drug in a class of medications known as sulfonylureas, closely related to sulfa drugs. It was developed in 1966 in a cooperative study between Boehringer Mannheim (now part of Roche) and Hoechst (now part of Sanofi-Aventis).[1] It is sold in doses of 1.25 mg, 2.5 mg and 5 mg, under the trade names Diabeta, Glynase and Micronase in the United States and Daonil, Semi-Daonil and Euglucon in the United Kingdom and Delmide in India. It is also sold in combination with metformin under the trade names Glucovance, Benimet and Glibomet.

glypizide

Glipizide is an oral rapid- and short-acting anti-diabetic drug from the sulfonylurea class. It is classified as a second generation sulfonylurea, which means that it undergoes enterohepatic circulation. Second-generation sulfonylureas are both more potent and have shorter half-lives than the first-generation sulfonylureas. Glucotrol XL 5 MG Extended Release 24 hour tablet Mechanism of action is produced by blocking potassium channels in the beta cells of the islets of Langerhans. By partially blocking the potassium channels, the cell remains depolarized, increasing the time the cell spends in the calcium release stage of cell, which results in signaling leading to calcium influx. The increase in calcium will initiate more insulin release from each beta cell. Sulfonylureas may also cause the decrease of serum glucagon and potentiate the action of insulin at the extrapancreatic tissues. Originally available in 1984, it is marketed by Pfizer under the brand name Glucotrol in the USA, where Pfizer sells Glucotrol in doses of 5 and 10 milligrams and Glucotrol XL (an extended release form of glipizide) in doses of 2.5, 5, and 10 milligrams. Other companies also market glipizide, most commonly extended release tablets of 5 and 10 milligrams.

Hydrochlorothiazide

Hydrochlorothiazide, abbreviated HCTZ, HCT, or HZT, is a diuretic drug of the thiazide class that acts by inhibiting the kidneys' ability to retain water. This reduces the volume of the blood, decreasing blood return to the heart and thus cardiac output and, by other mechanisms, is believed to lower peripheral vascular resistance.[2] Hydrochlorothiazide is a calcium-sparing diuretic, meaning it can help the body get rid of excess water while still keeping calcium. Hydrochlorothiazide is frequently used for the treatment of hypertension, congestive heart failure, symptomatic edema, diabetes insipidus, renal tubular acidosis, and the prevention of kidney stones.[3] It is also sometimes used for hypercalciuria, Dent's disease and Ménière's disease. For diabetes insipidus, the effect of thiazide diuretics is presumably mediated by a hypovolemia-induced increase in proximal sodium and water reabsorption, thereby diminishing water delivery to the ADH-sensitive sites in the collecting tubules and reducing the urine output. Thiazides are also used in the treatment of osteoporosis. Thiazides decrease mineral bone loss by promoting calcium retention in the kidney, and by directly stimulating osteoblast differentiation and bone mineral formation.[4] It is frequently given together with losartan (an angiotensin II receptor antagonist) as hydrochlorothiazide/losartan.

Glargine

Insulin glargine, marketed by Sanofi-Aventis under the name Lantus, is a long-acting basal insulin analogue, given once daily to help control the blood sugar level of those with diabetes. It consists of microcrystals that slowly release insulin, giving a long duration of action of 18 to 26 hours, with a "peakless" profile (according to the Lantus package insert). Pharmacokinetically, it resembles basal insulin secretion of non-diabetic pancreatic beta cells. Sometimes, in type 2 diabetes and in combination with a short acting sulfonylurea (drugs which stimulate the pancreas to make more insulin), it can offer moderate control of serum glucose levels. In the absence of endogenous insulin—type 1 diabetes, depleted type 2 (in some cases) or latent autoimmune diabetes of adults in late stage—Lantus needs the support of fast acting insulin taken with food to reduce the effect of prandially derived glucose.

Iodine

Iodine is a chemical element with symbol I and atomic number 53. The name is from Greek ἰοειδής ioeidēs, meaning violet or purple, due to the color of elemental iodine vapor.[2] Iodine and its compounds are primarily used in nutrition, and industrially in the production of acetic acid and certain polymers. Iodine's relatively high atomic number, low toxicity, and ease of attachment to organic compounds have made it a part of many X-ray contrast materials in modern medicine. Iodine has only one stable isotope. A number of iodine radioisotopes are also used in medical applications. Iodine is found on Earth mainly as the highly water-soluble iodide ion, I−, which concentrates it in oceans and brine pools. Like the other halogens, free iodine occurs mainly as a diatomic molecule I2, and then only momentarily after being oxidized from iodide by an oxidant like free oxygen. In the universe and on Earth, iodine's high atomic number makes it a relatively rare element. However, its presence in ocean water has given it a role in biology. It is the heaviest essential element utilized widely by life in biological functions (only tungsten, employed in enzymes by a few species of bacteria, is heavier). Iodine's rarity in many soils, due to initial low abundance as a crust-element, and also leaching of soluble iodide by rainwater, has led to many deficiency problems in land animals and inland human populations. Iodine deficiency affects about two billion people and is the leading preventable cause of intellectual disabilities.[3] Iodine is required by higher animals, which use it to synthesize thyroid hormones, which contain the element. Because of this function, radioisotopes of iodine are concentrated in the thyroid gland along with nonradioactive iodine. If inhaled, the radioisotope iodine-131, which has a high fission product yield, concentrates in the thyroid, but is easily remedied with potassium iodide treatment.

Iron

Iron is pervasive, but particularly rich sources of dietary iron include red meat, lentils, beans, poultry, fish, leaf vegetables, watercress, tofu, chickpeas, black-eyed peas, blackstrap molasses, fortified bread, and fortified breakfast cereals. Iron in low amounts is found in molasses, teff and farina. Iron in meat (heme iron) is more easily absorbed than iron in vegetables.[65] Although some studies suggest that heme/hemoglobin from red meat has effects which may increase the likelihood of colorectal cancer,[66][67] there is still some controversy,[68] and even a few studies suggesting that there is not enough evidence to support such claims.[69] Iron provided by dietary supplements is often found as iron(II) fumarate, although iron sulfate is cheaper and is absorbed equally well. Elemental iron, or reduced iron, despite being absorbed at only one third to two thirds the efficiency (relative to iron sulfate),[70] is often added to foods such as breakfast cereals or enriched wheat flour. Iron is most available to the body when chelated to amino acids[71] and is also available for use as a common iron supplement. Often the amino acid chosen for this purpose is the cheapest and most common amino acid, glycine, leading to "iron glycinate" supplements.[72] The Recommended Dietary Allowance (RDA) for iron varies considerably based on age, gender, and source of dietary iron (heme-based iron has higher bioavailability).[73] Infants may require iron supplements if they are bottle-fed cow's milk.[74] Blood donors and pregnant women are at special risk of low iron levels and are often advised to supplement their iron intake.[75] Uptake and storage Iron acquisition poses a problem for aerobic organisms, because ferric iron is poorly soluble near neutral pH. Thus, bacteria have evolved high-affinity sequestering agents called siderophores.[76][77][78] After uptake, in cells, iron storage is carefully regulated; "free" iron ions do not exist as such. A major component of this regulation is the protein transferrin, which binds iron ions absorbed from the duodenum and carries it in the blood to cells.[79] In animals, plants, and fungi, iron is often the metal ion incorporated into the heme complex. Heme is an essential component of cytochrome proteins, which mediate redox reactions, and of oxygen carrier proteins such as hemoglobin, myoglobin, and leghemoglobin. Inorganic iron contributes to redox reactions in the iron-sulfur clusters of many enzymes, such as nitrogenase (involved in the synthesis of ammonia from nitrogen and hydrogen) and hydrogenase. Non-heme iron proteins include the enzymes methane monooxygenase (oxidizes methane to methanol), ribonucleotide reductase (reduces ribose to deoxyribose; DNA biosynthesis), hemerythrins (oxygen transport and fixation in marine invertebrates) and purple acid phosphatase (hydrolysis of phosphate esters). Iron distribution is heavily regulated in mammals, partly because iron ions have a high potential for biological toxicity.[80] Regulation of uptake Main article: Hepcidin Iron uptake is tightly regulated by the human body, which has no regulated physiological means of excreting iron. Only small amounts of iron are lost daily due to mucosal and skin epithelial cell sloughing, so control of iron levels is mostly by regulating uptake.[81] Regulation of iron uptake is impaired in some people as a result of a genetic defect that maps to the HLA-H gene region on chromosome 6. In these people, excessive iron intake can result in iron overload disorders, such as hemochromatosis. Many people have a genetic susceptibility to iron overload without realizing it or being aware of a family history of the problem. For this reason, it is advised that people do not take iron supplements unless they suffer from iron deficiency and have consulted a doctor. Hemochromatosis is estimated to cause disease in between 0.3 and 0.8% of Caucasians.[82] MRI finds that iron accumulates in the hippocampus of the brains of those with Alzheimer's disease and in the substantia nigra of those with Parkinson disease.[83]

Levonorgestrel

Levonorgestrel (or l-norgestrel or D-norgestrel) (Plan B, Next Choice, and others[1]) is a second generation synthetic progestogen used as an active ingredient in some hormonal contraceptives, including combined oral contraceptive pills, progestogen only pills, emergency contraceptive pills, intrauterine systems, contraceptive implants, and hormone replacement therapy.

Levothyroxine

Levothyroxine, also L-thyroxine or T4, is a synthetic form of the thyroid hormone thyroxine, which is normally secreted by the follicular cells of the thyroid gland. It is also used to treat thyroid hormone deficiency, and occasionally to prevent the recurrence of thyroid cancer. Like its naturally secreted counterpart, levothyroxine is chemically in the chiral L-form. The related drug dextrothyroxine (D-thyroxine) was used in the past as a treatment for hypercholesterolemia (elevated cholesterol levels) but was withdrawn due to cardiac side-effects.

Liotrix

Liotrix is 4:1 mixture of thyroxine (T4) and triiodothyronine (T3) made synthetically. It is used to replenish thyroid hormones in thyroid deficiency and hypothyroidism. The only brand of liotrix available in the U.S. is Thyrolar, manufactured by Forest Laboratories.[1] Thyrolar has not been available since 2009 with no explanation from Forest Labs.

Lorcaserin

Lorcaserin (APD-356, trade name upon approval Belviq,[1][2] expected trade name during development, Lorqess[3][4]) is a weight-loss drug developed by Arena Pharmaceuticals. It has serotonergic properties and acts as an anorectic. On 22 December 2009 a New Drug Application (NDA) was submitted to the Food and Drug Administration (FDA) in the United States.[5] On 16 September 2010, an FDA advisory panel voted to recommend against approval of the drug based on concerns over both safety and efficacy.[6] In October 2010, the FDA stated that it could not approve the application for lorcaserin in its present form.[7] On 10 May 2012, after a new round of studies submitted by Arena, an FDA panel voted to recommend lorcaserin with certain restrictions and patient monitoring. The restrictions include patients with a BMI of over 30, or with a BMI over 27 and a comorbidity like high blood pressure or type 2 diabetes.[8] On 27 June 2012, the FDA officially approved lorcaserin for use in the treatment of obesity for adults with a BMI equal to or greater than 30 or adults with a BMI of 27 or greater who "have at least one weight-related health condition, such as high blood pressure, type 2 diabetes, or high cholesterol".[1][9] Due to its hallucinogenic properties, the US Drug Enforcement Administration has proposed classifying lorcaserin as a Schedule IV drug under the Controlled Substances Act.[10]

Losartan

Losartan (rINN) (pron.: /loʊˈsɑrtən/) is an angiotensin II receptor antagonist drug used mainly to treat high blood pressure (hypertension). Losartan was the first angiotensin II receptor antagonist to be marketed. Losartan potassium is marketed by Merck & Co. Inc. under the trade name Cozaar. As of 2009, In south east Asia Losartan potassium is marketed by Delta Pharma Ltd. under the trade name Anin. losartan is available in generic form. As with all angiotensin II type 1 receptor (AT1) antagonists, losartan is indicated for the treatment of hypertension. It may also delay progression of diabetic nephropathy, and is also indicated for the reduction of renal disease progression in patients with type 2 diabetes, hypertension and microalbuminuria (>30 mg/24 hours) or proteinuria (>900 mg/24 hours).[citation needed] Although clinical evidence shows calcium channel blockers and thiazide-type diuretics are preferred first-line treatments for most patients (from both efficacy and cost points of view), an angiotensin II receptor antagonist such as losartan is recommended as first-line treatment in patients under the age of 55 who cannot tolerate an ACE inhibitor.[1] The LIFE study demonstrated losartan was significantly superior to atenolol in the primary prevention of adverse cardiovascular events (myocardial infarction or stroke), with a significant reduction in cardiovascular morbidity and mortality for a comparable reduction in blood pressure. A study hints that losartan has a beneficial effect on mitochondria by reversing age related dysfunction in maintaining normal blood pressure and cellular energy usage.[2][3] The maximal effects on blood pressure usually occur within 3-6 weeks upon starting losartan.[4] Losartan is also available as hydrochlorothiazide/losartan, a combination drug with a low dose thiazide diuretic to achieve an additive antihypertensive effect.

Medroxyprogesterone acetate

Medroxyprogesterone acetate (INN, USAN, BAN), also known as 17α-hydroxy-6α-methylprogesterone acetate, and commonly abbreviated as MPA, is a steroidal progestin, a synthetic variant of the human hormone progesterone.[2][3] It is used as a contraceptive, in hormone replacement therapy and for the treatment of endometriosis as well as several other indications. MPA is a more potent derivative of its parent compound medroxyprogesterone (MP). While medroxyprogesterone is sometimes used as a synonym for medroxyprogesterone acetate,[3] what is normally being administered is MPA and not MP.[4]

Metformin

Metformin (BP, pronounced /mɛtˈfɔrmɨn/, met-fawr-min; originally sold as Glucophage) is an oral antidiabetic drug in the biguanide class. It is the first-line drug of choice for the treatment of type 2 diabetes, in particular, in overweight and obese people and those with normal kidney function.[1][2][3] Its use in gestational diabetes has been limited by safety concerns. It is also used in the treatment of polycystic ovary syndrome, and has been investigated for other diseases where insulin resistance may be an important factor. Metformin works by suppressing glucose production by the liver. Metformin is the only antidiabetic drug that has been conclusively shown to prevent the cardiovascular complications of diabetes. It helps reduce LDL cholesterol and triglyceride levels, and is not associated with weight gain. As of 2010, metformin is one of only two oral antidiabetics in the World Health Organization Model List of Essential Medicines (the other being glibenclamide).[4] When prescribed appropriately, metformin causes few adverse effects (the most common is gastrointestinal upset) and is associated with a low risk of hypoglycemia. Lactic acidosis (a buildup of lactate in the blood) can be a serious concern in overdose and when it is prescribed to people with contraindications, but otherwise, there is no significant risk. First synthesized and found to reduce blood sugar in the 1920s, metformin was forgotten for the next two decades as research shifted to insulin and other antidiabetic drugs. Interest in metformin was rekindled in the late 1940s after several reports that it could reduce blood sugar levels in people, and in 1957, French physician Jean Sterne published the first clinical trial of metformin as a treatment for diabetes. It was introduced to the United Kingdom in 1958, Canada in 1972, and the United States in 1995. Metformin is now believed to be the most widely prescribed antidiabetic drug in the world; in the United States alone, more than 48 million prescriptions were filled in 2010 for its generic formulations.[5][6]

Methimazole

Methimazole (also known as Tapazole or Thiamazole or MMI) is an antithyroid drug,[1] and part of the thioamide group. Like its counterpart propylthiouracil, a major side effect of treatment is agranulocytosis.

Montelukast

Montelukast (trade names Singulair, Montelo-10 and Monteflo in India) is a leukotriene receptor antagonist (LTRA) used for the maintenance treatment of asthma and to relieve symptoms of seasonal allergies.[1][2] It is usually administered orally. Montelukast is a CysLT1 antagonist; it blocks the action of leukotriene D4 (and secondary ligands LTC4 and LTE4) on the cysteinyl leukotriene receptor CysLT1 in the lungs and bronchial tubes by binding to it. This reduces the bronchoconstriction otherwise caused by the leukotriene and results in less inflammation. Because of its method of operation, it is not useful for the treatment of acute asthma attacks. Again because of its very specific focus of operation, it does not interact with other asthma medications such as theophylline. Another leukotriene receptor antagonist is zafirlukast (Accolate), taken twice daily. Zileuton (Zyflo), an asthma drug taken four times per day, blocks leukotriene synthesis by inhibiting 5-lipoxygenase, an enzyme of the eicosanoid synthesis pathway. The Mont in Montelukast stands for Montreal, the place where Merck developed the drug.[3]

NPH

NPH insulin (or neutral protamine Hagedorn) (also known as Humulin N, Novolin N, Novolin NPH, NPH Iletin II, and isophane insulin), is an intermediate-acting insulin given to help control the blood sugar level of those with diabetes. NPH was created in 1936 when Nordisk formulated "isophane" porcine insulin by adding neutral protamine to regular insulin. This is a suspension of crystalline zinc insulin combined with the positively charged polypeptide, protamine. When injected subcutaneously, it has an intermediate duration of action, meaning longer than that of regular insulin, and shorter than ultralente, glargine or detemir.

nedocromil

Nedocromil sodium is a medication used to prevent wheezing, shortness of breath, and other breathing problems caused by asthma. It is administered by an inhaler under the brand name Tilade (although its effects in this form are far less than those in albuterol or other well-known inhaler medications) and as an eye drop under the brand name Alocril. Liquid preparations are available in the UK under the name Rapitil for use for allergic eye reactions.[1] Nedocromil is classified as a cromone. Nedocromil acts as a mast cell stabilizer, inhibits the degranulation of mast cells, prevents release of histamine and tryptase, so preventing the synthesis of prostaglandins and leukotrienes. US Production of inhaled nedocromil ceased in April 2008.[2]

Niacin

Niacin (also known as vitamin B3, nicotinic acid and vitamin PP) is an organic compound with the formula C6H5NO2 and, depending on the definition used, one of the 40 to 80 essential human nutrients. Niacin is one of five vitamins (when lacking in human diet) associated with a pandemic deficiency disease: niacin deficiency (pellagra), vitamin C deficiency (scurvy), thiamin deficiency (beriberi), vitamin D deficiency (rickets), vitamin A deficiency (night blindness and other symptoms). Niacin has been used for over 50 years to increase levels of HDL in the blood and has been found to modestly decrease the risk of cardiovascular events in a number of controlled human trials.[3] This colorless, water-soluble solid is a derivative of pyridine, with a carboxyl group (COOH) at the 3-position. Other forms of vitamin B3 include the corresponding amide, nicotinamide ("niacinamide"), where the carboxyl group has been replaced by a carboxamide group (CONH2), as well as more complex amides and a variety of esters. Nicotinic acid and niacinamide are convertible to each other with steady world demand rising from 8500 tonnes per year in 1980s to 40,000 in recent years[4]. Niacin cannot be directly converted to nicotinamide, but both compounds could be converted to NAD and NADP in vivo. Nicotinic acid, nicotinamid and tryptophan (via quinoline acid) are co-factors for nicotinamide adenine dinucleotide (NAD) and nicotinamide adenine dinucleotide phosphate (NADP). NAD converts to NADP by phosphorylation using NAD-kinase enzyme. They are coenzyme of various (more than 100) hydrogenases being important in hydrogen transfer almost in every oxidation reduction reaction in the body [5]. NAD is important in catabolism of fat, carbohydrate, protein and alcohol as well as cell signaling and DNA repair and NADP mostly in anabolism reaction such as fatty acid and cholesterol synthesis [6]. High energy requirements (brain) or high turnover rate (gut, skin) organs are usually the most susceptible to their deficiency [7].Although the two are identical in their vitamin activity, nicotinamide does not have the same pharmacological effects (lipid modifying effects) as niacin. Nicotinamide does not reduce cholesterol or cause flushing.[8] Nicotinamide may be toxic to the liver at doses exceeding 3 g/day for adults.[9] Niacin is a precursor to NAD+/NADH and NADP+/NADPH, which play essential metabolic roles in living cells.[10] Niacin is involved in both DNA repair, and the production of steroid hormones in the adrenal gland.

Nifedipine

Nifedipine (brand names Adalat CC and Procardia, according to FDA Orange Book) is a dihydropyridine calcium channel blocker. Its main uses are as an antianginal (especially in Prinzmetal's angina) and antihypertensive, although a large number of other indications have recently been found for this agent, such as Raynaud's phenomenon, premature labor, and painful spasms of the esophagus such as in cancer and tetanus patients. It is also commonly used for the small subset of pulmonary hypertension patients whose symptoms respond to calcium channel blockers.

Nitroglycerine

Nitroglycerin (NG), also known as nitroglycerine, trinitroglycerin, trinitroglycerine, or nitro, is more correctly known as glyceryl trinitrate or more formally: 1,2,3-trinitroxypropane. It is a heavy, colorless, oily, explosive liquid most commonly produced by treating glycerol with white fuming nitric acid under conditions appropriate to the formation of the nitric acid ester. Chemically, the substance is an organic nitrate compound rather than a nitro compound, but the traditional name is often retained. Since the 1860s, nitroglycerin has been used as an active ingredient in the manufacture of explosives, mostly dynamite, and as such it is employed in the construction, demolition, and mining industries. Similarly, since the 1880s, it has been used by the military as an active ingredient, and a gelatinizer for nitrocellulose, in some solid propellants, such as Cordite and Ballistite. Nitroglycerin is also a major component in double-based smokeless gunpowders used by reloaders. Combined with nitrocellulose, there are hundreds of (powder) combinations used by rifle, pistol, and shotgun reloaders. Nitroglycerin is also used medically as a vasodilator to treat heart conditions, such as angina and chronic heart failure. Having been used for over 130 years, nitroglycerin is one of the oldest and most useful drugs for treating and preventing attacks of angina pectoris. Though it was previously known that these effects arise because nitroglycerin is converted to nitric oxide, a potent vasodilator, it was not until 2002 that the enzyme for this conversion was discovered to be mitochondrial aldehyde dehydrogenase.[2] Nitroglycerin comes in forms of tablets, sprays or patches.[3] It has been suggested for other uses also, such as an adjunct therapy in prostate cancer.[4]

Nitroglycerin

Nitroglycerin (NG), also known as nitroglycerine, trinitroglycerin, trinitroglycerine, or nitro, is more correctly known as glyceryl trinitrate or more formally: 1,2,3-trinitroxypropane. It is a heavy, colorless, oily, explosive liquid most commonly produced by treating glycerol with white fuming nitric acid under conditions appropriate to the formation of the nitric acid ester. Chemically, the substance is an organic nitrate compound rather than a nitro compound, but the traditional name is often retained. Since the 1860s, nitroglycerin has been used as an active ingredient in the manufacture of explosives, mostly dynamite, and as such it is employed in the construction, demolition, and mining industries. Similarly, since the 1880s, it has been used by the military as an active ingredient, and a gelatinizer for nitrocellulose, in some solid propellants, such as Cordite and Ballistite. Nitroglycerin is also a major component in double-based smokeless gunpowders used by reloaders. Combined with nitrocellulose, there are hundreds of (powder) combinations used by rifle, pistol, and shotgun reloaders. Nitroglycerin is also used medically as a vasodilator to treat heart conditions, such as angina and chronic heart failure. Having been used for over 130 years, nitroglycerin is one of the oldest and most useful drugs for treating and preventing attacks of angina pectoris. Though it was previously known that these effects arise because nitroglycerin is converted to nitric oxide, a potent vasodilator, it was not until 2002 that the enzyme for this conversion was discovered to be mitochondrial aldehyde dehydrogenase.[2] Nitroglycerin comes in forms of tablets, sprays or patches.[3] It has been suggested for other uses also, such as an adjunct therapy in prostate cancer.[4]Nitroglycerin was first used by William Murrell to treat anginal attacks in 1878, with the discovery published in 1878.[8][17] Nitroglycerin belongs to a group of drugs called nitrates, which includes many other nitrates like isosorbide dinitrate (Isordil) and isosorbide mononitrate (Imdur, Ismo, Monoket).[18] These agents all exert their effect by being converted to nitric oxide in the body by mitochondrial aldehyde dehydrogenase,[2] and nitric oxide is a potent natural vasodilator. In medicine, where it is generally called glyceryl trinitrate, nitroglycerin is used as a heart medication. It is used as a medicine for angina pectoris (ischemic heart disease) in tablets, ointment, solution for intravenous use, transdermal patches, or sprays administered sublingually. Patients who experience angina when doing certain physical activities can often prevent symptoms by taking nitroglycerin 5 to 10 minutes before the activity. Some forms of nitroglycerin last much longer in the body than others. These may come in the form of a pill taken one, two, or three times per day, or even as a patch. It has been shown that round-the-clock exposure to nitrates can cause the body to stop responding normally to this medicine. Experts recommend that the patches be removed at night, allowing the body a few hours to restore its responsiveness to nitrates. Shorter-acting preparations can be used several times a day with less risk of the body getting used to this drug.[19] Angina pectoris is due to an inadequate flow of blood and oxygen to the heart. It is believed that nitroglycerin corrects the imbalance between the flow of oxygen and blood to the heart.[20] The principal action of nitroglycerin is vasodilation—widening of the blood vessels. At low doses, nitroglycerin will dilate veins more than arteries, but at higher doses it also dilates arteries and is a potent antihypertensive agent. In cardiac treatment the lowering of pressure in the arteries reduces the pressure against which the heart must pump, thereby decreasing afterload.[18] Dilating the veins decreases cardiac preload and leads to the following therapeutic effects during episodes of angina pectoris: subsiding of chest pain, decrease of blood pressure, increase of heart rate, and orthostatic hypotension.

Norethindrone

Norethisterone (or norethindrone) (or 19-nor-17α-ethynyltestosterone) is a molecule used in some combined oral contraceptive pills, progestogen only pills and is also available as a stand-alone drug. It is a progestogen and can be used to treat premenstrual syndrome, painful periods, abnormal heavy bleeding, irregular periods, menopausal syndrome (in combination with oestrogen), or to postpone a period. It is also commonly used to help prevent uterine hemorrhage in complicated non-surgical or pre-surgical gynecologic cases. Norethindrone was the first orally highly active progestin to be synthesized. It was synthesized for the first time by chemists Luis Miramontes, Carl Djerassi, and George Rosenkranz at Syntex in Mexico City in 1951.[1] It was the progestin used in one of the first three oral contraceptives. Its related ester, norethisterone acetate, is used for the same indications.

Norgestimate

Norgestimate is a molecule used in hormonal contraceptives. Norgestimate is a form of progestin, which is a female hormone important for the regulation of ovulation and menstruation. Norgestimate is used with estradiol (a female sex hormone that is involved in the development and maintenance of the female reproductive system), to treat the symptoms of menopause. Norgestimate and ethinylestradiol are used as an oral contraceptive, indicated for the prevention of pregnancy in women. [edit]

Norgestrel

Norgestrel is a progestin used in hormonal contraceptives. Norgestrel is a mixture of two stereoisomers, dextro-norgestrel (CAS# 797-64-8) and levo-norgestrel (CAS# 797-63-7). Only levonorgestrel is biologically active. Therefore, while some medications may contain dextronorgestrel, they are often labeled in terms of their levonorgestrel content only, ignoring the inert isomer. It is used in the hormonal contraceptive Microgynon 30, among others. [edit]

Orilistat

Orlistat (also known as tetrahydrolipstatin) is a drug designed to treat obesity. It is marketed as a prescription under the trade name Xenical by Roche in most countries, and is sold over-the-counter as Alli[2] by GlaxoSmithKline in the United Kingdom and the United States.[3] Its primary function is preventing the absorption of fats from the human diet, thereby reducing caloric intake. It is intended for use in conjunction with a healthcare provider-supervised reduced-calorie diet. Orlistat is the saturated derivative of lipstatin, a potent natural inhibitor of pancreatic lipases isolated from the bacterium Streptomyces toxytricini.[4] However, due to its relative simplicity and stability, orlistat was chosen over lipstatin for development as an anti-obesity drug.[5] The effectiveness of orlistat in promoting weight loss is definite, though modest. Pooled data from clinical trials suggest that people given orlistat in addition to lifestyle modifications, such as diet and exercise, lose about 2-3 kilograms (4.4-6.6 lb) more than those not taking the drug over the course of a year.[6] Orlistat also modestly reduces blood pressure, and appears to prevent the onset of type 2 diabetes, whether due to weight loss itself or to other effects; in a large randomized controlled trial, orlistat was found to reduce the incidence of diabetes by nearly 40% in obese people.[7] Orlistat is notorious for its gastrointestinal side effects (sometimes referred to as treatment effects), which can include steatorrhea (oily, loose stools). These decrease with time, however, and are the most frequently reported adverse effects of the drug.[citation needed][8] In the United States, the European Union, and Australia, orlistat is available for sale without a prescription. Over-the-counter approval was controversial in the United States, with consumer advocacy group Public Citizen repeatedly opposing it on safety and efficacy grounds.[9] Generic formulations of orlistat are available in some countries.

Phenterimine

Phentermine, a contraction of "phenyl-tertiary-butylamine", is a psychostimulant drug of the phenethylamine class, with pharmacology similar to amphetamine. It is used medically as an appetite suppressant. It is approved as an appetite suppressant to help reduce weight in obese patients when used short-term and combined with exercise, diet, and behavioral modification. It is typically prescribed for individuals who are at increased medical risk because of their weight and works by helping to release certain chemicals in the brain that control appetite.

pioglitazone

Pioglitazone is a prescription drug of the class thiazolidinedione (TZD) with hypoglycemic (antihyperglycemic, antidiabetic) action to treat diabetes. It is used to improve glucose control in adults over the age of 18 with type 2 diabetes. Pioglitazone is marketed as trademarks Actos in the USA, Canada, the UK and Germany, Glustin in Europe, Glizone and Pioz in India by Zydus Cadila and USV Limited, respectively and Zactos in Mexico by Takeda Pharmaceuticals. Actos was the tenth-best selling drug in the U.S. in 2008, with sales exceeding $2.4 billion.[1] Its cardiovascular safety profile compares favorably with rosiglitazone (Avandia), which was withdrawn after concerns about an increased risk of cardiac events. However, pioglitazone has subsequently been found to be associated with bladder tumors and has been withdrawn in some countries.

Pramlintide

Pramlintide (Symlin) is a relatively new adjunct for diabetes (both type 1 and 2), developed by Amylin Pharmaceuticals (now a wholly owned subsidiary of Bristol Myers-Squibb). Pramlintide is delivered as an acetate salt.

Prazocin

Prazosin, trade names Minipress, Vasoflex, Pressin and Hypovase, is a sympatholytic drug used to treat high blood pressure and anxiety, PTSD, and panic disorder. It is an alpha-adrenergic blocker that is specific for the alpha-1 receptors. These receptors are found on vascular smooth muscle, where they are responsible for the vasoconstrictive action of norepinephrine. They are also found throughout the central nervous system.[1] In addition to its alpha-blocking activity, prazosin is an antagonist of the MT3 receptor (which is not present in humans), with selectivity for this receptor over the MT1 and MT2 receptors.[2]Prazosin is orally active and has a minimal effect on cardiac function due to its alpha-1 receptor selectivity. However, when prazosin is initially started, heart rate and contractility go up in order to maintain the pre-treatment blood pressures because the body has reached homeostasis at its abnormally high blood pressure. The blood pressure lowering effect becomes apparent when prazosin is taken for longer periods of time. The heart rate and contractility go back down over time and blood pressure decreases. The antihypertensive characteristics of prazosin make it a second-line choice for the treatment of high blood pressure.[3] Prazosin is also useful in treating urinary hesitancy associated with prostatic hyperplasia, blocking alpha-1 receptors, which control constriction of both the prostate and ureters. Although not a first line choice for either hypertension or prostatic hyperplasia, it is a choice for patients who present with both problems concomitantly.[3] This medication has shown to be effective in treating severe nightmares in children and people with PTSD symptoms.[4] Veterans have also been treated successfully at Seattle's VA Puget Sound Health Care System (VAPSHCS) for sleep disturbance related to PTSD. Doses are lower for this purpose than for control of blood pressure.[4] Prazosin holds promise as a pharmacologic treatment for alcohol dependence after a 2009 pilot trial l was completed. A larger controlled Phase II trial "Clinical Trial of the Adrenergic Alpha-1 Antagonist Prazosin for Alcohol Dependence" is currently underway, set to be completed November 2013.

Procainamide

Procainamide INN (pron.: /proʊˈkeɪnəmaɪd/; trade names Pronestyl, Procan, Procanbid) is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias, classified by the Vaughan Williams classification system as class Ia. It is a sodium channel blocker which blocks open sodium channels and prolongs the cardiac action potential (outward potassium (K+) currents may be blocked). This results in slowed conduction, and ultimately the decreased rate of rise of the action potential, which may result in widening of QRS on electrocardiogram.[3] [edit]

Procainamide

Procainamide INN (pron.: /proʊˈkeɪnəmaɪd/; trade names Pronestyl, Procan, Procanbid) is a pharmaceutical antiarrhythmic agent used for the medical treatment of cardiac arrhythmias, classified by the Vaughan Williams classification system as class IaIt is a sodium channel blocker which blocks open sodium channels and prolongs the cardiac action potential (outward potassium (K+) currents may be blocked). This results in slowed conduction, and ultimately the decreased rate of rise of the action potential, which may result in widening of QRS on electrocardiogram.[3] [edit]

progesterone

Progesterone also known as P4 (pregn-4-ene-3,20-dione) is a C-21 steroid hormone involved in the female menstrual cycle, pregnancy (supports gestation) and embryogenesis of humans and other species. Progesterone belongs to a class of hormones called progestogens, and is the major naturally occurring human progestogen.

Propranolol

Propranolol (INN) is a sympatholytic non-selective beta blocker. Sympatholytics are used to treat hypertension, anxiety and panic. It was the first successful beta blocker developed.[1] Propranolol is available in generic form as propranolol hydrochloride, Marketed in India under brand names like Ciplar and Ciplar LA Cipla ltd also other brands from AstraZeneca and Wyeth under the brand names Inderal, Inderal LA, Avlocardyl, Deralin, Dociton, Inderalici, InnoPran XL, Sumial, Anaprilinum, Bedranol SR (Sandoz).

Propylthiouracil

Propylthiouracil (PTU) or 6-n-propylthiouracil[1] (PROP) is a thiouracil-derived drug used to treat hyperthyroidism (including Graves' disease) by decreasing the amount of thyroid hormone produced by the thyroid gland.[2] Its notable side effects include a risk of agranulocytosis. On 3 June 2009, the FDA published an alert "notifying healthcare professionals of the risk of serious liver injury, including liver failure and death, with the use of propylthiouracil."[3] As a result, propylthiouracil is no longer recommended in non-pregnant adults and in children as the front line antithyroid medication.[4]

Quinidine

Quinidine is a pharmaceutical agent that acts as a class I antiarrhythmic agent (Ia) in the heart. It is a stereoisomer of quinine, originally derived from the bark of the cinchona tree. The drug causes increased action potential duration, as well as a prolonged QT interval.Like all other class I antiarrhythmic agents, quinidine primarily works by blocking the fast inward sodium current (INa). Quinidine's effect on INa is known as a 'use dependent block'. This means at higher heart rates, the block increases, while at lower heart rates, the block decreases. The effect of blocking the fast inward sodium current causes the phase 0 depolarization of the cardiac action potential to decrease (decreased Vmax). Quinidine also blocks the slowly inactivating, tetrodotoxin-sensitive Na current, the slow inward calcium current (ICa), the rapid (IKr) and slow (IKs) components of the delayed potassium rectifier current, the inward potassium rectifier current (IKI), the ATP-sensitive potassium channel (IKATP) and Ito. At micromolar concentrations, quinidine inhibits Na⁺/K⁺-ATPase by binding to the same receptor sites as the digitalis glycosides such as ouabain. The effect of quinidine on the ion channels is to prolong the cardiac action potential, thereby prolonging the QT interval on the surface ECG. Other ECG effects include a wide notched P wave, wide QRS complex, depressed ST segment, and U waves. These are the results of both slowed depolarization and repolarization.

Raloxifene

Raloxifene (marketed as Evista by Eli Lilly and Company) is an oral selective estrogen receptor modulator (SERM) that has estrogenic actions on bone and anti-estrogenic actions on the uterus and breast. It is used in the prevention of osteoporosis in postmenopausal women. In 2006, the National Cancer Institute announced that raloxifene was as effective as tamoxifen in reducing the incidence of breast cancer in postmenopausal women at increased risk. A major adverse effect of tamoxifen is uterine cancer; raloxifene had fewer uterine cancers. Tamoxifen increased the risk of cataracts, but raloxifene did not. Both groups had more blood clots in veins and the lungs, but that side effect was more common with tamoxifen than raloxifene.[2][3][4] On September 14, 2007, the U.S. Food and Drug Administration announced approval of raloxifene for reducing the risk of invasive breast cancer in postmenopausal women with osteoporosis and in postmenopausal women at high risk for invasive breast cancer.[5] An editorial in Lancet Oncology criticized the way that information about the drug was released.[6]

Albuterol

Salbutamol (INN) or albuterol (USAN) is a short-acting β2-adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma and chronic obstructive pulmonary disease. It is marketed as Ventolin among other brand names. Salbutamol was the first selective β2-receptor agonist to be marketed — in 1968. It was first sold by Allen & Hanburys under the brand name Ventolin. The drug was an instant success, and has been used for the treatment of asthma ever since.[2] Salbutamol sulfate is usually given by the inhaled route for direct effect on bronchial smooth muscle. This is usually achieved through a metered dose inhaler (MDI), nebulizer or other proprietary delivery devices (e.g. Rotahaler or Autohaler). In these forms of delivery, the maximal effect of salbutamol can take place within five to 20 minutes of dosing, though some relief is immediately seen. It can also be given intravenously.

Salmeterol

Salmeterol is a long-acting beta2-adrenergic receptor agonist drug that is prescribed for the treatment of asthma and chronic obstructive pulmonary disease(COPD). It is available as a dry powder inhaler that releases a powdered form of the drug. Before 2008, it was also available as a metered-dose inhaler (MDI).[1 It is a long-acting beta-adrenoceptor agonist (LABA), usually prescribed only for severe persistent asthma following previous treatment with a short-acting beta agonist such as salbutamol and is prescribed concurrently with a corticosteroid, such as beclomethasone. The primary noticeable difference of salmeterol to salbutamol is that the duration of action lasts approximately 12 hours in comparison with 4-6 hours of salbutamol. When used regularly every day as prescribed, inhaled salmeterol decreases the number and severity of asthma attacks. However, like all LABA medications, it is not for use for relieving an asthma attack that has already started. Inhaled salmeterol works like other beta 2-agonists, causing bronchodilation by relaxing the smooth muscle in the airway so as to treat the exacerbation of asthma. The long duration of action occurs by the molecules initially diffusing into the plasma membrane of the lung cells, and then slowly being released back outside the cell where they can come into contact with the beta-2 adrenoceptors, with the long carbon chain forming an anchor in the membrane. Interestingly, salmeterol binding to the beta-adrenoceptor does not induce desensitisation or internalisation of receptors which may also contribute to its long therapeutic duration of action. Formoterol has been demonstrated to have a faster onset of action than salmeterol as a result of a lower lipophilicity, and has also been demonstrated to be more potent—a 12 µg dose of formoterol has been demonstrated to be equivalent to a 50 µg dose of salmeterol. [edit]

Sildenafil

Sildenafil citrate, sold as Viagra, Revatio and under various other trade names, is a drug used to treat erectile dysfunction and pulmonary arterial hypertension (PAH). It was originally developed by British scientists and then brought to market by the US-based pharmaceutical company Pfizer.[1] It acts by inhibiting cGMP-specific phosphodiesterase type 5, an enzyme that promotes degradation of cGMP, which regulates blood flow in the penis. Since becoming available in 1998, sildenafil has been the prime treatment for erectile dysfunction; its primary competitors on the market are tadalafil (Cialis) and vardenafil (Levitra).

Spironolactone

Spironolactone (INN, BAN, USAN) (pronounced /ˌspaɪrɵnɵˈlæktoʊn/),[2] commonly referred to simply as "spiro",[3][4] and marketed primarily under the brand name Aldactone in most countries, is a synthetic, steroidal antimineralocorticoid agent with additional antiandrogen and weak progestogen properties, as well as some indirect estrogen and glucocorticoid effects, which is used primarily as a diuretic and antihypertensive, but also for the purpose of reducing elevated or unwanted androgen activity in the body.[5] It acts predominantly as a competitive antagonist of the aldosterone (or mineralocorticoid) receptor, and belongs to a class of pharmaceutical drugs known as potassium-sparing diuretics. Spironolactone is a relatively old drug, having been introduced clinically in 1959.[6][7] It has been predicted that spironolactone will be superseded in cardiovascular conditions (e.g., heart failure and hypertension) by the newer agents such as the structurally related compound eplerenone, which is also an aldosterone antagonist but is selective and lacks many of the actions and side effects of spironolactone, and as such is much more tolerable in comparison.[8] However, spironolactone is still far more widely used than eplerenone. Spironolactone nonetheless still finds frequent use as an antiandrogen.

Anything ending with -statin

Statins (or HMG-CoA reductase inhibitors) are a class of drugs used to lower cholesterol levels by inhibiting the enzyme HMG-CoA reductase, which plays a central role in the production of cholesterol in the liver. Increased cholesterol levels have been associated with cardiovascular diseases,[1] and statins are therefore used in the prevention of these diseases. Research has found that statins are most effective for treating cardiovascular disease (CVD) (secondary prevention), with questionable benefit in those without previous CVD, but with elevated cholesterol levels.[2][3] Statins have rare but severe adverse effects, particularly muscle damage, and some doctors believe they are overprescribed. The best-selling statin is atorvastatin, marketed as Lipitor (manufactured by Pfizer) and Torvast. By 2003, atorvastatin became the best-selling pharmaceutical in history,[4] with Pfizer reporting sales of US$12.4 billion in 2008.[5] As of 2010, a number of statins are on the market: atorvastatin (Lipitor and Torvast), fluvastatin (Lescol), lovastatin (Mevacor, Altocor, Altoprev), pitavastatin (Livalo, Pitava), pravastatin (Pravachol, Selektine, Lipostat), rosuvastatin (Crestor) and simvastatin (Zocor, Lipex).[6] Several combination preparations of a statin and another agent, such as ezetimibe/simvastatin, are also available.Statins act by competitively inhibiting HMG-CoA reductase, the first committed enzyme of the HMG-CoA reductase pathway. Because statins are similar to HMG-CoA on a molecular level, they take the place of HMG-CoA in the enzyme and reduce the rate by which it is able to produce mevalonate, the next molecule in the cascade that eventually produces cholesterol, as well as a number of other compounds. This ultimately reduces cholesterol via several mechanisms.

Tamoxifen

Tamoxifen is an antagonist of the estrogen receptor in breast tissue via its active metabolite, hydroxytamoxifen. In other tissues such as the endometrium, it behaves as an agonist, and thus may be characterized as a mixed agonist/antagonist. Tamoxifen is the usual endocrine (anti-estrogen) therapy for hormone receptor-positive breast cancer in pre-menopausal women, and is also a standard in post-menopausal women although aromatase inhibitors are also frequently used in that setting.[1] Some breast cancer cells require estrogen to grow. Estrogen binds to and activates the estrogen receptor in these cells. Tamoxifen is metabolized into compounds that also bind to the estrogen receptor but do not activate it. Because of this competitive antagonism, tamoxifen acts like a key broken off in the lock that prevents any other key from being inserted, preventing estrogen from binding to its receptor. Hence breast cancer cell growth is blocked. Tamoxifen was discovered by pharmaceutical company Imperial Chemical Industries[2] (now AstraZeneca) and is sold under the trade names Nolvadex, Istubal, and Valodex. However, the drug, even before its patent expiration, was and still is widely referred to by its generic name "tamoxifen."

Teriparetide

Teriparatide (Forteo, also available in generic form[1]) is a recombinant form of parathyroid hormone, used in the treatment of some forms of osteoporosis.[2] It is manufactured and marketed by Eli Lilly and Company.Teriparatide is a portion of human parathyroid hormone (PTH), amino acid sequence 1 through 34, of the complete molecule (containing 84 amino acids). Endogenous PTH is the primary regulator of calcium and phosphate metabolism in bone and kidney. PTH increases serum calcium, partially accomplishing this by increasing bone resorption. Thus, chronically elevated PTH will deplete bone stores. However, intermittent exposure to PTH will activate osteoblasts more than osteoclasts. Thus, once-daily injections of teriparatide have a net effect of stimulating new bone formation leading to increased bone mineral density.[4][5][6] Teriparatide is the first, and to date only, FDA approved agent for the treatment of osteoporosis that stimulates new bone formation.[7]

Theophylline

Theophylline, also known as dimethylxanthine, is a methylxanthine drug used in therapy for respiratory diseases such as COPD and asthma under a variety of brand names. As a member of the xanthine family, it bears structural and pharmacological similarity to caffeine.Like other methylated xanthine derivatives, theophylline is both a competitive nonselective phosphodiesterase inhibitor,[10] which raises intracellular cAMP, activates PKA, inhibits TNF-alpha [11][12] and inhibits leukotriene [13]synthesis, and reduces inflammation and innate immunity [13] nonselective adenosine receptor antagonist,[14] antagonizing A1, A2, and A3 receptors almost equally, which explains many of its cardiac effects Theophylline has been shown to inhibit TGF-beta-mediated conversion of pulmonary fibroblasts into myofibroblasts in COPD and asthma via cAMP-PKA pathway and suppresses COL1 mRNA, which codes for the protein collagen.[15] It has been shown that theophylline may reverse the clinical observations of steroid insensitivity in patients with COPD and asthmatics that are active smokers (a condition resulting in oxidative stress) via a distinctly separate mechanism. Theophylline in vitro can restore the reduced HDAC (histone deacetylase) activity that is induced by oxidative stress (i.e., in smokers), returning steroid responsiveness toward normal.[16] Furthermore, theophylline has been shown to directly activate HDAC2.[16] (Corticosteroids switch off the inflammatory response by blocking the expression of inflammatory mediators through deacetylation of histones, an effect mediated via histone deacetylase-2 (HDAC2). Once deacetylated, DNA is repackaged so that the promoter regions of inflammatory genes are unavailable for binding of transcription factors such as NF-κB that act to turn on inflammatory activity. It has recently been shown that the oxidative stress associated with cigarette smoke can inhibit the activity of HDAC2, thereby blocking the anti-inflammatory effects of corticosteroids.) Thus theophylline could prove to be a novel form of adjunct therapy in improving the clinical response to steroids in smoking asthmatics.[citation needed]The use of theophylline is complicated by its interaction with various drugs, chiefly cimetidine and phenytoin, and that it has a narrow therapeutic index, so, as in the case with many other asthma drugs, its use must be monitored to avoid toxicity. It can also cause nausea, diarrhea, increase in heart rate, arrhythmias, and CNS excitation (headaches, insomnia, irritability, dizziness and lightheadedness).[5][6] Seizures can also occur in severe cases of toxicity and is considered to be a neurological emergency.[7] Its toxicity is increased by erythromycin, cimetidine, and fluoroquinolones, such as ciprofloxacin. It can reach toxic levels when taken with fatty meals, an effect called dose dumping.[8] Theophylline toxicity can be treated with beta blockers. In addition to seizures, tachyarrhythmias are a major concern.[9] [edit]

Topirimate

Topiramate (brand name Topamax) is an anticonvulsant (antiepilepsy) drug. It was most recently approved for weight loss by the FDA in combination with phentermine. It has been used off label for this purpose before FDA approval was obtained. It was originally produced by Ortho-McNeil Neurologics and Noramco, Inc., both divisions of the Johnson & Johnson Corporation. It was also recently approved in a combination medication used for weight loss in late 2012. This medication was discovered in 1979 by Bruce E. Maryanoff and Joseph F. Gardocki during their research work at McNeil Pharmaceutical.[1][2][3] Topiramate was first approved by the US FDA in 1996.[4] Generic versions are available in Canada and these were approved by the Food and Drug Administration (FDA) in September 2006. Mylan Pharmaceuticals was recently granted final approval for generic topiramate 25, 100, and 200 mg tablets and sprinkle capsules by the FDA for sale in the United States. 50 mg tablets were granted tentative approval.[5] The last patent for topiramate in the U.S. was for pediatric use; this patent expired on February 28, 2009.[6]

Tranexamic acid

Tranexamic acid (commonly marketed in tablet form as Lysteda and in IV form as Cyklokapron in the U.S. and Australia and as Transamin,Transcam in Asia, and Espercil in South America. Also marketed as TRAXYL (Nuvista Pharma) in Bangladesh, Cyclo-F and Femstrual in UK.) is a synthetic derivative of the amino acid lysine. It is used to treat or prevent excessive blood loss during surgery and in various other medical conditions. It is an antifibrinolytic that competitively inhibits the activation of plasminogen to plasmin, by binding to specific sites of both plasminogen and plasmin, a molecule responsible for the degradation of fibrin. Fibrin is a protein that forms the framework of blood clots. It has roughly eight times the antifibrinolytic activity of an older analogue, ε-aminocaproic acid.

Triiodothyronine

Triiodothyronine, also known as T3, is a thyroid hormone. It affects almost every physiological process in the body, including growth and development, metabolism, body temperature, and heart rate.[1] Production of T3 and its prohormone thyroxine (T4) is activated by thyroid-stimulating hormone (TSH), which is released from the pituitary gland. This pathway is regulated via a closed-loop feedback process: Elevated concentrations of T3, and T4 in the blood plasma inhibit the production of TSH in the pituitary gland. As concentrations of these hormones decrease, the pituitary gland increases production of TSH, and by these processes, a feedback control system is set up to regulate the amount of thyroid hormones that are in the bloodstream. As the true hormone, the effects of T3 on target tissues are roughly four times more potent than those of T4.[2] Of the thyroid hormone that is produced, just about 20% is T3, whereas 80% is produced as T4. Roughly 85% of the circulating T3 is later formed in the thyroid by removal of the iodine atom from the carbon atom number five of the outer ring of T4. In any case, the concentration of T3 in the human blood plasma is about one-fortieth that of T4. This is observed in fact because of the short half-life of T3, which is only 2.5 days.[3] This compares with the half-life of T4, which is about 6.5 days.

Ulipristal

Ulipristal acetate (trade name EllaOne in the European Union, Ella in the U.S.,[1] HRA Pharma) is a selective progesterone receptor modulator (SPRM) for emergency contraception[2] within 120 hours (5 days) after an unprotected intercourse or contraceptive failure. It has shown to prevent about 60% of expected pregnancies,[3] which is comparable to the emergency contraception scheme with levonorgestrel. Ulipristal acetate is available by prescription only in the U.S. and Europe, but without a prescription in India.[4]

Verapamil

Verapamil (brand names: Isoptin, Verelan, Verelan PM, Calan, Bosoptin, Covera-HS) is an L-type calcium channel blocker of the phenylalkylamine class. It has been used in the treatment of hypertension, angina pectoris, cardiac arrhythmia, and most recently, cluster headaches.[1] It is also an effective preventive medication for migraine. Verapamil has also been used as a vasodilator during cryopreservation of blood vessels. It is a class IV antiarrhythmic, more effective than digoxin in controlling ventricular rate[2] and was approved by the U.S. Food and Drug Administration (FDA) in March 1982.[3]Verapamil's mechanism in all cases is to block voltage-dependent calcium channels. In cardiac pharmacology, calcium channel blockers are considered class IV antiarrhythmic agents. Since calcium channels are especially concentrated in the sinoatrial and atrio-ventricular nodes, these agents can be used to decrease impulse conduction through the AV node, thus protecting the ventricles from atrial tachyarrhythmias. Calcium channels are also present in the smooth muscle that lines blood vessels. By relaxing the tone of this smooth muscle, calcium-channel blockers dilate the blood vessels. This has led to their use in treating hypertension and angina pectoris. The pain of angina is caused by a deficit in oxygen supply to the heart. Calcium channel blockers like Verapamil will dilate blood vessels, which increases the supply of blood and oxygen to the heart. This controls chest pain, but only when used regularly. It does not stop chest pain once it starts. A more powerful vasodilator such as glyceryl trinitrate may be needed to control pain once it starts. Verapamil is also used intra-arterially to treat cerebral vasospasm.[4] Verapamil has been used to treat cluster headaches,[5] but it can also cause headaches as a side effect.

Calcium/Vit D

Vitamin D is a group of fat-soluble secosteroids responsible for intestinal absorption of calcium and phosphate. In humans, the most important related compounds of vitamin D are vitamin D2 and vitamin D3.[1] Cholecalciferol (vitamin D3) and ergocalciferol (vitamin D2) are unique as they constitute what we know as vitamin D and can be ingested from the diet and/or supplements.[1][2][3] The body can also synthesize vitamin D (from cholesterol) when sun exposure is adequate (hence its nickname, the "sunshine vitamin"). Although vitamin D is commonly called a vitamin, it is not actually an essential dietary vitamin in the strict sense, as it can be synthesized in adequate amounts by most mammals exposed to sunlight (cats and dogs cannot synthesize vitamin D efficiently and must receive it in their diet). An organic chemical compound (or related set of compounds) is only scientifically called a vitamin when it cannot be synthesized in sufficient quantities by an organism, and must be obtained from their diet. However, as with other compounds commonly called vitamins, vitamin D was discovered in an effort to find the dietary substance that was lacking in a disease, namely, rickets, the childhood form of osteomalacia.[4] Additionally, like other compounds called vitamins, in the developed world vitamin D is added to staple foods, such as milk, to avoid disease due to deficiency. Measures of serum levels reflect endogenous synthesis from exposure to sunlight as well as intake from the diet, and it is believed that synthesis may contribute generally to the maintenance of adequate serum concentrations. The evidence indicates that the synthesis of vitamin D from sun exposure works in a feedback loop that prevents toxicity but, because of uncertainty about the cancer risk from sunlight, no recommendations are issued by the Institute of Medicine, USA, for the amount of sun exposure required to meet vitamin D requirements. Accordingly, the Dietary Reference Intakes for vitamin D assume that no synthesis occurs and that all of a person's vitamin D is from their diet, although that will rarely occur in practice. In the liver vitamin D is converted to calcidiol, which is also known as calcifediol (INN), 25-hydroxycholecalciferol, or 25-hydroxyvitamin D—abbreviated 25(OH)D; and which is the specific vitamin D metabolite that is measured in serum to determine a person's vitamin D status.[5][6] Part of the calcidiol is converted by the kidneys to calcitriol, the biologically active form of vitamin D.[7] Calcitriol circulates as a hormone in the blood, regulating the concentration of calcium and phosphate in the bloodstream and promoting the healthy growth and remodeling of bone. Calcidiol is also converted to calcitriol outside of the kidneys for other purposes, such as the proliferation, differentiation and apoptosis of cells; calcitriol also affects neuromuscular function and inflammation.[8] Beyond its use to prevent osteomalacia or rickets, the evidence for other health effects of vitamin D supplementation in the general population is inconsistent.[9][10] The best evidence of benefit is for bone health[11] and a decrease in mortality in elderly women.[12]

Vitamin K

Vitamin K is a group of structurally similar, fat-soluble vitamins that the human body needs for posttranslational modification of certain proteins required for blood coagulation, and in metabolic pathways in bone and other tissue. They are 2-methyl-1,4-naphthoquinone (3-) derivatives. This group of vitamins includes two natural vitamers: vitamin K1 and vitamin K2.[1] Vitamin K1, also known as phylloquinone, phytomenadione, or phytonadione, is synthesized by plants, and is found in highest amounts in green leafy vegetables because it is directly involved in photosynthesis. It may be thought of as the "plant form" of vitamin K. It is active in animals and may perform the classic functions of vitamin K in animals, including its activity in the production of blood clotting proteins. Animals may also convert it to vitamin K2. Vitamin K2, the main storage form in animals, has several subtypes, which differ in isoprenoid chain length. These vitamin K2 homologs are called menaquinones, and are characterized by the number of isoprenoid residues in their side chains. Menaquinones are abbreviated MK-n, where M stands for menaquinone, the K stands for vitamin K, and the n represents the number of isoprenoid side chain residues. For example, menaquinone-4 (abbreviated MK-4) has four isoprene residues in its side chain. Menaquinone-4 (also known as menatetrenone from its four isoprene residues) is the most common type of vitamin K2 in animal products since it is normally synthesized from vitamin K1 in certain animal tissues (arterial walls, pancreas, and testes) by replacement of the phytyl tail with an unsaturated geranylgeranyl tail containing four isoprene units, thus yielding menaquinone-4. This homolog of vitamin K2 may have enzyme functions that are distinct from those of vitamin K1. Bacteria in the colon (large intestine) can also convert K1 into vitamin K2. In addition, bacteria typically lengthen the isopreneoid side chain of vitamin K2 to produce a range of vitamin K2 forms, most notably the MK-7 to MK-11 homologs of vitamin K2. All forms of K2 other than MK-4 can only be produced by bacteria, which use these forms in anaerobic respiration. The MK-7 and other bacteria-derived form of vitamin K2 exhibit vitamin K activity in animals, but MK-7's extra utility over menaquinone-4 (MK-4), if any, is unclear and is presently a matter of investigation. Three synthetic types of vitamin K are known: vitamins K3, K4, and K5. Although the natural K1 and all K2 homologs have proven nontoxic, the synthetic form K3 (menadione) has shown toxicity.[2]

Warfarin

Warfarin (also known under the brand names Coumadin, Jantoven, Marevan, Lawarin, Waran, and Warfant) is an anticoagulant normally used in the prevention of thrombosis and thromboembolism, the formation of blood clots in the blood vessels and their migration elsewhere in the body respectively. It was initially introduced in 1948 as a pesticide against rats and mice and is still used for this purpose, although more potent poisons such as brodifacoum have since been developed. In the early 1950s warfarin was found to be effective and relatively safe for preventing thrombosis and embolism (abnormal formation and migration of blood clots) in many disorders. It was approved for use as a medication in 1954 and has remained popular ever since; warfarin is the most widely prescribed oral anticoagulant drug in North America.[1] Despite its effectiveness, treatment with warfarin has several shortcomings. Many commonly used medications interact with warfarin, as do some foods (particularly leaf vegetable foods or "greens," since these typically contain large amounts of vitamin K1) and its activity has to be monitored by blood testing for the international normalized ratio (INR) to ensure an adequate yet safe dose is taken.[2] A high INR predisposes to a high risk of bleeding, while an INR below the therapeutic target indicates that the dose of warfarin is insufficient to protect against thromboembolic events. Warfarin and related 4-hydroxycoumarin-containing molecules decrease blood coagulation by inhibiting vitamin K epoxide reductase, an enzyme that recycles oxidized vitamin K1 to its reduced form after it has participated in the carboxylation of several blood coagulation proteins, mainly prothrombin and factor VII. Despite being labeled a vitamin K antagonist,[2] warfarin does not antagonize the action of vitamin K1, but rather antagonizes vitamin K1 recycling, depleting active vitamin K1.[3] Thus, the pharmacologic action may always be reversed by fresh vitamin K1. When administered, these drugs do not anticoagulate blood immediately. Instead, onset of their effect requires about a day before remaining active clotting factors have had time to naturally disappear in metabolism, and the duration of action of a single dose of warfarin is 2 to 5 days. Reversal of warfarin's effect when it is discontinued or vitamin K1 is administered, requires a similar time. Warfarin is a synthetic derivative of dicoumarol, a 4-hydroxycoumarin-derived mycotoxin anticoagulant originally discovered in spoiled sweet clover-based animal feeds. Dicoumarol, in turn, is derived from coumarin, a sweet-smelling but coagulation-inactive chemical found naturally in "sweet" clover (to which it gives its odor and name), tonka beans (also known as "cumaru" from which coumarin's name derives) and many other plants. The name warfarin stems from its discovery at the University of Wisconsin, incorporating the acronym for the organization which funded the key research (WARF, for Wisconsin Alumni Research Foundation) and the ending -arin, indicating its link with coumarin.

zafirlukast

Zafirlukast is an oral leukotriene receptor antagonist (LTRA) for the maintenance treatment of asthma, often used in conjunction with an inhaled steroid and/or long-acting bronchodilator. It is available as a tablet and is usually dosed twice daily. Another leukotriene receptor antagonist is montelukast (Singulair), taken once daily. Zileuton (Zyflo), also used in the treatment of asthma via its inhibition of 5-lipoxygenase, is taken four times per day. Zafirlukast blocks the action of the cysteinyl leukotrienes on the CysLT1 receptors, thus reducing constriction of the airways, build-up of mucus in the lungs and inflammation of the breathing passages. Zafirlukast is marketed by Astra Zeneca with the brand names Accolate, Accoleit, and Vanticon. It was the first LTRA to be marketed in the USA and is now approved in over 60 countries, including the UK, Japan, Taiwan, Italy, Spain, Canada, Brazil, China and Turkey.

zileuton

Zileuton (trade name ZYFLO) is an orally active inhibitor of 5-lipoxygenase, and thus inhibits leukotrienes (LTB4, LTC4, LTD4, and LTE4) formation. Zileuton is used for the maintenance treatment of asthma. Zileuton was introduced in 1996 by Abbott Laboratories and is now marketed in two formulations by Cornerstone Therapeutics Inc. under the brand names ZYFLO and ZYFLO CR. The original immediate-release formulation of zileuton, known as ZYFLO, is taken four times per day. The extended-release formulation, ZYFLO CR, is taken twice daily. Although the extended release formulation of zileuton is still available (Zyflo CR), the immediate release tablet was withdrawn from the U.S. market on February 12, 2008.[1][2]