Pharmocology Section #1 (Lexi + Emily+ Delaney)*

-Topical forms (cream, ointment- greasy, suppository) Aerosols Parenteral (IV): what are types of storing them?

Ampules (single dose) and vials (single or multi-dose)

Allergic reaction that occurs within 30 mins. Some symptoms include pruritus, urticaria, wheezing, stridor, hypotension, abdominal or uterine cramping.

Anaphylaxis or Anaphylactoid reaction

Allergic reaction that occurs minutes to days after initiation of therapy. Symptoms- mucosal lesion involvement, urticaria, swelling of central face, respiratory distress, and cardiovascular collapse.

Angioedema/Urticaria

"animal testing"

FDA makes an exception for some drugs for certain conditions such as, radiation exposure or anthrax, to be tested for efficacy in higher primates and not require human trials, only human safety trials

What did the Archives of Internal Medicine find about meds lasting?

Most of the active ingredients they contain were present in adequate amounts decades after the drugs' expiration dates. The medicines, which had expired 28 to 40 years ago, were found in a retail pharmacy in their original, unopened packaging.

alkalin urine ____ the speed of elimination

decreases

schedule 4

has lower potential for abuse relative to substances in schedule 3 may be filled 5 times within a 6 month period ex. benzodiazepines, tramadol

Schedule 1

has no medically accepted use in the US or lacks accepted safety for use in treatment under medical supervision -LSD Heroin

schedule 3

has potential for abuse, but less than c-2 abuse may lead to moderate or low physical dependence or high psychological dependence -may be refilled 5 times within a six month period ex. codeine with acetaminophin

schedule 5

lower potential for abuse compare to schedule 4 -may be prescription or OTC ex. some codeine containing cough syrups, diphenoxylate

Expiration: All meds much have an expiration date. Some states require the patient's individual Rx bottle to list the expiration date. The manufacturer states that the drug will ______, which ranges between 12 and 60 months, known as the drug's "___."

maintain its full potency up until that expiration date shelf life

The Medical Letter wrote the statement on the next slide. What about the difference in solids vs liquids?

"When no suitable alternative is available, outdated drugs may be effective. How much potency they retain varies with the drug, the lot, the preservatives (if any), and the storage conditions, especially heat and humidity; many solid dosage formulations stored under reasonable conditions in their original unopened containers retain ≥90% of their potency for at least 5 years after the expiration date on the label, and sometimes much longer. Solutions and suspensions are generally less stable. There are no reports of toxicity from degradation products of currently available drugs."

Health-care providers are experiencing more "_______ ________" caused by the increasing number of drug interaction warnings.

"alert fatigue"

This measure is used to define _____ drugs. This includes drugs such as digoxin (Lanoxin®), lithium (Lithane®) and warfarin (Coumadin®). Measurement of serum or plasma levels of drugs to assess treatment response and to avoid adverse effects is known as ______.

"narrow therapeutic index" (NTI) "therapeutic drug monitoring" (TDM).

Maculopapular, Urticaria, SJS/TEN, AGEP, Vasculitis, and Bullous eruption or the most common types of ______.

"rashes"

what is the average cost of developing a new prescription drug?

$4 million dollars - <20% of drugs that make it to phase 1 clinical trials make it to market

clinical trial phase 3

(1000-3000) people to confirm effectiveness, monitor side effects, compare to commonly used treatments, and collect info to allow it to be used safely

-Transdermal "patches" (Skin is good absorption) What is something to be careful of with patches? What about with procedures?

-Drug absorption from a patch can be dangerously increased by heat: bathing, heating pads, exercise, even a fever. -A fever of 104° F can potentially increase Duragesic® (fentanyl) levels by one-third -Transdermal systems should be removed before scanning with a MRI. Some patches are formulated with an aluminized backing that could cause injury to the patient. FDA is aware of two adverse events in which patients who were wearing a nicotine patch during an MRI experienced burns.

Suggestions for consumers to save of drug cost: -____ first, ____ second -Newer ______ -Make use of your _____ and know your plan's formulary. -Use ____ meds

-Lifestyle change first, meds second (like don't smoke) -Newer is not always better -Make use of your insurance plan. Buying 3 mo. worth at one time cost one or two months worth of co-pay instead of the usual three for separate prescriptions -Generic meds! You'll get the same compound and SAVE a lot. However, newer drugs are not available generically

Drugs may be packed into different forms, including: -Liquids -Tablets -Capsules

-Liquids (solution, elixir, suspension, eye drop, otic solution and suspension). Suspensions you must SHAKE, you don't have to shake syrup. -Tablets (enteric coated, compressed, scored, sublingual, buccal, vaginal, "melt-in-your-mouth"). Do not crush an enteric coated! They are coated to dissolve in the stomach. Compressed are not coated These dosage forms, as well as enteric-coated products, should not be crushed as this would destroy the dosage-release system.

Drugs are chemicals, and therefore, break-down in the presence of heat, light and moisture. Gives some examples we care for this.

-Some drugs need refrigeration; some do not. - Many drugs are sensitive to light, thus most are packaged in containers that protect from light, like in brown bottles

PAPs are patient assistant programs. Some PhRMA (pharaceuntical manufacturers) have programs to assist people who can't afford to buy the drugs they need

..

Prescription drugs account for _____% of overall U.S. health care expenditure. There is also a trend towards using drugs that are _____. For example, the new Hep C therapy was marketed at cost of $1,000 per day. That is A LOT for a patient.

11% ; increasingly complex, which are more extensive than traditional pharmaceuticals

when was the era of chemical synthesis?

1950s

Drugs available prior to ___________ were grandfathered and allowed to remain on the market until the FDA evaluated them

1962 *often referred to as legacy drugs *the manufacturers had to receive FDA approval

when was the biotechnology era?

1980s insulin was the first biotech drug developed in 1983 revolution began with Watson and Crick's discovery of DNA

What percent of patients are on five or more prescription medications? People 65 and older were most likely to be on ________.

20%..think about nursing homes. Many can take around 25 drugs and nurses spent 15 minutes per patient administering ; chronic meds

What percent of women age 50-64 are on antidepressants?

25%

How many classes of medications comprise the majority of all reports of allergic and pseudoallergic reactions?

5. 1. Antibiotics and Sulfonamides 2. Nonsteroidal anti-inflammatory drugs, Analgesics 3. Contrast media 4. Anticonvulsants 5. Anticoagulants

medication errors are responsible for _________ ED visits per year

700,000 *4 in 10 drugs are wrongly admitted in hospitals

Generics account for _____% of the total US pharmaceutical market volume. Brand-name drugs stay on the market an average of_____ years before facing generic competition.

84% 12.8

A drug is considered bioequivalent if it exhibits bioavailability properties (e.g., rate and extent of absorption) that are similar to the product being compared. The FDA requires that the ______ (not blood level) of these properties fall within the _______ of the brand product in the following 3 parameters: - - - Look at the picture on page 17

90% confidence interval 80%-125% range 1. Maximum concentration (Cmax) 2. Time to maximum concentration (Tmax) 3. Area under the curve (AUC)

What about safety of getting INTO medication containers?

All states require that medications be dispensed in child-resistant containers. Client may request a general waiver to dispense all medications in non-child-proof containers. Like a grandmother

"Beers list," "Zhan's list," Screening Tool of Older Persons potentially inappropriate Prescriptions (STOPP), and Screening Tool to Alert doctors to Right Treatment (START) are all guides for what??

A guide on what drugs you can and can't give to the elderly

Defined as the chemical changes or effects a drug has on body cells. These changes or effects may be reversible or irreversible.

Action of drug

Allergic reaction that appears 5 days after medication is started. Also known as "pustular drug eruption," and "toxic pustuloderma."

Acute Generalized Exanthematous Pustulosis (AGEP)

Drugs are restricted to pharmacy-only sales, but do not require a prescription. Examples of BTC drugs include pseudoephedrine and hormonal contraceptives.

Behind-the-counter (BTC) Before the FDA allows a drug to be sold without a prescription, federal regulators assess whether the medicine is safe enough for patients to use without a doctor's supervision. These drugs are held to the same FDA standards of drug effectiveness and safety as prescription (Rx) drugs- The FDA requires that the drug treat a medical condition that consumers can diagnose and manage themselves. The drug's label must also clearly explain the drug's potential adverse effects and directions for its use.

___ is a fact of life. (Bell-shaped curve of normal distribution). Start slow. We can draw a bell shaped curve, say we give it to this guy and we overdose him; then we give it to this guy and we under dose him.

Biological variation

Medicines that contain an active drug substance that is derived from or composed of a living organism highly similar to an existing FDA-approved biologic. Notwithstanding minor differences in clinically inactive components between the two types of medications, the biosimilar must have no clinically meaningful differences from the reference product in terms of quality, safety, or efficacy. A biosimilar is not considered a generic drug, because it is not chemically synthesized. Said another way, a "biosimilar" is a generic biological drug. These are listed in the ______.

Biosimilars "Purple Book" first published in 2015. Purple book for biosimilars, orange book for generics. Orange book generics must be A rated and purple book with biosimilars are in 80-125 range

___ is the delivery of medications in varying amounts during the 24-hour day, taking into consideration the day-night patterns in the risk of disease or exacerbation of symptoms as well as biological rhythm-dependent differences in patient tolerance to them.

Chronotherapeutics Example: most acid is secreted in the evening, give H-2 antagonists, e.g., Tagamet, Pepcid for ulcer disease at bedtime. Low-dose aspirin should be given at bedtime for optimum ant-platelet effects. Take aspirin at bed time because blood pressure will raise.

Is when the drug should not be used in a particular illness or disorder.

Contraindication (Metformin contraindicated in renal failure)

____ of the drug may have a placebo effect. Each group was given a "new codeine-like" placebo; one group was told the medication cost $2.50 per tablet, the other group's medication cost 10 cents. 85.4% of respondents reported analgesic effects with the more expensive treatment vs. 61% with the less expensive agent.

Cost

And some products, such as dietary supplements, can generally be marketed with NO prior approval under a separate law called the ________.

Dietary Supplement Health Education Act (DSHEA).

-Buccal films -Implants and pumps

Dissolves in cheek

Defined by FDA law as "an article (other than food) intended to affect the structure or any function of the body." Clinically it is defined as any substance used in the diagnosis, treatment, cure or prevention of disease or a condition.

Drug it can be anything (even nicotine, or water). By the FDA definition it can be water, you can die from water intox D5W

What is the most expensive drug in the US? How much does it cost?

Eculizumab (Soliris): it is a therapy for the life-threatening blood disorder paroxysmal nocturnal hemoglobinuria. It only affects 8,000 Americans. It cost $500,000 per year (it is a rare disorder that causes red blood cells to break down sooner than they should.)

Evaluating new drugs: E

Effectiveness a. The best effectiveness data will compare the new drug against the drug in current use. b. However, this type of direct comparison may not be available when a drug is first marketed.

____ is the actual effect and how well it accomplishes it. Explain potency vs. efficacy..

Efficacy Being more "potent" does not necessarily mean that a drug is more efficacious. For example, Bumex® is said to be 20 times more potent than Lasix®; but both have equal efficacy if given as 2 mg of Bumex® and 40 mg of Lasix®. If a drug is more potent, we take LESS

Interdisciplinary approach to clinical practice. Its basic principles are that all practical decisions made should 1) be based on research studies and 2) that these research studies are selected and interpreted according to some specific norms characteristic for EBP. Typically such norms disregard theoretical studies and qualitative studies and consider quantitative studies according to a narrow set of criteria of what counts as evidence. Evidence is comprised of research findings derived from the systematic collection of data through observation and experiment and the formulation of questions and testing of hypotheses

Evidence-Based Practice (EBP) or Evidence-Based Medicine (EBM)

T or F: all trials have a placebo arm?

F pg. 24 cancer drugs and antihypertensive agents do not

Drug nomenclature includes a chemical name, a generic (nonproprietary) name and a trade name. If a drug is available as a generic or "multi-source" product, and if the prescriber so deems, it can be legally "substituted" for a more expensive brand name drug IF the generic product is ______. What is not a bioequivalent?

FDA "A" rated to be bioequivalent to the brand name product as listed in the book: Approved Prescription Drug Products with Therapeutic Equivalents Reference (The "Orange Book"). A "B" rated product is NOT considered bioequivalent. If it is a equivalent generic, then it is A rated in the orange book. Most of them are A rated

A study concluded that patients' requests have a profound effect on physician prescribing in major depression and adjustment disorder.

Female actors feigning an adjustment disorder or depression made 298 visits to 152 doctors in 3 US cities, using one of three scripts. - Had seen a TV ad for Paxil® and asked for it by name - Had seen a TV program on depression and wondered whether a drug would help - Made no request when describing her symptoms Results: 55% of patients who mentioned the TV ad received a Rx, most often for Paxil® Patients who made a general request received a Rx 39% of the time Those who made no request received a Rx only 10% of the time

Allergic reaction that occurs 30 mins to 8 hours after re-exposure to drug. Lesion appears edematous, followed by erythema, which later darkens to a deep reddish to purple color.

Fixed Drug Eruption

_______ is recommended by the National Kidney Foundation for evaluating renal function in patients with chronic kidney disease.

Glomerular filtration rate (GFR)

An illness or disorder for which a specific drug has documented usefulness.

Indication (Metformin indicated in type II diabetes)

May be purchased without a prescription

Non-prescription or over-the-counter (OTC) drugs

only 25% of all drugs currently have approval by the FDA for use in children, thus ___-____ prescribing in pediatrics is common.

Off-label

The study of drug interactions within body tissue and how these effects are produced.

Pharmacodynamics (WORKS)

is the study of variability in drug response and toxicity due to genetic factors.

Pharmacogenetics -Can't give the same drug, same amount, and get the same response from everyone. Some people metabolize very quickly and have no affect. For now, we just shoot. In the future we will know how much to give for the specific patient.

Takes the information gained by pharmacogenetics and applies it to the development and use of medications. This is sometimes called "Precision Medicine."

Pharmacogenomics

The study of drug absorption, distribution, special tissue binding or affinity, metabolism and excretion (ADME)

Pharmacokinetics (how it MOVES)

The study of actions and effects of drugs within a living system. These include "legal" drugs such as antibiotics, "illegal" drugs such as heroin, and prescription and non-prescription drugs. Alcohol, nicotine and caffeine are also recognized as drugs.

Pharmacology

The last couple of decades have been working on the Human Genome Project. People are now having their genomes analyzed early in life to reveal their risks. Then, armed with that information, we can tailor medicines to individual needs. -Individual genomes are largely identical, but there are 10 million points in the sequence where individual codes can vary. These tiny discrepancies, known as _______, can be important markers of disease risk. -An individual's genetic profile may be used to choose a medication with minimal side effects by taking into account differences in the production of ____ enzymes.

Polymorphisms (outliers) CYP450

___ is how much of a drug is required to illicit a pharmacological effect.

Potency

Are drugs requiring a prescription to be dispensed. These are designated as Rx on the label.

Prescription (or Legend) drugs

Evaluating new drugs: P

Price a. Cost can be a complex subject. b. Does the price, if higher than the agent you currently use, justify the added benefits of the new drug? c. Included in your price considerations also should be the cost of additional monitoring that might be necessary with the new agent.

Drug Samples: What are some pros? Cons?

Pro: -Cost saving: allows pts. to test the drug to see if they can tolerate it without getting the full dose, resulting in saving money Con: -Practioners start the pt. on the more expensive branded sample, adding to overall cost long term -Practioner obtained samples by-pass the pharmacist's final check for accuracy and counseling

______ is NOT an allergy but looks like one with itching, hives and flushing.

Pseudoallergies

T or F: US deaths caused by drug use are more common than automobile accidents and either alcohol-induced or firearm-related deaths

T

T or F: death certificates on ICD codes for cause of death, so causes such as human and system errors and not recorded on them

T

T or F: after heart disease and cancer, medical errors kill more people than any other cause

T, according to a study at John Hopkins

delayed hypersensitivity is ______ dependent.

T-cell

How do we evaluate a new drug? Which is most important?

STEPS (Safety, Tolerability, Effectiveness, Price, simplicity) Does it pass all 5? What about all but the price? Maybe it is worth it..

Evaluating new drugs: S

Safety a. The safety profile of a drug applies to the risk of long-term or serious side effects caused by the drug. b. An older, more established drug may have more risks identified with it than a new drug that has been studied only in a limited number of patients. c. When safety is an issue, "watchful waiting" for the first year or so after a new drug is released will allow you to benefit from the experience of others without exposing your patients to unnecessary risk.

Allergic reaction that occurs 1-2 weeks after initiation of therapy. Symptoms- fever, arthralgia, and morbilliform lesions.

Serum sickness or serum sickness-like reaction

Evaluating new drugs: S

Simplicity a. Oftentimes, a new drug will offer greater simplicity. b. It can be taken less often, does not require special handling, e.g., refrigeration, or does not interact with other commonly used drugs.

What are the two types of review for drug applications?

Standard and priority review

Allergic reaction that occurs 1-3 weeks after initiation of therapy. Symptoms- erosions, small blisters, detachment of <10% of body surface area. Associated with medications or by viral infections.

Stevens-Johnson Syndrome (SJS)

What if a client asks about using a drug after an expiration date? What about if it has been opened?

The Medical Letter addresses this. The expiration date on the manufacturer's package is based on the stability of the drug in its original closed container. The date does not necessarily mean that the drug was found to be unstable after a longer period; it means only that real-time data or extrapolations from accelerated degradation studies indicate that the drug will still be stable at that date. The expiration date for new drugs is usually 2-3 years from the date of manufacture. Once the original container is opened for use or dispensing, the expiration date on the container no longer applies. Repackaged drugs must be labeled with a "beyond-use" date, generally one year or less from the date of repackaging.

_______ is the LD50/ED50 or the TD50/ED50—a measure of the margin of safety. Do we want to be high or low?

Therapeutic index TI is the difference between lethal and therapeutic range. we want it to be HIGH. some have very little wiggle room. All patients have different levels even with the same drug

What do FDA standards say about expiration dates?

To meet FDA standards, an active ingredient must be present in 90% to 110% of the amount indicated on the label. Drug expiration dates are set for 12 to 60 months after production, even though many compounds can persist far longer.

Evaluating new drugs: T

Tolerability a. Tolerability focuses on the less serious but bothersome side effects of a drug such as drowsiness or insomnia. b. Determining relative tolerability of two drugs can be difficult. Pooled dropout rates, the percentage of patients who stopped taking a particular drug during clinical trials, is a good method to sort this out.

Allergic reaction that occurs 1-3 weeks after initiation of therapy. Symptoms- lesions, large sheets of necrotic epidermis, total detachment of >30% of body surface area, and fever (nearly all cases). Sepsis is most common cause of death.

Toxic Epidermal Necrolysis (TEN)

Drugs play an important part in our society: T or F

True; people are interested in drugs

Except for the ___ and ____, no other country in the world allows manufacturers to market prescription drugs directly to consumers.

United States and New Zealand

schedule 2

has high potential for use -abuse may lead to severe psychic or physical dependence -original prescription required and may not be refilled ex. morphine, hydrocodone

How should we destruct drugs?

We used to think that flushing old drugs down the sink or toilet was okay (except for C-II), but not anymore. Significant traces of drugs are showing up in rivers, lakes, and treated water sources. Some drugs, e.g., C-IIs should still be flushed or taken to "drug take-back programs." -Seek out "drug take-back programs" instead of flushing their pills. -C-IIs can still be flushed -If one cannot take drugs to a drug take-back program (a with the exception of C-IIs) take the medication out of the vial, destroy the label and mix the drugs with coffee grounds, kitty litter, or another unpalatable substance, then put the concoction in an unmarked can or sealed bag. -To make it more effective, they now allow participating pharmacies, certain hospitals, clinics, and long-term care facilities to collect medication for proper disposal.

what is a "Dear Health Care Professional Letter" ?

What FDA requires the manufacturer to issue if adverse effects surface after the drug is marketed and it reaches the point of severity and/or frequency that the FDA considers clinically significant

What does the Table of Pharmacogenomic Biomarkers in Drug Labeling tell you?

a listing of FDA-approved drugs with pharmacogenomic information in their labeling

a. What percent of Americans are on at least one prescription drug? b. How many take two?

a. 70% b. more than half

side effects

additional effects of a drug, which are not necessarily the primary purpose of giving the drug. these effects may be desirable and undesirable *average of 70 per medication* -less to do with true toxicity and more to do with protecting from lawsuits

What are the most commonly prescribed drugs?

antibiotics, antidepressants, and painkilling opioids

ANDA (abbreviated new drug application)

application for a generic drug that allows faster marketing for them

All drugs _____; only the toxicities and doses required differ and drugs often show toxicities only after months or years of use

are toxic

Aviation rules

cannot fly within 8 hours of drinking while under influence of alcohol while using any drug that affects person's faculties while having 0.04% BAC must wait 6 hours after viagra use chantix is approved

what is the most common drug class associated with RN medication errors?

cardiovascular drugs -errors account for 24.7% of preventable errors -11.3% were associated with anticoagulants

patent rights

come 15-20 years from investigational new drug exemption (IND), but varies on factors such as selling of rights or submission of additional approved indications

infiltration or extravasation:

damage caused by leakage of solution from the vein to the surrounding tissue spaces during I.V. administration

clinical trial phase 2

drug or treatment given to a larger group (100-300) to see if it is effective and to further evaluate its safety

1970 - controlled substance act

established classes or schedules of abusable drugs based on their potential for abuse -prescriber must be registered with DEA - to see if needs to be controlled substance - must test on animals - the scheduling of drugs is subject to change

standard review

for drugs that appear to have therapeutic qualities similar to those of one or more already marketed drugs in the treatment, diagnosis, or prevention of a disease

The top reason cited for non adherence to medication for elderly adults was ______.

forgetfulness

_________ are intended to save money by restricting certain drugs and drug classes

formularies

1952 -

further distinguished between prescriptions and non-prescriptions

priority review

given to a drug that appears to have significant improvement compared to marketed products. Clinical trials may take several years without this

what are the most common medication errors made by nurses?

giving patients medicine earlier or later than they were meant to, failing to flush tubes in between administration of drugs, and use of wrong syringes to inject medication into feeding tubes

immediate hypersensitivity (drug allergy) is generally _____ mediated.

immunoglobulin E (IgE)

addiction:

impaired control over drug use, compulsive use, continued use despite harm, and craving.

TN controlled substance monitoring database

includes prescribing practitioner and date written, who filled it and whether it was a new Rx, patient info, name and form of medication that the patient received, and source of payment *rules and exemptions pg. 34-35

acidification of the urine _____ the speed of elimination

increases

photo allergic:

less common. mimic contact dermatitis. show up 24 hours later or more after sun exposure and may spread to areas NOT exposed to the sun

Saying that generic drugs are inferior to brand name drugs still lack documentation. Nevertheless, with _____ and _____, Medical Letter consultants recommend using one formulation (brand name or generic) consistently or, if consistency is not possible with generics, prescribing the brand name routinely.

levothyroxine and anti epileptic drugs (use brand name)

phototoxic:

look like exaggerated sunburn on sun-exposed areas. Occurs mins to hours of sun exposure

the extent to which a drug is affected by dialysis is determined by ____, ______, _____, ______, and ______.

molecular size, protein binding, volume of distribution, water solubility, and plasma clearance.

off label prescribing

occurs when clinicians give products to people with conditions not listed on the approved label, they depart from the approved drug dosage, method of administration, or patient population *marketing for off-label uses is illegal in the US, but prescribing for off-label uses is legal and encouraged by FDA *most common in pediatrics

photosensitivity:

occurs when some drugs react with UV light

Is one that has potential use in only a small number of people (<200,000 Americans) with the particular condition that is treated with a drug, but is significant enough for the FDA to provide incentives, e.g., tax breaks, to the company to research, develop and market the drug for a small number of patients.

orphan drug (very expensive, half of new drugs per year are orphan drugs so we don't really see them)

(PDMA) prescription drug marketing act

passes in 1987 to address issue of counterfeit drugs by: _ ban re-importation of US Rx from foreign countries - regulated drug samples - etc. pg 27

The ____ effect (and power of suggestion) is real and important. Explain this..

placebo Studies have shown that effect of drugs, particularly for pain relief, is not "all in your head" as evidenced by trials that show patients given morphine vs. saline injections both have analgesic effects that can be reversed by the narcotic analgesic naloxone (Narcan, Evzio®), even when they are told that the naloxone injection is "another pain shot." This effect is thought to be a result of the body's production of endogenous endorphins or "natural morphine." So..Narcan blocks the natural morphine so it doesn't work. Then the pain comes back. We produce a natural morphine in response to thinking pain shot. Then Narcan blocks it

Clinical trial phase 4

post marketed studies delineate additional information including the drug's risks, benefits, and optimal use

Clinical trials

randomized controlled trials that can be double blind, placebo-controlled, crossover

tachyphylaxis:

rapidly developing tolerance

A drug that has a chemical affinity and intrinsic activity for a ______ site and reacts in such a way to initiate a specific action is called an _____. If the drug has affinity for the receptor, but does not illicit an effect, it is called an ______.

receptor agonist antagonist -you can affect a receptor by putting the key in the lock. there can be a few cuts that are different. both keys fit in the lock (receptor). The drug goes in and turns (agonist) and has an affect. Some go in the receptor but don't turn, they just sit there and don't allow anything else in, blocking the receptor (antagonist).

Animal studies are conducted to determine:

toxicity (LD50/ED50) pharmacokinetic data (absorption, distribution, metabolism, excretion, half-life)

Drugs are excreted from the body via breast milk, feces, sweat ect. but the primary excretory mechanism is....?

renal excretion

1938 - Federal food, drug, and cosmetic act

required testing of all drugs and final products for harmful effects (due to elixir of sulfanilaminde)

1962 - Kefauver-Harris amendment

requires testing for efficacy as well as safety -in response to the thalidominde birth defect crisis

tolerance:

state of adaptation in which exposure to a drug induces changes that result in a diminution of one or more of the drugs effects over time.

physical dependence:

state of adaptation that is manifested by a withdrawal syndrome that can be produced by abrupt cessation, rabid dose reduction, decreasing blood level of the drug, and/or administration of an antagonist.

Therapeutic Drug Monitoring: -Obtain blood specimens only after ___ have been achieved—usually after 5 half-lives for most drugs -Unless otherwise directed, obtain ____ blood concentrations for most drugs. The rationale is that if the patient has therapeutic trough levels, he or she surely has therapeutic peak levels. For some narrow therapeutic index (NTI) drugs, you may need to obtain both peak and trough levels to monitor for adverse effects. -Obtain a blood specimen only after the drug is completely distributed in the body. Some drugs have long distributive phases. For example, digoxin levels should be obtained 6 to 8 hours after an oral dose. If not, excessively and alarmingly high levels may be measured.

steady state serum concentrations trough (low)

pharmacognosy

study of plant-based drugs -most early drugs were derived from plants

Risk evaluation and mitigation strategies (REMS)

system to manage medication risks that include letters, websites, and facts sheets, and elements to ensure safe use by requiring clinicians to become certified and participate in training, patient counseling, and monitoring

1914 harrison narcotic act

tax and regulate morphine and other opiates

Clinical trial phase 1

test an experimental drug or treatment in a small group of people (20-80) to evaluate safety, determine safe dose range, and ID side effects

What is a "black box" or "boxed Warning"

the strongest warning the FDA can require. intended to call attention to the importance of a particular adverse effect and carries legal significance as well as clinical significance

Non-adherence with prescriptions: Nearly ____ consumers admit they don't always take their prescriptions as directed. ____% admitted to some form of non-adherence behavior such as: forgot, not filled prescription, took less than the recommended dosage or substituted an OTC medication. If you are back within a month for the same thing (blood clot bc not taking Heprin (Elocyus at discharge), the hospital is fined

three out of every four 74%

1906 - Pure food and drug act

to prevent alteration and mislabeling and also establish USP (united states pharmacopeia) - requires manufacturers to list ingredients on label

What is the FDA's primary function? Most products—such as new drugs and complex medical devices—must be proven ______ and ______ before companies can put them on the market.

to write the label (indications, dose, contraindications, adverse effects, etc.) for each drug it approves. Safe and effective

The FDA must prove safeness and effectiveness before they are on the market. - FDA has authority to control nicotine levels in cigarettes and ____ and to dictate how tobacco firms can ____. The bill prohibits the FDA from banning smoking. -Other products—such as X-ray machines and microwave ovens—must measure up to performance standards

tobacco products; advertise their product

A measure of the difference between (therapeutic index) the lethal dose in 50% of the tested population (LD50) or the toxic dose (TD50) and the effective dose in 50% of the tested population (ED50).

toxicity (even water can be toxic, it is all a matter of DOSE)

adverse reactions

unintended and undesirable responses. often directly related to the drug

what are the leading counterfeit drugs in US?

viagra and Avastin

how to reports reach the FDA?

voluntary reports from health professionals and consumers OR reports from manufacturers - must report serious events within 15 days of becoming aware

Often, OTC medicines are approved in _______ — with lower amounts of active ingredients — than their prescription-only counterparts. Examples include Advil®, Motrin IB® and Nuprin®, 200 mg strengths of ibuprofen whereas the 300, 400, 600 and 800 mg strengths require a prescription.

weaker forms

two most important factors when figuring out a dose for a child are:

weight and age

What is at the heart of all FDA evaluation decisions?

whether the products benefits will outweigh its risks *no product is totally risk free

The FDA estimates that ________ of drugs in the US and other developed countries and _______ in developing countries are ______________

~1% up to %10 counterfeit