Chapter 25

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Acetic Acids Fenamates Oxicam Derivative Cyclooxygenase-2 Inhibitor

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Adverse effects:

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Anti-Arthitis Agents-Gold Compounds

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Anti-Inflammatory, Antiarthritis, and Related Agents

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Contracindications and Cautions:

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Drug Drug Interactions

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Nursing Considerations for Patients receiving Salicylates:

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Pharmacokinetics- salicylates are readily absorbed directly from the stomach reaching peak levels within 5 to 30 minutes. Thy are metabolized in the liver and excreted in the urine, with a half-life of 15 minutes to 12 hours, depending on the salicylate. Not safe in pregnancy.

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Tizanidine also known as zanaflex-an alpha-adrenergic agonist is thought to increase inhibition of presynaptic motor neurons in the CNS.

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Tylenol -acetaminophen. pain and fever. arthritis

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NSAID-Related Agents-Acetaminophen-Tylenol

Acetaminophen Tylenol- relief of pain and fever in variety of situations. It can be extremely toxic.

Drugs Acting on Cardiovascular System. Drugs affecting Blood Coagulation. Drugs affecting Clot formation and resolution.

Anticoagulants: Heparin, Generic. Warfarin, Coumadin Other Drugs Affecting Clot Formation: Low-Molecular-Weight Heparins. Enoxaprin, Lovenox

Nursing Considerations: Assessment-History and Examination Nursing Diagnosis Implementation with Rationale Evaluation

Assessment: Assess for contraindications. Assess for temp, skin color, lesions, CNS orientation, affect, reflexes, bilateral grip strength, and spasticity evaluation, bowl sounds and reported output, liver and renal function tests to determine baseline status before beginning therapy and for any potential adverse effects.

Centrally acting skeletal muscle relaxants, also known as spasmolytics include:

Baclofen Lioresal, carisoprodol Soma, chloroxazone Paraflex, cyclobenzaprine flexeril or amrix, metaxalone Skelaxin, methocarbamol robaxin, orphenadrine banflex or flexoject, and tizanidine zanaflex. Diazepam valium, a drug widely uses as an anxeity agent, also has been shown to be an effective centrally acting skeletal muscle relaxant. it may be advantageous in situations in which anxiety may be precipitating the muscle spasm. Using rest, heat, to increase blood flow to the area to remove pain-causing chemicals, physical therapy to return the muscle to normal tone and activity, and anti-inflammatory drugs NSAIDS if the underlying problem is related to injury or inflammation may help.

Baclofen should not be used to treat any spasticity that contributes to locomotion, upright position, or increased functions. Blocking this spasticity results in loss of these functions.

Baclofen is used for alleviation of signs and symptoms of spasticity; may be of use in spinal cord injuries or spinal cord diseases.

The centrally acting skeletal muscle relaxants work in the CNS to interfere with the relaxes that are causing the muscle spasm. The work in the upper levels of the CNS, possible depression must be anticipated with their use.

Because centrally acting skeletal muscle relaxants, drugs, lyse or destroy spasm, they are often referred to as spasmolytics. Most of these agents are rapidly absorbed and metabolized in the liver. Baclofen is not metabolized , but like the other skeletal muscle relaxants, it is excreted in the urine.

Adverse effects of Centerally acting skeletal muscle relaxants

CNS depression, drowsiness, fatigue, weakness, confusion, headache, and insomnia. GI disturbances, nausea, dry mouth, anorexia, constipation, hypotension, arrthymias, urinary frequency, enuresis, and feelings or urinary urgency. Tizanidine, Zanaflex has been associated with liver toxicity and hypotension in some patients. Chlorzoxazone also known as Paraflex. may discolor the urine. becoming orange to purple-red when metabolized and excreted.

All centrally acting skeletal muscle relaxants should be used cautiously in the following circumstances: history of epilepsy because the CNS depression and imbalance caused by these drugs may exacerbate the seizure disorder, cardiac dysfunction because muscle function may be depressed, with any condition marked by muscle weakness, which the drugs could make much worse, and with renal or hepatic dysfunction. Especially with Metexalone-Skelaxin or Tizanidine -Zanaflex, which could interfere with the metabolism and excretion of the drugs, leading to toxic levels.

Carisoprodol-Soma, may be safer than the over spasmolytics in older patients and in patients with renal or hepatic dysfunction. No good studies exist regarding the effects of these agents during pregnancy and lactation.

RESCRIBED FOR: Allopurinol is used for treating acute attacks of gout, erosive destructive gouty joint disease, uric acid deposits in tissues (tophi), gouty kidney disease, and uric acid stones. Allopurinol also is used to prevent elevation of blood uric acid in patients undergoing chemotherapy for the treatment of certain cancers and in patients with recurrent calcium kidney stones and elevated uric acid levels. DOSING: The dose range of allopurinol is 100-800 mg day. It should be taken with food to avoid irritation of the stomach. In order to avoid formation of kidney stones, patients should drink plenty of fluids while taking allopurinol. DRUG INTERACTIONS: Allopurinol increases blood levels of oral mercaptopurine (Purinethol) and azathioprine (Imuran) by reducing their breakdown in the body. Therefore, the dose of mercaptopurine and azathioprine should be reduced in order to avoid toxicity. There is an increased risk of skin rash in patients taking allopurinol in combination with penicillins.

Common reactions include diarrhea, nausea, rash and itching, and drowsiness. The most frequent side effect to allopurinol is skin rash. Allopurinol should be discontinued immediately at the first appearance of rash, painful urination, blood in the urine, eye irritation, or swelling of the mouth or lips, because these can be a signs of an impending severe allergic reaction that can be fatal. Allopurinol should be avoided by patients with a prior severe reaction to the drug. Allopurinol can cause a flare-up of gouty arthritis during initial therapy. Therefore, colchicine often is used simultaneously to prevent these flares. Rarely, allopurinol can cause nerve, kidney, and bone marrow damage. Allopurinol can cause a serious allergic liver toxicity that can be fatal. Appetite loss and itching can be signs of liver toxicity. The risk of this reaction increases in patients with kidney impairment. Patients with kidney impairment should receive lower doses of allopurinol.

Allopurinol, Zyloprim, Aloprim

DRUG CLASS AND MECHANISM: Allopurinol is used for treating gout caused by excessive levels of uric acid in the blood (hyperuricemia). Uric acid is a by product from the breakdown of certain proteins (purines) in the body. Hyperuricemia occurs when the body produces more uric acid than it can eliminate. The uric acid forms crystals in joints (gouty arthritis) and tissues, causing inflammation and pain. Elevated blood uric acid levels also can cause kidney disease and stones. Allopurinol prevents the production of uric acid by blocking the activity of the enzyme that converts purines to uric acid. Uric acid levels usually begin to fall within 2-3 days of starting treatment and return to their original levels within 7-10 days after allopurinol is stopped. It may take several months of therapy before attacks of gout are controlled. The FDA approved allopurinol prior to 1982.

NSAIDS-Nonsteriodal antiinflammatory Agents-

Drugs that block prostaglandin synthesis and act as anti-inflammatory, antipyretic, and analgesic agents. n

Propionic Acids

Fenoprofen Nalfon Ibuprofen Motrin, Advil, others Ketaprofen Orudis Naproxen Naprosyn Oxaprozin Daypro

General Anesthetic Agents-Nonbarbiturate General Anesthetics-Midazolam, Versed. Onset 15 minutes. Recovery 30 minutes. Duration 2-6 hours. Analgesia.

IV Midazolam, Versed is a non barbiturate anesthetic. It is very potent amnesiac. Indications: Sedation, anxiolysis, and amnesia before diagnostic, therapeutic, or endoscopic procedures, induction of anesthesia, continuous sedation of intubated patients. Actions: acts mainly at the limbic system and RAS; potentiates the effects of GABA; has little effect on cortical function;exact mechanism of action is not understood.

Drug Drug Interactions

If any of the centrally acting skeletal muscle relaxants are taken with other CNS depressants or alcohol, CNS depression may increase. Patients should be cautioned to avoid alcohol while taking these muscle relaxants; if this combination cannot be avoided, they should take extreme precautions.

Baclofen also known as Lioresal: centrally acting skeletal/ muscle relaxant spasmolytics. 40-80mg PO daily. 12-1500 mcg/d per intrathecal infusion pump. Pediatric intrathecal infusion pump, 24-1199 mcg/day-base dose on patient response. This medication is available in oral, intrathecal forms and may be delivered via a delivery pump. intrathecal means within a sheath; through the theca of the spinal cord into the subarachnoid space. This medication is not metabolized , but like the other skeletal muscle relaxants, it is excreted in the urine.

It is used to treat central spasticity. Spasticity means sustained muscle contractions. Baclofen also known as Lioresal is used to treat muscle spasticity with neuromuscular diseases such as multiple sclerosis, muscle rigidity, and spinal cord injuries.

Anti-Arthritis Agents-Other-Penicillamine-Depen 125-250mg PO daily

Penicillamine-Depen used for the treatment of severe, active RA in adults whose disease is unresponsive to conventional therapy.

Heparin, Generic 10,000-20,000 units SQ, then 8,000-10,000 units q8h, 5,000-10,000 units IV q4-6h Pediatric 50 units/kg IV bolus, then 100units/kg IV q4h

Prevention and treatment of venous thrombosis, pulmonary embolus, atrial fibrillation with embolization, prevention of clotting in blood samples, dialysis, and venous tubing; diagnosis and treatment- of disseminated intravascular coagulations. DIC in essence means the patient clots too much, resulting in the possibility of bleeding to death. also used as an adjunct in the treatment of MI and stroke. overdose of heparin, the antidote is protamine sulfate, generic. A dose of 1mg IV protamine neutralizes 90 USP. Administer slow-not to exceed 50mg IV in any 10 minute period.

Other Drugs Affecting Clot Formation Low-Molecular-Weight Heparins-Enoxaparin, Lovenox. Hip Surgery 30mg SQ q 12h for 7-10days.

Prevention of DVT that may lead to PE after hip replacement or abdominal surgery; with war fin to treat acute DVT or PE; prevention of ischemic complications of unstable angina or non Q-wave MI; prevention of DVT in patients with severely restricted mobility due to illness.

Metaxalone also known as Skelaxin a centrally acting skeletal muscle relaxant. A spasmolytic. Adults and children >12 years old: 800mg PO TID-QID. Reduce dose with hepatic impairment.

Relief of discomfit of acute musculoskeletal conditions; one of the few skeletal muscle relaxants with an established pediatric dose for children >12 years

Orphenadrine also known as Banflex or Flexoject. a centrally acting skeletal muscle relaxant. A spasmolytic. 100mg Po am and at bedtimes, or 60mg IV or IM q 12h

Relief of discomfort or acute musculoskeletal conditions in adults;under investigation for relief of quinidine-induced leg cramps

Narcotics-Morphine, Roxanol, Astramorph. Adult 2-10mg/70 kg IV over 4-5 minutes

Relief of moderate to severe chronic and acute pain, preoperatively and postop and durning labor. Intraspinal to reduce intractable pain. Acts as an agnoist at specific opioid receptors in the CNS to produce analgesia, euphoria, and sedations. Patients should be reassured that the risk of addiction to a narcotic during treatment is remote. They should be encouraged to ask for pain medication before the pain is acute, to get better coverage for their pain.

Salicylates block prostaglandin activity, which decreases the inflammatory response and relieves the signs and symptoms of inflammation. Salicylates can cause GI irritation, eight cranial nerve stimulation, and salicylism-ringing in the ears, acidosis, nausea, vomiting, diarrhea, mental confusion, and lassitude.

Salicylates are a popular anti-inflammatory agent not only because of their ability to block the inflammatory response, but also because of their antipyretic-or fever blocking and analgesic, pain blocking, properties. They are the oldest anti-inflammatory drugs used. They were extracted from willow bar, poplar trees, and other plants by ancient peoples. OTC. A person who does not response to one salicylate may respond to a different one.

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The NSAIDs are contraindicated in the presence of allergy to any NSAID or salicylate, and Celecoxib is also contraindicated in the presence of allergy to sulfonamides.

NSAID-PROPIONIC ACID-Ibuprofen-

Treatment and pain, arthritis, dsymenorrhea, juvenile arthritis

Aspirin. Name brands: Bayer, Empirin, others. It is a salsa late. Antiinflammatory-prophalyxis. Adult 325-650mg PO or PR q4h. Myocardial infarction MI: 300-325mg PO Pediatric 65-100mg/kg per day PO or PR in four to six divided doses if <2 year of age consult with prescriber

Treatment of fever, pain, inflammatory conditions, at low dose to prevent the risk of death and MI in patients with history of MI, prevention of transient ischemic attacks. TIA.

Warfin, Coumadin. 10-15mg/d PO, then 2-10 mg/d PO based on PT ratio or INR, use lower doses with geriatric patients.

Treatment of patients with atrial fib, artificial heart valves, or valvular damage that makes patient susceptible to thrombus and embolus formation/ Prevention and treatment of venous thrombosis, pulmonary embolus, embolus with atrial fib, systemic emboli after MI. Do not take with salicylates. thyroid drugs. reverse affects with vitamin K.

Cyclobenzaprine also known as Flexeril. a centrally acting skeletal muscle relaxant. A spasmolytic. 10 mg TID do not exceed 60mg/day. This medication is available in controlled release form for continual control of the discomfort without repeated dosing.

Used for relief of discomfort of acute musculoskeletal conditions in adults.

Methocarbamol also known as Robaxin, a centrally acting skeletal muscle relaxant. A spasmolytic. It is available in both oral and parenteral forms. Most of these agents are rapidly absorbed and metabolized in the liver. Adults 1.5g PO QID up to 30-60 mg/day. 1-2g IV or IM for tetanus. Pediatric 15mg/kg IV for tetanus 0.4mg/kg per day PO initially maintenance 0.2mg/kg per day.

Used for relief of discomfort of acute musculoskeletal conditions in adults. Treatment of tetanus in children to alleviate signs and symptoms of tetanus.

Chlorzoxazone also known as Paraflex

may discolor the urine. becoming orange to purple-red when metabolized and excreted.


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