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46 Cards in this Set
- Front
- Back
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What are the three main differences, in terms of action, between NSAIDs and narcotic analgesics?
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1. much lower maximal effects
2. no addiction 3. no unwanted cns side effects. |
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What are the common side effects of NSAIDs?
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1. GI ulceration
2. Blockade of platelet aggregation 3. Inhibition of uterine motility 4. Alterations in renal function 5. Hypersensitivity reactions |
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What is the effect of prolonged overuse of NSAIDs on the kidney?
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Analgesic abuse nephropathy=
papillary necrosis. Chronic interstitial nephritis |
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What are the beneficial effects of aspirin?
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Analgesic, antipyretic and anti-inflammatory
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What is the mechanism of action of aspirin on prostaglandin synthesis?
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Irreversibly inhibits cyclooxygenase and prevents prostaglandin synthesis.
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What is the recomended maximal dose for aspirin per day?
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4g/day
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What is an early warning for aspirin toxicity?
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Tinnitus or deafness
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What are the toxic effects of aspirin.
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Tinnitis, deafness
Decrease in renal function GI intolerance Hepatotoxicity Hypersensitivity |
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What effect does toxic salicylate administration have on acid-base regulation.
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It cuases an innitial respiratory alkalosis followed by a metabolic acidosis
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Give 3 uses for aspirin other than analgesia.
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Juvenile rheumatoid arthritis
Decrease the incidence of MI Decrease the incidence of colon cancer. |
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Reye's syndrome
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Caused by administraion of aspirin during viral infection especially influenza in children. Causes hepatotoxicity and microvesicular fat accumulation.
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Diflunisal
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Derivative of salicylic acid. Higher potency than aspirin but no antipyretic effect. Longer duration than aspirin
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Mesalamine
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Salicylate used in the treatment of IBD.
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What are the three main examples of salicylates given in lecture?
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Aspirin, Diflunisal, and Mesalamine
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What are the therapuetic effects of acetaminophen?
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analgesic and antipyretic. (No anti-inflammatory)
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What is the maximal dose of acetomenophen recomended per day?
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4-6 grams per day.
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What is used to treat toxic doses of acetaminophen?
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N-acetylcysteine (mucomyst)
Effective when given 8-10 hours after ingestion. |
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Ingestion of what substance causes increase of acetaminophen toxicity in the liver?
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Alcohol
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What are the three examples of indole derivatives given in class?
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Indomethacin, sulindac, etodolac.
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What drug inhibits renal secretion of indomethacin?
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Probenecid
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What adverse effects do the indole derivatives cause?
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GI symptoms=nausea vomitin, anorexia, abdominal pain.
Severe frontal headaches Depression |
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What is another use of the indole derivatives other than analgesia?
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Used to treat gout and ankylosing spondylitis and management of a patent ductus arteriosis.
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What is sulindac used to treat?
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Rheumatiod arthritis, osteoarthritis, and ankylosing spondylitis.
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Tolmetin
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Heteroaryl acetic acid derivative. Has moderate to severe GI side effects
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Diclofenac
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Heteroaryl acetic acid derivative. Reduces synthesis of PGs and leukotrienes. Less GI side effects than aspirin.
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In what type of patients is Diclofenac not indicated.
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Children, nursing mothers or pregnant women.
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Ketorolac
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Heteroaryl acetic acid derivative. Inhibits prostaglandin synthesis. Indicated for short term management of moderate to severe pain at the opiod level.
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What are the arylpropionic acid derivatives?
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Ibuprofen
Naproxen Ketoprofen Oxaprozin |
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Ibuprofen
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Mild anti-inflammatory and analgesic. Reduced gastric symptoms. Extensively metabolized in the liver and highly protein bound in the body.
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Naproxen
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Well absorbed orally, highly protein bound and excreted in the urine. Less GI symptoms than aspirin and 20x more potent.
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What two disorders are treated with naproxen but not other arylpropionic acid derivatives?
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Ankylosing spondylitis and juvenile rheumatiod arthritis.
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Ketoprofen
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Inhibits both cyclooxygenase and lipoxygenase.
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Oxaprozin
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Arylpropionic acid derivative. Long half life. Given once daily.
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What are the two enolic acids?
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Piroxicam and meloxicam
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Meloxicam
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Preferentially inhibits COX-2 over COX-1. Used in the treatment of osteoarthritis.
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Which enolic acid analgesic is approved for the treatment of osteoarthritis?
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Meloxicam
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Nabumetone
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Ketone produrg converted into an active acid derivative. Preferentially inhibits COX-2 at low doses. Low incidence of side effects.
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Celecoxib
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Selective COX-2 inhibition. Used in the treatment of osteo and rheumatiod arthritis. Does not affect platelet function or prothrombin time.
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What are the two selective COX-2 inhibitors that were pulled from the market?
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Rofecoxib and Valdecoxib
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Abatacept
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Inhibits T-cell activation. Used to treat adult rheumatoid arthritis and juevenile idiopathic arthritis.
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Rituximab
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Monoclonal antibody that binds specifically to CD20 antigen on B lymphocytes.
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What is a complication of using rituximab
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In some cases a fatal infusion reaction can occur.
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Etanercept
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Binds to TNF and blocks interaction with cell surface receptors. Antirheumatic drug.
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Adalimumab
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Binds to TNF alpha and blocks its interaction with cell receptors.
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What is a ptotential complication of using adalimumab?
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Infections. TB, fungal and other opportunistic infections.
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Infliximab
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Neutralizes biological activity of TNFa and prevents binding with receptors. May cuase increase risk of infections
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