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32 Cards in this Set
- Front
- Back
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MOA of cortisol
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Cortisol (naturally occurring corticosteroid) - Redistribution of neutrophils, lymphocytes, monocytes, eosinophil and basophils -> ↓ macrophage TNF-alpha, IL1, metalloproteinase, and plasminogen factor; ↓ synthesis of prostaglandins, leukotrienes, thromboxane and histamines from mast cells; ↓ COX2 expression
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What are the synthetic corticosteroids
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Prednisone, triamcinolone, dextametasone, fludrocortisone
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What are the difference between natural vs synthetic corticosteroids
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Affinity for mineralocorticoids and glucocorticoid receptors, protein binding affinity, rate of elimination and metabolic protucts
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If someone comes in a need severe anti-inflammatory response
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Use betamethasone (high anti-inflammatory activity 25-40)over hydrocortisone (low anti-inflammatory activity0.8)
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What corticosteroid has a mineral corticoid activity?
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fludrocortisone
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What are the clinical indications for corticosteroids
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Osteoarthritis, RA, psoriatic arthritis, bursitis, tenosynovitis, asthma, temporal arteritis, dermatitis, crohns disease, ulcerative colitis
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What are the side effects of corticosteroids
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Na+ retention -> hypertension, hypokalemia, osteoporosis, infections, hyperglycemia, glycosuria, and peptic ulcers
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What are the contraindications for corticosteroids
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Peptic ulcers, hypertension, osteoporosis, heart failure
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What is the function of NSAIDs
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Anti-inflammatory, anti-pyretic, and analgesic(↓ blood vessels sensitivity to bradykinin and histamine); ↓ GFR and may lead to kidney failure
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What is the MOA of NSAIDS?
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Inhibits COX1 and COX2 -> prevents generation of prostacyclin, prostaglandins, thromboxanes
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What are the adverse effects of NSAIDs?
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Long term use -> ↑ bleeding time, dyspepsia, subepithelial damage, hemorrhage
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What is the MOA of aspirin?
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Irreversible inhibition of COX1 and COX2 -> inhibits prostaglandins, thromboxanes, and prostacyclins
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What is the MOA of indomethacin, piroxicam, ibuprofen?
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Inhibits oxidative burst - ↓ NADPH oxidase (inhibits neutrophils oxidative burst)
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What does COX2 inhibition lead to?
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COX2 inhibition leads to ↑ aspirin-triggered lipoxins (medeates anti-inflammatory response)
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Pt w/ transient ischemic attacks, unstable angina and coronary artery thrombosis. What is the treatment?
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Aspirin
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Child who is given aspirin and has rapid liver degeneration + encephalitis
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Reye syndrome
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What happen when u take a person off chronic aspirin?
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When stop taking aspirin -> Creates more leukotrienes -> exacerbating problem -> can become asthamtic
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What is an adverse side effect of aspirin?
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Airway hyperacticity in asthamatic pt. aspirin alters the balance of arachidonic acid to be shoved to the lipoxygenase pathway -> ↑ bronchoconstriction
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What drug has a long T1/2 is 20x more potent than aspirin, and directly inhibits leukocyte function and causes less severe adverse effects than aspirin?
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Naproxen
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Drug that is used for arthritis, a. spondyliits, grout, primary dysmonorrhea
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Ibuprofen - propinoic acid derivatives
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Indomethacin
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Inhibits prostacyclin (PGI2) -> inhibits dilation -> closes patent ductus arteriosus in newborns
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Pt who is passing a kidney stone and has pain. What drug?
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Diclofenac - ↓ intracellular [arachidonic acid]
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Pt who has gone thru surgery and needs NSAID.
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Ketorolac - strong analgesic properties
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Pt who has 1 ° dysmenorrhea. Treatment?
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Mefenamate - antagonize prostanoids receptors - less anti-inflammatory activity and higher adverse effects then aspirin
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Which fenamate derivative is used for arthritis?
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Meclofenamate - antagonize prostanoids receptors - less anti-inflammatory activity and higher adverse effects then aspirin
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Which NSAID is as efficacious as aspirin, naproxen, ibuprofen agaisnt arthritis and is better tolerated?
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Piroxicam
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Which NSIAID is a pro-drug that is more selective for COX2 inhibitiors -> thus less GI disturbances?
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nabumetone
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Treatment for acetaminophen OD
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N-acetylcystine
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Which NSAID is good for use in children to bring down fever?
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Acetaminophen - has antipyritic activity but no anti-inflammatory activity.
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What is the adverse side effect of acetaminophen
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Kidney and liver toxicitie. CYP2E1 and CYP3A4 -> mediate toxicity via release of -N-acetyl-benzoquinoneimine
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What COX2 inhibitor is used to treat familial adenomatous polyposis?
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Celecoxib
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What is the side effect of celecoxib?
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↑ risk of heart attack and stroke
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