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35 Cards in this Set
- Front
- Back
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Metabolism of salicylates
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Dose-dependent due to saturation of conjugation pathways (esp. glycine conj.)
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What is salicylate?
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The deacetylated metabolite of aspirin
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About how much aspirin is excreted as salicylate by the kidneys
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10%
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NSAID metabolism
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Oxidative and conjugation rxns in the liver
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NSAIDs with short half lives (< 6hrs.)
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Aspirin
Ibuprofen Indomethacin |
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NSAIDs with long half-lives (> 6 hrs)
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Naproxen
Phenylbutazone Salicylate |
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Metabolism of p-Aminophenols
(I assume this is tylenol) |
In the liver by conjugation, dose dependent
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Hepatotoxicity of Acetominophen
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Increase after induction of P450 enzymes (e.g. by EtOH)
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MA of hepatotoxicity of tylenol
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Metabolites deplete glutathione, then reacts w/hepatic SH- impairs Ca handling--necrosis
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Are most NSAIDs found in free form in the body?
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No, most is bound to albumin
Free fraction increased in hypoalbuminemia |
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GI problems due to COX inhibitors
(there are 5) |
Dyspepsia
Peptic ulcers--perf Inflammation Gastric erosion Upper GI hemorrhage |
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Which COX inhibitor causes less GI toxicity?
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COX-2 selective
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Misoprostol (Cytotec)
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Prostaglandin analog, prevention of gastric ulceration
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Ranitidine
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H2 receptor antagonists--reduces acid secretion
Treatment for GI problems caused by NSAIDS |
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Omeprazole
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Reduces acid secretion, H+ blocking agent
Treament of NSAID GI problems |
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Sucralfate
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Mucosal protectants
Useful with NSAIDs |
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COX-2 and the kidneys :)
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COX-2 expression required for normal renal development
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NSAIDs renal effects
(there are 7) |
Decreased GFR
Edema Papillary necrosis Inhib of loop diuretics (requires PGs) Acute/Chronic renal failure Interstitial Nephritis Hyperkalemia |
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Hypertensive effects of NSAIDs
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Impairs HTN control in those taking B-adrenergic antags, diuretics, or ACEi
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How do we get around impaired HTN control in those taking NSAIDs
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Put them on Ca channel blockers for their HTN
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Why use caution with Celebrex (Celecoxib)?
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Increased risk of adverse CV effects with use of Celebrex (Celecoxib)
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Why use caution with Naproxen?
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Increased vascular risk
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Why do aspirin and other NSAIDs impair hemostatsis?
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Inhibit platelet aggregation
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MA of NSAID induced Asthma
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Blockage of COX shunts AA to leukotriene production-- BRONCHSPASM
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COX inhibitor skin effects
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Erythema multiforme, urticaria
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COX inhibitor CNS rxns
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Drowsiness and headache (10%)
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Rare COX inhibitor side rxns
(there are 5) |
Blood dyscrasias
Mild hepatic dysfxn Severe hepatitis Pneumonitis Neurologic problems |
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Reye Syndrome
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Caused by use of salicylate drugs during in viral infections (usually in kids)
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Aspirin toxicity symptoms
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Nausea, vomiting, tinnitus
GI bleeding Impaired hemostasis Resp. alkalosis Resp. and metabolic acidosis at high toxic levels |
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Tylenol toxicity sequlae
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Hepatotoxicity
Hypoglycemic coma Renal tubuar necrosis Hypersensitivity |
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NSAIDs may interact with what protein bound drugs?
(there are 4) |
Warfarin
Phenytoin Sulfonylureas Methotrexate |
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NSAIDS may inhibit the metabolism of which drug
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Phenylbutazone
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Which drug causes increased acid transport in the kidney and therefore increased NSAID toxicity?
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Probenecid
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NSAID rxn with 1) EtOH 2) lithium
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1) Increased risk of GI bleeding/hepatotoxicity
2) Decreased renal clearance, increased toxicity |
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NSAID rxn with 1)K+ sparing diuretics 2)B adrenergic antags, ACEi, diuretics
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1) Sudden hyperkalemia
2) Hypotensive effects |
