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15 Cards in this Set
- Front
- Back
- 3rd side (hint)
What are some examples of Phase I reactions?
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Oxidation (CYP450-mediated)
Reduction Deamination Hydrolysis |
May undergo before or after phase II
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What are some examples of Phase II reactions?
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Glucuronation
Acetatylation Glutathionation Glycination Sulfonation Methylation |
May undergo before or after phase I
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What properties are required to allow for elimination of the drug?
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Drug must be made more polar (lipid molecules more easily reabsorbed from renal tubule)
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Which drug is associated with slower metabolism in European-Americans and African-Americans than in most Asians?
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Isoniazid, Hydralazine, Procainamide
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Metabolized by N-acetylation
50% of white and African-American persons in US are 'slow acetylators'. Inherited as autosomal recessive gene |
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What are some common CYP indcuers?
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Smoking
Barbiturates (Phenobarbital) Carbamazepine Rifampin Omeprazole Phenytoin Ethanol Isoniazid |
CYP inhibitors decrease the level of CYP-metabolism-dependent drugs in the body
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What are some common CYP inhibitors?
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Cimetidine
Grapefruit juice Macrolides Azole antifungals (ketoconazole, fluconazole) Fluoroquinolones Isoniazid Amiodarone SSRIs Cyclosporine Erythromycin Tacrolimus |
CYP inhibitors increase the level of CYP-metabolism-dependent drugs in the body. Increase the risk of toxicity
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What are some drugs whose metabolism is inhibited or induced when combined with a CYP inhibitor or inducer?
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Acetaminophen
Clozapine Haloperidol Theophylline TCAs Warfarin Barbiturates Phenytoin Opioids Antiarrhythmics CCBs PPIs HMG-CoA reductase inhibitors SSRIs Trazodone |
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What drug is hydrolyzed by a plasma esterase that is abnormally low in activity in about 1 of every 2500 humans?
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Succinylcholine
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1 in 2500 humans have an abnormal form of plasma cholinesterase, which allows for an increased duration of action of succinylcholine (can last many hours instead of 5 minutes)
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What is the function of the P-glycoprotein?
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Functions to expel drugs from the intestinal mucosa into the lumen. Also found in the BBB and in drug-resistant cancer cells
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What are some inhibitors of P-glycoprotein?
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Verapamil
Mibefradil Grapefruit juice |
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What drugs are preferentially expelled by the P-glycoprotein?
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Digoxin
Cyclosporine Saquinavir |
Potentially toxic when given with a P-glycoprotein inhibitor
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What drug has a higher first-pass metabolism in men than in women?
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Ethanol
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Men have grater gastric metabolism of ethanol, creating a lower bioavailability than in women
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Chronic use of what drug may increase the toxicity of acetaminophen?
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Ethanol
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Acetaminophen is first acted upon by phase I reaction, creating a toxic metabolite. Normally phase II reaction would occur immediately, creating a nontoxic final product. Ethanol preferentially increases phase I reactions, increasing the production of the toxic metabolite.
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What drug, when used in combination with other anti-HIV drugs, permits dose reduction?
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Ritonavir
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Ritonavir inhibits hepatic drug metabolism. At low doses in combination regimens it allows dose reductions of other HIV protease inhibitors (indinavir)
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What are 3 important drugs that follow zero-order elimination kinetics?
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Alcohol
Phenytoin Aspirin |
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