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15 Cards in this Set

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What are some examples of Phase I reactions?
Oxidation (CYP450-mediated)
Reduction
Deamination
Hydrolysis
May undergo before or after phase II
What are some examples of Phase II reactions?
Glucuronation
Acetatylation
Glutathionation
Glycination
Sulfonation
Methylation
May undergo before or after phase I
What properties are required to allow for elimination of the drug?
Drug must be made more polar (lipid molecules more easily reabsorbed from renal tubule)
Which drug is associated with slower metabolism in European-Americans and African-Americans than in most Asians?
Isoniazid, Hydralazine, Procainamide
Metabolized by N-acetylation

50% of white and African-American persons in US are 'slow acetylators'. Inherited as autosomal recessive gene
What are some common CYP indcuers?
Smoking
Barbiturates (Phenobarbital)
Carbamazepine
Rifampin
Omeprazole
Phenytoin
Ethanol
Isoniazid
CYP inhibitors decrease the level of CYP-metabolism-dependent drugs in the body
What are some common CYP inhibitors?
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
What are some drugs whose metabolism is inhibited or induced when combined with a CYP inhibitor or inducer?
Acetaminophen
Clozapine
Haloperidol
Theophylline
TCAs
Warfarin
Barbiturates
Phenytoin
Opioids
Antiarrhythmics
CCBs
PPIs
HMG-CoA reductase inhibitors
SSRIs
Trazodone
What drug is hydrolyzed by a plasma esterase that is abnormally low in activity in about 1 of every 2500 humans?
Succinylcholine
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)
What is the function of the P-glycoprotein?
Functions to expel drugs from the intestinal mucosa into the lumen. Also found in the BBB and in drug-resistant cancer cells
What are some inhibitors of P-glycoprotein?
Verapamil
Mibefradil
Grapefruit juice
What drugs are preferentially expelled by the P-glycoprotein?
Digoxin
Cyclosporine
Saquinavir
Potentially toxic when given with a P-glycoprotein inhibitor
What drug has a higher first-pass metabolism in men than in women?
Ethanol
Men have grater gastric metabolism of ethanol, creating a lower bioavailability than in women
Chronic use of what drug may increase the toxicity of acetaminophen?
Ethanol
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.
What drug, when used in combination with other anti-HIV drugs, permits dose reduction?
Ritonavir
Ritonavir inhibits hepatic drug metabolism. At low doses in combination regimens it allows dose reductions of other HIV protease inhibitors (indinavir)
What are 3 important drugs that follow zero-order elimination kinetics?
Alcohol
Phenytoin
Aspirin