Pharmacologic, pharmacokinetic, and therapeutic differences among angiotensin II receptor antagonists.

Article Details

Citation

Song JC, White CM

Pharmacologic, pharmacokinetic, and therapeutic differences among angiotensin II receptor antagonists.

Pharmacotherapy. 2000 Feb;20(2):130-9.

PubMed ID
10678291 [ View in PubMed
]
Abstract

Over the past 4 years, six angiotensin II receptor antagonists (ARBs) were approved for treating essential hypertension. They differ with respect to dosing, metabolism, elimination, clinical efficacy, and investigational applications. Candesartan cilexetil is the only prodrug among the agents. Losartan is distinguished from other ARBs by cytochrome P450 (CYP) 3A4- and CYP2C9-mediated biotransformation to its active metabolite EXP-3174. No ARB requires dosage adjustment for renal impairment, but the initial dose of losartan should be reduced 50% in hepatically impaired patients. None of the drugs is significantly cleared by hemodialysis. Completion of continuing trials will elucidate the drugs' role in treating heart failure, cerebral stroke, and myocardial infarction.

DrugBank Data that Cites this Article

Drug Enzymes
DrugEnzymeKindOrganismPharmacological ActionActions
LosartanCytochrome P450 2C9ProteinHumans
Unknown
Substrate
Details
LosartanCytochrome P450 3A4ProteinHumans
Unknown
Substrate
Inhibitor
Details