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Effect of oral contraceptives on triazolam, temazepam, alprazolam, and lorazepam kinetics
Author(s) -
Stoehr Gary P,
Kroboth Patricia D,
Juhl Randy P,
Wender Donald B,
Phillips J Paul,
Smith Randall B
Publication year - 1984
Publication title -
clinical pharmacology and therapeutics
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.941
H-Index - 188
eISSN - 1532-6535
pISSN - 0009-9236
DOI - 10.1038/clpt.1984.240
Subject(s) - alprazolam , temazepam , triazolam , lorazepam , pharmacology , crossover study , glucuronidation , hypnotic , estrogen , chemistry , diazepam , ethinylestradiol , medicine , population , benzodiazepine , endocrinology , anesthesia , placebo , anxiety , biochemistry , receptor , alternative medicine , microsome , pathology , psychiatry , enzyme , environmental health , research methodology
The effects of low‐dose estrogen oral contraceptives (OC) on the elimination of the oxidized benzodiazepines triazolam (TRZ) and alprazolam (ALP) and the conjugated benzodiazepines temazepam (TMZ) and lorazepam (LOR) were studied in two parallel crossover studies of 20 women each. Women taking OC steroids containing low doses of estrogen and women matched for age, weight, and cigarette smoking received single oral doses of TRZ (0.5 mg) and TMZ (30 mg) or ALP (1 mg) and LOR (2 mg). Kinetics were determined as plasma concentrations during 48 hr after dosing. OCs inhibited the metabolism of ALP: The AUC increased and the elimination rate constant was greater in users of OCs. For TRZ, which has an intermediate extraction ratio, the AUC was increased by OCs but not significantly so. In contrast, OCs decreased the A UC for TMZ and the elimination rate constants for LOR and TMZ. The AUC of LOR was not affected by OCs. Low‐dose estrogen OCs may therefore inhibit the metabolism of some oxidized benzodiazepines and accelerate the metabolism of some conjugated benzodiazepines. Clinical Pharmacology and Therapeutics (1984) 36, 683–690; doi: 10.1038/clpt.1984.240