Effect of oral contraceptives on triazolam, temazepam, alprazolam, and lorazepam kinetics

@article{Stoehr1984EffectOO,
  title={Effect of oral contraceptives on triazolam, temazepam, alprazolam, and lorazepam kinetics},
  author={Gary P. Stoehr and Patricia D. Kroboth and Randy P. Juhl and Donald B. Wender and J. Paul Phillips and R. Blackwell Smith},
  journal={Clinical Pharmacology \& Therapeutics},
  year={1984},
  volume={36}
}
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… Expand
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Pharmacodynamic evaluation of the benzodiazepine–oral contraceptive interaction
TLDR
The data suggest that differences in benzodiazepine pharmacokinetics between OC users and control women do not account for observed differences in psychomotor impairment, and women taking OCs are more sensitive to the Psychomotor effects of single oral doses of Benzodiazepines. Expand
DISPOSITION ral contraceptives containing ethinyl estradiol nd gestodene markedly increase plasma oncentrations and effects of tizanidine by nhibiting cytochrome P 450 1 A 2
Background and Objective: Oral contraceptives (OCs) can inhibit drug metabolism, but their effect on various cytochrome P450 (CYP) enzymes and drugs can be different. Our objective was to study the… Expand
Effect of oral contraceptive steroids on the pharmacokinetics of phenprocoumon.
TLDR
The accelerated glucuronidation of phenprocoumon in OCS users suggests the need for careful monitoring of the anticoagulatory response in these subjects, especially when the OCS are withdrawn. Expand
The effect of ethinyloestradiol and levonorgestrel on the CYP2C19-mediated metabolism of omeprazole in healthy female subjects.
TLDR
Oral contraceptives containing ethinyloestradiol but not those containing only LNG decrease CYP2C19 activity and neither of the OC preparations seemed to have an inhibitory effect on the formation of omeprazole sulphone by CYP3A4. Expand
Alprazolam Pharmacokinetics in Women on Low‐Dose Oral Contraceptives
TLDR
Alprazolam free fraction in plasma was slightly but significantly greater in the oral contraceptive group as opposed to the control group, however, comparison of free clearance between groups revealed no significant difference. Expand
Lack of effect of oral contraceptive use on the pharmacokinetics of quinine.
The pharmacokinetics of quinine after a single 600 mg oral dose of quinine sulphate were studied in seven female subjects who used oral contraceptives and in seven age-matched female controls who did… Expand
Effect of an oral contraceptive preparation containing ethinylestradiol and gestodene on CYP3A4 activity as measured by midazolam 1'-hydroxylation.
TLDR
It is suggested that, at the doses used, ethinylestradiol and gestodene have a relatively small effect on CYP3A4 activity in vivo, and slightly increased the AUC of oral midazolam. Expand
Bromazepam pharmacokinetics: Influence of age, gender, oral contraceptives, cimetidine, and propranolol
TLDR
Bromazepam clearance is significantly impaired in elderly individuals, by coadministration of cimetidine and possibly propranolol, and in 11 young female users of oral contraceptive steroids, compared with seven age‐ and weight‐matched control women not using oral contraceptives. Expand
Oral contraception does not alter single dose saquinavir pharmacokinetics in women.
TLDR
Pharmacokinetic interactions of synthetic sexual steroids with saquinavir are not likely to account for the increased ADR to antiretroviral therapy seen in women. Expand
Pharmacokinetics of oxaprozin in women receiving conjugated estrogen
TLDR
Oxaprozin clearance, accomplished by a combination of oxidation and conjugation, is unimpaired by coadministration of conjugatedEstrogen, and the kinetics of a single 1200 mg oral dose was studied in 22 healthy female volunteers. Expand
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References

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TLDR
It is concluded that OCS exert a differential effect on the elimination of benzodiazepines, whereby oxidation of chlordiazepoxide is impaired while the glucuronidation of lorazepam and oxzepam is enhanced by OCS. Expand
Lorazepam and oxazepam kinetics in women on low‐dose oral contraceptives
TLDR
Women on low‐dose estrogen oral contraceptives (OC) and drug‐free control women matched for age, weight, and cigarette smoking habits, received single 2‐mg IV doses of lorazepam or single 30‐mg oral doses of oxazepams, two benzodiazepines metabolized by glucuronide conjugation, finding metabolic clearance by glucuridation is not significantly affected by OC. Expand
Differential effects of isoniazid and oral contraceptive steroids on antipyrine oxidation and acetaminophen conjugation.
TLDR
The capacities for drug oxidation and conjugation appear to be controlled by different mechanisms, and clearance of antipyrine and acetaminophen across both studies was not statistically significantly correlated within individuals. Expand
Impairment of diazepam metabolism by low-dose estrogen-containing oral-contraceptive steroids.
TLDR
The clinical result of the decrease in diazepam clearance reported here would be increased steady-state plasma diazepAM concentration after longterm use at a given daily dose, with the potential for increasing the clinical effects of diazep am in this population. Expand
Impairment of antipyrine metabolism by low‐dose oral contraceptive steroids
TLDR
Even low‐dose estrogen containing OCS may impair clearance of other drugs, since volume of distribution and body weight are of the same order in both groups, prolongation of antipyrine t½β is the result of decreased total metabolic clearance. Expand
Effects of oral contraceptive steroids on acetaminophen metabolism and elimination
TLDR
The data suggest that the increased clearance of acetaminophen from plasma in women taking OC steroids results from increased glucuronidation of the drug, although the mechanism is not known. Expand
Clinical Pharmacokinetics of Oxazepam and Lorazepam
TLDR
3-hydroxy benzodiazepine derivatives used as sedatives and anxiolytics and Oral and intramuscular lorazepam are rapidly absorbed, with systemic availability averaging 90 % or more. Expand
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TLDR
There is considerable interspecies and interdrug variability in the effect of sex differences and oral contraceptive steroids on hepatic drug elimination and women on OC steroids had a lower plasma binding and a higher volume of distribution, but these differences were not statistically significant. Expand
Increased Metabolic Clearance of Acetaminophen with Oral Contraceptive Use
TLDR
Low-dose estrogen oral contraceptive steroid may stimulate the metabolism of a conjugatively metabolized drug such as acetaminophen, in contrast to contraceptive steroid impairment of the clearance of some oxidatively metabolizer drugs, with antipyrine being the prototype. Expand
Impaired elimination of caffeine by oral contraceptive steroids.
TLDR
It is concluded that OCS impair the elimination of caffeine, and women on OCS had a significantly lower total plasma clearance and free clearance than women not taking OCS. Expand
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