Effects of age, gender and oral contraceptives on intramuscular midazolam pharmacokinetics. NLM AIDSLINE Important note: Information in this article was accurate in 1989. The state of the art may have changed since the publication date.

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Effects of age, gender and oral contraceptives on intramuscular midazolam pharmacokinetics.

J Clin Pharmacol. 1988 Nov;28(11):1040-5. Unique Identifier : AIDSLINE MED/89214738
Holazo AA; Winkler MB; Patel IH; Department of Drug Metabolism, Hoffmann-La Roche Inc., Nutley,; New Jersey 07110.

Abstract: The effects of age, gender and low-dose (50 mcg or less) oral contraceptive steroids (OCS) on the pharmacokinetics of midazolam were evaluated following a single 7.5 mg intramuscular dose to five groups (8/group) of healthy volunteers consisting of young males, young females, elderly males, elderly females, and young female users of oral contraceptives. Blood samples were collected at specified times over a 24-hour period, and plasma concentrations of midazolam and its 1-hydroxymethyl metabolite were determined by a GC-EC assay. Midazolam was rapidly absorbed following intramuscular administration to the different groups. Comparison of young men vs elderly men, young women vs elderly women, young men vs young women, elderly men vs elderly women, and young women OCS-users vs young women non-OCS users indicated no substantial differences in the pharmacokinetic profile of midazolam between groups except for the comparison between the young and elderly men groups. The rate of elimination of midazolam was significantly slower in the elderly males compared to the young men. The pharmacokinetic profile of 1-hydroxymethyl midazolam paralleled that of the parent compound. This is to be expected since this metabolite exhibits formation rate-limited kinetics. Except for one subject who reported hives and itching, considered to be remotely related to test drug, no other adverse experiences or laboratory abnormalities were reported.
Keywords: Adult Aged Aged, 80 and over Aging/*METABOLISM Contraceptives, Oral, Hormonal/*PHARMACOLOGY Female Human Injections, Intramuscular Male Midazolam/ADMINISTRATION & DOSAGE/BLOOD/*PHARMACOKINETICS Sex Factors JOURNAL ARTICLE

KWDadultagedaged,80andoveraging/KWDmetabolismcontraceptives,oral,hormonal/KWDpharmacologyfemalehumaninjections,intramuscularmalemidazolam/administration&dosage/blood/KWDpharmacokineticssexfactorsjournalarticle
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M8980790

Copyright © 1989 - National Library of Medicine. Reproduced under license with the National Library of Medicine, Bethesda, MD.

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