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Br J Clin Pharmacol. 1986 Aug;22(2):135-42.

Influence of gender and oral contraceptive steroids on the metabolism of salicylic acid and acetylsalicylic acid.

Abstract

Salicylic acid and acetylsalicylic acid (aspirin) disposition after an oral dose of aspirin, 900 mg (equivalent to 689.7 mg of salicylic acid) was studied in eight males, eight females and eight females receiving oral contraceptive steroids (OCS). Salicylic acid clearance was 61% higher in males compared to the control female group, an effect due largely to enhanced activity of the glycine conjugation pathway (salicyluric acid formation) in males. Salicylic acid clearance was 41% higher in OCS-users compared to the control female group due to increases in both the glycine and glucuronic acid conjugation pathways in the pill users. There was no difference in any salicylic acid disposition parameter between males and OCS-users. Area under the plasma concentration-time curve (AUC) and elimination half-life of aspirin was significantly greater and aspirin plasma hydrolysis rate was significantly lower in both female groups compared to males. There was no difference between OCS-users and the control female group in any of these parameters. Aspirin AUC and elimination half-life were significantly correlated with aspirin plasma hydrolysis rate. These data confirm the importance of hormonal factors in the regulation of drug conjugation reactions in humans and suggest that sex-related differences in salicylic acid and aspirin disposition may be of clinical importance.

PIP:

To characterize the influence of gender and oral contraceptives (OCs) on drugs metabolized by conjugation reactions, salicylic metabolism was studied in 8 males, 8 females, and 8 additional females taking OCs. In addition, differences in acetylsalicylic acid (aspirin) disposition were studied in these 3 groups of subjects. Salicylic acid clearance was 61% higher in males than in female controls due to enhanced activity of the glycine conjugation pathway (salicyluric acid formation) in males. Salicylic acid clearance was 41% higher in OC users than in female controls due to increases in both the glycine and glucuronic acid conjugation pathways in the OC users. There were no differences in salicylic acid disposition parameters between males and OC users. The area under the plasma concentration time curve and the elimination half-life of aspirin were significantly lower in both female groups compared to males, as was the aspirin plasma hydrolysis rate. Overall, these data confirm the importance of hormonal factors in the regulation of drug conjugation reactions in humans and suggest that sex-related differences in salicylic acid and aspirin disposition may be of clinical significance.

PMID:
3756063
PMCID:
PMC1401110
[PubMed - indexed for MEDLINE]
Free PMC Article
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