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Effect of oral contraceptive steroids on the pharmacokinetics of phenprocoumon.
Author(s) -
Monig H,
Baese C,
Heidemann HT,
Ohnhaus EE,
Schulte HM
Publication year - 1990
Publication title -
british journal of clinical pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.216
H-Index - 146
eISSN - 1365-2125
pISSN - 0306-5251
DOI - 10.1111/j.1365-2125.1990.tb03750.x
Subject(s) - phenprocoumon , pharmacokinetics , pharmacology , medicine , levonorgestrel , mestranol , metabolic clearance rate , family planning , research methodology , population , warfarin , environmental health , atrial fibrillation
1. The effect of chronic administration of oral contraceptive steroids (OCS) on the pharmacokinetics of the oral anticoagulant phenprocoumon was investigated in seven healthy females. 2. Plasma concentrations of phenprocoumon and the urinary recovery of unchanged as well as conjugated drug were measured following a single oral dose of 0.22 mg kg‐1. A group of seven non‐smoking, drug‐free women matched for age and body weight served as controls. 3. Administration of OCS was associated with a significant increase in the clearance of phenprocoumon from 1.6 +/− 0.7 to 2.0 +/− 0.7 ml min‐1 kg‐1 (P less than 0.05). The urinary recovery of phenprocoumon glucuronide was significantly higher in OCS users (21.0 +/− 16 vs 14.0 +/− 10 (% of dose); P less than 0.05). No difference in plasma protein binding of phenprocoumon was observed, being 99.2 +/− 0.07 in both groups. 4. 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suggests the need for careful monitoring of the anticoagulatory response in these subjects, especially when the OCS are withdrawn.