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Marked alterations in dose‐dependent prednisolone kinetics in women taking oral contraceptives
Author(s) -
Legler Udo F,
Benet Leslie Z
Publication year - 1986
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.1986.66
Subject(s) - prednisolone , medicine , volume of distribution , oral administration , oral dose , endocrinology , corticosteroid , distribution (mathematics) , pharmacokinetics , mathematical analysis , mathematics
Six healthy women chronically (>6 months) using oral contraceptives were age‐ and weight‐matched with female controls. Each subject received prednisolone, 0.53 and 0.14 mg/kg iv. In the subjects taking oral contraceptives there were significant decreases in total clearance, unbound clearance, and volume of distribution at steady state for total drug, and significant increases in total and unbound prednisolone t ½ and hydrocortisone concentrations compared with control subjects at both the high and low prednisolone doses. Both the oral contraceptive group and the control group had significantly higher total clearance, volume of distribution for total drug, and unbound fraction for the high dose compared with the low dose. Data suggest that chronic low‐dose contraceptive steroid use results in a marked decrease in prednisolone clearance; however, dose‐dependent changes in kinetics are still observed. Clinical Pharmacology and Therapeutics (1986) 39, 425–429; doi: 10.1038/clpt.1986.66