Biomaterial Database

Pharmacokinetic interaction of contraceptive steroids with prednisone and prednisolone. 1984

B M Frey, and H J Schaad, and F J Frey

The oestrogenic component of oral contraceptives affects the activity of liver enzymes and the concentrations of plasma proteins implicated in steroid metabolism and transport. The present study was designed to determine these effects on the kinetics of prednisone and prednisolone. After an oral dose of prednisone, women on oral contraceptive steroids (n = 10) had higher mean (+/- SD) area under the plasma concentration versus time curves of total (428 +/- 67 micrograms/ml/min vs 188 +/- 28 micrograms/ml/min, p less than 0.001) and unbound prednisolone (64 +/- 10 micrograms/ml/min vs 41 +/- 10 micrograms/ml/min, p less than 0.001) than women not taking oral contraceptive steroids (n = 10). The differences were attributable to a lower non-renal clearance of prednisolone and to a higher apparent systemic availability of the drug in contraceptive users than in the controls. The affinity of albumin and transcortin for prednisolone was lower in women on oral contraceptives than in controls (p less than 0.001). Thus, altered kinetics and protein binding may account for the known increase in glucocorticoid efficacy by oestrogens.

UI	MeSH Term	Description	Entries
D007700	Kinetics	The rate dynamics in chemical or physical systems.
D011239	Prednisolone	A glucocorticoid with the general properties of the corticosteroids. It is the drug of choice for all conditions in which routine systemic corticosteroid therapy is indicated, except adrenal deficiency states.	Di-Adreson-F,Predate,Predonine,Di Adreson F,DiAdresonF
D011241	Prednisone	A synthetic anti-inflammatory glucocorticoid derived from CORTISONE. It is biologically inert and converted to PREDNISOLONE in the liver.	Dehydrocortisone,delta-Cortisone,Apo-Prednisone,Cortan,Cortancyl,Cutason,Dacortin,Decortin,Decortisyl,Deltasone,Encorton,Encortone,Enkortolon,Kortancyl,Liquid Pred,Meticorten,Orasone,Panafcort,Panasol,Predni Tablinen,Prednidib,Predniment,Prednison Acsis,Prednison Galen,Prednison Hexal,Pronisone,Rectodelt,Sone,Sterapred,Ultracorten,Winpred,Acsis, Prednison
D011485	Protein Binding	The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments.	Plasma Protein Binding Capacity,Binding, Protein
D003276	Contraceptives, Oral	Compounds, usually hormonal, taken orally in order to block ovulation and prevent the occurrence of pregnancy. The hormones are generally estrogen or progesterone or both.	Low-Dose Oral Contraceptive,Oral Contraceptive,Oral Contraceptives,Oral Contraceptives, Low-Dose,Oral Contraceptives, Phasic,Contraceptive, Low-Dose Oral,Contraceptive, Oral,Contraceptives, Low-Dose Oral,Contraceptives, Phasic Oral,Low Dose Oral Contraceptive,Low-Dose Oral Contraceptives,Oral Contraceptive, Low-Dose,Oral Contraceptives, Low Dose,Phasic Oral Contraceptives
D003277	Contraceptives, Oral, Combined	Fixed drug combinations administered orally for contraceptive purposes.	Combined Oral Contraceptive,Contraceptive Agents, Female, Combined,Oral Contraceptives, Combined,Combined Oral Contraceptives,Contraceptive, Combined Oral,Contraceptives, Combined Oral,Oral Contraceptive, Combined
D004347	Drug Interactions	The action of a drug that may affect the activity, metabolism, or toxicity of another drug.	Drug Interaction,Interaction, Drug,Interactions, Drug
D005260	Female		Females
D006801	Humans	Members of the species Homo sapiens.	Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000328	Adult	A person having attained full growth or maturity. Adults are of 19 through 44 years of age. For a person between 19 and 24 years of age, YOUNG ADULT is available.	Adults

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