Absorption:Rapidly absorbed from the GI tract (oral, IM). T max is 1.5 to 2.3 h (oral); 6.8 h (8% gel); 9.2 h (90 mg IM); 19.3 h (insert). C max is 17.3 to 60.6 ng/mL (oral); 14.9 ng/mL (8% gel); 53.8 ng/mL (90 mg IM); 19.9 ng/mL (insert). AUC is 43.3 to 175.7 ng•h/mL (oral); 1,378.9 ng•h/mL (IM 90 mg); 296.8 ng•h/mL (8% gel); 316 ng•h/mL (insert).
Distribution:Protein binding is 96% to 99%, primarily to serum albumin (50% to 54%) and transcortin (43% to 48%).
Metabolism:Metabolized in the liver to pregnanediols and pregnenolones, which are conjugated to glucuronide and sulfate metabolites.
Elimination:Excreted in the kidney (50% to 60% metabolites), bile/feces (approximately 10% metabolites), and small amount as unchanged in the bile. Absorption t ½ is 25 to 50 h (gel). Elimination t ½ is approximately 19.6 h (IM) and 34.8 h (gel).
Special Populations: Renal Function Impairment Use with caution and only with careful monitoring because metabolites are eliminated this way.
Hepatic Function Impairment Contraindicated.
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