Citations for: Nanda, K.; Stuart, G. S.; Robinson, J.; Gray, A. L.; Tepper, N. K.; Gaffield, M. E. Drug Interactions between Hormonal Contraceptives and Antiretrovirals. AIDS 2017, 31 (7), 917–952.

Entry Type
Name
Value
Parent Entry
Pharmacology Data Field
CYP3A3, CYP3A4, CYP2A6
Nomegestrol Acetate (API)
Pharmacology Data Field
CYP3A4
Dienogest (API)
Pharmacology Data Field
Metabolized by CYP3A4, CYP2C9, UGT
Ethinyl Estradiol (API)
Pharmacology Data Field
CYP3A4. No hepatic first pass effects after oral intake.
Medroxy­progesterone Acetate (API)
Pharmacology Data Field
CYP3A4
Levonorgestrel (API)
Pharmacology Data Field
CYP3A4
Etonogestrel (API)
Pharmacology Data Field
At least 20 different metabolites observed in urine and feces. Metabolites generated independently of the cytochrome P450 system, with only minor metabolism by CYP3A4.
Drospirenone (API)
Pharmacology Data Field
CYP3A4
Norethindrone (API)
Pharmacology Data Field
Hepatic, CYP3A4
Norgestimate (API)
Pharmacology Data Field
Hepatic, primarily by CYP3A4
Gestodene (API)
Pharmacology Data Field
  • Inhibits CYP2C9, CYP2C19, CYP3A4, CYP2B6
  • After formation of very reactive intermediate by oxidation of C17 ethinyl, can irreversibly inhibit cytochrome P450 enzymes (e.g. CYP2C8, CYP3A4). Thus it exerts strong effects on hepatic metabolism.
  • Nuclear receptor subfamily 1 group I member 2: agonist
  • Bile salt export pump: inhibitor, inducer
  • Sodium/bile acid cotransporter: inducer
  • Canalicular multispecific organic anion transporter 1: inducer
  • Multidrug resistance protein 1: substrate
  • Uridine diphosphate glucuronosyltransferase (UGT): inducer
Ethinyl Estradiol (API)
Pharmacology Data Field
CYP3A4, CYP2C9
Desogestrel (API)
Pharmacology Data Field
CYP3A4
Norelgestromin (API)
Pharmacology Data Field
Metabolized by CYP3A4, CYP2C9, UGT
Estradiol Valerate (API)
Pharmacology Data Field
CYP3A4
Norgestrel (API)
Pharmacology Data Field
Metabolized by CYP3A4, CYP2C9, UGT
Estradiol Cypionate (API)
Pharmacology Data Field
Inhibits CYP3A4, CYP2C9, CYP2B6 Induces UGTs
Estradiol Cypionate (API)
Pharmacology Data Field
Inhibits CYP2C19, CYP3A4, CYP2B6
Induces UGTs
Estradiol Valerate (API)