Pharmacokinetics Brexanolone has low oral bioavailability of less than 5%, necessitating non-oral administration. The volume of distribution of brexanolone is<unk> proximately 3 L/kg. Its plasma protein binding is more than 99%. Brexanolone is metabolized by keto-reduction mediated via aldo-keto reductases. The compound is also conjugated by glucuronidation via glucuronosyltransferases and sulfation via sulfotransferases. It is not metabolized importantly by the cytochrome P450 system. The three main metabolites of brexanolone are inactive. The elimination half-life of brexanolone is 9 hours. Its total plasma clearance is 1 L/h/kg. It is excreted 47% in feces and 42% in urine. Less than 1% is excreted as unchanged brexanolone.
Allopregnanolone
Vinyltestosterone
Pregnanolone
Ethinylestradiol sulfonate
Estradiol enantate
Hydroxyprogesterone acetate
Methandriol propionate
Ethinylestradiol