Chemical formula: C₂₂H₃₀O Molecular mass: 310.473 g/mol PubChem compound: 40973
Desogestrel is a progestogen. Like other progestogen-only pills, desogestrel is best suited for use during breast feeding and for women who may not or do not want to use oestrogens. In contrast to traditional progestogen-only pills, the contraceptive effect of desogestrel is achieved primarily by inhibition of ovulation. Other effects include increased viscosity of the cervical mucus.
After oral dosing desogestrel (DSG) is rapidly absorbed and converted into etonogestrel (ENG). Under steady-state conditions, peak serum levels are reached 1.8 hours after tablet-intake and the absolute bioavailability of ENG is approximately 70%.
ENG is 95.5-99% bound to serum proteins, predominantly to albumin and to a lesser extent to SHBG.
DSG is metabolised via hydroxylation and dehydrogenation to the active metabolite ENG. ENG is primarily metabolised by the cytochrome P450 3A (CYP3A) isoenzyme and subsequently conjugated with sulphate and glucuronide.
ENG is eliminated with a mean half-life of approximately 30 hours, with no difference between single and multiple dosing. Steady-state levels in plasma are reached after 4-5 days. The serum clearance after i.v. administration of ENG is approximately 10 l per hour. Excretion of ENG and its metabolites either as free steroid or as conjugates, is with urine and faeces (ratio 1.5:1). In lactating women, ENG is excreted in breast milk with a milk/serum ratio of 0.37-0.55. Based on these data and an estimated milk intake of 150 ml/kg/day, 0.01-0.05 microgram etonogestrel maybe ingested by the infant.
No studies were performed to evaluate the effect of renal disease on the pharmacokinetics of DSG.
No studies were conducted to evaluate the effect of hepatic disease on the pharmacokinetics of DSG. However, steroid hormones may be poorly metabolized in women with impaired liver function.
No studies were performed to assess pharmacokinetics in ethnic groups.
Toxicological studies did not reveal any effects other than those, which can be explained from the hormonal properties of desogestrel.
h3 .Environmental Risk Assessment (ERA)
The active substance etonogestrel shows an environmental risk to fish.
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