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Pharmacotherapeutic group: hormonal contraceptives for systemic use. ATC code: G03A C09.
Pharmacology: Pharmacodynamics: Cerazette is a progestogen-only pill, which contains the progestogen desogestrel. Like other progestogen-only pills, Cerazette is best suited for use during breast-feeding and for women who may not or do not want to use estrogens. In contrast to traditional progestogen-only pills, the contraceptive effect of Cerazette is achieved primarily by inhibition of ovulation. Other effects include increased viscosity of the cervical mucus.
When studied for 2 cycles, using a definition of ovulation as a progesterone level greater than 16 nmol/L for 5 consecutive days, the ovulation incidence was found to be 1% (1/103) with a 95% confidence interval of 0.02% - 5.29% in the ITT group (user and method failures). Ovulation inhibition was achieved from the first cycle of use. In this study, when Cerazette was discontinued after 2 cycles (56 continuous days), ovulation occurred on average after 17 days (range 7-30 days).
In a comparative efficacy trial (which allowed a maximum time of 3 hours for missed pills) the overall ITT Pearl-Index found for Cerazette was 0.4 (95% confidence interval 0.09 - 1.20), compared to 1.6 (95% confidence interval 0.42 - 3.96) for 30 μg levonorgestrel.
The Pearl-Index for Cerazette is comparable to the one historically found for combined OCs in the general OC-using population. Treatment with Cerazette leads to decreased estradiol levels, to a level corresponding to the early follicular phase. No clinically relevant effects on carbohydrate metabolism, lipid metabolism, and haemostasis have been observed.
Pharmacokinetics: Absorption: After oral dosing of Cerazette desogestrel (DSG) is rapidly absorbed and converted into its biologically active metabolite 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%.
Distribution: ENG is 95.5-99% bound to serum proteins, predominantly to albumin and to a lesser extent to SHBG.
Metabolism: DSG is metabolised via hydroxylation and dehydrogenation to the active metabolite ENG. ENG is metabolised via sulphate and glucuronide conjugation.
Elimination: 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 per kg body weight per day may be ingested by the infant.
Toxicology: Preclinical safety data: Toxicological studies did not reveal any effects other than those, which can be explained from the hormonal properties of desogestrel.
