Source: Health Products Regulatory Authority (IE) Revision Year: 2021 Publisher: Gedeon Richter Plc, Gyömroi út 19-21, H-1103, Budapest, Hungary
Pharmacotherapeutic group: Hormonal contraceptives for systemic use, Progestogens
ATC code: G03AC09
Azalia is a progestogen-only pill, which contains the progestogen desogestrel. Like other progestogen-only pills, Azalia film-coated tablet can be used for women who may not or do not want to use oestrogens. In contrast to traditional progestogen-only pills, the contraceptive effect of Azalia film-coated tablet 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 intention-to-treat (ITT) group (user and method failures). Ovulation inhibition was achieved from the first cycle of use. In this study, when desogestrel 75 microgram tablet 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 intention-to-treat Pearl-Index found for desogestrel 75 microgram tablet was 0.4 (95% confidence interval 0.09‑1.20), compared to 1.6 (95% confidence interval 0.42-3.96) for 30 microgram levonorgestrel.
The Pearl-Index for desogestrel 75 microgram tablet is comparable to the one historically found for COCs in the general COC-using population.
Treatment with desogestrel 75 microgram tablets leads to decreased oestradiol levels, to a level corresponding to the early follicular phase. No clinically relevant effects on carbohydrate metabolism, lipid metabolism and haemostasis have been observed.
No clinical data on efficacy and safety are available in adolescents below 18 years.
After oral dosing of Azalia desogestrel is rapidly absorbed and converted into etonogestrel. Under steady-state conditions, peak serum levels are reached 1.8 hours after tablet-intake and the absolute bioavailability of etonogestrel is approximately 70%.
Etonogestrel is 95.5‑99% bound to serum proteins, predominantly to albumin and to a lesser extent to sex hormone binding globuline (SHBG).
Desogestrel is metabolised via hydroxylation and dehydrogenation to the active metabolite etonogestrel. Etonogestrel is primarily metabolised by the cytochrome P450 3A (CYP3A) isoenzyme and subsequently conjugated with sulphate and glucuronide.
Etonogestrel 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 etonogestrel is approximately 10 L per hour. Excretion of etonogestrel and its metabolites either as free steroid or as conjugates, is with urine and faeces (ratio 1.5:1). In lactating women, etonogestrel 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 desogestrel.
No studies were conducted to evaluate the effect of hepatic disease on the pharmacokinetics of desogestrel. 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.
The active substance etonogestrel shows an environmental risk to fish.
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