Products
Desogestrel is commercially available as a monopreparation in the form of film-coated tablets (Cerazette, 75 µg, generic). The active ingredient was approved in the 1980s. In 2014, generic versions were registered for the first time in many countries.
Structure and properties
Desogestrel (C22H30O, Mr = 310.5 g/mol) exists as a white crystalline powder that is sparingly soluble in water. It is a prodrug of etonogestrel (3-keto-desogestrel), which is also present in the contraceptive ring (+ ethinylestradiol) and the contraceptive stick. The active metabolite is formed by CYP2C9 through hydroxylation and dehydration and is structurally related to progesterone.
Effects
Desogestrel (ATC G03AC09) has contraceptive properties. The effects are based on inhibiting ovulation and increasing the viscosity of cervical mucus. This prevents the eggs from being fertilized. Desogestrel can also be used during breastfeeding and in cases of estrogen intolerance. According to recent studies, efficacy is comparable to combined oral contraceptives (Pearl Index: 0.14 to 0.4). The half-life of the active metabolite etonogestrel is approximately 30 hours.
Indications
For oral contraception.
Dosage
According to the SmPC. The film-coated tablets are taken continuously without a break once daily every 24 hours and always at the same time. If the intake is forgotten, it can be made up within 12 hours. The next tablet is then to be administered at the usual time.
Contraindications
- Hypersensitivity
- Pregnancy
- Unexplained vaginal bleeding
- Acute venous thromboembolic symptoms
- Existing or previous severe liver disease.
- Liver tumors
- Sex hormone sensitive malignancies
For complete precautions, see the drug label.
Interactions
The active metabolite etonogestrel is metabolized by CYP3A4. Corresponding drug-drug interactions with CYP inhibitors and inducers are possible. CYP inducers may reduce efficacy. Activated charcoal used for diarrhea may decrease the absorption of desogestrel and should therefore not be taken concomitantly.
Adverse effects
A major disadvantage of the progestin pill is irregular bleeding (spotting, bleeding between periods). Other common adverse effects include absence of menstruation, acne, breast pain, weight gain, headache, mood changes, decreased libido, and nausea.
