Desogestrel

When ATH:
G03AA09

Pharmacological action

Sinteticheskiй progestin, chemical structure similar to levonorgestrel. It has progestogenic activity. It causes the transition of the epithelium of the endometrium proliferative secretory phase. It reduces the viscosity of cervical mucus. It inhibits the secretion of LH by the pituitary gland and, thus, It causes inhibition of ovulation. It has a weak androgenic activity, which can not be shown.

Pharmacokinetics

Desogestrel is rapidly and almost completely absorbed from the gastrointestinal tract and immediately metabolized in the liver and in the intestinal wall in the 3-keto-desogestrel, which is the biologically active metabolite of desogestrel. C_max achieved through 1.5 h and is 2 ng / ml. Bioavailability – 62-81%. 3-keto-desogestrel is bound to plasma proteins, mainly to albumin and globulin, sex hormone binding. V_d is 5 l / kg. C_ss It is set to the second half of the menstrual cycle, when the level of 3-keto-desogestrel increases 2-3 times. Products further metabolism ketodesogestrel pharmacologically inactive, some of them converted by conjugation to polar metabolites, primarily sulfates and glucuronides. T_1/2 is 38 no. The metabolites are excreted with urine and faeces (in relation to 6:4).

Testimony

Oral Contraception (in combined preparations).

Dosage regimen

Average daily dose 150 g.

Side effect

Maybe: changes in libido, headache, nausea, vomiting, breast tenderness, weight gain, increased tendency to thrombosis and increased risk of thromboembolism.

Contraindications

Vaginal bleeding of unknown etiology, severe liver disease, thrombosis, thromboembolism, artery disease, Hypersensitivity to desogestrel.

Pregnancy and lactation

Progestin, having androgenic activity are contraindicated during pregnancy.

Cautions

Desogestrel can be used in combination with ethinyl estradiol.

Drug Interactions

The data is not provided.