DRUG TITLE

Provera (Medroxyprogesterone)

Pharmacological action

Gestagen. It has no androgenic and estrogenic activity. Inhibits the secretion of gonadotropic hormones (especially LH). At low doses, it suppresses ovulation. It has an inhibitory effect on the changes necessary to prepare the endometrium for implantation of the fertilized egg and increases the viscosity of cervical mucus.

At higher doses, it has an antitumor effect in hormone-sensitive malignant neoplasms. This effect is apparently caused by the action on steroid hormone receptors and on pituitary-gonadal system.

Pharmacokinetics

After the intravenous administration of medroxyprogesterone, its release is slow, which provides low but constant concentrations in blood plasma.

The time to reach Cmax after IV/m injection is approximately 4-20 days. Medroxyprogesterone can be detected in plasma 7-9 months after an I/M injection. T1/2 after I/m injection is 6 weeks.

After oral administration, medroxyprogesterone is rapidly absorbed from the gastrointestinal tract, Cmax in plasma is observed after about 2-4 hours. At a simultaneous food intake bioavailability of medroxyprogesterone increases, thus T1/2 does not change. T1/2 at intake is from 12 to 17 hours.

Binding of medroxyprogesterone with plasma proteins is about 90-95%.

Medroxyprogesterone penetrates the BBB and the placental barrier, and is excreted with breast milk.

Medroxyprogesterone is largely metabolized with the participation of cytochrome CYP3A4 in liver microsomes by hydroxylation with subsequent conjugation. At least 16 metabolites of medroxyprogesterone are currently known. Most are excreted through the intestine by biliary secretion.

Contraindications to use

Hypersensitivity to medroxyprogesterone; pregnancy, breastfeeding (during the first 6 weeks of the postpartum period); vaginal bleeding of unclear genesis; severe hepatic impairment; acute thrombosis and thromboembolism at present (incl. including deep vein thrombosis, pulmonary embolism); migraine; in oncology for oral administration - children under 18 years old, parenterally - before the onset of menarche.

With caution

Thrombophlebitis, thromboembolism or stroke (increased risk of or in anamnesis), epilepsy, bronchial asthma, cardiac, renal failure, diabetes, depressed states; patients whose condition may be adversely affected by fluid retention in the body.

Administration during pregnancy and lactation

Contraindicated for use during pregnancy and lactation (breast-feeding).

Administration in patients with liver dysfunction

Contraindicated for patients with severe liver dysfunction.

Administration in patients with impaired renal function

Caution should be exercised when using in patients with renal insufficiency.

Administration in children

It is necessary to strictly follow the instructions in the instructions of medroxyprogesterone drugs for contraindications for use in children by age and the onset of menarche of specific dosage forms of medroxyprogesterone.

Use in Elderly Patients

If use in elderly patients is necessary, the risk of exacerbation of chronic diseases should be borne in mind.

Indications of active substances of Provera

For use in gynecology: contraception, endometriosis, vasomotor symptoms during menopause.

For use in oncology: additional and palliative treatment of recurrent and metastatic endometrial or renal cancer; palliative treatment of hormone-dependent forms of recurrent breast cancer in postmenopausal women; prostate cancer, cancer cachexia in advanced tumors of various localizations.

Dosing regimen

Should be strictly in accordance with the drug used dosage form of a particular drug indications for use and the dosing regimen.

It is set individually, depending on the indications, stage of the disease, and therapy regimen.