Included in the formulation
АТХ:G.03.A.C.02 Linestrone
G.03.A.C Progestogens
Pharmacodynamics:Synthetic progestogen causes formation of a complex with specific cytoplasmic receptors, binding to the chromatin of target cells and altering the synthetic processes in the cell. Initiate the transition of the endometrium from the proliferation phase to the secretory phase. Suppresses ovulation. The mechanism of contraceptive action is associated mainly with peripheral gestagenic effect on the reproductive system, which is expressed in decreasing the amount and increasing the viscosity of cervical mucus, reducing the penetrating ability of spermatozoa. Oppresses the transport function of the fallopian tubes, reduces the implantation properties of the endometrium.
Pharmacokinetics:Absorption is high. Biotransformation occurs in the liver (active metabolite - norethisterone). Elimination by the kidneys. After oral administration linestrone It is rapidly absorbed and is converted into a pharmacologically active liver norethisterone. Cmax norethisterone in the blood plasma is observed in 2-4 hours after taking the drug. Half-life from plasma norethisterone after taking linestrenol is approximately 8-11 hours. Linestrenol and its metabolites are mainly excreted by the kidneys, and to a lesser extent through the intestine.
Indications:Dysfunctional uterine bleeding, amenorrhea, oligomenorrhoea, dysmenorrhea, premenstrual syndrome, endometriosis, endometrial carcinoma, benign breast tumor, postponement of normal menstruation, hormone replacement therapy with estrogens (as an additional tool).
II.C51-C58.C54 Malignant neoplasm of uterine body
XIV.N60-N64.N60.1 Diffuse cystic mastopathy
XIV.N80-N98.N80 Endometriosis
XIV.N80-N98.N91 Absence of menstruation, meager and rare menstruation
XIV.N80-N98.N94.3 Premenstrual tension syndrome
XIV.N80-N98.N94.6 Dysmenorrhea, unspecified
Contraindications:Severe violations of liver function, intrahepatic cholestasis, congenital disorders of bilirubin metabolism, uterine bleeding of unclear etiology; itching, otosclerosis, heart failure, hypertension, depression, thrombophlebitis.
Insulin-dependent diabetes mellitus, pregnancy, including ectopic (in the anamnesis), porphyria.
Pregnancy and lactation:Do not apply.Progestins penetrate the placenta, can cause developmental disorders of the fetus: hypospadias in a male fetus, virilization of external genital organs in a female fetus.
The FDA category is not defined.
Dosing and Administration:Inside. With endometriosis, dysmenorrhea, to suppress menstruation - 1-3 tablets a day for at least 6 months; with carcinoma of the endometrium - 6-10 tablets per day; to delay normal menstruation - 1-2 tablets a day for 1-2 weeks before the start of the expected menstruation. In addition to estrogen therapy - 1 / 2-1 tablet per day for 12-15 days of each month in the second phase of the cycle. In the case of amenorrhea or oligomenorrhea after estrogen preparation of the endometrium and with other indications - 1-2 tablets a day, starting from 14-25 days.
Side effects:Bleeding breakthrough, spotting discharge from the genital tract, hirsutism, chloasma, changing libido, nausea, diarrhea, headache, dizziness, nervousness, depression.
Chest pain, weight gain, decreased glucose tolerance, changes in bilirubin concentration, prothrombin index, lipoprotein profile, transaminase activity; genital candidiasis, acne, itchy skin.
Overdose:Nausea, vomiting.
Treatment is symptomatic.
Interaction:β-Adrenoblockers, ciclosporin - linestrone increases their plasma concentration.
Barbiturates, rifampicin, laxatives - reducing the effectiveness of contraception.
Macrolides - increased risk of toxic damage to the liver with simultaneous application with linestrenol.
Special instructions:When developing chloasma, avoid exposure to the sun.