Included in the formulation
АТХ:G.03.A.A Progestogens and estrogens (fixed combinations)
Pharmacodynamics:Combined oral means, has estrogen-progestational, contraceptive effect. The therapeutic and contraceptive effect of the drug is associated with the difficulty of the transformation processes of the tertiary follicles and with the lengthening of the ovulation period. Promotes the restoration of reproductive function and has a haemostatic effect in dysfunctional uterine bleeding.
Atsetomepregenol causes a transition in the uterine mucosa secretory phase, promotes the development of the fertilized egg, reduces the excitability of muscle and contractility of the uterus and fallopian tubes, stimulates the formation of the end elements of the breast. Ethinylestradiol It causes endometrial proliferation, and activates the development of the uterus of female secondary sex characteristics (including in their underdevelopment) eliminates common disorders, occurring in the body at deficiency female gonads (menopause, gynecological operations) involved in the formation of bone tissue.
Pharmacokinetics:Absorption when ingestion is high; slowly released within a few hours. Well absorbed from the vagina, from the mucous membranes, subcutaneous tissue. It is distributed in most tissues, especially in the mammary glands, uterus, vagina, hypothalamus and pituitary gland. Characterized by high affinity for adipose tissue. The connection with plasma proteins is moderate or high (50-80%, with albumin and globulin binding sex hormones). It is exposed to the effect of the first passage through the liver, where it is metabolized by oxidation with the formation of inactive 2-OH-ethynyl-estradiol and 2-methoxyethyne-estradiol. Subsequently, the latter are subjected to glucuronidation and sulfation to less active metabolites, non-steroidal compounds that can interact with catecholamine receptors of the central nervous system, and rapidly eliminated conjugates with glucuronic acid. In the tissues there are transformations of both estrogens into others and their metabolites. The place of metabolism of synthetic estrogens is not completely determined (presumably in the liver). When using exogenous estrogen in the urine are allocated estradiol, estrone, estriol (the main metabolite), glucuronides and sulfates. Eliminated by the kidneys (40%) and feces (60%). Excessed intestinal hepatic recirculation. Elimination slows down with obesity. Depending on the physiological state (pregnancy, individual phases of the ovarian-menstrual cycle), age and other conditions, the rate of excretion is different.
Indications:Contraception, functional infertility, dysfunctional uterine bleeding, hypothalamic syndrome during puberty.
XIV.N80-N98.N93 Other abnormal bleeding from the uterus and vagina
XIV.N80-N98.N94.6 Dysmenorrhea, unspecified
XIV.N80-N98.N97 Female infertility
XXI.Z30-Z39.Z30 Monitoring the use of contraceptives
Contraindications:Hypersensitivity, pregnancy, lactation, liver disease, stomach ulcer, arterial hypertension, thromboembolism, allergic diseases, bronchial asthma, eczema, epilepsy, tumor diseases.
Carefully:Diseases of the liver and gallbladder, epilepsy, depression, ulcerative colitis, uterine myoma, mastopathy, tuberculosis, kidney disease, adolescence (without regular ovulatory cycles).
Pregnancy and lactation:Action category for the fetus by Food and Drug Administration (US Food and Drug Administration) - H.
In the absence of two consecutive menstrual cycles, you should cancel the appointment and exclude pregnancy. If the scheme of taking the drug is violated, pregnancy should be excluded after the first absent cycle. After the withdrawal of funds in order to attempt to become pregnant, you should take a break for 1-2 months or wait for regular menstruation.
Penetrates into breast milk. Depending on the type of drug and dosage regimen, it can increase, decrease or not affect the quality and quantity of milk. It is not recommended to use high doses during the period of breastfeeding (treatment is started after lactation is established).
Dosing and Administration:Inside, regardless of food intake.
At a threatening miscarriage - 0.0005-0.001 g 1-3 times a day for 7-10 days. With the usual miscarriage - 0.0005-0.002 g for 1-2 months (course - 0.003-0.006 g).
With dysfunctional uterine bleeding - 0.0005-0.0025 g per day from the 15th to the 24th day of the cycle.
For contraception - 0.0005 g per night (for a maximum of 1 year), starting from 5th day of the menstrual cycle for 21 days (with the omission of the reception the next day take 2 tablets (morning and night)..
With functional infertility - 0.0005-0.0025 g from the 5th to the 25th day for 2-3 cycles with a subsequent 2-month break.
Side effects:Nausea, headache, breast engorgement, abdominal pain, intermenstrual bleeding, swelling of the face and legs, allergic reactions, skin rash, change in libido, weakness, drowsiness, weight gain that weakens or disappears completely during treatment. With a pronounced side effect, the drug is canceled.
Overdose:Nausea, vomiting.
Treatment is symptomatic.
Interaction:Ethinyl estradiol increases the effectiveness of lipid-lowering drugs. Weakens the effects of male sex hormones, diuretic, hypotensive and hypoglycemic drugs, anticoagulants. Folic acid and thyroid drugs strengthen the action of ethinyl estradiol, barbiturates - reduce.
Special instructions:Duration of treatment - no more than 1 year.