Ethinylestradiol (Ethinylestradiol)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

"Estrogens, gestagens, their homologues and antagonists"

Antineoplastic hormonal agents and hormone antagonists

Included in the formulation
  • Diane-35®
    pills inwards 
    Bayer Pharma AG     Germany
    • АТХ:

    G.03.C.A.01   Ethinylestradiol

    Pharmacodynamics:

    Synthetic estrogen. Just like endogenous estrogens, it stimulates the development of the uterus, fallopian tubes, secondary sexual characteristics, causes proliferative changes in the endometrium, increases the excitability of the uterus. Regulates nitrogen metabolism, reduces the level of lipids and cholesterol in the blood, has a weak anabolic effect. Increases the absorption of calcium and the formation of calcium depots in the bones. In high doses, it causes sodium and water retention.

    Pharmacokinetics:

    It binds mainly to plasma albumins. Metabolized in the liver with the formation of hydroxylated and methylated metabolites.

    It is excreted as metabolites by the kidneys - 40% and through the intestine - 60%.

    Indications:

    Contraception (mainly in combination preparations).

    Manifestations of climacteric syndrome associated with estrogen deficiency; female hypogonadism, dysmenorrhea. Palliative treatment of malignant tumors of the breast in the postmenopausal period. Common acne.

    Palliative treatment of malignant tumors of the prostate.

    ICD-10

    II.C60-C63.C61   Malignant neoplasm of prostate

    II.C50   Malignant neoplasm of breast)

    IV.E20-E35.E28   Dysfunction of the ovaries

    XII.L60-L75.L70   Acne

    XIV.N80-N98.N91   Absence of menstruation, meager and rare menstruation

    XIV.N80-N98.N92   Abundant, frequent and irregular menstruation

    XIV.N80-N98.N93   Other abnormal bleeding from the uterus and vagina

    XIV.N80-N98.N94.6   Dysmenorrhea, unspecified

    XIV.N80-N98.N95.1   Menopause and menopause in women

    XXI.Z40-Z54.Z51.5   Palliative Care

    XIV.N80-N98.N97   Female infertility

    XXI.Z30-Z39.Z30.0   General advice and advice on contraception

    Contraindications:

    Breast cancer and other estrogen-dependent neoplasms, vaginal bleeding of unknown origin, herpes of pregnant women in anamnesis, endometriosis, pregnancy, lactation (breastfeeding), thrombosis and thromboembolism (including history), severe cardiovascular diseases, hepatic insufficiency, sickle cell anemia .

    Carefully:

    With caution apply for bronchial asthma, epilepsy, migraine, heart and kidney disease, as well as hypertension, hypercalcemia, multiple sclerosis, systemic lupus erythematosus, otosclerosis.

    Pregnancy and lactation:

    Action category for the fetus by FDA - X. Contraindicated in pregnancy and lactation (breastfeeding). Do not apply!

    Dosing and Administration:

    Individual, depending on the indications. The daily intake for oral administration varies from 10 μg to 3 mg.

    Intramuscularly, with amenorrhea and oligomenorrhea - 0,02-0,1 mg per day for 20 days, then intramuscularly injected progesterone for 5 days - 5 mg per day.

    With dysmenorrhea, treatment begins with the 4th-5th day of the menstrual cycle - 0.01-0.03 mg per day (for 3 doses) for 20 days, the course of treatment is repeated every 2-3 months.

    To stop lactation, 0.02 mg 3 times a day is prescribed for the first three days after birth, then 0.01 mg 3 times a day for the next three days, then 0.01 mg per day for 3 days .

    In the treatment of common acne - 0,03-0,06 mg per day.

    When prostate cancer is prescribed in the initial dose of 0.05-0.1 mg 3 times a day with a gradual decrease to the maintenance dose of 0.05 mg per day.

    With menopausal syndrome - to 0.05 mg per day.

    Side effects:

    From the side digestive system: nausea, vomiting, abnormal gastrointestinal function, impaired liver function, jaundice, formation of gallstones.

    From the side endocrine system: possible soreness and enlargement of the mammary glands, a change in the libido, a violation of the menstrual cycle and bleeding after cancellation, a decrease in glucose tolerance.

    From the side metabolism: possible swelling, weight gain.

    From the side CNS: possible depression, headache, migraine, dizziness.

    Dermatological reactions: possible hyperpigmentation of the skin.

    From the side blood coagulation system: there is an increased tendency to thrombosis and an increased risk of thromboembolism.

    Overdose:

    Symptoms: nausea, vomiting, in some cases - metrorrhagia.

    Treatment: maintenance of vital functions (against drug withdrawal), symptomatic therapy.

    Interaction:

    Estrogens can reduce the effects of anticoagulants, antihypertensive and hypoglycemic drugs.

    With simultaneous use of ethinylestradiol and drugs that induce hepatic enzymes (barbiturates, carbamazepine, griseofulvin and rifampicin), a decrease in the level of ethinylestradiol in blood plasma is possible.

    Special instructions:

    Can be used in combination with gestagens (including drospirenone, dienogest, gestodene, norelgestromin), as well as with cyproterone.

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