Ethinylestradiol

Этинилэстрадиол Constitutional formula

The description is actual on 18.01.2016

  • Latin name: Aethinyloestradiolum
  • ATH code: G03CA01, L02AA03, G03AA16
  • Chemical formula: C20H24O2
  • CAS code: 57-63-6

Chemical name

(The 17th alpha) - 19-norpregna-1,3,5 (10) - a triene-20-in-3,17-diol

Chemical properties

Ethinylestradiol, what is it? Ethinylestradiol is a synthetic hormone of an estrogenic row which is normal produced at women by ovaries and a bast layer of adrenal glands. Substance is responsible for development of secondary female sexual characters and bodies, processes of proliferation of an endometria, development of a uterus.

Ethinylestradiol on Latin: Aethinyloestradiolum or in a genitive case of Aethinyloestradioli. Artificially synthesized hormone represents powder, white or white with a cream shade, which is practically not dissolved in water, but we will well dissolve in alcohols and oils of a plant origin. Drug is let out in the form of 10 and 50 mkg of tablets. Most often this substance is in a combination with other hormones.

Pharmacological action

Anabolic, hypolipidemic, oestrogenic.

Pharmacodynamics and pharmacokinetics

Ethinylestradiol what hormone is? A sex hormone after receipt in an organism enters interaction with special estrogenic receptors. Synthetic hormone stimulates proliferation of epithelial fabrics in a neck of uterus, a vagina, uterine tubes, channels of mammary glands, external genitals. Under the influence of synthetic hormone degree of sensitivity of muscles of a uterus and uterine tubes to the means exciting motility raises.

Ethinylestradiol possesses gipokholesterinemichesky action, increases concentration of beta lipoproteids, increases sensitivity of an organism to insulin, stimulates processes of utilization of sugars. High dosages of drug are capable to detain liquid and Na in body tissues, to inhibit processes of formation of erythrocytes and to reduce secretion of FSG of a hypophysis.

This substance causes oppression of processes of formation of spermatozoa in men, leads to development of atrophic changes in testicles, allocation of androgens is suppressed. At a combination to other synthetic hormones substance possesses contraceptive properties, possesses weak anabolic activity.

Medicine quickly and practical are completely absorbed through mucous membranes and an integument. The metabolism of substance proceeds by means of gepatoenteralny recirculation which accompanies effect of "the first passing" through a liver where in an effect is oxidized and forms 2-it-ethinylestradiol and 2-metoksietinilestradiol. Further metabolites are exposed to reactions of sulphonation and a glyukuronirovaniye. Products are removed through kidneys with urine and bile. Speed of removal of means depends on a physiological condition of the patient.

Indications to use

Means is applied:

  • for contraception as a part of the combined drugs;
  • to eliminate negative manifestations of a climax;
  • at a female hypogonadism;
  • for treatment of a dysmenorrhea;
  • as a part of complex therapy of a tumor of a mammary gland during a climax;
  • for palliative treatment of malignant tumors of a prostate at men.

Contraindications

Medicine is not used:

  • at a breast cancer and other ekstrogenzavisimy tumors;
  • if at the patient vaginal bleeding of an unknown origin developed;
  • at herpes at pregnant women, including in the anamnesis;
  • for treatment of patients with endometriosis;
  • at pregnant women;
  • at serious heart diseases and vessels;
  • at the persons suffering from a liver failure;
  • during a lactation;
  • at a sickemia.

Side effects

Ethinylestradiol can cause:

  • nausea, disturbances in work of a gastrointestinal tract, vomiting, liver diseases, formation of stones in a gall bladder, jaundice;
  • puffiness, swelling and increase in mammary glands, decrease or opposite increase of a libido, morbidity in mammary glands;
  • failures in a menstrual cycle, suddenly arising bleedings after drug withdrawal;
  • decrease in tolerance of an organism to glucose, increase in weight;
  • indigestion, migraines, headaches and dizziness;
  • increase of risk of development of a thromboembolism, increase of quantity of blood clots in vessels;
  • hyperpegmentation of an integument, depression.

Ethinylestradiol, application instruction (Way and dosage)

Depending on indications, a dosage form and concentration of active ingredient appoint from 10 mkg to 3 mg of drug a day.

For treatment of an amenorrhea and an oligomenorrhea medicine is entered intramusculary in a dosage of 0,02-0,1 mg a day, by 20 days. Then pass to use of progesterone 5 mg a day within 5 days.

At a dysmenorrhea begin to carry out therapy from 5 in the afternoon a menstrual cycle. Use 0,01-0,03 mg of synthetic hormone a day (distribute on 3 receptions). Treatment duration – 20 days. It is possible to repeat a course each 2-3 months.

To stop a lactation use 0,02 mg of means, 3 times a day during the first several days after the delivery. The next 3 days enter 0,01 mg, 3 times a day, and once – 0,01 mg of substance.

During a climax reception of 0,05 mg of drug during the day is shown to women. For treatment of acne rash appoint from 0,03 to 0,06 mg of means a day.

The cancer therapy of a prostate is carried out in a complex with other drugs and procedures. The recommended dosing mode on 0,15-0,3 mg a day distributed on 3 receptions. After stabilization of a condition of the patient the dosage can be lowered to 0,05 mg a day.

Overdose

At reception of very high doses of this medicine there can be nausea, vaginal bleeding and vomiting. Treatment – according to the shown symptoms.

Interaction

This medicine can reduce efficiency of anti-hypertensive means, hypoglycemic drugs, anticoagulants.

Drug intake with the carbamazepine, rifampicin, barbiturates, griseofulvin and other drugs inducing liver enzymes can lead to decrease in plasma concentration of synthetic hormone.

Terms of sale

The recipe is necessary.

Special instructions

Extra care needs to be observed at treatment by drug of patients with epilepsy, bronchial asthma, migraine, diseases of kidneys and a liver, with the increased arterial pressure, multiple sclerosis, a lupus erythematosus, a hypercalcemia, an otosclerosis.

As a part of drugs this substance often is in a combination from gestodena, drospirenony, levonorgestrel, diyenogesty, dezogestrely, tsiproterony.

Hormonal drugs it is the best of all to make treatment according to the recommendation, and after consultation with the attending physician.

At pregnancy and a lactation

Synthetic hormone is contraindicated at pregnancy and during a lactation except for cases when feeding by a breast needs to be stopped.

Drugs in which contains (Analogues)

Coincidence on the ATH code of the 4th level:

Substance is active components of the tablets Ethinylestradiol,  the medicine Microfollinum.

Ethinylestradiol + Drospirenon are in composition of drugs: Yarina, Vidora, Jes, Midiana, Modell Trend, Vidora micro, Dailla, Dimia, Modell Pro, Simitsia.

Ethinylestradiol + Dezogestrel – active components of drugs Novinet, Marvelon, Regulon, Mersilon, Three - Mercy.

Often in drugs it is possible to meet a combination of Ethinylestradiol and Diyenogest. For example, in tablets Rangning, Bonade, Siluyet, Diyetsiklen.

Ethinylestradiol + Gestoden — active ingredients of medicines: Femoden, Lindinet, Gestarella, Mirell, Logest.

Responses

About drugs on the basis of this hormone good. At the correct selection of a dosage and use of medicine in compliance with recommendations of the attending physician probability of development of undesirable side reactions low.

Section: Active ingredients
PAY ATTENTION! Information on active ingredients on the website is help generalizing, collected from public sources and can form the basis for making decision on use of these substances it is not aware of treatment. Before substance Ethinylestradiol use surely consult with the attending physician.