Ethinil Estradiol (Ethinylestradiol)
Ethinyl estradiol pronounced is named also ethinyl estradiol (EE), is a derivative of ethinyl estradiol. Ethinyl estradiol is an orally bio-active estrogen used in almost all modern formulations of combined oral contraceptive pills (the Pill). It is one of the most commonly used medications.
The same contraindications and precautions apply for Ethinyl estradiol as with other estrogen medications.
Ethinyl was a preparation of Ethinyl estradiol alone that was used for the management of menopausal symptoms and female hypogonadism.
Ethinyl estradiol is released into the environment as a xenoestrogen from the urine and feces of people who take it as a medication.
While ethinyl estradiol is readily absorbed when taken orally, it is also quickly inactivated by the liver. Substitution at C17 of the estrane steroid with an ethinyl estradiol group proved to provide an estrogen that is much more resistant to degradation and paved the way for the development of oral contraceptives.
Ethinyl estradiol is absorbed in the small intestine and reaches a serum peak about 2 hours later. It undergoes extensive metabolism in the liver involving the cytochrome P450 3A4 isoenzyme. Ethinyl estradiol and its metabolites are in excreted with the bile. Due to the effect of enterohepatic circulation a second peak is seen several hours later. Individually, wide variations exist in the overall absorption process, and can be further modified by ethinyl estradiol drugs (i.e. antibiotics) that affect the enterohepatic circulation or liver enzymes. In circulation Ethinyl estradiol is almost fully bound to plasma albumin. It is metabolized by hydroxylation of the aromatic ring and excreted in both, feces and urine, in part as glucuronide and sulfate conjugate.
Ethinyl estradiol is hormonally effective by activating the estrogen receptor and thus is an estrogen. It finds its most common use in the estrogen-progestin combination preparations of oral contraceptives. Over time, formulations have decreased the Ethinyl estradiol dose from as high as 100 μg to as low as 20 μg.
Ethinyl estradiol Indications:
Congenital anomalies [defects] genital organs (Q50-Q56)
Hypopituitarism
Hypo and other violations of pituitary
Hyperplasia of prostate
Pain and other conditions associated with female genital organs and menstrual cycle
Diseases of the skin and subcutaneous tissue (L00-L99)
Disorders of skin appendages (L60-L75)
Amenorrhea unspecified
Secondary amenorrhea
Secondary oligomenoreya
Secondary dysmenorrhea
Malignant neoplasms of prostate
Violations of menopause, and other violations in by menopause period
Oligomenoreya unspecified
Postmenopausal atrophic vaginitis
Subacute and chronic vaginitis
Subacute and chronic vulval
Acute vaginitis
Acute vulval
The absence of menstruation, scanty and rare menstruation
Primary amenorrhea
Primary oligomenoreya
Primary dysmenorrhea
Menopause and menopausal status in women
The states associated with artificially induced menopause
Acne
Acne ordinary
Acne varioliform
Acne unspecified
Acne tropical
Acne spherical
Other inflammatory diseases of vagina and vulva
Other acne
Dysmenorrhea unspecified
Female infertility
Female infertility of cervical origin
Female infertility due to lack of ovulation
Ethinyl estradiol Pharmacodynamics
Ethinyl estradiol interact with specialized receptors of estrogen, has a specific influence on the relevant organs (target organs). Influenced Ethinyl Estradiol in the Fallopian tubes, cervix, vagina, external genital organs that bring duct breast epithelial proliferation noted. It increases the sensitivity of muscles of the uterus and tubes to their exciting motility agents. Assists hipocholesterol effect, increase the content in the blood of beta-lipoproteins, the sensitivity to the action of insulin, improves glucose utilization. In high doses, Ethinyl Estradiol detain water and sodium in the body, inhibits erythropoesis. In high doses, the drug slows down, but in small activates secretion of follicle-stimulating hormone. Men inhibits spermatogenesis in the testicles can develop atrophic changes that reduced secretion of androgens. For Ethinyl Estradiol characterized by a weak anabolic effect. estrogens, proliferative, anabolic, hypolipidemic. Under certain conditions, provides contraceptive effect and is an integral part of a series of oral contraceptives.
Ethinyl estradiol Pharmacokinetics
Absorption - The fast, the existence of economies of "first-pass " NULL; Ethinyl Estradiol and its metabolites egest kidneys, with gall and subjected hepatoenteral recycling. Depending on the physiological state (pregnancy, single-phase ovarian-menstrual cycle), age and other conditions of excretion of the drug varies . Ethinyl Estradiol metabolized with the formation of 2-OH-Ethinyl Estradiol and 2-methoxy Ethinyl Estradiol.
Ethinyl Estradiol Indications
Ethinyl estradiol lack of ovarian function (primary and secondary amenorrhea, hypomenorrhea, oligomenorrhea, demeanor), infertility, vaginitis in girls and in old age, hypogenitalism, infantilism, secondary sexual inadequacy, post castration and menopausal disorders, hypoplasia of sexual apparatus and the secondary sexual characteristics, acne, for suppression of lactation, breast cancer, adenoma of the prostate, prostate cancer.
Ethinyl Estradiol Metering mode
When hypogenitalism (primary amenorrhea), usually assigned ethinyl estradiol to 0.05-0.1 mg 2 times / day for 3-4 weeks, after which should be applied hestogene preparations for 6-8 days. The course of treatment ethinyl estradiol is repeated 5-6 times. When hypo ovaries and secondary amenorrhea should appoint a ethinyl estradiol drug in the same dose, 1-2 times / day for 2-3 weeks, and within 6-8 days gestagenic drugs (progesterone for 5-10 mg / day / m or pregnin 10 -30 mg under the tongue 3 times / day). In climacteric disorders in women under 45 years of age should be appointed on 0.01-0.02-0.05 mg of the ethinyl estradiol drug daily for several days in succession, followed by progesterone or pregnin within 6-8 days. The treatment should be repeated 2-3 times. To address the neuro-vascular disorders with estrogen deficiency drug should be taken to ethinyl estradiol 0.01-0.02 mg / day for 10-15 days, treatment can be repeated after an interval of several days. When dismenoree in women with signs of underdevelopment should appoint Ethinyl Estradiol uterus immediately after menstruation to 0.01 mg per day for 2-3 weeks every day or every other day. In the treatment of prostate cancer and breast cancer (women over 60 years) drug designate up to 3 mg / day in combination with long-term radiation therapy. This dose is gradually reduced to maintenance - ethinyl estradiol 0.01 mg / day. For suppression of lactation appoint 0.02 mg 3 times / day during the first 3 days after birth, within the next 3 days - to 0.01 mg 1 time / day. When acne appoint 0.03-0.06 mg / day for children - 0.01-0.03 mg / day. Children: the average dose after puberty 0.03-0.06 mg / day.
Ethinyl estradiol Adverse effects
Nausea, vomiting, dizziness, rash, swelling of eyelids, erythropeny, breast tenderness. When long-term use: the feminization of men (decrease sexual function, swelling of the mammary glands, nipple pigmentation, reducing the size of the testicles), ovarian sclerosis, metabolic, sodium, calcium and water in the body, increase body weight, increased blood pressure, uterine bleeding, congestive jaundice.
Ethinyl Estradiol Contraindications
Hypersensitivity, breach of liver function, pregnancy, a violation of liver and kidney, malignant and benign tumors of the reproductive organs and mammary glands (cancer of the uterus, uterine myoma, cervical cancer, vulval cancer, ovarian cancer, breast cancer, breast) for women to 60 years old, inflammatory diseases of female genital organs (salpingooforit, endometritis), hyperfolliculoidism stage of menopause, the propensity to flood, trombus, pulmonary artery embolism, stroke, otosclerosis, sickle cell anemia.
Ethinyl Estradiol Interaction
Folic acid and thyroid medications increase the effect Ethinyl Estradiol. The drug enhances the effect hypocholesterolemic means, diuretic, antiarhythmic, hypotensive drugs, anticoagulants. Reduces the effects of drugs of male sex hormones.
Ethinyl Estradiol Cautions
Before starting treatment it is necessary to hold a general medical and gynecological examination (including breast examination). To designate the drug with caution arterial hypertension, carried thromboses disease.
