Microfollin (Tablets) Instructions for Use

Marketing Authorization Holder

Gedeon Richter, Ltd. (Hungary)

ATC Code

G03CA01 (Ethinylestradiol)

Active Substance

Ethinylestradiol

Dosage Form

Microfollin

Tablets 50 mcg: 10 pcs.

Dosage Form, Packaging, and Composition

Tablets are almost white, convex, odorless, with two dots marked on one side.

Excipients: colloidal anhydrous silicon, magnesium stearate, gelatin, talc, corn starch, lactose monohydrate.

10 pcs. – blister packs (1) – cardboard packs.

Clinical-Pharmacological Group

Estrogenic drug

Pharmacotherapeutic Group

Estrogen

Pharmacological Action

[I] – Instructions for medical use approved by the Pharmacological Committee of the Ministry of Health of the Russian Federation

Ethinylestradiol is an estrogen that is absorbed from the gastrointestinal tract, stimulates the proliferation of epithelial cells of the uterus and vagina, and, together with progesterone, stimulates the development of the mammary glands.

The drug increases the sensitivity of the uterine musculature to oxytocin, nonspecifically inhibits the action of androgens, enhances calcium absorption and the formation of calcium depots in the bones, has an antigonadotropic effect, and reduces the activity of the sebaceous glands.

Pharmacokinetics

Ethinylestradiol is rapidly and almost completely absorbed from the intestine. C_max in plasma is reached within 1-1.5 hours. T_1/2 is approximately 26 hours. Ethinylestradiol has a first-pass effect through the liver (the so-called “first pass” effect). Metabolism occurs in the liver and intestine.

When taken orally, the T_1/2 of ethinylestradiol is 5.8 hours. 12 hours after oral administration, the drug is not detected in the blood plasma.

Metabolites of ethinylestradiol: water-soluble sulfates and glucuronides, after conjugation, enter the intestine with bile, where they are broken down by intestinal bacteria.

Indications

• Amenorrhea;
• Oligomenorrhea;
• Dysmenorrhea;
• Menorrhagia;
• Metrorrhagia (including during the climacteric period);
• To stop lactation;
• Acne vulgaris;
• Prostate cancer;
• Climacteric syndrome.

To avoid complications, use strictly as prescribed by a doctor.

ICD codes

Dosage Regimen

Orally. For amenorrhea and oligomenorrhea – 20-100 mcg/day for 20 days, after which 5 mg of progesterone is administered intramuscularly for 5 days.

For climacteric disorders in women under 45 years of age – 50 mcg/day.

For dysmenorrhea – 10-30 mcg per day (in 3 doses), starting from the 4th-5th day of the menstrual cycle, for 20 days every 2-3 months.

For the treatment of prostate cancer and breast cancer ( in women over 60 years of age) – 50-100 mcg 3 times/day, long-term, in combination with radiation therapy. The dose is gradually reduced to a maintenance dose of 50 mcg/day.

To suppress lactation – 20 mcg 3 times/day for the first 3 days after childbirth, for the next 3 days – 10 mcg 3 times/day, then – 10 mcg once/day for 3 days.

For acne – 30-60 mcg/day, during puberty – 10-30 mcg/day.

Adverse Reactions

In women: soreness, tenderness and enlargement of the mammary glands, amenorrhea, breakthrough bleeding, menorrhagia, intermenstrual “spotting” vaginal discharge, breast tumor, increased libido.

In men: soreness and tenderness of the breast, gynecomastia, decreased libido.

Peripheral edema, gallbladder obstruction, hepatitis, pancreatitis. Intestinal or biliary colic, flatulence, anorexia, nausea, diarrhea, dizziness, headache (including migraine), contact lens intolerance, vomiting (mainly of central origin, mainly when using large doses).

When treating breast and prostate cancer (additionally): thromboembolism, thrombosis.

Contraindications

• Pregnancy;
• Liver dysfunction;
• Condition after hepatitis;
• History of idiopathic jaundice of pregnancy or pruritus of pregnancy;
• Dubin-Johnson and Rotor syndromes;
• Presence or history of thrombophlebitis or thromboembolism;
• Cerebrovascular accident;
• Presence or suspicion of hormone-dependent tumors of the mammary glands or endometrium and cervix;
• Endometriosis;
• Vaginal bleeding of unknown etiology;
• Lipid metabolism disorders;
• Otosclerosis, aggravated during previous pregnancies.

Use in Pregnancy and Lactation

Large doses of estrogen prescribed in the early stages of pregnancy can cause fetal development disorders, so pregnancy should be ruled out before prescribing.

Use in Hepatic Impairment

Contraindicated: liver dysfunction.

Use in Renal Impairment

Estrogens can cause sodium and water retention in the body, so they should be prescribed with extreme caution in case of renal impairment.

Special Precautions

The drug should be discontinued immediately if previously unobserved, frequent migraine-like headache occurs, if acute visual impairment occurs, at the first signs of thrombophlebitis or thromboembolism, if blood pressure increases, if jaundice (cholestatic) appears, or during prolonged immobilization (for example, after accidents).

Estrogens can cause sodium and water retention in the body, so they should be prescribed with extreme caution in case of cardiovascular disorders, renal impairment, arterial hypertension, epilepsy, and bronchial asthma. In angle-closure glaucoma, it may increase intraocular pressure. In diabetes mellitus, the possibility of decreased glucose tolerance should be taken into account.

Before prescribing the drug, a thorough general medical examination with examination of the breasts and pelvic organs and blood pressure measurement is necessary. With long-term use of the drug, the examination should be repeated after the first six months, and then at least once a year.

Due to the danger of breakthrough uterine bleeding, the drug should be prescribed cyclically even in case of chronic use.

Some liver function tests and endocrine studies give reliable results only 2-4 months after the end of treatment with ethinylestradiol.

It should be taken into account that Ethinylestradiol has a contraceptive effect under certain conditions and is a component of a number of oral contraceptive drugs.

Overdose

Cases of toxic effects due to overdose are unknown.

Symptoms of accidental overdose may be as follows: nausea, withdrawal bleeding (in women).

In case of severe overdose symptoms, gastric lavage and symptomatic treatment are recommended. There is no antidote.

Drug Interactions

Use with caution together with drugs that are metabolism inducers (may enhance the metabolism of the drug).

Storage Conditions

Store at a temperature of 15-30°C, in a place inaccessible to children.

Shelf Life

Shelf life – 5 years.

Do not use after the expiration date printed on the package.

Dispensing Status

The drug is dispensed by prescription.

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.