Estrofem^® (Tablets) Instructions for Use

Marketing Authorization Holder

Novo Nordisk A/S (Denmark)

ATC Code

G03CA03 (Estradiol)

Active Substance

Estradiol (Rec.INN registered by WHO)

Dosage Form

Estrofem®

Film-coated tablets, 2 mg: 28 pcs.

Dosage Form, Packaging, and Composition

28 pcs. – plastic discs (1) – cardboard packs.

Clinical-Pharmacological Group

Anticlimacteric estrogenic drug

Pharmacotherapeutic Group

Estrogen

Pharmacological Action

Estrogen. A follicular hormone necessary for the development of the female body and reproductive system.

Exogenous Estradiol exerts the same physiological action as natural hormones: it stimulates the development of the uterus, fallopian tubes, the development of secondary sexual characteristics in cases of their underdevelopment, causes proliferative changes in the endometrium, increases the excitability of the uterus, and in large doses suppresses lactation.

Estradiol regulates nitrogen metabolism, reduces the level of lipids and cholesterol in the blood, and has a weak anabolic effect.

It helps maintain the balance between osteoblasts and osteoclasts, reduces bone resorption and promotes its formation.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract.

It undergoes the “first-pass” effect through the liver.

It is metabolized to less active metabolites – estriol and estrone.

Metabolites are excreted by the kidneys, a small part – through the intestines.

Indications

Primary and secondary amenorrhea; hypoplasia of the reproductive system and secondary sexual characteristics; hormone replacement therapy for disorders observed during natural or surgically induced menopause (including vasomotor disturbances, hot flashes, increased sweating, sleep disorders, atrophic processes of the vagina and lower urinary tract), the cause of which is a deficiency in the production of endogenous estrogens; prevention of recurrent infectious and inflammatory diseases of the vagina and lower urinary tract; prevention and treatment of postmenopausal osteoporosis.

ICD codes

Dosage Regimen

Establish the dosage individually based on the clinical indication and therapeutic goal.

For hormone replacement therapy in women with an intact uterus, administer one 2 mg tablet daily in a continuous regimen.

Always combine estradiol therapy with a progestogen for a minimum of 10 to 12 days per calendar month to mitigate the risk of endometrial hyperplasia.

Initiate treatment with the lowest effective dose for the shortest duration necessary to control symptoms.

Take tablets orally at approximately the same time each day, with or without food.

For women transitioning from another estradiol product, begin Estrofem^® at an equivalent therapeutic dose.

In cases of primary or secondary amenorrhea, follow a cyclic regimen, typically for the first 21 days of a 28-day cycle.

For the prevention of postmenopausal osteoporosis, ensure long-term, continuous administration and supplement with progestogen as required.

Regularly re-evaluate the need for continued therapy, at least on an annual basis.

Adverse Reactions

From the CNS: headache, dizziness, depression are possible.

From the digestive system: nausea, vomiting, cholestatic jaundice, impaired liver function, gallstone formation are possible.

From the endocrine system: uterine and vaginal bleeding, breast tension and enlargement, changes in libido, endometrial proliferation, development of endometrial carcinoma (in women with an intact uterus after menopause), edema, weight gain are possible.

Allergic reactions: urticaria, skin rash are possible.

Dermatological reactions: erythema multiforme, chloasma, melanoderma are possible.

Contraindications

Breast and endometrial cancer, uterine fibroids, endometriosis, uterine bleeding of unknown etiology; severe liver damage, severe cardiovascular diseases, collagenoses, porphyria, pituitary tumors, otosclerosis, thrombophlebitis, thromboembolism; history of hepatitis, jaundice, prolonged itching, herpes during previous pregnancy; pregnancy, lactation period (breastfeeding).

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

Contraindicated in severe liver damage, history of hepatitis, jaundice. Should be used with caution in patients with impaired liver function.

Use in Renal Impairment

Should be used with caution in patients with impaired renal function.

Special Precautions

Before starting treatment, a gynecological examination is necessary; with long-term therapy, it should be performed at least once a year.

Treatment with estradiol is advisable to combine with progestogenic drugs.

Should be used with caution in patients with coronary artery disease, circulatory insufficiency, migraine, bronchial asthma, epilepsy, severe arterial hypertension, impaired liver and/or kidney function.

Estradiol may cause an increase in existing uterine fibroids.

During the use of estradiol, liver function and blood pressure should be systematically monitored; in patients with diabetes mellitus, blood glucose concentration should be monitored.

Drug Interactions

With simultaneous use, estrogens may reduce the effects of anticoagulants, antihypertensive, and hypoglycemic drugs.

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

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

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.