Clomifene (Tablets) Instructions for Use

Marketing Authorization Holder

Mir-Pharm, LLC (Russia)

Manufactured By

OHFK, JSC (Russia)

ATC Code

G03GB02 (Clomifene)

Active Substance

Clomifene (Rec.INN registered by WHO)

Dosage Form

Clomifene

Tablets 50 mg: 10, 20, 30, 40, or 100 pcs.

Dosage Form, Packaging, and Composition

10 pcs. – dark glass jars (1) – cardboard packs.
10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (4) – cardboard packs.
10 pcs. – contour cell packs (10) – cardboard packs.

Clinical-Pharmacological Group

Gonadotropin production stimulant

Pharmacotherapeutic Group

Anti-estrogen

Pharmacological Action

Stimulator of gonadotropin production. An agent with anti-estrogenic and estrogenic activity. It has a non-steroidal structure that is close to chlorotrianisene.

It is believed that the action of clomifene is due to specific binding with estrogen receptors of the hypothalamus and pituitary gland, which increases the secretion of pituitary gonadotropic hormones.

This in turn stimulates the maturation and endocrine activity of the follicle in the ovary, as well as the subsequent formation and stimulation of the corpus luteum function.

In high doses, it inhibits the secretion of gonadotropins. It does not possess progestogenic or androgenic activity.

Pharmacokinetics

When taken orally, it is well absorbed from the gastrointestinal tract. It is metabolized in the liver. Undergoes enterohepatic recirculation.

The T_1/2 is 5-7 days. It is excreted mainly with bile.

Indications

Anovulatory infertility (induction of ovulation); amenorrhea (dysgonadotropic form), secondary amenorrhea, postcontraceptive amenorrhea; Stein-Leventhal syndrome (polycystic ovary syndrome); oligomenorrhea; galactorrhea (against the background of a pituitary tumor); Chiari-Frommel syndrome (syndrome of prolonged postpartum amenorrhea-galactorrhea); androgen deficiency; in men – oligospermia.

ICD codes

Dosage Regimen

Administer orally as a single daily dose.

Initiate therapy at a dose of 50 mg (one tablet) daily for five days.

Start treatment on or about the fifth day of the menstrual cycle following spontaneous or induced bleeding.

If ovulation occurs without conception, repeat this 50 mg five-day course for at least three more cycles.

If ovulation does not occur, increase the dose to 100 mg daily for five days in the next cycle.

This course may be repeated, starting on or about the fifth day of the subsequent cycle.

Do not exceed a single daily dose of 100 mg.

Do not continue treatment for more than six cycles.

For the management of male infertility due to oligospermia, the typical dose is 50 mg once daily.

Alternatively, a regimen of 25 mg daily for 25 days, followed by a five-day rest period, may be used.

Continue treatment for a minimum of six months in male patients.

Discontinue therapy immediately if ovarian hyperstimulation or visual disturbances occur.

Perform regular gynecological examinations, including ovarian ultrasound, to monitor response and detect complications.

Adverse Reactions

From the digestive system nausea, vomiting; rarely – gastralgia, flatulence, diarrhea, acute abdomen syndrome.

From the nervous system headache, dizziness, drowsiness; rarely – slowing of mental and motor reactions, increased excitability, depression, insomnia.

From the organ of vision impaired light perception, double vision, blurred contours, photophobia.

From the urinary system frequent urination; rarely – polyuria.

From the reproductive system and mammary glands breast induration, lower abdominal pain, dysmenorrhea, pathological uterine bleeding, ovarian enlargement (including cystic); rarely – vaginal dryness, menorrhagia.

Allergic reactions rarely – rash, urticaria, allergic dermatitis, vasomotor disorders.

Other rarely – increased appetite, increase or decrease in body weight, alopecia, soreness in the breast area, hot flashes.

Contraindications

Hypersensitivity to clomifene; hepatic and/or renal failure; pregnancy, lactation period (breastfeeding); ovarian cysts (except for polycystic ovary syndrome); pituitary tumor or hypofunction; thyroid or adrenal dysfunction; metrorrhagia of unclear etiology; long-standing or recently developed visual disturbances; neoplasms of the genital organs; endometriosis; ovarian insufficiency against the background of hyperprolactinemia.

Use in Pregnancy and Lactation

Contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

Contraindicated for use in hepatic failure.

Use in Renal Impairment

Contraindicated for use in renal failure.

Special Precautions

It is recommended to check liver function before starting the use of clomifene.

Before using clomifene, a thorough gynecological examination must be performed. The use of clomifene is indicated in cases where the total level of gonadotropin in the urine is below the lower limit of normal or at the normal level, palpation of the ovaries does not reveal deviations from the norm, and the functions of the thyroid gland and adrenal glands are normal.

In the absence of egg maturation, all other possible causes of infertility should be excluded or treated before using clomifene. If ovarian enlargement or their cystic transformation is detected, the use of clomifene is not allowed until the ovaries return to normal size. Subsequently, the dose or duration of treatment should be reduced.

During treatment, constant supervision by a gynecologist is necessary, ovarian function should be monitored, vaginal examinations should be performed, and the “pupil” phenomenon should be observed. Often during the course of treatment, it is difficult to determine the moment of ovulation, and corpus luteum insufficiency is often observed. Therefore, after conception, it is recommended to start prophylactic administration of progesterone.

When treated with clomifene, the likelihood of multiple pregnancy, ectopic pregnancy, endometriosis, and growth of an existing uterine fibroid increases.

Hot flashes observed during the course of treatment stop after the end of clomifene intake. Cystic enlargement of the ovaries may also be observed, especially in Stein-Leventhal syndrome. In these cases, the size of the ovaries can reach 4-8 cm. In this case, body temperature should be monitored and treatment should be stopped as soon as it becomes biphasic.

Effect on ability to drive vehicles and mechanisms

During the treatment period, caution must be exercised when driving vehicles and engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Drug Interactions

Compatible with gonadotropic hormone preparations.

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.