Instruction for use: Tibolone (Tibolonum)

Pharmacological group

Estrogens, gestagens; Their homologues and antagonists

Antineoplastic hormonal agents and hormone antagonists

Nosological classification (ICD-10)

M82.1 Osteoporosis in endocrine disorders (E00-E34 +)

N95.1 menopausal and menopausal status of women

Atrophy of the mucosa of the lower genital tract, caused by estrogen deficiency; Vaginal dryness; Autonomic dysfunction in women; gipoestrogeniya state; Deficiency of estrogen in menopausal women; Degenerative changes of the mucous membrane in the menopause; Natural menopause; an intact uterus; climacteric; Menopause women; Menopause in women; menopausal depression; Climacteric ovarian dysfunction; Menopause; Climacteric neurosis; Menopause; Menopausal symptoms complicated psychovegetative; Climacteric syndrome; Climacteric vegetative disorders; Climacteric psychosomatic disorder; menopausal disorders; Menopausal disorders in women; menopausal condition; Climacteric vascular disorders; Menopause; Menopausal vasomotor symptoms; menopausal period; Lack of estrogen; Feeling the heat; Pathological menopause; perimenopause; menopause; postmenopausal; Premature menopause; premenopauznom period; tides; hot flashes; flushing in the Meno and postmenopausal; Hot flashes / hot flashes in menopause; Heart attack during menopause; Early menopause in women; Disorders of menopause; climacteric syndrome; Vascular complications of menopause; Physiological menopause; Estrogendefitsitnye state; premature Menopause

Code CAS5630-53-5

Pharmacology

The pharmacological action is estrogen-gestagenic.

It also has weakly expressed androgenic and anabolic activity. It alleviates climacteric changes in the hypothalamic-pituitary system. Reduces the level of FSH and LH in women in menopause. In fertile women suppresses ovulation.

Has a stimulating effect on the mucous membrane of the vagina. Prevents osteoporosis, reduces the level of phosphates and calcium in the blood serum. Reduces the severity of climacteric autonomic dysfunction (hot flashes, increased sweating, headaches), improves libido and psycho-emotional state (increases the level of central and peripheral opioids).

After oral administration, it is quickly and completely absorbed from the digestive tract. Biotransformed with the formation of three pharmacologically active metabolites: 3-alpha-OH-tibolone and 3-beta-OH-tibolone have predominantly estrogenic activity, delta-4-isomer tibolone has progestagenic and weak androgenic activity. Cmax 3-alpha-OH- and 3-beta-OH metabolites are reached after 1-1.5 h, T1 / 2 - about 7 h, do not accumulate. It is excreted mainly in the form of metabolites, mainly with feces, a small amount - with urine.

Application of Tibolone

Menopause (natural and surgical), osteoporosis with estrogen insufficiency (prophylaxis).

Contraindications

Hypersensitivity, hormone-dependent tumors (or suspicion of them), vaginal bleeding of unclear etiology, thrombophlebitis and thromboembolism (including in history), severe violations of the liver, cardiovascular insufficiency, cerebrovascular disorders; Otosclerosis, which occurred during pregnancy or when treated with steroids; In the period less than 1 year after the last menstruation, untreated endometrial hyperplasia, porphyria, pregnancy, breast-feeding.

Restrictions for use

Leiomyoma, endometriosis, endometrial hyperplasia in the anamnesis, renal insufficiency, violation of carbohydrate metabolism, hypercholesterolemia, epilepsy, migraine or severe headaches, systemic lupus erythematosus, bronchial asthma.

pregnancy and lactation

Use during pregnancy is contraindicated. In case of pregnancy during treatment, treatment should be stopped immediately.

Use during breastfeeding is not recommended.

Side effects

From the nervous system and sensory organs: headache, dizziness, blurred vision, depression.

On the part of the digestive tract (gastrointestinal tract): nausea, diarrhea, increased activity of hepatic transaminases.

From the genitourinary system: metrorrhagia, proliferation of the endometrium.

Other: swelling of the legs, pain in the back, hands and feet, weight change, increased hair growth on the face, itching, rash, seborrheic dermatitis.

Interaction

Strengthens the effect of anticoagulants, increases the need for hypoglycemic agents (reduces glucose tolerance). Activity decreases with simultaneous use of rifampicin, carbamazepine.

Overdose

Symptoms: a violation of the function of the gastrointestinal tract (gastrointestinal tract).

Treatment: symptomatic.

Routes of administration

Inside.

Precautions

Do not take the drug in the period before the expiration of 12 months after the last natural menstruation. If the drug is taken before the specified time, the probability of irregular bloody discharge / bleeding from the vagina increases.

Regular monitoring of appropriate laboratory parameters in patients with hypercholesterolemia, renal dysfunction and diabetes mellitus is necessary. It should be borne in mind that against the background of tibolone, a decrease in the levels of total and free thyroxin and thyroxin-binding globulin is possible.

When symptoms of thromboembolism, jaundice or persistent pathological changes in functional hepatic tests appear, treatment is discontinued.