2010/06/14

DANAZOL

Pharmacological action

Inhibition of production of gonadotropic hormones. It is a reversible suppression of the production of both LH and FSH pituitary gland in men and women. Do not have estrogen and gestagen activity. It has a weak androgenic activity with concomitant anabolic effect.

Inhibits proliferation and causes atrophy of normal and ectopic endometrial tissue.

It reduces menstrual blood loss, the mechanism of this action is not completely installed.

Inhibits ovulation and reduces the level of 17β-estradiol in the blood plasma. It remains unclear whether the inhibition of proliferation of the endometrium due to a decrease the level of estradiol or the direct influence of danazol on estrogen receptors in the endometrium.

After the abolition of danazol ovulation usually resumes within 5 weeks, accompanied by a characteristic sharp increase in LH and a slight increase in FSH.


Pharmacokinetics

After oral danazol absorbed from the gastrointestinal tract. Absorption increases while eating. Metabolised in the liver, the main metabolite is 2-gidroksimetiltestosteron. T 1 / 2 is about 4.5 hours


Statement

Endometriosis associated with infertility, benign tumors of the breast, primary menorrhagia, premenstrual syndrome, gynecomastia.


Dosage regimen

Dose, frequency and duration of treatment admission are determined individually. The maximum dose for adults - 800 mg / day.


Side effect

On the part of the endocrine system: amenorrhea, facial flush, increased perspiration, reducing the size of breasts, changes in libido, vaginitis, emotional lability, nervousness, acne, increased secretion of the sebaceous glands, slight hirsutism, edema, weight gain, deepening of the voice, androgenic alopecia, violations of spermatogenesis.

On the part of the digestive system: dysfunction of the digestive tract, increased liver enzymes; rarely - cholestatic jaundice.

From the side of the central nervous system: possible headache, dizziness, tremor, depression, fatigue, sleep disorders rarely - a small increase in intracranial pressure.

On the part of the hemopoietic system: an increase or decrease in the number of blood cells.

Dermatological reactions: skin rash.

On the part of metabolism: giperglyukagonemiya, violations of glucose tolerance, increased serum concentrations of LDL-cholesterol, reduce serum concentrations of HDL-cholesterol.

Since the cardiovascular system: rarely - tachycardia, hypertension.

Other: back pain, muscle spasms or cramps; rarely - visual impairment.


Contraindications

Severe liver dysfunction and / or kidneys, heart, porphyria, thromboembolic disorders (including history), androgenozavisimye tumors, vaginal bleeding of unknown origin, pregnancy, lactation.


Application of pregnancy and breastfeeding

Contraindicated during pregnancy and lactation.

In women of childbearing age before starting treatment danazol should be excluded pregnancy. Because danazol is not a contraceptive means in the period of treatment should use non-hormonal methods of contraception.


Cautions

With caution used in patients with liver, kidney, hypertension and other cardiovascular diseases, conditions that could worsen due to fluid retention (including diabetes, epilepsy, polycythemia, lipid metabolism).

Not recommended for use danazol in elderly patients and children.


Drug Interactions

Danazol inhibits the metabolism in the liver carbamazepine, cyclosporine.

Reported hypercalcemia caused by danazol, against the background of alfacalcidol in a patient with gipoparatireoidizmom.