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Instructions

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Instruction for use: Danazol (Danazolum)

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Chemical name

(17alpha) -Pregna-2,4-dien-20-yno [2,3-d] isoxazol-17-ol

Pharmacological group

Hormones of the hypothalamus, pituitary gland, gonadotropins and their antagonists

Nosological classification (ICD-10)

D24 Benign neoplasm of breast

Benign neoplasm of mammary glands, Benign mammary gland disease, Neoplastic processes in the mammary gland, Tumors of the mammary glands, Papilloma of the ducts of the mammary gland

D84.1 Defect in the complement system

Hereditary angioedema

E30.1 Premature puberty

Premature puberty, Premature sexual development, Premature puberty in girls, Early puberty, Primary premature puberty

N60.1 Diffuse cystic mastopathy

Benign cystic change in mammary glands, Cystic fibrosis mastopathy, Fibrous-cystic mastopathy, Pre-cancerous condition of mammary glands, Benign mammary gland disease, Benign breast tumor

N62 Hypertrophy of the breast (breast) gland

Gynecomastia, Hypertrophy of the mammary glands, Macromastia

N80 Endometriosis

Endometrioid endometriosis

N92 Abundant, frequent and irregular menstruation

Metromenorragii, Menorrhagia, Menorrhagia primary, Polymenorea, Idiopathic menorrhagia, Menorrhagia, Functional metronormorragia, Primary menorrhagia

N94.3 Premenstrual tension syndrome

Pronounced premenstrual syndrome, Menstrual psychosomatic disorder, Menstrual syndrome, Premenstrual tension, Premenstrual status, Premenstrual period, Premenstrual syndrome, Menstruation syndrome

N97 Female infertility

Female infertility in anovulation, Hyperprolactinemic infertility, Hyperprolactinaemia with infertility, Endocrine infertility, Infertility due to hypothalamic-pituitary dysfunction, Infertility infertility, Infertility, Infertility on the background of hyperprolactinaemia, Functional infertility, Marriage is infertile, Infertility of ovarian genesis, Stimulation of the growth of a single follicle

T78.3 Angioedema

Edema Quincke, Laryngeal exacerbation with angioneurotic edema, Recurrent angioedema, Allergic edema, Recurrent swelling of Quincy

Code CAS17230-88-5

Characteristics

Synthetic androgen derived from ethidone.

White or pale yellow crystalline powder. Virtually nerastvorim in water, soluble in chloroform and acetone. It melts at a temperature of 225 C with a slight decomposition. Molecular weight 337.45.

Pharmacology

The pharmacological action is antigonadotropic.

Has a pronounced reversible (60-90 days after discontinuation) antigonadotropic action in combination with insignificant, in comparison with testosterone, androgenic and anabolic effects. Antigonadotropic effect is realized in several ways, including. By inhibiting the release of gonadotropin releasing hormone (GnRH), or suppressing the production of pituitary gland FSH and LH in men and women. In women, ovarian activity is inhibited, ovulation is inhibited. Danazol can directly inhibit steroidogenesis by interacting with androgenic, progesterone and glucocorticoid receptors in target tissues, by binding to a steroid-binding beta-globulin, increasing the metabolic clearance of progesterone.

It has an immunosuppressive effect and suppresses the proliferation of lymphocytes in vitro. Reduces the level of IgA, IgG and IgM, as well as the concentration of phospholipids and the production of autoantibodies in patients with endometriosis.

In the treatment of endometriosis, it damages both normal and ectopic endometrial tissue, leading to its inactivation and atrophy. Reduces pain syndrome, concomitant endometriosis, causes regressive changes in endometriotic foci.

Changes in cervical mucus and cytology of the vaginal smear when taking danazol reflect its overwhelming effect on the pituitary-ovarian system.

With fibrocystic mastopathy contributes to the partial or complete disappearance of nodular seals and complete relief of pain syndrome.

Clinical efficacy in hereditary angioedema may be due to an increase in the content of the inhibitor of esterase C1 (a congenital deficit of which is characteristic for this disease) and, as a result, an increase in the plasma level of the C4 complement component.

After oral administration, danazol is rapidly and extensively metabolized. Eating (fat more than 30 g) delays absorption for 30 minutes, increases bioavailability and Cmax. Bioavailability does not increase in proportion to the dose increase: when the dose is doubled, the plasma concentration rises by 35-40%. Cmax in plasma is achieved within 2-8 hours. When taking 100 mg twice a day, Cmax is 200-800 ng / ml, 200 mg twice a day for 2 weeks - 250 ng / ml-2 μg / ml . Biotransformiruetsya in the liver with the formation of the main metabolites - etisterone and 17-hydroxymethylethylidone. T1 / 2 danazol is variable and can range from 4.5 to 29 hours. It is excreted by the kidneys.

Indications

Endometriosis with concomitant infertility, benign neoplasms of the mammary gland (including fibrocystic mastopathy), primary menorrhagia, premenstrual syndrome, primary premature puberty, gynecomastia. Prevention of all types (cutaneous, abdominal, laryngeal) exacerbations with hereditary angioedema.

Contraindications

Hypersensitivity, porphyria (possibly exacerbation of the disease), breast cancer, androgen-dependent tumors, incl. Prostate cancer, thromboembolism, genital bleeding (to clarify their cause), moderate or severe renal and / or hepatic insufficiency, severe heart failure, pregnancy, breast-feeding.

Restrictions of use

Diabetes mellitus, epilepsy, migraine, violation of plasma mechanisms of hemostasis, old age.

pregnancy and lactation

In studies in pregnant rats, oral administration of danazol at doses up to 250 mg / kg / day (7-15 MPhR) from 6 to 15 days of pregnancy showed no embryotoxicity and teratogenicity, differences in the size of the offspring, viability, body weight of the offspring In comparison with the control. However, in studies in rabbits with oral doses of 60 mg / kg / day (2-4 MPhR) from the 6th to the 18th day of pregnancy, the development of fetuses was delayed.

Contraindicated in pregnancy. The effect of danazol in utero can lead to adverse androgenic effects in female fetuses.

The action category for fetus by FDA is X.

During breastfeeding, use is usually not recommended, because Possible androgenic effects in the child - such as premature puberty in boys, virilization in girls.

Side effects

From the nervous system and sensory organs: dizziness, fainting, emotional lability, nervousness, muscle spasm, headache, increased intracranial pressure, lumbalgia, paresthesia, sleep disorders, visual disturbances.

On the part of the intestinal tract: nausea, liver dysfunction, reversible increase in liver transaminase activity, hepatitis, epigastric pain, cholestatic jaundice, hepatoadenoma.

From the endocrine system: violations of menstrual function, incl. Irregular menstrual periods, amenorrhea; Symptoms that indicate a decrease in the level of estrogen - flushes to the face, excessive sweating, vaginal dryness, painful sensitivity and a decrease in the size of the mammary glands.

Allergic reactions: urticaria, pruritus, exfoliative dermatitis; Rarely - stuffy nose; Sometimes - a rash (maculopapular, vesicular, papular), petechiae.

Other: androgen-like effects, incl. Weight gain, seborrhea, acne, minor hirsutism, swelling, alopecia, coarsening of the voice (may take the form of hoarseness), pharyngitis - may continue after discontinuation of therapy; Rarely - clitoral hypertrophy. Moderate impairment of spermatogenesis in men, abnormalities in laboratory tests (including creatine phosphokinase level, glucose tolerance, steroid-binding globulin level), fever, low back pain, change in libido, thrombocytosis or thrombocytopenia, erythrocytosis, leukocytosis, increased bleeding risk in patients With hemophilia.

Interaction

When combined with coumarinic anticoagulants and indanedione derivatives, the effect of anticoagulants may be enhanced (hepatic synthesis of procoagulant factors decreases, bleeding is possible). Danazol can increase blood glucose levels and insulin resistance due to changes in the metabolism of carbohydrates (you may need to adjust the dose of hypoglycemic agents and insulin). When used with carbamazepine, the inhibition of carbamazepine metabolism is possible, leading to increased concentrations in the blood and toxicity. Danazol can increase the concentration in the blood of cyclosporine and tacrolimus (risk of nephrotoxicity), glucagon.

Overdose

Symptoms: headache, dizziness, tremors, convulsions, nausea, vomiting.

Treatment: gastric lavage, symptomatic therapy.

Routes of administration

Inside.

Precautions

Periodically monitor the level of hepatic transaminases and bilirubin in the blood serum.

At the onset of pregnancy during treatment with danazol, it is necessary to cancel the drug and warn the patient about the possible risk to the fetus. During treatment it is recommended to use nonhormonal methods of contraception.

When appointing patients with diabetes it is necessary to adjust the dose of insulin.

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