Danazol (Danazolum)

Pharmacodynamics Pharmacokinetics Indications Carefully Contraindications Dosing and Administration Side effects
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Clinical and pharmacological group: & nbsp

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

Included in the formulation
  • Danol®
    capsules inwards 
    Sanofi-Synthelabo Co., Ltd.     United Kingdom
    • АТХ:

    G.03.X.A.01   Danazol

    Pharmacodynamics:

    Synthetic preparation of steroid structure, 17α-ethynyl-testosterone derivative, partial agonist gestagen (and also androgen and glucocorticoid) receptors. Actually, gestagenic activity is low, so the drug does not cause peripheral gestagenic effects. Penetrating through the blood-brain barrier, it stimulates the gestagen receptors of the hypothalamus and pituitary gland. This leads to suppression of the increment of gonadotropic releasing hormone and gonadotropic hormones in the anterior pituitary gland, which in turn leads to suppression of the secretion of sex hormones and a decrease in the proliferation of hormone-dependent tissues.

    Has an immunosuppressive effect due to suppression of lymphocyte proliferation in vitro.

    Pharmacokinetics:

    The half-life of 4.5-29 hours, biotransformation in the liver, excretion of the kidneys.

    Indications:

    - Gynecomastia;

    - Primary menorrhagia, premenstrual syndrome;

    - Endometriosis;

    - Benign neoplasm of the mammary glands;

    - Hereditary angioedema;

    - Premature puberty.

    ICD-10

    II.D10-D36.D24   Benign neoplasm of breast

    III.D80-D89.D84.1   Defect in the complement system

    IV.E20-E35.E30.1   Premature puberty

    XIV.N60-N64.N60.1   Diffuse cystic mastopathy

    XIV.N60-N64.N62   Hypertrophy of the breast

    XIV.N80-N98.N80   Endometriosis

    XIV.N80-N98.N92   Abundant, frequent and irregular menstruation

    XIV.N80-N98.N94.3   Premenstrual tension syndrome

    XIV.N80-N98.N97   Female infertility

    XIX.T66-T78.T78.3   Angioedema

    Contraindications:

    Porphyria, breast cancer, chronic kidney and / or liver disease, pregnancy, breast-feeding, hypersensitivity, thromboembolism, heart failure, prostate cancer, uterine bleeding.

    Carefully:

    Diabetes mellitus, age over 65, migraine, violation of plasma mechanisms of hemostasis, epilepsy.

    Pregnancy and lactation:

    Category FDA - X. The use during pregnancy causes androgenic effects in female embryos (pathology of the genitals, clitoris hypertrophy, fusion of the labia, atresia of the vagina). Do not apply! It is recommended to stop breastfeeding during treatment with danazol.

    Dosing and Administration:

    Inside, 2-4 times a day. Dose, the frequency of admission, as well as the duration of therapy is determined by the doctor. The maximum daily dose of the drug for adults is 800 mg per day.In menorrhagia, usually take 100-400 mg per day for 3 months, with endometriosis the first dose is 400 mg per day, then the dose can be raised to the maximum, the course is 6 months, with mastopathy - 300 mg dose per day, children with premature puberty dose is selected strictly individually, usually it is 100-400 mg.

    Side effects:

    From the gastrointestinal tract: hepatoadenoma, epigastric pain, cholestatic jaundice, liver function disorders, nausea, hepatitis.

    From the nervous system: lumbulgia, visual disturbances, sleep disorders, fainting, emotional lability, paresthesia, muscle spasm, nervousness, headache.

    From the endocrine system: increased sweating, flushing to the face, reducing the size of the mammary glands, tenderness of the mammary glands, amenorrhea, menstrual dysfunction, vaginal dryness, increased sweating.

    Others: androgen-like effects (weight gain, seborrhea, acne, minor hirsutism, swelling, alopecia, coarsening of the voice - can take the form of hoarseness, pharyngitis), changes in libido, leukocytosis, increased bleeding hazard in hemophilia patients, fever, glucose tolerance.

    Overdose:

    Tremor, convulsions, nausea, headache, vomiting, dizziness. Treatment is symptomatic.

    Interaction:

    When taken concomitantly with insulin danazol reduces its activity, so blood glucose level can increase due to changes in the metabolism of carbohydrates (you may need to adjust the dose of hypoglycemic agents and insulin).

    When combined with indirect anticoagulants, the effect of anticoagulants is increased (hepatic synthesis of procoagulant factors decreases, bleeding is possible).

    When used with carbamazepine, it is possible to inhibit carbamazepine metabolism, resulting in increased blood concentrations and toxicity.

    Danazol potentiates the action of antiepileptic drugs (phenytoin, phenobarbital).

    Special instructions:

    It is able to cause hypercalcemia when taking alfacalcidol with primary hypoparathyroidism.

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

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

    Impact on the ability to drive vehicles and mechanisms

    There have been no reports of a significant effect of danazol on the ability to drive and other mechanisms.

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