Composition, form of production and packaging
Capsules hard gelatinous, opaque, size 3, with white body and gray lid, body and lid marked "DANOL 100"; the contents of the capsules are white or almost white powder, practically odorless.
1 caps.
danazol (micronized) 100 mg
Excipients: corn starch, lactose monohydrate, talc, magnesium stearate.
The composition of the capsule body: gelatin, titanium dioxide (E171).
Composition of capsule capsule: gelatin, titanium dioxide (E171), ferric oxide black oxide (E172).
Ink composition: Opacode S-1-8100HV Black 1007 (shellac, soy lecithin, dimethylpolysiloxane, ferric oxide black oxide (E172)).
10 pieces. - blisters (6) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
Capsules hard gelatinous, opaque, size No. 1, with a white body and brownish-pink lid, the body and the lid are marked "DANOL 200"; the contents of the capsules are white or almost white powder, practically odorless.
1 caps.
danazol (micronized) 200 mg
Excipients: corn starch, lactose monohydrate, talc, magnesium stearate.
The composition of the capsule body: gelatin, titanium dioxide (E171).
Composition of capsule capsule: gelatin, titanium dioxide (E171), iron oxide red (E172), iron oxide yellow (E172).
Ink composition: Opacode S-1-8100HV Black 1007 (shellac, soy lecithin, dimethylpolysiloxane, ferric oxide black oxide (E172)).
10 pieces. - blisters (6) - packs of cardboard.
10 pieces. - blisters (10) - packs of cardboard.
INSTRUCTION FOR THE SPECIALIST.
The product description was approved by the manufacturer for the 2009 print edition.
PHARMACHOLOGIC EFFECT
Antigonadotropnoe means, which is a synthetic androgen, obtained from etisterona. Suppresses the production of pituitary gonadotrophic hormones LH and FSH in men and women. Women are depressed by ovarian activity, inhibits ovulation, causes endometrial atrophy. The effect is reversible, the drug is deprived of estrogenic or gestagenic action, has a high and low dose of androgenic activity with concomitant anabolic effect.
When endometriosis damages both normal and ectopic endometrial tissue, leading to its inactivation and atrophy. Reduces pain syndrome, concomitant endometriosis, causes regressive changes in endometriotic foci. It has an immunosuppressive effect and inhibits the proliferation of lymphocytes in vitro. Significantly reduces the level of immunoglobulins (Ig) and the production of autoantibodies in patients with endometriosis. 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 (congenital deficiency of which is characteristic for this disease) and, as a result, an increase in the plasma level of the C4 complement component.
PHARMACOKINETICS
Eating (fat more than 30 g) delays absorption for 30 minutes, increases bioavailability and C max . With the appointment of 100 mg 2 times / day C max - 200-800 ng / ml, 200 mg 2 times / day for 2 weeks - 250 ng / ml-2 mcg / ml.
Metabolized in the liver with the formation of etisterone and 17-hydroxymethylethylidone.
T 1/2 - up to 24 hours. Bioavailability does not increase in proportion to the increase in dose. When the dose is doubled, the plasma concentration rises by 35-40%.
INDICATIONS
- endometriosis with concomitant infertility;
- Benign neoplasms of the mammary gland (fibrocystic mastopathy);
- primary menorrhagia and premenstrual syndrome, premature puberty, gynecomastia;
hereditary angioedema.
DOSING MODE
Inside. As a rule, the lowest effective doses are used.
Adults: Usually the daily dose is from 200 to 800 mg, it is divided into 2-4 admission.
Treatment of endometriosis should begin at a dose of 400 mg / day. This dose, if necessary, is increased or decreased. The duration of treatment is 4-6 months.
For the treatment of benign breast diseases or severe cyclic mastalgia, the recommended daily dose is 100 to 400 mg (usually 300 mg), for 3-6 months.
The dose for primary menorrhagia and premenstrual syndrome is 100-400 mg / day (usually 200 mg), for 3 months.
With gynecomastia, men are prescribed 200-600 mg (usually 400 mg) of the drug / day (no more than 6 months).
To prevent angioedema, the initial dose should be 200 mg, followed by a decrease (in the absence of exacerbations) within 1-3 months.
Children: can be prescribed only to children with premature puberty in a daily dose of 100 to 400 mg, depending on the age and severity of the disease.
SIDE EFFECT
On the part of the endocrine system: acne, swelling, hypersecretion of the sebaceous glands, hirsutism, virile syndrome, reduction in the size of the mammary glands, coarsening of the voice, weight gain, hair loss (alopecia), spermatogenesis, "tides" of blood to the skin of the face, profuse sweat, increased sweating, increased nervous excitability, emotional lability, changes in libido, migraine headache, menstrual irregularities, dysmenorrhea, lack of menstruation, vaginitis.
On the part of the hematopoiesis system: leukocytosis, increase in the number of erythrocytes or platelets, leukopenia or thrombocytopenia.
From the coagulation system of blood: quotas in patients with hemophilia.
From the cardiovascular system: worsening of the course of arterial hypertension, tachycardia.
From the side of the central nervous system: increased intracranial pressure.
From the digestive system: increased activity of liver enzymes, rarely cholestasis or cholestatic jaundice, hepatitis, nausea, increased insulin requirements, hypoglycemia, increased activity of creatine kinase, dyslipidemia.
Rarely: visual impairment, nausea, increased appetite, spasm of skeletal muscles, lumbulgia, paresthesia, skin rashes, photosensitivity, dizziness, fatigue, sleep disorders, depressive conditions and weighting of epilepsy, fluid retention.
CONTRAINDICATIONS
- pregnancy, the period of breastfeeding,
- porphyria;
- mammary cancer;
- carcinoma;
- androgen-dependent tumors;
bleeding from the vagina of unknown origin;
- Hepatic and / or renal insufficiency;
- Chronic heart failure;
- thromboembolism;
- hypersensitivity to danazol or any other ingredients of the drug.
With caution: epilepsy, migraine, diabetes, violation of plasma mechanisms of hemostasis.
PREGNANCY AND LACTATION
During pregnancy and lactation, danazol is contraindicated, may cause virilization of female fetuses.
Pregnancy should be ruled out before starting therapy with the drug. If a woman becomes pregnant during treatment, danazol treatment should be discontinued, and the patient is informed of the potential risk to the fetus.
APPLICATION FOR FUNCTIONS OF THE LIVER
Contraindication: renal failure.
APPLICATION FOR VIOLATIONS OF THE FUNCTION OF KIDNEYS
Contraindication: liver failure.
APPLICATION FOR CHILDREN
Children: may be prescribed only to children with premature puberty at a daily dose of 100 to 400 mg, depending on the age and severity of the disease.
SPECIAL INSTRUCTIONS
Treatment with danazol requires careful monitoring of patients, especially if they have liver and kidney disease, hypertension and / or other cardiovascular diseases, conditions accompanied by fluid retention, epilepsy, impaired lipoprotein metabolism, thrombosis (also in history) and migraine.
All patients receiving danazol require regular examination of liver function, including liver enzymes and the number of peripheral blood cells. With prolonged treatment (6 months) and repeated courses of treatment, an ultrasound examination of the pelvic and liver organs is recommended (at least 2 times per year). Caution is necessary when used in patients with a previous androgenic reaction to sex hormone therapy. Danazol affects some laboratory parameters of sex hormones (for example, increases the level of testosterone).
When appointing patients with diabetes it is necessary to correct the dose of insulin. The appointment of high doses of danazol prevents ovulation. However, ovulation is possible at low doses, so non-hormonal contraceptive methods should be used during treatment with danazol.
Due to the possible androgenic effect on the fetus, danazol should not be administered during pregnancy, so treatment in all cases should begin, with the exception of pregnancy, on the first day of menstruation. In patients with amenorrhea, a pregnancy test should be performed before starting therapy.
Impact on the ability to drive vehicles and manage mechanisms
Data is not available.
OVERDOSE
Symptoms: headache, dizziness, tremor, convulsions, nausea, vomiting.
Treatment: removal of the drug from the gastrointestinal tract with the help of artificially induced vomiting or gastric lavage, symptomatic therapy. Dynamic observation.
DRUG INTERACTION
Danazol enhances the effect of anticoagulants coumarinic series and derivatives of indandion (increases the risk of bleeding).
Weakens the action of insulin and oral hypoglycemic drugs (affecting carbohydrate metabolism, increases the concentration of glucose in the blood).
Increases the concentration of glucagon in the blood plasma.
Danazol can reduce the effectiveness of antihypertensive drugs, possibly by stimulating fluid retention in the body.
Suppresses the metabolism of antiepileptic drugs (carbamazepine, phenytoin and phenobarbital) and increases their concentration in the blood.
Increases the concentration in the blood plasma of cyclosporine and tacrolimus (the risk of nephrotoxicity increases).
Danazol may increase the calcium response to alpha-calcidol in primary hypoparathyroidism, which requires a reduction in the dose of this drug.
TERMS OF RELEASE FROM PHARMACY
On prescription.
TERMS AND CONDITIONS OF STORAGE
List B. In a dry place at a temperature of no higher than 25 В° C. Keep out of the reach of children. Shelf life - 5 years.
