2010/06/14

DANOL

Pharmacological properties: danazol (17-b-pregna-2 ,4-dien-20-foreign-[2,3-d]-isoxazole-17-ol) has a pronounced affinity for the androgen receptor, less pronounced affinity for progesterone receptors and the minimum affinity for estrogen receptors.

Danazol is a weak androgen, marked by its anti-androgenic, progestogens, antiprogestogennye, estrogens and antiestrogens properties. It prevents the synthesis of sex hormones, possibly through the suppression of an enzyme cleaving the side chain of cholesterol, and other enzymes of steroidogenesis. Danazol can also suppress the accumulation of cAMP in the cells of the corpus luteum in response to gonadotropic hormones.

Danazol can reduce the average concentration in plasma FSH and LH after menopause.

Danazol affects the plasma proteins: increased level of prothrombin, plasminogen, antithrombin III, alpha 2-macroglobulin, an inhibitor of C 1-esterase and erythropoietin, and reduces levels of fibrinogen, globulin, binding thyroid hormones and sex hormones. Danazol increases the concentration of free testosterone in blood plasma.

The overwhelming effect of danazol on the hypothalamic-pituitary-gonadal axis is reversible, cyclic activity is restored within 60-90 days after completion of treatment.

After oral absorption of healthy older women danazol dose-dependent manner, has an almost linear fashion at the reception of repeated doses of 100-400 mg twice a day. Suction danazol affects food intake, absorption of the drug increases about 2 times when you receive it directly after a meal compared with the reception for 2 hours before meals.

The main metabolites of danazol, apparently, are ethisterone and 17-gidroksimetiletisteron. The average half-life of danazol is about 24 hours

INDICATIONS:

Endometriosis - to reduce the severity of symptoms associated with endometriosis and / or suspension or reduction of the spread of endometriosis. Dunawley can be used in combination with surgery or as a hormone monotherapy in patients in whom other treatment is ineffective.

Benign fibrocystic disease of the breast - symptomatic used to reduce the severity of pain and sensitivity. Dunawley should be used only in patients in whom other therapeutic measures are ineffective or not recommended.

Angioedema.

APPLICATION: inside. The treatment Dunawley begin during menstruation. Throughout the course of treatment should be applied effective non-hormonal method of contraception. The drug is used in the lowest effective dose.

The recommended dose of endometriosis is 200-800 mg per day, course of treatment - 3-6 months.

In benign fibrocystic disease of the breast (including cyclical mastalgia) the recommended dose is usually 100-400 mg / day course of treatment - 3-6 months.

Hereditary angioedema. The recommended starting dose is 200 mg 2-3 times a day. Upon reaching a satisfactory result of the transition to the lowest effective dose for the continuous supports the prophylactic use of the drug.

Contraindications: pregnant and breast-feeding, elderly and children's age, marked disturbances of liver function, kidney or heart failure, porphyria, androgen tumor, abnormal genital bleeding of unknown origin, acute thrombosis and thromboembolism, as well as references to them in history.

SIDE EFFECTS: Androgenic effects - acne, weight gain, increased appetite, seborrhea, hirsutism, hair loss, changes in voice, rarely - hypertrophy of the clitoris, water retention, menstrual cycle, intermenstrual bleeding, amenorrhea, hot flashes, dryness and irritation mucosa of the vagina, the change of sexual attraction, and in some cases - reducing the size of breasts, increased resistance to insulin, glucagon levels in blood plasma and glucose intolerance, in some cases - raising the level of LDL cholesterol, lowering HDL, lower apolipoprotein AI and AII, induction of aminolevulinic acid synthetase (ALA) and a decrease of binding globulin to T 4 thyroid gland with increased seizure of T 3, but unchanged from tireoidstimuliruyuschego hormone or free tiroksinovogo index; rash (Makulo-papular, petechial or purpura), which may accompanied by fever, swelling of the face and photosensitivity, rare - rash, very rarely - nodular erythema, changes in skin pigmentation, exfoliative dermatitis and polymorphous erythema; back pain, muscle cramps, sometimes - with higher levels of CK, tremor, fastsikulyatsiya, pain in the limbs, arthralgia and swelling in joints, hypertension, palpitations, tachycardia, thrombosis, including sagittal sinus thrombosis and cerebrovascular thrombosis, peripheral arterial disease, in some cases - myocardial infarction; rare - visual impairment, difficulty in focusing the image, discomfort with the use of contact lenses and a violation of refraction, requiring correction, emotional imbalance, anxiety, depressed mood, irritability, headache, rare - dizziness, benign intracranial hypertension, is very rare - the worsening of the epilepsy, migraine provoking, often - increasing the number of red blood cells and platelets, polycythemia, leukopenia and thrombocytopenia, a rarely - eosinophilia, in some cases can be observed an isolated increase in transaminase activity in serum, cholestatic jaundice, benign adenoma of the liver, pancreatitis, and very rarely (if long-term use) - malignant tumor of the liver, nausea, rarely - fatigue, very rarely - hematuria (long-term use of the drug in case of angioedema), pain in the epigastric region and in the chest, carpal tunnel syndrome, interstitial pneumonitis.

Cautions: Dunawley want to cancel, if noted such side effects: virilization (continued taking the drug in this case increases the risk of irreversible changes), papilledema, headache, blurred vision or other signs or symptoms of increased intracranial pressure, jaundice or other signs of liver failure, thrombosis or thromboembolism.

If necessary, repeat treatment should be careful, because the data regarding the safety of repeated courses of treatment available. Prolonged use of 17-alkylated steroids may develop benign hepatic adenoma, and carcinoma of the liver pelioz that should be taken into account when long-term use, as Dunawley close in chemical structure to these compounds.

Preliminary results of epidemiological studies indicate that the use of Dunawley may increase the risk of ovarian cancer patients who received treatment for endometriosis.

Particular caution should be exercised when applying Dunawley in patients with kidney or liver disease, hypertension or other diseases of the cardiovascular system, any disease that may progress with fluid retention in the body, diabetes mellitus, polycythemia, epilepsy, abnormal balance of lipoproteins, expressed or stable androgen responses to the previously applied gonadotherapy; migraine.

It is recommended that careful clinical monitoring for all patients receiving Dunawley. With long-term treatment (more than 6 months) or repeated courses of treatment recommended 2 times a year liver ultrasound, laboratory monitoring of liver function and hematological status.

Before treatment Dunawley necessary (at least) to conduct a thorough clinical examination to exclude the presence of hormone carcinoma. The survey is conducted, if at the time of treatment nodules in the mammary gland does not disappear or increase.

Dunawley contraindicated during pregnancy because of the risk of virilization female fetuses, so women of reproductive age before starting treatment to exclude pregnancy. If pregnancy occurred during treatment Dunawley, the drug should be abolished. Dunawley can have androgenic effects on children who are breastfed, so it is necessary to interrupt treatment Dunawley or refuse to breastfeed.

The drug can affect the results of determining the level of testosterone or proteins in blood plasma.

INTERACTION: Dunawley may raise carbamazepine in plasma and affect the patient's reaction to the use of this drug, and phenytoin. Such interaction is possible and with phenobarbital.

Dunawley can cause resistance to insulin, to potentiate the action of warfarin, reduce the effectiveness of antihypertensive agents, raise the level of cyclosporine and tacrolimus in the blood plasma, increasing the nephrotoxicity of these drugs interact with sex hormones, increase kaltsiemichesky response to the use of alfacalcidol in the primary gipoparatireoidizme.

OVERDOSE: available data suggest that acute overdose of the drug is not a matter of serious immediate reactions. Despite this, should take measures to reduce the absorption of the drug (gastric lavage, the use of activated charcoal), and the patient must be under medical observation in case of delayed reactions.

Storage: Store in a dry place below 25 ° C.