of gonadotropin secretion inhibitor.
Pharmacological properties Pharmacodynamics antigonadotropnym agent is a synthetic androgen derived from ethisterone. It inhibits production of pituitary gonadotropins LH and FSH levels in men and women. In women, ovarian activity inhibits, inhibits ovulation, causes atrophy of the endometrium. Action reversible, the drug is devoid of estrogen or progestin action in high doses has a weak androgenic activity with concomitant anabolic effect. In endometriosis affects both normal and ectopic endometrial tissue, leading to its inactivation and atrophy. Reduces pain, associated endometriosis causes regressive changes of endometrial lesions. It has immunosuppressive effect and suppresses lymphocyte proliferation in vitro. Significantly reduces the level of immunoglobulin (Ig) and production of autoantibodies in patients with endometriosis. With fibrocystic breast promotes partial or complete disappearance of nodular seals and complete relief of pain.Clinical efficacy in hereditary angioedema, possibly due to an increase in the content of inhibitor of esterase C1 (congenital deficiency of which is characteristic of the disease), and, as a result, an increase in plasma levels of C4 component of complement. Pharmacokinetics Eating (fat 30 g) delays absorption by 30 min increases Cmax and bioavailability. When assigning 100 mg 2 times daily Cmax – 200-800 ng / ml, 200 mg 2 times a day for 2 weeks – 250 ng / ml 2 ug / ml. It is metabolized in the liver to form ethisterone and 17 gidroksimetiletisterona. T1 / 2 -. The bioavailability of up to 24 hours does not increase in proportion to the increase in dose. By doubling the dose plasma concentration increases by 35-40%.
Endometriosis with concomitant infertility; benign neoplasm of breast (fibrocystic breast disease); primary menorrhagia and premenstrual syndrome, precocious puberty, gynecomastia; hereditary angioedema.
: Hypersensitivity to Sustanon 350 or any other ingredients of the drug, pregnancy, lactation, porphyria, breast cancer, cancer, androgen tumor, vaginal bleeding of unknown origin, hepatic and / or renal failure, chronic heart failure, thromboembolism.
Be wary .
Epilepsy, migraine, diabetes mellitus, disturbance of plasma haemostatic mechanisms.
Pregnancy and lactation .
During pregnancy and lactation is contraindicated the use of Sustanon 350 may cause virilization of female fetuses.
Pregnancy must be excluded before the start of drug therapy. If a woman becomes pregnant during treatment, medication Sustanon 350 should be stopped and the patient informed of the potential risk to the fetus.
Dosing and Administration
Inside. Typically used lowest effective dose. Adults: usual daily dose is from 200 to 800 mg, it is divided into 2 – 4 doses. Endometriosis treatment should begin with a dose of 400 mg per day. This dose is, by necessity, increases or decreases. The duration of treatment is 4-6 months. Breast or severe cyclical mastalgia recommended daily dose for the treatment of benign diseases of from 100 to 400 mg (usually 300 mg) for 3-6 months. The dose primary menorrhagia and premenstrual syndrome is 100 – . 400 mg per day (usually 200 mg) for 3 months at gynecomastia men administered 200 – 600 mg (usually 400 mg) of the drug per day (no more than 6 months). initial dose to prevent angioedema should be 200 mg followed by reduction (in the absence of exacerbations) during 1-3 months. Children: may be assigned only for children with precocious puberty in a daily dose of 100 to 400 mg depending on the age and severity of disease.
Side effects of
acne, swelling, hypersecretion of the sebaceous glands, hirsutism, virility syndrome, decrease in breast size, deepening of voice, weight gain, hair loss (alopecia), disruption of spermatogenesis, “tides” of blood to the skin of the face, profuse sweating, increased sweating, increased nervous irritability, emotional instability, changes in libido, migrenepodobnaya headache, menstrual disorders, dysmenorrhea, absence of menstruation, vaginitis. Leukocytosis, increase in the number of red blood cells or platelets, leukopenia or thrombocytopenia. Bleeding in patients with hemophilia. The worsening of arterial hypertension, tachycardia. Increased intracranial pressure. The increased activity of “liver” enzymes, rarely cholestasis or cholestatic jaundice, hepatitis, nausea, increased requirements for insulin, hypoglycemia, increased creatine kinase activity, dyslipidemia.
Rare: blurred vision, nausea, increased appetite, spasm of skeletal muscles, lumbodynia, paresthesia, rash , photosensitivity, dizziness, fatigue, sleep disturbances, depression and exacerbation of epilepsy, fluid retention.
Symptoms: Headache, dizziness, tremors, convulsions, nausea, vomiting. Treatment: removal of the drug from the gastrointestinal tract by means of artificially induced vomiting or gastric lavage, symptomatic therapy. Dynamic observation.
Interaction with other drugs
Sustanon 350 increases the effect of anticoagulants coumarin and derivatives indandiona (increases the risk of bleeding).
Reduces the action of insulin and neroralnyh hypoglycemic drugs (affecting carbohydrate metabolism, increases the concentration of glucose in the blood).
Increasing the concentration of glucagon in the blood plasma.
Sustanon 350 may reduce the effectiveness of antihypertensive drugs, possibly through sustanon 350 stimulation fluid retention.
Inhibits metabolism antiepileptic drugs (carbamazepine, phenytoin and phenobarbital), and increases their concentration in the blood.
increases concentration of plasma cyclosporin and tacrolimus blood (risk of nephrotoxicity increases).
Sustanon 350 can increase the calcemic response kaltsidol alpha in primary hypoparathyroidism, which requires reducing the dose of the drug.
Treatment Sustanon 350 requires careful observation of the patient, especially if they have liver disease and kidney disease, hypertension and / or other cardiovascular diseases, conditions, accompanied by fluid retention, epilepsy, lipoprotein metabolism, thrombosis (also in history), and migraine.
All patients receiving Sustanon 350, require regular inspection of liver function, including liver enzymes and the number of peripheral blood cells. In long-term treatment (6 months) and repeated courses of treatment is recommended to perform an ultrasound examination of the pelvic organs and the liver (at least 2 times a year). Care should be taken when used in patients with a prior response to treatment of androgenic sex hormones. Sustanon 350 affects some laboratory parameters of sex hormones (for example, increases the level of testosterone).
When administered to patients with diabetes require insulin dose adjustment. Appointment of high-dose Sustanon 350 prevents ovulation. However, ovulation is possible at low doses, so during treatment with Sustanon 350 should use non-hormonal methods of contraception.
In view of a possible androgenic effects on the fetus Sustanon 350 should not be administered during pregnancy, therefore, drug treatment in all cases must begin, to the exclusion of pregnancy, in the first day of menstruation. In patients with amenorrhea before the start of therapy it is necessary to test for the absence of pregnancy.