Pharmacological properties testosterone enanthate cycle relates to antitumor antibiotic is a mixture of water-soluble salts of structurally related glycopeptide antibiotics. The basis of the mechanism of action of testosterone enanthate cycle is DNA fragmentation, destruction of its spiral structure, which leads to inhibition of cell division.To a lesser degree affected by testosterone enanthate cycle RNA and protein synthesis.
It has a selective effect against tumors of epidermal origin due to its ability to accumulate in the cells of the skin. Selectivity due to low content of tumor cells in the enzyme-inactivating testosterone enanthate cycle hydrolase.
Unlike most other cytostatics, testosterone enanthate cycle less toxic to bone marrow, has no immunosuppressive action without cardiotoxic and neurotoxic drug.
When intraplevralnom introduction shows sclerosing properties.
After intramuscular injection at a dose of 15 IU / m2 body surface maximum plasma concentration is reached after 30 minutes.
testosterone enanthate cycle is rapidly distributed in the body tissues with the greatest concentration in the skin, lungs, kidney, lymph nodes, and peritoneum. When intraplevralnoy instillation systemic absorption is 45%. It does not cross the blood-brain barrier. Communication to plasma proteins is insignificant.
Hitherto unknown mechanism biotransformation testosterone enanthate cycle. Inactivation is carried out with the assistance of the drug testosterone enanthate cycle hydrolase enzyme is mainly in the plasma, liver and other organs, and to a lesser extent in skin and lungs.
The half-life of testosterone enanthate cycle is approximately 2-3 hours. Approximately • 60-70% testosterone enanthate cycle amount administered in normal kidney function is excreted unchanged in the urine, apparently due to glomerular filtration. The concentration of drug in plasma increases sharply in the case of the introduction of the usual dose of testosterone enanthate cycle in patients with impaired renal function. If creatinine clearance <35 mL / min in the urine is allocated only 20% of the formulation.
Indications for use
testosterone enanthate cycle is typically used in combination with other cytotoxic drugs and / or radiation therapy for the treatment of squamous forms of head and neck cancer, esophagus, lung, cervix, vulva, skin cancer, penile cancer, germ cell tumors, kidney cancer, Hodgkin’s disease and non-Hodgkins lymphoma (including lymphosarcoma and retikulosarkomu), malignant testicular tumors, malignant pleurisy (as a sclerosing agent).
- increased sensitivity to testosterone enanthate cycle;
- acute pulmonary infections;
- expressed in lung function;
- pronounced renal dysfunction;
- teleangiektaticheskaya ataxia (Louis-Bar syndrome)
- pregnancy and lactation.
Precautions: during concomitant or previous radiation therapy, acute infectious or viral diseases, renal impairment, in children.
Dosing and Administration
Blenamaks can be administered intramuscularly, intravenously, subcutaneously or intrapleural.
In each individual case when choosing the dose and mode of administration Blenamaksa should use the data of literature. Doses are calculated per unit of total body surface area.
– Intramuscularly or subcutaneously (in 5.1 ml of water for injection or 0.9% sodium chloride solution, alternating the injection sites) at a dose of 10-20 IU / m 2 once or twice a week
– intravenously (5-10 ml 0.9% sodium chloride solution or water for injection for 5-10 minutes) at a dose of 10-20 IU / m 2 once or twice a week
– in the form of intravenous infusion of 6-24 hours (in 200-1000 ml 0.9% sodium chloride) at a dose of 10-20 IU / m 2 for 4-7 days every 3-4 weeks;
– intraplevralno (50-100 ml 0.9% sodium chloride solution after evacuation of the maximum possible amount of exudate ) 60 units once.
Because of the increased risk of anaphylactic reactions in patients with malignant lymphomas initial dose may be reduced (eg, to 2-3 IU / m 2 ). In the absence of acute infusion reactions, further treatment can be continued in a normal dose.
The total cumulative dose Blenamaksa should not exceed 400 units and continuation of administration can be carried out only after an assessment of lung function. In applying the drug in combination with other anticancer drugs pulmonary toxicity may also occur at lower cumulative doses Blenamaksa.
Use in the elderly:
In elderly patients, the dose is determined as follows:
|Age (years)||The total dose||Weekly dose|
|80 and over||100 U||15 IU|
|70-79||150-200 IU||30 units|
|60-69||200-300 IU||U 30-60|
|younger than 60||400 units||U 30-60|
Introduction Blenamaksa children may be carried out only in special cases. Dose is determined based on the total surface of the unit body.
Patients with renal impairment:
In patients with impaired renal function Blenamaksa dose is calculated as follows:
– at the level of serum creatinine 130-180 mmol / l dose should be reduced by 50%.
– If the level of serum creatinine over 180 mmol / l introduction of the drug is delayed until the normalization of the creatinine level indicators.
Side effect On the part of hematopoiesis: testosterone enanthate cycle little depressing bone marrow hematopoiesis. Occasionally there may be a small reversible thrombocytopenia
Immune system: urticaria, anaphylactic reaction (decrease in blood pressure, confusion, fever, chills, wheezing). Similar reactions were observed in approximately 1% of patients with malignant lymphomas, usually after the first or second injection.
From the nervous system: headache, dizziness, paresthesia, and hyperesthesia;
Cardio-vascular system: describes episodes of acute dystonia in patients with Hodgkin’s disease treated with high doses of testosterone enanthate cycle. Lowering blood pressure (when administered intravenously). Rarely resulting vascular disorders may occur cerebral arteritis, thrombotic microangiopathy, myocardial infarction, stroke, Raynaud’s syndrome;
From the respiratory system: in 2-10% of cases of interstitial pneumonia (the appearance of shortness of breath, coughing, wheezing in the lungs), often with the outcome of pulmonary fibrosis or even fatal (1%).
Skin and skin appendages: dyskeratosis in the elbow or knee joints, hands, fingers, buttocks, shoulder blades; redness, rash, striae, hyperpigmentation, skin itching, deformation and brittle nails, skin hypersensitivity and distal (nail) phalanges, hyperemia fingertips, alopecia. Disorders of the skin occur in approximately 50% of cases, usually after a total dose of testosterone enanthate cycle – 150-200 DB. In rare cases, it is pronounced and usually disappear after treatment is completed. There were isolated reports of the development of scleroderma in patients treated with testosterone enanthate cycle.
From the gastrointestinal tract:
anorexia, nausea, vomiting, diarrhea, stomatitis, weight loss (with prolonged use).
Local reactions: local thrombophlebitis, venous occlusion developing usually by intravenous administration of the drug. When injected into the pleural cavity may experience soreness at the injection site.
Other: plevroperikardit, fatigue, pain in the tumor mass; changes in liver and kidney function tests, pain in bones and joints.
Fever (temperature rise with chills) is observed in 20-60% of patients, usually after the first 6.2 hours after the injection of testosterone enanthate cycle. The frequency of fever during the subsequent injection of testosterone enanthate cycle is significantly reduced.
immediate reaction in case of an overdose include decreased blood pressure, fever, rapid pulse and general symptoms of shock. There is no specific antidote. Treatment is symptomatic. If complications from bronchopulmonary system patients should be given treatment glyukokortikosteroidamn and broad spectrum antibiotics.
Interaction with other medicinal products and other forms of interaction
testosterone enanthate cycle reduces the bioavailability of digoxin and affect its efficacy in combination with testosterone enanthate cycle vinca alkaloids may develop Raynaud’s syndrome. testosterone enanthate cycle phenytoin reduces plasma
The combined use of testosterone enanthate cycle with nephrotoxic drugs (cisplatin) leads to a decrease in clearance of testosterone enanthate cycle. The combined use of cisplatin and testosterone enanthate cycle can cause severe and even fatal pulmonary toxicity
When administered simultaneously with carmustine testosterone enanthate cycle, mitomycin, cyclophosphamide, and methotrexate, filgrastim and other cytokines, as well as previous or ongoing at this time radiation therapy of the chest at increased risk of developing pulmonary toxicity.
Patients who were treated with testosterone enanthate cycle, have an increased risk of pulmonary toxicity when using oxygen. during anesthesia for surgical interventions. Such patients recommended decrease in oxygen concentration during and after surgery.
Vaccination with live vaccines against application of testosterone enanthate cycle can lead to an intensification of the process of replication of vaccine virus, enhancing its side / adverse effects and / or reduce the production of antibodies in the patient’s body in response to the vaccine.
Treatment should be implemented under the supervision of a physician with experience in anticancer therapy.
Patients undergoing treatment with testosterone enanthate cycle should regularly study of respiratory function, as well as X-ray examination of the chest.
When coughing, shortness of breath, wheezing or radiographic evidence of interstitial pneumonitis should stop administering testosterone enanthate cycle as long as the toxic effects of the drug will not be eliminated. If necessary, prescribe antibiotics and steroids.
The toxicity of testosterone enanthate cycle increases when a cumulative dose of 400 IU (225 IU / m 2 ), but the toxic dose can be much lower in elderly patients, in patients with impaired renal function, a lung disease in history, in the case of the previously held light irradiation, as well as smoking.
Increased sensitivity to testosterone enanthate cycle in elderly patients.
For relief of fever can take antipyretics.
testosterone enanthate cycle concentration in blood plasma increases dramatically with the introduction of the drug in patients with impaired renal function.
Because of the potential teratogenic effects of testosterone enanthate cycle in respect of male and female reproductive cells should use reliable methods of contraception during treatment with testosterone enanthate cycle, and within three months after completion of treatment.
Normal precautions should be observed in the process of preparing a solution of the drug and its administration. If the product enters the skin or mucous membrane of these places should be rinsed with plenty of water.
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