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Bleotsin relates to antitumor antibiotic is a mixture of water-soluble salts of structurally related glycopeptide antibiotics. The basis of the mechanism of action is Bleotsina DNA fragmentation, destruction of its helical structure, leading to inhibition of cell division. To a lesser extent Bleotsin effect on RNA and protein synthesis. Unlike most other cytostatics Bleotsin less toxic to bone marrow does not have immunosuppressive activity and are not to be neurotoxic and cardiotoxic medication. At intraplevralnom introduction exhibits sclerosing properties. Pharmacokinetics. After intramuscular injection at a dose of 15 mg / m² body surface of the maximum plasma concentration is reached after 30 minutes. after administration. Bleotsin rapidly distributed in the body tissues with the greatest concentration in the skin lungs, lymph nodes, and peritoneum. When intraplevralnoy installation systemic absorption is 45%. Communication to plasma proteins is insignificant. Hitherto unknown mechanism Bleotsina biotransformation. Inactivation is carried out with the assistance of the drug buy testosterone enanthate hydrolase enzyme is mainly in the plasma, liver and other organs, and to a lesser extent in the skin and lungs. The half-life is approximately 2-3 Bleotsina hours. Approximately 60-70% of the injected amount Bleotsina excreted unchanged in the urine by glomerular filtration. Most of the dose is excreted within 8-12 hours. The concentration of drug in plasma increases dramatically when administered Bleotsina usual dose for patients with impaired renal function. If creatinine clearance of 35 mL / min urine is allocated only 20% of the formulation.

Indications

Bleotsin usually used in combination with other cytotoxic drugs and / or radiation therapy for the treatment of squamous forms of head and neck cancer, esophageal, lung, cervix, vulva, penis, germ cell tumors, kidney cancer, Hodgkin’s disease and non-Hodgkin’s limform (including lymphosarcoma and retikulosarkomu), malignant testicular tumors, malignant pleurisy (as a sclerosing agent)

Contraindications

 

  • Increased sensitivity to buy testosterone enanthate;
  • Acute pulmonary infection;
  • Expressions of lung function;
  • Severe renal impairment;
  • Pregnancy and lactation.Precautions : If concomitant or previous radiation therapy, acute infectious or viral diseases, renal impairment, in children.Dosage and administration
    in each individual case when choosing the dose and mode of administration Bleotsina should use the data of literature.
    Bleotsin can be administered intramuscularly, intravenously, subcutaneously or intrapleural.
    Recommended dosage: intramuscular injection (1-5 ml of water for injection, alternating injection sites) or intravenously (0.9 mL in 5.10% sodium chloride solution or water for injection for 5-10 minutes) at a dose of 10-15 mg / m² once or twice a week intraplevralno (50-100 ml 0 9% sodium chloride solution after the evacuation of the maximum possible amount of exudate) 60 mg once daily.
    Because of the increased risk of anaphylactic reactions in patients with malignant lymphomas initial dose may be reduced (eg to 2-3 mg / m²). In the absence of acute infusion reactions, further treatment can be continued in a normal dose.
    Total Bleotsina total dose should not exceed 400 mg and continuation of administration may be carried out only after the assessment of lung function.
    In elderly patients, the dose is defined as follows:

     

    Age (years) The total dose Weekly dose
    80 and over 100 mg 15 mg
    70-79 150-200 mg 30 mg
    60-69 200-300 mg 30-60 mg
    Less than 60 400 mg 30-60 mg

    Introduction Bleotsina children can be performed only in special cases, determining the dose should be administered at the rate of body surface area.
    In Bleotsina radiotherapy dose should be reduced because the irradiated tissue more susceptible. Adjusting the dose should be carried out in the case if Bleotsin used in combination with other chemotherapeutic agents.
    In patients with impaired renal function Bleotsina dose varies as follows: – at the level of serum creatinine 130-180 mmol / l dose should be reduced by 50% at the level of serum creatinine over 180 mmol / l administration of the drug is delayed until the normalization of the creatinine level indicators.

    Side effect On the part of the respiratory system: in 2-10% of cases of interstitial pneumonia (When the appearance of shortness of breath, coughing, wheezing in the lungs), lung fibrosis of the skin and skin appendages: dyskeratosis (thinning or thickening of the skin) in the area of the elbow or knee joints, hands , buttocks, shoulder blades; redness, rash, striae, hyperpigmentation, skin itching, deformation and brittle nails, skin hypersensitivity and distal (nail) phalanges, hyperemia fingertips, alopecia. Violations of the skin occurs in approximately 50% of cases, usually after reaching total doly Bleotsina – 150-200 mg. In rare cases, are pronounced and usually disappear after the completion of the course. On the part of the digestive tract: anorexia, nausea, vomiting, diarrhea, stomatitis, weight loss (with prolonged use). Allergic reactions: 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. Other: fever and chills (observed in 20-60% of patients, usually after 2 -6 hrs after the first injection Bleotsina significantly reduced during subsequent injections), vascular disorders (including cerebral arteritis, thrombotic microangiopathy, myocardial infarction, Raynaud’s syndrome), plevroperikardit, fatigue, pain in the tumor formations, local pain when intraplevralnom administration; changes in liver and kidney function tests, a slight suppression of bone marrow function.

    Overdose

    immediate sharp reaction in cases of overdose is hypotension, fever, rapid pulse and general symptoms of shock. Treatment is symptomatic. If complications from bronchopulmonary system patients should be given treatment corticosteroids and broad spectrum antibiotics.

    Interaction with other medicinal products and other forms of interaction
    Simultaneous administration Bleotsina with carmustine (BCNU), mitomycin C, cyclophosphamide and methotrexate, filgrastim and other cytokines, as well as previous or ongoing at this time of radiation therapy to the chest area increased lung toxicity of risk .
    Patients who were treated with Bleotsina have an increased risk of pulmonary toxicity when administered to them of oxygen during anesthesia for surgical interventions. Such patients recommended kontsedschttsii decreased oxygen during and after surgery.
    In patients with testicular cancer undergoing combined treatment Bleotsinom and drugs from the class vinkoalkaloidov described Raynaud’s syndrome.

    Specific guidance
    Treatment should be supervised by a physician who has experience in anticancer therapy.
    Patients undergoing treatment Bleotsinom, periodic pulmonary function tests and X-rays of the chest.
    Toxicity Bleotsina increases when a cumulative dose of 400 mg (225 mg / m ), 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 conducted irradiation of light and smoke.
    Sensitive to Bleotsinu increased in elderly patients.
    When a cough, shortness of breath, wheezing or radiographic evidence of interstitial pneumonia should stop administering Bleotsina as long as the toxic effects of the drug will not be eliminated. If necessary, prescribe antibiotics and steroids.
    For relief of fever can take antipyretics.
    Concentration Bleotsina in blood plasma increases dramatically with the introduction of the drug in patients with impaired renal function.
    During treatment Bleotsinom and for at least 3 months after you should use reliable methods contraception.
    Normal precautions should be observed in the preparation of the drug and its administration. If the product enters the skin or mucous membrane of these places should be washed for a long period of time.

    Release form
    Valium for solution for injection 15 mg vials of neutral glass with colorectal golden ring for easy opening or a vial of neutral glass, sealed with a rubber stopper, crimped aluminum cap with a plastic insert FLIP OFF Green (control of the first opening). 1 ampoule or 1 bottle with instruction on use – in a carton box.
    There are 10 bottles in a cardboard tray with partitions, along with instructions for use – in a carton box.

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