Bleocin-S (Bleomycin, Bleolem) por. for in. 15ME - Instructions

Bleocin-S (Bleomycin, Bleolem) por. for in. 15ME - Instructions

Release form

Bleocin is a lyophilisate for the preparation of a solution for injection, 15 mg in an ampoule.

Compound

One ampoule or bottle of Bleocin contains: active substance: bleomycin 15 mg (in the form of bleomycin hydrochloride).

pharmachologic effect

Bleocin is an antitumor antibiotic and is a mixture of structurally related water-soluble salts of glycopeptide antibiotics. The mechanism of action of Bleocin is based on DNA fragmentation, destruction of its helical structure, which leads to inhibition of cell division. To a lesser extent, Bleocin affects RNA and protein synthesis. Unlike most other cytostatics, Bleocin is less toxic to the bone marrow, does not have an immunosuppressive effect and is not a neurotoxic or cardiotoxic drug. When administered intrapleurally, it exhibits sclerosing properties.

Pharmacokinetics.

After intramuscular administration of the drug at a dose of 15 mg/m² of body surface, the maximum concentration in plasma is achieved after 30 minutes. after administration of the drug. Bleocin is rapidly distributed in body tissues with the highest concentrations in the skin of the lungs, peritoneum and lymph nodes. With intrapleural installation, systemic absorption is 45%. The connection with blood plasma proteins is insignificant. To date, the mechanism of biotransformation of Bleocin is unknown. Inactivation of the drug is carried out with the participation of the enzyme bleomycin hydrolase, mainly in the blood plasma, liver and other organs and to a lesser extent in the skin and lungs.

The half-life of Bleocin is about 2-3 hours. Approximately 60-70% of the administered amount of Bleocin is excreted unchanged in the urine due to glomerular filtration. Most of the drug dose is eliminated within 8-12 hours.

The concentration of the drug in plasma increases sharply when the usual dose of Bleocin is administered to patients with impaired renal function. With a creatinine clearance of 35 ml/min, only 20% of the drug is excreted in the urine.

Indications for use

Bleocin is used in combination with other cytostatics and/or radiation therapy for the treatment of squamous cell cancers of the head and neck, esophagus, lungs, cervix, vulva, penis, germ cell tumors, kidney cancer, Hodgkin's disease and non-Hodgkin's lymphforms (including lymphosarcoma and reticulosarcoma). , malignant testicular tumors, malignant pleurisy (as a sclerosing agent)

Directions for use and dosage

In each individual case, when choosing the dose and mode of administration of Bleocin, you should use data from special literature. Bleocin can be administered intramuscularly, intravenously, subcutaneously or intrapleurally.

Recommended doses: intramuscularly (in 1-5 ml of water for injection, alternating injection sites) or intravenously (in 5-10 ml of 0.9% sodium chloride solution or water for injection for 5-10 minutes) at a dose of 10-15 mg/m² once or twice a week intrapleurally (in 50-100 ml of 0.9% sodium chloride solution after evacuation of the maximum possible amount of exudate) 60 mg once. Due to the increased risk of developing an anaphylactic reaction in patients with malignant lymphomas, the initial dose may be reduced (for example, to 2-3 mg/m²). In the absence of an acute reaction to the administration of the drug, further therapy can be continued at the usual dose. The total total dose of Bleocin should not exceed 400 mg and further continued administration of the drug can be carried out only after assessing pulmonary function.

In elderly patients, the dose of the drug is determined as follows:

Bleocin can be administered to children only in special cases; the dose of the drug should be determined based on the body surface area.

When carrying out radiation therapy, the dose of Bleocin should be reduced, since the irradiated tissues are more sensitive to the drug. The dose of the drug should also be adjusted if Bleocin is used in combination with other chemotherapy drugs.

In patients with impaired renal function, the dose of Bleocin changes as follows: if the serum creatinine level is 130-180 µmol/l, the dose of the drug should be reduced by 50%; if the serum creatinine level is more than 180 µmol/l, the administration of the drug is postponed until the creatinine level is normalized.

Side effects

From the respiratory system: in 2-10% of cases interstitial pneumonia (with the appearance of shortness of breath, cough, wheezing in the lungs) pulmonary fibrosis

From the skin and skin appendages: dyskeratosis (thinning or thickening of the skin) in the area of ​​the elbow or knee joints, palms, buttocks, shoulder blades; hyperemia, rash, stretch marks, hyperpigmentation, itching, deformation and brittleness of nails, hyperesthesia of the skin and distal (nail) phalanges, hyperemia of the fingertips, alopecia.

Skin disorders occur in approximately 50% of cases, usually after reaching the total dose of Bleocin - 150-200 mg. In rare cases, they are pronounced and usually disappear after completion of the course.

From the gastrointestinal tract: anorexia, nausea, vomiting, diarrhea, stomatitis, weight loss (with long-term use).

Allergic reactions: urticaria, anaphylactic reactions (low blood pressure, confusion, fever, chills, wheezing).

Similar reactions were observed in approximately 1% of patients with malignant lymphomas, usually after the first or second administration of the drug.

Other: fever and chills (observed in 20-60% of patients, usually 2-6 hours after the first injection of Bleocin, significantly decreases with subsequent injections), vascular disorders (including cerebral arteritis, thrombotic microangiopathy, heart attack myocardium, Raynaud's syndrome), pleuropericarditis, increased fatigue, pain in the area of ​​tumor formations, local pain with intrapleural injection; changes in liver and kidney function tests, slight suppression of bone marrow function.

Contraindications

Contraindications to the use of the drug Bleocin are: hypersensitivity to bleomycin; acute pulmonary infections; severe pulmonary dysfunction; severe renal dysfunction; pregnancy and lactation period.

With caution: with concomitant or previous radiation therapy, acute infectious or viral diseases, impaired renal function, in childhood.

Pregnancy and breastfeeding

If it is necessary to use Bleocin during lactation, breastfeeding should be discontinued. Women of childbearing potential receiving bleomycin therapy should use reliable methods of contraception. Experimental studies have established the teratogenic and embryotoxic effects of bleomycin.

Interaction with other drugs

With simultaneous administration of Bleocin with carmustine (BCNU), mitomycin C, cyclophosphamide and methotrexate, filgrastim and other cytokines, as well as previous or current radiation therapy to the chest area, the risk of developing pulmonary toxicity increases. Patients treated with Bleocin have an increased risk of pulmonary toxicity when oxygen is administered during anesthesia during surgery. In such patients, it is recommended to reduce oxygen concentration during and after surgery. Raynaud's syndrome has been described in patients with a malignant testicular tumor who undergo combined treatment with Bleocin and drugs from the vincoalkaloid class.

Overdose

Immediate acute reactions in case of Bleocin overdose are arterial hypotension, fever, rapid pulse and general symptoms of shock. Treatment is symptomatic. In case of complications from the bronchopulmonary system, patients should be prescribed treatment with glucocorticosteroids and broad-spectrum antibiotics.

Features of application

Treatment must be carried out under the supervision of a physician experienced in antitumor therapy. Patients treated with Bleocin should undergo regular pulmonary function testing, as well as chest x-ray.

The toxicity of Bleocin increases when the cumulative dose reaches 400 mg (225 mg/m2), however, the toxic dose may be significantly lower in elderly patients, in patients with impaired renal function, with a history of lung disease, in the case of previous lung irradiation and smoking. Sensitivity to Bleocin increases in elderly patients.

If cough, shortness of breath, wheezing or radiological signs of interstitial pneumonia occur, the administration of Bleocin should be discontinued until the toxic effects of the drug are eliminated. If necessary, antibiotics and glucocorticosteroids should be prescribed. Antipyretics can be taken to relieve fever.

The concentration of Bleocin in the blood plasma increases sharply when the drug is administered to patients with impaired renal function. During treatment with Bleocin and for at least 3 months after, reliable methods of contraception should be used.

Normal precautions must be observed during preparation and administration. If the drug gets on the skin or mucous membrane, these areas should be rinsed with water for a long period of time.

Storage conditions

List A. At a temperature not higher than + 30°C in a dry place, protected from light and out of reach of children.

Vacation category

On prescription.

Bleomycin - use and indications

Bleomycin is one of the representatives of a group of structurally similar natural compounds that have antitumor activity (bleomycin A2, B2, etc.). The mechanism of their cytotoxic (cell-damaging action) is associated with the ability to cause fragmentation (separation) of the DNA molecule (deoxyribonucleic acid - a component of the cell nucleus responsible for the transfer of hereditary information). Bleomycin has the ability to accumulate (with parenteral (bypassing the digestive tract) administration) in the skin, and therefore it is especially effective against cancer of the skin and mucous membranes. It inhibits bone marrow hematopoiesis relatively little. Does not have a significant immunosuppressive (suppressing the body's defenses) effect.

Indications for use:

It is used mainly for squamous cell cancer of the mucous membranes of the oral cavity, nasopharynx, larynx, esophagus, lung, thyroid gland, cervix, as well as cancer of the penis, teratoblastoma (a tumor arising from cells that were incorrectly formed during fetal development) and lymphogranulomatosis (cancer lymphatic system, in which dense formations consisting of rapidly growing cells form in the lymph nodes and internal organs).

The drug is more effective in the early stages. For metastases of malignant tumors (new tumors that have appeared in other organs and tissues as a result of the transfer of cancer cells with blood or lymph from the primary tumor), no therapeutic effect was noted. For esophageal cancer it is recommended in combination with radiation therapy, for teratoblastoma - in combination with rosevin or other antitumor drugs.

Adverse events:

Various side effects may occur when using bleomycin. On the day of administration, body temperature sometimes rises, nausea, vomiting, anorexia (lack of appetite), stomatitis (inflammation of the oral mucosa), conjunctivitis (inflammation of the outer membrane of the eye), vulvitis (inflammation of the external female genital organs), alopecia (complete or partial) are possible. hair loss). Skin changes are often observed: focal hyperkeratoses (thickening of individual areas of the skin), hyperpigmentation (increased pigment deposition), dermatitis (inflammation of the skin). Hyperesthesia of the distal phalanges (increased sensitivity of the fingertips), redness of the fingertips, and brittle nails may also be noted. Typically, these phenomena develop towards the end of the course of treatment, are benign and do not require cessation of treatment. Long-term side effects may include pneumonia (pneumonia), fibrosis (overgrowth of connective tissue) of the lung tissue. During treatment with bleomycin and after 3-4 weeks. At the end of treatment, it is necessary to perform an X-ray examination of the chest. If signs of pneumonia are detected during treatment, treatment is stopped.

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