Bleocin, lyophilizate 15 mg

Pharmacodynamics

Antitumor agent. It is an A₂ fraction isolated from Streptomyces verticillus culture containing the antitumor antibiotic itself. The mechanism of action is associated with the ability to cause fragmentation of DNA molecules. It has weakly expressed myelodepressive and immunosuppressive activity.

Pharmacokinetics

Protein binding is 1%. Subjected to metabolism, the pathways of which are not precisely determined.

T_1/2 with a CK of more than 35 ml/min is 115 min. It is excreted by the kidneys, 60-70% mostly unchanged.

Indications

Active ingredient

Composition

Active ingredients:

Bleomycin (in the form of hydrochloride) – 15 mg.

In a vial 15 mg of lyophilizate.

Package contains 1 vial.

How to take, the dosage

Bleocin should be used in each individual case to choose the dose and mode of administration of Bleocin.

Bleocin can be administered intramuscularly, intravenously, subcutaneously or intrapleural.
Recommended doses: intramuscularly (in 1-5 ml of water for injection, alternating the injection sites) or intravenously by trickle (in 5-10 ml of 0.9% sodium chloride solution or water for injection for 5-10 minutes) at the dose of 10-15 mg/m² once or twice a week intrapleural (in 50-100 ml of 0.9% sodium chloride solution after evacuation of the maximum possible amount of exudate) 60 mg once.

Because of the increased risk of anaphylactic reaction in patients with malignant lymphoma, the initial dose may be reduced (e.g., to 2-3 mg/m²). If there is no acute reaction to the drug administration, further therapy may be continued at the usual dose.

The total cumulative dose of Bleocin should not exceed 400 mg and further continuation of the drug should be performed only after evaluation of lung function.
In elderly patients, the dose of the drug is determined as follows:

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

The dose of Bleocin must be reduced if radiation therapy is administered because the irradiated tissues are more sensitive to the drug. Adjustment of the dose of the drug should also be made if Bleocin is used in combination with other chemotherapy drugs.

In patients with renal dysfunction the dose of Bleocin is changed as follows: if serum creatinine levels are 130-180 µmol/l, the drug dose should be reduced by 50%; if serum creatinine levels are more than 180 µmol/l, the drug should be delayed until creatinine levels normalize.

Interaction

Bleomycin increases the risk of pneumotoxic effects in patients receiving oxygen (e.g., as part of general anesthesia).

Concomitant use with drugs with myelotoxic and pneumotoxic effects may increase the risk of side effects.

The clearance of bleomycin may be delayed and its toxic effects increased even when used in low doses due to the nephrotoxic effect of cisplatin.

Special Instructions

With caution, use in patients with lung disease (including a history of lung disease), with renal dysfunction, with CHD, heart defects, in the elderly, and in patients who have received or are receiving radiotherapy.

Perhaps with caution in patients with varicella zoster (including those who have had it recently or after exposure to the disease), herpes zoster and acute infectious diseases.

In the course of treatment, systematic monitoring of respiratory function, chest x-ray examination, and control of kidney and liver function are necessary. If coughing or dyspnea occurs, treatment should be stopped and GCS and antibiotics should be prescribed.

The safety of use in pediatric practice has not been established.

The carcinogenic and mutagenic effects of bleomycin have been established in experimental studies. That is why extreme caution is necessary when using bleomycin for treatment of other diseases (fungal mycosis, common warts).

Contraindications

Side effects

Respiratory system: interstitial pneumonia, pulmonary fibrosis.

Digestive system disorders: nausea, vomiting, anorexia, angular stomatitis, liver function disorders.

Urinary system disorders: renal dysfunction, frequent and painful urination.

CNS disorders: headache, dizziness.

Reproductive system disorders: azoospermia, amenorrhea.

Allergic reactions: erythema, urticaria, anaphylactoid reactions. Dermatological reactions: focal hyperkeratoses, hyperpigmentation, dermatitis, nail deformities, alopecia.

Others: fever, leukopenia; rarely – toxic effects on blood vessels (including cerebral arteritis, stroke, myocardial infarction).

Overdose

Symptoms: immediate acute reactions in case of overdose are arterial hypotension, fever, rapid pulse and general symptoms of shock.

Treatment: symptomatic. In case of complications of the bronchopulmonary system, patients should be prescribed treatment with glucocorticosteroids and broad-spectrum antibiotics.

Pregnancy use

Bleomycin is contraindicated in pregnancy. Breast-feeding should be discontinued if use during lactation is necessary.

Women of childbearing age receiving therapy with bleomycin should use reliable contraceptive methods.

The teratogenic and embryotoxic effects of bleomycin have been established in experimental studies.