Generic Name: Bleomycin sulfate
Dosage Form: injection, powder, lyophilized, for solution
Bleomycin for Injection USP
Rx Only
It is recommended that Bleomycin for Injection USP be administered under the supervision of a qualified physician experienced in the use of cancer chemotherapeutic agents. Appropriate management of therapy and complications is possible only when adequate diagnostic and treatment facilities are readily available.
Pulmonary fibrosis is the most severe toxicity associated with Bleomycin. The most frequent presentation is pneumonitis occasionally progressing to pulmonary fibrosis. Its occurrence is higher in elderly patients and in those receiving greater than 400 units total dose, but pulmonary toxicity has been observed in young patients and those treated with low doses.
A severe idiosyncratic reaction consisting of hypotension, mental confusion, fever, chills, and wheezing has been reported in approximately 1% of lymphoma patients treated with Bleomycin.
Bleomycin Description
Bleomycin for Injection USP is a mixture of cytotoxic glycopeptide antibiotics isolated from a strain of Streptomyces verticillus. It is freely soluble in water. Bleomycin for Injection USP contains sterile Bleomycin sulfate equivalent to 15 units or 30 units of Bleomycin. Sulfuric acid or sodium hydroxide can be used, if necessary, to adjust pH.
Bleomycin for Injection USP may be given by the intramuscular, intravenous or subcutaneous routes.
Its chemical name is N’-[3-(dimethylsul-phonio)propyl]Bleomycin-amide (Bleomycin A2) and N’-[4-(guaniodobutyl)]Bleomycin-amide (Bleomycin B2). (Main component: Bleomycin A2, in which R is [CH3]2S+CH2CH2CH2-)
The molecular formula of Bleomycin A2 is C55H84N17O21S3 and a calculated molecular weight of 1414. The molecular formula of Bleomycin B2 is C55H84N20O21S2 and a calculated molecular weight of 1425. The structural formula of Bleomycins A2 and B2 are shown below.



Note: A unit of Bleomycin is equal to the formerly used milligram activity. The term milligram activity is a misnomer and was changed to units to be more precise.
Bleomycin - Clinical Pharmacology
Mechanism of Action
Although the exact mechanism of action of Bleomycin is unknown, available evidence indicates that the main mode of action is the inhibition of DNA synthesis with some evidence of lesser inhibition of RNA and protein synthesis.
Bleomycin is known to cause single, and to a lesser extent, double-stranded breaks in DNA. In in vitro and in vivo experiments, Bleomycin has been shown to cause cell cycle arrest in G2 and in mitosis.
When administered into the pleural cavity in the treatment of malignant pleural effusion, Bleomycin acts as a sclerosing agent.
Pharmacokinetics
Absorption
Bleomycin is rapidly absorbed following either intramuscular, subcutaneous, intraperitoneal, or intrapleural administration reaching peak plasma concentrations in 30 to 60 minutes. Systemic bioavailability of Bleomycin is 100% and 70% following intramuscular and subcutaneous administrations, respectively, and 45% following both intraperitoneal and intrapleural administrations, compared to intravenous and bolus administration.
Following intramuscular doses of 1 to 10 units/m2, both peak plasma concentration and AUC increased in proportion with the increase of dose.
Following intravenous bolus administration of 30 units of Bleomycin to one patient wit