Bleomycin

Table of contents

  • Brand Names
  • Chemistry
  • Pharmacologic Category
  • Mechanism of Action
  • Therapeutic Use
  • Unlabeled Use
  • Pregnancy and Lactation Implications
  • Contraindications
  • Warnings and Precautions
  • Adverse Reactions
  • Toxicological Effects
  • Caution and personalized dose adjustment in patients with the following genotypes
  • Other genes that may be involved
  • Drug Interactions
  • Nutrition/Nutraceutical Interactions
  • Dosage
  • Pharmacokinetics and Pharmacodynamics
  • Special Considerations

Brand Names

Europe

Austria: Bleomycin; Belgium: Bleomin, Bleomycine; Bulgaria: Bleocin, Bleomycin; Czech Republic: Bleocin, Bleomycin; Denmark: Bleomycin; Estonia: Bleocin; Finland: Bleomycin; France: Bleomycine; Germany: Bleo, Bleomycin; Greece: Bleocin; Hungary: Bleocin, Bleomycin; Ireland: Bleomycin; Italy: Bleomicina; Luxembourg: Bleomycine; Netherlands: Bleomycine; Poland: Bleocin; Portugal: Bleocin, Bleomicina; Slovakia: Bleocin; Slovenia: Bleomicin; Spain: Bleomicina; Sweden: Bleomycin; UK: Bleo-Kyowa.

North America

Canada: Blenoxane, Bleomycin; USA: Blenoxane.

Latin America

Argentina: Bileco, Bleocris, Bleomicina, Blocamicina, Cytorich; Brazil: Blenoxane, Bonar, Tecnomicina; Mexico: Blanoxán, Bleolem, Bleomax.

Asia

Japan: Bleo.

Drug combinations

Chemistry

Bleomycin Sulfate: The sulfate salt of bleomycin, a mixture of basic cytotoxic glycopeptides produced by the growth of Streptomyces verticillus, or produced by other means. CAS-9041-93-4; CAS-11056-06-7 (bleomycin)(1971).

Pharmacologic Category

Antineoplastic Agents; Cytotoxic Antibiotics and Related Substances; Antibiotic. (ATC-Code: L01DC01).

Mechanism of action

Active against Gram-positive and Gram-negative bacteria and fungi. May inhibit DNA synthesis and to a lesser extent inhibition of RNA and protein synthesis. Binds to DNA leading to single- and double-strand breaks by a Fe^2+^-O~2~-catalyzed free radical reaction. Inhibits incorporation of thymidine into DNA. Exhibits no immunosuppressive activity.

Therapeutic use

Palliative treatment of squamous cell carcinoma, testicular carcinoma, and germ cell tumors. Hodgkin’s lymphoma, non-Hodgkin lymphoma, renal carcinoma, and soft tissue sarcoma. Sclerosing agent to control malignant effusions.

Pregnancy and lactiation implications

Teratogenic and abortifacient effects in animal studies. There are no adequate studies in pregnant women. Breast-feeding is not recommended.

Unlabeled use

Intrapleural management of pneumothorax associated with acquired immunodeficiency syndrome and Pneumocystis jiroveci (Pneumocystis carinii) pneumonia.

Contraindications

Hypersensitivity to bleomycin or any component of the formulation. Severe pulmonary disease. Pregnancy.

Warnings and precautions

May cause idiosyncratic reaction (chills, fever, hypotension, mental confusion, and wheezing) usually after the first or second dose (bleomycin is contraindicated in known hypersensitivity or idiosyncrasy to the drug). May produce pulmonary fibrosis. Caution when administering O~2~ during surgery to patients who have received bleomycin (may promote pulmonary toxicity). Avoid use in underlying lung disease or lung metastases. May cause pleuropericarditis, or Raynaud’s phenomenon. May cause renal toxicity. Bleomycin should be administered with extreme caution to patients with clinically important impairment of renal function or compromised pulmonary function. Risk of developing dose-related adverse mucocutaneous effects (e.g. erythema, hyperpigmentation, rash, skin tenderness, striae, vesiculation, and less commonly hyperkeratosis, nail changes, alopecia, pruritus, stomatitis). Hepatic toxicity may occur at any time after bleomycin initiation. Bleomycin has been shown to be mutagenic in vitro and in vivo, although it is not known if bleomycin is carcinogenic in humans (an increased incidence of nodular hyperplasia, site fibrosarcomas and various renal tumors observed in rats).

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