Contents

Search

bleomycin (Blenoxane)

Tradename: Blenoxane. Indications: 1) treatment & management of malignancies a) squamous cell carcinomas of the head & neck b) squamous cell carcinomas of the penis & cervix c) testicular cancer d) Hodgkin's disease & non-Hodgkin's lymphoma e) sarcomas (including lymphomas) f) germ cell neoplasm [7] 2) sclerosing agent - pleural effusion [7] Dosage: 1) test dose of 1-2 units in 50 mL IV over 15 minutes 2) 10-20 units/m2* weekly or every other week IV/IM/SC 3) continuous infusion 15-20 units/m2*/day for 4-5 days * meter squared body surface area Infusions: 60 units in 50-100 mL of normal saline Stability: 1) stable for 24 hours reconstituted at room temperature 2) stable for 24-48 hours reconstituted & refrigerated 3) stability decreases iin PVC bags 4) incompatible with amino acid solutions, ascorbic acid, cefazolin, furosemide, diazepam, hydrocortisone, mitomycin, nafcillin, penicillin G, aminophylline 5) prepare solution in glass bottles, not plastic bags Powder for injection: 15 units. Dose reduction in renal failure: creatinine (mg/dL) % of usual dosage 2.5-4 25 4-6 20 6-10 10 Pharmacokinetics: 1) 50-70% of the drug is eliminated into the urine unchanged 2) metabolized drug is degraded by cellular enzymes Adverse effects: 1) common (> 10%) a) systemic: - mild febrile reactions, chills, nausea/vomiting (mild), stomatitis, anorexia b) skin, mucous membranes & skin appendages - erythema, induration, hyperkeratosis, peeling of skin, hyperpigmentation, alopecia#, nailbed changes 2) less common (1-10%) - weight loss, anaphylactoid reactions in 1% of patients with lymphoma 3) uncommon (< 1%) - myocardial infarction, renal toxicity, stroke, hepatotoxicity, skin thickening, dyspnea, tachypnea, non-productive cough, rales 4) other a) pneumonitis resulting in pulmonary fibrosis with cumulative dose > 150 units/m2*, > 400 units or < 30 units/single dose - onset 1-6 months after exposure - resolves in most cases, but may be fatal [5,6] - risk factors: - advanced age, tobacco, renal insufficiency, mediastinal radiation, oxygen therapy - consolidation ground glass opacities due to diffuse alveolar damage - management: - discontinue bleomycin treatment - treatment with glucocorticoids is controversial [5] b) mild myelosuppression (rare) - onset 7 days - nadir 14 days - recovery 21 days c) pain at tumor site d) Raynaud's phenomenon e) phlebitis # alopecia should resolve after discontinuation of drug * meter squared body surface area Drug interactions: 1) radiation therapy may increase pulmonary toxicity of bleomycin 2) vinblastine in combination may cause Raynaud's syndrome 3) cisplatin 4) digoxin 5) phenytoin 6) vincristine Test interactions: increases serum K+ Mechanism of action: A group of related glycopeptide antibiotics isolated from Streptomyces verticillus. Bleomycin A2 is main component of bleomycin employed clinically. It is believed to react with DNA & cause single & double strand DNA scission. Bleomycin has also been shown to have a type of oxygen transferase activity. Most of the cytotoxic effects of bleomycin are seen in the G2 phase of the cell cycle. Mechanism of drug resistance: -> increased drug inactivation via activation of bleomycin hydrolase

Interactions

drug interactions

Related

bleomycin hydrolase; BLM hydrolase (BMH, BH, BLMH)

Specific

peplomycin phleomycin

General

antibacterial glycopeptide antibiotic antineoplastic agent sclerosing agent

Properties

MOTIF: glycosylation site MISC-INFO: elimination route KIDNEY 1/2life 3-6 HOURS

References

  1. Merck Index 10th ed. 1983
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 533
  5. Medical Knowledge Self Assessment Program (MKSAP) 15, 16, 17. American College of Physicians, Philadelphia 2009, 2012, 2015
  6. Sleijfer S. Bleomycin-induced pneumonitis. Chest. 2001 Aug;120(2):617-24. PMID: 11502668
  7. Deprecated Reference
  8. Martin WG, Ristow KM, Habermann TM et al Bleomycin pulmonary toxicity has a negative impact on the outcome of patients with Hodgkin's lymphoma. J Clin Oncol. 2005 Oct 20;23(30):7614-20. PMID: 16186594

Component-of

doxorubicin (Adriamycin)/bleomycin/vinblastine/dacarbazine (ABVD)

Databases & Figures

PUBCHEM correlations Therapeutic Inducers of Apoptosis