bleomycin (Blenoxane)
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Introduction
Tradename: Blenoxane.
Indications
- treatment & management of malignancies
- squamous cell carcinomas of the head & neck
- squamous cell carcinomas of the penis & cervix
- testicular cancer
- Hodgkin's disease & non-Hodgkin's lymphoma
- sarcomas (including lymphomas)
- germ cell neoplasm[7]
- sclerosing agent
Dosage
- test dose of 1-2 units in 50 mL IV over 15 minutes
- 10-20 units/m2* weekly or every other week IV/IM/SC
- 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:
- stable for 24 hours reconstituted at room temperature
- stable for 24-48 hours reconstituted & refrigerated
- stability decreases iin PVC bags
- incompatible with amino acid solutions, ascorbic acid, cefazolin, furosemide, diazepam, hydrocortisone, mitomycin, nafcillin, penicillin G, aminophylline
- 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
- 50-70% of the drug is eliminated into the urine unchanged
- metabolized drug is degraded by cellular enzymes
elimination via kidney
1/2life = 3-6 hours
Adverse effects
- common (> 10%)
- systemic:
- skin, mucous membranes & skin appendages
- erythema, induration, hyperkeratosis, peeling of skin, hyperpigmentation, alopecia#, nailbed changes
- less common (1-10%)
- weight loss, anaphylactoid reactions in 1% of patients with lymphoma
- uncommon (< 1%)
- myocardial infarction, renal toxicity, stroke, hepatotoxicity, skin thickening, dyspnea, tachypnea, non-productive cough, rales
- other
- 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]
- mild myelosuppression (rare)
- onset 7 days
- nadir 14 days
- recovery 21 days
- pain at tumor site
- Raynaud's phenomenon
- phlebitis
- pneumonitis resulting in pulmonary fibrosis with cumulative dose > 150 units/m2*, > 400 units or < 30 units/single dose
# alopecia should resolve after discontinuation of drug
* meter squared body surface area
Drug interactions
- radiation therapy may increase pulmonary toxicity of bleomycin
- vinblastine in combination may cause Raynaud's syndrome
- cisplatin
- digoxin
- phenytoin
- vincristine
- drug interaction(s) anticonvulsants with anti-bacterial agents
- drug interaction(s) of antibiotics with warfarin
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
More general terms
More specific terms
Additional terms
Component of
References
- ↑ Merck Index 10th ed. 1983
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Harrison's Principles of Internal Medicine, 14th ed. Fauci et al (eds), McGraw-Hill Inc. NY, 1998, pg 533
- ↑ 5.0 5.1 5.2 Medical Knowledge Self Assessment Program (MKSAP) 15, 16, 17. American College of Physicians, Philadelphia 2009, 2012, 2015
- ↑ 6.0 6.1 Sleijfer S. Bleomycin-induced pneumonitis. Chest. 2001 Aug;120(2):617-24. PMID: https://www.ncbi.nlm.nih.gov/pubmed/11502668
- ↑ 7.0 7.1 7.2 Deprecated Reference
- ↑ 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: https://www.ncbi.nlm.nih.gov/pubmed/16186594