lomustine (CCNU, CeeNU, Belustine)
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Introduction
Tradename: CeeNu.
Indications
- brain tumors (astrocytoma, glioblastoma multiforme[3])
- Hodgkin's disease
- non-Hodgkin's lymphoma
- advanced lung cancer
- gastrointestinal carcinomas
- multiple myeloma
- stem cell transplantation
Dosage
- 100-130 mg/m2 once every 6 weeks
- reduce dose 25% for creatinine clearance of 10-50 mL/min
- 50% reduction in dosage if creatinine clearance < 10 mL/min
Capsule: 10, 40, 100 mg.
Pharmacokinetics
- well absorbed orally
- distributes to all tissues
- concentrated in the CSF
- metabolized by the liver
- eliminated in the urine
- dose reductions recommended in renal dysfunction
- 1/2life is approximately 70 hours
- not dialyzable
Adverse effects
- common (> 10%)
- nausea/vomiting
- occurs 3-6 hours after oral administration
- emetic potential high
- 60-90% < 60 mg
- > 90% > 60 mg
- myelosuppression
- onset 14 days
- nadir 4-5 weeks
- recovery 6 weeks
- nausea/vomiting
- less common (1-10%)
- uncommon (< 1%)
- hepatotoxicity, alopecia, renal failure, pulmonary fibrosis with cumulative doses > 600 mg, disorientation, lethargy, ataxia, dysarthria
Toxicity:
- No known antidotes
- Treatment of toxicity is symptomatic & supportive
Drug interactions
- cimetidine may increase myelosuppression
- phenobarbital
Mechanism of action
- alkylating agent
- interferes with DNA & RNA synthesis
More general terms
Component of
References
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ 3.0 3.1 Wick W, Gorlia T, Bendszus M et al Lomustine and Bevacizumab in Progressive Glioblastoma. N Engl J Med 2017; 377:1954-1963. November 16, 2017 <PubMed> PMID: https://www.ncbi.nlm.nih.gov/pubmed/29141164 <Internet> http://www.nejm.org/doi/full/10.1056/NEJMoa1707358