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lomustine (CCNU, CeeNU, Belustine)

Tradename: CeeNu. Indications: 1) brain tumors (astrocytoma, glioblastoma multiforme [3]) 2) Hodgkin's disease 3) non-Hodgkin's lymphoma 4) advanced lung cancer 5) gastrointestinal carcinomas 6) multiple myeloma 7) stem cell transplantation Dosage: 1) 100-130 mg/m2 once every 6 weeks 2) reduce dose 25% for creatinine clearance of 10-50 mL/min 3) 50% reduction in dosage if creatinine clearance < 10 mL/min Capsule: 10, 40, 100 mg. Pharmacokinetics: 1) well absorbed orally 2) distributes to all tissues 3) concentrated in the CSF 4) metabolized by the liver 5) eliminated in the urine 6) dose reductions recommended in renal dysfunction 7) 1/2life is approximately 70 hours 8) not dialyzable Adverse effects: 1) common (> 10%) a) nausea/vomiting - occurs 3-6 hours after oral administration - emetic potential high - 60-90% < 60 mg - > 90% > 60 mg b) myelosuppression - onset 14 days - nadir 4-5 weeks - recovery 6 weeks 2) less common (1-10%) - anemia, neurotoxicity, renal failure, stomatitis, diarrhea skin rash, alopecia 3) 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: 1) cimetidine may increase myelosuppression 2) phenobarbital Mechanism of action: 1) alkylating agent 2) interferes with DNA & RNA synthesis

Interactions

drug adverse effects of alkylating agents

General

alkylating agent nitrosourea

Properties


Database Correlations

PUBCHEM cid=3950

References

  1. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  2. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. 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 PMID: 29141164 http://www.nejm.org/doi/full/10.1056/NEJMoa1707358

Component-of

lomustine/procarbazine/vincristine (PCV)