Lomustine
Indications
Lomustine is used for:
Brain tumours, Hodgkin's disease, Lung cancer, Malignant melanoma
Adult Dose
Oral
Brain tumours; Hodgkin's disease, resistant or relapsed; Malignant melanoma; Lung cancer
Adult: 100-130 mg/m2 as a single dose every 6 wk. Adjust dose according to platelet and leukocyte counts.
Compromised marrow function: 100 mg/m2 as a single dose every 6 wk.
Child Dose
Oral
Brain tumours; Hodgkin's disease, resistant or relapsed; Malignant melanoma; Lung cancer
Child: 75-150 mg/m2 as a single dose every 6 wk. Readjust dose according to platelet and leukocyte counts.
Renal Dose
Renal impairment:
CrCl (ml/min) Dosage Recommendation
10-50 Admin 75% of normal dose.
<10 Admin 25-50% of normal dose.
Administration
Should be taken on an empty stomach. Take on an empty stomach. May be taken at bedtime to reduce occurrence of nausea.
Contra Indications
Pregnancy and lactation.
Precautions
Monitor CBC with differential platelet count wkly for at least 6 wk after a dose. Periodically perform pulmonary function studies and LFTs.
Lactation: Unknown if metabolites present in breast milk; avoid nursing during treatment and for 2 weeks after final dose
Pregnancy-Lactation
Interactions
Increased levels/effects with CYP2D6 inhibitors.
Adverse Effects
Side effects of Lomustine :
>10%
Nausea (54%), Vomiting (54%)
1-10%
Neurotoxicity, Myelosuppression (delayed 4-5 weeks)
Frequency Not Defined
Ataxia, Lethargy, Disorientation, Stomatitis, Mucositis, Pulmonary fibrosis (rare), Pulmonary toxicity, Elevated LFTs, Leukemia, Renal toxicity, Hepatic toxicity, Infertility, Alopecia, Optic atrophy (rare)
Potentially Fatal: Delayed bone marrow suppression and permanent marrow damage following prolonged use.
Mechanism of Action
Lomustine inhibits the synthesis of DNA and RNA via alkylation although carbamoylation and modification of cellular proteins may also be involved.