Lomustine

Indications
 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: 75-150 mg/m2 as a single dose every 6 wk. Readjust dose according to platelet and leukocyte counts.
CrCl (ml/min)Dosage Recommendation
10-50Admin 75% of normal dose.
<10Admin 25-50% of normal dose.


Special Populations: Dosage adjustment in renal impairment: CrCl 10-50 mL/min: 75% of normal dose; <10 mL/min: 50% of normal dose.
Contraindications
 Pregnancy and lactation.
Warnings / Precautions
 Monitor CBC with differential platelet count wkly for at least 6 wk after a dose. Periodically perform pulmonary function studies and LFTs.
Adverse Reactions
 Pulmonary infiltrates, pulmonary fibrosis, nausea, vomiting, hepatotoxicity, nephrotoxicity, stomatitis, alopecia, disorientation, lethargy, dysarthria, ataxia, visual disturbances.
Potentially Fatal: Delayed bone marrow suppression and permanent marrow damage following prolonged use.
Overdose Reactions
 Symptoms: Pancytopenia, hepatic dysfunction, abdominal pain, pulmonary toxicity with tachypnoea and hypoxaemia, confusion and disorientation. Severe myelosuppression. Management: Symptomatic and supportive.
Drug Interactions
 Increased levels/effects with CYP2D6 inhibitors.
See Below for More lomustine Drug Interactions
Mechanism of Actions
 Lomustine inhibits the synthesis of DNA and RNA via alkylation although carbamoylation and modification of cellular proteins may also be involved.
Absorption: Rapidly absorbed from the GI tract (oral); also absorbed after topical application. Peak plasma concentrations of metabolites after 1-6 hr (oral).
Distribution: Widely distributed; drug and metabolites cross the blood-brain barrier; active metabolites appear in CSF within 30 min (oral); metabolites present in milk.
Metabolism: Hepatic via hydroxylation; enterohepatically recycled.
Excretion: Via urine (approx 50%); via faeces (<5%); via expired air (<10%).
Administration
 Should be taken on an empty stomach. (Take on an empty stomach. May be taken at bedtime to reduce occurrence of nausea.)
Storage Conditions
 Oral: Store at 15-30°C (59-86°F).
ATC Classification
 L01AD02 - lomustine ; Belongs to the class of alkylating agents, nitrosoureas. Used in the treatment of cancer.
Storage
 Oral: Store at 15-30°C (59-86°F).
Available As
  • Lomustine 40 mg

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