Lomustine (2 brand names, 1 dosage form, 1 route)
Available dosage forms: CAPSULE.
Routes of administration: ORAL.
Brand Names
- GLEOSTINE
- LOMUSTINE
Boxed Warning
DELAYED MYELOSUPPRESSION Lomustine causes myelosuppression including fatal myelosuppression. Myelosuppression is delayed, dose-related, and cumulative; occurring 4 to 6 weeks after drug administration and persisting for 1 to 2 weeks. Thrombocytopenia is generally more severe than leukopenia. Cumulative myelosuppression from lomustine is manifested by greater severity and longer duration of cytopenias. Monitor blood counts for at least 6 weeks after each dose. Do not give lomustine more frequently than every 6 weeks [see Warnings and Precautions (5.1), Dosage and Administration (2.2, 2.3)] . RISK OF OVERDOSAGE PRESCRIBE, DISPENSE, AND ADMINISTER ONLY ENOUGH CAPSULES FOR ONE DOSE. Fatal toxicity occurs with overdosage of lomustine. Both physician and pharmacist should emphasize to the patient that only one dose of lomustine is taken every 6 weeks [see Dosage and Administration (2.1), Warnings and Precautions (5.2), Overdosage (10)] .
Contraindications
None.
Adverse Reactions
The following serious adverse reactions are discussed in greater detail in other sections of the labeling: Delayed myelosuppression [see Warnings and Precautions (5.1)] Risks of overdosage [see Warnings and Precautions (5.2)] Pulmonary toxicity [see Warnings and Precautions (5.3)] Secondary malignancies [see Warnings and Precautions (5.4)] Hepatotoxicity [see Warnings and Precautions (5.5)] Nephrotoxicity [see Warnings and Precautions (5.6)] The following adverse reactions associated with the use of lomustine were identified in clinical trials or postmarketing reports. Because these reactions were reported from a population of uncertain size, it is not possible to estimate their frequency, reliability, or establish a causal relationship to drug exposure. Gastrointestinal disorders: nausea, vomiting, and stomatitis Ocular disorders: optic atrophy, visual disturbances, and blindness Neurologic disorders: disorientation, lethargy, ataxia, and dysarthria Other: alopecia
Mechanism of Action
Lomustine alkylates DNA and RNA. As with other nitrosoureas, it may also inhibit several key enzymatic processes by carbamoylation of amino acids in proteins.
Overdosage
Overdosage with lomustine has occurred, including fatal cases [see Dosage and Administration (2.1), Warnings and Precautions (5.2)]. Overdosage causes severe myelosuppression, as well as abdominal pain, diarrhea, vomiting, anorexia, lethargy, dizziness, abnormal hepatic function, cough, and shortness of breath. No antidotes exist for lomustine overdosage.