Nitrosoureas
2870
Summary
The nitrosoureas carmustine and lomustine are alkylating agents that crosslink DNA after being bioactivated by P450 enzymes in the liver. These drugs have a unique ability to cross the blood-brain barrier, making them useful for treating brain tumors, but this ability can also lead to CNS toxicity in patients taking these medications.
Key Points
- Nitrosoureas
- Drugs
- Carmustine
- Lomustine
- Mechanism
- Crosslinks DNA
- Requires bioactivation by liver (P450)
- Crosses blood-brain barrier (BBB) into the CNS
- Crosslinks DNA
- Clinical Use
- Brain tumors
- Because it crosses BBB
- Including glioblastoma multiforme
- Brain tumors
- Adverse Effects
- CNS toxicity
- Symptoms including ataxia, convulsions, dizziness
- CNS toxicity
- Drugs