Nitrosoureas
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Oncology Pharm
- Bleomycin
- Dactinomycin, Actinomycin D
- Doxorubicin, Daunorubicin
- Azathioprine, 6-MP
- Cladribine
- Cytarabine
- Busulfan
- Cyclophosphamide, Ifosfamide
- Nitrosoureas
- Paclitaxel
- Vincristine, Vinblastine
- Cisplatin, Carboplatin, Oxaliplatin
- Etoposide, Teniposide
- Irinotecan, Topotecan
- Bevacizumab
- Erlotinib
- Cetuximab, Panitumumab
- Imatinib, Dasatinib
- Rituximab
- Bortezomib, Carfilzomib
- Trastuzumab
- Dabrafenib, Vemurafenib
- Raloxifene and Tamoxifen
- Hydroxyurea
- Procarbazine
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