Classifications: antineoplastic; alkylating agent; Therapeutic: antineoplastic
Pregnancy Category: D
10 mg, 40 mg, 100 mg capsules
Lipid-soluble alkylating nitrosourea with actions like those of carmustine (e.g., cell-cycle-nonspecific activity against
rapidly proliferating cell populations). Inhibits synthesis of both DNA and RNA.
Has antineoplastic and myelosuppressive effect.
Palliative therapy in addition to other modalities or with other chemotherapeutic agents in primary and metastatic brain
tumors and as secondary therapy in Hodgkin's disease.
GI, lung, and renal carcinomas, non-Hodgkin's lymphomas, malignant melanoma, and multiple myelomas.
Immunization with live virus vaccines, viral infections; severe bone marrow suppression; active infection; pregnancy (category
Patients with decreased circulating platelets, leukocytes, or erythrocytes; kidney or liver function impairment; previous
cytotoxic or radiation therapy; pulmonary disease.
Route & Dosage
Adult: PO 130 mg/m2 as single dose, repeated in 6 wk; subsequent doses based on hematologic response (WBC >4000/mm3, platelets >100,000/mm3)
Child: PO 75150 mg/m2 q6wk
- Give on an empty stomach to reduce possibility of nausea, may also give an antiemetic before drug to prevent nausea.
- Store capsules away from excessive heat (over 40° C).
Adverse Effects (≥1%)CNS:
Lethargy, ataxia, disorientation. GI:
Anorexia, nausea, vomiting, stomatitis
, transient elevations of LFTs. Hematologic:
Delayed (cumulative) myelosuppression
: (thrombocytopenia, leukopenia
. Skin: Alopecia
, skin rash, itching. Urogenital:
Nephrotoxicity. Respiratory: Pulmonary toxicity
can increase bone marrow toxicity
increase risk of bleeding.
Readily absorbed from GI tract. Peak:
16 h. Distribution:
Readily crosses bloodbrain barrier; crosses placenta; distributed into breast milk. Metabolism:
In liver to several active metabolites. Elimination:
In urine. Half-Life:
Assessment & Drug Effects
- Lab tests: Monitor blood counts weekly for at least 6 wk after last dose. Liver and kidney function tests should be performed
- A repeat course is not given until platelets have returned to above 100,000/mm3 and leukocytes to above 4000/mm3.
- Avoid invasive procedures during nadir of platelets.
- Thrombocytopenia occurs about 4 wk and leukopenia about 6 wk after a dose, persisting 12 wk.
- Inspect oral cavity daily for S&S of superinfections (see Appendix F) and stomatitis or xerostomia.
Patient & Family Education
- Nausea and vomiting may occur 35 h after drug administration, usually lasting less than 24 h.
- Anorexia may persist for 2 or 3 d after a dose.
- Notify physician of signs of sore throat, cough, fever. Also report unexplained bleeding or easy bruising.
- Use reliable contraceptive measures during therapy.
- Be aware of the possibility of hair loss while taking this drug.
- A given dose may include capsules of different colors; the pharmacist prepares prescribed dose by combining various capsule