Absorption: Rapidly converted to MTIC, the active metabolite.
Distribution: Unknown.
Metabolism/Excretion: Further metabolism results in the formation of methylhydrazine, which is responsible for most activity.
Half-life: 1.8 hr.
(effect on blood counts)
| ROUTE | ONSET | PEAK | DURATION |
|---|---|---|---|
| PO/IV (WBC) | unknown | 28 days (range 144 days) | 14 days |
| PO/IV (platelets) | unknown | 26 days (range 2140 days) | 14 days |
Contraindicated in:
Use Cautiously in:
CNS: SEIZURES, fatigue, headache, abnormal coordination, anxiety, depression, dizziness, drowsiness, mental status changes, weakness.
EENT: abnormal vision, diplopia.
Resp: cough.
CV: peripheral edema.
GI: HEPATOTOXICITY, nausea, vomiting, abdominal pain, anorexia, constipation, diarrhea, dysphagia.
Derm: pruritus, rash.
Endo: adrenal hypercorticism.
Hemat: leukopenia, thrombocytopenia, anemia.
Metab: ↑weight.
MS: abnormal gait, back pain.
Neuro: hemiparesis, myalgia.
Misc: breast pain (women), fever, injection site reactions, pain at injection site, secondary malignancies (rare).
Drug-Drug:
(Generic available)
1.5 x 109/L, a platelet count of
100 x 109/L and common toxicity criteria (CTC) non-hematological toxicity
Grade 1 (except for alopecia, nausea and vomiting). Obtain CBC weekly. If ANC is
0.5 and <1.5 x 109/L or platelet count is
10 and <100 x 109/L or CTC is Grade 2 during any cycle, interrupt therapy until ANC and platelet count have returned to above parameters. If ANC <0.5 x 10 9/L or platelet count is <10 x 10 9/L or CTC is Grade 3 or 4, discontinue therapy. For the Maintenance Phase, see manufacturer's recommended dosing guidelines. Anaplastic astrocytomaObtain CBC on Day 22 (21 days after first dose) or within 48 hr of that day, and weekly until ANC is above 1.5 x 109/L and platelet count exceeds 100 x 109/L. If the ANC falls to <1.0 x 109/L or the platelet count is <50 x 109/L during any cycle, the next cycle should be reduced by 50 mg/m2, but not below 100 mg/m2, the lowest recommended dose. See manufacturer's recommendations for specific guidelines. Women and geriatric patients are at greater risk for developing myelosuppression. Nadir for thrombocytopenia usually occurs at 26 days and for neutropenia usually occurs at 28 days. Recovery usually occurs within 14 days of the nadir.
1.5 x 109/L and platelet count exceeds 100 x 109/L.IV Administration:
NDC Code*