Dosing and uses of Hexalen (altretamine)
Adult dosage forms and strengths
capsule
- 50mg
Recurrent Ovarian Cancer
Indicated for recurrence following alkylating agent or cisplatin treatment
260 mg/sq.meter/day divided QID PO x14-21 days of a 28-day cycle
Other Information
Administration: PC & Hs
Monitor: peripheral blood counts at least qMonth
Dosage adjustment
- Discontinue temporarily and restart at 200 mg/sq.meter/day if any of the following develop
- GI intolerance unresponsive to symptomatic treatment
- WBC <2000/cu.mm or granulocytes <1000/cu.mm
- Platelets <75,000/cu.mm
- Progressive neurotoxicity
Other Indications & Uses
Palliative treatment of persistent or recurrent ovarian cancer following alkylating agent or cisplatin treatment
Pediatric dosage forms and strengths
Safety & efficacy not established
Hexalen (altretamine) adverse (side) effects
>10%
Anemia (33%)
Nausea/vomiting (33%)
Peripheral sensory neuropathy (31%)
Thrombocytopenia (31%)
1-10%
Alk phos increased (9%)
Leukopenia (5%)
Anorexia (1%)
Seizures (1%)
<1%
Alopecia
Rash
Depression
Dizziness
Hepatotoxicity
Tremor
Warnings
Black box warnings
Administer under the supervision of an experienced cancer chemotherapy physician
Bone marrow suppression
- Perform peripheral blood counts routinely before and after drug therapy
Neurotoxicity
- Perform neurologic examinations routinely before and after drug therapy
Contraindications
Hypersensitivity
Pre-existing severe bone marrow suppression or severe neurologic toxicity
Pregnancy
Cautions
Neurotoxic-perform regular neurologic exams
Previous tx w/ other myelosuppressive drugs or pre-existing neurotoxicity
Discontinue indefinitely if neurologic sx persist on reduced dose
Risk of orthostatic hypotension with concomitant MAO inhibitors, esp in >60 yo
Avoid pregnancy
Pregnancy and lactation
Pregnancy category: d
Lactation: excretion in milk unknown/not recommended
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Hexalen (altretamine)
Absorption: well absorbed
Distribution: highly concentrated in liver, kidney & small intestine
Protein Bound: to plasma proteins
Peak Plasma Time: 0.5-3 hr
Metabolism: hepatic; rapid & extensive demethylation to active metabolites
Excretion: urine (90%; <1% as unchanged drug)
Mechanism of action
Unclear, reactive intermediates covalently bind to microsomal proteins & DNA, possibly causing DNA damage
Metabolism required for cytotoxicity
