altretamine (Discontinued)

Brand and Other Names:Hexalen
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

capsule

  • 50mg

Recurrent Ovarian Cancer

Indicated for recurrence following alkylating agent or cisplatin treatment

260 mg/m²/day PO divided q6hr for 14-21 days of a 28-day cycle  

Dosage Modifications

Renal or hepatic impairment: Dose adjustment not required

Temporarily hold and restart at 200 mg/m²/day if any of the following develop

  • GI intolerance unresponsive to symptomatic treatment
  • WBC <2000/mm³ or granulocytes <1000/mm³
  • Platelets <75,000/mm³
  • Progressive neurotoxicity

Safety and efficacy not established

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Interactions

Interaction Checker

and altretamine

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse 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

            Vertigo

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            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

            Cautions

            Neurotoxic-perform regular neurologic exams

            Previous treatment with other myelosuppressive drugs or pre-existing neurotoxicity

            Discontinue indefinitely if neurologic symptoms persist on reduced dose

            Risk of orthostatic hypotension with concomitant MAO inhibitors, esp in >60 years

            Avoid pregnancy

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            Pregnancy & 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.

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            Pharmacology

            Mechanism of Action

            Unclear, reactive intermediates covalently bind to microsomal proteins & DNA, possibly causing DNA damage

            Metabolism required for cytotoxicity

            Pharmacokinetics

            Absorption: Well absorbed

            Distribution: Highly concentrated in liver, kidney & small intestine

            Protein Bound: Plasma proteins

            Peak Plasma Time: 0.5-3 hr

            Half-life: 7 hr

            Metabolism: Liver; rapid & extensive demethylation to active metabolites

            Excretion: Urine (90%; <1% as unchanged drug)

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            Administration

            Oral Administration

            Administer after meals and at bedtime

            Monitor: Peripheral blood counts at least qMonth

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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.