altretamine (Discontinued)

Brand and Other Names:Hexalen

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

            All Interactions Sort By:
             activity indicator 

            Contraindicated (0)

              Serious - Use Alternative (2)

              • influenza virus vaccine quadrivalent, adjuvanted

                altretamine decreases effects of influenza virus vaccine quadrivalent, adjuvanted by pharmacodynamic antagonism. Avoid or Use Alternate Drug. Immunosuppressive drugs may reduce the immune response to influenza vaccine.

              • ropeginterferon alfa 2b

                ropeginterferon alfa 2b, altretamine. Either increases toxicity of the other by Other (see comment). Avoid or Use Alternate Drug. Comment: Myelosuppressive agents can produce additive myelosuppression. Avoid use and monitor patients receiving the combination for effects of excessive myelosuppression.

              Monitor Closely (3)

              • isavuconazonium sulfate

                altretamine and isavuconazonium sulfate both decrease immunosuppressive effects; risk of infection. Use Caution/Monitor.

              • ofatumumab SC

                ofatumumab SC, altretamine. Either increases effects of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Consider the risk of additive immune system effects when coadministering immunosuppressive therapies with coadministration. When switching from therapies with immune effects, take into account the duration and mechanism of action of these therapies when initiating ofatumumab SC.

              • trastuzumab deruxtecan

                trastuzumab deruxtecan, altretamine. Either increases toxicity of the other by immunosuppressive effects; risk of infection. Use Caution/Monitor. Neutropenia or febrile neutropenia incidence were increased when trastuzumab was coadministered with myelosuppressive chemotherapy. .

              Minor (0)

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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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                Images

                No images available for this drug.
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                Patient Handout

                A Patient Handout is not currently available for this monograph.
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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.