Altretamine


Concise Prescribing Info
Indications/Uses
Palliative treatment of ovarian carcinoma.
Dosage/Direction for Use
Adult : 260 mg/m2/day in 4 divided doses, for 14 or 21 consecutive days out of a 28-day cycle, up to 12 cycles. Therapy should be temporarily discontinued for ≥14 days prior to restarting at 200 mg/m2/day if AR occur.
Dosage Details
Oral
Palliative treatment of ovarian carcinoma
Adult: 260 mg/m2 daily in 4 divided doses, for 14 or 21 consecutive days out of a 28-day cycle, up to 12 cycles. If WBC count is <2,000/mm3, granulocyte count is <1,000/mm3, platelet count is <75,000/mm3, or if neurotoxicity or intolerable GI symptoms occur, therapy should be temporarily discontinued for ≥14 days prior to restarting at 200 mg/m2 daily.
Administration
Should be taken with food.
Contraindications
Pre-existing severe bone marrow depression, severe neurologic toxicity. Lactation. Concomitant use w/ antidepressants of the MAOI class.
Special Precautions
Patient previously treated w/ other myelosuppressive agents. Pregnancy.
Adverse Reactions
Bone marrow depression, manifested by leucopenia, thrombocytopenia, anaemia; nausea, vomiting, peripheral (e.g. neuropathy) and central (e.g. ataxia, depression, confusion, drowsiness, hallucination, mood disorder, dizziness, vertigo) neurotoxicity. Rarely, rashes, pruritus, alopecia, hepatotoxicity.
Patient Counseling Information
This drug is an irritant, avoid contact w/ skin or mucous membranes.
MonitoringParameters
Perform peripheral blood counts at least mthly, prior to initiation of each course of therapy and as clinically indicated. Monitor neurologic function regularly. Monitor for GI upset and anaemia.
Drug Interactions
Reduced activity w/ pyridoxine. Increased half-life and toxicity w/ inhibitors of microsomal metabolism (e.g. cimetidine).
Potentially Fatal: May cause severe orthostatic hypotension w/ antidepressants of the MAOI class (e.g. phenelzine).
Action
Description: Altretamine, a synthetic triazine derivative, is a cytotoxic antineoplastic agent structurally similar to triethylenemelamine, although its mode of action may be different. While its cytotoxic effect is not fully characterised, it is theorised that its activated oxidative N-demethylation metabolites bind to and damage DNA.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. Time to peak plasma concentration: 0.5-3 hr.
Distribution: Distributed into tissues high in lipid content and tumour tissues.
Metabolism: Rapidly and extensively metabolised in the liver via oxidative N-demethylation into pentamethylmelamine and tetramethylmelamine.
Excretion: Via urine (90%, mainly as metabolites and <1% as unchanged drug). Elimination half-life: 4-10 hr.
Chemical Structure

Chemical Structure Image
Altretamine

Source: National Center for Biotechnology Information. PubChem Database. Altretamine, CID=2123, https://pubchem.ncbi.nlm.nih.gov/compound/Altretamine (accessed on Jan. 20, 2020)

Storage
Store at or below 25°C.
ATC Classification
L01XX03 - altretamine ; Belongs to the class of other antineoplastic agents. Used in the treatment of cancer.
References
Anon. Altretamine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 22/07/2016.

Buckingham R (ed). Altretamine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 22/07/2016.

Hexalen Capsule (Eisai Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 22/07/2016.

Hexalen Capsule (MGI Pharma, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 22/07/2016.

McEvoy GK, Snow EK, Miller J et al (eds). Altretamine. AHFS Drug Information (AHFS DI) [online]. American Society of Health-System Pharmacists (ASHP). https://www.medicinescomplete.com. Accessed 22/07/2016.

Disclaimer: This information is independently developed by MIMS based on Altretamine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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