The precise mechanism by which altretamine exerts its anti-cancer effect is unknown but it is classified by MeSH as an alkylating antineoplastic agent.
This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediatedN-demethylation. Administered orally, altretamine is extensively metabolized on first pass, producing primarily mono- and didemethylated metabolites. Additional demethylation reactions occur in tumor cells, releasingformaldehyde in situ before the drug is excreted in the urine. Thecarbinolamine (methylol) intermediates of CYP450-mediated metabolism also can generate electrophilic iminium species that are capable of reacting covalently with DNA guanine and cytosine residues as well as protein. Iminium-mediated DNA cross-linking and DNA-protein interstrand cross-linking, mediated through both the iminium intermediate and formaldehyde, have been demonstrated, although the significance of DNA cross-linking on altretamine antitumor activity is uncertain.
What side effects may I notice from receiving this medicine? Side effects that you should report to your doctor or health care professional as soon as possible:
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• Hair loss
• Loss of appetite
• Stomach upset
What special precautions should I follow?
Before taking altretamine,
- tell your doctor and pharmacist if you are allergic to altretamine, any other medications, or any of the ingredients in altretamine capsules. Ask your pharmacist for a list of the ingredients.
- tell your doctor and pharmacist what other prescription and nonprescription medications, vitamins, nutritional supplements, and herbal products you are taking or plan to take. Be sure to mention any of the following: cimetidine (Tagamet), isocarboxazid (Marplan), phenelzine (Nardil), pyridoxine (Vitamin B6) and tranylcypromine (Parnate). tell your doctor if you have ever received or taken certain chemotherapy medications such as bendamustine (Treanda), cisplatin (Platinol), carmustine (BiCNU, Gliadel Wafer), cyclophosphamide (Cytoxan), ifosfamide (Ifex), lomustine (CeeNU), melphalan (Alkeran), procarbazine (Mutalane), temozolomide (Temodar), or thioguanine. Your doctor may need to monitor you carefully for side effects.
- tell your doctor if you have nervous system disorders or blood disorders. Your doctor may tell you not to take altretamine.
- tell your doctor if you are pregnant, plan to become pregnant, or are breast-feeding. You should not become pregnant or breast-feed while you are taking altretamine. If you become pregnant while taking altretamine, call your doctor. Altretamine may harm the fetus.