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:
• Allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
• Low blood counts – this medicine may decrease the number of white blood cells, red blood cells and platelets. You may be at increased risk for infections and bleeding.
• Signs of infection – fever or chills, cough, sore throat, pain or difficulty passing urine
• Signs of decreased platelets or bleeding – bruising, pinpoint red spots on the skin, black, tarry stools, blood in the urine
• Signs of decreased red blood cells – unusually weak or tired, fainting spells, lightheadedness
• Muscle weakness
• Pain, tingling, numbness in the hands or feet
• Problems with balance, walking, talking
• Trouble passing urine or change in the amount of urine
• Vomiting Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
• 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.