Altretamine
Gale Encyclopedia of Cancer:
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Altretamine
Key Terms: Antiemetic.
Definition
Altretamine, also known by the brand name Hexalen, is an anticancer agent used to treat ovarian cancer.
Purpose
Altretamine is used to treat persistent or recurrent ovarian cancer, usually after treatment of the cancer with cisplatin and/or an alkylating agent fails to effectively treat the tumor.
Description
The mechanism of action of altretamine is not known. However, it is thought that it may inhibit DNA and RNA synthesis.
Recommended Dosage
Alretamine is administered orally. Doses for the drug may be different depending on the protocol that is used by the physician. Some example dosing regimens are: 4 to 12 mg per kg in three to four divided doses for 21 to 90 days; 240 to 320 mg per square meter of body surface area in three to four divided doses for 21 days, repeated every six weeks; 260 mg per square meter of body surface area per day for 14 to 21 days of a 28 days cycle in four divided doses; or 150 mg per square meter of body surface area in three to four divided doses for 14 days of a 28 day cycle. The dose of altretamine may be decreased if the patient has intolerable stomach side effects, low blood count of cells that fight infection (white blood cells) or cells that prevent bleeding (platelets), or if the patient has progressive toxicity affecting the nerves of the brain and body.
Precautions
Caution is usually taken in prescribing altretamine to patients with decreased kidney or liver function or damage to nerves due to previous chemotherapy. Careful monitoring of nerve, kidney, and liver function is required for these patients.
Pregnant women should be warned before taking this drug, as it may cause permanent harm to the fetus. Women who are of childbearing age should apply contraceptive methods to avoid pregnancy until they have discontinued drug use. Altretamine may also affect fertility. Additionally, although it is not known whether this drug is excreted in the breast milk, nursing mothers are cautioned not to breast feed while being treated with altretamine.
Side Effects
Nausea and vomiting may gradually occur as patients receive continuous high dose of altretamine. In most instances, antiemetics can help control these side effects. However, some patients may experience severe nausea and vomiting that requires either reducing the dose or stopping treatment with altretamine. Other common side effects include loss of appetite (anorexia) and diarrhea. Patients may also experience nerve toxicity, which is described as numbness, tingling, and burning sensations in the fingers and toes. Patients can also have difficulty walking because of these sensation changes. Patients may also commonly experience: thrombocytopenia, a decrease of the platelet cells responsible for blood clotting; anemia, a decrease of the red blood cells responsible for oxygen transport to tissues and organs; and leukopenia, a decrease of the white blood cells responsible for fighting infections. Less common side effects include seizures, depression, dizziness, stomach cramps, liver toxicity, rash, and hair loss (alopecia).
Interactions
Persons taking altretamine and monoamine oxidase inhibitors (MAO inhibitors) may experience severe hypotension (low blood pressure) when standing up. Additionally, the drug cimetidine may increase the toxicity of altretamine. Prior to starting any over-the-counter medications, herbal medications, or new medications, patients should consult with their physician, nurse, or pharmacist to ensure that there are no potential drug interactions.
—Michael Zuck, Ph.D.
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Altretamine
Drug Info:
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Altretamine
Brand names: Hexalen®
Chemical formula:
- Drug Forms:
- Altretamine capsules (below)
- Altretamine Oral capsule
Altretamine capsules
What are altretamine capsules?
ALTRETAMINE (Hexalen®) is a type of chemotherapy for treating ovarian cancer. Altretamine interferes with the way cancer cells grow. Generic altretamine capsules are not yet available.What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:• blood disorders
• dental disease
• loss of feeling, pain or numbness in the hands or feet
• recent radiation therapy
• infection (especially virus infection such as chickenpox or herpes)
• an unusual or allergic reaction to altretamine, other chemotherapy, other medicines, foods, dyes, or preservatives
• pregnant or trying to get pregnant
• breast-feeding
How should I take this medicine?
Take altretamine capsules by mouth. Follow the directions on the prescription label. Swallow the capsules with a drink of water. If altretamine upsets your stomach, take it after meals. Take your doses at regular intervals. Do not take your medicine more often than directed. Finish the full course prescribed by your doctor or health care professional, even if the capsules make you feel unwell. Do not stop taking except on your prescriber's advice.Contact your pediatrician or health care professional regarding the use of this medicine in children. Special care may be needed.
What if I miss a dose?
If you miss a dose, take it as soon as you can. If it is almost time for your next dose, take only that dose. Do not take double or extra doses. If you vomit after taking a dose, call your prescriber or health care professional for advice.What drug(s) may interact with altretamine?
• cimetidine• live virus vaccines
• phenobarbital
Tell your prescriber or health care professional about all other medicines you are taking, including nonprescription medicines, nutritional supplements, or herbal products. Also tell your prescriber or health care professional if you are a frequent user of drinks with caffeine or alcohol, if you smoke, or if you use illegal drugs. These may affect the way your medicine works. Check with your health care professional before stopping or starting any of your medicines.
What should I watch for while taking altretamine?
Visit your prescriber or health care professional for regular checks on your progress.Altretamine may make you feel generally unwell. This is not uncommon because altretamine affects good cells as well as cancer cells. Report any side effects as above, but continue your course of medicine even though you feel ill, unless your prescriber or health care professional tells you to stop.
While you are taking altretamine, you will be more susceptible to infection. Try to avoid people with colds, flu, and bronchitis. Do not have any vaccinations without your prescriber's approval and avoid anyone who has recently had oral polio vaccine.
Call your prescriber or health care professional for advice if you get a fever, chills or sore throat. Do not treat yourself.
Altretamine can cause blood problems. This can mean slow healing and a risk of infection. Try to avoid cutting or injuring yourself. Problems can arise if you need dental work, and in the day to day care of your teeth. Try to avoid damage to your teeth and gums when you brush or floss your teeth.
What side effects may I notice from taking altretamine?
Side effects that you should report to your prescriber or health care professional as soon as possible:• black tarry stools
• blood in urine
• confusion, agitation, clumsiness
• depression
• fever or chills, sore throat
• lower back pain
• pain or difficulty passing urine
• red spots on the skin
• seizures (convulsions)
• tingling, pain or numbness in the hands or feet
• unusual bleeding or bruising
• unusual tiredness or weakness
• vomiting
Side effects that usually do not require medical attention (report to your prescriber or health care professional if they continue or are bothersome):
• diarrhea
• loss of appetite
• nausea
• stomach pains or cramps
Where can I keep my medicine?
Keep out of the reach of children in a container that small children cannot open.Store at room temperature between 15 and 30 degrees C (59 and 86 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
Mosby's Dental Dictionary:
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altretamine
n
trade name: Hexalen; drug class: antineoplastic; action: products of metabolism interact with tissue macromolecules, including DNA, which may be responsible for cytotoxicity; uses: palliative treatment of recurrent, persistent ovarian cancer.
Wikipedia on Answers.com:
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Altretamine
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| Systematic (IUPAC) name | |
| N2,N2,N4,N4,N6,N6-hexamethyl-1,3,5-triazine-2,4,6-triamine | |
| Clinical data | |
| AHFS/Drugs.com | monograph |
| MedlinePlus | a601200 |
| Pregnancy cat. | D (US) |
| Legal status | ℞-only (US) |
| Pharmacokinetic data | |
| Protein binding | 94% |
| Half-life | 4.7-10.2 hours |
| Identifiers | |
| CAS number | 645-05-6  |
| ATC code | L01XX03 |
| PubChem | CID 2123 |
| DrugBank | DB00488 |
| ChemSpider | 2038 |
| UNII | Q8BIH59O7H |
| KEGG | D02841 |
| ChEBI | CHEBI:24564 |
| ChEMBL | CHEMBL1455 |
| Chemical data | |
| Formula | C9H18N6 |
| Mol. mass | 210.28 g/mol |
| SMILES | eMolecules & PubChem |
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Altretamine (also hexalen) is an antineoplastic agent. It was approved by the FDA in 1990.
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Contents
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Uses
It is used to treat refractory ovarian cancer.
It is not considered a first-line treatment,[1] but it can be useful as salvage therapy.[2] It also has the advantage of being less toxic than other drugs used for treating refractory ovarian cancer.[3]
Mechanism
The precise mechanism by which altretamine exerts its anti-cancer effect is unknown but it is classified by MeSH as an alkylating antineoplastic agent.[4] This unique structure is believed to damage tumor cells through the production of the weakly alkylating species formaldehyde, a product of CYP450-mediated N-demethylation. Administered orally, altretamine is extensively metabolized on first pass, producing primarily mono- and didemethylated metabolites. Additional demethylation reactions occur in tumor cells, releasing formaldehyde in situ before the drug is excreted in the urine. The carbinolamine (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.[5]
Side effects
Side effects include nausea, vomiting, anemia and peripheral sensory neuropathy.[6]
Interactions
Combination with pyridoxine (vitamin B6) decreases neurotoxicity but has been found to reduce the effectiveness of an altretamine/cisplatin regime. MAO inhibitor can cause severe orthostatic hypotension when combined with altretamine; and cimetidine can increase its elimination half-life and toxicity.[6]
See also
References
- ^ Keldsen N, Havsteen H, Vergote I, Bertelsen K, Jakobsen A (2003). "Altretamine (hexamethylmelamine) in the treatment of platinum-resistant ovarian cancer: a phase II study". Gynecol. Oncol. 88 (2): 118–22. doi:10.1016/S0090-8258(02)00103-8. PMID 12586589.
- ^ Chan JK, Loizzi V, Manetta A, Berman ML (2004). "Oral altretamine used as salvage therapy in recurrent ovarian cancer". Gynecol. Oncol. 92 (1): 368–71. doi:10.1016/j.ygyno.2003.09.017. PMID 14751188.
- ^ Malik IA (2001). "Altretamine is an effective palliative therapy of patients with recurrent epithelial ovarian cancer". Jpn. J. Clin. Oncol. 31 (2): 69–73. doi:10.1093/jjco/hye012. PMID 11302345.
- ^ Damia G, D'Incalci M (1995). "Clinical pharmacokinetics of altretamine". Clinical pharmacokinetics 28 (6): 439–48. doi:10.2165/00003088-199528060-00002. PMID 7656502.
- ^ "Foy`s principles of Medical chemistry", edited by Thomas L. Lemke, sixth edition, 2008, pages=1162, ISBN=978-0-7817-6879-5.
- ^ a b Drugs.com: Altretamine Monograph
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Gale Encyclopedia of Cancer
Gale Encyclopedia of Cancer. Copyright © 2006 by The Gale Group, Inc. All rights reserved.
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Saunders Veterinary Dictionary
Saunders Comprehensive Veterinary Dictionary 3rd Edition. Copyright © 2007 by D.C. Blood, V.P. Studdert and C.C. Gay, Elsevier. All rights reserved.
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Mosby's Dental Dictionary
Mosby's Dental Dictionary. Copyright © 2004 by Elsevier, Inc. All rights reserved.
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