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Why Would I Use Methadone?

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Updated June 12, 2008

Why Would I Use Methadone? Photo © Medioimages/Photodisc/Getty Images
Question: Why Would I Use Methadone?
Methadone -- isn’t that the drug for heroine addicts?

That’s a question I’m accustomed to hearing from leery patients and families when I inform them that their physician has ordered Methadone for pain. While it’s true that methadone is used to treat narcotic withdrawal symptoms, methadone is also a very effective medication to treat moderate to severe pain.

Morphine has earned the title of the Gold Standard for pain control, the opioid all others are compared with because of its effectiveness, ease of administration and low cost. If morphine is so great, why would we ever use methadone?

Answer:

If we’re going to start comparing methadone with morphine, we need to start with the basic principles of pain. Pain can be divided into two types of physiological explanations: nociceptive and neuropathic. Nociceptive pain is generally caused by tissue injury (somatic pain) or injury to internal organs (visceral pain). Neuropathic pain is caused by injury or insult to nerves in either the central nervous system or the peripheral body.

We are blessed with opiate receptors in our brains that allow our bodies to respond to opioid pain medications. The majority of these receptors are classified at mu and delta receptors and a smaller percentage are NMDA. Nociceptive pain is primarily mediated by the mu receptors and neuropathic pain by delta and NMDA receptors; morphine binds to mu receptors only, while methadone binds to mu, delta and NMDA. Morphine does an excellent job of treating many types of pain, but because of its ability to bind to 100% of opiate receptors, methadone may do it even better.

Opiate Toxicity and Side Effects

Opiates, such as morphine, produce metabolites when they are broken down within the body. These metabolites can build up in the body and cause symptoms of opiate toxicity. Opiate toxicity is essentially an overdose of an opiate leading to poisonous levels in the body and causes symptoms such as restlessness, hallucinations, tremors and lethargy.

Methadone doesn’t produce metabolites and therefore doesn’t have a “ceiling," or maximum dose. Methadone is also easier to metabolize by the liver, and its lack of metabolites makes it an excellent choice of pain medication for many patients with decreased liver function or renal failure.

Common side effects of opiates include constipation, nausea and vomiting, drowsiness, itching, confusion and respiratory depression (difficulty breathing). Many patients have reported a decrease in adverse affects after switching to methadone from another opiate.

More Benefits of Methadone

So methadone is more effective than morphine at treating pain and typically causes less adverse effects, but the good news doesn’t stop there. Another benefit of methadone is its extended half-life. A half-life is the time required for half the quantity of a drug to be metabolized or eliminated by normal biological processes. Because of this extended half-life, methadone has a pain-relieving effect of 8 to 10 hours, while regular nonextended release morphine only relieves pain for 2 to 4 hours. This translates into less frequent dosing for the patient, usually two or three times a day.

And last, but not least, methadone is extremely cost-effective. A typical month supply of methadone costs about $8, while morphine will typically cost over $100. Other opiates, such as Oxycontin and Fentanyl, will cost even more.

Barriers to Methadone Use

Do I have you convinced that methadone is a great medication for pain? If so, you may find yourself wondering why it’s not used more often. I’ve asked the same question to several physicians, and I’ve found that beyond the stigma that methadone carries, many physicians just aren’t comfortable prescribing it.

Because of methadone’s extended half-life, it slowly builds up in the body and may take 5 to 7 days for levels to stabilize. During this time, the patient needs to be monitored closely for signs of toxicity. This is generally not a problem for patients on palliative or hospice care, because they are already being followed closely and usually have access to nurses and physicians 24 hours a day. A typical doctor's office doesn’t have the capacity to monitor patients that closely, which may be part of their hesitation to prescribe it.

Other barriers are physician education and patient’s reluctance. Methadone is still widely known as the drug for drug addicts. That stigma is slowly being chipped away at as physicians continue to educate their peers on its benefits and the public sees more and more patients finding relief because of it.

Sources:

Ayonrinde OT, Bridge DT. The rediscovery of methadone for cancer pain management. Med J Aust 2000;173:536-40.

Davis MP, Walsh D. Methadone for relief of cancer pain: a review of pharmacokinetics, pharmacodynamics, drug interactions and protocols of administration. Support Care Cancer 2001;9:73-83.

Toobs JD, Kral, LA. Methadone Treatment for Pain States. Am Fam Physician 2005;71:1353-8.

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