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The Four Molecules of Opiate Detox

2 June 2011 No Comment

Opiate addiction is a growing public health menace and over the years, efforts have been made to help addicts overcoming their opiate dependence. The most successful intervention method is opiate replacement therapy followed by dose reduction until the addict is fully recovered. Once, the only drug used for opiate detox is methadone. In the last decade, new molecules have been introduced and approved to help overcome opiate dependency.

Methadone was introduced in the US in 1947 to treat addicts and help wean them off drugs. Not until 2000 was a new drug, Suboxone, approved for use. Suboxone contains two molecules, buprenorphine and naloxone. Subutex which contains only buprenorphine is also used in opiate detox. Naltrexone is the newest molecule used for this purpose. It was introduced in 2010 in the US as Vivitrol.

Methadone, buprenorphine, naloxone and naltrexone represent a shift in the way opiate addiction and detox are understood and treated. Each drug is intended to improve on the major demerits of the last ones. However, considering the nature of opiate addiction and opioids, long-term studies are needed to thoroughly weigh the therapeutic advantage of each drug over the rest.

Methadone is a full opioid receptor agonist. It occupies opioid receptors in the brain much like the opiates it replaces and produces similar but muted and longer-lasting psychotropic effects. It was introduced to replace the likes of heroin and morphine while maintaining patient’s addiction in legal, controlled settings. Opiate addiction involves an unhealthy even criminal lifestyle. With methadone, addicts can attend methadone clinics and have their daily doses given to them. With time, it is assumed that a full detox can be achieved by reducing the dose given to each addict. The chief advantage of methadone is that it considerably reduces the withdrawal symptoms experienced when addicts get off opiates.

Buprenorphine, on the other hand, is a partial opioid receptor agonist. This means that while it occupies the same opioid receptors as methadone and the opiates, it produces a considerable weaker psychotropic effect. This way, it acts as an opiate replacement and mitigates the withdrawal symptoms much like methadone. However, like methadone, it possesses an addictive potential too. Therefore, there is a chance that addicts can get hooked on the drug too and need detox to get off.

Naloxone is a fast acting reversible opioid receptor antagonist. It occupies the same opioid receptors in the brain as opiates, methadone and buprenorphine and it cannot be displaced by the opiates. As an antagonist, naloxone produces no psychotropic effects. It is not used only in opiate detox but combined with buprenorphine (in Suboxone). Like methadone, suboxone requires daily administration. However, unlike methadone, it employs a dual effect to help patients overcome their opiate addiction.

Naltrexone (the drug inside Vivitrol) is also a reversible opioid receptor antagonist but unlike naloxone it is longer-acting. Therefore, it is more useful in the management of opiate addiction and detox. Naloxone faster action is more suited for emergency opiate overdose treatment. Naltrexone for opiate detox is available as an intramuscular injection and as an implant. The injectable form is the approved formulation and it is known as Vivitrol.

Naltrexone blocks the opioid receptors in the brain and prevents opiates from binding to it. Like naloxone, it is non-narcotic and non-addictive. Furthermore, it is formulated in Vivitrol as an extended release drug and is, therefore, administered once every month. This presents a clear advantage over methadone and suboxone’s daily administrations.

While the non-narcotic, non-addictive and longer dosing cycles of naltrexone make it the current champion of opiate detox, it is not without its own withdrawal side effects and unlike methadone, it lacks a exhaustive body of scientific studies done over the years to ascertain its relative efficacy and long-tern safety. An initial methadone clinical evaluation is important to help determine which of these molecules will provide the best benefits and the least side-effects for each opiate addict. But now more than ever, full opiate detox is achievable.

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