Buprenorphine as Opioid Receptor Antagonist

buprenorphineBuprenorphine is a semi-synthetic opioid derived from thebaine. It is a pain killer and has gained a great deal of notoriety for its ability to interrupt severe opiate addiction, including heroin and methadone addictions. It got approved in 2002 by the FDA for use as an opiate addiction treatment. Dependence on pain drugs is common but very dangerous and that is why buprenorphine is of importance in fighting opioid independence.

Today, buprenorphine is being used in office based treatment of opioid dependent patients. Buprenorphine is a partial mu-opioid receptor agonist. Several clinical studies indicate buprenorphine is effective in managing opioid addiction and dependence. In all of the clinical tests Buprenorphine was found to be more effective than placebo for managing opioid addiction. However, it may not be superior to methadone incase high doses are needed. It is comparable to lower doses of methadone, however. When using buprenorphine, there are critical phases that must be followed. These phases include; include induction, stabilization, and maintenance. Experts advise that Buprenorphine therapy should be initiated at the onset of withdrawal symptoms and adjusted to address withdrawal symptoms and cravings. Advantages of buprenorphine include low abuse potential and high availability for office use. Disadvantages include high cost and possible lack of effectiveness in patients who require high methadone doses. Most family physicians are required to complete eight hours of training before they can prescribe buprenorphine for opioid addiction. Let’s get all the detailed facts here.

It is estimated that 898,000 adults in the United States are opioid dependent. Treating opioid dependence as a chronic disorder improves outcomes and opioid maintenance is the most effective way to decrease illicit use in patients who are addicted to opioids. Without opioid maintenance, it will be easy for any user of opiates for pain to be an addict of the same therefore various strategies must be put in place to exercise opioid maintenance for the safety of the patients. Over the past years Methadone has been the treatment of choice in the United States; however, methadone maintenance programs typically have stringent entrance criteria, long waiting lists, and primarily are located in urban areas. It has been verified that only 14 percent of patients who are addicted to opioids are treated in traditional methadone clinics. Research from the 1970s demonstrated that the analgesic buprenorphine (Subutex), a partial mu-opioid receptor agonist, may effectively treat patients with heroin addiction.

In the Drug Addiction Treatment Act of 2000 physicians are authorized to provide office-based treatment for opioid addiction. Through this act physicians are allowed to prescribe Schedule III, IV, or V “narcotic” medications that are approved by the U.S. Food and Drug Administration (FDA) for patients with narcotic-use disorders. In 2002, buprenorphine and combination buprenorphine/naloxone (Suboxone) was approved by the FDA to manage opioid dependence .It is therefore a legally usable drug that is available in health centers and clinics.

How to use

As stated earlier the Management of opioid addiction with buprenorphine can be divided into three phases: induction, stabilization, and maintenance. The induction phase includes the initial transition from illicit opioid use to buprenorphine and typically lasts three to seven days. Patient education is important during this phase and should emphasize the risk of precipitating withdrawal if buprenorphine is initiated too soon after opioid use. Generally, buprenorphine should be initiated 12 to 24 hours after short-acting opioid use and 24 to 48 hours after long-acting opioid use. It is preferable for most patients to use combination of buprenorphine/naloxone tablets.  It is however advised that pregnant women who are to use buprenorphine and some patients using long-acting opioids such as methadone should use the buprenorphine-only formulation. For those who are on long- acting opioid use, the methadone dose should be less than 30 mg and the patient should switch to the combination tablet after several days.

When the patient has shown opioid withdrawal symptoms, the initial doses should be administered under physician observation (4/1 mg buprenorphine/naloxone or 2 mg buprenorphine if the patient is dependent on a long-acting opioid). It is important for the physician to monitor the patient for precipitated withdrawal and excessive side effects like sedation). If the patient continues to exhibit signs of opioid withdrawal after two hours, another 4/1 mg dose of buprenorphine/naloxone should be administered. Patients who are dependent on long-acting opioids should receive 2 mg buprenorphine every one to two hours. The maximum recommended first-day dosage of buprenorphine is 8 to 12 mg. If the patient continues to show signs of withdrawal, the physician may administer adjunctive nonopioid and symptomatic treatments to help the situation.

Difference between methadone and morphine

There are some differences between methadone and morphine. Some of the differences lie in their costs and uses. Here are some of the differences.

Methadone is much cheaper as compared to morphine. For this reason many physicians favor methadone. Methadone also lasts longer than morphine- it lasts ten times longer than morphine. Methadone also lasts longer than morphine in the body. It takes 24 hours while morphine takes only 2-3 hours only in the body. However methadone should not be used for slight pain despite its availability and cheaper cost.

Another difference is that methadone is excreted through urine while morphine is excreted through the liver and bile ducts before its exit in the urine.


BuprenorphineThese drugs are also used in different situations. Methadone is mostly used after unsuccessful use of morphine or when the patient has a history of drug abuse. If tis patient is morphine it may lead to relapse hence methadone is considered safer than morphine. Morphine is addictive while methadone is not addictive.

Here at AWAREmed we are dedicated to finding the best solutions to chronic illnesses and that is why Dr. Dalal Akoury (MD) is always in the forefront advocating for integrative medicine since it is only through integrative medicine that a person can be healed wholly. Do not hesitate to call on her for help in managing any sort of chronic pain as well as other diseases.


Buprenorphine as Opioid Receptor Antagonist