Buprenorphine Abuse Treatment


Buprenorphine (C29H41NO4) is the chemical structural formula for the brand name opioids, Suboxone and Subutex, manufactured by Reckitt-Benckiser. A derivative of thebaine, its chemical name is 17-(Cyclopropylmethyl)-alpha-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro- 3-hydroxy-6-methoxy-alpha-methyl-6,14-ethenomorphinan-7-methanol.

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Buprenorphine, a derivative of thebaine was first marketed in the United States as the Schedule V parenteral analgesic Buprenex. In 2002, after a review of evidence about the potential for abuse, diversion, addiction, and side effects, the DEA reclassified buprenorphine from a Schedule V to a Schedule III narcotic.

Both Subutex and Suboxone are approved for the treatment of opiate dependence and pain relief. The active ingredient buprenorphine hydrochloride, reduces the symptoms of opiate dependence. Suboxone is a combination of two proven medications, buprenorphine and naloxone. Buprenorphine, a partial opioid agonist, reduces withdrawal symptoms and blocks the effects of subsequently administered opioids, suggesting it might help reduce illicit opioid use. Due to the presence of naloxone, Suboxone is very likely to produce severe withdrawal symptoms if misused intravenously. When used as prescribed, no such effect is likely.

Subutex and Suboxone are the first opiate addiction treatments approved for in-office prescribing under the federal Drug Addiction Treatment Act of 2000 (DATA). Other buprenorphine brand names are Temgesic and Buprenex.

In October 2002, Reckitt Benckiser received FDA approval to market two products: Subutex, a buprenorphine monotherapy product, and Suboxone, a buprenorphine/naloxone combination product. These two products are indicated for use in opioid addiction treatment, with Suboxone designed to reduce injection abuse. Both drugs are currently the only Schedule III, IV, or V medications with FDA approval for this purpose.

The FDA approval of these buprenorphine formulations does not alter the status of other medication-assisted opioid addiction treatments, such as methadone and LAAM (levo-alpha-acetyl-methadol), both only available within the context of an Opioid Treatment Program.

Buprenorphine is used as a pain reliever and to treat opiate addiction. It produces less of a “high” than other opioids, such as codeine and morphine. For this reason, it is less susceptible to abuse and may be easier to stop taking.

Candidates for opioid addiction treatment with buprenorphine need to meet the following criteria:

· objective diagnosis of opioid addiction
· willing to comply with treatment safety precautions
· likely to comply with treatment guidelines
· no contraindications to buprenorphine

Buprenorphine’s primary action is to prevent withdrawal symptoms, enabling people addicted to an opioid drug to stop taking the drug. Only doctors experienced in the use of buprenorphine can determine if it is the right choice for a the opiate addicted patient. CSAT (Center for Substance Abuse Treatment) maintains a database to help patients locate qualified doctors.

The two buprenorphine drugs approved for use in treating opiate addiction are:

Subutex, the initial product formulation, contains only buprenorphine hydrochloride. It is generally given during the first few days of treatment.
Suboxone contains an additional ingredient called naloxone to prevent abuse. Suboxone is indicated for the maintenance phase of treatment and is used in the majority of patients.

Both medications come in 2 mg and 8 mg strengths as sublingual (placed under the tongue to dissolve) tablets. The half-life of buprenorphine is 24–60 hours. Tablets should not be chewed or swallowed or they will not work properly and may cause withdrawal symptoms.

Injecting buprenorphine is dangerous and may result in severe withdrawal symptoms. In addition, buprenorphine may cause withdrawal symptoms if taken too soon after a dose of morphine, methadone or another opiate agonist.

Only qualified doctors with the necessary DEA (Drug Enforcement Agency) identification number can prescribe these medications.

Never increase the amount or frequency without your doctor’s approval, or take this drug for any reason other than the one prescribed.

Simply put, as a partial opioid agonist, buprenorphine reduces withdrawal symptoms and blocks the effects of subsequently administered opioids. Suboxone also exhibits a “ceiling effect” on respiratory depression, thereby decreasing the danger of overdose compared to other opioids.

As an opioid partial agonist, buprenorphine produces typical opioid agonist effects and side effects such as euphoria and respiratory depression. However, its maximum effects are less than those of full agonists like heroin and methadone. At low doses, buprenorphine provides satisfactory agonist effect for opioid-addicted individuals to discontinue the abuse of opioids and avoid withdrawal. In fact, in high doses and under certain circumstances, buprenorphine blocks the effects of full opioid agonists, precipitating withdrawal symptoms if administered to an opioid-addicted individual while a full agonist is in the bloodstream.

Side Effects:
Side effects of buprenorphine are similar to those of other opioids and include nausea, vomiting, and constipation. Buprenorphine can expedite opioid withdrawal with symptoms including, but not limited to: depression, nausea or vomiting, muscle aches and cramps, runny eyes and nose, dilated pupils, sweating, diarrhea, yawning, low fever, insomnia, cravings, and irritability.

Cautionary Notes:
Fast Facts:
* Buprenorphine can cause a potentially fatal overdose if mixed and injected with a tranquilizer.
* Buprenorphine can cause drug dependence, resulting in withdrawal symptoms if the medicine is suddenly stopped. Withdrawal symptoms may also occur at the start of treatment due to dependence on another drug.
* Buprenorphine may seriously impair your ability to drive a car or operate machinery.
* Avoid alcohol while taking buprenorphine because alcohol can dramatically increase the drowsiness and dizziness associated with this medication.

Possible Food and Drug Interactions when taking this Medication:

Buprenorphine may dramatically increase the effects of other drugs that cause drowsiness. These include antidepressants, alcohol, antihistamines, sedatives, pain relievers, anxiety medicines, and muscle relaxants. Make sure your doctor knows about all medications you are using, including over-the-counter medicine and herbal products.

It is especially important to check with your doctor before combining buprenorphine with the following:

· Benzodiazepines (Valium, Ativan, Xanax, etc.)
· Erythromycin; clarithromycin (Biaxin)
· Itraconazole (Sporanox) or ketoconazole (Nizoral)
· HIV protease inhibitors such as indinavir (Crixivan), ritonavir (Norvir) or saquinavir (Fortovase, Invirase); rifampin (Rifadin, Rimactane), rifapentine (Priftin), or rifabutin (Mycobutin)
· Phenytoin (Dilantin)
· Carbamazepine (Tegretol)
· Barbiturates such as phenobarbital, mephobarbital (Mebaral), and others

Do not take Buprenorphine without telling your doctor if you have lung problems or difficulty breathing; a head injury; liver or kidney problems; adrenal gland problems, such as Addison’s disease; hypothyroidism; enlarged prostate gland; a curve in the spine that affects breathing; severe mental problems or hallucinations; or alcoholism.


Buprenorphine overdoses can lead to dangerous opiate-overdose symptoms. Some evidence suggests that addiction and habituation can be a problem for some users. Symptoms of a overdose include slow breathing, seizures, dizziness, weakness, loss of consciousness, coma, confusion, tiredness, cold and clammy skin, and constricted pupils.

While buprenorphine’s primary purpose is to treat opiate addiction, it can still cause drug dependence. Due to its opioid agonist effects, buprenorphine can be abused, particularly by those not physically dependent on opioids. With Suboxone, naloxone is added to buprenorphine to decrease the likelihood of diversion and abuse of the combination product.

When patients no longer require buprenorphine, they should work with their physician to set a gradual taper schedule to avoid acute withdrawal.

Both Suboxone and Subutex can cause drug dependence which can result in withdrawal symptoms if the medicine is suddenly stopped. Since buprenorphine is a partial agonist, withdrawal is less severe than with full agonists. If a patient has a dependence on another opiate, he may experience withdrawal symptoms at the beginning of treatment. These drugs are not for irregular use and should never be stopped without first consulting your doctor. Generally, doctors will gradually reduce the dose to avoid or minimize withdrawal symptoms.

Buprenorphine is a partial agonist at the mu-opioid receptor and chronic administration produces dependence similar to the opioid type, characterized by moderate withdrawal upon abrupt discontinuation or rapid taper.

To avoid severe withdrawal symptoms, chronic Suboxone/Subutex users should taper down slowly under a knowledgeable physician’s care. Dependence resulting from even a few weeks of regular use can usually be handled under a physician’s supervision with minimal discomfort.

However a person chooses to free themselves from the clutches of a drug, there is one constant each needs: Support. Narcotics Anonymous remains a successful choice for many addicts, with world-wide availability. The “information age” has produced numerous on line support forums, popular with many recovering addicts, useful to some addicts as their sole means of support and for others, as adjunct therapy. Drug addiction is treatable, with help out there for everyone.

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