Buprenorphine Drug Information

Classification

bup_structure Buprenorphine (Suboxone, Subutex) is a semi-synthetic opioid that has both analgesic and antagonist properties. As an analgesic, buprenorphine is approximately 25 to 40 times more potent than morphine, and as an opioid antagonist it is roughly equivalent to naltrexone. Buprenorphine is a partial opioid agonist. Its opioid effects, such as euphoria and respiratory depression, reach a ceiling of maximum response. Buprenorphine is often co-administered with the full opioid antagonist Naloxone. When buprenorphine is taken by individuals addicted to heroin or other opioids, it reduces cravings and prevents abuse.

Metabolism

Buprenorphine is rapidly metabolized in the liver by the cytochrome P450 system to form a pharmacologically active N-dealkylated metabolite, norbuprenorphine and glucuronide conjugates. Buprenorphine and norbuprenorphine are excreted in urine almost exclusively as glucuronides with very little free drug being detected. Studies indicate that concentration of free buprenorphine and norbuprenorphine in urine can be less than 1 ng/mL following therapeutic administration but can range up to 20 ng/mL in abuse situations. Total buprenorphine and norbuprenorphine concentrations in urine, ranging from 0.5 - 2936 ng/mL and 4.0 - 4462 ng/mL respectively, have been reported following daily doses between 0.2 - 24 mg.

Abuse

Buprenorphine can be abused, particularly by individuals who are not physically dependent on opioids. Compared with methadone, buprenorphine has a relatively lower risk of abuse, dependence, and side effects, and it has a longer duration of action. Overdose symptoms include confusion, dizziness, pinpoint pupils, hallucinations, hypotension, respiratory difficulty, seizures and coma. Fatalities due to buprenorphine overdosage alone and by poly-drug use have been reported. Buprenorphine may be safer than methadone, as long as it is not combined with sedatives such as tranquilizers or alcohol. Buprenorphine can result in the opioid withdrawal syndrome. Symptoms of opioid withdrawal can include: dysphoria, nausea and vomiting, muscle aches and cramps, sweating, tearing, diarrhea, mild fever, running nose, insomnia, and irritability.

Laboratory drug testing: Methods of Analysis

Enzyme immunoassay (EIA) is used as a screening method for the detection of buprenorphine. Confirmation of screened positive urines should be performed by a specific method such as gas chromatography-mass spectrometry (GC-MS) or liquid chromatography-tandem mass spectrometry (LC-MS/MS).

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Drug information data is not definitive and should be used for reference guidelines only.