What is Buprenorphine?

Opioid prescription soared in the US in the 1990s, resulting in an opioid epidemic.  It is estimated that more than 11 million people misuse prescription drug in the US each year, and above 2.1 million are living with opioid use disorder. Buprenorphine is one drug that is used to combat this epidemic.

Buprenorphine is a semi-synthetic drug that is created from an alkaloid derived from the opium poppy. However, it acts a bit differently from morphine on the various brain receptors, partially activating opioid receptors.

The FDA has approved buprenorphine for pain management, and opioid detoxification and opioid maintenance to treat opioid use disorder. For more on opioid use disorder, we’ve written this article

History of Buprenorphine

Regretfully, for almost a century, people addicted to various substances have been refused treatment due to various legal barriers.

With the introduction of the Drug Abuse Treatment Act, this allowed for controlled substances to be used for the treatment of addiction in outpatient settings. Prior to the passage of this act, controlled substances to treat opioid use disorder were only allowed in designated addiction treatment centers.  Substance addiction is now seen in medicine as a chronic disease that needs medical treatment. Buprenorphine was approved by the FDA for addiction treatment in 2002.

Why use buprenorphine?

Buprenorphine is used for detoxification or maintenance therapy. Opiates like heroin or morphine act on the mu opioid receptors in the brain leading to addictive effects. Buprenorphine also acts on these receptors, but partially activates them. This partial activation leads to less euphoric effects. Secondly, unlike methadone or heroin, its effect does not increase with higher doses. Thirdly, it has a high affinity for mu opioid receptors, meaning that it can block the action of other drugs taken after it. Buprenorphine is also a long-acting opiate. Therefore it has several favorable outcomes,  it can partially block the effect of other addictive drugs, prevent withdrawals, with long-lasting effects, making it a great candidate for the treatment of addiction.

One of the issues with using buprenorphine is that it has poor bioavailability when taken orally. Studies show that only about 10% of it will make to the blood when taken as an oral dose.  Bioavailability of buprenorphine is 30% to 50% when taken sublingually, or underneath the tongue.

When taken sublingually it starts acting within 30 minutes to 3.5 hours. Its half-life is 28 to 37 hours when taken sublingually. 

Buprenorphine side effects

Buprenorphine has now been used in a few hundred thousand people. It is well tolerated, with side effects similar to other opioids but much less severe. Thus, it may cause constipation, nausea, headache, sedation, and urinary retention. It may also cause respiratory depression. Additionally, because of buprenorphine partial antagonist properties, pain management with opioids is often difficult.

Fatal overdose is rare, but a possibility especially when taken intravenously or combination with other drugs especially sedatives like benzodiazepines. 

It is metabolized in the liver; thus, in some people, it may cause changes in the liver enzymes (AST and ALT). It may interact with other drugs using a similar metabolic pathway like phenobarbital, carbamazepine, fluconazole, erythromycin, metronidazole, and some medications used to treat HIV infection.

Although it is not recommended for use in pregnancy due to a lack of safety data, some results show that it can improve outcomes in women with substance use disorder. It has been used in adolescents as a first-line treatment of drug addiction and appears to be quite safe.

Hepatitis C is frequently found in those addicted to various drugs. Since buprenorphine may not be good for the liver, the doctor will monitor liver function carefully. However, hepatitis is not a contradiction to starting treatment. Similarly, it may interact with some drugs used to treat HIV, especially protease inhibitors.

To conclude, buprenorphine is among the safer medications used to treat drug addiction, especially opioid addiction. In most cases, it can considerably improve the life of a patient, and its benefits far outweigh the risks involved in such a treatment.

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