Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It can be used under the tongue (sublingual), in the cheek (buccal), by injection (intravenous and subcutaneous), as a skin patch (transdermal), or as an implant. For opioid use disorder, it is typically started when withdrawal symptoms have begun and for the first two days of treatment under direct observation of a health-care provider. The combination formulation of buprenorphine/naloxone (Suboxone) is recommended to discourage misuse by injection. Maximum pain relief is generally within an hour with effects up to 24 hours.
Side effects may include respiratory depression (decreased breathing), sleepiness, adrenal insufficiency, QT prolongation, low blood pressure, allergic reactions, constipation, and opioid addiction. Among those with a history of seizures, a risk exists of further seizures. Opioid withdrawal following stopping buprenorphine is generally less severe than with other opioids. Whether use during pregnancy is safe is unclear, but use while breastfeeding is probably safe, since the dose the infant receives is 1-2% that of the maternal dose, on a weight basis. Buprenorphine affects different types of opioid receptors in different ways. Depending on the type of receptor, it may be an agonist, partial agonist, or antagonist.
Buprenorphine was patented in 1965, and approved for medical use in the United States in 1981. It is on the World Health Organization's List of Essential Medicines. In 2017, 14.6 million prescriptions for the medication were written in the United States. It is also a common medication used to treat opioid use disorders, such as addiction to heroin. Buprenorphine may also be used recreationally by injection or in the nose for the high it produces. In the United States, it is a schedule III controlled substance.
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