Buprenorphine
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| Trade names | Suboxone, Subutex, others |
| AHFS/Drugs.com | Monograph |
| MedlinePlus | a605002 |
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Sublingual, buccal, IM, IV, transdermal, intranasal, rectally, by mouth |
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| Pharmacokinetic data | |
| Bioavailability | Sublingual: 30% Intranasal: 48% |
| Protein binding | 96% |
| Metabolism | Hepatic (CYP3A4, CYP2C8) |
| Biological half-life | 37 hours (range 20–70 hours) |
| Excretion | Biliary and renal |
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| ECHA InfoCard | 100.052.664 |
| Chemical and physical data | |
| Formula | C29H41NO4 |
| Molar mass | 467.64 g/mol |
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Buprenorphine, sold under the brand name Suboxone among others, is an opioid used to treat opioid addiction, moderate acute pain and moderate chronic pain. The combination buprenorphine/naloxone is also used for opioid addiction.
It is a semisynthetic and derivative of thebaine. It is a mixed partial agonist opioid receptor modulator.
Buprenorphine was approved for medical use in the United States in 1981.
Its primary uses in medicine are in the treatment of those addicted to opioids, such as heroin and oxycodone, but it may also be used to treat pain, and sometimes nausea in antiemetic intolerant individuals, most often in transdermal patch form.
It has veterinary medical use for treatment of pain in dogs and cats.
Both buprenorphine and methadone are medications used for detoxification, short- and long-term opioid replacement therapy. Buprenorphine has the advantage of being only a partial agonist; hence negating the potential for life-threatening respiratory depression in cases of abuse. Studies show the effectiveness of buprenorphine and methadone are almost identical, and largely share adverse-effect profiles apart from more sedation among methadone users. At low flexible doses from 2 to 6 mg, however, buprenorphine has a lower retention rate than low doses from 40 mg or less of methadone.
Rehabilitation programs consist of "detox" and "treatment" phases. The detoxification ("detox") phase consists of medically supervised withdrawal from the drug of dependency onto buprenorphine, sometimes aided by the use of medications such as benzodiazepines like oxazepam or diazepam (modern milder tranquilizers that assist with anxiety, sleep, and muscle relaxation), clonidine (a blood-pressure medication that may reduce some opioid withdrawal symptoms), and anti-inflammatory/pain relief drugs such as ibuprofen and aspirin.
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