Buprenorphine

Generic Name
Buprenorphine
Brand Names
Belbuca, Brixadi, Buprenex, Buprenorphine, Butrans, Sublocade, Suboxone, Subutex, Zubsolv, Buvidal, Sixmo
Drug Type
Small Molecule
Chemical Formula
C29H41NO4
CAS Number
52485-79-7
Unique Ingredient Identifier
40D3SCR4GZ
Background

Buprenorphine is a weak partial mu-opioid receptor agonist and a weak kappa-opioid receptor antagonist used for the treatment of severe pain. It is also commonly used as an alternative to methadone for the treatment of severe opioid addiction. Buprenorphine is commercially available as the brand name product Suboxone which is formulated in a 4:1 fixed-dose combination product along with naloxone, a non-selective competitive opioid receptor antagonist. Combination with naloxone is intended to reduce the abuse potential of Suboxone, as naloxone is poorly absorbed by the oral route (and has no effect when taken orally), but would reverse the opioid agonist effects of buprenorphine if injected intravenously. Buprenorphine has poor gastrointestinal absorption and is therefore formulated as a sublingual tablet.

Buprenorphine has a number of unique pharmacokinetic and pharmacodynamic properties that make it a preferred agent for the treatment of conditions requiring high doses of strong opioids. For example, buprenorphine dissociates from opioid receptors very slowly, resulting in a long duration of action and relief from pain or withdrawal symptoms for upwards of 24-36 hours. Use of once-daily buprenorphine may benefit individuals who have developed tolerance to other potent opioids and who require larger and more frequent doses. Buprenorphine may also be a preferred agent over methadone (which is also commonly used to treat severe pain and opioid use disorder), as it has less effect on Qtc interval prolongation, fewer drug interactions, reduced risk of sexual side effects, and an improved safety profile with a lower risk of overdose and respiratory depression.

Buprenorphine acts as a partial mu-opioid receptor agonist with a high affinity for the receptor, but lower intrinsic activity compared to other full mu-opioid agonists such as heroin, oxycodone, or methadone. This means that buprenorphine preferentially binds the opioid receptor and displaces lower affinity opioids without activating the receptor to a comparable degree. Clinically, this results in a slow onset of action and a clinical phenomenon known as the "ceiling effect" where once a certain dose is reached, buprenorphine's effects plateau. This effect can be beneficial, however, as dose-related side effects such as respiratory depression, sedation, and intoxication also plateau at around 32mg, resulting in a lower risk of overdose compared to methadone and other full agonist opioids. It also means that opioid-dependent patients do not experience sedation or euphoria at the same rate that they might experience with more potent opioids, improving quality of life for patients with severe pain and reducing the reinforcing effects of opioids which can lead to drug-seeking behaviours.

Treatment of opioid addiction with buprenorphine, methadone, or slow-release oral morphine (SROM) is termed Opioid Agonist Treatment (OAT) or Opioid Substitution Therapy (OST). The intention of substitution of illicit opioids with the long-acting opioids used in OAT is to prevent withdrawal symptomns for 24-36 hours following dosing to ultimately reduce cravings and drug-seeking behaviours. Use of OAT is also intended to improved social stabilization including a reduction in crime rates, marginalization, incarceration, and use of illicit substances such as heroin or fentanyl. Illegally purchased opioids can often be injected and may be laced with other substances that increase the risk of harm or overdose. Provision of OAT is often combined with education about harm reduction including use of clean needles and injection supplies in an effort to reduce the risks associated with injection drug use which includes contraction of HIV and Hepatitis C and other complications including skin infections, abscesses, or endocarditis.

Indication

Buprenorphine is available in different formulations, such as sublingual tablets, buccal films, transdermal films, and injections, alone or in combination with naloxone.

The buccal film, intramuscular or intravenous injection, and transdermal formulation are indicated for the management of pain severe enough to require an opioid analgesic and for which alternate treatments are inadequate.

The extended-release subcutaneous injections of buprenorphine are indicated for the treatment of moderate to severe opioid use disorder in patients who have initiated treatment with a single dose of a transmucosal buprenorphine product or who are already being treated with buprenorphine. Injections are part of a complete treatment plan that includes counselling and psychosocial support.

Sublingual tablets and buccal films, in combination with naloxone, are indicated for the maintenance treatment of opioid dependence as part of a complete treatment plan that includes counselling and psychosocial support.

Associated Conditions
Opioid Dependence, Severe Pain, Moderate Opioid Dependence, Moderate Pain, Severe Opioid Dependence
Associated Therapies
-

Extended Release Naltrexone for Opioid-Dependent Youth

First Posted Date
2013-04-30
Last Posted Date
2021-11-10
Lead Sponsor
Friends Research Institute, Inc.
Target Recruit Count
288
Registration Number
NCT01843023
Locations
🇺🇸

Friends Research Institute, Baltimore, Maryland, United States

🇺🇸

Mountain Manor Treatment Center, Baltimore, Maryland, United States

An Interventional Study to Assess the Efficacy and Safety of Buprenorphine in Korean Patients With Spinal Disorders

Phase 4
Completed
Conditions
Interventions
First Posted Date
2013-03-26
Last Posted Date
2015-10-22
Lead Sponsor
Mundipharma Korea Ltd
Target Recruit Count
245
Registration Number
NCT01818700
Locations
🇰🇷

Samsung Medical Center, Seoul, Korea, Republic of

RCT Comparing the Analgesic Efficacy of 4 Therapeutic Strategies Based on 4 Different Major Opioids (Fentanyl, Oxycodone, Buprenorphine vs Morphine) in Cancer Patients With Moderate/Severe Pain, at the Moment of Starting 3rd Step of WHO Analgesic Ladder.

First Posted Date
2013-03-12
Last Posted Date
2015-12-24
Lead Sponsor
Mario Negri Institute for Pharmacological Research
Target Recruit Count
518
Registration Number
NCT01809106
Locations
🇮🇹

Multimedica, Sesto San Giovanni, Italy

🇮🇹

Istituto Scientifico San Raffaele, Milano, Italy

🇮🇹

Arcispedale S. Maria Nuova Azienda Ospedaliera, Reggio Emilia, RE, Italy

and more 6 locations

Multiple Dose Pharmacokinetics Depot Buprenorphine in Opioid-Dependent Subjects

Phase 2
Completed
Conditions
Interventions
First Posted Date
2012-11-30
Last Posted Date
2018-02-23
Lead Sponsor
Indivior Inc.
Target Recruit Count
124
Registration Number
NCT01738503
Locations
🇺🇸

Vince and Associates Clinical Research, Overland Park, Kansas, United States

Neurocognitive Effects of Opiate Agonist Treatment

First Posted Date
2012-11-27
Last Posted Date
2022-02-11
Lead Sponsor
Albert Einstein College of Medicine
Target Recruit Count
135
Registration Number
NCT01733693
Locations
🇺🇸

Albert Einstein College of Medicine of Yeshiva University, Bronx, New York, United States

🇺🇸

Fordham University, Bronx, New York, United States

Diversion to Treatment for Injection Drug Users Arrested for Possession of Heroin

First Posted Date
2012-11-08
Last Posted Date
2014-12-11
Lead Sponsor
Johns Hopkins University
Target Recruit Count
1
Registration Number
NCT01723527
Locations
🇺🇸

Center for Learning and Health, Baltimore, Maryland, United States

Comparison of Buprenorphine to Morphine in Treatment of Neonatal Abstinence Syndrome (NAS)

First Posted Date
2012-10-17
Last Posted Date
2018-08-15
Lead Sponsor
Pediatrix
Target Recruit Count
29
Registration Number
NCT01708707
Locations
🇺🇸

Banner - University Medical Center Phoenix, Phoenix, Arizona, United States

Efficacy Study to Evaluate Buprenorphine HCl Buccal Film in Opioid-Experienced Subjects

Phase 3
Completed
Conditions
Interventions
First Posted Date
2012-08-29
Last Posted Date
2017-02-27
Lead Sponsor
BioDelivery Sciences International
Target Recruit Count
815
Registration Number
NCT01675167
Locations
🇺🇸

Horizon Research Group. Inc / Alabama Orthopedice, Mobile, Alabama, United States

🇺🇸

FPA Clinical Research, Kissimmee, Florida, United States

🇺🇸

Global Research, Anaheim, California, United States

and more 63 locations

Buprenorphine Disposition and Cyclosporine

Not Applicable
Completed
Conditions
Interventions
First Posted Date
2012-07-24
Last Posted Date
2020-01-22
Lead Sponsor
Washington University School of Medicine
Target Recruit Count
25
Registration Number
NCT01648270
Locations
🇺🇸

Washington University School of Medicine, Saint Louis, Missouri, United States

Norspan Transdermal Patches Study in Osteoarthritis Patients

Phase 1
Completed
Conditions
Interventions
First Posted Date
2012-07-18
Last Posted Date
2015-07-08
Lead Sponsor
Mundipharma (China) Pharmaceutical Co. Ltd
Target Recruit Count
30
Registration Number
NCT01643759
Locations
🇨🇳

Investigational Site: Peking Union Medical Hospital(PUMC), Beijing, China

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