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
-

Effects of Gabapentin Versus Placebo on Buprenorphine Detoxification of Opioid-dependent Individuals

First Posted Date
2010-12-17
Last Posted Date
2013-06-21
Lead Sponsor
University of Arkansas
Target Recruit Count
30
Registration Number
NCT01262092
Locations
🇺🇸

University of Arkansas for Medical Sciences, Little Rock, Arkansas, United States

Efficacy and Safety Study of Buprenorphine HCl Buccal Film in Subjects With Low Back Pain

Phase 3
Completed
Conditions
Interventions
First Posted Date
2010-12-08
Last Posted Date
2017-02-27
Lead Sponsor
BioDelivery Sciences International
Target Recruit Count
334
Registration Number
NCT01256450
Locations
🇺🇸

Coastal Clinical Research, Inc., Mobile, Alabama, United States

🇺🇸

Alabama Orthopaedic Center - Research, Birmingham, Alabama, United States

🇺🇸

Neuro-Pain Medical Center, Fresno, California, United States

and more 21 locations

Buprenorphine 8 mg Sublingual Tablets Under Fasting Conditions

Phase 1
Completed
Conditions
Interventions
First Posted Date
2010-07-05
Last Posted Date
2020-01-18
Lead Sponsor
Teva Pharmaceuticals USA
Target Recruit Count
40
Registration Number
NCT01157169
Locations
🇺🇸

CEDRA Clinical Research, LLC, Austin, Texas, United States

A Within Subject Comparison of Opioid Withdrawal in Opioid Dependent Individuals

First Posted Date
2010-06-03
Last Posted Date
2017-03-03
Lead Sponsor
Johns Hopkins University
Target Recruit Count
12
Registration Number
NCT01136356
Locations
🇺🇸

Behavioral Pharmacology Research Unit, Baltimore, Maryland, United States

A Six-Month Randomized Controlled Trial (RCT) of Probuphine Safety and Efficacy in Opioid Addiction

First Posted Date
2010-05-03
Last Posted Date
2018-12-31
Lead Sponsor
Titan Pharmaceuticals
Target Recruit Count
287
Registration Number
NCT01114308
Locations
🇺🇸

BPRU, Behavioral Biology Research Center, Baltimore, Maryland, United States

🇺🇸

David Geffen School of Medicine at UCLA, Los Angeles, California, United States

🇺🇸

Friends Research Institute, Torrance, California, United States

and more 17 locations

Buprenorphine for Late-Life Treatment Resistant Depression

Phase 2
Completed
Conditions
Interventions
First Posted Date
2010-02-19
Last Posted Date
2018-03-09
Lead Sponsor
University of Pittsburgh
Target Recruit Count
15
Registration Number
NCT01071538
Locations
🇺🇸

Western Psychiatric Institute and Clinica, University of Pittsburgh School of Medicine, Pittsburgh, Pennsylvania, United States

Norspan Versus Oxycontin as Postoperative Painkiller to Proximal Extracapsular Fractures of the Femur

Phase 4
Completed
Conditions
Interventions
First Posted Date
2009-08-25
Last Posted Date
2014-12-08
Lead Sponsor
Vejle Hospital
Target Recruit Count
76
Registration Number
NCT00964808
Locations
🇩🇰

Orthopaedic Department, Vejle, Denmark

Effects of Buprenorphine on Ulnar Nerve Motor Block

Phase 4
Terminated
Conditions
First Posted Date
2009-07-30
Last Posted Date
2014-03-17
Lead Sponsor
University of Zurich
Target Recruit Count
20
Registration Number
NCT00949299
Locations
🇨🇭

University Hospital Zurich, Institut of Anaesthesiology, Zurich, ZH, Switzerland

A Study to Characterize the Pharmacokinetics and Tolerability of Buprenorphine Patches in Children With Moderate to Severe Mouth Pain

Phase 1
Terminated
Conditions
Interventions
First Posted Date
2009-07-28
Last Posted Date
2018-10-24
Lead Sponsor
Mundipharma Research Limited
Target Recruit Count
25
Registration Number
NCT00947466
Locations
🇬🇧

Dr Howell, Liverpool, United Kingdom

Study of Buprenorphine HCl Buccal Film in the Treatment of Dental Pain

First Posted Date
2009-07-17
Last Posted Date
2017-02-27
Lead Sponsor
BioDelivery Sciences International
Target Recruit Count
153
Registration Number
NCT00941304
Locations
🇺🇸

Donald P. Bandy, DDS, San Marcos, Texas, United States

🇺🇸

Premier Research Group Limited, Salt Lake City, Utah, United States

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