Buprenorphine

SubutexSuboxoneProbuphineBupeBuprenexBuprenorphrineSubutex" (''Buprénorphine'')Transtec
Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain.wikipedia
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Buprenorphine/naloxone

SuboxoneBuprenorphine + Naloxone
For longer term treatment of addiction a combination formulation of buprenorphine/naloxone (Suboxone) is recommended to discourage misuse by injection.
Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a combination medication that includes buprenorphine and naloxone.

Heroin

diamorphinediacetylmorphinesmack
It is also a common drug of abuse, being used in place of heroin.
Medications can include buprenorphine, methadone, or naltrexone.

Opioid use disorder

heroin addictionopioid addictionheroin addict
Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain.
Individuals with an opioid use disorder are often treated with opioid replacement therapy using methadone or buprenorphine.

Opioid

opioidsopioid-induced constipationopioid analgesic
Buprenorphine, sold under the brand name Subutex, among others, is an opioid used to treat opioid addiction, acute pain, and chronic pain.
Buprenorphine was discovered in 1972.

Transdermal patch

patchtransdermaltransdermal drug delivery
It can be used under the tongue, by injection, as a skin patch, or as an implant.

Analgesic

analgesiaanalgesicspainkillers
It is difficult to achieve acute opioid analgesia in persons using buprenorphine for opioid replacement therapy.
Buprenorphine is a partial agonist of the μ-opioid receptor, and tramadol is a serotonin norepinephrine reuptake inhibitor (SNRI) with weak μ-opioid receptor agonist properties.

Partial agonist

partialpartial agonismpartially
Depending on the type of receptor it may be an agonist, partial agonist, or antagonist. In simplified terms, buprenorphine can essentially be thought of as a non-selective, mixed agonist–antagonist opioid receptor modulator, acting as a weak partial agonist of the MOR, an antagonist of the KOR, an antagonist of the DOR, and a relatively low-affinity, very weak partial agonist of the ORL-1.
Some currently common drugs that have been classed as partial agonists at particular receptors include buspirone, aripiprazole, buprenorphine, nalmefene and norclozapine.

Naloxone

NarcanNaloxone hydrochlorideEvzio
The usual reversal agents for opioids, such as naloxone, may be only partially effective and additional efforts to support breathing may be required.
Naloxone is poorly absorbed when taken by mouth, so it is commonly combined with a number of oral opioid preparations, including buprenorphine and pentazocine, so that when taken by mouth, only the opioid has an effect.

Κ-opioid receptor

κ-opioidKORkappa opioid receptor
The KOR antagonists buprenorphine, as ALKS-5461 (a combination formulation with samidorphan), and CERC-501 (LY-2456302) are currently in clinical development for the treatment of major depressive disorder and substance use disorders.

Receptor antagonist

antagonistantagonistscompetitive antagonist
Depending on the type of receptor it may be an agonist, partial agonist, or antagonist. In simplified terms, buprenorphine can essentially be thought of as a non-selective, mixed agonist–antagonist opioid receptor modulator, acting as a weak partial agonist of the MOR, an antagonist of the KOR, an antagonist of the DOR, and a relatively low-affinity, very weak partial agonist of the ORL-1. Buprenorphine/samidorphan, a combination product of buprenorphine and samidorphan (a preferential μ-opioid receptor antagonist), appears useful for treatment-resistant depression.
Buprenorphine, a partial agonist of the μ-opioid receptor, binds with weak morphine-like activity and is used clinically as an analgesic in pain management and as an alternative to methadone in the treatment of opioid dependence.

Norbuprenorphine

Buprenorphine is metabolized by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).
Norbuprenorphine is a major active metabolite of the opioid modulator buprenorphine.

Nociceptin receptor

NOPnociceptoidnociceptin
Several commonly used opioid drugs including etorphine and buprenorphine have been demonstrated to bind to nociceptin receptors, but this binding is relatively insignificant compared to their activity at other opioid receptors in the acute setting (however the non-analgesic NOPr antagonist SB-612,111 was demonstrated to potentiate the therapeutic benefits of morphine).

Opioid modulator

opioid receptor modulator
In simplified terms, buprenorphine can essentially be thought of as a non-selective, mixed agonist–antagonist opioid receptor modulator, acting as a weak partial agonist of the MOR, an antagonist of the KOR, an antagonist of the DOR, and a relatively low-affinity, very weak partial agonist of the ORL-1.
An example of an opioid modulator is buprenorphine, which is a partial agonist of the μ-opioid receptor and an antagonist of the κ-opioid receptor.

Buprenorphine-3-glucuronide

Buprenorphine-3-glucuronide has affinity for the MOR (K i = 4.9 pM), DOR (K i = 270 nM) and ORL-1 (K i = 36 μM), and no affinity for the KOR.
Buprenorphine-3-glucuronide (B3G) is a major active metabolite of the opioid modulator buprenorphine.

Norbuprenorphine-3-glucuronide

Norbuprenorphine-3-glucuronide has no affinity for the MOR or DOR, but does bind to the KOR (K i = 300 nM) and ORL-1 (K i = 18 μM).
Norbuprenorphine-3-glucuronide (N3G) is a major active metabolite of the opioid modulator buprenorphine.

CYP3A4

cytochrome P450 3A43A4cytochrome P450-3A4
Buprenorphine is metabolized by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).

Buprenorphine/samidorphan

ALKS-5461
Buprenorphine/samidorphan, a combination product of buprenorphine and samidorphan (a preferential μ-opioid receptor antagonist), appears useful for treatment-resistant depression.
Buprenorphine/samidorphan (developmental code name ALKS-5461) is a combination formulation of buprenorphine and samidorphan which is under development as an add on to antidepressants in treatment-resistant depression (TRD).

TLR4

Toll-like receptor 4TLR 4TLR-4
Similarly to various other opioids, buprenorphine has also been found to act as an agonist of the toll-like receptor 4, albeit with very low affinity.

Physical dependence

dependencedrug dependencyphysical
Physical dependence and withdrawal from buprenorphine itself remain important issues since buprenorphine is a long-acting opioid.

Opioid receptor

opioid receptorsopioidopiate receptor
Buprenorphine affects different types of opioid receptors in different ways.
Activation of this receptor produces strong analgesia and release of met-enkephalin; a number of widely used opioid agonists, such as the μ agonist etorphine and the κ agonist bremazocine, have been shown to act as agonists for this effect (even in the presence of antagonists to their more well known targets), while buprenorphine has been shown to act as an epsilon antagonist.

CYP2C8

2C8cytochrome P450 2C8
Buprenorphine is metabolized by the liver, via CYP3A4 (also CYP2C8 seems to be involved) isozymes of the cytochrome P450 enzyme system, into norbuprenorphine (by N-dealkylation).

Biological half-life

elimination half-lifehalf-lifeterminal half-life
The elimination half-life of buprenorphine is 20 to 73 hours (mean 37 hours).

Naltrexone

Revianaltrexone hydrochlorideSinclair method
In combination with samidorphan or naltrexone (μ-opioid receptor antagonists), buprenorphine is under investigation for the treatment of cocaine dependence, and recently demonstrated effectiveness for this indication in a large-scale (n = 302) clinical trial (at a high buprenorphine dose of 16 mg but not a low dose of 4 mg).
It has benefits over methadone and buprenorphine in that it is not a restricted medication.