Buprenorphine

SuboxonesubutexBuprenorphrineTranstec
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 is recommended to prevent misuse by injection.
Buprenorphine/naloxone, sold under the brand name Suboxone among others, is a combination medication that includes buprenorphine and naloxone.

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 disorders are often treated with opioid replacement therapy using methadone or buprenorphine.

Opioid

opioidsopioid analgesicendogenous opioids
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.
Two opioid medications used to provide round-the-clock relief for severe pain are often prescribed in patch form, fentanyl CII (marketed as Duragesic) and buprenorphine CIII (marketed as BuTrans).

Heroin

diamorphinediacetylmorphinesmack
Occasionally it is used recreationally instead of heroin.
Medications can include buprenorphine, methadone, or naltrexone.

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.

Naloxone

NarcaninjectionNaloxone (1961)
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 orally, just the opioid has an effect, but if misused by injecting, the naloxone blocks the effect of the opioid.

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.

Κ-opioid receptor

κ-opioidKORkappa opioid receptor
κ-Opioid receptor (KOR): Antagonist.
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.

Controlled Substances Act

Schedule ISchedule IIschedule III
In the United States it is a Schedule III controlled substance.
Buprenorphine (semi-synthetic opioid; active in Suboxone, Subutex)

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
Nociceptin receptor (NOP, ORL-1): Weak affinity. Very weak partial agonist. May be involved in lack of respiratory depression with buprenorphine in overdose.
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

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 drug formulation of buprenorphine and samidorphan acting as a κ-opioid receptor (KOR) antagonist which is under development by Alkermes as an adjunct to antidepressant therapy in treatment-resistant depression (TRD).

Δ-opioid receptor

DORδ-opioiddelta opioid receptor
δ-Opioid receptor (DOR): Antagonist.
Buprenorphine

TLR4

toll-like receptor 4TLR-4CD284
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.
Buprenorphine

Physical dependence

Physicaldependencedrug dependency
Physical dependence and withdrawal from buprenorphine itself remain important issues since buprenorphine is a long-acting opioid.
All µ-opioids with any (even slight) agonist effect, such as (partial list) morphine, heroin, codeine, oxycodone, buprenorphine, nalbuphine, methadone, and fentanyl, but not agonists specific to non-µ opioid receptors, such as salvinorin A (a k-opioid agonist), nor opioid antagonists or inverse agonists, such as naltrexone (a universal opioid inverse agonist)

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).

Neonatal withdrawal

neonatal abstinence syndromeneonatal withdrawal syndromewithdrawal symptoms in the newborn
Buprenorphine has been used in the treatment of the neonatal abstinence syndrome, a condition in which newborns exposed to opioids during pregnancy demonstrate signs of withdrawal.
Neonatal abstinence syndrome may occur when a pregnant woman takes opioids such as heroin, codeine, oxycodone, methadone or buprenorphine.