Buprenorphine
Also called Buprenex, Subutex, Butrans, Cizdol, Addnok, Transtec
Dosage
Insufflated bands as drawn from PsychonautWiki's ranges below. The table is the source of truth.
Insufflated
| Source | Threshold | Light | Common | Strong | Heavy |
|---|---|---|---|---|---|
| PsychonautWiki | < 0.2 mg PW | 0.2–0.4 mg PW | 0.4–0.8 mg PW | 0.8–1.5 mg PW | 1.5 mg+ PW |
Sublingual
Oral
NOTE: The ceiling dose for Buprenorphine is usually between 16mg and 32mg, anything above this will not produce any increase in effects. Also, after dosing 4mg your opioid receptors are completely covered. TS
TripSit dose text
TripSit's factsheet also states its doses as text.
Light: 0.2-0.4mg Common: 0.4-0.8mg Strong: 0.8-1.5mg Heavy: 1.5mg+ | NOTE: The ceiling dose for Buprenorphine is usually between 16mg and 32mg, anything above this will not produce any increase in effects. Also, after dosing 4mg your opioid receptors are completely covered. TS
What dose are you on? (self-reported, unverified)
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Duration
| Route · source | Onset | Come-up | Peak | Offset | Total | After-effects |
|---|---|---|---|---|---|---|
| Insufflated · PsychonautWiki | 30–60 minutes PW | – | 4–8 hours PW | – | 8–14 hours PW | 1–3 days PW |
| Sublingual · PsychonautWiki | 40–80 minutes PW | – | 1.5–2 hours PW | – | 18–24 hours PW | 1–3 days PW |
TripSit factsheet
Mixing
Acute combinations: what happens when these are taken close together. Entries backed by a medical journal or agency are listed first.
Backed by medical journals
PsychonautWiki also lists dangerous combinations shared across a whole group (opioids) in a table this page does not copy. Read that list on PsychonautWiki.
TripSit combination chart
TripSit rates each pairing. Only pairings with a number carry a citation from TripSit. See the whole chart, with TripSit's note for every pairing.
Risks and toxicity
Buprenorphine has a low toxicity relative to dose: the ceiling dose for buprenorphine is usually between 16mg and 32mg, and anything above this will not produce an increase in respiratory depression (the primary cause of death in opioid overdose is severe respiratory depression, leading to respiratory collapse). Thus increasing the dose of buprenorphine above this level will not continue to increase risk of death in a fashion similar to other μ-opioid receptor agonists. As with all opioids, long-term effects can vary but can include diminished libido, apathy and memory loss. PW
Regardless of the ceiling dose, an important distinction has to be made in the dose used in opioid naive individuals and opioid experienced individuals. Even low doses in individuals with no tolerance can cause unpleasant side-effects like dizziness, loss of balance, and vomiting. Because of the long half-life of buprenorphine, these side-effects can last a long while in opioid naive individuals which creates the risk of severe dehydration from uncontrollable vomiting. PW
Buprenorphine is often sold under the brand name Suboxone, which also contains naloxone. Naloxone is not orally active except at higher doses, so when large amounts of Suboxone are taken, the naloxone takes effect and reverses the effects of the buprenorphine. This is done to deter abuse of Suboxone. PW
It is strongly recommended that one use harm reduction practices when using this drug. PW
Tolerance and addiction potential
As with other opioids, the chronic use of buprenorphine can be considered moderately addictive with a high potential for abuse and is capable of causing psychological dependence among certain users. When addiction has developed, cravings and withdrawal symptoms may occur if a person suddenly stops their usage. PW
Tolerance to many of the effects of buprenorphine develops with prolonged and repeated use. The rate at which this occurs develops at different rates for different effects, with tolerance to the constipation-inducing effects developing particularly slowly for instance. This results in users having to administer increasingly large doses to achieve the same effects. After that, it takes about 3 - 7 days for the tolerance to be reduced to half and 1 - 2 weeks to be back at baseline (in the absence of further consumption). Buprenorphine presents cross-tolerance with all other opioids, meaning that after the consumption of buprenorphine all opioids will have a reduced effect. PW
Precipitated withdrawal syndrome
Buprenorphine has the ability to precipitate withdrawal symptoms in opiate-dependent individuals. This is due to buprenorphine only being a partial agonist, which does not activate the receptor with the appreciable efficacy of a full agonist, as well as having a very high binding affinity for the μ-opioid receptor (Kᵢ = 1.5nM), displacing other agonists that may still be attached when the buprenorphine is ingested. PW
Note: It is a common misconception that naloxone, in some buprenorphine formulations, is what causes the precipitated withdrawal syndrome to manifest. This is false, as naloxone has a lower binding than Buprenorphine, as well as being inactive through most routes of administration. PW
Testing
Effects
EuphoriaDry MouthMood liftItchinessRelaxantConstipationPupil constrictionAnalgesia TS
Overview
Buprenorphine is a semisynthetic opioid of the morphinan chemical class. It functions as a mixed partial agonist opioid receptor modulator. PW
A semi-synthetic opioid analgesic also known as subutex. Often administered as Butrans patches, or in combination with Naloxone as Suboxone, a heroin replacement therapy drug. Will cause withdrawals if you have an opioid tolerance and don't wait long enough (typically around 48 hours) before taking this.[1] TS
Buprenorphine is an opioid used to treat opioid use disorder, acute pain, and chronic pain. It is administered under the tongue, in the cheek, by injection (intravenous or subcutaneous), or as a skin patch or implant. Maximum pain relief generally occurs within an hour and lasts up to 24 hours. In the United States, buprenorphine/naloxone (Suboxone) is usually prescribed to discourage injection misuse. Both formulations are Schedule III controlled substances.[2]
Buprenorphine acts as an agonist, partial agonist, or antagonist at different opioid receptors. It relieves opioid withdrawal and reduces the effects of other opioids. Unlike full agonists such as heroin and methadone, it has a ceiling effect for some effects, including respiratory depression, but retains misuse potential.[2]
Side effects include respiratory depression, sleepiness, adrenal insufficiency, QT prolongation, low blood pressure, allergic reactions, constipation, and opioid addiction. It may increase seizure risk in susceptible people; opioid withdrawal after discontinuation is generally less severe than with other opioids. Safety during pregnancy is unclear, but use while breastfeeding is probably safe: infants receive approximately 1–2% of the maternal weight-adjusted dose.[2]
Buprenorphine was patented in 1965, FDA approved for medical use as an analgesic in 1981, and FDA approved for treating opioid use disorder in 2002. It is on the World Health Organization's List of Essential Medicines. Despite originally being marketed as an analgesic it is far more commonly prescribed and used to treat opioid use disorders, such as addiction to heroin. In 2020, it was the 186th most commonly prescribed medication in the United States, with more than 2.8 million prescriptions.[2]
History
History
Buprenorphine was first synthesised from thebaine in 1966. In 1969, researchers at Reckitt and Colman (now Reckitt Benckiser) had spent 10 years attempting to synthesize an opioid compound "with structures substantially more complex than morphine [that] could retain the desirable actions whilst shedding the undesirable side effects". Physical dependence and withdrawal from buprenorphine itself remain important issues since buprenorphine is a long-acting opioid. Reckitt found success when researchers synthesized RX6029 which had shown success in reducing dependence in test animals. RX6029 was named buprenorphine and began trials on humans in 1971. Buprenorphine was approved for use in humans in 1977 in the UK and 1982 in the US. Buprenorphine was first used in dogs in the 1980s and in cats in the 1990s. A 0.3mg/ml formulation for use in cats was approved in 1995, a higher strength 1.8mg/ml formulation was approved in 2014, and a transdermal patch was approved in 2022.[14–17] WP
Legal status
- In the European Union, buprenorphine can be prescribed either alone or in combination with another substance and is approved for the treatment of opioid addiction.[18] PW
- Austria: Buprenorphine is legal for medical use under the AMG (Arzneimittelgesetz Österreich) and illegal when sold or possessed without a prescription under the SMG (Suchtmittelgesetz Österreich). PW⚠ PsychonautWiki itself has flagged this text: citation needed.
- Canada: Buprenorphine is a schedule I substance in Canada and is only available with a valid prescription.[19] PW
- Germany: Buprenorphine is controlled under Anlage III BtMG (Narcotics Act, Schedule III) as of September 1, 1984. It can only be prescribed on a narcotic prescription form.[20]
[21] PW - Netherlands: Buprenorphine a List II drug of the Opium Law, although special rules apply to its prescription and dispensation. PW⚠ PsychonautWiki itself has flagged this text: citation needed.
- Russia: Buprenorphine is a Schedule II controlled substance.[22] PW
- Sweden: Buprenorphine is a class IV controlled substance.[23] PW
- Switzerland: Buprenorphine is a controlled substance specifically named under Verzeichnis A. Medicinal use is permitted.[24] PW
- United States: Buprenorphine, either alone or in combination with naloxone (as, for example, Suboxone), is a Schedule III drug. PW⚠ PsychonautWiki itself has flagged this text: citation needed.
- Prior to the approval of Suboxone in the U.S. for treating opioid addiction, the Drug Addiction Treatment Act of 2000 was passed. This law gives the Secretary of Health and Human Services the authority to grant a waiver to all physicians with appropriate training to prescribe and administer narcotics from Schedules III-V in the treatment of drug addiction. Prior to the passage of this law such authority was restricted solely to physicians working in an outpatient clinic specifically designed for treatment of addiction. The waiver, which requires the physician to undergo an 8-hour training course, initially allowed that physician to treat only 10 patients in this manner; as of 2016, this limit has been increased to 275.[25] PW
United states
In the United States, buprenorphine and buprenorphine with naloxone were approved for opioid use disorder by the Food and Drug Administration in October 2002. The DEA rescheduled buprenorphine from a schedule V drug to a schedule III drug just before approval. The ACSCN for buprenorphine is 9064, and being a schedule III substance, it does not have an annual manufacturing quota imposed by the DEA. The salt in use is hydrochloride, which has a free-base conversion ratio of 0.928.[26]
In the years before buprenorphine/naloxone was approved, Reckitt Benckiser had lobbied Congress to help craft the Drug Addiction Treatment Act of 2000, which gave authority to the Secretary of Health and Human Services to grant a waiver to physicians with certain training to prescribe and administer schedule III, IV, or V narcotic drugs for the treatment of addiction or detoxification. Before this law was passed, such treatment was permitted only in clinics designed specifically for drug addiction.[29] WP
The waiver, which can be granted after the completion of an eight-hour course, was required for outpatient treatment of opioid addiction with buprenorphine from 2000 to 2021. Initially, the number of people each approved physician could treat was limited to 10. This was eventually modified to allow approved physicians to treat up to 100 people with buprenorphine for opioid addiction in an outpatient setting. This limit was increased by the Obama administration, raising the number of patients to which doctors can prescribe to 275. On 14 January 2021, the US Department of Health and Human Services announced that the waiver would no longer be required to prescribe buprenorphine to treat up to 30 people concurrently.[30]
New Jersey authorized paramedics to give buprenorphine to people at the scene after they have recovered from an overdose.[33] WP
Europe
In the European Union, Subutex and Suboxone, buprenorphine's high-dose sublingual tablet preparations, were approved for opioid use disorder treatment in September 2006. In the Netherlands, buprenorphine is a list II drug of the Opium Law, though special rules and guidelines apply to its prescription and dispensation. In France, buprenorphine prescription by general practitioners and dispensed by pharmacies has been permitted since the mid-1990s as a response to HIV and overdose risk. Deaths caused by heroin overdose were reduced by four-fifths between 1994 and 2002, and the incidence of AIDS among people who inject drugs in France fell from 25% in the mid-1990s to 6% in 2010.[34]
Barriers to access
In the US, the list price for a long-acting injectable form is five to 20 times as much as a daily pill. This has reduced the number of people who are able to get a single monthly dose, instead of daily pills. Some jails consider the more expensive form a positive tradeoff: a single monthly injection may be simpler and easier for the staff to manage than daily trips to the dispensary to have a nurse provide a pill and make sure that it has been swallowed.[36] WP
Brand names
Buprenorphine is available under the brand names Cizdol, Brixadi (approved in the US by FDA for addiction treatment in 2023), Suboxone (with naloxone), Subutex (typically used for opioid use disorder), Zubsolv, Bunavail, Buvidal (approved in the UK, Europe and Australia for addiction treatment in 2018), Sublocade (approved in the US in 2018), Probuphine, Temgesic (sublingual tablets for moderate to severe pain), Buprenex (solutions for injection often used for acute pain in primary-care settings), Norspan, and Butrans (transdermal preparations used for chronic pain). In Poland buprenorphine is available under the trade names Bunondol (for pain treatment, when morphine is too little; amounts of 0.2 mg and 0.4 mg) and Bunorfin (for addicts substitution in amount of 2 and 8 mg).[37–40] WP
Pharmacology
Opioid receptor modulator
Buprenorphine has been reported to possess these following pharmacological activities:[43] WP
- μ-Opioid receptor (MOR): extremely high affinity partial agonist: at low doses, the MOR-mediated effects of buprenorphine are comparable to those of other narcotics, but these effects reach a "ceiling" as the receptor population is saturated. This behavior is responsible for several unique properties: buprenorphine greatly reduces the effect of most other MOR agonists, can cause precipitated withdrawal when used in actively opioid dependent persons, and has a lower incidence of respiratory depression relative to full MOR agonists.[46]
[51] [52] [53] WP - κ-Opioid receptor (KOR): High affinity antagonist/weak partial agonist —this activity is hypothesized to underlie some of the effects of buprenorphine on mood disorders and addiction.[51]
[54] [55] [56] WP - δ-Opioid receptor (DOR): High affinity antagonist[51]
[57] WP - Nociceptin receptor (NOP, ORL-1): Weak affinity, very weak partial agonist[51] WP
In simplified terms, buprenorphine can essentially be thought of as a nonselective, mixed agonist–antagonist opioid receptor modulator, acting as an unusually high affinity, weak partial agonist of the MOR, a high affinity antagonist of the KOR and DOR, and a relatively low affinity, very weak partial agonist of the ORL-1/NOP.[46]
Although buprenorphine is a partial agonist of the MOR, human studies have found that it acts like a full agonist with respect to analgesia in opioid-intolerant individuals. Conversely, buprenorphine behaves like a partial agonist of the MOR with respect to respiratory depression.[63] WP
Buprenorphine is also known to have high binding affinity with antagonistic activity at the putative ε-opioid receptor.[64]
Full analgesic efficacy of buprenorphine requires both exon 11- and exon 1-associated μ-opioid receptor splice variants.[66]
The active metabolites of buprenorphine are not thought to be clinically important in its CNS effects.[63] WP
In positron emission tomography (PET) imaging studies, buprenorphine was found to decrease whole-brain MOR availability due to receptor occupancy by 41% (i.e., 59% availability) at 2 mg, 80% (i.e., 20% availability) at 16 mg, and 84% (i.e., 16% availability) at 32 mg.[68–71] WP
Other actions
Unlike some other opioids and opioid antagonists, buprenorphine binds only weakly to and possesses little if any activity at the sigma receptor.[72]
Buprenorphine also blocks voltage-gated sodium channels via the local anesthetic binding site, and this underlies its potent local anesthetic properties.[50] WP
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.[48] WP
Pharmacokinetics
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). The glucuronidation of buprenorphine is primarily carried out by UGT1A1 and UGT2B7, and that of norbuprenorphine by UGT1A1 and UGT1A3. These glucuronides are then eliminated mainly through excretion into bile. The elimination half-life of buprenorphine is 20 to 73 hours (mean 37 hours). Due to the mainly hepatic elimination, no risk of accumulation exists in people with renal impairment.[74] WP
One of the major active metabolites of buprenorphine is norbuprenorphine, which, in contrast to buprenorphine itself, is a full agonist of the MOR, DOR, and ORL-1, and a partial agonist at the KOR. However, relative to buprenorphine, norbuprenorphine has extremely little antinociceptive potency (1/50th that of buprenorphine), but markedly depresses respiration (10-fold more than buprenorphine). This may be explained by very poor brain penetration of norbuprenorphine due to a high affinity of the compound for P-glycoprotein. In contrast to norbuprenorphine, buprenorphine and its glucuronide metabolites are negligibly transported by P-glycoprotein.[75]
The glucuronides of buprenorphine and norbuprenorphine are also biologically active, and represent major active metabolites of buprenorphine. Buprenorphine-3-glucuronide has affinity for the MOR (Kᵢ = 4.9 pM), DOR (Kᵢ = 270 nM) and ORL-1 (Kᵢ = 36 μM), and no affinity for the KOR. It has a small antinociceptive effect and no effect on respiration. Norbuprenorphine-3-glucuronide has no affinity for the MOR or DOR, but does bind to the KOR (Kᵢ = 300 nM) and ORL-1 (Kᵢ = 18 μM). It has a sedative effect but no effect on respiration.[78] WP
Detection in body fluids
Buprenorphine and norbuprenorphine may be quantified in blood or urine to monitor use or non-medical recreational use, confirm a diagnosis of poisoning, or assist in a medicolegal investigation. A significant overlap of drug concentrations exists in body fluids within the possible spectrum of physiological reactions ranging from asymptomatic to comatose. Therefore, knowing both the route of administration of the drug and the level of tolerance to opioids of the individual is critical when results are interpreted.[79] WP
Receptor binding · Wikipedia
Buprenorphine
| Site | Kᵢ (nM) | Action | Species | Stimulation |
|---|---|---|---|---|
| MOR (μ-Opioid receptor) | 0.2~0.9; 0.081 | Partial agonist | Human; Monkey | 48%±5%[41–45] WP |
| DOR (δ-Opioid receptor) | 2.9–6.1; 0.82 | Antagonist | Human; Monkey | 0[41] |
| KOR (κ-Opioid receptor) | 0.62–2.5; 0.44 | Antagonist/functional antagonism | Human; Monkey | 9%±5[41] |
| NOP (Nociceptin receptor) | 77.4 | Partial agonist | Human | ~50%±10% (8 mg≥)[42] |
| σ₁ | >100,000 | ND (No data) | ND (No data) | [45] |
| σ₂ | ND (No data) | ND (No data) | ND (No data) | [45] WP |
| NMDA (N-Methyl-D-aspartate receptor) | ND (No data) | ND (No data) | ND (No data) | [45] WP |
| TLR4 (Toll-like receptor 4) | >10,000 | Agonist | Human | [45] |
| SERT (Serotonin transporter) | >100,000 | ND (No data) | Rat | [45] |
| NET (Norepinephrine transporter) | >100,000 | ND (No data) | Rat | [45] |
| DAT (Dopamine transporter) | ND (No data) | ND (No data) | ND (No data) | [45] WP |
| VGSC (Voltage-gated sodium channel) | 33,000 (IC₅₀) | Inhibitor | Rodent | [45] |
Chemistry
- Formula
- C29H41NO4 PC
- CAS number
- 52485-79-7 PC
- Molar mass (g/mol)
- 467.6 PC
- IUPAC name (computed by PubChem)
- (1S,
2S, PC6R, 14R, 15R, 16R) - 5- (cyclopropylmethyl) - 16- [(2S) - 2- hydroxy- 3, 3- dimethylbutan- 2- yl] - 15- methoxy- 13- oxa- 5- azahexacyclo[13.2.2.12, 8.01, 6.02, 14.012, 20] icosa- 8(20) , 9, 11- trien- 11- ol - SMILES
- C[C@]
([C@H] PC1C[C@@] 23CC[C@@] 1([C@H] 4[C@@] 25CCN([C@@H] 3CC6=C5C(=C(C=C6) O) O4) CC7CC7) OC) (C(C) (C) C) O - InChIKey
- RMRJXGBAOAMLHD-
IHFGGWKQSA- PCN - PubChem CID
- 644073
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References
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