Buprenorphine

Fatal overdose may occur when opiates are combined with other depressants such as benzodiazepines, barbiturates, gabapentinoids, thienodiazepines, alcohol or other GABAergic substances. It is strongly discouraged to combine these substances, particularly in common to heavy doses.

Buprenorphine
Chemical Nomenclature
Common names	Buprenex, Subutex, Butrans, Cizdol, Addnok, Transtec
Systematic name	(2S)-2-[(5R,6R,7R,14S)-9α-cyclopropylmethyl-4,5-epoxy-6,14-ethano-3-hydroxy-6-methoxymorphinan-7-yl]-3,3-dimethylbutan-2-ol
Class Membership
Psychoactive class	Opioid
Chemical class	Morphinan
Routes of Administration
WARNING: Always start with lower doses due to differences between individual body weight, tolerance, metabolism, and personal sensitivity. See responsible use section. ⇣ Sublingual Dosage Bioavailability 30% Threshold <=0.3 mg Light 1 - 2 mg Common 2 - 4 mg Strong 4 - 8 mg Heavy 8mg + Duration Total 18 - 24 hours Onset 40 - 80 minutes Peak 1.5 - 2 hours After effects 1 - 3 days ⇣ Insufflated Dosage Bioavailability 48% Threshold < 0.2 mg Light 0.2 - 0.4 mg Common 0.4 - 0.8 mg Strong 0.8 - 1.5 mg Heavy 1.5 mg + Duration Total 8 - 14 hours Onset 30 - 60 minutes Peak 4 - 8 hours After effects 1 - 3 days DISCLAIMER: PW's dosage information is gathered from users and resources for educational purposes only. It is not a recommendation and should be verified with other sources for accuracy.
Interactions
Stimulants
MAOIs
Nitrous
PCP
Alcohol
Benzodiazepines
DXM
GHB
GBL
Ketamine
MXE
Tramadol
Grapefruit

Summary sheet: Buprenorphine

Buprenorphine is a semisynthetic opioid within the morphinan family. It functions as a mixed partial agonist opioid receptor modulator. At higher dosages, it is used to treat opioid addiction in higher, in lower dosages it is used to control moderate-acute pain in non-opioid-tolerant individuals and in even lower dosages it is used to control moderate chronic pain.

Chemistry

Buprenorphine is a semi-synthetic morphinan derivative of the opioid alkaloid thebaine. Like many opioids, such as codeine or hydrocodone, it is has a morphinan backbone.

Buprenorphine and other molecules of this class contain a polycyclic core of three benzene rings fused in a zig-zag pattern called phenanthrene. A fourth nitrogen containing ring is fused to the phenanthrene at R₉ and R₁₃. Buprenophine (along with other morphinans) contains an ether bridge between two of its rings, connecting the benzene and opposite cyclohexane ring through an oxygen group. Buprenorphine is unique to human medical opioids as it contains an addition fused ring which connects to the lower cyclohexane ring at R₆ and R₁₄. This structure is called a endoethenotetrahydrooripavine backbone, often found in veterinarian opioids. It contains a hydroxy group (OH-) substituted on the benzene ring and a methoxy group bound to the lower cyclohexane ring. The backbone of buprenorphine is also substituted with a methyl cyclopropyl moeity on its amino group. Adjacent to its methoxy attachment, the cyclohexane ring is bonded to R₂ of a 2-butanol chain.

Pharmacology

This pharmacology section is incomplete. You can help by adding to it.

Buprenorphine acts as a partial agonist of the μ-opioid receptor with a binding affinity of K~i~ = 1.5 nM; it also acts as an antagonist of the κ-opioid receptor with a binding affinity of K~i~ = 2.5 nM and the δ-opioid receptor with a binding affinity of K~i~ = 6.1 nM.

Buprenorphine exerts its effects by binding to and activating the μ-opioid receptor. This occurs because opioids structurally mimic endogenous endorphins which are naturally found within the body and also work upon the μ-opioid receptor set. The way in which opioids structurally mimic these natural endorphins results in their euphoria, pain relief and anxiolytic effects. This is because endorphins are responsible for reducing pain, causing sleepiness, and feelings of pleasure. They can be released in response to pain, strenuous exercise, orgasm, or general excitement.

Subjective effects

The effects listed below are based upon the subjective effects index and personal experiences of PsychonautWiki contributors. The listed effects will rarely (if ever) occur all at once, but heavier dosages will increase the chances and are more likely to induce a full range of effects.

Physical effects

The general head space of buprenorphine is described by many as one of euphoria, relaxation, anxiety suppression and pain relief.

• Pain relief
• Physical euphoria - This particular substance can be considered as less intense in its physical euphoria when compared with that of morphine or diacetylmorphine (heroin) due to it being a partial agonist of the μ-opioid receptor. The sensation itself can be described as extreme feelings of intense physical comfort, warmth and bliss which spreads throughout the body.
• Itchiness
• Respiratory depression - Buprenorphine causes less respiratory depression than other opioids due to it being a partial agonist of the μ-opioid receptor.
• Dizziness
• Sedation
• Decreased heart rate
• Constipation
• Cough suppression
• Decreased libido
• Difficulty urinating
• Pupil constriction
• Nausea - Buprenorphine causes substantially more nausea and vomiting than other opioids.
• Appetite suppression
• Orgasm suppression

Cognitive effects

• Cognitive euphoria - This particular substance can be considered as less intense in its cognitive euphoria when compared with that of morphine or diacetylmorphine (heroin) due to it being a partial agonist of the μ-opioid receptor. It is still, however, capable of extreme intensity and overwhelming bliss at heavier dosages with a low tolerance. The sensation itself can be described as powerful and overwhelming feeling of emotional bliss, contentment, and happiness.
• Anxiety suppression

Visual effects

• Internal hallucinations - One may experience a state of semi-consciousness and hypnagogia (colloquially, "nodding") during heavy dosage which results in dream-like states and up to level 3 imagery. This is often accompanied by ill-defined geometry.

Experience reports

There are currently no anecdotal reports which describe the effects of this compound within our experience index. Additional experience reports can be found here:

• Erowid Experience Vaults: Buprenorphine

Toxicity and harm potential

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.

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.

It is strongly recommended that one use harm reduction practices when using this drug.

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.

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 [[Cross-tolerance::all other opioids]], meaning that after the consumption of buprenorphine all opioids will have a reduced effect.

Dangerous interactions

Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption.

• Depressants (1,4-Butanediol, 2m2b, alcohol, barbiturates, benzodiazepines, GHB/GBL, methaqualone) - This combination can result in dangerous or even fatal levels of respiratory depression. These substances potentiate the muscle relaxation, sedation and amnesia caused by one another and can lead to unexpected loss of consciousness at high doses. There is also an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If unconsciousness occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Dissociatives - This combination can result in an increased risk of vomiting during unconsciousness and death from the resulting suffocation. If unconsciousness occurs, users should attempt to fall asleep in the recovery position or have a friend move them into it.
• Stimulants - It is dangerous to combine buprenorphine, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedative effect of buprenorphine, which is the main factor most people consider when determining their level of intoxication. Once the stimulant wears off, the effects of buprenorphine will be significantly increased, leading to intensified disinhibition as well as other effects. If combined, one should strictly limit themselves to only taking a certain amount of buprenorphine.

Legal issues

This legality section is a stub. As such, it may contain incomplete or wrong information. You can help by expanding it.

In the United States, buprenorphine, either alone or in combination with naloxone (as, for example, Suboxone), is a Schedule III drug.

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.

In the European Union, buprenorphine can be used either alone or in combination with another substance and is approved for the treatment of opioid addiction. In the Netherlands it is a List II drug of the Opium Law, although special rules apply to its prescription and dispensation.

See also

• Responsible use
• Depressants
• Oxycodone
• Kratom

External links

• Buprenorphine (Wikipedia)
• Buprenorphine (Erowid)
• Buprenorphine (TripSit)