Buprenorphine acts as a partial agonist of the μ-opioid receptor with a binding affinity of Ki = 1.5 nM in contrast to full agonists like morphine. It also acts as an antagonist of the κ-opioid receptor with a binding affinity of Ki = 2.5 nM and the δ-opioid receptor with a binding affinity of Ki = 6.1 nM. The ratio of these binding affinities is important, if you compare morphine's binding ratio of 1:50:176 to Buprenorphine's ratio of 15:25:61, it is apparent that the side-effect profile will be much higher to Buprenorphine and μ-opioid stimulation for euphoric effects, sequentially the drug will also bind to delta and kappa opioid receptors to a comparatively high degree.
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.
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.
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.
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.
As with other opioids,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.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,3 - 71 - 2 weeks to be back at baseline (in the absence of further consumption). Buprenorphine presents cross-tolerance with Cross-all other opioids, meaning that after the consumption of buprenorphine all opioids will have a reduced effect.
- 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.
- 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.
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.
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).
Canada: Buprenorphine is a schedule I substance in Canada and is only available with a valid prescription.
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.
Netherlands: Buprenorphine a List II drug of the Opium Law, although special rules apply to its prescription and dispensation.
Russia: Buprenorphine is a Schedule II controlled substance.
Sweden: Buprenorphine is a class IV controlled substance.
Switzerland: Buprenorphine is a controlled substance specifically named under Verzeichnis A. Medicinal use is permitted.
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.
Responsible use
Depressants
Oxycodone
Kratom
Buprenorphine (Wikipedia)
Buprenorphine (Erowid Vault)
Buprenorphine (Isomer Design)
Buprenorphine (DrugBank)
Buprenorphine (Drugs.com)
Buprenorphine (Drugs-Forum)
Buprenorphine can be administered via insufflated, sublingual. The route of administration can influence both the onset and intensity of pain relief.