BUPRENORPHINE HYDROCHLORIDE

BUPRENORPHINE HYDROCHLORIDE Property

Melting point:

260-262?C (dec.)

storage temp. 

-0°C

solubility 

Sparingly soluble in water, freely soluble in methanol, soluble in ethanol (96 per cent), practically insoluble in cyclohexane.

form 

Powder

Water Solubility 

Soluble to 25 mM in water and to 50 mM in ethanol

Safety

Hazard Codes 

Xn,T,F

Risk Statements 

22-62-63-39/23/24/25-23/24/25-11

Safety Statements 

26-36-45-36/37-16-7

WGK Germany 

3

RTECS 

KM7758000

HS Code 

2939110000

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H361Suspected of damaging fertility or the unborn child

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P281Use personal protective equipment as required.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P308+P313IF exposed or concerned: Get medical advice/attention.

P330Rinse mouth.

P405Store locked up.

P501Dispose of contents/container to..…

BUPRENORPHINE HYDROCHLORIDE Chemical Properties,Usage,Production

Description

Buprenorphine (hydrochloride) (CRM) (Item No. ISO60178) is a certified reference material that is structurally categorized as an opioid. It is a partial agonist of the μ-opioid receptor (K_i = 4.18 nM) that less potently acts at δ- and κ-opioid receptors (K_is = 25.8 and 12.9 nM, respectively). Buprenorphine is used, alone or with naloxone (Item Nos. ISO60194 | 15594), to counter opiate addiction. This product is intended for research and forensic applications.

Chemical Properties

White Solid

Uses

Controllled substance (narcotic). Analgesic that demonstrates narcotic agonist-antagonist properties.

Definition

ChEBI: The hydrochloride salt of buprenorphine.

brand name

Buprenex (Reckitt Benckiser); Subutex (Reckitt Benckiser).

Acquired resistance

Buprenorphine is 20 to 50 times more potent than morphine in producing an ED50 analgesic effect in animal studies; however, it cannot produce an ED100 (compared to morphine) in these tests. Thus, buprenorphine is a potent partial agonist at μ opioid receptors. It also is a partial agonist at κreceptors but more of an antagonist at δ receptors. Buprenorphine, at 0.4 mg intramuscular dose, will produce the same degree of analgesia as 10 mg of morphine. Because of its partial agonist properties, it has a lower ceiling on its analgesic action but also produces less severe respiratory depression. It is incapable of producing tolerance and addiction comparable to full μ agonists. In fact, buprenorphine's partial agonist action, very high affinity for opioid receptors, and high lipophilicity combine to give buprenorphine a tolerance, addiction, and withdrawal profile that is unique among the opioids. When given by itself to opioid-naive patients, little tolerance or addictive potential (Schedule 5) is observed. A mild withdrawal can occur some 2 weeks after the last dose of buprenorphine. Buprenorphine will precipitate withdrawal symptoms in highly addicted individuals, but it will suppress symptoms in individuals who are undergoing withdrawal from opioids. It effectively blocks the effect of high doses of heroin. Because of these properties, buprenorphine has been approved for office-based use in treating opioid dependence. It also has been reported to suppress cocaine use and addiction.

Biological Activity

ORL 1 receptor agonist that also displays mixed antagonist/partial agonist activity at κ , δ and μ -opioid receptors.

Biochem/physiol Actions

Full agonist at ORL1 receptors, antagonist or partial agonist at μ, κ, and δ opioid receptors.

Clinical Use

Buprenorphine undergoes extensive first-pass 3-O-glucuronidation, which negates its usefulness after oral dose. It is available in parenteral and sublingual dosage forms. The typical dose is 0.3 to 0.6 mg three times per day by intramuscular injection for analgesia or 8 mg/day as a sublingual tablet for opioid-dependence maintenance. The duration of analgesic effect is 4 to 6 hours. After parenteral dose, approximately 70% of the drug is excreted in the feces, and the remainder appears as N-dealkylated and conjugated metabolites in the urine. Naloxone is not an effective antagonist to buprenorphine because of the latter's high binding affinity to opioid receptors.

storage

Store at RT

References

[1] BART G. Maintenance medication for opiate addiction: the foundation of recovery.[J]. Journal of Addictive Diseases, 2012, 31 3: 207-225. DOI: 10.1080/10550887.2012.694598
[2] JEANETTE M TETRAULT D A F. Current and potential pharmacological treatment options for maintenance therapy in opioid-dependent individuals.[J]. Drugs, 2012, 72 2: 217-228. DOI: 10.2165/11597520-000000000-00000
[3] KELLY YAN CHEN  Jianren M  Lucy Chen. Buprenorphine-naloxone therapy in pain management.[J]. Anesthesiology, 2014, 120 5: 1262-1274. DOI: 10.1097/aln.0000000000000170
[4] M.M. VANDEPUTTE. Detection, Chemical Analysis and Pharmacological Characterization of Dipyanone and other New Synthetic Opioids Related to Prescription Drugs[J]. Emerging trends in drugs, addictions, and health, 2024, 4: Article 100130. DOI: 10.1016/j.etdah.2023.100130