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HOME >> API >> API List 4 >> Buprenorphine HCl >> Drug Description

DRUG DESCRIPTION
Buprenorphine HCl CAS No: [53152-21-9]

Buprenorphine hydrochloride is a white powder, weakly acidic with limited solubility in water (17 mg/mL). Chemically, buprenorphine is 17-(cyclopropylmethyl)-α-(1,1-dimethylethyl)-4,5-epoxy-18,19-dihydro-3-hydroxy-6-methoxy-α-methyl-6,14-ethenomorphinan-7-methanol, hydrochloride [5α,7α(S|]-. Buprenorphine hydrochloride has the molecular formula C₂₉H₄₁NO₄ HCI and the molecular weight is 504.10.

A thebaine derivative, buprenorphine is a synthetic partial opiate agonist. It occurs as a white, crystalline powder with a solubility of 17 mg/ml in water and 42 mg/ml in alcohol. The commercially available injectable product has a pH of 3.5-5 and is a sterile solution of the drug dissolved in D5W. Terms of potency are expressed in terms of buprenorphine. The commercial product contains 0.324 mg/ml of buprenorphine HCl, which is equivalent to 0.3 mg/ml of buprenorphine.

Buprenorphine has partial agonist activity at the mu receptor. This is in contrast to pentazocine which acts as an antagonist at the mu receptor. Buprenorphine is considered to be 30 times as potent as morphine and exhibits many of the same actions as the opiate agonists; it produces a dose-related analgesia. It appears to have a high affinity for mu receptors in the CNS, which may explain its relatively long duration of action.

The cardiovascular effects of buprenorphine may cause a decrease in both blood pressure and cardiac rate. Rarely, human patients may exhibit increases in blood pressure and cardiac rate. Respiratory depression is a possibility, and decreased respiratory rates have been noted in horses treated with buprenorphine. Gastrointestinal effects appear to be minimal with buprenorphine

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