Buprenorphine: A Review of its Pharmacological Properties and Therapeutic Efficacy

@article{Heel2012BuprenorphineAR,
  title={Buprenorphine: A Review of its Pharmacological Properties and Therapeutic Efficacy},
  author={Rennie C. Heel and Rex N. Brogden and Trevor M. Speight and Graeme S. Avery},
  journal={Drugs},
  year={2012},
  volume={17},
  pages={81-110}
}
SummarySynopsis: Buprenorphine1, a derivative of the morphine alkaloid thebaine, is a strong analgesic with marked narcotic antagonist activity. In studies in relatively small groups of postoperative patients with moderate to severe pain, one or a few doses of buprenorphine parenterally (by intramuscular or slow intravenous injection) or sublingually2 were at least as effective as standard doses of other strong analgesics such as morphine, pethidine or pentazocine, and buprenorphine was longer… 
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References

SHOWING 1-10 OF 78 REFERENCES
Pentazocine: A Review of its Pharmacological Properties, Therapeutic Efficacy and Dependence Liability
TLDR
There may be a limit to the analgesia which pentazocine can provide, although such a phenomenon has not been demonstrated in man, and the respiratory depressant effect of pentazOCine in comparison with that of other strong analgesic drugs remains a disputed point.
Butorphanol: A Review of its Pharmacological Properties and Therapeutic Efficacy
TLDR
Studies in animal models and in a few volunteers have suggested that butorphanol may have a lower dependence liability than narcotic drugs such as morphine or pethidine, and if this is indeed the case it will offer an important advantage over these agents.
Human pharmacology and abuse potential of the analgesic buprenorphine: a potential agent for treating narcotic addiction.
TLDR
Buprenorphine has potential for treating narcotic addiction since it is acceptable to addicts, is long-acting, produces a low level of physical dependence such that patients may be easily detoxified, is less toxic than drugs used for maintenance therapy, and blocks the effects of narcotics.
Buprenorphine hydrochloride: Determination of analgesic potency
  • A. Dobkin
  • Medicine
    Canadian Anaesthetists' Society journal
  • 1977
TLDR
It was concluded that buprenorphine hydrochloride 0.2 to 0.4 mg provided relief of severe pain probably as well as is observed with morphine 10 mg for the average-size patient, but the duration of pain relief with the new compound is substantially longer than with other strong analgesics previously tested.
A comparison of buprenorphine and pethidine for immediate postoperative pain relief by the i.v. route.
TLDR
When the drugs were compared on a "dose per body weight" basis the results supported a ratio of potency in the order of 1 : 200 in favour of buprenorphine, but a similar frequency of nausea was observed with both agents.
Buprenorphine: a new potent long-acting synthetic analgesic. Comparison with morphine.
TLDR
A new thebaine derivative, buprenorphine, 0.6 mg, was compared with morphine 15 mg in a double-blind trial, in patients recovering from elective Caesarean section, with no serious side-effects encountered.
The role of analgesics in respiratory depression: a rabbit model
TLDR
Both pethidine and its metabolites are factors in the persisting depression, while buphrenorphine compared well with pETHidine and fentanyl.
A double blind comparison of buprenorphine and morphine in conscious subjects following administration by the intramuscular route.
TLDR
Buprenorphine produced a more prolonged displacement of the carbon dioxide response curve than morphine, and there was a linear relationship over the dose range 0.15-1.2 mg in terms of respiratory depression.
Comparison of buprenorphine, pethidine and pentazocine for the relief of pain after operation.
  • B. Hovell
  • Medicine, Biology
    British journal of anaesthesia
  • 1977
TLDR
Buprenorphine 4-8 microgram-kg-1 was shown to be an effective analgesic, superior in some cases to the other drugs in the doses employed in the study.
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