Pentazocine: A Review of its Pharmacological Properties, Therapeutic Efficacy and Dependence Liability

@article{Brogden2012PentazocineAR,
  title={Pentazocine: A Review of its Pharmacological Properties, Therapeutic Efficacy and Dependence Liability},
  author={Rex N. Brogden and Trevor M. Speight and Graeme S. Avery},
  journal={Drugs},
  year={2012},
  volume={5},
  pages={6-91}
}
SummarySynopsis: Pentazocine2, the N-allyl derivative of the narcotic analgesic phenazocine, is a strong analgesic with weak narcotic antagonist activity. It is advocated for the relief of moderate to severe pain. Pentazocine has a low abuse potential and is not controlled by narcotic regulations. Therapeutic trials comparing pentazocine with other strong analgesics have shown it to possess a strong analgesic effect when given intramuscularly and a lesser analgesic effect when administered… 
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References

SHOWING 1-10 OF 198 REFERENCES
Profiles of Activity in Rodents of Some Narcotic and Narcotic Antagonist Drugs
TLDR
New tests in rodents are described that are devised to indicate those features of the activity of pentazocine that are important for its clinical usefulness in man and from antipyretic analgesics, such as aspirin and mefenamic acid.
THE PAIN‐RELIEVING PROPERTIES OF PENTAZOCINE, A NEW NON‐NARCOTIC ANALGESIC
  • M. Ende
  • Medicine, Biology
    Journal of the American Geriatrics Society
  • 1965
TLDR
The investigation described in this report was undertaken to investigate the N-dimethylallyl analog of phenazocine, a known narcotic-antagonist, which has been shown in a number of clinical studies to be a highly effective analgesic with no serious side effects.
Studies of analgesic drugs
TLDR
Methylphenidate significantly antagonized the respiratory depression of pentazocine compared to a placebo in a complete crossover study of six healthy subjects.
The reversal of pentazocine–induced respiratory depression
TLDR
The present work was undertaken to evaluate the antagonistic action of a more commonly used analeptic, nikethamide, which is of interest because the World Health Organisation have recommended that it need not at present be subject to international or national narcotics contro12.
Oral pentazocine: a study of its sedative properties.
TLDR
It is suggested that the mild sedative properties of pentazocine will enable this drug to be used with benefit in patients with chronic pain while if relief of anxiety is desired, the concomitant administration of a sedative drug may be required.
Pentazocine: massive dosage without side effects.
TLDR
Pentazocine (Talwin) is a potent but non-narcotic analgesic agent that has the analgesic effect of 50 to 75 mg of meperidine or 10 mg of morphine.
Tolerance and dependence on pentazocine.
TLDR
The effects of pentazocine administered for prolonged periods in two patients with chronic pain of nonmalignant origin, claimed not to produce tolerance and physical dependence are reported.
Measurement of the analgesic efficacy and potency of pentazocine by the D'Amour and Smith method.
TLDR
With suitable adjustment of stimulus strength, the analgesic action of pentazocine may be demonstrated in rats by the method of D9Amour and Smith and the rank order for potency and efficacy was morphine > meperidine > pentazo cine.
An assessment of the analgesic efficacy of oral pentazocine.
TLDR
It is concluded that oral pentazocine represents a useful addition to the analgesic range, and its freedom from narcotic control should encourage the use of the drug for chronic pain.
The analgesic effectiveness of nalorphine and nalorphine-morphine combinations in man.
TLDR
The data suggest a significant species difference in nalorphine effect in animals, and the difficulties involved in the formulation of clinically useful naloralorphine-morphine mixtures are discussed.
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