Evaluation of pentamorphone in humans: a new potent opiate.

Abstract

We evaluated the analgesic properties of 14-beta-n-pentylaminomorphinone (pentamorphone), a new morphinan derivative, in 23 male volunteers divided into 6 groups who were given either placebo (1 per group) or 0.015, 0.03, 0.06, 0.12, 0.24, 0.48 microgram.kg-1 pentamorphone intravenously. Analgesia was evaluated by the maximal tolerance to a spring-loaded rod on the tibia and manubrium. Analgesic assessments and arterial blood samples were taken prior to and at set time intervals following drug administration. Pentamorphone produced a linear increase in pain tolerance with increasing dose as well as a dose-dependent depression of ventilation. Pentamorphone had no effect on blood pressure or heart rate in the doses used. Plasma histamine levels at 5 minutes were not elevated with any of the dosages. Pentamorphone appears to be an analgesic with clinically tolerable side effects in the range 0.12 to 0.24 microgram.kg-1 that merits further evaluation under clinical conditions.

• Authors: P S Glass, E M Camporesi, D Shafron, T Quill, J G Reves
• Journal: Anesthesia and analgesia (Anesth Analg) Vol. 68 Issue 3 Pg. 302-7 (Mar 1989) ISSN: 0003-2999 [Print] United States
• PMID: 2465708 (Publication Type: Clinical Trial, Controlled Clinical Trial, Journal Article, Research Support, U.S. Gov't, P.H.S.)

Chemical References

• Analgesics
• pentamorphone
• Hydromorphone

Topics

• Analgesics (adverse effects, pharmacology)
• Dose-Response Relationship, Drug
• Humans
• Hydromorphone (analogs & derivatives, pharmacology)
• Male
• Pain (physiopathology)
• Respiration (drug effects)
• Sensory Thresholds (drug effects)