Pentazocine

Chemical formula: C₁₉H₂₇NO  Molecular mass: 285.431 g/mol  PubChem compound: 441278

Mechanism of action

Pentazocine has both agonist and antagonist action at opioid receptors. Pentazocine interrupts nociceptive input in the spinal cord. These analgesic effects are probably due to agonist actions at ĸ-receptors. Pentazocine is a weak antagonist at µ-opioid receptors with about one fiftieth the potency of nalorphine.

Pharmacodynamic properties

Pentazocine is an opioid, benzomorphan derivative analgesic with actions and uses similar to those of morphine. It has weak narcotic antagonist actions.

Prolonged use of high doses of pentazocine may produce dependence. It is subject to abuse.

Pharmacokinetic properties

Absorption

Pentazocine is absorbed from the gastro-intestinal tract.

Distribution

Following administration by mouth, peak plasma concentrations are reached in 1 to 3 hours. After intramuscular injection, peak plasma concentrations are reached in 15 minutes to 1 hour. Pentazocine diffuses across the placenta.

Biotransformation

Pentazocine is metabolised in the liver.

Elimination

Only a small proportion of the dose administered appears unchanged in the urine.

Preclinical safety data

There are no preclinical safety data of relevance to the prescriber which are additional to that already included in other sections of this summary.

Related medicines

© All content on this website, including data entry, data processing, decision support tools, "RxReasoner" logo and graphics, is the intellectual property of RxReasoner and is protected by copyright laws. Unauthorized reproduction or distribution of any part of this content without explicit written permission from RxReasoner is strictly prohibited. Any third-party content used on this site is acknowledged and utilized under fair use principles.