Monday, February 19, 2018

Pentazocine-opioid antagonist and its pharmacology

The first mixed agonist and antagonist analgesic to be marketed. It is an agonist at the kappa and sigma opoid receptor and has a weak antagonist action at the mu receptor.

Therapeutic Uses
-Pentazocine is used to treat pain.

Side effects
-Joint and muscle pain.
-Painful or difficult urination
-Sore throat
-Shortness of breath
-Chest pain

Bioavailability                                 20% orally
Metabolism                                      Hepatic
Onset of action                                15min
Biological half-life                            2 to 3 hours
Excretion                                            Renal     

Mechanism of action
The preponderance of evidence suggests that pentazocine antagonizes the opioid effects by competing for the same receptor sites, especially the opioid mu receptor.

Drug-drug interaction
1-Pentazocine+Acepromazine= It may increase the hypotensive activities of                                                                           
2-Pentazocine+Amphetamine= It may increase the analgesic activities of                        
3-Pentazocine+Amiloride= The risk or severity of adverse effect can be increase.
4-Pentazocin+Azelastine= Pentazocine may increase the centralnervous system 
                                               depressant activities of azelastin


Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no 479,480,482

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