INTRODUCTION:-
* It is an analgesic in the opioid category, patented (1955) and manufactured by Eli Lilly and Company.
* It is intended to treat mild pain and also has anti-tussive and local anaesthetic effects. The drug has been taken off the market in Europe and the US due to concerns of fatal overdoses and heart arrhythmias. An estimated 10 million patients have used these products.
* The drug is often referred to as the general form, “propoxyphene”, however only the dextro-isomer (dextropropoxyphene) has any analgesic effect. The levo-isomer appears to exhibit a very limited antitussive effect.
MECHANISM OF ACTION:-
* It acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the central nervous system (CNS).
* It primarily affects OP3 receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins
PHARMACOKINETICS:-
* VOLUME OF DISTRIBUTION:- 16L/Kgusu
HALF LIFE :- 6-12 hrs
* ROUTE OF ELIMINATION:- Kidney
DRUG-DRUG INTERACTIONS:-
* LYRICA+ DEXTROPROPOXYPHENE= Respiratory depression.
* ARICEPT+DEXTROPROPOXYPHENE=Liver disease
SIDE EFFECTS :-
* Dizziness
* Sedation
* Nausea
* Vomiting
* Delirium
* Somnolence
* Ataxia
* Coma
* Syncope and respiratory depression.]
THERAPEUTIC USES :-
* It is an analgesic in the opioid category.
* It is intended to treat mild pain and also has antitussive and local anaesthetic effects
REFERENCE:-Tripathi K.D;"Essentials of medical pharamacology,7th edition ,page no 476
No comments:
Post a Comment