Wednesday, February 14, 2018

Dexmedetomidine analgesic sedation action

INTRODUCTION :- This compound belongs to the class of organic compounds known as benzene and substituted derivatives. These are aromatic compounds containing one monocyclic ring system consisting of benzene.

MECHANISM OF ACTION :-
* It is a specific and selective alpha-2 adrenoceptor agonist. 
* By binding to the presynaptic alpha-2 adrenoceptors, it inhibits the release if norepinephrine, therefore, terminate the propagation of pain signals. 
* Activation of the postsynaptic alpha-2 adrenoceptors inhibits the sympathetic activity decreases blood pressure and heart rate.

PHARMACOKINETICS :-
* Protein binding :- 94%
* Volume of distribution :- 118 L
* Half life :- 2 hrs
* Route of administration :-:- Urine and 4% in feces.

SIDE EFFECTS :- 
* Decreased blood pressure observed at lower concentrations 
* Elevated blood pressure at higher concentrations.
* Rapid IV administration or bolus has been associated with slow heart rate (bradycardia)
* Low blood pressure (hypotension) due to peripheral α2-receptor stimulation.

 DRUG-DRUG INTERACTIONS :-
* CERITINIB+ DEXMEDETOMIDINE=   It may increase the bradycardic activities of Ceritinib.
* DULOXETINE+ DEXMEDETOMIDINE=  It may increase the orthostatic hypotensive activities of Duloxetine.
* HEPTABARBITAL + DEXMEDETOMIDINE= It  may increase the hypotensive activities of Dexmedetomidine.

THERAPEUTIC USES :- 
* It is most often used in the intensive care setting for light to moderate sedation. 
* It is used in veterinary medicine for its analgesic and sedative properties.

REFERENCE: Tripathi K.D, "Essentials of medical pharmacology" Edition- 7th, page no.-384

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