Dexmedetomidine hydrochloride Series

Dexmedetomidine was launched in the US as an i.v. infusion for sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care unit, This imidazole derivative is the (S)-enantiomer of medetomidine that can be obtained via fractional crystallization of the tartrate salt of the racemic mixture. Dexmedetomidine is a full agonist of α2 adrenoceptors with 1300-fold selectivity versus α1 compared to the less selective partial α2 agonist clonidine, a veterinary hypnotic. Dexmedetomidine is unique compared with currently available sedatives in that it provides sedation, analgesia and anxiolysis with the ability of patients to be easily awakened. Besides, it causes minimal respiratory depression unlike other available drugs such as benzodiazepines or opioids. Pharmacological studies in transgenic mice showed that the sedative, anesthetic and analgesic effects of dexmedetomidine are specifically due to t...