Dexmedetomidine hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
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 the stimulation of the a
2A
subtype receptor. Like other α2 adrenoceptor agonists, dexmedetomidine can provoke
hypotension and bradycardia probably because of its non-selective action on peripheral
a
2B subtype receptors in vascular smooth muscle. Dexmedetomidine is extensively
metabolized into methyl and glucuronide conjugates which are mainly eliminated by renal
excretion. It was found to be a CYP2D6 inhibitor but less potent than the clinically relevant
standard quinidine.
Physikalische Eigenschaften
Dexmedetomidine hydrochloride is a white or almost white powder that is freely soluble in water and has a pKa of 7.1.
Verwenden
Dexmedetomidine hydrochloride has been used to study its effects on primary neonatal rat cardiomyocytes under hypoxic/reoxygenation conditions. It has also been used to study the effects of dexmedetomidine pretreatment on lipopolysaccharide-induced acute lung injury in mice.
benefits
The chemical name of dexmedetomidine hydrochloride is (S) -4- [1- (2,3- 3,5-dimethylphenyl) ethyl] -1H- imidazole hydrochlorides. Dexmedetomidine hydrochloride has an anti-sympathetic town. The effect of quiet and analgesic, compared with U.S. support pyrimidine, with higher selectivity and a short half-life, can be clinically used for Intensive Care Therapy. Start intubation and calmness using a lung ventilator patient during treatment. Meanwhile, the medicine can also reduce narcotic consumption, improve hand incidence of hemodynamic stability, and reduce myocardial ischaemia in art.
Biologische Aktivität
Active isomer of Medetomide (4-[1-(2,3-Dimethylphenyl)ethyl]-1H-imidazolehydrochloride ), a potent, highly selective α 2 -adrenoceptor agonist (K i values are 1.08 and 1750 nM for α 2 - and α 1 -adrenoceptors respectively). Displays greater selectivity over α 1 -adrenoceptors than clonidine and UK 14,304 (1620-, 220- and 300-fold respectively). Active in vivo ; displays hypotensive, bradycardic, sedative, anxiolytic, hypothermic and analgesic effects.
Dexmedetomidine hydrochloride Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
