Name: | Dexmedetomidine |
---|---|
PubChem Compound ID: | 123602 |
Description: | A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound. |
Molecular formula: | C13H17ClN2 |
Molecular weight: | 236.74 g/mol |
Synonyms: |
Precedex; 1H-Imidazole, 4-(1-(2,3-dimethylphenyl)ethyl)-, monohydrochloride, (S)-; Dexmedetomidine hydrochloride; 4-((S)-alpha,2,3-trimethylbenzyl)imidazole monohydrochloride; 145108-58-3; Dexmedetomidine hydrochloride [USAN]
|
Name: | Dexmedetomidine |
---|---|
Name (isomeric): | DB00633 |
Drug Type: | small molecule |
Description: | A imidazole derivative that is an agonist of ADRENERGIC ALPHA-2 RECEPTORS. It is closely-related to MEDETOMIDINE, which is the racemic form of this compound. |
Synonyms: |
Medetomidine; Medetomidina [Spanish]; Medetomidinum [Latin]
|
Brand: | PRECEDEX |
Category: | Adrenergic alpha-Agonists, Analgesics, Non-Narcotic, Hypnotics and Sedatives, Analgesics |
CAS number: | 113775-47-6 |
Indication: | For sedation of initially intubated and mechanically ventilated patients during treatment in an intensive care setting, also used in pain relief; anxiety reduction and analgesia |
---|---|
Pharmacology: | Dexmedetomidine activates 2-adrenoceptors, and causes the decrease of sympathetic tone, with attenuation of the neuroendocrine and hemodynamic responses to anesthesia and surgery; it reduces anesthetic and opioid requirements; and causes sedation and analgesia. |
Mechanism of Action: |
Dexmedetomidine 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...
show more » |
Protein binding: | 94% |
Biotransformation: | Hepatic |
Route of elimination: | A mass balance study demonstrated that after nine days an average of 95% of the radioactivity, following intravenous administration of radiolabeled dexmedetomidine, was recovered in the urine and 4% in the feces. Fractionation of the radioactivity excreted in urine demonstrated that products of N-glucuronidation accounted for approximately 34% of the cumulative urinary excretion. The majority of metabolites are excreted in the urine. |
Half Life: | 2 hours |
Clearance: | 39 L/h [Healthy volunteers receiving IV infusion (0.2-0.7 mcg/kg/hr)] |
Affected organisms: | Humans and other mammals |
Drug interaction: |
|
---|