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QuickView for Dexmedetomidine (compound)


PubChem
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]
DrugBank
Identification
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
Pharmacology
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...
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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
Interactions
Drug interaction:
TrimipramineTrimipramine may reduce the antihypertensive effect of the alpha2-agonist, Dexmedetomidine. Trimipramine may also increase the rebound hypertensive effect of Clonidine. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Clonidine if Trimipramine is initiated, discontinued or dose changed. Dexmedetomidine should be withdrawn very gradually to reduce the risk of hypertensive crisis.
TranylcypromineTranylcypromine, a strong CYP2A6 inhibitor, may decrease the metabolism and clearance of Dexmedetomidine.
TreprostinilAdditive hypotensive effect. Monitor antihypertensive therapy during concomitant use.

Targets