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. Avtivation of the postsynaptic alpha-2 adrenoceptors inhibits the sympathetic activity decreases blood pressure and heart rate.
Drug Category: Adrenergic alpha-Agonists; Analgesics; Hypnotics and Sedatives; ATC:C02A
Brand Names/Synonyms: Dexmedetomidine; Medetomidina [Spanish]; Medetomidine; Medetomidinum [Latin]; PRECEDEX; Precedex
Dosage Forms: Not Available
Absorption: Not Available
Interactions:
DrugBank: Interactions for Dexmedetomidine
Interactions for Dexmedetomidine:
General
In vitro studies in human liver microsomes demonstrated no evidence of cytochrome P450-mediated drug interactions
that are likely to be of clinical relevance.
Anesthetics/Sedatives/Hypnotics/Opioids
Co-administration of PRECEDEX with anesthetics, sedatives, hypnotics, and opioids is likely to lead to an
enhancement of effects. Specific studies have confirmed these effects with sevoflurane, isoflurane, propofol,
alfentanil, and midazolam. No pharmacokinetic interactions between dexmedetomidine and isoflurane, propofol,
alfentanil, and midazolam have been demonstrated. However, due to possible pharmacodynamic interactions, when
co-administered with PRECEDEX, a reduction in dosage of PRECEDEX on the concomitant anesthetic, sedative, hypnotic or
opioid may be required.
Neuromuscular Blockers
In one study of 10 healthy volunteers, administration of PRECEDEX for 45 minutes at a plasma concentration of 1
(one) ng/mL resulted in no clinically meaningful increases in the magnitude or neuromuscular blockade associated with
rocuronium administration.
Chemical IUPAC Name: 4-[1-(2,3-dimethylphenyl)ethyl]-3H-imidazole
Chemical Formula: C13H16N2
Half Life: 2 hours
Drug Type: Approved Drug
# Accession No: APRD00578
CAS Registry Number: 113775-47-6
