Brands, Medical Use, Clinical Data
Drug Category
- Adrenergic alpha-Agonists
- Analgesics
- Hypnotics and Sedatives
Dosage Forms
Brands / Synonyms
Medetomidina [Spanish]; Medetomidine; Medetomidinum [Latin]; Precedex; PRECEDEX
Indications
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.
Absorption
Not Available
Toxicity
Not Available
Biotrnasformation / Drug Metabolism
Hepatic
Contraindications
No specific information available.
Drug Interactions
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.
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