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Active ingredient: Dexmedetomidine - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Adrenergic alpha-Agonists
  • Analgesics
  • Hypnotics and Sedatives

Dosage Forms

  • Not Available

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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