Pharmacology of Sedative-Analgesic Agents: Dexmedetomidine, Remifentanil, Ketamine, Volatile Anesthetics, and the Role of Peripheral Mu Antagonists
Section snippets
Remifentanil
Remifentanil is an ultra–short-acting opioid that acts as a mu-receptor agonist; it is 250 times more potent than morphine. In 1996, the FDA approved remifentanil as an analgesic agent for the induction and maintenance of anesthesia. In 2002, the European Medicines Agency approved its use for analgesia in mechanically ventilated adult patients in intensive care for up to 3 days.76 Although remifentanil is used and studied extensively in the operating room, its popularity in the critical care
Ketamine
Clinical reports of the use of ketamine, a nonbarbiturate phencyclidine derivative, first appeared more than four decades ago.96 Because it provides analgesia and apparent anesthesia with relative hemodynamic stability, ketamine was considered an ideal “battlefield anesthetic” and was popularized during the Vietnam war.97
Ketamine binds with N-methyl-d-aspartate (NMDA) and sigma opioid receptors to produce intense analgesia and a state termed dissociative anesthesia; patients become unresponsive
Volatile anesthetic agents
Volatile anesthetics such as isoflurane, sevoflurane, and desflurane are in daily use in the operating room in the delivery of general anesthesia. A major advantage of these halogenated ethers is their quick onset, quick offset, and ease of titration in rendering the patient unconscious, immobile, and amnestic. Although volatile anesthetics are generally associated with stable hemodynamics with little variation, dose-dependent vasodilatation, cardiac depression, and arrhythmias can occur.137,
Peripheral opioid receptor antagonists
Opioids remain the primary class of analgesic drugs in the ICU and may be infused for many days in critically ill patients. Undesired side effects are legion, and in addition to nausea, vomiting, pruritus, and urinary retention, they include delayed gastric emptying, suppression of bowel motility, constipation, and ileus. Methylnaltrexone and alvimopan are members of a new class of drugs—peripherally acting mu opioid receptor antagonists (PAMORAs). In contrast to naloxone, these medications do
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Ketamine is not associated with more post-intubation hypotension than etomidate in patients undergoing endotracheal intubation
2022, American Journal of Emergency MedicineCitation Excerpt :Etomidate is a reversible inhibitor of 11-beta-hydroxylase and has been found to cause transient adrenocortical suppression [42,43]. Ketamine has sympathomimetic properties secondary to the indirect release of catecholamines that may increase blood pressure [17]. Particularly in hypotensive patients, ketamine may offer added hemodynamic support and thus has seen an increase in utilization for RSI induction [1,4,18–24,47].
Influence of perioperative dexmedetomidine on the incidence of postoperative delirium in adult patients undergoing cardiac surgery
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2022, Revue NeurologiqueCitation Excerpt :In the general ICU population, the only evidenced benefit of dexmedetomidine is an increase in the number of days without delirium or coma [58]. Dexmedetomidine may have attractive features for patients with acute brain injury, such as the lack of respiratory depression, an ease of sensorium and neurological assessment with ongoing infusion and sympatholysis [59]. However, dexmedetomidine is in the early stages of evaluation in brain injury patients and there is little evidence in the literature.
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