Remifentanil

What is Remifentanil? 1

  • Ultra-short-acting synthetic opioid analgesic.
  • Used for pain management and as an adjunct to anesthesia.
  • Rapid onset and short duration of action.

Mechanism of Action & Pharmacokinetics 12

  • Acts primarily on mu-opioid receptors in the brain and spinal cord with minimal or no activity on delta and kappa opioid receptors.
    • The mu receptor is predominantly responsible for analgesia, hypoventilation, and euphoria
  • Rapidly metabolized by nonspecific esterases in blood and tissues, leading to quick clearance without redistribution.

Pharmacodynamics 12

Cardiovascular

  • May decrease heart rate and blood pressure
  • The degree of hypotension and bradycardia is dose-dependent, predictable, and quickly reversible due to rapid metabolism.

Respiratory

  • Can cause skeletal muscle and chest wall rigidity, particularly with continuous infusion, leading to decreased minute ventilation, respiratory depression, and apneas.

Indications 1

  • Induction and maintenance of general anesthesia.
  • Analgesia during short/intense surgical procedures.
  • MAC sparing agent, reducing the MAC of inhalation anesthetics.

Dosage 2

  • Bolus:
    • 1-2 µg/kg IV bolus for sympathectomy during laryngoscopy and as a co-induciton agent.
  • Analgesia during surgery:
    • 0.5 to 1 µg/kg IV bolus.
    • Followed by an infusion of 0.05 to 0.2 µg/kg/min.

Complications 123

  • Rapid onset and high potency can lead to pronounced hypotension, bradycardia, muscle rigidity, and respiratory depression or arrest.
  • Common opioid-related side effects include nausea, vomiting, pruritus, and postoperative shivering.
  • Due to its rapid offset, there is a risk of postoperative hyperalgesia if not bridged with longer-acting analgesics upon discontinuation.

References

  1. Birdi T, Sullivan P. Ottawa Anesthesia Primer. Toronto, Ontario: Echo Book Publishing; 2012.  2 3 4 5

  2. Remifentanil: Drug Information. UpToDate.  2 3 4

  3. Rosow, Carl E. (1999). An overview of remifentanil. Anesthesia & Analgesia, 89(4S): 1. DOI: 10.1097/00000539-199910001-00001.