Remifentanil

Remifentanil

Mechanism of action

  • Opioid analgesic (ultra-short duration of action)
  • Analgesic properties are based mostly on its selective agonism to the μ-opioid receptor (MOR) which is crucial for transmission of information about pain throughout the central nervous system. These receptors are located mostly in brainstem and thalamus.

Indications and dose

Pharmacokinetics

Onset of action: rapid (about 1 minute)

Duration of action: 3–10 minutes after discontinuation 

Half-life of elimination: 1–20 minutes

Metabolism: Nonspecific blood and tissue esterases

Elimination: Kidneys

Medicinal forms

Powder for Solution for Injection/Infusion – 1 mg, 2 mg, 5 mg

e.g. 2 mg ad 50 ml F1/1

Side-effects

Respiratory depression

Muscle rigidity

CNS depression

Cardiovascular depression (hypotension, bradycardia)

Serotonin syndrome

Nausea, vomiting

Seizures

Reversal

Rapid reversal may be achieved with Naloxone.

See more about it in Naloxone list.

References

  1. Remifentanil: Uses, Interactions, Mechanism of Action | DrugBank Online
  2. Remifentanil 5 mg powder for concentrate for solution for injection/infusion - Summary of Product Characteristics (SmPC) - (emc) (medicines.org.uk)
  3. Remifentanil | SpringerLink
  4. Remifentanil Uses, Side Effects & Warnings - Drugs.com