Remifentanil

Products

Remifentanil is commercially available as a powder for the preparation of a concentrate for solution for injection or infusion (Ultiva, generic). It has been approved in many countries since 1996.

Structure and properties

Remifentanil (C20H28N2O5, Mr = 376.4 g/mol) is present in drugs as remifentanil hydrochloride, a white powder. The drug is rapidly hydrolyzed in vivo by nonspecific esterases to the relatively inactive remifentanilic acid and is therefore useful in organ failure. Remifentanil is structurally related to fentanyl and is a 4-anilidopiperidine like alfentanil and sufentanil.

Effects

Remifentanil (ATC N01AH06) has analgesic and sedative properties. It is a selective µ-opioid agonist with rapid and predictable onset of action (approximately 1 minute) and very short duration of action. The half-life is only 3-10 minutes. The effects can be reversed with opioid antagonists such as naloxone. Because of its pharmacokinetic properties, remifentanil can be considered a soft drug.

Indications

  • Anesthesia during surgical procedures.
  • Continuation of analgesia in the immediate postoperative period.
  • Analgesia and sedation in intensive care.

Dosage

According to the SmPC. Remifentanil is administered intravenously.

Contraindications

  • Hypersensitivity

For complete precautions, see the drug label.

Interactions

Drug-drug interactions have been described with anesthetics, benzodiazepines, central depressant agents, and cardiodepressant agents (beta blockers, calcium channel blockers).

Adverse effects

The most common potential adverse effects include skeletal muscle rigidity, cardiodepression (low blood pressure, slow pulse), nausea, vomiting, acute respiratory depression, apnea, pruritus, postoperative tremor, and constipation.