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

Brands, Medical Use, Clinical Data

Drug Category

• Analgesics, Opioid
• Anesthetics, Intravenous
• Hypnotics and Sedatives

Dosage Forms

• Powder for solution

Brands / Synonyms

Remifentanyl; Ultiva; Ultiva

Indications

For use during the induction and maintenance of general anesthesia.

Pharmacology

Remifentanil is an opioid agonist with rapid onset and peak effect and ultra-short duration of action. The opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone. The analgesic effects of remifentanil are rapid in onset and offset. Its effects and side effects are dose dependent and similar to other opioids. Remifentanil in humans has a rapid blood-brain equilibration half-time of 1 ± 1 minutes (mean ± SD) and a rapid onset of action.

Mechanism of Action

Remifentanil is a µ-opioid agonist with rapid onset and peak effect, and short duration of action. The µ-opioid activity of remifentanil is antagonized by opioid antagonists such as naloxone.

Absorption

Not Available

Toxicity

Not Available

Biotrnasformation / Drug Metabolism

By hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases.

Contraindications

Due to the presence of glycine in the formulation, ULTIVA is contraindicated for epidural or intrathecal administration. ULTIVA is also contraindicated in patients with known hypersensitivity to fentanyl analogs.

Drug Interactions

In animals the duration of muscle paralysis from succinylcholine is not prolonged by remifentanil.

Remifentanil clearance is not altered by concomitant administration of thiopental, isoflurane, propofol, or temazepam during anesthesia. In vitro studies with atracurium, mivacurium, esmolol, echothiophate, neostigmine, physostigmine, and midazolam revealed no inhibition of remifentanil hydrolysis in whole human blood by these drugs.