Molecule

Drug Groups

approved

Description

Remifentanil (marketed by Abbott as Ultiva) is a potent ultra short-acting synthetic opioid analgesic drug. It is given to patients during surgery to relieve pain and as an adjunct to an anaesthetic. Remifentanil is a specific mu-type-opioid receptor agonist. Hence, it causes a reduction in sympathetic nervous system tone, respiratory depression and analgesia.

Indication

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.

Affected Organisms

Biotransformation

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

Half Life

1-20 minutes

Protein Binding

70% (bound to plasma proteins)

Elimination

Remifentanil is an esterase-metabolized opioid. The carboxylic acid metabolite is essentially inactive (1/4600 as potent as remifentanil in dogs) and is excreted by the kidneys with an elimination half-life of approximately 90 minutes.

Distribution

* 350 mL/kg
* 452 ± 144 mL/kg [neonates]
* 223 ± 30.6 mL/kg [adolescents]

Clearance

* 40 mL/min/kg [young, healthy adults]

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