Chemical: Drug

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2D structure from PubChem
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Generic Names
  • Remifentanyl
Trade Names
  • Ultiva
Brand Mixture Names

PharmGKB Accession Id





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.

Source: Drug Bank


For use during the induction and maintenance of general anesthesia.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

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

Source: Drug Bank


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.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity


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

Source: Drug Bank

Protein Binding

70% (bound to plasma proteins)

Source: Drug Bank


1-20 minutes

Source: Drug Bank


Source: Drug Bank

Route of 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.

Source: Drug Bank

Volume of Distribution

Source: Drug Bank

Chemical Properties

Chemical Formula


Source: Drug Bank

Isomeric SMILES


Source: OpenEye

Canonical SMILES


Source: Drug Bank

Average Molecular Weight


Source: Drug Bank

Monoisotopic Molecular Weight


Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
OPRD1 (source: Drug Bank)
OPRK1 (source: Drug Bank)
OPRM1 (source: Drug Bank)

Drug Interactions

Drug Description
remifentanil Possible increased risk of serotonin syndrome. (source: Drug Bank)
remifentanil The CNS depressants, Triprolidine and Remifentanil, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)
remifentanil The CNS depressants, Triprolidine and Remifentanil, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. (source: Drug Bank)

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to remifentanil: 1

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Reversal of opioid-induced bladder dysfunction by intravenous naloxone and methylnaltrexone. Clinical pharmacology and therapeutics. 2007. Rosow C E, et al. PubMed


Web Resource:
National Drug Code Directory:
KEGG Compound:
PubChem Compound:
PubChem Substance:
Drugs Product Database (DPD):
Therapeutic Targets Database:
FDA Drug Label at DailyMed:

Clinical Trials

These are trials that mention remifentanil and are related to either pharmacogenetics or pharmacogenomics.

No trials found.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.