Drug reference

Remifentanil

Opioid Analgesic · Analgesic

Opioid AnalgesicAnalgesic

CDSCO approvedSchedule H

EXCRETION

—

not curated

INTERACTIONS

12 major

SEVERE in our sources

PREGNANCY

[MHRA/CHM advice]. . Opioids: reminder of risk of potentially fatal respiratory

FDA category + note

Top interactionssee all 12 →

AcetaminophenSevereTextbookHarrison 22e · p98-99
BarbituratesSevereTextbookKDT 7e · p401
BenzodiazepinesSevereTextbookKDT 7e · p383
Chlordiazepoxide HydrochlorideSevereTextbookG&G 14e

Mechanism

Remifentanil is an ultra-short-acting synthetic mu-opioid receptor agonist of the phenylpiperidine class that is unique in containing an ester linkage that is rapidly hydrolyzed by non-specific tissue and plasma esterases — not hepatic metabolism. This gives it a context-sensitive half-time of approximately 3-4 minutes regardless of infusion duration, enabling minute-to-minute titration of analgesic depth during surgery. Recovery from its effects occurs within 5-10 minutes of stopping infusion, even after prolonged administration.

Indications

Intra-operative analgesiaintense analgesia for short, painful proceduresblunting of stress responsesanalgesia during perioperative period (particularly for procedures that are briefly painful)

Dosing

Adult: Induction bolus: 0.25-1 mcg/kg over ≥30 seconds. Induction infusion: 30-60 mcg/kg/h. Maintenance (ventilated): 3-120 mcg/kg/h. ICU sedation: initially 6-9 mcg/kg/h, adjust by 1.5 mcg/kg/h.

Pharmacokinetics

Onset

1–1.5 min following intravenous administration

Duration

Analgesic effects: 1-1.5 min; Recovery of respiratory function: 3-5 min after 3-5 h infusions; Full recovery from all effects: 15 min

Half-life

8–20 min (elimination); 5 min (peak respiratory depression after bolus)

Bioavailability

—

Protein binding

92%

Metabolism

Very rapidly metabolized by esterases in plasma

Excretion

Renal excretion (primary metabolite)

Contraindications

intraspinal administration (due to glycine formulation)

Side effects

Common

nauseavomitingpruritus

Serious

Potentially fatal respiratory depression
respiratory depression

Pregnancy & lactation

Pregnancy

[MHRA/CHM advice]. . Opioids: reminder of risk of potentially fatal respiratory

Drug interactions

Acetaminophen

Severe

Textbook

Acetaminophen-related hepatotoxicity, a significant cause for liver failure.

Many practitioners have moved away from opioid-acetaminophen combination analgesics to avoid the risk of excessive acetaminophen exposure.

Source: Harrison 22e · p98-99

Barbiturates

Severe

Textbook

Exaggerated CNS depression.

Source: KDT 7e · p401

Benzodiazepines

Severe

Textbook

Marked depression of respiration, cardiac contractility, and blood pressure.

Carefully monitor respiratory and cardiovascular functions when co-administering benzodiazepines with opioids due to increased risk of severe depression of vital signs.

Source: KDT 7e · p383

Chlordiazepoxide Hydrochloride

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.

Source: G&G 14e

Clomethiazole

Severe

Textbook

Increased rates of accidental overdose and death.

Caution is advised, especially for patients with a history of drug abuse.