BLACK BOX WARNING
- respiratory depression and death (requires monitoring and resuscitation equipment)
remifentanil
Brand: Ultiva
⚠ BBW ISMP High Alert Prototype: morphine
Drug Class: opioid analgesic
Drug Family: opioid
Subclass: ultra-short-acting mu-opioid agonist
Organ Systems: cns
Mechanism of Action
Potent, selective mu-opioid agonist with a unique ester linkage in its structure that is hydrolyzed by nonspecific blood and tissue esterases, producing an ultra-short duration of action independent of hepatic or renal function — context-sensitive half-time remains constant regardless of infusion duration.
mu-opioid receptor (MOR)
Indications
- induction and maintenance of general anesthesia
- analgesia in mechanically ventilated ICU patients (short-term)
- procedural sedation/analgesia
Contraindications
- epidural or intrathecal administration (formulation contains glycine, a neurotoxin)
- use as sole anesthetic (without consciousness-ablating agent)
Adverse Effects
Common
- apnea
- respiratory depression
- hypotension
- bradycardia
- muscle rigidity (chest wall rigidity at high doses)
Serious
- respiratory arrest without mechanical ventilation support
- opioid-induced hyperalgesia (with prolonged use)
- acute opioid tolerance
Pharmacokinetics (ADME)
| Absorption | IV only; no oral formulation |
| Distribution | protein binding ~70%; Vd ~0.35 L/kg |
| Metabolism | ester hydrolysis by nonspecific blood and tissue esterases; independent of liver and kidney function |
| Excretion | primarily renal (as inactive metabolites) |
| Half-life | 3-10 minutes (context-sensitive half-time constant at 3-4 minutes regardless of infusion duration) |
| Onset | 30-60 seconds IV |
| Peak | 1-3 minutes |
| Duration | 5-10 minutes (offset driven by metabolism, not distribution) |
| Protein Binding | 70% |
| Vd | 0.35 L/kg |
Drug Interactions
| Drug / Agent | Mechanism | Severity |
|---|---|---|
| CNS depressants (propofol, benzodiazepines) | synergistic respiratory depression; dose reduction of both required | major |
| volatile anesthetics | synergistic anesthetic and respiratory depression | major |
Nursing Considerations
- Remifentanil must only be administered in settings with full resuscitation capabilities (mechanical ventilation, naloxone, crash cart); never administer without these resources immediately available.
- The ultra-short duration means analgesia terminates abruptly within 5-10 minutes of stopping the infusion; transition to alternative analgesia before discontinuation to avoid uncontrolled pain.
- Chest wall rigidity ('wooden chest') at high infusion rates can impede ventilation and must be managed with succinylcholine or rocuronium.
- Do not dilute in or administer with lactated Ringer's solution — incompatible; use normal saline or D5W for dilution.
Clinical Pearls
- Remifentanil is the only opioid whose pharmacokinetics are independent of organ function; because plasma esterases metabolize it, its elimination is unaffected by hepatic or renal failure.
- The clinical consequence of remifentanil's ultra-short action is that analgesia ends abruptly upon discontinuation — failure to pre-emptively establish alternative analgesia (multimodal or longer-acting opioid) results in severe acute pain.
Safety Profile
Pregnancy use-with-caution
Lactation use-with-caution
Renal Adjustment Not required
Hepatic Adjustment Not required
TDM Not required
Concordance Terms
Cross-referenced clinical concepts — click any term to see all content where it appears.