Remifentanil Stats & Data
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DrugBankDescription
Remifentanil (marketed by Abbott as Ultiva) is a potent ultra short-acting synthetic opioid given to patients during surgery for pain relief and adjunctive to an anaesthetic. Remifentanil is a specific mu-type-opioid receptor agonist which means it reduces sympathetic nervous system tone, and causes respiratory depression and analgesia.
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.
Pharmacodynamics
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.
Metabolism
By hydrolysis of the propanoic acid-methyl ester linkage by nonspecific blood and tissue esterases.
Indication
For use during the induction and maintenance of general anesthesia.
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.
Volume of Distribution
* 350 mL/kg * 452 ± 144 mL/kg neonates * 223 ± 30.6 mL/kg adolescents
Effect Profile
CuratedStrong euphoria and pain relief with moderate itching/nausea, low sedation
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Clinically, meaningful tolerance to remifentanil’s analgesia can develop within hours of infusion; tolerance decays over days to weeks after cessation. Values are approximate and based on clinical observations of acute tolerance rather than long-term dependence.
Cross-Tolerances
Harm Reduction
drugs.wikiStandard anaesthetic practice uses continuous infusions of 0.05–0.25 µg kg⁻¹ min⁻¹; analgesia ceases within ~5 min of pump stoppage due to ester hydrolysis. Context-sensitive half-life is ~3–4 min regardless of infusion length. Bolus dosing outside monitored settings is strongly discouraged because apnoea or chest wall rigidity can occur before the syringe is empty. Chest/truncal rigidity with potent opioids is more likely with rapid IV pushes; slow administration and airway support are essential in clinical settings. Metabolism is by nonspecific blood/tissue esterases to an inactive acid; CYP inhibitors are not expected to prolong effect. Remifentanil can produce acute tolerance and opioid-induced hyperalgesia, especially after higher doses or abrupt cessation of infusions; expect rebound pain/craving within minutes once stopped. In overdose, prioritize airway/ventilation; give naloxone in small, titrated IV boluses (e.g., 0.04 mg) to restore breathing while minimizing severe withdrawal, and be prepared for re-sedation if longer-acting opioids or other depressants are present. Non-medical IV use carries high risks of hypoxia, infection, and BBVs; if people use regardless, sterile technique, low-dead-space syringes, never using alone, and access to naloxone/overdose response training reduce but do not eliminate risk.
References
Drugs.wiki References
- DrugBank – Remifentanil monograph
- PubChem – Remifentanil compound page
- StatPearls – General Anesthesia for Surgeons (opioids can cause chest wall rigidity)
- NCBI Bookshelf – Community Management of Opioid Overdose (naloxone dosing/titration, airway first)
- MedGen – Hyperalgesia (Remifentanil-induced hyperalgesia, 2024 systematic review)
- TripSit Wiki – Drug combinations (benzos + opioids marked dangerous)
- EUDA (EMCDDA) – Non-medical benzodiazepine use and co-use with opioids increases overdose risk
- EUDA European Drug Report 2024/2025 – Overdose patterns, polydrug risks (benzos, xylazine with opioids)
- DrugWise – Harm reduction for drug users (never use alone, naloxone, sterile injecting)
- DrugWise – Drug consumption rooms (benefits of supervised consumption)