WARNINGDANGER OF DEATH
High doses alone or ordinary doses in combination with other depressants can fatally stop breathing.
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Sufentanil
Sufentanil is a potent synthetic anilidopiperidine analgesic1 that produces pain relief and depressant effects.2 It was first synthesized at Janssen Pharmaceutica in 1974. It is used medically in anesthesia3 and for severe acute pain.2 Compared with heroin, users report less euphoria but stronger sedation and respiratory depression. It is also habit-forming.4
Dosage & Duration
Dosage
Doses are population estimates that vary widely between individuals.
Duration
Subjective Effects
Pharmacology
Pharmacodynamics
Sufentanil acts primarily as an agonist at μ-opioid receptors, to which it binds highly selectively.5 Its opioid action reduces intracellular cAMP and neurotransmitter release, contributing to analgesia.6 It also opens calcium-dependent inwardly rectifying potassium channels, reducing neuronal excitability.6 Additional interactions include agonism at δ-opioid receptors and binding to κ-opioid receptors.
Pharmacokinetics
Sufentanil is rapidly metabolized in the liver and small intestine, mainly through oxidative N- and O-dealkylation, producing inactive metabolites.5 It is a CYP3A4 substrate.5 Sublingual bioavailability is 52% after a single tablet and falls to 35% with repeated dosing.7 Following intravenous administration, distribution and redistribution times are 1.4 and 17.1 minutes, respectively,3 with a central distribution volume of approximately 14 L and a steady-state distribution volume of approximately 350 L.5 Plasma protein binding depends on alpha acid glycoprotein concentrations and is approximately 93% in healthy males, 91% in mothers, and 79% in neonates.3 Adult intravenous elimination half-life is 164 minutes; elimination is faster in infants and children and slower in neonates.4 After a single 15-microgram sufentanil sublingual tablet, observed mean terminal half-lives ranged from 6 to 10 hours; after multiple administrations, a longer mean terminal half-life of up to 18 hours was determined.8 Approximately 80% of the administered dose is excreted within 24 hours, with only 2% eliminated unchanged.3 Total plasma clearance after a single intravenous administration is reported as about 917 L/min. Sufentanil clearance in healthy neonates is approximately half that in adults and children and can be further reduced by up to a third in neonates with cardiovascular disease.4 After incremental epidural doses totaling 5-40 micrograms during labor and delivery, maternal and neonatal sufentanil plasma concentrations were at or near the detection limit of 0.05-0.1 ng/mL and were slightly higher in mothers than in their infants.4 In cats, sufentanil has a longer half-life than fentanyl and alfentanil.
Caution
Use cautionThese combinations are not usually physically harmful, but may produce undesirable effects, such as physical discomfort or overstimulation. Extreme use may cause physical health issues. Synergistic effects may be unpredictable. Care should be taken when choosing to use this combination.
Tolerance
Tolerance timelines are rules of thumb, not exact schedules, and vary widely between individuals and use patterns.
Harm Potential
Addiction & Dependence
Psychological
Sufentanil has habit-forming potential.9
Toxicity
| Species | Route | Value |
|---|---|---|
| Mouse | Intravenous | 18.7 mg/kg |
Sufentanil can cause respiratory depression,10 and overdose can produce respiratory arrest.
Sufentanil can cause orthostatic hypotension, syncope, and bradycardia.9
Sufentanil reduces gastrointestinal motility and increases smooth muscle tone, delaying intestinal transit and causing constipation.9
High intravenous doses of sufentanil can cause muscle rigidity.10
Intravenous sufentanil at 2.5 times the maximum human dose caused embryonic death in rats and rabbits treated for 10–30 days during pregnancy; this effect was thought to result from maternal toxicity.
History & Culture
Sufentanil was first synthesized at Janssen Pharmaceutica in 1974. AcelRx Pharmaceuticals and the United States Department of Defense collaborated to develop…
Legality
By Country
SwitzerlandIllegalReferences
Source Pages
Citations
Further Reading
Article Status
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