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Sugammadex
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Sulfentanil is a potent, short-acting synthetic opioid used in anesthesia and critical care. First synthesized by Janssen Pharmaceutica in 1974. It is the most potent opioid licensed for use in humans.
- OWC 1800
- pKa 8.0
- Potency 5-10x fentanyl, 500x morphine.
- Vd 3 L/kg
- Protein binding 93%
- Clearance 12 mL/kg/min
- tß½ 3 hours
- CSHT(8h) 30 min (alfentanil ~60 m)
- mu agonist, also stimulates serotonin release and at high dose has local anaeshetic effect.
- Structurally different from fentanyl, with a methoxymethyl group on the piperidine ring (increases potency and reduces duration of action) and thiophene instead of phenyl ring.
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A barbiturate derivative (Brevital™, Brietal™) intravenous anaesthetic agent, no longer available in Australia although still used in other parts of the world.
Preferred for use in electroconvulsive therapy for its pro-seizure effects and comparatively short duration.
Compared to thiopentone
- Oxybarbiturate
- Made up in 50 mL to 1% solution
- 3x more potent
- 3x clearance (12 mL/kg/min)
- tß½ 3 h (STP 8h)
- Greater ionised proportion
- Less protein binding (65%)
- More rapid recovery: 2-3 min (smaller fat compartment, no active metabolites, ⇡ clearance)
- Higher incidence of pain on injection
- Pro-convulsant/epileptiform EEG (excitatory in 30%)
- PONV (30%)
- Less dec MAP, more inc HR than STP
- More pronounced resp depression
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