SUGAMMADEX
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SUGAMMADEX (SUGAMMADEX).
Selective relaxant binding agent that forms a complex with neuromuscular blocking agents (rocuronium, vecuronium) in plasma, reducing their concentration at the nicotinic receptor.
| Metabolism | Not metabolized; primarily eliminated unchanged in urine via glomerular filtration. |
| Excretion | Primarily renal excretion of unchanged drug; approximately 70% of the dose recovered in urine over 24 hours, with minimal biliary/fecal elimination (<5%) |
| Half-life | Terminal elimination half-life approximately 2 hours (range 1.5-2.5 hours); clinically, recovery from neuromuscular blockade occurs within minutes after administration due to rapid redistribution and encapsulation of rocuronium/vecuronium |
| Protein binding | Primarily bound to gamma-cyclodextrin; negligible binding to plasma proteins (<1%) |
| Volume of Distribution | Approximately 0.2-0.3 L/kg, indicating mainly intravascular distribution with limited extravascular distribution |
| Bioavailability | Not applicable; only intravenous administration is used; oral bioavailability is negligible due to high polarity and degradation in GI tract |
| Onset of Action | Intravenous: reversal of moderate neuromuscular blockade (TOF count 2) occurs within 2-3 minutes; reversal of deep blockade (PTC 1-2) within 5 minutes |
| Duration of Action | Duration of reversal effect is dose-dependent; typically provides sustained reversal without recurrence of blockade for at least 60 minutes; in some cases, re-curarization may occur if inadequate dose given for depth of block |
4 mg/kg IV as a single bolus for routine reversal of moderate neuromuscular blockade (train-of-four [TOF] count of 2); 2 mg/kg IV as a single bolus for deep blockade (post-tetanic count [PTC] of 1-2); 16 mg/kg IV as a single bolus for immediate reversal of rocuronium-induced blockade (1.2 mg/kg rocuronium) given 3 minutes after administration.
| Dosage form | INJECTION |
| Renal impairment | For severe renal impairment (CrCl <30 mL/min): No dose adjustment required for 2 mg/kg or 4 mg/kg. For 16 mg/kg, use with caution; data insufficient. No data for end-stage renal disease. |
| Liver impairment | No dose adjustment required for mild to moderate hepatic impairment (Child-Pugh A or B). For severe hepatic impairment (Child-Pugh C): use with caution; limited data. |
| Pediatric use | Children (2-17 years): 4 mg/kg IV for moderate blockade (TOF count of 2); 2 mg/kg for deep blockade (PTC of 1-2). Safety and efficacy not established for infants <2 years. |
| Geriatric use | No specific dose adjustment required; however, consider increased sensitivity to neuromuscular blocking agents and potential for slower recovery. Monitor TOF ratio closely. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SUGAMMADEX (SUGAMMADEX).
| Breastfeeding | No human data on excretion in breast milk. M/P ratio unknown. Sugammadex has low oral bioavailability; unlikely to cause effects in nursing infant. Use with caution. |
| Teratogenic Risk | Insufficient human data; animal studies (rat, rabbit) show no teratogenicity at up to 40 mg/kg/day (AUC 11-18 times human exposure). No fetal adverse effects reported. Risk cannot be excluded; use only if clearly needed. |
| Fetal Monitoring |
■ FDA Black Box Warning
None
| Serious Effects |
["Known hypersensitivity to sugammadex or any of its components."]
| Precautions | ["Risk of bradycardia, cardiac arrest, and hypersensitivity reactions.","Monitor for recurrence of neuromuscular blockade.","Use with caution in severe renal impairment."] |
Loading safety data…
| Monitor for recurrence of neuromuscular blockade; standard anesthesia monitoring including heart rate, blood pressure, oxygen saturation, and neuromuscular transmission (train-of-four). |
| Fertility Effects | No human data on fertility. Animal studies (rat) showed no impairment of fertility or reproductive performance at doses up to 40 mg/kg/day. |