SUGAMMADEX SODIUM
Clinical safety rating: caution
Comprehensive clinical and safety monograph for SUGAMMADEX SODIUM (SUGAMMADEX SODIUM).
Selective binding to aminosteroidal neuromuscular blocking agents (e.g., rocuronium, vecuronium), encapsulating them and reducing their concentration at the nicotinic acetylcholine receptor, thereby reversing neuromuscular blockade.
| Metabolism | Not metabolized; eliminated unchanged in urine via glomerular filtration. |
| Excretion | Primarily renal excretion (approximately 95% of dose excreted unchanged in urine over 24 hours); minimal biliary/fecal elimination (<5%). |
| Half-life | Terminal elimination half-life is approximately 2 hours (range 1.5–3 hours); clinically, this supports rapid recovery from neuromuscular blockade. |
| Protein binding | Minimal protein binding; approximately <10% bound to plasma proteins (mainly albumin). |
| Volume of Distribution | Steady-state volume of distribution (Vdss) approximately 0.21–0.25 L/kg (mean ~0.23 L/kg); this small Vd indicates limited extravascular distribution, consistent with a hydrophilic cyclodextrin that remains largely in the central compartment. |
| Bioavailability | Not applicable orally; available only as intravenous injection (100% bioavailability). |
| Onset of Action | Intravenous administration: recovery of T4/T1 ratio to 0.9 occurs in approximately 2 minutes following 4 mg/kg dose for moderate blockade; dose-dependent (4 mg/kg: median 2 min; 2 mg/kg: median 3 min; 16 mg/kg: median 1.5 min). |
| Duration of Action | Duration of effect is dose-dependent and correlates with elimination half-life. Clinical recovery (T4/T1 ≥0.9) is typically achieved within 5–10 minutes after sugammadex administration, with no clinically relevant recurarization observed. |
4 mg/kg IV as a single bolus for routine reversal of moderate neuromuscular blockade (train-of-four count 2); 2 mg/kg IV for deep blockade (train-of-four count 0-1); 16 mg/kg IV for immediate reversal after a single dose of rocuronium 1.2 mg/kg.
| Dosage form | INJECTABLE |
| Renal impairment | No dose adjustment required for mild to moderate renal impairment (CrCl ≥30 mL/min). For severe renal impairment (CrCl <30 mL/min), dose adjustment not established; use with caution due to prolonged exposure and limited data. |
| 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; no specific dosing recommendations available. |
| Pediatric use | Children (2-17 years): 4 mg/kg IV for routine reversal (train-of-four count 2); 2 mg/kg for deep blockade. Infants and toddlers (1 month to <2 years): 4 mg/kg IV; limited data for deep blockade. Neonates (full-term <1 month): 4 mg/kg IV; no data for deep blockade. |
| Geriatric use | No specific dose adjustment required; however, consider age-related decline in renal function. Monitor for prolonged recovery due to potentially reduced clearance in elderly patients. |
| 1st trimester | Consult provider |
| 2nd trimester | Consult provider |
| 3rd trimester | Consult provider |
Clinical note
Comprehensive clinical and safety monograph for SUGAMMADEX SODIUM (SUGAMMADEX SODIUM).
| Breastfeeding | Not known if excreted in human milk. M/P ratio not reported. Caution advised, consider risk-benefit. |
| Teratogenic Risk | No evidence of teratogenicity in animal studies. Limited human data; risk cannot be excluded. Use only if clearly needed. |
| Fetal Monitoring | Monitor for signs of neuromuscular blockade reversal (adequate muscle strength). In pregnant patients, monitor fetal heart rate if appropriate. |
■ FDA Black Box Warning
No black box warning issued by FDA.
| Serious Effects |
["Known hypersensitivity to sugammadex or any of its excipients"]
| Precautions | ["Hypersensitivity reactions including anaphylaxis","Bradycardia and cardiac arrest, especially in patients with pre-existing bradycardia or receiving other drugs that slow heart rate","Reversal failure: ensure adequate recovery of neuromuscular function","Re-administration of neuromuscular blocking agents after sugammadex may be difficult if needed within 24 hours","Use in renal impairment: not recommended in severe impairment (CrCl <30 mL/min) or dialysis patients"] |
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| Fertility Effects | No adverse effects on fertility observed in animal studies. Human data lacking. |