Keshuting Sugammadex Sodium Injection

1. Indications and Usage
Reversal of Neuromuscular Blockade (NMB):
Reversal of rocuronium bromide or vecuronium bromide neuromuscular blockade in adult and pediatric patients (2 years of age and older).
Note: It is indicated for the reversal of moderate to deep blockade.
2. Dosage and Administration
Route of Administration:
For Intravenous (IV) Injection ONLY.
Recommended Dosage (Adults):
Reversal of Moderate Blockade:
Dose: 2 mg/kg.
Timing: When 1–2 twitches are present in a Train-of-Four (TOF) monitoring.
Reversal of Deep Blockade:
Dose: 4 mg/kg.
Timing: When 1–2 Post-Tetanic Count (PTC) stimuli are present.
Immediate Reversal (Emergency):
Dose: 16 mg/kg.
Timing: Immediately after administration of rocuronium (e.g., “Cannot Intubate, Cannot Ventilate” scenario).
Critical Administration Instructions:
Administer as a single IV bolus injection over 10 seconds or less.
Must be administered by anesthesia professionals familiar with neuromuscular monitoring.
3. Mechanism of Action
Selective Binding Agent:
Sugammadex is a chemically modified γ-cyclodextrin with a lipophilic core and a hydrophilic exterior.
Encapsulation (Host-Guest Chemistry):
It selectively binds to rocuronium and vecuronium (steroidal NMBAs) in a 1:1 stoichiometric ratio, forming a tight, non-covalent inclusion complex.
Therapeutic Result: By sequestering the free NMBA molecules in the plasma, it creates a concentration gradient that pulls the NMBA away from the neuromuscular junction, rapidly reversing the blockade.
Specificity: It does not bind to benzylisoquinolinium NMBAs (e.g., cisatracurium, mivacurium) or succinylcholine.
4. Safety and Warnings
Hypersensitivity Reactions:
Serious hypersensitivity reactions (e.g., anaphylaxis, angioedema, rash) have been reported.
Reappearance of Blockade:
Reappearance of neuromuscular blockade may occur after initial reversal. Patients must be monitored for at least 24 hours (or until stable) to ensure adequate recovery of muscle function.
Renal Impairment:
Sugammadex is primarily excreted unchanged by the kidneys.
Contraindication: Not recommended for patients with severe renal impairment (CrCl < 30 mL/min) or those requiring dialysis, as the complex may accumulate and cause prolonged paralysis.
Bleeding Risk:
Caution is advised in patients with coagulation disorders or those undergoing procedures with high bleeding risk.
5.Adverse Reactions
Most Common:
Headache, nausea, vomiting, hypotension, hypertension, coughing, and incomplete reversal.
6.Drug Interactions
Hormonal Contraceptives:
Sugammadex binds to progesterone. It may reduce the efficacy of hormonal contraceptives.
Action: Patients should use an alternative non-hormonal contraceptive method for 7 days after receiving Sugammadex.
Other Drugs:
Interaction with drugs that are highly protein-bound is theoretically possible but clinically rare.
7.Pharmaceutical Information
Chemical Composition:
Active Ingredient: Sugammadex Sodium.
Appearance: Clear, colorless to slightly yellow solution.
Excipients: Hydrochloric acid, sodium hydroxide, Water for Injection.
Storage: Store at 25°C (77°F); excursions permitted to 15–30°C (59–86°F).