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AI-Generated response:

What is Sugammadex?

Answer generated on June 4, 2024

The AI-generated responses are for illustration purposes only and should not be used for medical purposes.

Sugammadex, marketed as Bridion, is a modified gamma cyclodextrin used to reverse neuromuscular blockade induced by rocuronium and vecuronium, with noted risks of marked bradycardia and cardiac arrest following administration.[1-2]

  • Sugammadex is specifically designed to reverse the effects of the steroidal neuromuscular blocking agents rocuronium and vecuronium, which are commonly used during surgical procedures to induce muscle relaxation.[1-2]

  • It is administered intravenously, typically as a single bolus injection, and the dosage can vary depending on the depth of neuromuscular blockade and the timing of the reversal.[2]

  • The drug works by forming a complex with rocuronium or vecuronium, reducing their availability to bind to nicotinic cholinergic receptors at the neuromuscular junction, thereby reversing the muscle paralysis.[1-2]

  • Sugammadex is cleared primarily through renal excretion, and its pharmacokinetics can be significantly altered in patients with renal impairment, necessitating dose adjustments.[1]

  • It has been associated with serious adverse effects including marked bradycardia and cases of cardiac arrest shortly after administration, necessitating close monitoring of hemodynamic parameters.[1]

Additional info

Sugammadex's unique mechanism of action and its specific interaction with rocuronium and vecuronium make it a critical drug in the arsenal of anesthetics, particularly useful in surgeries where rapid reversal of deep neuromuscular blockade is required. However, its safety profile requires careful consideration, especially in patients with underlying cardiac issues or those with severe renal impairment, as these conditions can alter the drug's effectiveness and safety. Monitoring hemodynamic parameters during and after administration of sugammadex is crucial due to the risk of severe bradycardia and cardiac arrest. This drug is not recommended for reversing neuromuscular blockade induced by nonsteroidal neuromuscular blocking agents or other steroidal agents besides rocuronium and vecuronium.[1] The use of sugammadex provides a significant advantage in managing the depth of neuromuscular blockade with precision, but its use must be judicious and well-monitored.

References

Reference 1

1.

Elsevier ClinicalKey Drug Monograph

Content last updated: April 3, 2024.

Mechanism Of Action Sugammadex is a modified gamma cyclodextrin that forms a complex with the neuromuscular blocking agents rocuronium and vecuronium. This results in a reduction in the amount of neuromuscular blocking agent available to bind to nicotinic cholinergic receptors in the neuromuscular junction, and the neuromuscular blockade induced by rocuronium or vecuronium is thereby reversed.

Description Sugammadex is a modified gamma cyclodextrin for the reversal of neuromuscular blockade effects of rocuronium and vecuronium in adults and pediatric patients 2 years and older undergoing surgery. Sugammadex use for reversal of neuromuscular blockade in the intensive care unit or for reversal of nonsteroidal neuromuscular blocking agents or steroidal neuromuscular blocking agents other than rocuronium and vecuronium has not been studied. Cases of marked bradycardia, some resulting in cardiac arrest, have been observed within minutes of sugammadex administration; monitor hemodynamic parameters for changes during and after sugammadex receipt.

Description Bridion is a modified gamma cyclodextrin for the reversal of neuromuscular blockade effects of rocuronium and vecuronium in adults and pediatric patients 2 years and older undergoing surgery. Bridion use for reversal of neuromuscular blockade in the intensive care unit or for reversal of nonsteroidal neuromuscular blocking agents or steroidal neuromuscular blocking agents other than rocuronium and vecuronium has not been studied. Cases of marked bradycardia, some resulting in cardiac arrest, have been observed within minutes of bridion administration; monitor hemodynamic parameters for changes during and after bridion receipt.

Pharmacokinetics Sugammadex is administered intravenously. The observed steady-state Vd in adult patients with normal renal function is 11 to 14 L. Sugammadex and the complex of sugammadex and rocuronium do not bind to plasma proteins or erythrocytes. No metabolites of sugammadex have been observed in clinical studies and only renal excretion of the unchanged product was observed as the route of elimination. More than 90% of the dose is excreted within 24 hours with at least 95% as unchanged drug. The elimination half-life of sugammadex in adults is about 2 hours, and the estimated plasma clearance is about 88 mL/minute. Sugammadex was retained in sites of active mineralization, such as bone and teeth, with a mean half-life of 172 and 8 days, respectively, in animal studies. Affected cytochrome P450 isoenzymes and drug transporters: none ** • Route-Specific Pharmacokinetics** **Intravenous Route** Linear kinetics are observed when sugammadex is administered within the dosage range of 1 to 16 mg/kg as an IV bolus. ** • Special Populations** **Renal Impairment** In adult patients with mild, moderate, and severe renal impairment, the half-life of sugammadex is prolonged to 4, 6, and 19 hours, respectively. In a clinical trial of adult patients with severe renal impairment, exposure was 17 times higher than that seen in patients with normal renal function, and low concentrations of sugammadex were detectable for at least 48 hours after administration. In a second study, sugammadex clearance progressively decreased and the half-life progressively increased with declining renal function. In adult patients with moderate and severe renal impairment, exposure was 2 and 5 times higher, respectively, than patients with normal renal function. Sugammadex concentrations were not detectable beyond 7 days post-dose in patients with severe renal impairment. **Pediatrics** Sugammadex exposure (AUC0-inf and Cmax) increased in a dose-dependent, linear manner after administration of intravenous doses of 2 and 4 mg/kg in pediatric patients 2 to 16 years of age.

Indications And Dosage **General Dosing Information** * The use of sugammadex for reversal of neuromuscular blockade following rocuronium or vecuronium administration in the intensive care unit has not been studied. * Do not use sugammadex for reversal of neuromuscular blockade following nonsteroidal neuromuscular blocking agents (e.g., succinylcholine) or steroidal neuromuscular blocking agents other than rocuronium or vecuronium.

Reference 2

2.

Food and Drug Administration (DailyMed).

Publish date: May 3, 2023.

Mechanism Of Action 12.1 Mechanism of Action BRIDION (sugammadex) is a modified gamma cyclodextrin. It forms a complex with the neuromuscular blocking agents rocuronium and vecuronium, and it reduces the amount of neuromuscular blocking agent available to bind to nicotinic cholinergic receptors in the neuromuscular junction. This results in the reversal of neuromuscular blockade induced by rocuronium and vecuronium.

Description 11 DESCRIPTION BRIDION (sugammadex) injection, for intravenous use, contains BRIDION (sugammadex) sodium, a modified gamma cyclodextrin chemically designated as 6 A,6 B,6 C,6 D,6 E,6 F,6 G,6 H -Octakis-S-(2-carboxyethyl)-6 A,6 B,6 C,6 D,6 E,6 F,6 G,6 H -octathio- γ -cyclodextrin sodium salt (1:8) with a molecular weight of 2178.01. The structural formula is: BRIDION (sugammadex) is supplied as a sterile, non-pyrogenic aqueous solution that is clear, colorless to slightly yellow-brown for intravenous injection only. Each mL contains 100 mg BRIDION (sugammadex), which is equivalent to 108.8 mg BRIDION (sugammadex) sodium. The aqueous solution is adjusted to a pH of between 7 and 8 with hydrochloric acid and/or sodium hydroxide. The osmolality of the product is between 300 and 500 mOsmol/kg. BRIDION (sugammadex) may contain up to 7 mg/mL of the mono OH-derivative of BRIDION (sugammadex) [see Clinical Pharmacology (12.2) ].

Clinical Pharmacology 12 CLINICAL PHARMACOLOGY 12.1 Mechanism of Action BRIDION (sugammadex) is a modified gamma cyclodextrin. It forms a complex with the neuromuscular blocking agents rocuronium and vecuronium, and it reduces the amount of neuromuscular blocking agent available to bind to nicotinic cholinergic receptors in the neuromuscular junction. This results in the reversal of neuromuscular blockade induced by rocuronium and vecuronium. 12.2 Pharmacodynamics BRIDION (sugammadex) has been administered in doses ranging from 0.5 mg/kg to 16 mg/kg in dose response trials of rocuronium-induced blockade (0.6, 0.9, 1 and 1.2 mg/kg with and without maintenance doses) and vecuronium-induced blockade (0.1 mg/kg with or without maintenance doses) at different time points/depths of block. In these trials a clear dose-response relationship was observed. BRIDION (sugammadex) may contain up to 7% of the mono OH-derivative of BRIDION (sugammadex). In preclinical pharmacology studies, the mono OH-derivative was demonstrated to have ~50% of the affinity as BRIDION (sugammadex) for rocuronium and vecuronium and that product with up to 7% of the mono OH-derivative has nearly similar efficacy in reversing rocuronium- or vecuronium-induced blockade.

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