Sugammadex sodium

Mechanism of Action

Selective relaxant binding agent; 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

Distribution

Vd: 11-14 L

Metabolism

No metabolites of sugammadex have been observe

Elimination

Clearance: 88 mL/min

Excretion: 96% urine; <0.02% feces or expired air

Half-life

• Normal renal function: 2 hr
• Mild renal impairment: 4 hr
• Moderate renal impairment: 6 hr
• Severe renal impairment: 19 hr

Selective relaxant binding agent; modified γ-cyclodextrin.1 3 4 7 15 17 18

Pharmacokinetics of sugammadex are based on the total concentration of free plus complex-bound sugammadex; the pharmacokinetics of complex-bound sugammadex are assumed to be the same as those of free sugammadex.1

Absorption

Bioavailability

Exhibits linear pharmacokinetics over dose range of 1–16 mg/kg.1

Onset

Recovery of neuromuscular function occurred at approximately 1.4–2.1 minutes when administered at reappearance of T2 for rocuronium- or vecuronium-induced neuromuscular blockade.1

Recovery of neuromuscular function occurred at approximately 2.7–3.3 minutes when administered at 1–2 PTC for rocuronium- or vecuronium-induced neuromuscular blockade.1

Distribution

Extent

Distributes into and is retained in sites of active mineralization (e.g., bone, teeth).1

Not known if distributed into milk.1

Plasma Protein Binding

None.1

Elimination

Metabolism

Not metabolized.1

Elimination Route

Excreted principally in urine as unchanged drug; <0.02% excreted in the feces or expired.1 >90% of a dose excreted within 24 hours.1

Hemodialysis using a high-flux filter removes about 70% of the drug over 3–6 hours.1

Half-life

Plasma: About 2 hours.1

Bone and teeth: 172 and 8 days, respectively.1

Special Populations

Plasma elimination half-life is 4, 6, or 19 hours in patients with mild, moderate, or severe renal impairment, respectively.1

• A modified γ-cyclodextrin that binds selectively to and forms a complex with (i.e., encapsulates) steroidal nondepolarizing neuromuscular blocking agents (e.g., rocuronium, vecuronium); reduces amount of neuromuscular blocking agent available to bind to nicotinic cholinergic receptors in the neuromuscular junction and thus reverses neuromuscular blockade. 1 3 4 7 15 17 18 121

• Forms a complex with free rocuronium or vecuronium molecules in plasma in a 1:1 ratio.1 Because of cyclodextrin structure (hydrophilic molecule with a lipophilic core), specifically encapsulates lipophilic (e.g., steroidal) molecules.1 15 18

• Exhibits higher binding affinity for rocuronium than vecuronium and a much lower affinity for pancuronium.15 121

• No affinity for succinylcholine, mivacurium, atracurium, or cisatracurium.15 18 121

• Importance of informing women that sugammadex can substantially decrease the effectiveness of hormonal contraceptives, including oral and non-oral forms; advise women to use additional nonhormonal forms of contraception for 7 days after sugammadex administration.1

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1

• Importance of informing patients of other important precautionary information.1 (See Cautions.)

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.