Brand name: Bridion
Drug class: Antidotes
Chemical name: C72H104Na8O48S8
Molecular formula: 6A,6B,6C,6D,6E,7F,6G,6H-Octakis-S-(2-carboxyethyl)-6A,6B,6C,6D,6E,6F,6G,6H-octathio-γ-cyclodextrin
CAS number: 343306-79-6
Selective relaxant binding agent; modified γ-cyclodextrin.
Uses for Sugammadex
Reversal of Neuromuscular Blockade
Used to reverse neuromuscular blockade induced by rocuronium or vecuronium in patients undergoing surgery.
Reduces time to recovery of neuromuscular function when administered at moderate (reappearance of the second twitch [T2] in a train-of-four [TOF] stimulation) or deep (1–2 posttetanic counts [PTC] and no twitch responses to TOF stimulation) neuromuscular blockade compared with neostigmine.
Highest recommended dose of 16 mg/kg may be used for immediate reversal of profound neuromuscular blockade induced by high-dose (1.2 mg/kg) rocuronium bromide if clinically indicated; when given shortly (approximately 3 minutes) after the onset of blockade, reduces time to recovery of neuromuscular function compared with spontaneous recovery from succinylcholine.
Effective reversal agent for steroidal neuromuscular blocking agents rocuronium and vecuronium only; not indicated for reversal of nonsteroidal neuromuscular blocking agents (e.g., succinylcholine, benzylisoquinolinium compounds [atracurium, mivacurium]).
Not studied in the intensive care unit (ICU) setting.
Appropriate reversal of neuromuscular blocking agents is critical for preventing postoperative residual neuromuscular blockade. Reversal of neuromuscular blockade should always be considered unless there is quantitative evidence indicating that no reversal is needed (TOF >0.9).
Sugammadex may provide potential clinical benefits over cholinesterase inhibitors (e.g., neostigmine) including fast and predictable reversal of any degree of block, less potential for adverse effects (due to lack of effect on the acetylcholinesterase receptor system), and reduced incidence of residual block on recovery.
Sugammadex Dosage and Administration
- Patient Monitoring
Monitor patient for adequate ventilation and maintenance of patent airway until complete recovery of neuromuscular function (based on assessment of skeletal muscle tone, respiratory measurements, and response to peripheral nerve stimulation). Adequate recovery of neuromuscular function generally defined as a TOF ratio ≥0.9 in addition to the patient's ability to maintain satisfactory ventilation and a patent airway.
Ventilatory support required until recovery of adequate spontaneous respiration and ability to maintain a patent airway is assured. (See Respiratory Function Monitoring under Cautions.)
- Dispensing and Administration Precautions
Administer only by trained clinicians experienced in the use of neuromuscular blocking agents and reversal agents.
For solution and drug compatibility information, see Compatibility under Stability.
Administer by direct IV (“bolus”) injection over 10 seconds into an existing IV line. The drug has only been administered as a single direct IV injection in clinical studies.
Available as sugammadex sodium; dosage expressed in terms of sugammadex.
Determine appropriate dose and timing based on twitch response monitoring and the extent of spontaneous recovery that has occurred. Dose does not depend on the anesthetic regimen used.
Calculate dose based on actual body weight (ABW).
No clinically relevant differences in pharmacokinetic parameters observed between obese patients and the general population when dosed according to ABW. The current evidence supports use of ABW-based dosing in patients who are morbidly obese (BMI ≥40 kg/m2) irrespective of the depth of neuromuscular blockade.
Routine Reversal of Rocuronium- or Vecuronium-induced Neuromuscular Blockade
For reversal of moderate blockade (i.e., spontaneous recovery has reached the reappearance of T2 in a TOF stimulation) following rocuronium or vecuronium: 2 mg/kg.
For reversal of deep blockade (i.e., spontaneous recovery of the twitch response has reached 1–2 PTC and no twitch responses to TOF stimulation) following rocuronium or vecuronium: 4 mg/kg.
Immediate Reversal of Rocuronium-induced Neuromuscular Blockade
For reversal immediately (approximately 3 minutes) after a single 1.2-mg/kg dose of rocuronium bromide if clinically indicated: 16 mg/kg.
Efficacy of the 16-mg/kg dose for rapid reversal of vecuronium not established.
No specific dosage recommendations. (See Hepatic Impairment under Cautions.)
Mild or moderate renal impairment: No dosage adjustment required.
Severe renal impairment, including dialysis: Use not recommended. (See Renal Impairment under Cautions.)
No dosage adjustment required. However, careful dosage selection advised because of age-related decreases in renal function.
Cautions for Sugammadex
Known hypersensitivity to sugammadex or any ingredient in the formulation.
Anaphylaxis and Hypersensitivity
Serious, potentially fatal, hypersensitivity reactions reported. Manifestations have ranged from isolated skin reactions (e.g., flushing, urticaria, erythematous rash) to more severe systemic reactions (e.g., anaphylaxis) requiring use of vasopressors, prolonged hospitalization, and/or additional respiratory support.
Monitor for hypersensitivity reactions and ensure ability to manage such reactions.
Marked bradycardia may occur minutes after sugammadex administration; cardiac arrest precipitated by bradycardia also reported. Closely monitor for hemodynamic changes and administer anticholinergic agents (e.g., atropine) if clinically important bradycardia occurs.
Respiratory Function Monitoring
Delayed or minimal reversal of neuromuscular blockade following sugammadex administration has occurred in some patients. Neuromuscular blockade also may recur following extubation. Respiratory depression may persist after complete recovery of neuromuscular function.
Monitor respiratory function and provide ventilatory support until adequate spontaneous respiration is restored and the ability to maintain a patent airway is assured. If neuromuscular blockade persists or recurs, take appropriate steps to provide adequate ventilation.
Readministration of Neuromuscular Blocking Agents
If readministration of a steroidal neuromuscular blocking agent is necessary (e.g., for intubation) after reversal with sugammadex, observe a minimum wait time based on dose of sugammadex and renal function.
Following administration of sugammadex (2 or 4 mg/kg), a minimum wait time of 5 minutes is recommended before readministration of rocuronium bromide 1.2 mg/kg, and a minimum wait time of 4 hours is recommended before readministration of rocuronium bromide 0.6 mg/kg or vecuronium bromide 0.1 mg/kg. If rocuronium bromide 1.2 mg/kg is administered ≤30 minutes after sugammadex, the onset of neuromuscular blockade may be delayed up to approximately 4 minutes and the duration of blockade shortened by approximately 15 minutes.
Following administration of sugammadex 16 mg/kg, a minimum wait time of 24 hours is recommended before rocuronium or vecuronium is readministered.
In patients with mild or moderate renal impairment, a minimum wait time of 24 hours is recommended after administration of sugammadex (2 or 4 mg/kg) before rocuronium bromide 0.6 mg/kg or vecuronium bromide 0.1 mg/kg is readministered. If a shorter wait time is necessary, the rocuronium bromide dose for a new blockade should be 1.2 mg/kg.
If neuromuscular blockade is required before the recommended wait times have elapsed, consider use of a nonsteroidal neuromuscular blocking agent (e.g., succinylcholine). However, onset of neuromuscular blockade with depolarizing neuromuscular blocking agents may be delayed in this setting.
Recurrence of Neuromuscular Blockade
Risk of recurrence of neuromuscular blockade may be increased with concurrent use of certain drugs (i.e., drugs that displace rocuronium or vecuronium from sugammadex binding sites) or use of lower than recommended doses of sugammadex. Mechanical ventilation may be required.
Risk also may be increased with use of drugs that potentiate neuromuscular blockade during postoperative period; consult prescribing information for rocuronium or vecuronium for specific drugs that may potentiate neuromuscular blockade. (See Interactions.)
Coagulopathy and Bleeding
Increased coagulation parameters (e.g., aPTT, PT, INR) observed. However, does not appear to correlate with an increased risk of bleeding.
Risk of bleeding not evaluated with sugammadex 16 mg/kg in patients receiving thromboprophylaxis drugs. Risk of bleeding also not evaluated in patients with known coagulopathies or receiving therapeutic anticoagulation or thromboprophylaxis with drugs other than heparin and low molecular weight heparin. Carefully monitor coagulation parameters in such patients.
Signs of light anesthesia (e.g., movement, coughing, grimacing, suckling of the tracheal tube) may be noted if neuromuscular blockade is reversed during anesthesia.
No clinical trial data regarding use of sugammadex in pregnant women. Malformations not observed in animal studies; however, incomplete ossification and reduced fetal body weight observed at dose exposures greater than the maximum recommended human dose.
Distributed into milk in rats; not known whether distributed into human milk. Consider benefits of breast-feeding and importance of the drug to the woman; also consider potential adverse effects on the breast-fed infant from the drug or underlying maternal condition.
Safety and efficacy not established in pediatric patients.
Has been used in some pediatric patients for reversal of moderate rocuronium-induced neuromuscular blockade. Some evidence suggests similar efficacy and safety in pediatric patients 2–17 years of age and adults.
Animal toxicity studies indicate possible adverse effects on developing bone; increased bone deposition, decreased bone length, and tooth enamel abnormalities observed in juvenile animals receiving daily IV doses of sugammadex.
Median time to recovery following administration of sugammadex 2 mg/kg at reappearance of T2 after rocuronium-induced blockade was 2.5 and 3.6 minutes in geriatric patients 65–74 and ≥75 years of age, respectively, compared with 2.2 minutes in patients 18–64 years of age. Median time to recovery following sugammadex 4 mg/kg at 1–2 PTC was 2.5 minutes in geriatric patients ≥65 years of age compared with 2 minutes in younger adults.
Pharmacokinetics not studied in patients with hepatic impairment; not metabolized or excreted by the liver. Use with caution in patients with hepatic impairment accompanied by coagulopathy or severe edema.
Not recommended by manufacturer in patients with severe renal impairment, including those requiring dialysis, because of prolonged and increased overall drug exposure and insufficient experience in such patients. (See Renal Impairment under Dosage and Administration.) Limited experience in some patients with end-stage renal impairment and patients undergoing renal transplantation.
If patients with mild or moderate renal impairment require readministration of a neuromuscular blocking agent, a minimum wait time may be required. (See Readministration of Neuromuscular Blocking Agents under Cautions.)
Common Adverse Effects
Vomiting, pain, nausea, hypotension, headache.
Interactions for Sugammadex
Not likely to be metabolized by CYP isoenzymes; therefore, CYP-mediated drug interactions not expected.
Potential decreased exposure and reduced efficacy of hormonal contraceptive
Advise women to use an additional, non-hormonal method of contraception for 7 days following sugammadex administration
Displacement of rocuronium or vecuronium by toremifene can result in recurrence of neuromuscular blockade
Recovery of neuromuscular function may be delayed
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.
Exhibits linear pharmacokinetics over dose range of 1–16 mg/kg.
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.
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.
Distributes into and is retained in sites of active mineralization (e.g., bone, teeth).
Not known if distributed into milk.
Plasma Protein Binding
Excreted principally in urine as unchanged drug; <0.02% excreted in the feces or expired. >90% of a dose excreted within 24 hours.
Hemodialysis using a high-flux filter removes about 70% of the drug over 3–6 hours.
Plasma: About 2 hours.
Bone and teeth: 172 and 8 days, respectively.
Plasma elimination half-life is 4, 6, or 19 hours in patients with mild, moderate, or severe renal impairment, respectively.
Pharmacokinetics do not appear to be affected by age, gender, race, or obesity.
25°C (may be exposed to 15–30°C). Protect from light; use within 5 days if not protected from light.
For information on systemic interactions resulting from concomitant use, see Interactions.
Dextrose 2.5% in sodium chloride 0.45%
Dextrose 5% in sodium chloride 0.9%
Dextrose 5% in water
Isolyte P in dextrose 5%
Ringer’s injection, lactated
Sodium chloride 0.9%
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.
Forms a complex with free rocuronium or vecuronium molecules in plasma in a 1:1 ratio. Because of cyclodextrin structure (hydrophilic molecule with a lipophilic core), specifically encapsulates lipophilic (e.g., steroidal) molecules.
Exhibits higher binding affinity for rocuronium than vecuronium and a much lower affinity for pancuronium.
No affinity for succinylcholine, mivacurium, atracurium, or cisatracurium.
Advice to Patients
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.
Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.
Importance of informing patients of other important precautionary information. (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.
100 mg (of sugammadex) per mL
AHFS DI Essentials™. © Copyright 2023, Selected Revisions December 13, 2021. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.
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