Sugammadex sodium

Indications

Sugammadex sodium is used for: Reversal of Neuromuscular Blockers

Adult Dose

Intravenous Reversal of Neuromuscular Blockers Selective relaxant binding agent for reversal of neuromuscular blockade (NMB) induced by rocuronium or vecuronium in adults undergoing surgery Doses and timing of administration should be based on monitoring for twitch responses and the extent of spontaneous recovery that has occurred Administer as single IV bolus injection infused over 10 seconds into existing IV line Dose on actual body weight For rocuronium and vecuronium A dose of 4 mg/kg is recommended if spontaneous recovery of the twitch response has reached 1-2 post-tetanic counts (PTC) and there are no twitch responses to train-of-four (TOF) stimulation following rocuronium- or vecuronium-induced neuromuscular blockade A dose of 2 mg/kg is recommended if spontaneous recovery has reached the reappearance of the second twitch (T2) in response to TOF stimulation following rocuronium- or vecuronium-induced neuromuscular blockade For rocuronium only A dose of 16 mg/kg is recommended if there is a clinical need to reverse neuromuscular blockade soon (~3 minutes) after administration of a single dose of 1.2 mg/kg of rocuronium The efficacy of the 16-mg/kg dose following administration of vecuronium has not been studied

Child Dose

Renal Dose

Administration

IV Administration Administer by IV bolus into existing running IV line (see IV compatibilities) Ensure the infusion line is adequately flushed (eg, with 0.9% NaCl) between sugammadex sodium and administration of other drugs

Contra Indications

Known hypersensitivity to sugammadex or any of its components Hypersensitivity reactions that occurred varied from isolated skin reactions to serious systemic reactions (ie, anaphylaxis, anaphylactic shock) and have occurred in patients with no prior exposure to sugammadex Not recommended for patients with severe renal impairment (CrCl <30 mL/min) and those on dialysis

Precautions

Marked bradycardia reported, some resulting in cardiac arrest, within minutes following sugammadex administration Ventilatory support is mandatory for patients until adequate spontaneous respiration is restored and the ability to maintain a patent airway is assured A small number of patients experienced a delayed or minimal response to sugammadex; it is important to monitor ventilation until recovery occurs Lower than recommended sugammadex doses may lead to an increased risk of recurrence of neuromuscular blockade after initial reversal and is not recommended Drugs that potentiate neuromuscular blockade (eg, aminoglycosides, opioids) are used in the postoperative phase, so special attention should be paid to the possibility of recurrence of neuromuscular blockade Do not use to reverse blockade induced by nonsteroidal neuromuscular blocking agents (eg, succinylcholine, benzylisoquinolinium compounds) Risk of adverse reactions may be greater in patients with impaired renal function; care should be taken in the elderly when selecting dose, may be useful to monitor renal function Do not use to reverse neuromuscular blockade induced by steroidal neuromuscular blocking agents other than rocuronium or vecuronium Lactation Unknown if distributed in human breast milk Present in rat milk

Pregnancy-Lactation

Pregnancy There are no data on use in pregnant women to inform any drug-associated risks In animal reproduction studies, there was no evidence of teratogenicity following daily IV administration to rats and rabbits during organogenesis at exposures of up to 6 and 8 times, respectively, the maximum recommended human dose (MRHD) of 16 mg/kg However, there was an increase in the incidence of incomplete ossification of the sternebra and reduced fetal body weights in rabbits Lactation Unknown if distributed in human breast milk Present in rat milk Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for the drug, and any potential adverse effects on the breastfed infant from the drug or from the underlying maternal condition

Interactions

Toremifene has a relatively high binding affinity for sugammadex, and therefore, some displacement of vecuronium or rocuronium from the sugammadex binding complex could occur and result in recurrence of neuromuscular blockade Hormonal contraceptives May bind to progestogen, thereby decreasing progestogen exposure Administration of a bolus dose of sugammadex is considered to be equivalent to missing dose(s) of oral contraceptives containing an estrogen or progestogen; if an oral contraceptive is taken on the same day that sugammadex is administered, the patient must use an additional, nonhormonal contraceptive method or backup method of contraception (eg, condoms and spermicides) for the next 7 days In the case of hormonal hormonal contraceptives not taken orally, the patient must use an additional, hormonal contraceptive method or backup method of contraception (eg, condoms and spermicides) for the next 7 days Sugammadex may also interfere with serum progesterone assay

Adverse Effects

Side effects of Sugammadex sodium : >10% Pain (36-52%) Nausea (23-26%) Vomiting (11-15%) Hypotension (4-13%) 1-10% Headache (5-10%) Pyrexia (5-9%) Hypertension (5-9%) Airway complication of anesthesia (1-9%) Anesthetic complication (1-9%) Procedural complication (1-8%) Cough (1-8%) Chills (3-7%) Incision site pain (4-6%) Abdominal pain (4-6%) Dizziness (3-6%) Pain in extremity (1-6%) QT interval abnormal (1-6%) Oropharyngeal pain (3-5%) Insomnia (2-5%) Tachycardia (2-5%) Bradycardia (1-5%) Pruritus (2-3%) Flatulence (1-3%) Hypoesthesia (1-3%) Anxiety (1-3%) Wound hemorrhage (1-2%) Dry mouth (1-2%) Restlessness (1-2%) Depression (1-2%) Decreased RBCs (1-2%) Increased CPK (1-2%) Musculoskeletal pain (1-2%) Myalgia (1-2%) Erythema (1-2%) Hypocalcemia (1-2%)

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