BRIMADEX

What it is

Brimadex contains sugammadex, a modified gamma cyclodextrin which is a selective relaxant binding agent. It forms a complex with the neuromuscular blocking agents rocuronium or vecuronium and reduces the amount of neuromuscular blocking agent available to bind to nicotinic receptors in the neuromuscular junction. This results in the reversal of neuromuscular blockade induced by rocuronium or vecuronium. Brimadex solution for injection contains sugammadex 100 mg/mL.

Approved indications

— Reversal of neuromuscular blockade induced by rocuronium or vecuronium in patients 2 years of age and older.

Dosing overview

The recommended dose of sugammadex depends on the level of neuromuscular blockade to be reversed. A dose of 4.0 mg/kg sugammadex is recommended if recovery has reached 1–2 post-tetanic counts (PTC) following rocuronium- or vecuronium-induced blockade. A dose of 2.0 mg/kg sugammadex is recommended if spontaneous recovery has occurred up to the reappearance of T2 following rocuronium- or vecuronium-induced blockade. If there is a clinical need for immediate reversal following administration of rocuronium, a dose of 16.0 mg/kg sugammadex is recommended. Sugammadex should be administered intravenously as a single bolus injection. The bolus injection should be given rapidly, within 10 seconds, into an existing IV line.

Key safety warnings

In rare instances, marked bradycardia has been observed within minutes after administration of sugammadex for reversal of neuromuscular blockade. Isolated cases of bradycardia with cardiac arrest have been reported. Patients should be closely monitored for haemodynamic changes during and after reversal of neuromuscular blockade. Treatment with anti-cholinergic agents such as atropine should be administered if clinically significant bradycardia is observed. Hypersensitivity reactions, including anaphylaxis, have occurred in some patients and healthy volunteers. In clinical trials of surgical patients, these reactions were reported uncommonly (≥1/1000 to <1/100) and for post-marketing reports the frequency is unknown. These reactions varied from isolated skin reactions to serious systemic reactions (i.e. anaphylaxis, anaphylactic shock) and have occurred in patients with no prior exposure to sugammadex. Clinicians should be prepared for the possibility of drug hypersensitivity reactions (including anaphylactic reactions) and take the necessary precautions. In a study of volunteers, doses of 4 mg/kg and 16 mg/kg of sugammadex resulted in maximum mean prolongations of activated partial thromboplastin time (aPTT) by 17 and 22 per cent, and of prothrombin time international normalised ratio (PT(INR)) by 11 and 22 per cent, respectively. These limited mean aPTT and PT(INR) prolongations were of short duration (≤30 minutes). Although there is limited data on peri- or postoperative bleeding events in the clinical trial database, there is no indication of a clinically relevant increased incidence of bleeding events after sugammadex alone, or after sugammadex in combination with anticoagulants.

Contraindications

Hypersensitivity to the active substance or to any of the excipients.

PBS listing

Brimadex is registered on the ARTG in two strengths: sugammadex (as sodium) 200 mg/2 mL solution for injection vial and sugammadex (as sodium) 500 mg/5 mL solution for injection vial, both first listed on 30 January 2024 under licence category RE.

Regulatory history

Brimadex was first registered on the Australian Register of Therapeutic Goods (ARTG) on 30 January 2024.