DESUGOMYL 100 mg/ml

Indications

• Routine reversal of neuromuscular blockade induced by rocuronium
• Immediate reversal of neuromuscular blockade induced by vecuronium

Dosage

Adults: For adults, the recommended dosage is 16 mg/kg administered intravenously

Mechanism of action

Sugammadex forms very tight, water-soluble complexes with steroidal neuromuscular blocking drugs at a 1:1 ratio, with a higher affinity for rocuronium compared to vecuronium and pancuronium. This complexation creates a concentration gradient that drives the movement of the neuromuscular blocker from the neuromuscular junction into the plasma, effectively reversing the blockade. The bound neuromuscular blockers in the plasma are then tightly held by sugammadex, enhancing the diffusion of remaining molecules from the neuromuscular junction.

Pharmacodynamics

The pharmacodynamic effect of sugammadex is characterized by its ability to provide rapid reversal of neuromuscular blockade. By sequestering neuromuscular blocking agents, sugammadex allows for rapid recovery of neuromuscular function, which is critical in managing patients post-surgery or in emergency scenarios. Its effectiveness is particularly noted in cases where rapid recovery is desired, thus allowing for earlier patient mobilization and reduced risk of postoperative complications.

Pharmacokinetics

Sugammadex is administered intravenously and exhibits rapid onset of action. It is eliminated primarily through the kidneys, with a clearance that is dependent on renal function. The half-life of sugammadex ranges from 1 to 2 hours in healthy individuals, but it may be prolonged in patients with renal impairment. This necessitates careful consideration of dosing in patients with reduced kidney function. As sugammadex binds tightly to neuromuscular blockers, its pharmacokinetics are closely tied to the pharmacodynamics of the drugs it neutralizes.

Contra-indications

• Hypersensitivity to sugammadex or any of its excipients
• Severe renal impairment (creatinine clearance less than 30 mL/min)

Adverse effects

• Abdominal pain
• Arrhythmias
• Bradycardia
• Cough
• Dizziness
• Headache
• Hypersensitivity reactions
• Nausea
• Procedural complications
• Skin reactions
• Taste alterations
• Vomiting
• Bronchospasm

Interactions

• Sugammadex may decrease the efficacy of hormonal contraceptives including desogestrel, etonogestrel, levonorgestrel, medroxyprogesterone, norethisterone
• Combined hormonal contraceptives may have reduced exposure when used with sugammadex

Precautions

• Should only be administered by, or under the direct supervision of, personnel experienced in its use
• Monitor respiratory function until fully recovered post-administration
• Caution in patients with cardiovascular disease as recovery may be delayed
• Pre-existing coagulation disorders

Pregnancy

Use with caution due to lack of comprehensive safety information.

Breast-feeding

It is not known if sugammadex is excreted in human milk; exercise caution.

Storage

Store in a refrigerator (2°C to 8°C). Do not freeze. Protect from light.

Formulations

• Sugammadex 100 mg/ml solution for injection (Bridion)
• Sugammadex 500 mg/5 ml solution for injection
• Sugammadex 200 mg/2 ml solution for injection

Mechanism of action

Sugammadex is a modified gamma-cyclodextrin which forms very tight water soluble complexes at a 1:1 ratio with steroidal neuromuscular blocking drugs (rocuronium > vecuronium >> pancuronium). Sugammadex creates a concentration gradient which favors movement of rocurionium from the neuromuscular junction into the plasma, which quickly reverses rocuronium-induced neuromuscular blockade. The free rocuronium in the plasma are then bound tightly to sugammadex, assisting the diffusion of the remaining rocuronium molecules out of the neuromuscular junction and increasing bound and free rocuronium in the plasma.