Gantacurium

Gantacurium chloride (formerly recognized as AV430A and GW280430A) is a novel experimental neuromuscular-blocking drug or muscle relaxant in the category of non-depolarizing curare-mimetic benzylisoquinoline neuromuscular-blocking drugs, developed for the purpose of anesthesia during surgical procedures.

Pharmacology

Gantacurium represents a new class of muscle relaxants based on a three-point attachment concept that was designed to speed up onset and recovery. It is a member of a class of symmetrically bis-quaternary ammonium compounds that bind to the acetylcholine receptors at the neuromuscular junction.

Clinical Use

Gantacurium is not currently available for clinical use. It is in Phase II clinical trials. The most common side effects observed in clinical trials were slight, transient decreases in blood pressure and transient increases in heart rate.

Mechanism of Action

Gantacurium acts by binding competitively to the cholinergic receptors on the motor end-plate. This antagonizes the action of acetylcholine, resulting in flaccid muscle paralysis.

Pharmacokinetics

The onset of action with gantacurium is rapid (typically 2-3 minutes after administration), and the duration of muscle relaxation is relatively short.

See Also

• Neuromuscular-blocking drug
• Muscle relaxant
• Curare
• Benzylisoquinoline
• Acetylcholine receptor