Basic Profile / Key Facts
Drug Category
Dosage Forms
Indications
Used as an adjunct with succinylcholine (or suxamethonium chloride) to prolong muscle relaxation and to prevent succinylcholine-induced muscle fasciculations.
Pharmacology
Hexafluorenium is a cholinesterase antagonist that can be used to prolong the relaxation effects of succinylcholine or suxamethonium chloride. Suxamethonium acts as a depolarizing muscle relaxant. It imitates the action of acetylcholine at the neuromuscular junction and is degraded by pseudocholinesterase, a plasma cholinesterase. The prolonged stimulation of the acetylcholine receptor results first in disorganized muscle contractions, then in profound relaxation. Cholinesterases catalyze the hydrolysis of the neurotransmitter acetylcholine into choline and acetic acid, a reaction necessary to allow a cholinergic neuron to return to its resting state after activation. There are two types of cholinesterase acetylcholinesterase and pseuodocholinesterase. The first hydrolyses acetylcholine more quickly; the latter hydrolyses butyrylcholine and succinylcholine more quickly. An absence or mutation of the pseudocholinesterase enzyme leads to a medical condition known simply as pseudocholinesterase deficiency. This is a silent condition that only manifests itself when people who have the deficiency receive the muscle relaxants succinylcholine or mivacurium during a surgery.
Mechanism of Action
Hexafluorenium is a non-competitive reversible inhibitor of human plasma cholinesterase or pseudocholinesterase. It is used in conjunction with suxamethonium or succinylcholine to extend the effects of this muscle relaxant
Absorption
Not Available
Toxicity
LD50 = 280 mg/kg (mouse, oral)
Biotrnasformation / Drug Metabolism
Not Available
Contraindications
Not Available
Drug Interactions
Not Available
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