hexafluorenium

502.746

502.335

55W5L6G81R

M - Musculo-skeletal system

0

-0.06

153.5

SRP: At the time of review, criteria for land treatment or burial (sanitary landfill) disposal practices are subject to significant revision. Prior to implementing land disposal of waste residue (including waste sludge), consult with environmental regulatory agencies for guidance on acceptable disposal practices.

Manufacturers, packers, and distributors of drug and drug products for human use are responsible for complying with the labeling, certification, and usage requirements as prescribed by the Federal Food, Drug, and Cosmetic Act, as amended (secs 201-902, 52 Stat. 1040 et seq., as amended; 21 U.S.C. 321-392).

LD50 = 280 mg/kg (mouse, oral)

CONSISTENT WITH ITS STABILIZING ACTION, IT POTENTIATES NEUROMUSCULAR BLOCKADE BY TUBOCURARINE & ANTAGONIZES THAT BY DECAMETHONIUM, BUT ITS EFFECTS ON BLOCKADE BY GALLAMINE ARE ERRATIC. PARADOXICALLY, IT MARKEDLY POTENTIATES & PROLONGS NEUROMUSCULAR ACTIONS OF SUCCINYLCHOLINE. /HEXAFLUORENIUM BROMIDE/|INTERACTION OF HEXAFLUORENIUM BROMIDE WITH ACETYLCHOLINE IODIDE, CARBACHOL & SUXAMETHONIUM CHLORIDE WITH REGARD TO DEPOLARIZATION OF THE END-PLATE OF RAT DIAPHRAGM WAS STUDIED.

Used as an adjunct with succinylcholine (or suxamethonium chloride) to prolong muscle relaxation and to prevent succinylcholine-induced muscle fasciculations.

Neuromuscular Nondepolarizing Agents; Cholinesterase Inhibitors|IT POSSESSES WEAK NEUROMUSCULAR BLOCKING ACTIVITY OF STABILIZING TYPE, BUT ACTIONS ARE TOO WEAK TO CAUSE USEFUL MUSCLE RELAXATION EXCEPT UNDER DEEP ETHER ANESTHESIA. /HEXAFLUORENIUM BROMIDE/|CLINICALLY, HEXAFLUORENIUM IS USED ONLY TO POTENTIATE & PROLONG EFFECTS OF SUCCINYLCHOLINE, SO THAT IT MAY BE USED IN PROLONGED SURGICAL PROCEDURES. /HEXAFLUORENIUM BROMIDE/|... IS SELECTIVE INHIBITOR OF PLASMA CHOLINESTERASE WITH MILD COMPETITIVE NEUROMUSCULAR BLOCKING POTENCY. IT IS GIVEN TO PROLONG BLOCKING ACTION OF SUCCINYLCHOLINE & TO MINIMIZE FASCICULATION THAT OCCURS PRIOR TO NEUROMUSCULAR BLOCK WITH THIS AGENT. /HEXAFLUORENIUM BROMIDE/|For more Therapeutic Uses (Complete) data for HEXAFLUORENIUM (8 total), please visit the HSDB record page.

@ PRESENT, THERE IS INSUFFICIENT DATA ON ADVERSE EFFECTS OF HEXAFLUORENIUM ALONE. /HEXAFLUORENIUM BROMIDE/|IN COMBINATION WITH SUCCINYLCHOLINE, ADVERSE EFFECTS ARE THOSE OF LARGE DOSES OF SUCCINYLCHOLINE & INCL EFFECTS, SUCH AS BRONCHOSPASM & VARYING DEG OF ATRIOVENTRICULAR BLOCK, THAT ARE RARELY SEEN WITH SUCCINYLCHOLINE ALONE. /HEXAFLUORENIUM BROMIDE/|COMBINATION /OF SUCCINYLCHOLINE & HEXAFLUORENIUM BROMIDE/ IS RELATIVELY CONTRAINDICATED IN BRONCHIAL ASTHMA. /HEXAFLUORENIUM BROMIDE/|THE NEUROMUSCULAR BLOCKING AGENTS ARE POTENTIALLY HAZARDOUS DRUGS. CONSEQUENTLY, THEY SHOULD BE ADMINISTERED TO PATIENTS ONLY BY ANESTHESIOLOGISTS & OTHER CLINICIANS WHO HAVE HAD EXTENSIVE TRAINING IN THEIR USE & IN A SETTING WHERE FACILITIES FOR RESPIRATORY & CARDIOVASCULAR RESUSCITATION ARE IMMEDIATELY AT HAND. /NEUROMUSCULAR BLOCKING AGENTS/|For more Drug Warnings (Complete) data for HEXAFLUORENIUM (6 total), please visit the HSDB record page.

Hexafluronium bromide 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.

Drugs that bind to nicotinic cholinergic receptors (RECEPTORS, NICOTINIC) and block the actions of acetylcholine or cholinergic agonists. Nicotinic antagonists block synaptic transmission at autonomic ganglia, the skeletal neuromuscular junction, and at central nervous system nicotinic synapses. (See all compounds classified as Nicotinic Antagonists.)

Hexafluronium bromide is a non-competitive reversible inhibitor of human plasma cholinesterase or pseudocholinesterase. Hexafluornium probably binds to anionic side receptors near the active center, causing a conformational change in the enzyme, preventing acylation of the esteratic site. The esteratic site on cholistereases is where acetylcholine is hydrolyzed to acetic acid and choline.|... WORK ... HAS LED TO PROPOSAL THAT PREJUNCTIONAL MOTOR-NERVE TERMINAL IS PRIMARY SITE OF ACTION OF COMPETITIVE & DEPOLARIZING NEUROMUSCULAR BLOCKING AGENTS. /NEUROMUSCULAR BLOCKING AGENTS/|...DESTRUCTION BY PLASMA CHOLINESTERASE IS...PRINCIPAL MEANS WHEREBY SUCCINYLCHOLINE IS DEGRADED, PROLONGATION OF ACTION MIGHT BE EXPLAINED BY ANTICHOLINESTERASE ACTION. HOWEVER, MARKED POTENTIATION CANNOT BE SO EXPLAINED, & VARIOUS EXPTL OBSERVATIONS INDICATE...INTERACTION @ NEUROMUSCULAR JUNCTION. /HEXAFLUORENIUM BROMIDE/

POISONING FROM NEUROMUSCULAR BLOCKING AGENTS IS ALMOST ALWAYS RESULT OF CLINICAL OVERDOSAGE OR THEIR INJUDICIOUS USE. IMPORTANT UNTOWARD RESPONSES ARE PROLONGED APNEA, CARDIOVASCULAR COLLAPSE, & THOSE RESULTING FROM HISTAMINE RELEASE. /NEUROMUSCULAR BLOCKING AGENTS/

hexafluorenium

DRUG IS AVAILABLE IN SOLN IN 10-ML VIALS (20 MG/ML). /HEXAFLUORENIUM BROMIDE/