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SUCCINYLCHOLINE CHLORIDE

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SUCCINYLCHOLINE CHLORIDE Basic information
SUCCINYLCHOLINE CHLORIDE Chemical Properties
Safety Information
  • Safety Statements 7/8
  • RIDADR 3249
  • RTECS GA2360000
  • HazardClass 6.1(b)
  • PackingGroup III
  • ToxicityLD50 i.v. in mice: 0.45 mg/kg (Anttila, Ertama)
SUCCINYLCHOLINE CHLORIDE Usage And Synthesis
  • Chemical Propertieswhite powder
  • UsesA neuromuscular blocking agent. Muscle relaxant (skeletal).
  • DefinitionChEBI: A chloride salt in which the negative charge of the chloride ions is balanced by succinylcholine dications.
  • brand nameAnectine (Sandoz); Quelicin (Hospira); Sucostrin (Apothecon).
  • World Health Organization (WHO)Suxamethonium chloride is a short-acting muscle relaxant. It is used in surgery. Suxamethonium chloride is listed in the WHO Model List of Essential Drugs.
  • Biological FunctionsSuccinylcholine chloride (Anectine) is the only depolarizing- type blocker that is in widespread clinical use. It produces neuromuscular block by overstimulation, so that the end plate is unable to respond to further stimulation. Structurally, succinylcholine is equivalent to two ACh molecules joined back to back. The resulting 10- carbon atom spacing between the two quaternary ammonium heads is important for activation of the two binding sites on the AChR. Because the succinylcholine molecule is “thin,” binding to the two sites does not sterically occlude the open channel, and cations are allowed to flow and depolarize the end plate.
    Neuromuscular block with succinylcholine occurs by two sequential events. An initial depolarization of the end plate produces muscle action potentials and fasciculation. Maintained depolarization past the threshold for firing produces Na channel inactivation, so that muscle action potentials cannot be generated. This is called phase I, or depolarization block. In the continued presence of succinylcholine, the membrane becomes repolarized, Na channel inactivation is reversed, and muscle membrane excitability is restored. Nonetheless, the neuromuscular block persists because of desensitization of the AChR. This is known as phase II, or desensitization block.
    Although the mechanism for phase II block is not completely understood, a series of allosteric transitions in the AChR is suspected. One model to describe this has the AChR in equilibrium among four conformations: resting, active, inactive, and desensitized. Agonists stabilize the active and desensitized states, whereas antagonists tend to stabilize the resting and possibly the desensitized state.
  • General DescriptionSuccinylcholine chloride,choline chloride succinate (2:1) (Anectine, Sucostrin),is a white, odorless, crystalline substance that is freely solublein water to give solutions with a pH of about 4. It isstable in acidic solutions but unstable in alkali. Aqueous solutionsshould be refrigerated to ensure stability.
    Succinylcholine chloride is characterized by a very shortduration of action and a quick recovery because of its rapidhydrolysis after injection. It brings about the typical muscularparalysis caused by blocking nervous transmission at themyoneural junction. Large doses may cause temporary respiratorydepression, as with similar agents. Its action, in contrastwith that of (1)-tubocurarine, is not antagonized byneostigmine, physostigmine, or edrophonium chloride.These anticholinesterase drugs actually prolong the action ofsuccinylcholine chloride, which suggests that the drug isprobably hydrolyzed by cholinesterases. The brief durationof action of this curare-like agent is said to render an antidoteunnecessary if the proper supportive measures are available.Succinylcholine chloride has a disadvantage, however, inthat the usual antidotes cannot terminate its action promptly.
  • General DescriptionFine white powder.
  • Air & Water ReactionsWater soluble.
  • Fire HazardFlash point data for SUCCINYLCHOLINE CHLORIDE are not available. SUCCINYLCHOLINE CHLORIDE is probably combustible.
  • Clinical UseSuccinylcholine Chloride is used as a muscle relaxant for the same indications asother curare agents. It may be used for either short or longperiods of relaxation, depending on whether one or severalinjections are given. In addition, it is suitable for continuousintravenous drip administration.
    Succinylcholine chloride should not be used withthiopental sodium because of the high alkalinity of the latter.If used together, they should be administered immediatelyafter mixing; however, separate injection is preferable.
  • Veterinary Drugs and TreatmentsSuccinylcholine chloride is indicated for short-term muscle relaxation needed for surgical or diagnostic procedures, to facilitate endotracheal intubation in some species, and reducing the intensity of muscle contractions associated with electro- or pharmacological- induced convulsions. Dogs, cats, and horses are the primary veterinary species where succinylcholine chloride has been used.
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