Сукцинилхолин

Description

Succinylcholine (suxamethonium) is a quaternary ammonium ion, which is a bischoline ester of succinic acid. Solid substance. According to the classification, ChEBI belongs to both quaternary ammonium ions and succinate esters; databases record its functions as a neuromuscular agent, muscle relaxant and drug allergen. It is a quaternary muscle relaxant used in the form of bromide, chloride or iodide. By type of action - a depolarizing relaxant: the effect develops in approximately 30 seconds, the average duration of action is from three to five minutes. Used in surgical, anesthetic and other procedures where a short period of muscle relaxation is required.

Mechanism of action

Succinylcholine is a depolarizing neuromuscular blocker whose physiological effect is neuromuscular depolarizing blockade. The substance binds to nicotinic receptors at the neuromuscular junction and opens ligand-gated channels in the same way as acetylcholine. This leads to membrane depolarization and suppression of neuromuscular transmission. Depolarization is prolonged because succinylcholine is resistant to the action of acetylcholinesterases: the result is disorganized muscle contraction, followed by relaxation of skeletal muscles and flaccid paralysis.

Inactivation occurs in a different way - through plasma butyrylcholinesterase, which sequentially hydrolyzes ester bonds. The first stage produces succinyl monocholine, the second - succinic acid and choline. The speed of the first stage determines the short duration of action of the drug.

Identification

• CAS No.: 306-40-1
• Chemical formula: C14H30N2O4 (dication)
• Molecular weight: 290.404; exact mass: 290.221
• EU number: 200-747-4
• UNII: J2R869A8YF
• DSSTox ID: DTXSID7048455
• NCI Thesaurus Code: C61955
• ATX code: M03AB01; group M - musculoskeletal system

Physico-chemical properties

• Appearance: solid
• PSA Specifications: 52.6
• XLogP3: 0.6

The molecule carries two permanent positive charges on the quaternary nitrogen atoms. The constant charge excludes passive passage through lipid membranes: the substance does not penetrate the blood-brain barrier and is distributed in the extracellular fluid. Salts - chloride, bromide, iodide - are highly soluble in water, which allows the drug to be used intravenously.

Scope of application

• Anesthesiology: muscle relaxation during tracheal intubation, including during rapid sequential induction, when the speed of onset of the effect is important; short-term surgical and diagnostic interventions requiring muscle relaxation.
• Pharmaceutical production: substance for injection preparations based on chloride, bromide or iodide.
• Analytical standard for forensic chemistry laboratories where the substance is determined together with its metabolite succinyl monocholine by HPLC-MS/MS.
• Pharmacological studies of nicotinic cholinergic receptors at the neuromuscular junction.

Features that determine circulation

• The speed of onset and short duration of action depend on the activity of plasma butyrylcholinesterase; with its genetically determined deficiency, the block is delayed.
• The substance is listed in the database as a drug allergen.
• Preparations based on it are classified as drugs used exclusively when artificial ventilation is possible.

Safety Information

The GHS classification, hazard statements, precautionary statements and transport data for this substance are not available on the original card. The regulations for handling are determined not so much by chemical, but by pharmacological danger: the compound causes paralysis of skeletal muscles, including respiratory muscles. Work is carried out with gloves, safety glasses and a gown, all operations with powder are carried out under a hood. Access to the substance is limited to a circle of authorized employees, and quantitative records of receipts and consumption are maintained.

Storage and handling

Succinylcholine salts hydrolyze in aqueous solutions, and the faster the higher the temperature and pH. Hence the standard requirements: sealed containers, dry room, low temperature, for ready-made solutions - refrigerated storage and a limited shelf life. The solutions are not mixed with alkaline media. The specific storage mode and expiration date are clarified using the batch passport from the supplier.