Cisatracurium Besilate Skeletal Muscle Relaxant

English name：Cisatracurium besylate

CAS number：96946-42-8

Molecular formula: C53H72N2O12.2C6H5O3S

Molecular weight: 1243.49

EINECS number: 620-579-9

Related category

Pharmaceutical raw materials; Chemical products - Organic chemicals; Intermediate; Raw materials; Pharmaceutical raw materials; Medical muscle relaxants; Pharmaceutical intermediates; Small molecule inhibitor; Analytical reagents - reference products; Medical raw materials; Neuromuscular Blocking Agent; Aromatics; Hetero Chemical book cycles; Intermediates & Fine Chemicals; Pharmaceuticals; Other APIs; Analgesic series; Ingredients; Pharmaceutical, pesticide and dye intermediates; Chemical materials; Pharmaceutical raw materials; Impurity reference; Chemical reagent

Mol file：96946-42-8.mol

Structural formula:

Properties of cisatracurium benzenesulfonate

Melting point :90-93°C

Storage conditions :Sealed in dry,Store in freezer, under -20°C

Solubility: Solubility in water is 1mg/mL

Form: Powder

Color: White

InChIKey：XXZSQOVSEBAPGS-UHFFFAOYSA-L

Muscle relaxant

Cisatracurium benzenesulfonate, the benzenesulfonate form of atracurium, is a neuromuscular blocker that binds to cholinergic receptors on the motor endplate to antagonize the action of acetylcholine, resulting in a competitive neuromuscular block effect similar to tubocurarine, with an onset time of 1 minute and a duration of 15 minutes. The therapeutic dose does not affect the heart, liver and kidney function. No accumulation. In large doses, the Chemicalbook can promote the release of histamine. Used to relax muscles or control breathing during surgery. Compared with the main clinical muscle relaxants, cisatracurium bensulate has the characteristics of metabolism through non-hepatic and non-renal pathways and cardiovascular stability, and the muscle relaxant effect is 3 times stronger than atracurium, without cardiovascular side effects. It is mainly suitable for general anesthesia, and can be widely used in tracheal intubation, liver and kidney dysfunction, cardiovascular surgery and elderly and pediatric patients.

Compared with atracurium, this product does not have the adverse effect of dose-dependent histamine release. The disadvantage is that patients with liver and kidney dysfunction should be used with caution.

Since the drug was first marketed in the UK in 1996, foreign countries have gradually replaced vecuronium bromide and atracuronium, becoming the mainstream of clinical muscle relaxants.

Market conditions

Benzene sulfonic shun atracurium injection by GlaxoSmithKline (GlaxoSmithKline) cooperate with abbott laboratories (AbbotChemicalbooktLaboratories) research and development of drugs to the depolarization of skeletal muscle relaxation. It was first released in the UK in August 1995.

The product successively in 1996, Germany, France and Italy and other European countries in 2004, the product imported to China, the holder for AspenPharmaTradingLimited, Producers for GLAXOSMITHKLINChemicalbookEMANUFACTURINGSPA (Italy), ning/Nimbex commodity called game machine, specifications of 2 mg/ml (2.5 ml: 5 mg, 5 ml: 10 mg and 10 ml: 20 mg). The product is not yet available in Japan.

Pharmacological action

The mechanism of action of cisolenesulfoatracurium is similar to tubocurine chloride, but this product is a non-depolarizing muscle relaxant, mainly blocking the conduction of nerve impulse, so that muscle relaxation can release histamine, but it is less than tubocurine, and its characteristics are fast onset, high muscle relaxant effect.

Pharmacokinetics

After injection into the body tissue, this product quickly exerts pharmacological effects at the target site, can cross the placenta and enter the fetal circulation.

Clinical application

Cisatracurium bensulate is suitable for tracheal intubation, mechanical ventilation and various surgeries that require skeletal muscle relaxation. Atracurium, due to its long half-life and low Huffman elimination pathway dependence, makes it suitable for prolonged surgery and maintenance of muscle relaxation in intensive care patients.

Cisatracurium benzenesulfonate

Cis-atracurium is one of the 10 isomers of atracurium and accounts for about 15% of the total atracurium mixture. It is a benzyl isoquinoline non-depolarized muscle relaxant like the parent. The ED95 of cis-atracurium was 0.05mg/kg, and the titer of muscle relaxant was 3 ~ 5 times that of atracurium. Its lipid solubility is low, it is not directly hydrolyzed by plasma non-specific esterase, and 80% is inactivated by Hofmann degradation. There is no histamine release effect and the incidence of allergic reaction is low. Clinical data showed that there was no histamine release sign in healthy patients undergoing elective surgery after rapid intravenous infusion of 8×ED95 Chemicalbook with cis-atracurium. Atracurium 2×ED95 has histamine release effect. The effect on cardiovascular function is mild. The metabolites are few, the decomposition product of cis-atracurium n-methyltetrahydropapaverine is about 1/3 to 1/10 of the equivalent dose of atracurium, and long-term application will not cause convulsion due to high plasma concentration. It can be used for endotracheal intubation and maintenance of muscle relaxation during general anesthesia, especially for the anesthesia of patients with hepatic and renal insufficiency. This information was edited by Chemicalbook Xiaonan (2015-09-17).

Stability

Sealed, dark, 2 ~ 8℃ store, do not freeze. The original injection is light yellow to yellowish green and clear. Store at room temperature for 3 to 6 weeks. After opening and diluting, it should not be used again >24h.

Use

A non-depolarizing neuromuscular blocker.

Safety information

Dangerous Goods Mark :T

Danger category code :25-36

Safety note :45

Dangerous Goods Transport Code :UN 2811 6.1 / PGIII

WGK Germany:3

Customs Code :29145090

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