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Last modified
11/08/2018 - 09:13

Cisatracurium besylate

Product Details

Name Cisatracurium besylate
Alias Nimbex
CAS  No. 96946-42-8
Formula C65H82N2O18S2
Weight 1,243.49 g/mol
Usage Pharmaceuticals
Appearance White powder

Product Description

Cisatracurium besylate is a bisbenzyltetrahydroisoquinolinium that has effect as a neuromuscular-blocking drug or skeletal muscle relaxant in the category of non-depolarizing neuromuscular-blocking drugs, used adjunctively in anaesthesia to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. 

Cisatracurium besylate is the latest generation muscle relaxants, cis-benzene sulfonamide atracurium mainly used in general anesthesia, and can be widely used in endotracheal intubation, liver and kidney dysfunction, cardiovascular surgery and elderly and pediatric patients. This product has the characteristics of not liver kidney metabolism by and cardiovascular stability, muscle relaxant effect three times stronger than atracurium effect, no cardiovascular side effects. Shun benzene sulfonic atracurium is mainly used with systemic anaesthesia and can be widely used in endotracheal intubation, liver and kidney dysfunction, cardiovascular surgery and elderly and pediatric patients.

It shows the intermediate duration of action. Cisatracurium is one of the ten isomers of the parent molecule, atracurium. Moreover, cisatracurium represents approximately 15% of the atracurium mixture.

After the drug in Britain for the first time in 1996, overseas has gradually instead of vecuronium bromide and atracurium, become the mainstream of clinical and muscle relaxants.

Function

Cisatracurium besylate is the benzenesulfonate salt form of atracurium. It is a kind of artificially synthetic non-depolarizing muscle relaxants with its role similar as tubocurarine. It has an onset time of 1 minute and duration time of 15 minutes. The treatment dose does not affect the heart, liver and kidney function. It also has no accumulation property. It also can induce the release of histamine when used at large doses.

Cisatracurium Besylate binds to the nicotinic acetycholine (cholinergic) receptors in the motor endplate and blocks access to the receptors. In the process of binding, the receptor is actually activated - causing a process known as depolarization. Since it is not degraded in the neuromuscular junction, the depolarized membrane remains depolarized and unresponsive to any other impulse, causing muscle paralysis.

For muscle relaxation or breathing control required in surgery, compared with current clinical major muscle-relaxing anaesthetic drugs, cisatracurium besylate is not metabolized through liver or kidney, and has cardiovascular stability; its effect of muscle relaxation is 3 times as strong as atracurium without any cardiovascular side effects. Cisatracurium besylate is mainly applied to general anaesthesia and can be widely used in intubation, treating liver and kidney dysfunction, used in cardiovascular surgery and elderly and pediatric patients. 

Compared with atracurium, this product has no dose-dependent adverse effects of histamine release; however, the disadvantage is that patients with liver and kidney dysfunction should administrate with caution. 

In vitro studies using human plasma indicated that cisatracurium spontaneously degrades at physiological pH via Hofmann elimination to yield laudanosine and the quaternary monoacrylate. Subsequent ester hydrolysis of the monoacrylate generates the monoquaternary alcohol, although the rate-limiting step is Hofmann elimination.

 As is evident with the parent molecule, atracurium, cisatracurium is also susceptible to degradation by Hofmann elimination and ester hydrolysis as components of the in vivo metabolic processes. Because Hofmann elimination is a temperature- and plasma pH-dependent process, cisatracurium's rate of degradation in vivo is highly influenced by body pH and temperature just as it is with the parent molecule, atracurium: thus, an increase in body pH favours the elimination process, whereas a decrease in temperature slows down the process. 

One of the metabolites of cisatracurium via Hofmann elimination is laudanosine – see the atracurium page for further discussion of the issue regarding this metabolite. 80% of cisatracurium is metabolized eventually to laudanosine and 20% is metabolized hepatically or excreted really. 10-15% of the dose is excreted unchanged in the urine. Since Hofmann elimination is an organ-independent chemodegradative mechanism, there is little or no risk to the use of cisatracurium in patients with liver or renal disease when compared with other neuromuscular blocking agents. The two reverse ester linkages in the bridge between the two isoquinolinium groups make atracurium and cisatracurium poor targets for plasma cholinesterase, unlike mivacurium which has two conventional ester linkages.

A recent study showed that cisatracurium pretreatment effectively decreases the incidence and severity of pain induced by propofol general anaesthesia.

Application

Cisatracurium besylate is generally used for maintaining muscle relaxing or facilitating the mechanical respiration; Since 1996 for the first time when this drug has entered into the market in the UK, foreign countries have gradually applied it to replace vecuronium and atracurium as the mainstream of clinical muscle relaxants.

Cisatracurium besylate is about 3 times more potent than the mixture of atracurium isomers as a neuromuscular blocking agent and is used as a muscle relaxant for endotracheal intubation, to aid controlled ventilation, and in general anaesthesia.

As with other nondepolarizing neuromuscular blocking agents, the more profound the neuromuscular block at the time of reversal, the longer the time required for recovery of neuromuscular function. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action.

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