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Cisatracurium | CAS No: 96946-41-7 | GMP-certified suppliers
A medication that facilitates tracheal intubation and provides skeletal muscle relaxation during surgery and mechanical ventilation in adult and pediatric patients.
Therapeutic categories
Primary indications
- Cisatracurium is indicated as an adjunct to general anesthesia to facilitate tracheal intubation in adults and pediatric patients 1 month to 12 years of age
- Cisatracurium is also indicated to provide skeletal muscle relaxation during surgery in adults and pediatric patients 2 to 12 years of age as a bolus or infusion maintenance and for mechanical ventilation in the ICU in adults
Product Snapshot
- Cisatracurium is formulated as an injectable solution for intravenous administration
- It is primarily used to facilitate tracheal intubation and provide skeletal muscle relaxation during surgery and mechanical ventilation in ICU settings
- Cisatracurium is approved for use in the US and Canada, with both approved and investigational statuses noted
Clinical Overview
Clinically, cisatracurium is utilized as an adjunct in general anesthesia to facilitate tracheal intubation in adults and pediatric patients aged one month to twelve years. It also provides skeletal muscle relaxation during surgery in adults and children aged two to twelve years, administered either as a bolus or continuous infusion. Additionally, it is employed for skeletal muscle relaxation during mechanical ventilation in intensive care settings in adults.
Pharmacodynamically, cisatracurium produces a dose-dependent neuromuscular blockade by competitively binding to nicotinic cholinergic receptors at the motor end-plates of skeletal muscle, inhibiting acetylcholine-mediated depolarization. This blockade prevents generation of end-plate potentials and consequent muscle contraction. The agent’s onset and duration of action are intermediate relative to other neuromuscular blockers, with an ED95 of approximately 0.05 mg/kg in adults under opioid/nitrous oxide/oxygen anesthesia. Reversal of cisatracurium-induced blockade is achieved via acetylcholinesterase inhibitors such as neostigmine.
Absorption, distribution, metabolism, and excretion (ADME) parameters are notable for cisatracurium’s organ-independent metabolism through Hofmann elimination, a plasma chemical process that does not rely on hepatic or renal function, rendering it advantageous in patients with organ impairment.
Safety considerations include the potential for residual neuromuscular blockade and an elevated risk of seizures, particularly with medication errors or concurrent administration of other potentiating drugs. The risk of histamine-mediated side effects is lower compared to atracurium.
Widely used in critical care and surgical anesthesia worldwide, cisatracurium is marketed under several brand names depending on the region and regulatory approval. It is classified within multiple therapeutic categories, including muscle relaxants and nicotinic receptor antagonists.
For API sourcing, quality control should emphasize the consistent stereochemical purity given the specific isomeric requirement, compliance with regulatory standards, and verification of impurities related to synthesis or degradation. Reliable supply chains are critical due to cisatracurium’s narrow therapeutic index and application in critical care settings.
Identification & chemistry
| Generic name | Cisatracurium |
|---|---|
| Molecule type | Small molecule |
| CAS | 96946-41-7 |
| UNII | QX62KLI41N |
| DrugBank ID | DB00565 |
Pharmacology
| Summary | Cisatracurium is a non-depolarizing neuromuscular blocking agent that competitively inhibits acetylcholine binding at nicotinic receptors in the motor end-plate, preventing neuromuscular transmission. This results in skeletal muscle relaxation by blocking ion channel activation and subsequent muscle cell depolarization. The drug's pharmacodynamics exhibit dose-dependent onset and duration of neuromuscular blockade, with activity reversible by acetylcholinesterase inhibitors. |
|---|---|
| Mechanism of action | Like other non-depolarising neuromuscular blocking agents, cisatracurium binds competitively to cholinergic receptors in motor end-plate neurons, blocking acetylcholine from accessing the receptors. Therefore, in the presence of cisatracurium, an end-plate potential cannot be developed. Ion channels remain closed, the cell does not depolarize, and an action potential is not transmitted. |
| Pharmacodynamics | The dose required to produce 95% suppression of twitch response to nerve stimulation (ED<sub>95</sub>) of cisatracurium is 0.05 mg/kg in adults receiving opioid/nitrous oxide/oxygen anesthesia. The degree and duration of the neuromuscular block produced by cisatracurium increases in a dose-dependent manner, while the time to maximum neuromuscular block decreases. Compared to other neuromuscular blocking agents, it is intermediate in its onset and duration of action. Cisatracurium acts on cholinergic receptors, blocking neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors such as neostigmine. The use of cisatracurium may lead to residual paralysis, as well as a higher risk of seizure. Medication errors increase the risk of death, and the use of certain drugs may potentiate the neuromuscular blocking action of cisatracurium. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Neuronal Acetylcholine (nACh) Receptor Subunits | Humans | antagonist |
| Acetylcholine receptor subunit alpha | Humans | antagonist |
| Muscarinic acetylcholine receptor M2 | Humans | antagonist |
ADME / PK
| Absorption | The pharmacokinetics of cisatracurium follow a two-compartment open model. Cisatracurium is metabolized into laudanosine and monoquaternary alcohol metabolite (MQA). Following the IV infusion of cisatracurium, the C<sub>max</sub> of laudanosine and MQA were 6% and 11% of the parent compound, respectively. Compared to young patients, the volume of distribution of cisatracurium is slightly larger in elderly patients, which also leads to longer half-life values. The plasma clearance of cisatracurium was not affected by age. Patients with hepatic impairment have a slightly higher volume of distribution and plasma clearance values; however, these minor pharmacokinetic differences are not considered clinically significant. Additionally, the pharmacokinetic parameters of cisatracurium in patients with end-stage renal disease were similar to those detected in healthy adult patients. |
|---|---|
| Half-life | Cisatracurium has an elimination half-life of 22 minutes. |
| Protein binding | The binding of cisatracurium to plasma proteins has not been successfully studied due to its rapid degradation at physiologic pH. |
| Metabolism | The degradation of cisatracurium is largely independent of liver metabolism. Cisatracurium undergoes Hofmann elimination (a pH and temperature-dependent chemical process) to form laudanosine and the monoquaternary acrylate metabolite. Non-specific plasma esterases hydrolyze the monoquaternary acrylate metabolite to form the monoquaternary alcohol metabolite (MQA). The MQA can also undergo Hofmann elimination, but the rate of this process is slower than the one detected for cisatracurium. Laudanosine is further metabolized to desmethyl metabolites that are conjugated with glucuronic acid and excreted in the urine. Laudanosine may cause transient hypotension and, in higher doses, cerebral excitatory effects when administered to several animal species; however, the effects of laudanosine in humans have not been established. |
| Route of elimination | The predominant elimination mechanism of cisatracurium is Hofmann elimination, a chemical process dependent on pH and temperature (approximately 80% in healthy surgical patients). The liver and kidney play a minor role in the elimination of cisatracurium (about 20%); however, they have a significant role in the metabolism of cisatracurium metabolites. In healthy male patients (n=6) given <sup>14</sup>C-cisatracurium, 4% of the recovered dose was found in feces, and 95% was found in urine, mostly as conjugated metabolites. Less than 10% of the cisatracurium dose was excreted as the unchanged patent drug. In another group of patients with Foley catheters for surgical management given non-radiolabeled cisatracurium (n=12), 15% of the cisatracurium dose was excreted unchanged in urine. |
| Volume of distribution | Cisatracurium has a volume of distribution at steady state of 145 mL/kg. The volume of distribution of cisatracurium besylate is small due to its relatively large molecular weight and high polarity. |
| Clearance | Cisatracurium has a plasma clearance of 4.57 mL/min/kg. |
Formulation & handling
- Cisatracurium is a small molecule drug primarily formulated for parenteral administration via intravenous routes.
- Due to its low water solubility and high molecular weight, formulations typically use injection solutions for direct systemic delivery.
- Handling should ensure protection from moisture and avoid prolonged exposure to aqueous environments to maintain stability.
Regulatory status
| Lifecycle | The API's key patents expired in the United States in September 2012 and in Canada in July 2011, indicating that the product is in a mature market phase with generic competition in both the US and Canadian markets. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for cisatracurium includes multiple originator companies involved in both production and packaging, reflecting a diversified supply chain. Branded products are primarily marketed in the US and Canada, with several established manufacturers active in these regions. Given that key patents have expired or are near expiration, there is an existing presence of generic competition in the market. |
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Safety
| Toxicity | Overdosage with neuromuscular blocking agents such as cisatracurium may result in neuromuscular block beyond the time needed for surgery and anesthesia. Maintenance of a patent airway and controlled ventilation until recovery of normal neuromuscular function is the primary treatment for overdose cases. To facilitate further recovery, a cholinesterase inhibitor in conjunction with an appropriate cholinergic inhibitor may be administered once recovery from the neuromuscular block begins. If complete neuromuscular blockade is evident or suspected, cholinesterase inhibitors should not be administered. The reversal of paralysis may not be sufficient to maintain a patent airway and an appropriate level of spontaneous ventilation. The long-term carcinogenicity of cisatracurium has not been evaluated. In an _in vitro_ mouse lymphoma forward gene mutation assay, cisatracurium besylate led to mutations in the presence and absence of exogenous metabolic activation. Other assays did not show evidence of mutagenicity or clastogenicity. |
|---|
- Overdosage may cause prolonged neuromuscular blockade
- Supportive respiratory management is critical until neuromuscular function recovers
- Cholinesterase inhibitors are contraindicated if complete neuromuscular blockade is present or suspected due to risk of inadequate airway maintenance
Cisatracurium besylate is a type of Neuromuscular blocking agents
Neuromuscular blocking agents (NMBAs) belong to a vital category of pharmaceutical active pharmaceutical ingredients (APIs) used in the field of medicine. These agents play a crucial role in the neuromuscular blockade, a pharmacological state that inhibits the transmission of nerve impulses at the neuromuscular junction. By doing so, NMBAs induce temporary paralysis in skeletal muscles, making them indispensable in various medical procedures and surgical interventions.
NMBAs work by targeting the neuromuscular junction, where motor neurons communicate with skeletal muscle fibers. They achieve this by interfering with the transmission of acetylcholine, a neurotransmitter responsible for signaling muscle contraction. By blocking the action of acetylcholine, NMBAs prevent muscle movement and promote muscle relaxation, allowing surgeons to perform intricate procedures more effectively.
These pharmaceutical APIs are extensively used during surgeries requiring muscle relaxation, such as abdominal surgeries, orthopedic procedures, and endotracheal intubation. Furthermore, NMBAs find application in critical care settings, assisting in mechanical ventilation and facilitating optimal patient-ventilator synchronization.
It is worth mentioning that the usage of NMBAs necessitates close monitoring and expertise, as their administration requires precise dosing and careful titration to maintain the desired level of muscle relaxation while avoiding excessive paralysis. Anesthesia professionals and intensivists meticulously administer these agents, taking into consideration factors such as patient age, weight, and individual response.
In conclusion, Neuromuscular blocking agents are an essential API category within the pharmaceutical industry, vital for achieving muscle relaxation during surgical procedures and critical care management. Their precise and skillful utilization significantly contributes to the success of medical interventions and patient outcomes.
Cisatracurium besylate API manufacturers & distributors
Compare qualified Cisatracurium besylate API suppliers worldwide. We currently have 8 companies offering Cisatracurium besylate API, with manufacturing taking place in 4 different countries. Use the table below to review supplier type, countries of origin, certifications, product portfolio and GMP audit availability.
| Supplier | Type | Country | Product origin | Certifications | Portfolio |
|---|---|---|---|---|---|
| Aesica Queenborough | Producer | United Kingdom | United Kingdom | CoA, GMP | 4 products |
| CF Pharma | Producer | Hungary | Hungary | CoA, GMP, USDMF | 7 products |
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 55 products |
| Shaoxing Hantai Pharma | Distributor | China | China | CoA | 162 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001 | 764 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | CoA, GMP | 66 products |
| Utopharm (Shanghai) Compa... | Producer | China | China | CoA | 12 products |
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