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Succinylcholine | CAS No: 306-40-1 | GMP-certified suppliers
A medication that provides rapid and short-term skeletal muscle relaxation to facilitate tracheal intubation and support surgical procedures under general anesthesia.
Therapeutic categories
Primary indications
- Succinylcholine is indicated as an adjunct to general anesthesia, to facilitate tracheal intubation, and to provide skeletal muscle relaxation during surgery or mechanical ventilation
Product Snapshot
- Succinylcholine is a parenteral injectable small molecule available in solution and powder forms for solution
- It is primarily used as a neuromuscular blocking agent to facilitate tracheal intubation and provide skeletal muscle relaxation during surgery or mechanical ventilation
- Succinylcholine is approved for use in the US and Canadian markets
Clinical Overview
Therapeutically, succinylcholine is indicated as an adjunct to general anesthesia to assist with tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation. Pharmacodynamically, it acts by binding postsynaptic cholinergic receptors at the motor endplate, causing sustained depolarization of the muscle membrane. This leads first to transient fasciculations followed by flaccid paralysis. The paralysis occurs in a progressive manner, initially affecting facial muscles and the glottis, then extending to intercostal muscles, diaphragm, and other skeletal muscles. Succinylcholine does not affect cardiac or smooth muscles directly nor does it act on presynaptic or ganglionic acetylcholine receptors. Notably, it has no effect on consciousness or nociception, necessitating concomitant administration of adequate anesthesia.
Key safety concerns include rare but severe risks of acute rhabdomyolysis with hyperkalemia, especially in pediatric patients with underlying, often undiagnosed, skeletal myopathies such as Duchenne’s muscular dystrophy. These events can precipitate life-threatening arrhythmias and cardiac arrest. For this reason, succinylcholine use in children should be limited to emergency settings when no suitable alternatives are available. Vigilant monitoring and prompt treatment of hyperkalemia are critical if adverse events occur.
Pharmacokinetic data highlight rapid hydrolysis by plasma butyrylcholinesterase, resulting in a brief duration of action. Clinicians should consider variability in enzyme activity that may prolong drug effect.
For API procurement and quality assurance, succinylcholine should meet stringent purity standards owing to its potent neuromuscular effects and narrow therapeutic window. Sourcing from manufacturers with robust quality management systems and validated analytic methods is essential to ensure consistent pharmacological performance and safety profiles. Regulatory compliance with relevant pharmacopeial monographs is also recommended for global distribution.
Identification & chemistry
| Generic name | Succinylcholine |
|---|---|
| Molecule type | Small molecule |
| CAS | 306-40-1 |
| UNII | J2R869A8YF |
| DrugBank ID | DB00202 |
Pharmacology
| Summary | Succinylcholine is a depolarizing neuromuscular blocker that binds to post-synaptic nicotinic acetylcholine receptors at the motor endplate, causing sustained membrane depolarization and subsequent skeletal muscle paralysis. Its pharmacodynamic effect includes rapid onset of muscle relaxation primarily affecting skeletal muscles without direct impact on smooth or cardiac muscle. Succinylcholine's action facilitates tracheal intubation and muscle relaxation during surgical procedures or mechanical ventilation. |
|---|---|
| Mechanism of action | Succinylcholine is a depolarizing neuromuscular blocker, meaning it causes a prolonged period of membrane depolarization in order to exert its therapeutic effects. It binds to the post-synaptic cholinergic receptors found on motor endplates, thereby inducing first transient fasciculations followed by skeletal muscle paralysis. |
| Pharmacodynamics | Succinylcholine's neuromuscular blockade takes effect within 60 seconds of intravenous administration and lasts between four to six minutes. Similar to acetylcholine, it binds to cholinergic receptors of the motor endplate to induce membrane depolarization and, eventually, muscle paralysis, which may be maintained for as long as an adequate concentration of succinylcholine remains at the receptor site. Succinylcholine has no direct action on smooth or cardiac muscle, nor does it appear to act on pre-synaptic or ganglionic acetylcholine receptors. The paralysis induced by succinylcholine has been described as "progressive", first involving the muscles of the face and glottis, then the intercostals and diaphragm, then followed by other skeletal muscles. Succinylcholine has no effect on consciousness or pain threshold, and must therefore be used in conjunction with adequate anesthesia. There have been rare reports of the development of acute rhabdomyolysis with hyperkalemia - resulting in ventricular dysrhythmias, cardiac arrest, and death - after the intravenous administration of succinylcholine to apparently healthy pediatric patients who were subsequently found to have undiagnosed skeletal myopathy (most frequently Duchenne's muscular dystrophy). Infants or children experiencing seemingly idiopathic cardiac arrest soon after the administration of succinylcholine should therefore be treated immediately for hyperkalemia. Given that patients may not present with any apparent risk factors, the use of succinylcholine in pediatric patients should be restricted to emergency intubation or other situations in which a suitable alternative is unavailable. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Neuronal Acetylcholine (nACh) Receptor Subunits | Humans | agonist |
| Muscarinic acetylcholine receptor M2 | Humans | agonist |
| Muscarinic acetylcholine receptor M3 | Humans | agonist |
ADME / PK
| Half-life | The mean half-life of elimination following intravenous administration is 47 seconds. |
|---|---|
| Metabolism | Succinylcholine is rapidly metabolized by plasma cholinesterase in the bloodstream to succinylmonocholine, which is then further hydrolyzed (albeit more slowly) to succinic acid and choline. |
| Route of elimination | Approximately 10% of an administered dose is excreted unchanged in the urine. |
| Volume of distribution | At intravenous doses of 1 mg/kg and 2 mg/kg in 14 patients, the mean apparent volumes of distribution were 16.4 ± 14.7 and 5.6 ± 6.8 mL/kg, respectively. |
| Clearance | The mean _in vivo_ plasma clearance of succinylcholine following an intravenous dose of 1 mg/kg in 18 patients was approximately 4.17 ± 2.37 L/min. |
Formulation & handling
- Succinylcholine is a small molecule API primarily formulated for parenteral administration via intravenous or intramuscular injection. Its low water solubility and highly polar nature require preparation as aqueous injection solutions or powders for reconstitution. Stability considerations include protection from prolonged exposure to aqueous environments before use, as hydrolysis may occur.
Regulatory status
| Lifecycle | The API is currently marketed in the US and Canada, with key patents having expired, leading to the availability of generic versions and increased market competition. The lifecycle is in the mature phase with established usage across these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The succinylcholine supply landscape involves multiple originator manufacturers, including Sandoz Canada Inc., Hospira Inc., and Organon USA Inc., with several packagers supporting distribution. Branded products, primarily marketed under the name Anectine, have a presence mainly in the US and Canadian markets. Given the established presence of multiple manufacturers and lack of recent patent activity, generic competition appears to be existing or well-established in these regions. |
|---|
Safety
| Toxicity | Overdosage of succinylcholine is likely to extend the neuromuscular blockade beyond the time needed for surgery. Symptoms are likely to be consistent with its therapeutic effects, although more pronounced, and may therefore include skeletal muscle weakness, decreased respiratory reserve, low tidal volume, or apnea. Treatment of succinylcholine overdose involves airway and respiratory support until recovery of normal respiration is assured. Depending on the extent of the overdose, the characteristic depolarizing (i.e. Phase I) neuromuscular blockade may switch to resemble more closely a non-depolarizing (i.e. Phase II) neuromuscular blockade. This occurs primarily when succinylcholine is given over a prolonged period of time or with particularly large doses, and may result in significant respiratory muscle paralysis or weakness. |
|---|
- Succinylcholine overdosage may prolong neuromuscular blockade, resulting in extended skeletal muscle paralysis and respiratory compromise
- Prolonged or high-dose administration can induce a Phase II neuromuscular blockade phenotype, resembling non-depolarizing blockade with significant muscle weakness
- Handling requires precautions to prevent inadvertent overdose and ensure appropriate airway and respiratory support measures are available
Succinylcholine 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.
Succinylcholine API manufacturers & distributors
Compare qualified Succinylcholine API suppliers worldwide. We currently have 7 companies offering Succinylcholine API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Global Pharma Tek | Distributor | India | India | BSE/TSE, CoA, FDA, GMP, ISO9001, MSDS | 484 products |
| Harman Finochem | Producer | India | India | CoA, USDMF | 34 products |
| Mac Chem Products | Producer | India | India | CEP, CoA, FDA, GMP, USDMF, WC | 25 products |
| Minakem | Producer | France | France | CoA, FDA, GMP, USDMF | 31 products |
| SEDANAH | Distributor | Jordan | World | CoA, GMP | 70 products |
| Sequent Scientific | Producer | India | India | CEP, CoA, FDA, WC | 8 products |
| Zydus Takeda Healthcare | Producer | India | India | CoA, WC | 7 products |
When sending a request, specify which Succinylcholine API quality you need: for example EP (Ph. Eur.), USP, JP, BP, or another pharmacopoeial standard, as well as the required grade (base, salt, micronised, specific purity, etc.).
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