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Atracurium besylate | CAS No: 64228-81-5 | GMP-certified suppliers
A medication that supports general anesthesia by enabling endotracheal intubation and providing reliable skeletal muscle relaxation during surgical procedures or mechanical ventilation in critical care settings.
Therapeutic categories
Primary indications
- For use, as an adjunct to general anesthesia, to facilitate endotracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation
Product Snapshot
- Atracurium besylate is supplied as a parenteral injectable solution
- It is used as a neuromuscular blocking agent adjunct to general anesthesia for intubation and surgical or ventilatory muscle relaxation
- It is approved in the US and Canada
Clinical Overview
Pharmacologically, atracurium acts as a peripheral neuromuscular blocker that reduces skeletal muscle contractility without affecting consciousness or pain perception. The clinical effect is typically monitored using peripheral nerve stimulation to guide dosing and maintain an appropriate depth of neuromuscular block. Its duration of action is shorter than that of agents such as d‑tubocurarine, metocurine, and pancuronium when compared at equipotent doses. Increases in dose shorten onset time and extend the duration of maximal effect. When repeat maintenance doses are administered after recovery has begun, no cumulative prolongation of neuromuscular block is observed.
The mechanism of action involves competitive antagonism of acetylcholine at nicotinic receptors on the motor end plate. This prevents depolarization and subsequent muscle contraction. The blockade can be reversed with acetylcholinesterase inhibitors such as neostigmine, edrophonium, or pyridostigmine, which increase synaptic acetylcholine concentrations and competitively displace the neuromuscular blocker.
Key pharmacokinetic features include in vivo degradation through Hofmann elimination and ester hydrolysis, processes that are largely independent of renal or hepatic function. These pathways contribute to predictable offset even in patients with organ impairment. Atracurium’s metabolites are generally considered less active, although some may be associated with histamine release at higher doses.
Safety considerations include potential histamine-mediated reactions, such as hypotension or flushing, particularly with rapid administration. Careful titration and monitoring are standard practice to mitigate these risks.
For API procurement, sourcing should prioritize manufacturers with demonstrated control of stereochemistry, impurity profiles, and stability, given the compound’s susceptibility to degradation and the need for consistent neuromuscular blocking performance.
Identification & chemistry
| Generic name | Atracurium besylate |
|---|---|
| Molecule type | Small molecule |
| CAS | 64228-81-5 |
| UNII | 40AX66P76P |
| DrugBank ID | DB00732 |
Pharmacology
| Summary | Atracurium is a nondepolarizing neuromuscular blocker that competitively inhibits acetylcholine at nicotinic receptors on the motor end‑plate, producing reversible skeletal muscle paralysis. Its pharmacologic effect is characterized by dose‑dependent onset and duration of neuromuscular block without cumulative activity during repeated administration. The drug is used as an adjunct to general anesthesia to facilitate intubation and maintain muscle relaxation during surgical procedures or mechanical ventilation. |
|---|---|
| Mechanism of action | Atracurium antagonizes the neurotransmitter action of acetylcholine by binding competitively with cholinergic receptor sites on the motor end-plate. This antagonism is inhibited, and neuromuscular block reversed, by acetylcholinesterase inhibitors such as neostigmine, edrophonium, and pyridostigmine. |
| Pharmacodynamics | Atracurium is a nondepolarizing skeletal muscle relaxant. Atracurium can be used most advantageously if muscle twitch response to peripheral nerve stimulation is monitored to assess degree of muscle relaxation. The duration of neuromuscular block produced by Atracurium is approximately one third to one half the duration of block by d-tubocurarine, metocurine, and pancuronium at initially equipotent doses. As with other nondepolarizing neuromuscular blockers, the time to onset of paralysis decreases and the duration of maximum effect increases with increasing doses of Atracurium. Repeated administration of maintenance doses of Atracurium has no cumulative effect on the duration of neuromuscular block if recovery is allowed to begin prior to repeat dosing. Moreover, the time needed to recover from repeat doses does not change with additional doses. Repeat doses can therefore be administered at relatively regular intervals with predictable results. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-2 | Humans | antagonist |
ADME / PK
| Half-life | The elimination half-life is approximately 20 minutes. |
|---|
Formulation & handling
- Formulated exclusively for parenteral use; oral listings are not relevant given its quaternary ammonium structure and negligible oral bioavailability.
- Requires aqueous solution as the besylate salt due to very low intrinsic solubility of the base.
- Temperature‑ and pH‑sensitive (Hofmann degradation), necessitating controlled storage and avoidance of alkaline conditions during handling and compounding.
Regulatory status
| Lifecycle | Patent‑expiry information was not provided, so the product’s lifecycle status cannot be precisely characterized. In Canada and the US, market maturity will depend on the remaining patent or exclusivity period, with generic entry expected once those protections lapse. |
|---|
| Markets | Canada, US |
|---|
Supply Chain
| Supply chain summary | Atracurium besylate is supplied by a limited number of originator and packager entities, with Baxter identified among the primary manufacturers for North American markets. Branded and injectable presentations are established in the US and Canada, indicating mature market availability. Patent protection for atracurium besylate has long expired, supporting the presence of existing generic competition. |
|---|
Safety
| Toxicity | Excessive doses can be expected to produce enhanced pharmacological effects. Overdosage may increase the risk of histamine release and cardiovascular effects, especially hypotension. |
|---|
- High concentrations may intensify pharmacodynamic activity, including potentiation of neuromuscular blockade
- Overexposure is associated with histamine-mediated reactions and cardiovascular instability, with hypotension as the primary concern
- Handle with controls that minimize aerosolization or accidental exposure to reduce risk of systemic pharmacologic effects
Atracurium besylate is a type of Muscle relaxants
Muscle relaxants are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) commonly used to alleviate muscle spasms and promote muscle relaxation. These medications act on the central nervous system (CNS) or directly on muscle fibers to reduce muscle tone and tension.
Muscle relaxants can be classified into two main groups: spasmolytics and neuromuscular blockers. Spasmolytics primarily target the CNS to inhibit the transmission of nerve signals, thus reducing muscle spasms. They are often prescribed for conditions such as back pain, muscle strains, and spasms caused by neurological disorders.
Neuromuscular blockers, on the other hand, act at the neuromuscular junction to prevent the transmission of nerve impulses, resulting in temporary paralysis of skeletal muscles. These medications are primarily used during surgical procedures to induce muscle relaxation and facilitate intubation.
Commonly prescribed muscle relaxants include benzodiazepines, such as diazepam and lorazepam, which have sedative properties and can provide relief from muscle spasms. Another class of muscle relaxants is the centrally acting skeletal muscle relaxants, including carisoprodol and cyclobenzaprine, which work by affecting neurotransmitters in the CNS.
It is important to note that muscle relaxants can cause side effects such as drowsiness, dizziness, and impaired coordination. They should only be used under the guidance of a healthcare professional, and the dosage and duration of treatment should be strictly followed to avoid dependence or other complications.
In conclusion, muscle relaxants are pharmaceutical APIs used to alleviate muscle spasms and promote muscle relaxation. They are available in different forms and can target the CNS or directly act on muscle fibers. It is crucial to consult a healthcare professional for proper diagnosis, prescription, and monitoring when using muscle relaxants.
Atracurium besylate (Muscle relaxants), classified under Skeletal muscle relaxants
Skeletal muscle relaxants are a category of pharmaceutical active pharmaceutical ingredients (APIs) that are commonly used in the treatment of musculoskeletal conditions characterized by muscle spasms, stiffness, or tension. These medications work by targeting the central nervous system to reduce muscle activity and promote relaxation.
Skeletal muscle relaxants act on various receptors in the central nervous system, such as gamma-aminobutyric acid (GABA) receptors, to inhibit the transmission of nerve impulses and decrease muscle tone. This results in a reduction in muscle spasms, pain relief, and improved mobility.
There are different classes of skeletal muscle relaxants, including benzodiazepines, antispasmodics, and centrally acting muscle relaxants. Benzodiazepines, such as diazepam and lorazepam, exert their muscle relaxant effects by enhancing the activity of GABA receptors. Antispasmodics like cyclobenzaprine work by inhibiting the release of certain neurotransmitters involved in muscle contractions. Centrally acting muscle relaxants, such as baclofen and tizanidine, directly target the spinal cord to reduce muscle hyperactivity.
Skeletal muscle relaxants are commonly prescribed for conditions like muscle spasms, back pain, fibromyalgia, and multiple sclerosis. However, they are typically used for short-term treatment due to their potential side effects, including drowsiness, dizziness, and sedation.
It is important to note that skeletal muscle relaxants should only be used under the supervision and prescription of a qualified healthcare professional. Proper dosage and duration of treatment should be determined based on the patient's condition and medical history to ensure safe and effective use of these medications.
Atracurium besylate API manufacturers & distributors
Compare qualified Atracurium besylate API suppliers worldwide. We currently have 4 companies offering Atracurium besylate 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 |
|---|---|---|---|---|---|
| Alkaloids Corporation | Producer | India | India | CoA, ISO9001 | 11 products |
| CF Pharma | Producer | Hungary | Hungary | CoA, GMP | 7 products |
| Shandong Boyuan | Producer | China | China | BSE/TSE, CoA, MSDS | 55 products |
| Sinoway industrial Co.,Lt... | Distributor | China | China | CoA, ISO9001 | 757 products |
When sending a request, specify which Atracurium besylate 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.).
Use the list above to find high-quality Atracurium besylate API suppliers. For example, you can select GMP, FDA or ISO certified suppliers. Visit our help page to learn more about sourcing APIs via Pharmaoffer.
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