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Mivacurium | CAS No: 133814-19-4 | GMP-certified suppliers
A medication that facilitates tracheal intubation and provides skeletal muscle relaxation as an adjunct to general anesthesia during surgery or mechanical ventilation.
Therapeutic categories
Primary indications
- For inpatients and outpatients, as an adjunct to general anesthesia, to facilitate tracheal intubation and to provide skeletal muscle relaxation during surgery or mechanical ventilation
Product Snapshot
- Mivacurium is a parenteral injectable non-depolarizing neuromuscular blocking agent
- It is indicated for skeletal muscle relaxation during surgical procedures and mechanical ventilation
- The product is approved for use in the US and Canadian markets
Clinical Overview
Pharmacologically, mivacurium acts as a short-acting, nondepolarizing muscle relaxant. It exerts its effect by competitively binding to nicotinic cholinergic receptors located on the motor end-plate of the neuromuscular junction. This antagonism prevents acetylcholine from activating these receptors, thereby blocking neuromuscular transmission and inducing muscle relaxation. The neuromuscular blockade produced by mivacurium can be reversed with anticholinesterase agents such as neostigmine, which increase acetylcholine availability at the receptor site.
Mivacurium is hydrolyzed rapidly by plasma cholinesterase, a key factor contributing to its short duration of action. Because of this rapid metabolism, spontaneous recovery of neuromuscular function typically occurs quickly, and routine pharmacological reversal may not always provide additional clinical benefit. The depth of neuromuscular block at the time of reversal influences both recovery time and the required dose of reversal agents.
From a safety perspective, mivacurium may be associated with histamine release, which can result in transient hypotension or tachycardia. Monitoring for potential adverse effects during administration is advised, particularly in patients with altered plasma cholinesterase activity or sensitivity to neuromuscular blockers.
Mivacurium belongs chemically to the class of benzylisoquinolines, characterized by an isoquinoline core attached to benzyl groups. It is registered and approved for clinical use as a nondepolarizing neuromuscular-blocking agent.
For API procurement, it is important to ensure the substance meets strict purity criteria and is manufactured in compliance with Good Manufacturing Practices (GMP). Due to its metabolism by plasma cholinesterase, attention should be given to the compound's chemical stability and potential impurities that could affect safety or efficacy in final pharmaceutical formulations.
Identification & chemistry
| Generic name | Mivacurium |
|---|---|
| Molecule type | Small molecule |
| CAS | 133814-19-4 |
| UNII | 77D66S9Q93 |
| DrugBank ID | DB01226 |
Pharmacology
| Summary | Mivacurium is a short-acting, nondepolarizing neuromuscular blocking agent that competitively inhibits acetylcholine binding at nicotinic cholinergic receptors on the motor end-plate, blocking neuromuscular transmission. Its effects are rapidly reversed by acetylcholinesterase inhibitors due to its hydrolysis by plasma cholinesterase. Mivacurium facilitates skeletal muscle relaxation during surgical procedures and mechanical ventilation. |
|---|---|
| Mechanism of action | Mivacurium binds competitively to cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine, resulting in a block of neuromuscular transmission. This action is antagonized by acetylcholinesterase inhibitors, such as neostigmine. |
| Pharmacodynamics | Mivacurium is a short-acting, nondepolarizing skeletal neuromuscular blocking agent which is hydrolyzed by plasma cholinesterase. Mivacurium results in a blockade of neuromuscular transmission by binding competitively with cholinergic receptors on the motor end-plate to antagonize the action of acetylcholine. The neuromuscular block produced by mivacurium is readily antagonized by anticholinesterase agents. The deeper the level of neuromuscular block at reversal, the longer the time required for recovery of neuromuscular function and the greater the dose of anticholinesterase agent required. Because spontaneous recovery after mivacurium is rapid, routine reversal may not always result in a clinical benefit. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Neuronal acetylcholine receptor subunit alpha-2 | Humans | antagonist |
| Muscarinic acetylcholine receptor M2 | Humans | antagonist, partial agonist |
| Muscarinic acetylcholine receptor M3 | Humans | antagonist |
ADME / PK
| Half-life | The mean elimination half-life ranges from 1.7 to 2.6 minutes in healthy, young adults administered 0.1 to 0.25 mg/kg mivacurium. In 9 patients with end-stage liver disease undergoing liver transplant surgery, plasma clearance was approximately 50% lower than that in 8 control patients with normal hepatic function, while the elimination half-life increased to 4.4 minutes from the 1.8 minute control value. |
|---|---|
| Protein binding | The protein binding of mivacurium has not been determined due to its rapid hydrolysis by plasma cholinesterase. |
| Metabolism | Extensive and rapid via enzymatic hydrolysis catalyzed by plasma cholinesterase. Biotransformation may be significantly slowed in patients with abnormal or decreased plasma cholinesterase activity, especially individuals with a homozygous atypical cholinesterase gene abnormality. |
Formulation & handling
- Mivacurium is a small molecule injectable administered exclusively via intravenous or parenteral routes.
- It exhibits low water solubility despite being provided as an aqueous solution, requiring careful formulation to maintain stability.
- Handling should consider its liquid state and potential sensitivity to degradation, necessitating appropriate storage conditions to ensure potency.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) has patent protection recently expired in the US and Canada, allowing for generic competition and greater market availability. The product is transitioning into a mature market phase in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing landscape for Mivacurium includes several originator companies supplying branded products primarily in the US and Canadian markets. The presence of multiple brand samples suggests established branded formulations in these regions. Given the generic availability of Mivacurium Chloride, patent expiries have likely occurred, enabling existing generic competition. |
|---|
Safety
| Toxicity | Overdosage with neuromuscular blocking agents may result in neuromuscular block beyond the time needed for surgery and anesthesia. |
|---|
- Prolonged neuromuscular blockade may occur following overdosage
- Monitor and manage accordingly in clinical settings
- Avoid unintended exposure to minimize risks of extended muscle paralysis
Mivacurium 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.
Mivacurium API manufacturers & distributors
Compare qualified Mivacurium API suppliers worldwide. We currently have 2 companies offering Mivacurium API, with manufacturing taking place in 2 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 |
|---|---|---|---|---|---|
| Farmabios | Producer | Italy | Italy | CoA, ISO9001, USDMF | 58 products |
| Tianjin Pharmacn Medical ... | Producer | China | China | BSE/TSE, CoA, GMP, MSDS | 66 products |
When sending a request, specify which Mivacurium 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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