Filters
Custom request?
Type
Production region
Qualifications
Country of origin
Esmolol API Manufacturers & Suppliers
6 verified results
Commercial-scale Suppliers
Employees: 550+
All certificates
Employees: >600
All certificates
Employees: 19
All certificates
Employees: 700+
All certificates
All certificates
All certificates
Total market transparency
Supplier trade data access
Buyer / supplier flow comparison
Esmolol | CAS No: 81147-92-4 | GMP-certified suppliers
A medication that provides rapid, short‑term control of ventricular rate in atrial fibrillation, atrial flutter, or acute sinus tachycardia in perioperative and emergent settings.
Therapeutic categories
Primary indications
- For the rapid control of ventricular rate in patients with atrial fibrillation or atrial flutter in perioperative, postoperative, or other emergent circumstances where short term control of ventricular rate with a short-acting agent is desirable
- Also used in noncompensatory sinus tachycardia where the rapid heart rate requires specific intervention
Product Snapshot
- Esmolol is an intravenous injectable small‑molecule beta‑blocker supplied mainly as solutions or concentrates for parenteral use
- It is used for short‑term ventricular rate control in atrial fibrillation or flutter and for managing noncompensatory sinus tachycardia in acute settings
- It has been marketed in the US and Canada with approvals in these regions, though some presentations have been withdrawn
Clinical Overview
Esmolol produces dose‑dependent beta‑1 blockade in cardiac tissue, attenuating the chronotropic and inotropic effects of endogenous catecholamines. By competitively inhibiting epinephrine and norepinephrine at beta‑1 receptors, it reduces sinoatrial node automaticity and slows atrioventricular nodal conduction. At therapeutic exposures it demonstrates minimal beta‑2 blockade and lacks intrinsic sympathomimetic or membrane‑stabilizing activity. Its antiarrhythmic properties align with Class II agents in the Vaughan Williams system.
The pharmacokinetic profile is characterized by rapid onset and very short duration. Esmolol is rapidly hydrolyzed by circulating esterases to an inactive metabolite, resulting in a brief elimination half‑life and permitting fine titration during continuous infusion. Distribution is largely confined to extracellular fluid, with limited potential for accumulation. Metabolites and unchanged drug are eliminated primarily via renal pathways.
Safety considerations include risk of hypotension, bradycardia, heart block, and potential exacerbation of heart failure in susceptible patients. Beta‑blockade may mask hypoglycemia symptoms. Caution is warranted in bronchospastic disease at higher doses where cardioselectivity may diminish. Abrupt withdrawal should be avoided in patients with underlying ischemic heart disease.
For API procurement, sourcing should ensure control of stereochemistry, residual solvents, and impurity profiles appropriate for parenteral use. Suppliers should provide full regulatory documentation, established stability data, and evidence of compliance with current good manufacturing practices.
Identification & chemistry
| Generic name | Esmolol |
|---|---|
| Molecule type | Small molecule |
| CAS | 81147-92-4 |
| UNII | MDY902UXSR |
| DrugBank ID | DB00187 |
Pharmacology
| Summary | Esmolol is a short‑acting, cardioselective beta‑1 adrenergic receptor blocker that reduces the effects of sympathetic stimulation on cardiac pacemaker and conduction tissues. By competitively inhibiting beta‑1 receptors without intrinsic sympathomimetic or membrane‑stabilizing activity, it decreases heart rate and conduction velocity. Its pharmacologic profile supports rapid, temporary control of tachyarrhythmias. |
|---|---|
| Mechanism of action | Similar to other beta-blockers, esmolol blocks the agonistic effect of the sympathetic neurotransmitters by competing for receptor binding sites. Because it predominantly blocks the beta-1 receptors in cardiac tissue, it is said to be cardioselective. In general, so-called cardioselective beta-blockers are relatively cardioselective; at lower doses they block beta-1 receptors only but begin to block beta-2 receptors as the dose increases. At therapeutic dosages, esmolol does not have intrinsic sympathomimetic activity (ISA) or membrane-stabilizing (quinidine-like) activity. Antiarrhythmic activity is due to blockade of adrenergic stimulation of cardiac pacemaker potentials. In the Vaughan Williams classification of antiarrhythmics, beta-blockers are considered to be class II agents. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | antagonist |
ADME / PK
| Absorption | Rapidly absorbed, steady-state blood levels for dosages from 50-300 µg/kg/min (0.05-0.3 mg/kg/mm) are obtained within five minutes. |
|---|---|
| Half-life | Rapid distribution half-life of about 2 minutes and an elimination half-life of about 9 minutes. The acid metabolite has an elimination half-life of about 3.7 hours. |
| Protein binding | 55% bound to human plasma protein, while the acid metabolite is 10% bound. |
| Metabolism | Esmolol undergoes rapid hydrolysis of ester linkage which is catalyzed by esterases found in the cytosol of red blood cells (RBCs). The plasma cholinersterases or RBC membrane acetylcholinesterases are not involved in this metabolic reaction. Metabolism of the drug occurs mainly in RBCs to form a free acid metabolite (with 1/1500 the activity of esmolol) and methanol. |
| Route of elimination | Consistent with the high rate of blood-based metabolism of esmolol hydrochloride, less than 2% of the drug is excreted unchanged in the urine. The acid metabolite has an elimination half-life of about 3.7 hours and is excreted in the urine with a clearance approximately equivalent to the glomerular filtration rate. Excretion of the acid metabolite is significantly decreased in patients with renal disease, with the elimination half-life increased to about ten-fold that of normals, and plasma levels considerably elevated. |
| Clearance | * 20 L/kg/hr [Men] |
Formulation & handling
- Esmolol is a small‑molecule beta‑blocker used exclusively in intravenous formulations due to rapid ester hydrolysis and unsuitable oral bioavailability.
- Aqueous concentrates require dilution before administration, and the API’s ester linkage makes it susceptible to hydrolysis, influencing pH control and solution stability during compounding.
- Low–moderate water solubility may require solubilizers or buffered systems to maintain clarity and stability in ready‑to‑use solutions.
Regulatory status
| Lifecycle | Most US and Canadian protection for this API lapsed between 2021 and 2022, but remaining US patents extending to 2033 indicate ongoing exclusivity for certain aspects of the product. Overall, the API is in a mixed‑maturity stage in the US and largely post‑exclusivity in Canada. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Multiple manufacturers and packagers supply esmolol, indicating a well‑established production base without reliance on a single originator, although branded Brevibloc products remain present in the US and Canada. Market availability appears concentrated in North America. Earlier patent expiries in 2021–2022 suggest existing generic presence, while later patents extending to 2033 indicate remaining protected elements that may influence the extent of future competitive entry. |
|---|
Safety
| Toxicity | Symptoms of overdose include cardiac arrest, bradycardia, hypotension, electromechanical dissociation and loss of consciousness. |
|---|
- Overexposure may precipitate severe cardiac depression, including bradycardia, hypotension, electromechanical dissociation, and potential cardiac arrest
- Loss of consciousness can occur at toxic levels, indicating significant central and cardiovascular compromise
- Materials handling should account for the compound’s potential to induce abrupt hemodynamic effects if inadvertently absorbed or mis-dosed during manufacturing or testing
Esmolol is a type of Beta blockers
Beta blockers are a subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs) widely used in the medical field. These medications work by blocking the effects of adrenaline and other stress hormones on the beta receptors in the body. This action helps to reduce the heart rate and blood pressure, making them effective in treating various cardiovascular conditions.
Beta blockers are commonly prescribed to manage conditions such as hypertension (high blood pressure), angina (chest pain), arrhythmias (irregular heart rhythms), and certain types of heart failure. They can also be used in the prevention of migraines and to alleviate symptoms associated with anxiety disorders.
By targeting the beta receptors, these APIs provide a significant impact on the sympathetic nervous system, reducing the fight-or-flight response and promoting a state of calmness. This mechanism of action allows beta blockers to be effective in controlling heart-related conditions.
Some well-known beta blockers include metoprolol, propranolol, atenolol, and carvedilol. These APIs are available in various forms such as tablets, capsules, and injectables, allowing for flexibility in administration and dosage.
It is important to note that the use of beta blockers should be done under medical supervision due to potential side effects and contraindications. Common side effects may include fatigue, dizziness, cold hands and feet, and sexual dysfunction. Patients with certain conditions like asthma or diabetes may require cautious monitoring while using beta blockers.
In conclusion, beta blockers are a vital subcategory of pharmaceutical APIs used to treat cardiovascular conditions by blocking the effects of stress hormones. Their effectiveness and versatility make them a valuable tool in managing various medical conditions, enhancing the well-being of patients.
Esmolol (Beta blockers), classified under Antihypertensive agents
Antihypertensive agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat high blood pressure, also known as hypertension. These medications are designed to lower blood pressure and reduce the risk of associated cardiovascular complications.
Antihypertensive agents function by targeting various mechanisms involved in blood pressure regulation. Some common classes of antihypertensive agents include angiotensin-converting enzyme (ACE) inhibitors, angiotensin II receptor blockers (ARBs), beta-blockers, calcium channel blockers (CCBs), and diuretics.
ACE inhibitors work by inhibiting the enzyme responsible for converting angiotensin I to angiotensin II, a hormone that constricts blood vessels. ARBs, on the other hand, block the receptors to which angiotensin II binds, thereby preventing its vasoconstrictive effects.
Beta-blockers reduce blood pressure by blocking the effects of adrenaline and noradrenaline, which are responsible for increasing heart rate and constricting blood vessels. CCBs inhibit calcium from entering the smooth muscles of blood vessels, resulting in relaxation and vasodilation. Diuretics promote the elimination of excess fluid and sodium from the body, reducing blood volume and thereby lowering blood pressure.
Antihypertensive agents are typically prescribed based on the individual patient's condition and specific needs. They can be used alone or in combination to achieve optimal blood pressure control. It is important to note that antihypertensive agents should be taken regularly as prescribed by a healthcare professional and may require periodic monitoring to ensure their effectiveness and manage any potential side effects.
In summary, antihypertensive agents play a vital role in the management of hypertension by targeting various mechanisms involved in blood pressure regulation. These medications offer significant benefits in reducing the risk of cardiovascular complications associated with high blood pressure.
Esmolol API manufacturers & distributors
Compare qualified Esmolol API suppliers worldwide. We currently have 6 companies offering Esmolol API, with manufacturing taking place in 5 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 |
|---|---|---|---|---|---|
| Minakem | Producer | France | Canada | CoA, FDA, GMP, USDMF | 31 products |
| MSN Labs. | Producer | India | India | CoA, GMP, USDMF, WC | 119 products |
| PharmaZell | Producer | Germany | France, India | BSE/TSE, CoA, EDMF/ASMF, FDA, GDP, GMP, MSDS, USDMF, WC, WHO-GMP | 31 products |
| SETV Global | Producer | India | India | CoA, FDA, GMP | 515 products |
| Veeprho Group | Producer | Czech Republic | Czech Republic | CoA | 136 products |
| Zhejiang Hengkang Pharmac... | Producer | China | China | BSE/TSE, CoA, MSDS, USDMF | 31 products |
When sending a request, specify which Esmolol 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 Esmolol 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.
Frequently asked questions about Esmolol API
Sourcing
What matters most when sourcing GMP-grade Esmolol?
Which documents are typically required when sourcing Esmolol API?
Which manufacturers are known to produce Esmolol API?
How can I request quotes for Esmolol API from GMP suppliers?
Is a GMP audit report available for Esmolol manufacturers?
How many suppliers offer Esmolol API on Pharmaoffer?
Which countries are known to manufacture Esmolol API?
Which certifications do suppliers of Esmolol usually hold?
Technical
What is Esmolol (CAS 81147-92-4) used for?
Which therapeutic class does Esmolol fall into?
What conditions is Esmolol mainly prescribed for?
How does Esmolol work?
What should someone know about the safety or toxicity profile of Esmolol?
What are important formulation and handling considerations for Esmolol as an API?
Is Esmolol a small molecule?
Are there special stability concerns for oral Esmolol?
Regulatory
Where is Esmolol approved or in use globally?
What’s the regulatory and patent landscape for Esmolol right now?
Pharmaoffer
How does Pharmaoffer’s Smart Sourcing Service help with Esmolol procurement?
Is Esmolol included in the PRO Data Insights coverage?
Where can I access the API market report for Esmolol?
