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Isoprenaline | CAS No: 7683-59-2 | GMP-certified suppliers
A medication that treats various heart block conditions, manages bronchospasm during anesthesia, and supports adjunctive therapy in shock and cardiac arrest emergencies.
Therapeutic categories
Primary indications
- Isoprenaline is indicated to treat mild or transient episodes of heart block not requiring electric shock or pacemakers, serious episodes of heart block and Adams-Stokes attacks not caused by ventricular tachycardia or fibrillation, and bronchospasm during anesthesia
- Isoprenaline is also indicated for cases of cardiac arrest until preferable treatments like electric shock and pacemakers are available
- Isoprenaline is also indicated as an adjunct therapy to fluid and electrolyte replacement therapy in hypovolemic shock, septic shock, hypoperfusion, congestive heart failure, and cardiogenic shock
Product Snapshot
- Isoprenaline is available as injectable solutions, tablets, and metered aerosol formulations suitable for various routes including intravenous, intramuscular, subcutaneous, and inhalation
- It is primarily indicated for cardiac conditions such as heart block, Adams-Stokes attacks, cardiac arrest, and bronchospasm during anesthesia, as well as adjunctive therapy in shock and heart failure
- Isoprenaline is approved for use in the US and Canada and is available in both approved and investigational status
Clinical Overview
Therapeutically, isoprenaline is indicated for the treatment of mild or transient heart block episodes that do not warrant electrical intervention or pacing, as well as for serious heart block and Adams-Stokes attacks not induced by ventricular tachyarrhythmias. It is also employed to manage bronchospasm during anesthesia. Additionally, isoprenaline serves as an emergency intervention in cardiac arrest situations when advanced treatments such as defibrillation or pacemakers are not immediately accessible. Adjunctive use alongside fluid and electrolyte replenishment is recognized in hypovolemic shock, septic shock, hypoperfusion, congestive heart failure, and cardiogenic shock.
Pharmacodynamically, isoprenaline stimulates both beta-1 and beta-2 adrenergic receptors. Beta-1 receptor agonism enhances cardiac contractility, conduction velocity, relaxation rate, and heart rate by initiating a G-protein coupled receptor signaling cascade. This cascade involves activation of adenylate cyclase, elevation of cyclic AMP, and subsequent activation of protein kinase A (PKA), leading to phosphorylation and activation of L-type calcium channels (Cav1.2) in cardiac myocytes.
Beta-2 receptor activation induces glycogenolysis in hepatic tissues, promotes glucagon secretion, and stimulates the renin-angiotensin-aldosterone axis. In pulmonary alveoli, beta-2 agonism modulates ion channel activity, including sodium channels, CFTR chloride channels, and sodium-potassium ATPase, facilitating alveolar fluid clearance through enhanced active sodium and chloride transport.
Isoprenaline exhibits a rapid onset but a short duration of action due to swift metabolic clearance. Safety considerations include caution in cardiogenic shock following myocardial infarction, potential worsening of heart block, and precipitating Adams-Stokes attacks.
Approved by the FDA since 1948, isoprenaline remains an important therapeutic agent in specific acute cardiovascular and respiratory conditions. Notable use contexts encompass emergency cardiac care and perioperative bronchospasm management.
From an API sourcing perspective, considerations should include ensuring the compound's chemical purity and compliance with pharmacopeial standards due to its narrow therapeutic applications and potent pharmacological activity. Reliable supply chains with validated manufacturing processes and thorough documentation for regulatory submissions are essential for maintaining product quality and global regulatory compliance.
Identification & chemistry
| Generic name | Isoprenaline |
|---|---|
| Molecule type | Small molecule |
| CAS | 7683-59-2 |
| UNII | L628TT009W |
| DrugBank ID | DB01064 |
Pharmacology
| Summary | Isoprenaline is a non-selective beta-adrenergic receptor agonist targeting beta-1 and beta-2 receptors to modulate cardiac and pulmonary function. Activation of beta-1 receptors enhances cardiac contractility, conduction, relaxation, and heart rate through cAMP-mediated phosphorylation of L-type calcium channels. Beta-2 receptor agonism promotes glycogenolysis, glucagon release, and alveolar fluid clearance via regulation of ion channels and transporters, contributing to bronchodilation and vascular effects. |
|---|---|
| Mechanism of action | Isoprenaline is a non-selective beta adrenergic receptor agonist. Agonism of beta-1 and beta-2 adrenergic receptors causes the alpha subunit of G-protein coupled receptors to exchange GMP for GTP, activating them, and allowing the alpha subunit to dissociate from the beta and gamma subunits. Dissociation of the alpha subunit activates adenylate cyclase, converting ATP to cyclic AMP. Cyclic AMP activates protein kinase A (PKA), which phosphorylates cardiac L-type calcium channels such as Ca<sub>v</sub>1.2. These channels depolarize cells by inward active transport of calcium ions. Agonism of beta-1 adrenergic receptors lead to increased strength of contractility, conduction of nerve impulses, speed of relaxation, and rate in the heart. Agonism of beta-2 adrenergic receptors leads to glycogenolysis in the liver, glucagon release from the pancreas, and activation of the renin-angiotensin-aldosterone system. In the alveoli, agonism of beta-2 adrenergic receptors, activates similar pathways to the heart, however the end result is regulation of sodium channels, the cystic fibrosis transmembrane conductance regulator (CFTR), and sodium potassium ATPase. PKA phosphorylates scaffolding proteins and sodium channels, increasing the number of sodium channels on the apical side of alveolar cells and increasing active transport of sodium ions into cells. Agonism of beta-2 adrenergic receptors can also increase chloride ion transport across CFTR. Together, these actions lead to passive transport of water out of the alveoli, and the clearance of alveolar fluid. |
| Pharmacodynamics | Isoprenaline is a non-selective beta adrenergic receptor agonist used in a number of indications for the heart, as well as bronchospasm in anesthesia. Isoprenaline has a short duration of action as it is rapidly cleared, and a wide therapeutic index. Patients should be counselled regarding the risks of isoprenaline in the treatment of cardiogenic shock following myocardial infarction, paradoxical worsening of heart block, or precipitation of Adams-Stokes attacks. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-1 adrenergic receptor | Humans | agonist |
| Beta-2 adrenergic receptor | Humans | agonist, binder |
| Beta-3 adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | Data regarding absorption kinetics of isoprenaline are not readily available. |
|---|---|
| Half-life | The half life of intravenous isoprenaline is 2.5-5 minutes. Oral isoprenaline has a half life of 40 minutes. |
| Protein binding | Isoprenaline is 68.8 ± 1.2% protein bound in plasma, mainly to serum albumin. |
| Metabolism | Isoprenaline is predominantly metabolized to glucuronide conjugates. Isoprenaline can also be O-methylated by catechol O-methyltransferase to the metabolite 3-O-methylisoprenaline, which can also be further glucuronidated. |
| Route of elimination | Isoprenaline is 12.2-27.0% recovered in the feces and 59.1-106.8% recovered in the urine after 48 hours. The majority of the recovered dose in the urine is conjugated isoprenaline, with 6.5-16.2% free isoprenaline, and 2.6-11.4% 3-O-methylisoprenaline and conjugates. |
| Volume of distribution | In pediatric patients, the volume of distribution was 216 ± 57 mL/kg. |
| Clearance | In pediatric patients, the clearance of isoprenaline was 42.5 ± 5.0 mL/kg/min. |
Formulation & handling
- Isoprenaline is a small molecule catechol derivative available for multiple administration routes including intravenous, intramuscular, subcutaneous, intracardiac, respiratory inhalation, and sublingual.
- Due to its catechol structure, the API may be sensitive to oxidation and light, requiring protection during storage and handling to maintain stability.
- Its moderate water solubility and low logP support formulation as injectable solutions, inhalation aerosols, and sublingual tablets without extensive solubilization aids.
Regulatory status
| Lifecycle | The API's primary patents have expired in both the US and Canada, allowing for generic competition in these markets. As a result, the product is in a mature phase with established presence and multiple available generics. |
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| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Isoprenaline involves multiple packagers catering primarily to the US and Canadian markets. Originator companies have established branded products under various names, including Duo-Medihaler and Isoproterenol formulations. Patent expiration on these products indicates the presence of generic competition in the current market. |
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Safety
| Toxicity | Patients experiencing an overdose may present with tachycardia, arrhythmias, palpitations, angina, hypotension, or hypertension. Overdose should be treated by reducing or stopping administration of isoprenaline and monitoring blood pressure, pulse, respiration, and ECG. In rats, the LD<sub>50</sub> is 2221 mg/kg orally, 128 mg/kg intraperitoneally, and 600 mg/kg subcutaneously. In mice, the LD<sub>50</sub> is 1260 orally and 450 mg/kg intraperitoneally. |
|---|
- Exposure to isoprenaline may cause cardiovascular effects including tachycardia, arrhythmias, and blood pressure fluctuations
- Acute toxicity varies by administration route
- LD50 values range from 128 mg/kg (intraperitoneal in rats) to 2221 mg/kg (oral in rats)
Isoprenaline is a type of Adrenergic agents
Adrenergic agents are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that target the adrenergic system in the body. This system is responsible for regulating various physiological responses, including heart rate, blood pressure, and smooth muscle contraction.
Adrenergic agents can be further divided into two main groups: adrenergic agonists and adrenergic antagonists. Adrenergic agonists stimulate the adrenergic receptors, leading to an increase in sympathetic nervous system activity. This can result in effects such as vasoconstriction, bronchodilation, and increased heart rate. Adrenergic agonists are commonly used in the treatment of conditions such as asthma, hypotension, and cardiac arrest.
On the other hand, adrenergic antagonists block the adrenergic receptors, thereby inhibiting the effects of sympathetic nervous system activation. These agents are often employed to lower blood pressure, treat certain heart conditions, and manage symptoms associated with conditions like benign prostatic hyperplasia. Adrenergic antagonists can be further classified into alpha-adrenergic antagonists and beta-adrenergic antagonists, based on their selectivity for different adrenergic receptor subtypes.
Pharmaceutical companies extensively utilize adrenergic agents as key components in the development of various medications. Adrenergic APIs offer targeted effects on the adrenergic system, allowing for precise modulation of physiological responses. The understanding of adrenergic agents and their mechanisms of action is vital for the design and optimization of drugs used in the treatment of numerous medical conditions. Researchers and scientists continue to explore and innovate within this subcategory to develop new adrenergic agents with enhanced efficacy and fewer side effects, ultimately improving patient outcomes.
Isoprenaline (Adrenergic agents), classified under Central Nervous System Agents
Central Nervous System (CNS) Agents are a crucial category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that specifically target the central nervous system. The CNS encompasses the brain and spinal cord, playing a vital role in regulating and controlling various bodily functions, including cognition, movement, emotions, and sensory perception. These agents are designed to interact with specific receptors, enzymes, or ion channels within the CNS to modulate neural activity and restore normal functioning.
CNS agents comprise a diverse range of pharmaceutical APIs, including analgesics, anesthetics, antipsychotics, sedatives, hypnotics, anti-epileptics, and antidepressants. Each subcategory addresses distinct neurological disorders and conditions. For instance, analgesics alleviate pain by targeting receptors in the brain and spinal cord, while antipsychotics are employed to manage psychosis symptoms in mental illnesses such as schizophrenia.
The development of CNS agents involves rigorous research, molecular modeling, and extensive clinical trials to ensure safety, efficacy, and specific target engagement. Pharmaceutical companies invest significant resources in identifying novel drug targets, synthesizing new compounds, and optimizing their pharmacological properties. These agents undergo rigorous regulatory evaluations and must adhere to stringent quality standards and guidelines.
Given the prevalence of CNS disorders globally, the market demand for effective CNS agents is substantial. The development of innovative CNS APIs not only improves patient outcomes but also provides valuable commercial opportunities for pharmaceutical companies. Continued advancements in CNS agent research and development hold the promise of groundbreaking therapies that can improve the quality of life for individuals affected by neurological conditions.
Isoprenaline API manufacturers & distributors
Compare qualified Isoprenaline API suppliers worldwide. We currently have 8 companies offering Isoprenaline 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 |
|---|---|---|---|---|---|
| Biophore India | Producer | India | India | CEP, CoA, GMP, USDMF | 46 products |
| Edmond Pharma (Recipharm) | Producer | Italy | Italy | CoA, USDMF | 20 products |
| Emcure Pharma | Producer | India | India | CoA, USDMF | 80 products |
| Harman Finochem | Producer | India | India | CoA, USDMF | 34 products |
| Hospira Boulder | Producer | United States | United States | CoA, USDMF | 5 products |
| Medinex Labs. | Producer | India | India | CoA, GMP, WC | 8 products |
| Micro Labs | Producer | India | India | CoA, USDMF | 38 products |
| Wuhan Wuyao | Producer | China | China | CoA, WC | 8 products |
When sending a request, specify which Isoprenaline 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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