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Orciprenaline | CAS No: 586-06-1 | GMP-certified suppliers
A medication that treats bronchospasm and airway obstruction in asthma, chronic bronchitis, and emphysema by providing bronchodilation and respiratory relief.
Therapeutic categories
Primary indications
- For the treatment of bronchospasm, chronic bronchitis, asthma, and emphysema
Product Snapshot
- Orciprenaline is available in multiple formulations including oral tablets, syrups, and parenteral and aerosol solutions for inhalation
- It is primarily used for the treatment of bronchospasm associated with chronic bronchitis, asthma, and emphysema
- The product is approved for commercial use in the US and Canadian markets
Clinical Overview
Pharmacologically, orciprenaline acts predominantly as a moderately selective β2-adrenergic receptor agonist. It stimulates β2 receptors located primarily in the bronchial smooth muscle, leading to the activation of adenylate cyclase. This activation increases intracellular cyclic adenosine monophosphate (cAMP) levels, resulting in relaxation of bronchial smooth muscles. Additionally, elevated cAMP inhibits the release of inflammatory mediators from mast cells, thereby mitigating immediate hypersensitivity reactions that contribute to airway constriction.
The mechanism of action is characterized by selective β2-adrenergic stimulation with minimal alpha-adrenergic receptor activity. Such selectivity underlies its role as a bronchodilator with reduced cardiovascular side effects compared to non-selective beta agonists. Orciprenaline’s effects extend to the uterus and skeletal muscle vasculature through β2 receptor engagement.
Key absorption, distribution, metabolism, and excretion (ADME) parameters are consistent with aminophenol beta-agonists, although detailed pharmacokinetic data are not provided here. Safety considerations include monitoring for potential tachycardia and hypertension, as orciprenaline can produce sympathetic stimulation. Careful dosing adjustment is required in populations sensitive to beta-adrenergic activation.
Orciprenaline is approved for systemic use in respiratory indications and is recognized within drug categories such as adrenergics, bronchodilators, and anti-asthmatic agents. It is formulated primarily as inhalants or oral preparations for airway disease treatment.
From an API sourcing perspective, quality control should ensure compliance with pharmacopeial standards for beta-adrenergic agonists, with stringent impurity profiling given the compound’s phenolic and amino alcohol functionalities. Stability under storage conditions and absence of degradation products are critical parameters to guarantee consistent therapeutic performance in finished pharmaceutical products.
Identification & chemistry
| Generic name | Orciprenaline |
|---|---|
| Molecule type | Small molecule |
| CAS | 586-06-1 |
| UNII | 53QOG569E0 |
| DrugBank ID | DB00816 |
Pharmacology
| Summary | Orciprenaline is a moderately selective β2-adrenergic receptor agonist that targets receptors primarily in the lungs, leading to bronchodilation. Its mechanism involves activation of adenylate cyclase and increased intracellular cAMP, resulting in relaxation of bronchial smooth muscle and inhibition of inflammatory mediator release. This pharmacodynamic profile supports its therapeutic use in managing bronchospasm and obstructive airway conditions. |
|---|---|
| Mechanism of action | Orciprenaline stimulates the β2-adrenergic receptor expressed in the lungs, uterus, and vasculature supplying skeletal muscles by acting as a moderately selective agonist. It exerts minimal or no effect on alpha-adrenergic receptors. Intracellularly, the actions of orciprenaline are mediated by cAMP, the production of which is augmented by beta stimulation. The drug is believed to work by activating adenylate cyclase, the enzyme responsible for producing the cellular mediator cAMP. |
| Pharmacodynamics | Orciprenaline (also known as metaproterenol), a synthetic amine, is structurally and pharmacologically similar to isoproterenol. Orciprenaline is used exclusively as a bronchodilator. The pharmacological effects of beta adrenergic agonist drugs, such as orciprenaline, are at least in part attributable to stimulation through beta adrenergic receptors of intracellular adenyl cyclase, the enzyme which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic- 3',5'- adenosine monophosphate (c-AMP). Increased cAMP levels lead to relaxation of bronchial smooth muscles and inhibition of the release of inalammatory mediators from mast cells that are involved in promoting immediate hypersensitivity . |
Targets
| Target | Organism | Actions |
|---|---|---|
| Beta-2 adrenergic receptor | Humans | agonist |
ADME / PK
| Absorption | 3% (oral bioavailability of 40%) |
|---|---|
| Half-life | 6 hours |
| Metabolism | Hepatic and gastric. The major metabolite, orciprenaline-3-0-sulfate, is produced in the gastrointestinal tract. Orciprenaline is not metabolized by catechol-0-methyltransferase nor have glucuronide conjugates been isolated to date. |
Formulation & handling
- Orciprenaline is a small molecule suitable for oral, parenteral, and inhalation formulations, including aerosols and syrups.
- The compound shows low lipophilicity (LogP 0.21) with high water solubility, facilitating aqueous-based formulations.
- Absorption is unaffected by food intake, but caffeine consumption should be limited during therapy.
Regulatory status
| Lifecycle | The API's primary patents have expired in both the US and Canada, allowing for generic manufacturing and increased market competition. As a result, the product is in a mature phase with multiple approved generics available in these markets. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Orciprenaline is manufactured by multiple originator and generic companies, indicating a well-established supply base with extensive B2B sourcing options. Branded products such as Alupent are mainly present in the US and Canadian markets, reflecting a regional focus for originator companies. Given the diversity of manufacturers and generic packagers involved, patent expiry has likely led to existing generic competition within these markets. |
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Safety
| Toxicity | Symptoms of overdose include angina, hypertension or hypotension, arrhythmias, nervousness, headache, tremor, dry mouth, palpitation, nausea, dizziness, fatigue, malaise and insomnia. LD<sub>50</sub>=42 mg/kg (orally in rat). |
|---|
- Handle with care to avoid exposure due to potential cardiovascular and neurological adverse effects
- Overdose may cause arrhythmias, blood pressure changes, and central nervous system symptoms
- Toxicity data: oral LD50 in rats is 42 mg/kg, indicating moderate acute toxicity
Orciprenaline 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.
Orciprenaline (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.
Orciprenaline API manufacturers & distributors
Compare qualified Orciprenaline API suppliers worldwide. We currently have 3 companies offering Orciprenaline 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 |
|---|---|---|---|---|---|
| Bidachem | Producer | Italy | Italy | CEP, CoA, FDA, GMP | 14 products |
| Cambrex | Producer | Italy | Unknown | CoA, USDMF | 104 products |
| Lusochimica | Producer | Italy | Italy | CoA, USDMF | 23 products |
When sending a request, specify which Orciprenaline 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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