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Mephenesin | CAS No: 59-47-2 | GMP-certified suppliers
A medication that treats muscle spasticity in neurological disorders such as Parkinson’s disease and Multiple Sclerosis by providing central nervous system–mediated muscle relaxation.
Therapeutic categories
Primary indications
- Mephenesin was used for the treatment of muscle spasticity in diseases like Parkinson's or Multiple Sclerosis
Product Snapshot
- Mephenesin is formulated as a topical ointment
- It is indicated primarily for the treatment of muscle spasticity associated with neurological disorders such as Parkinson's disease and Multiple Sclerosis
- The product is approved for marketing in Canada
Clinical Overview
Clinically, mephenesin has been used in the management of muscle spasticity associated with neurological disorders such as Parkinson's disease and Multiple Sclerosis. Its therapeutic effect is attributed to its ability to produce transient muscle relaxation and paralysis by depressing central nervous system activity.
Pharmacodynamically, mephenesin reduces neuronal excitability which leads to a decrease in action potentials transmitted to muscle fibers, ultimately mitigating spasticity. Its mechanism of action is not fully elucidated; however, evidence suggests that it inhibits inward sodium and calcium ion currents in neurons. This ion channel blockade contributes to its muscle-relaxing effects and results in physiological effects that counteract those produced by strychnine, a known neurotoxin.
Pharmacokinetic data, including absorption, distribution, metabolism, and excretion parameters, are limited in the literature. Safety considerations emphasize the potential for central nervous system depression, which may result in sedation or respiratory depression at higher doses. Careful dose titration and monitoring are advised to minimize toxicity risks.
Mephenesin is categorized among a diverse group of central nervous system agents including alcohols, glycols, and centrally acting muscle relaxants. While it has been largely supplanted by newer muscle relaxants with improved safety profiles, mephenesin remains of interest in specific clinical and research contexts.
From an API sourcing perspective, quality attributes such as purity, compliance with pharmacopeial standards, and control of residual solvents are critical. Due to its chemical nature as a phenol ether and potential instability, suppliers must ensure robust manufacturing controls and validated analytical methods to guarantee consistent quality suitable for pharmaceutical formulation.
Identification & chemistry
| Generic name | Mephenesin |
|---|---|
| Molecule type | Small molecule |
| CAS | 59-47-2 |
| UNII | 7B8PIR2954 |
| DrugBank ID | DB13583 |
Pharmacology
| Summary | Mephenesin acts by inhibiting inward sodium and calcium currents in neurons, leading to reduced neuronal excitability. This results in decreased muscle fiber action potentials, producing a reduction in muscle spasticity. It is primarily utilized to address spasticity associated with neurological conditions such as Parkinson's disease and Multiple Sclerosis. |
|---|---|
| Mechanism of action | The exact mechanism of action of mephenesin is not known. It has been observed to block both inward sodium and inward calcium currents in neurons . It has a physiological effect which opposes that of strychnine. |
| Pharmacodynamics | Mephenesin reduced neuronal excitability leading to decreases action potentials to muscle fibers which ultimately produces a reduction in spasticity . |
Formulation & handling
- Mephenesin is a small molecule intended for topical application, not suitable for oral or injectable formulations.
- Its moderate water solubility and logP value suggest balanced lipophilicity, supporting skin permeation in topical formulations.
- Handle as a solid with consideration for stability in ointment bases, avoiding exposure to conditions that may affect aromatic ether groups.
Regulatory status
| Lifecycle | The active pharmaceutical ingredient (API) is marketed in Canada, where its patent has expired, resulting in the availability of multiple generic versions and increased market competition. The product is currently in a mature phase of its lifecycle. |
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| Markets | Canada |
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Supply Chain
| Supply chain summary | The manufacturing and supply landscape for Mephenesin in Canada includes originator companies responsible for branded products such as Decontractyl Baume. The branded presence appears primarily in Canada, with limited information on US or EU markets. Patent expiry indicates the potential for existing or upcoming generic competition in this therapeutic area. |
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Safety
| Toxicity | Mephenesin can produce hemolysis leading to hemoglobinuria with intravenous administration of concentrations greater than 10% . As a central nervous system depressant it can also produce paralysis and respiratory depression. |
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- Intravenous administration of Mephenesin solutions exceeding 10% concentration may induce hemolysis and hemoglobinuria
- Mephenesin acts as a central nervous system depressant with potential to cause paralysis and respiratory depression
- Appropriate handling measures should be implemented to mitigate exposure risks associated with neurotoxic and hemolytic effects
Diflucortolone Valerate is a type of Corticosteroids
Corticosteroids are a vital subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that play a crucial role in the field of medicine. These synthetic drugs mimic the effects of hormones naturally produced by the adrenal glands. Corticosteroids exhibit potent anti-inflammatory and immunosuppressive properties, making them widely used in the treatment of various medical conditions.
The main therapeutic applications of corticosteroids include the management of inflammatory disorders such as asthma, rheumatoid arthritis, and dermatological conditions like eczema and psoriasis. They are also employed in the treatment of allergic reactions, organ transplantations, and certain types of cancer.
Corticosteroids function by inhibiting the production of inflammatory mediators and suppressing immune responses. They act on specific receptors present in cells throughout the body, modulating gene expression and influencing various metabolic processes. These APIs are available in various formulations, including oral tablets, injectables, inhalers, nasal sprays, and topical creams.
It is crucial to note that corticosteroids must be prescribed and used under medical supervision due to their potential side effects, which can include adrenal suppression, osteoporosis, increased susceptibility to infections, and glucose intolerance. The dosage and duration of treatment vary depending on the condition being treated, and physicians carefully monitor patients to minimize any adverse effects.
In summary, corticosteroids are a vital class of pharmaceutical APIs with powerful anti-inflammatory and immunosuppressive properties. They are extensively used in the treatment of diverse medical conditions, providing relief to patients worldwide. However, their usage requires careful consideration and medical supervision to ensure optimal outcomes and minimize potential risks.
Diflucortolone Valerate (Corticosteroids), classified under Respiratory Tract Agents
Respiratory Tract Agents are a vital category of pharmaceutical APIs (Active Pharmaceutical Ingredients) designed to treat respiratory conditions and diseases. These agents are specifically formulated to target the respiratory system, which includes the lungs, airways, and nasal passages. They play a crucial role in managing various respiratory disorders, such as asthma, chronic obstructive pulmonary disease (COPD), and allergic rhinitis.
Respiratory Tract Agents encompass a wide range of medications, including bronchodilators, corticosteroids, antihistamines, and mucolytics. Bronchodilators are commonly used to relieve airway constriction and facilitate smooth breathing by relaxing the muscles in the airways. Corticosteroids help reduce inflammation in the respiratory system, alleviating symptoms and preventing exacerbations. Antihistamines work by blocking histamine receptors, thus mitigating allergic reactions that often impact the respiratory tract. Mucolytics aid in loosening and thinning mucus, making it easier to expel from the airways.
These APIs are developed through rigorous research and development processes, ensuring their efficacy, safety, and compliance with regulatory standards. Pharmaceutical manufacturers rely on advanced technologies and stringent quality control measures to produce high-quality Respiratory Tract Agents. These APIs are subsequently incorporated into various dosage forms, including inhalers, nasal sprays, nebulizers, and oral medications.
Respiratory Tract Agents are essential in the management of respiratory conditions, providing relief from symptoms, improving lung function, and enhancing the overall quality of life for patients. They are prescribed by healthcare professionals and often used in combination therapies to achieve optimal results. As respiratory disorders continue to affect a significant portion of the global population, the development and availability of effective Respiratory Tract Agents play a vital role in addressing these health challenges and improving patient outcomes.
Diflucortolone Valerate API manufacturers & distributors
Compare qualified Diflucortolone Valerate API suppliers worldwide. We currently have 2 companies offering Diflucortolone Valerate API, with manufacturing taking place in 1 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 |
|---|---|---|---|---|---|
| Coral Drugs | Producer | India | India | BSE/TSE, CoA, EDMF/ASMF, FDA, GMP, WC, WHO-GMP | 25 products |
| Gonane Pharma | Producer | India | India | BSE/TSE, CoA, GMP, MSDS | 166 products |
When sending a request, specify which Diflucortolone Valerate 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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