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Niflumic acid | CAS No: 4394-00-7 | GMP-certified suppliers
A medication that provides analgesic and anti-inflammatory effects for managing rheumatoid arthritis and related musculoskeletal inflammatory conditions.
Therapeutic categories
Primary indications
- Used in the treatment of rheumatoid arthritis
Product Snapshot
- Niflumic acid is available in oral capsule and topical cream and gel formulations
- It is primarily indicated for the symptomatic treatment of rheumatoid arthritis
- The compound is currently in experimental status and not approved in major regulatory markets
Clinical Overview
Pharmacodynamically, niflumic acid functions as a calcium-activated chloride channel blocker. Its mechanism of action involves dual inhibition of phospholipase A2 and cyclooxygenase-2 (COX-2) enzymes. By suppressing these key enzymes, niflumic acid decreases the synthesis of pro-inflammatory mediators such as prostaglandins, contributing to reduced inflammation and pain.
Pharmacokinetic data on niflumic acid remain limited due to its experimental application. However, its metabolic profile suggests involvement of hepatic metabolism with interactions noted towards the UGT1A9 enzyme system. Absorption, distribution, and elimination characteristics are not extensively characterized in the literature. The compound’s activity as a nephrotoxic agent and its potential to cause hyperkalemia and hypertension warrant careful safety assessments during development and clinical use.
Niflumic acid is structurally related to fenamates and shares pharmacological properties common to nonsteroidal anti-inflammatory drugs (NSAIDs), including its classification under selective COX-2 inhibitors. Its applications have been explored in topical formulations for local joint and muscular pain relief, although systemic use remains investigational.
From a sourcing and quality perspective, procurement of niflumic acid APIs requires stringent adherence to purity specifications and the absence of impurities associated with organofluorine compounds. Due to its experimental status, comprehensive documentation on stability, solubility, and polymorphism is advisable to ensure consistent quality. Suppliers should provide detailed certificates of analysis compliant with regulatory standards appropriate for investigational medicinal products.
Identification & chemistry
| Generic name | Niflumic acid |
|---|---|
| Molecule type | Small molecule |
| CAS | 4394-00-7 |
| UNII | 4U5MP5IUD8 |
| DrugBank ID | DB04552 |
Pharmacology
| Summary | Niflumic acid is a nonsteroidal anti-inflammatory agent that inhibits phospholipase A2 and cyclooxygenase-2 (COX-2), reducing the production of pro-inflammatory mediators. It also functions as a calcium-activated chloride channel blocker, targeting membrane ion transport. These combined actions contribute to its therapeutic use in inflammatory conditions such as rheumatoid arthritis. |
|---|---|
| Mechanism of action | Niflumic acid is able to inhibit both phospholipase A2 as well as COX-2, thereby acting as an antiinflamatory and pain reduction agent. |
| Pharmacodynamics | Niflumic acid, a nonsteroidal anti-inflammatory fenamate, is a Ca<sup>2+</sup>-activated Cl<sup>-</sup> channel blocker. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Phospholipase A2 | Humans | inhibitor |
| Prostaglandin G/H synthase 2 | Humans | inhibitor |
| Chloride channel protein ClC-Ka | Humans | inducer |
ADME / PK
| Absorption | Well absorbed following oral administration. |
|---|---|
| Half-life | 2.5 hours |
| Protein binding | 90% bound to plasma proteins. |
| Metabolism | Hepatic. |
Formulation & handling
- Niflumic acid is a small molecule suitable for oral and topical formulations, with limited water solubility indicating potential need for solubilizing strategies.
- Not classified as a peptide or biologic, it is chemically stable under standard handling conditions but may require protection from moisture due to its solid state.
- Due to its oral and topical routes, no special sensitivity to food interactions is noted, but formulation should consider its lipophilicity (LogP 3.21) for optimal absorption.
Regulatory status
Safety
| Toxicity | Oral, mouse: LD<sub>50</sub> = 350 mg/kg; Oral, rat: LD<sub>50</sub> = 250 mg/kg |
|---|
- Exhibits moderate acute oral toxicity with LD50 values of 350 mg/kg in mice and 250 mg/kg in rats
- Handling requires appropriate protective equipment to minimize exposure risk
- Inhalation or ingestion of dust or powder should be avoided due to potential systemic toxicity
Niflumic Acid is a type of Non-opioid analgesics
Non-opioid analgesics are a subcategory of pharmaceutical active pharmaceutical ingredients (APIs) that are widely used for the management of pain. Unlike opioids, which are known to have addictive properties, non-opioid analgesics offer pain relief without the risk of dependence or addiction.
These APIs work by inhibiting the production of prostaglandins, which are substances in the body that contribute to pain and inflammation. Non-opioid analgesics are typically available over-the-counter (OTC) and come in various forms such as tablets, capsules, creams, and gels.
One of the most common non-opioid analgesics is acetaminophen, which is highly effective in relieving mild to moderate pain. It is commonly used to alleviate headaches, toothaches, and musculoskeletal pain. Another popular non-opioid analgesic is non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen and naproxen. These medications not only reduce pain but also have anti-inflammatory properties, making them particularly useful for conditions such as arthritis.
Non-opioid analgesics are generally well-tolerated but can have potential side effects, including gastrointestinal disturbances and, in rare cases, liver or kidney damage. It is important to follow recommended dosages and consult a healthcare professional if there are any concerns or underlying medical conditions.
In conclusion, non-opioid analgesics are a vital category of pharmaceutical APIs that offer effective pain relief without the risk of addiction. Their accessibility, diverse formulations, and relatively favorable safety profile make them a popular choice for individuals seeking relief from various types of pain.
Niflumic Acid (Non-opioid analgesics), classified under Analgesics
Analgesics are a category of pharmaceutical Active Pharmaceutical Ingredients (APIs) that are commonly used to relieve pain. They are designed to alleviate discomfort by targeting the body's pain receptors or by reducing inflammation. Analgesics are widely utilized in the medical field to manage various types of pain, ranging from mild to severe.
One of the primary classes of analgesics is nonsteroidal anti-inflammatory drugs (NSAIDs). NSAIDs work by inhibiting the production of prostaglandins, substances that contribute to pain and inflammation. This class includes well-known drugs like ibuprofen and naproxen. Another class of analgesics is opioids, which are derived from opium or synthetic compounds that mimic the effects of opium. Opioids act on the central nervous system to reduce pain perception and provide potent pain relief. Examples of opioids include morphine, codeine, and oxycodone.
Analgesics are available in various forms, such as tablets, capsules, creams, and injections, allowing for different routes of administration based on the patient's needs. They are commonly used to manage pain associated with conditions like arthritis, headaches, dental procedures, and post-operative recovery.
It is important to note that analgesics should be used under medical supervision, as improper use or overuse can lead to adverse effects, including gastrointestinal complications, addiction, and respiratory depression in the case of opioids. Therefore, it is crucial for healthcare professionals to assess each patient's individual needs and prescribe the appropriate analgesic and dosage.
In summary, analgesics are a vital category of pharmaceutical APIs used to alleviate pain by targeting pain receptors or reducing inflammation. With various classes and forms available, they provide valuable options for pain management when used responsibly and under medical guidance.
Niflumic Acid API manufacturers & distributors
Compare qualified Niflumic Acid API suppliers worldwide. We currently have 4 companies offering Niflumic Acid API, with manufacturing taking place in 3 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 |
|---|---|---|---|---|---|
| Curia | Producer | United States | France | CEP, CoA, GMP, MSDS | 106 products |
| Euticals | Producer | Italy | France | CEP, CoA, FDA, GMP | 48 products |
| Gedeon Richter | Producer | Hungary | Hungary | CoA, GMP | 48 products |
| Pen Tsao Chemical Industr... | Producer | Germany | China | CoA | 18 products |
When sending a request, specify which Niflumic Acid 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 Niflumic Acid 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.
