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Diflunisal | CAS No: 22494-42-4 | GMP-certified suppliers
A medication that provides symptomatic relief of mild to moderate pain and inflammation in musculoskeletal conditions, osteoarthritis, and rheumatoid arthritis without narcotic effects.
Therapeutic categories
Primary indications
- For symptomatic treatment of mild to moderate pain accompanied by inflammation (e
- G
- Musculoskeletal trauma, post-dental extraction, post-episiotomy), osteoarthritis, and rheumatoid arthritis
Product Snapshot
- Diflunisal is an oral small molecule available primarily in tablet and capsule formulations
- It is indicated for the symptomatic treatment of mild to moderate pain associated with inflammation, including musculoskeletal trauma, post-dental extraction pain, osteoarthritis, and rheumatoid arthritis
- Diflunisal is approved for use in the US and Canada, with both approved and investigational statuses noted
Clinical Overview
The mechanism of action of diflunisal is primarily attributed to the inhibition of prostaglandin synthesis via the arachidonic acid pathway, although the exact pathways remain incompletely defined. By inhibiting prostaglandin synthetase (cyclooxygenase), diflunisal reduces the production of prostaglandins in peripheral tissues. Prostaglandins play a role in sensitizing afferent nerves and potentiating pain mediators such as bradykinin, thus their reduction accounts for the drug’s analgesic and anti-inflammatory effects. Diflunisal acts peripherally and does not exhibit narcotic properties, with no reported habituation, tolerance, or addiction.
Pharmacokinetic data indicate that diflunisal is not metabolized to salicylic acid, distinguishing it from aspirin, and its fluorine atoms remain intact during metabolism. The drug is mainly eliminated renally, and it is known to inhibit renal organic anion transporters such as OAT1/SLC22A6. Notable pharmacodynamic considerations include its potential to cause hyperkalemia, hypertension, and nephrotoxicity, requiring caution in patients with renal impairment or cardiovascular risk factors. Additionally, diflunisal can induce photosensitivity and should be monitored accordingly.
Diflunisal is approved in various markets under multiple formulations, predominantly for rheumatologic and musculoskeletal indications. Quality considerations for active pharmaceutical ingredient (API) procurement include confirmation of chemical purity, stereochemical integrity of the biphenyl structure, absence of fluorine displacement, and compliance with regulatory standards for NSAIDs. Tight control of residual solvents, heavy metals, and endotoxins is critical to ensure API suitability for pharmaceutical formulation.
Identification & chemistry
| Generic name | Diflunisal |
|---|---|
| Molecule type | Small molecule |
| CAS | 22494-42-4 |
| UNII | 7C546U4DEN |
| DrugBank ID | DB00861 |
Pharmacology
| Summary | Diflunisal is a nonsteroidal anti-inflammatory drug that exerts analgesic and anti-inflammatory effects primarily through inhibition of prostaglandin G/H synthase 1 and 2 enzymes. This inhibition reduces prostaglandin synthesis in peripheral tissues, which are key mediators of pain and inflammation. Diflunisal’s pharmacodynamic profile includes analgesic, anti-inflammatory, and antipyretic properties without known risk of habituation or addiction. |
|---|---|
| Mechanism of action | The precise mechanism of the analgesic and anti-inflammatory actions of diflunisal is not known. Diflunisal is a prostaglandin synthetase inhibitor. In animals, prostaglandins sensitize afferent nerves and potentiate the action of bradykinin in inducing pain. Since prostaglandins are known to be among the mediators of pain and inflammation, the mode of action of diflunisal may be due to a decrease of prostaglandins in peripheral tissues. |
| Pharmacodynamics | Diflunisal is a nonsteroidal drug with analgesic, anti-inflammatory and antipyretic properties. It is a peripherally-acting non-narcotic analgesic drug. Habituation, tolerance and addiction have not been reported. Diflunisal is a difluorophenyl derivative of salicylic acid. Chemically, diflunisal differs from aspirin (acetylsalicylic acid) in two respects. The first of these two is the presence of a difluorophenyl substituent at carbon 1. The second difference is the removal of the 0-acetyl group from the carbon 4 position. Diflunisal is not metabolized to salicylic acid, and the fluorine atoms are not displaced from the difluorophenyl ring structure. |
Targets
| Target | Organism | Actions |
|---|---|---|
| Prostaglandin G/H synthase 2 | Humans | inhibitor |
| Prostaglandin G/H synthase 1 | Humans | inhibitor |
ADME / PK
| Absorption | Rapidly and completely absorbed following oral administration, with a bioavailability of 80-90%. Peak plasma concentrations are achieved 2 - 3 hours following oral administration. |
|---|---|
| Half-life | 8 to 12 hours |
| Protein binding | At least 98 to 99% of diflunisal in plasma is bound to proteins. |
| Metabolism | Hepatic, primarily via glucuronide conjugation (90% of administered dose). |
| Route of elimination | The drug is excreted in the urine as two soluble glucuronide conjugates accounting for about 90% of the administered dose. Little or no diflunisal is excreted in the feces. |
Formulation & handling
- Diflunisal is a small molecule administered orally, available primarily in tablet and capsule forms.
- The compound has low water solubility and high lipophilicity (LogP 3.91), which may impact formulation strategies for dissolution and bioavailability.
- Co-administration with food is advised to minimize gastrointestinal irritation; avoid alcohol as it may exacerbate adverse effects.
Regulatory status
| Lifecycle | The API’s primary patents have expired or are nearing expiry in the US and Canada, leading to a mature market with multiple generic products available. Ongoing regulatory approvals continue to influence product availability in these regions. |
|---|
| Markets | US, Canada |
|---|
Supply Chain
| Supply chain summary | Diflunisal is manufactured by multiple companies, including originator and generic manufacturers, reflecting a competitive supply landscape. Branded products are primarily present in the US and Canadian markets, with extensive packaging and distribution networks. Patent expiry has allowed for the introduction of numerous generic versions, indicating established generic competition. |
|---|
Safety
| Toxicity | Oral LD<sub>50</sub> in rat, mouse, and rabbit is 392 mg/kg, 439 mg/kg, and 603 mg/kg, respectively. Symptoms of overdose include drowsiness, nausea, vomiting, diarrhea, hyperventilation, tachycardia, sweating, tinnitus, disorientation, stupor, and coma. As a monotherapy, the smallest dosage capable of causing death was reported as 15 grams. <p>Selective COX-2 inhibitors have been associated with increased risk of serious cardiovascular events (e.g. myocardial infarction, stroke) in some patients. Current data is insufficient to assess the cardiovascular risk of diflunisal. Short-term use does not appear to be associated with increased cardiovascular risk (except when used immediately following coronary artery bypass graft (CABG) surgery). Risk of GI toxicity including bleeding, ulceration and perforation. Risk of direct renal injury, including renal papillary necrosis. Severe hepatic reactions, including cholestasis and/or jaundice, have been reported. May cause rash or hypersensitivity syndrome.</p> |
|---|
- Oral LD50 values indicate moderate acute toxicity
- Overdose symptoms include central nervous system depression and gastrointestinal disturbances
- Potential for serious cardiovascular and gastrointestinal adverse effects, including bleeding, ulceration, and increased risk of myocardial infarction or stroke
Diflunisal is a type of NSAIDs
NSAIDs (Non-Steroidal Anti-Inflammatory Drugs) are a widely used subcategory of pharmaceutical Active Pharmaceutical Ingredients (APIs). These medications are commonly prescribed for their analgesic (pain-relieving), anti-inflammatory, and antipyretic (fever-reducing) properties. NSAIDs work by inhibiting the production of certain enzymes called cyclooxygenases (COX), which play a crucial role in the synthesis of prostaglandins, substances that contribute to pain, inflammation, and fever.
These pharmaceutical APIs are available in various formulations, including tablets, capsules, creams, and gels, making them convenient for different administration routes. Some popular examples of NSAIDs include aspirin, ibuprofen, naproxen, and diclofenac.
NSAIDs are commonly used to treat a wide range of conditions such as arthritis, musculoskeletal injuries, dental pain, menstrual pain, and headaches. They are also effective in managing inflammatory conditions like rheumatoid arthritis and ankylosing spondylitis.
While NSAIDs are generally safe and effective when used as directed, they may have side effects. These can include gastrointestinal issues such as stomach ulcers or bleeding, cardiovascular risks, and kidney problems. Therefore, it is essential to follow the recommended dosage and consult with healthcare professionals to ensure proper and safe usage.
In conclusion, NSAIDs are a subcategory of pharmaceutical APIs that offer analgesic, anti-inflammatory, and antipyretic properties. Their versatility and effectiveness in treating various conditions make them widely prescribed medications. However, it is crucial to be aware of potential side effects and consult healthcare providers for appropriate usage.
Diflunisal (NSAIDs), classified under Anti-inflammatory Agents
Anti-inflammatory agents are a crucial category of pharmaceutical active pharmaceutical ingredients (APIs) used to treat various inflammatory conditions. These agents play a vital role in alleviating pain, reducing swelling, and controlling inflammation in the body. They are widely employed in the management of diverse medical conditions, including arthritis, autoimmune disorders, asthma, and skin conditions like dermatitis.
Anti-inflammatory APIs primarily function by inhibiting the production of specific enzymes called cyclooxygenases (COX) and lipoxygenases (LOX). These enzymes are responsible for the synthesis of pro-inflammatory molecules known as prostaglandins and leukotrienes, respectively. By suppressing the activity of COX and LOX, anti-inflammatory agents effectively curtail the production of these inflammatory mediators, thereby mitigating inflammation.
Common examples of anti-inflammatory APIs include non-steroidal anti-inflammatory drugs (NSAIDs) like ibuprofen, aspirin, and naproxen. These agents exhibit analgesic, antipyretic, and anti-inflammatory properties. Another group of anti-inflammatory APIs includes corticosteroids, such as prednisone and dexamethasone, which are synthetic hormones that modulate the body's immune response to control inflammation.
In conclusion, anti-inflammatory agents are a vital category of pharmaceutical APIs widely used to manage inflammation-related disorders. They target enzymes involved in the synthesis of pro-inflammatory molecules, effectively reducing pain and swelling. NSAIDs and corticosteroids are commonly prescribed anti-inflammatory APIs due to their efficacy in controlling inflammation.
Diflunisal API manufacturers & distributors
Compare qualified Diflunisal API suppliers worldwide. We currently have 1 companies offering Diflunisal 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 |
|---|---|---|---|---|---|
| Chemi S.p.A. | Producer | Italy | Italy | CoA, GMP, USDMF | 18 products |
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