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Trolamine salicylate
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Looking for Trolamine salicylate API 2174-16-5?
- Description:
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- API | Excipient name:
- Trolamine salicylate
- Synonyms:
- Cas Number:
- 2174-16-5
- DrugBank number:
- DB11079
- Unique Ingredient Identifier:
- H8O4040BHD
General Description:
Trolamine salicylate, identified by CAS number 2174-16-5, is a notable compound with significant therapeutic applications. Trolamine salicylate is an organic compound or a salt formed between triethanolamine and salicylic acid. Triethanolamine neutralizes the acidity of the salicylic acid. It is a topical analgesic used for temporary relief of minor pain associated with arthritis, simple backache, muscle strains, sprains, and bruises. Unlike other topical analgesics, trolamine salicylate has no distinct odor which improves patient acceptability . It also displays low systemic absorption upon dermal or topical administration and has low skin irritant properties . As with other salicylates, trolamine salicylate is an inhibitor of cyclo-oxygenase (COX) enzymes with no reported selectivity towards a specific enzyme isoform. Trolamine salicylate serves as an active ingredient in topical over-the-counter products for temporary management of mild to moderate muscular and joint pains.
Indications:
This drug is primarily indicated for: Indicated for the temporary relief of aches, and pains of muscles and joints associated with backache, lumbago, strains, bruises, sprains and arthritic or rheumatic pain, pain of tendons and ligaments . Its use in specific medical scenarios underscores its importance in the therapeutic landscape.
Absorption:
The absorption characteristics of Trolamine salicylate are crucial for its therapeutic efficacy: Following topical administration of 10% trolamine salicylate in healthy volunteers, salicylic acid could not be detected in serum indicating low systemic absorption . The drug's ability to rapidly penetrate into cells ensures quick onset of action.
Route of Elimination:
The elimination of Trolamine salicylate from the body primarily occurs through: Following topical administration of 10% trolamine salicylate in healthy volunteers, urinary recovery of total salicylate during the first 24 hours was 6.9 mg (p < 0.05), which is 1.4% of total dose . Understanding this pathway is essential for assessing potential drug accumulation and toxicity risks.
Volume of Distribution:
Trolamine salicylate is distributed throughout the body with a volume of distribution of: Topical administration of 1 gram of 10% trolamine salicylate in abdominal rat skin resulted in an approximate extravascular volume of distribution (V/F) of 24.0 mL . This metric indicates how extensively the drug permeates into body tissues.
Pharmacodynamics:
Trolamine salicylate exerts its therapeutic effects through: Trolamine salicylate is a salicylate that inhibits cyclo-oxygenase (COX) enzymes responsible for generating pro-inflammatory factors such as to induce pain and inflammation. It is thought to mediate its analgesic effect through inhibition of COX-2 enzyme, which is an induced enzyme responsible for inflammatory responses and pain in muscle and joint disorders. By inhibiting fatty acid COX enzyme, trolamine salicylate inhibits the production of prostaglandins and thromboxanes in inflammatory cells involved in generating pain and inflammation . It thereby works to temporarily reduce mild to moderate pain. In subjects with muscle soreness from exercise, administration of topical trolamine salicylate was associated with reduced duration and severity of muscule soreness compared to placebo . In subjects with osteoarthritis in hands, trolamine salicylate cream was shown to be effective in achieving temporary relief of minor pain and stiffness . The drug's ability to modulate various physiological processes underscores its efficacy in treating specific conditions.
Mechanism of Action:
Trolamine salicylate functions by: Inflammation and tissue damage in different conditions including arthritis, bursitis, joint disorder, bruises, and strains or sprains of muscle origin, induce mild to moderate pain and are associated with increase prostaglandin synthesis . This is thought to be a result of COX-2 enzyme induction. COX-2 is induced in inflammatory cells in case of cell injury, infection or activation from inflammatory cytokines such as interleukin (IL)-1 and tumor necrosis factor (TNF)-α. Upon activation, COX-2 produces prostanoid mediators of inflammation such as prostaglandins and thromboxanes . Trolamine salicylate mediates its analgesic effect by inhibiting the production of inflammatory mediators that sensitize nociceptive nerve endings and generate pain . This mechanism highlights the drug's role in inhibiting or promoting specific biological pathways, contributing to its therapeutic effects.
Toxicity:
Classification:
Trolamine salicylate belongs to the class of organic compounds known as 1,2-aminoalcohols. These are organic compounds containing an alkyl chain with an amine group bound to the C1 atom and an alcohol group bound to the C2 atom, classified under the direct parent group 1,2-aminoalcohols. This compound is a part of the Organic compounds, falling under the Organic nitrogen compounds superclass, and categorized within the Organonitrogen compounds class, specifically within the Amines subclass.
Categories:
Trolamine salicylate is categorized under the following therapeutic classes: Acids, Carbocyclic, Agents causing hyperkalemia, Anti-Inflammatory Agents, Anti-Inflammatory Agents, Non-Steroidal, Anti-Inflammatory Agents, Non-Steroidal (Non-Selective), Benzene Derivatives, Benzoates, Hydroxy Acids, Hydroxybenzoates, Nephrotoxic agents, Non COX-2 selective NSAIDS, Phenols, Salicylates, Sunscreen Agents. These classifications highlight the drug's diverse therapeutic applications and its importance in treating various conditions.
Experimental Properties:
Further physical and chemical characteristics of Trolamine salicylate include:
- Water Solubility: Soluble
- Melting Point: 50
- Boiling Point: Decomposes
Trolamine salicylate is a type of 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.