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Salicylamide
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Salicylamide is a non-prescription drug with analgesic and antipyretic properties. Its medicinal uses are similar to those of acetylsalicylic acid (Aspirin). It is often used in combination with acetylsalicylic acid and caffeine in the over-the-counter pain remedies (1). In France, it is used in a topical pharmaceutical product containing hydroxyethyl (glycol) salicylate, dexamethasone acetate, and salicylamide marketed for treatment of benign joint conditions such as mild tendinitis, small joint arthritis and sprains (2).
Inflammation
Published in George Feuer, Felix A. de la Iglesia, Molecular Biochemistry of Human Disease, 2020
George Feuer, Felix A. de la Iglesia
The nonsteroid acidic anti-inflammatory drugs (aspirin, phenylbutazone, flufenamic acid, indomethacin) inhibit several biochemical reactions, such as hydrolysis of proteins by proteolytic enzymes resembling trypsin, biosynthesis of histamine by histidine decarboxylase, and mitochondrial processes, including oxidative phosphorylation (Figure 29). Nonacidic derivatives of these drugs, such as salicylamide N-arylanthranilamides, and the amide of indomethacin are ineffective anti-inflammatory agents. These compounds elicit no inhibitory activity against enzyme reactions. Whereas the biochemical reactions are dissimilar, it has been shown that a common radical, an e-amino group of a lysine residue of the protein involved in the process, is essential in the enzyme-substrate interaction. The lysine ϵ-amino group belongs either to the protein substrate or to part of the enzyme protein. The acidic nonsteroid drugs form anions and become bound to the lysyl ϵ-amino group of the enzyme protein. Through this binding these agents interfere with the enzyme reactions that require the presence of these free ϵ-amino groups. Reactions dependent on such an amino group include the specific effect of trypsin-like proteolytic activity which occurs at a peptide bond adjacent to a lysine residue. Binding of pyridoxal phosphate as coenzyme of decarboxylase are necessary to histamine biosynthesis and mitochondrial oxidative phosphorylation.
Migraine: diagnosis and treatment
Published in Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby, Headache in Clinical Practice, 2018
Stephen D. Silberstein, Richard B. Upton, Peter J. Goadsby
Nonselective COX inhibitors inhibit both C0X1 and COX2 and include aspirin, naproxen, indomethacin, piroxicam, diclofenac, and ibuprofen. Some salicylates (sodium salicylate, salicylamide, and magnesium trisalicylate) can be used safely in patients with aspirin–induced asthma.57 Marketed highly selective C0X2 inhibitors include celecoxib and rofecoxib,58 and many other compounds are in development.
Non-specific binding of compounds in in vitro metabolism assays: a comparison of microsomal and hepatocyte binding in different species and an assessment of the accuracy of prediction models
Published in Xenobiotica, 2022
Iain Gardner, Mandy Xu, Chunyan Han, Yi Wang, Xingjin Jiao, Masoud Jamei, Hiba Khalidi, Peter Kilford, Sibylle Neuhoff, Roz Southall, David B. Turner, Helen Musther, Barry Jones, Simon Taylor
Test compounds were purchased as solids from Sigma (St Louis, MO, USA), Cerilliant (Round Rock, TX, USA), Tokyo Chemical Industry (Tokyo, Japan), National Institutes for Food and Drug Control (Beijing, China), MCE Chemicals and Equipment Co. (Malta, NY, USA) or Alfa Aesar (Haverhill, MA). 1-Aminobenzotriazole (1-ABT) and salicylamide were obtained from MCE and Sigma, respectively. Leibovitz’s L-15 Medium was obtained from Gibco (Waltham, MA, USA). Mouse (male CD-1, 400 donor pool) and minipig (male Göttingen, 3 donor pool) liver microsomes were purchased from BioIVT (Westbury, NY, USA). Rat (male Sprague-Dawley, 711 donor pool) and Dog (male Beagle, 8 donor pool) liver microsomes were purchased from Xenotech (Kansas City, KS, USA). Monkey (Cynomolgus male, 2 donor pool) and minipig (male Bama, 3 donor pool) liver microsomes were purchased from RILD (Shanghai, China). Human (mixed gender, 150 donor pool) liver microsomes, were purchased from Corning (New York, NY, USA).