Antipyretic activity

Naphthylacetic acid derivatives, showiag antiinflammatory, analgesic, and antipyretic activities ate prepared by Ftiedel-Crafts acylation of methyl 1-naphthyl acetate at the 4 position with (CH2)2CHCOCl followed by Clemmensen reduction (97). 

A large number of salts of sahcyhc acid have been prepared and evaluated for therapeutic or other commercial use. Table 7 hsts those most frequently referenced. Sodium sahcylate has analgesic, antiinflammatory, and antipyretic activities and was used extensively in the sixteenth and seventeenth centuries as a remedy, prepared from natural sources, for arthritis and rheumatism. In the 1990s the salt can be obtained directly from Kolbe-Schmitt carboxylation or by the reaction of sahcyhc acid with either aqueous sodium bicarbonate or sodium carbonate. The resulting mixture is heated until effervescence stops the salt is then isolated by filtration and evaporation to dryness at low temperatures. Generally, the solution must be kept slightly acidic so that a white product is obtained if the mixture is basic, a colored product results. The USP product contains 99.5—100.5% NaC H O (anhydrous). The May 1996 price was 8.15/kg (18). 

Uses. Aspirin has analgesic, antiinflammatory, and antipyretic activity. It is used for the reHef of less severe types of pain, such as headache, neuritis, acute and chronic rheumatoid arthritis, and toothache. Aspirin can be purchased in a variety of OTC and prescription dosage forms made and formulated by many companies. Tablets, ie, buffered, plain, or enteric-coated, are the most familiar in the United States, but other forms such as powder and effervescent formulations are of considerable importance in other parts of the world. 

Knorr reported the first pyrazole derivative in 1883. The reaction of phenyl hydrazine and ethylacetoacetate resulted in a novel stmcture identified in 1887 as l-phenyl-3-methy 1-5-pyrazolone 9. His interest in antipyretic compounds led him to test these derivatives for antipyretic activity which led to the discovery of antipyrine 10. He introduced the name pyrazole for these compounds to denote that the nucleus was derived from the pyrrole by replacement of a carbon with a nitrogen. He subsequnently prepared many pyrazole analogs, particularly compounds derived from the readily available phenyl hydrazine. The unsubstituted pyrazole wasn t prepared until 1889 by decarboxylation of liT-pyrazole-3,4,5-tricarboxylic acid. ... 

The thiophene analog of methadone (253) and isomethadone have been prepared and shown to be active analgesies. Heterocyclic acetamides of the type (254) have been prepared for evaluation of their analgesic and antipyretic activity. - ... 

The oldest effective drug for the treatment of this disease is indisputably quinine. Although the antipyretic activity of cinchona bark was known to the Incas, it remained for the Jesuit missionaries to uncover its antimalarial properties in the early seventeenth century. The advance of organic chemistry led to the isolation and identification of the alkaloid, quinine, as the active compound at the turn of this century. The emerging clinical importance of this drug led up to the establishment of cinchona plantations in the Dutch East Indies. This very circum-... 

Di-tert-butyl-4-hydroxyphenyl)-7//-triazolo [3,2-b][l, 2,4]triazin-7-one (HWA-131)is anon-immunosuppressive drug that effectively inhibited carrageenan-induced paw edema, attenuated the active Arthus reaction, and demonstrated antierythema as well as antipyretic activity. Part of the antiinflammatory effect of this new compound is most probably related to its antioxidative activity as well as inhibition of lipoxygenase... 

Acetaminophen is a nonsalicylate nonnarcotic analgesic whose mechanism of action is unknown. Lake the salicylates, acetaminophen has analgesic and antipyretic activity. However, acetaminophen does not possess antiinflammatory action and is of no value in the treatment of inflammation or inflammatory disorders. 

Acetaminophen has analgesic and antipyretic activity but little antiinflammatory action. It is highly hepatotoxic on overdose. 

Phenyluracils with alkyl groups substituted in the 5- and 6-positions, such as (L), are reported to have analgesic and antipyretic activity [376, 377]. The 1-position may also be alkylated. Such compounds are prepared by the treatment of a-alkyl-/3-aminocrotonates with phenyl isocyanate. When the 5-substituent is an isopropyl group, the resulting compound is a sodiuretic without increase in potassium excretion. 

The trialkyl-5-amino derivatives possess analgesic activity. Their quaternary salts with methyl bromide are very toxic. Most 5-dialkylamino derivatives, as well as the amides, showed analgesic, hypothermic, and antipyretic activity, with less toxicity than aminopyrine. They also appear to have a tranquillizing action. 

Other derivatives of this class of compound show marked analgesic and antipyretic activity. Thus 2,6-dimethyl-3-pyridazone (LI, R = CHs)... 

Cho, C. H., Chuang, C. Y. and Chen, C. F. 1986. Study of the antipyretic activity of matrine, a lupin alkaloid isolated from Sophora subprostata. Planta Medica, 343-345. 

The nitrosoimine derivative RE 2047 (45) in combination with pentoxifylline demonstrates potent antithrombotic activity <95AP(328)71). Other sydnones with pharmacological activity include derivatives of the general formulas (46) and (47). These agents were shown to have antiinflammatory, analgesic, and antipyretic activity <95JPS263). 3-Arylsydnones have been intensively studied because... 

Ketorolac (Toradol) is an NS AID with very mild antiinflammatory and antipyretic activity. It is a potent analgesic for postoperative pain. Its efficacy is equivalent to that of low doses of morphine in the control of pain. For this reason it is often combined with opioids to reduce opioid dose and related side effects while providing adequate pain relief. It is also used to replace the opioids in some patients with opioid sensitivity. The mechanism of action of ketorolac involves the inhibition of COX and decreased formation of prostaglandins. However, some evidence exists that ketorolac may stimulate the release of endogenous opioids as a part of its analgesic activity. 

Antipyretic activity. Ethanol (50%) extract of the plant, administered intraperito-neally to guinea pigs, was inactive " . Anti-thrombotic effect. Olive oil extract of the fmit, administered intragastrically to male rabbits at a dose of 150 g/kg, was active. Lipid profile was improved with decreased platelet hyperactivity and subendot-helial thrombogenicity and less severe morphological lesion of the endothelium and vascular wall . 

ZO099 Kurokawa, M., C. A. Kumeda, ]. Ya-mamura, T. Kamiyama, and K. Shiraki. Antipyretic activity of cinnamyl derivatives and related compounds in influenza virus-infected mice. Eur J Pharmacol 1998 348(1) 45-51. 

Non-steroidal antiinflammatory drugs (NSAIDs) are also known as nonopioid analgesics. They relieve pain without interacting with opioid receptors and do not depress CNS and have no drug dependence or drug abuse property and possess antipyretic activity also. They act primarily on peripheral pain mechanisms and also in CNS to raise pain threshold. 

Piroxicam is a new NSAID and has anti-inflammatory, analgesic and antipyretic activity. It provides effective and long-lasting relief of pain and stiffness. Its convenient once daily dosage provides round the clock relief of symptoms. 

It exhibits antiinflammatory, analgesic and antipyretic activities which are believed to be due to inhibition of COX-2. At therapeutic concentrations in humans, celecoxib does not inhibit COX-1 enzyme. 

Ketorolac, which appears to have a greater analgesic than anti-inflammatory or antipyretic activity, is widely used to treat postoperative as well as chronic pain. The tromethamine salt possesses sufficient water solubility to allow for parenteral administration. When administered orally or intramuscularly, ketorolac is rapidly and well absorbed, with peak plasma concentrations attained between 30 min and 50 min. In doses of 10-30 mg intramuscularly it is... 

Sargentodoxa cuneata L. Hong Teng (leaf, stem) Acetylsalicylic acid.50226 Antibacterial, antipyretic, activates blood flow. 

The title compounds (568) were prepared by reaction of anthranilic acids with y-chloroacid chlorides, followed by cyclization with hydroxylamine (77AF766). The title compounds exhibited antiinflammatory, analgesic and antipyretic activities (77AF766). 

Almost all non-opioid analgesics are non-steroidal anti-inflammatory drugs (NSAIDs) and have varying degrees of analgesic, anti-inflammatory and antipyretic activity. Acetylsalicylic acid (Aspirin ), used to relieve mild to moderate pain and certain types of severe pain, is the archetypal NSAID and is probably the best known and most used therapeutic drug worldwide. 

An analgesic with greater antiinflammatory and antipyretic activity than Naproxen is a-methyl-4-(2-thienylcarbonyl)benzeneacetic acid, Suprofen.63 This compound has been tested only as a racemic mixture, and any difference in the activity of the enantiomers is not known. Hydroformylation of 4-(2-thienylcarbonyl)styrene (entry 3, Table 4) to the 2-aiylpropanal was achieved in 78% ee for the branched aldehyde [(-t-)-enantiomer in excess], which can be converted to Suprofen by oxidation. 

Diflunisal Dolobid Has potency 3-4 times greater than aspirin in terms of analgesic and anti-inflammatory effects but lacks antipyretic activity. 

Sulindac is a new nonsteroid anti-inflammatory drug with analgesic and antipyretic activity - 2. 

NSAIDs are groups of unrelated organic acids such as mefenamic acid, which have analgesic, antiinflammatory, and antipyretic activities. NSAIDs are used to relieve mild to moderate pain, raised temperature, and acute and chronic inflammatory disorders such as osteoarthritis, rheumatoid arthritis, juvenile chronic arthritis, and ankylosing spondylitis. NSAIDs are applied locally for the relief of muscular pain and are useful in ophthalmic preparations for inflammatory eye disorders.1-4 NSAIDs have been used to relieve pain, particularly in cancer patients, forming a cornerstone in pain management. NSAIDs also are used... 

Many other sydnones and sydnonimines have been tested for antiinflammatory, antitumor, antibacterial, analgesic and antipyretic activity (67JPS149, 79MI42100, 80MI42102). 

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