Analgesics and antipyretics

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). 

Analgesic and antipyretic ibuprofen, 2-(p-isobutylphenyl)propionic acid, is converted to its monohydroxyaluminum salt by converting the acid to its sodium salt using dilute caustic, foUowed by concurrent addition of equimolar amounts of aluminum nitrate and sodium bicarbonate (84). This salt can also... 

Most of the pharmacologically active indazole derivatives are useful as antiinflammatory drugs, e.g. bendazac or [(1-benzyl-l J/-indazol-3-yl)oxy]acetic acid (LDso in mice and rats of 355 and 388mgkg i.p., respectively) and benzydamine or l-benzyl-3-[3-(dimethyl-amino)propoxy]-l//-indazole (LDso in mice and rats of 110 and lOOmgkg" i.p., respectively). The last cited compound also has analgesic and antipyretic properties (B-76MI40404). 

Oxyphenbutazone (712), y-hydroxyphenylbutazone and kebuzone (715) are metabolites of phenylbutazone in liver. The first cited is an equally potent antiinflammatory agent but slightly less toxic. Compounds (711) and (712) are rarely used as analgesics and antipyretics because of their toxicities. The first one is used in therapy of rheumatoid disorders characterized by a lack of detectable antiglobulin and antinuclear antibodies in the serum. The y-hydroxyphenylbutazone has marked uricosuric activity but little antirheumatic effect. Kebuzone (715) is an antiinflammatory agent still widely used in Europe. 

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 different furanones 104 were tested for their potency as inhibitors of PGE2 production both in transfected Chinese hamster ovarian (CHO) cells expressing human COX-2 and in human whole blood. Compound 104r proved to be an orally active and selective COX-2 inhibitor that is devoid of the ulcerogenic effect at >100 times the dose for antiinflammatory, analgesic, and antipyretic effects (99BMC3187). 

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. 

Amabeoku GJ, Eagles P, Scott G, Mayeng I, Springfield E. Analgesic and antipyretic effects of Dodonaea angustifolia and Salvia africana-lutea. J Ethnopharmacol 2001 75 117-124. 

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

Vincamine (91) is the major alkaloid of V. minor, a plant used against headache and vertigo. It exerts a sedative CNS action and produces a fall in blood pressure. The principal activity is a moderate cerebral vasodilation. Clinical studies have demonstrated that i.v. administration of 91 to humans reduces the arterial blood pressure and increases cerebral blood flow and oxygen consumption. The improved cerebral hemodynamic conditions significantly and positively affect the state of patients with advanced arteriosclerosis with beneficial effects on memory, concentration, and behavior. It has thereafter been introduced under several trade names as a pharmaceutical in many European countries (232). Vobasine (32) has been widely studied it exhibits a weak CNS depressive, analgesic, and antipyretic action (21). 

From a series of 5,6-diphenylpyridazines prepared in Italy [91], chloro derivatives of type (20, R = 4-Me2NC6H4, 4-MeOC6H4) have been found to be anti-inflammatory, analgesic and antipyretic agents superior to phenylbutazone when tested in mice or rats. 

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. 

Acetylsalicylic acid (ASA) exerts an antiinflammatory effect, in addition to its analgesic and antipyretic actions. 

Another analgesic, acetaminophen, is a derivative of /7-aminophenol. Although it is an analgesic and antipyretic, acetaminophen shows little if any... 

Determination of various analgesic and antipyretic pharmaceuticals on reversed phase has included not only the analysis of serum levels of aspirin, salicylic acid and salicyluric acid using acidified acetonitrile (557), or methanol (338), but also suUinpyrazone under isocratic conditions (339), and 6-chloro-a-methylcarbazole-2-acetic acid (340). The polar thiol metabolites of acetaminophen were analyzed by RPC and the method was found to be superior to other chromatographic techniques used in this analysis (341). 

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

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... 

The enumeration of these effects of prostaglandins makes it understandable that the inhibition of the cycloxigenases will result in antiinflammatory, analgesic and antipyretic effects. Another important function of PGE2 is the vasodilatation it can induce in the renal circulation. Locally produced PGE2 increases the renal perfusion. 

Paracetamol, synonym acetaminophen, is world wide probably the most popular analgesic and antipyretic. Its mechanism of action is not well understood. It is not really an NSAID as it is only a very weak inhibitor of cyclo-oxygenase and has hardly any anti-inflammatory activity. For the same reason paracetamol gives only negligible gastrointestinal irritation and gives hardly any blockade of platelet aggregation. Paracetamol concentrations in plasma reach a peak in 30-60 minutes, and the half-life in plasma is about 2 hours. Almost 100% of... 

Tolmetin (Tolectin) is an antiinflammatory, analgesic, and antipyretic agent that produces the usual gastric distress and ulceration observed with NSAIDs. However, tolmetin is better tolerated than aspirin and produces less tinnitus and vertigo. Tolmetin is a substitute for indomethacin in indomethacin-sensitive patients and is unique among such drugs in that it can be used to treat juvenile arthritis. 

It is a potent antiinflammatory agent. It has poor analgesic and antipyretic action. Mechanism of action is similar to other NSAIDs. 

It is indole acetic acid derivative possessing potent antiinflammatory property and having a good analgesic and antipyretic action also. Mechanism of action is same as other NSAIDs. 

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