Analgesics, antipyretics, and antiinflammatory agents

Kirk-Othmer Encyclopedia of Chemical Technology (4th Edition) 

155N31O23. The latter is further cleaved to dynorphin A(l—8) and dynorphin B(l—3). 

P-endorphin [60617-12-1] H-TyrGlyGlyPheMetThrSerGluLysSerGlnThrProLeu-ValThrLeuPheLysAsnAlalle V alLys Asn AlaHisLys LysGlyGln- OH 

Opium is the dried, powdered sap of the unripe seed pod of Papaver somniferum, a poppy plant indigenous to Asia minor. Theophrastus described its medical properties in the third century BC, but the Sumerians, ca BC 4000, probably perceived its utility. Arab physicians knew of the dmg, and Arab traders carried it to the Orient where it was used as a treatment for dysentery. Paracelsus is credited with repopularizing the dmg in western Europe in the early sixteenth century by formulating opium into laudanum , which is still in use. More than 20 different alkaloids (qv) of two different classes comprise 25% of the weight of dry opium. The benzylisoquinolines, characterized by papaverine [58-74-2] (1.0%), a smooth muscle relaxant, and noscapine [128-62-1] (6.0%), an antitussive agent, do not have any analgesic effects. The phenanthrenes, the second group, are the more common and include 10% morphine (1, = R = H), 0.5% codeine [76-57-3], C gH2 N03, (1, R = H, R = CH3), and 0.2 thebaine [115-37-7], C 2H2 N03, (2). 

Codeine, mol wt 299.3, is a significantly less potent analgesic than morphine, requiring 60 mg (0.20 mmol) to equal the effectiveness of 10 mg (0.04 mmol) of morphine. However, codeine is orally effective, and it is less addictive and associated with less nausea than morphine. Codeine is used as an antitussive agent, although newer, nonaddictive agents are preferred (see Expectorants, antitussives, and related agents). 

Introduced in 1898, heroin was heralded as a nonaddictive alternative to morphine. Subsequent clinical experience showed it to be highly addictive and preferred by addicts over morphine (13). Heroin is approximately ten times more potent than morphine, with quicker onset and shorter duration of 

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ANALGESICS,ANTIPYRETICS,AND ANTIINFLAMMATORY AGENTS] (Vol2) Buprenorphme [52485-79-7]... 

See Analgesics, antipyretics, and antiinflammatory agents Chemotherapeutics, anticancer Immunotherapeutic agents. 

Nonsteroidal Antiinflammatory Drugs. Nonsteroidal antiinflammatory dmgs (NSAIDs) include, among the numerous agents of this class, aspirin (acetylsaflcyhc acid), the arylacetic acids indomethacin and sulindac, and the arylpropionic acids, (5)-(147) and (R)-(148) ibuprofen, (5)-(149) and (R)- (150), flurbiprofen naproxen (41), and fenoprofen (see Analgesics, antipyretics, and antiinflammatory agents Salicylic acid and related compounds). 

Many 1,2,3,5-benzenetetrol derivatives are used mediciaaHy. For example, khellin [82-02-0] (65), which is a naturally occurring benzopyranone, is used as a coronary vasodilator and bronchodilator (233). Derivatives of khellin are effective local anesthetics and antiarrythmics (234). Similarly, amine derivatives (68) that are prepared from khellinone oxime (66) exhibit hypnotic, sedative, anticonvulsant, antiinflammatory, cardiac analeptic, diuretic, and antiulcerous activity (235) (see Analgesics, antipyretics, and antiinflammatory agents). 

It is an unfortunate consequence of the use of Christian name abbreviation (A. Spirin), that Alex always evokes for me a well known analgesic, antipyretic and antiinflammatory agent, which John Vane showed in 1971 to be an inhibitor of the synthesis of prostaglandins from arachadonic acid. 

Related to salicylic acid as isomers are / -hydroxybenzoic acid [99-06-9] andy>-hydroxybenzoic acid [99-96-7]. The three are commonly known as the monohydroxybenzoic acids because of the shared chemical reactions, the three isomers are discussed together herein. These monohydroxybenzoic acids have a broad range of applications from paper coatings and liquid crystal preparations to drugs. Salicylic acid and its derivatives are interesting because of their demonstrated activity as analgesics, antipyretics, and antiinflammatory agents, whereas the para-substituted acids and esters known as parabens have activity as preservatives for food. 

ANALGESICS,ANTIPYRETICS, AND ANTIINFLAMMATORY AGENTS] (Vol 2) -from acetic anhydride [ACETIC ACID AND DERIVATIVES - ANHYDRIDE] (Vol 1)... 

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