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rand dTWO NEW NONSTEROIDALANTI -INFLAMMATORY DRUGS
Two new anti- inflammatory drugs [diflumidone (R807) and
R. 8051. w hich are acidic by virtue of a sulphonanilide ratherthan carboxyl gro up as in most other nons teroidal antiinflam matory agents, were examined to determine the ir effecton prostaglandin biosynt hesis and platelet aggregation .Compariso n of these su(phonanilides with other drugs in thisgroup showed the followi ng order of potency aga instprostaglandin synthetase activity: indomethacin > flufenamicacid > diflumidcne > R-80S > phenylbutazone :> aspirinAgainst arachidonic acid-induced platelet aggregation thefollowing order of potency was demonstrated: indomethacin> diflumidone > R-80 S > flufenamic acid >phenylbutazone > aspirin. However . in contrast to thecarboxylic acid agents. the 2 sulphonanil ide agents did not
show a cor relation between their inh ibition of prostaglandinsyn thesis in vuro and anti-inflam matory potency determinedby carrageenan-induced oedema assay in vivo. In fact, R· 805was more potent than diflumidone in vivo whereas in vilro theoppos ite was true. If inhibition of prostaglandin synthesis isrelated to car rageenan- induced inflammation , Ihis lack ofcorrelation may be due to differences of absorption,distr ibution or metabolism . It was concluded that both theseagents owe at least part of their anti-inflamma tory activity toinhibition of prostag landin synthesis.
'Furthermore, in view of the well-documented invotvemem ofplatelet aggregation in the inhibition of arterial thrombosis andthe evidence that aspirin -like drugs may be effective amithrombogenic agents, fu rther evaluation ofR ·805, R-807 andother su((onani/idesfor this indication may be warranted. '
ViCdahl. R.L. and Tukey. R.H.: Biochemical Pharmacoklgy 26: 307 (l 5 Feb 1977)
INPHARMA 21s 1 May; 1977 p8
