Antipyretics-analgesics and antiinflammatory agents - PowerPoint PPT Presentation

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Antipyretics-analgesics and antiinflammatory agents

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Title: PowerPoint Author: kubs Last modified by: Tianluo Created Date: 9/7/1998 1:31:14 AM Document presentation format: (4:3) – PowerPoint PPT presentation

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Title: Antipyretics-analgesics and antiinflammatory agents


1
  • ???????
  • Antipyretics-analgesics and antiinflammatory
    agents
  • ?.????
  • (?)??????(non steroidal anti inflammatory
    drugs ,NSAIDs) ?????????????????????
  • ?????(????),???(??????),????(???),
  • ??????(?????????????????)

2
  • (?)??????
  • ???? ????A2??????????
  • ?????????(cyclo-oxygenase,COX )?
  • ??????(PGG, PGH)?????PGI2
  • (????,???????,?????),
  • PGE2?PGF2 (??????????),
  • TXA2(???,???????,????)??pp17?
  • ?????????????,?????????,?????

3
  • (?)????(PGs)???????????
  • 1.???? ?PGE2??,??????
  • ??(?????????????)???????????????????????? PGE???
    ?????????????????
  • 2. ???? ? PG?????,???????????????????????
    ???
  • 3.???? PG?????,??????????????,?????????,
  • ???????????????

4
  • ?.  ????
  • (?)????(aspirin)?pp16?
  • 1.???? ????????????,
  • ????,pKa?3.5,?????????????,???????8090,
  • ?????????????????,???
  • ?????(1???)????????,t1/2 23??,???????????
  • ?????(1???)?????????,??????????,????,
  • ???????????,????????????,???????,???16??

5
  • 2.????
  • ?????(cyclo-oxygenase ,COX),
  • ??PGs???COX?COX1?COX2 ,
  • COX1??constitutive enzyme,????????,?????,?????????
    ????????,??????
  • COX2???????iL-1?TNF???,??COX2???????????.
  • ??????????,??????
  • ?????(??cox2/cox1? IC50)?COX1-aspirin(166),
  • ????piroxicam(600),????indomethacin(60)
    ?COX2-????( nimesulide ) (0.007),???ibuprofen
    (15) ?????????naproxen(0.8)

6
  • 3.?????????
  • 1/ ???????? ???,
  • ??????,??????????????
  • ?????12????,????????????,
  • ???????????????,??????????,?????
  • 2/ ??????
  • ???(4080mg)?????????TXA2??,???????,??????????
  • ???????????PGI2?????????TXA2,??????,?????????

7
  • 4.????
  • 1/ ????? ?????????????,???????????,?????????
    ,?????????(PGE)???
  • 2/ ???? ??????????
  • 3/ ????? ??????????????????????????????????
  • 4/ ???? ??????,??????,??PG?????LTs,?????????
  • 5/ ??(Reye)??? ????????????????,???????????,??,
    ???(30???)??????? ?pp18?

8
  • (?)??????(acetaminophen)
  • 1.???
  • ????????????,?????(phenacetin)??????,
  • Phenacetin?????,??????????
  • ?????????????????????,????????(???)??pp19?
  • 2.????????? ??????
  • ???????COX,?????????,
  • ????????????,??????
  • 3.???? ?????????

9
  • (?)???(phenylbutazone)
  •   1.??????????(98),t 1/2 5065??,
  • ????????(???3??)?????,
  • ?????????????,????????,????????,
  • ??????????
  • 2.????
  • ??????????????,????????????????????,
  • ????????

10
  • 1. ???????
  • 1/ ?????,??????
  • 2/ ????,???????????
  • 3/ ????,???????????,???????
  • 4/ ????,??????????
  • 5/ ???????,??????????????
  • 6/ ???????????????????,
  • ??????????,????????????????????????????????

11
  • (?)????(indomethacin)
  •   1.???? ?????????,??????????????????
  • 2.??????? ?????????????????????,???????
  • ???????????????
  • ???????,????????,???
  • ???,????????,???????,????????

12
  • (?)???(ibuprofen)
  • ???2-???(4-?????)??
  • ?????? ?pp20?
  • ????????,???,??,
  • ?????????????,????????,???????????
  • ????????????????
  • ?????aspirin?,??
  • ??,??????2(?1?Piroxicam),??????,??????????(1997).

13
  • ?.????????????
  • 3.1????
  • 1899?????????(???NSAIDs),???????????
  • 20??50????????????,????????,???20????????,???????
    ?
  • 60??????,????????????,???,?????????????,?????,????
    ?????????,?????????????
  • 70???????????????????,????????????????????
  • 80????????????
  • 90?????????-2(COX-2)???,???
  • ??????????,?????????????

14
  • 3.2 ??
  • ??????(NSAIDs)????????????????
  • ?????????????????????????????(?????????????)??????
    ????????????????????????1991?NSAIDs???70???
  • ????????????,????????????,?????????,???????
  • ??NSAIDs????????????????????????????????

15
  • 3.3 ??
  • 3 .3 .1 ????,???????,?????????????,??????????????
    ?????
  • 3 .3 .2 ????????????????????,????????.???????????
    ????.
  • 3.3..3 ??????????????????????????????????????,???N
    SAIDs???
  • 3.3..4 ????? ,?????????,???????,???????????,
  • 3.3.5 ????????????? ??????????????????NSAIDs?50,?
    ?????????????????????????
  • 3.3.6 ??????????????????,??????NSAIDs???????????95
    .

16
?
17
?
18
?
19
?
20
?
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