??????? ANTIPYRETIC ANALGESIC AND ANTI-INFLAMMATOGY DRUDS

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???????ANTIPYRETIC ANALGESIC ANDANTI-INFLAMMATOG
Y DRUDS

• ????????????????
• ???

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???????antipyretic, analgesic, and
antiinflammatory drugs

• These drugs relieve the pain associated with
  inflammation,including that from arthritis and
  gout.
• ?????????
• (antipyretic, analgesic, and antiinflammatory
  drugs)?
• They produce their anti-inflammatory action
  through a different mechanism,not as
  glucocorticoid.
• 1974???????????
• ????????
• (non-steroidal anti-inflammatordrugs,NSAIDs) ?

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???????

• ???? Antipyretil action

hypothalamus
antipyretic analgesic
external fever
endogenous pyrogen
PL
virus bacteria Bacterial product endotoxin TD Ag-A
b
phagocyte (GC)
inhibition
unsaturated fatty acid
PGS
PG
TEMP SET cells
febrile
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???????Antipyretic analgesic and anti
inflammatory drugs

• ???? Antipyretil action
• Febrileendogenous pyrogen ?CNS
• ?release PG? ?thermotaxic center ?
  Febrile
• Antipyretil inhibit PG synthetase,decrease
  synthesis of PG ?hypothermy

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???????Antipyretic analgesic and anti
inflammatory drugs

• ???? analgesic action
• depression
• bradykinin
  pain sensor
• antipyretic analgesic painstimulus PG
• PG synthesis
  sensitization
• depression

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???????Antipyretic analgesic and anti
inflammatory drugs

• ???? analgesic action
• Mechanisms
• Effect on periphery,inhibit the synthesis of
  prostaglandins and prevent bradykinin from
  stimulating pain receptors,also inhibit the
  recognition of pain impulses centrally and
  peripherally.

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???????Antipyretic analgesic and anti
inflammatory drugs

• ????Anti-inflammatory action
• Mechanisms Inhibit a primary pathway
• in PG synthesis?
• Summary Inhibit the PG synthesis to
• antipyretil, analgesic
  and Anti-inflammatory

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Classification

• ??? (Salicylates) ?
• ????aspirin?
• ??? (Aniline)
• ??????acetaminophen
• (????)?
• ??? (Pyrazoketone) ?
• ???Phenylbutazone??????Oxyphenbutazone?
• ????????brufen?????Piroxicam?

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??????? ???? ????
???? Aspirin
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????Salicylates???? aspirin

• ?physiological disposition?
• oral?absorbed from gut?distribution,
  metabolism?kenosis
• (enter articular cavity?CSF)

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???? aspirin

• ?Pharmacological action?
• Atipyretiltemperature drop qiuckly
• Analgesic medium intensity
• Anti-rheumaticinhibit antigen-antibody
  reaction,antibody formation
• antigen antibody union,blood
  sedimentation?,relieve flare of articulus.

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???? aspirin

• Clinical Indications Antipyretic analgesic and
  anti inflammatory
• headache,toothache,algomenorrhea,
• neuralgiacourbature,arthralgia?
• fever
• acute rheumatism,rheumatoid arthritis

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???? aspirin

• ? Pharmacological action Clinical Indications ?
• Effect on thrombosis
• Inhibit cycloxygenase
  cyclo-oxygenase,reduce TXA2 synthesis
• Inhibit PA effect on
  thromboxane synthesis
• 
  aspirin TXA2synthetase
• 
  
• PM phospholipid AA
  endoperoxide? TXA2?
• 
  
• thrombosis?
  PA? platelet releasion?
  
• 
  
• Clinical Indicationslow dose,long term use could
  prevent CHDthrombosis,cerebral thrombosis

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Salicylates???? aspirin

• ?Untoward Reaction?
• Gastrointestinal tract reaction
• Block blood coagulation
• NS reactionsalicylism,nausea?vomiting?
• dizziness?tinnitus?acouesthesia?
• Anaphylactic response
• Nephrotoxicity

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??????? ??? ??????
?????? paracetamol (????) ???? phenacetin
Pharmacologic action
Phenacetin
strong antipyretil analgesic effect weak
anti-rheumatic effect(inhibition for center
epoxidase is stronger than that for external
epoxidase)
P-aminophenetole
Paracetamol
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???? phenacetin

• ?Pharmacokinetics?
• Oral,absorb?hepatic metabolism ?kenosis
• 
  ? 60combine with GA
• de-ET(70-80)?Paracetamol?35combine
  with H2SO4,fail
• ?
  ?bare?hydroxide
• ????
• ?
• de-Ac?P-aminophenetole ?
  hydroxide?hemoglobin ?oxidation metahemoglobin
  
  
  ?
• ???????
  

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??????(????),????phenacetin

• ?Untoward Reaction?
• Allergy occasionally rash?drug fever?M.M damage
• overdose(10-15g/day)?acute poisoning?hepatonecrosi
  s
• overdose?methemoglobinemia,cyanosis,hypoxia ,HA
• Kidney damage

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??????? ????
??? phenylbutazone
Pharmacologic action
Strong anti-inflammatory, anti-rheumatic effects
,but weak atipyretil,analgesic effects?
Primary used to rheumatism and rheumatoid
arthritis
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???pyrazoketone????phenylbutazone

• ?Physiological disposition?
• Oral to absorb,penetration synovia membrane?the
  concentration in synovia intermembrance space is
  50 of that in blood(high concentration in joint
  tissue )

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???phenylbutazone

• ?Side effrcts?
• Stomach intestine reaction
• Water-sodium retention
• Anaphylactic respons
• Liverkidney damage
• Thyromegaly and myxedema

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??????? ????
???? indometacin (???)
One of the most potent inhibitors of COX
isozymes Effects on inflammatory,atipyretil
analgesic and rheumatism significantly Use to the
cases which difficult to cure above-mentioned?
Untoward Reaction
Lots of untoward reaction,high incidence rate,
Stomach intestine reaction (ulcer)?C.N.S
reaction? Inhibit hematopoietic
system?anaphylactic response
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????????Brufen ???fenbid

• Pharmacologic action
• Less stomach intestine reactions,good tolerance
• 99 combine with plasma-albumin?enter synovial
  membrane tune slowly,keep high concentration
• Effect is similar with aspirin,stronger than
• Paracetamol
• used to rheumatism and rheumatoid arthritis
• light dyspepsia,rash occasionally

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Compound preparation (67types)

• Coldrine
• Compound Aminopyrine Phenacetin Tablets
• APC
• PseudoephedrineParacetamolDextromethorphan
• Chlorphenamine Maleate
• Paracetamol
• Compound Chlorphenamine Maleate
• Essential component
• APC aspirin paracetamol caffeine
• ??? aminophenazone PAC caffeine

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