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解热镇痛抗炎药 Antipyretic analgesic and anti-inflammatory drugs. 北京协和医学院基础医学院药理学系 叶菜英. Antipyretic analgesic and anti-inflammatory drugs. These drugs relieve the pain associated with inflammation, including that from arthritis and gout. Antipyretic, analgesic, and antiinflammatory drugs.

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antipyretic analgesic and anti inflammatory drugs

解热镇痛抗炎药Antipyretic analgesic and anti-inflammatory drugs

北京协和医学院基础医学院药理学系

叶菜英

antipyretic analgesic and anti inflammatory drugs2
Antipyretic analgesic and anti-inflammatory 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.

Classed into non-steroidal anti-inflammatordrugs (NSAIDs) in 1974.

slide3

Antipyretic action

hypothalamus

antipyretic analgesic

external fever

endogenous pyrogen

PL

virus

bacteria

Bacterial product

endotoxin

TD

Ag-Ab

phagocyte (GC)

inhibition

unsaturated fatty acid

PGS

PG

TEMP SET cells

febrile

slide4

Antipyretic action

  • Febrile:

endogenous pyrogen→CNS→release PG↑ →thermotaxic center → Febrile

  • Antipyretil:inhibit PG synthetase,decrease synthesis of PG →hypothermy
analgesic action
Analgesic action

depression

bradykinin painsensor

antipyretic analgesic painstimulusPG

PG synthesissensitization

depression

analgesic action6
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.

slide7
Anti-inflammatory action
  • Mechanisms:Inhibit a primary pathway

in PG synthesis.

  • Summary:Inhibit the PG synthesis to antipyretil,

analgesic and anti-inflammatory

slide8
解热镇痛抗炎药分类
  • 水杨酸类:

阿司匹林等

  • 苯胺类:

对乙酰氨基酚(扑热息痛)等

  • 吡唑酮类:

保泰松、羟基保泰松等

  • 芳基烷酸类:布洛芬、炎痛喜康等
aspirin
Aspirin

【physiological disposition】:

Oral, absorbed from gut→distribution, metabolism→kenosis(enter articular cavity, CSF)

aspirin11
Aspirin

【Pharmacological action】

  • Atipyretic: temperature drop qiuckly
  • Analgesic:medium intensity
  • Anti-rheumatic: inhibit antigen-antibody reaction, antibody formation, antigen antibody union,blood sedimentation↓, relieve flare of articulus.
aspirin12
Aspirin

【 Clinical Indications 】

Antipyretic analgesic and anti –inflammatory

  • Headache,toothache, algomenorrhea,

neuralgiacourbature, arthralgia.

  • Fever
  • Acute rheumatism, rheumatoid arthritis
aspirin13
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 Indications: low dose, long term use could prevent

CHDthrombosis, cerebral thrombosis

aspirin14
Aspirin

【Untoward reaction】

  • Gastrointestinal tract reaction
  • Block blood coagulation
  • NS reaction: salicylism, nausea, vomiting,

dizziness, tinnitus, acouesthesia↓

  • Anaphylactic response
  • Nephrotoxicity
slide15

Aniline Paracetamol

Paracetamol & Phenacetin

【Pharmacological action】

  • Strong antipyretic analgesic effect;
  • weak anti-rheumatic effect.

(inhibition for center epoxidase is

stronger than that for external

epoxidase)

Phenacetin

P-aminophenetole

Paracetamol

p henacetin
Phenacetin

【Pharmacokinetics】

Oral, absorb→hepatic metabolism →kenosis

↗ 60%combine with GA

de-ET(70%-80%)→Paracetamol→35%combine with H2SO4,fail

↗↘bare→hydroxide

Phenacetin

de-Ac→P-aminophenetole→hydroxide→hemoglobin →oxidationmetahemoglobin ↓

toxic metabolin

paracetamol phenacetin
Paracetamol & Phenacetin

【Untoward Reaction】

  • Allergy occasionally: rash, drug fever, M.M damage
  • Overdose (10~15g∕day)→acute poisoning→hepatonecrosis
  • Overdose→methemoglobinemia, cyanosis, hypoxia, HA
  • Kidney damage
slide18

Pyrazoketone

Phenylbutazone (保泰松)

【Pharmacologic action】

Strong anti-inflammatory, anti-rheumatic effects, but weak atipyretil, analgesic effects.

Primary used to rheumatism and rheumatoid arthritis

slide19

Pyrazoketone

Phenylbutazone (保泰松)

【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)

slide20

Phenylbutazone (保泰松)

【Side effects】

  • Stomach intestine reaction
  • Water-sodium retention
  • Anaphylactic respons
  • Liver&kidney damage
  • Thyromegaly and myxedema
slide21

Organic acids

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), CNS reaction,

Inhibit hematopoietic system, anaphylactic response

brufen fenbid
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.
compound preparation 67 types
Compound preparation (67 types)
  • Coldrine
  • Compound Aminopyrine Phenacetin Tablets
  • APC
  • Pseudoephedrine+Paracetamol+Dextromethorphan+

Chlorphenamine Maleate

  • Paracetamol
  • Compound Chlorphenamine Maleate

【Essential component】

  • APC: aspirin paracetamol caffeine
  • Somedon: aminophenazone PAC caffeine
thanks
Thanks!

Thanks!