Antipyretic, analgesic and anti-inflammatory drugs. Liming Zhou ( 周黎明） Department of pharmacology Huxi medical center Sichuan university. Contents. Overview History Common pharmacological effects Aspirin 阿斯匹林 Selective COS-2 inhibitor Other Drugs. Overview.
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Liming Zhou (周黎明）Department of pharmacology
Huxi medical center
These drugs show the same pharmacological effects
Blocks pyrogen-induced prostaglandin production in thermoregulatory center (CNS)
Heat dissipation ↓
0.5g of aspirin is a weak or mild analgesic that is effective in short, intermittent types of pain as encountered in neuralgia, myalgia (肌肉痛), toothache.
Musculature, dental work , vascular , postpartum conditions, arthritis , bursitis
peripherally -- sites of inflammation
Nerve ending of pain
--kallikrein system mediators
--inhibits granulocyte adherence
--inhibits leukocyte migration
The Mechanism of NSAIDs
The principal pharmacological effect of NSAIDs is due to their ability to inhibit prostaglandin synthesis by blocking the cyclooxygenase （COX） activity of both COX-1 and COX-2.
NSAIDs----- acetylation of COX
(reversible or irreversible)
Symptoms of inflammation
rapidly hydrolyzed --------- acetic acid + salicylate, catalyzed by tissue/blood esterases
dose ＜1g/day：one-order elimination T1/2: 3--5 hrs
dose ＞1g/day：zero-order elimination
do not influence the progress of disease
Reduced platelet aggregation
reduces thromboxane A2 (TXA2) formation
No new COX1 produce
TXA2 production ↓
New COX1produceLow doses 40-100mg/day
5. Other effects
(high doses 3-6g) T1/2 > 12 hours
0 rheumatic fever
0 rheumatoid arthritis
0 other inflammatory joint diseases
GI inflammation : 5-amido-salicylic acid
salicylic acid reaction: Headaches; confusion; hallucinations; tremors; vertigo; behavior disturbance
PGE2 & PGI2↓
Esophagitis; gastric ulcerations; GI hemorrhage
3. Liver & renal toxicity
a potentially fatal disease that causes numerous detrimental effects to many organs, especially the brain and liver.
The disease causes hepatitis with jaundice and encephalopathy
Hematologic: decreased platelet aggregation; prolonged bleeding time.
Exacerbations of asthma
More potent than aspirin
As an anti-inflammatory agent
More adverse reaction
Fewer adverse reaction
Brufen；Benzeneacetic acid； Fenbid； Emodin；Motrin 异丁苯丙酸；异丁洛芬；拔怒风；芬必得；炎痛停；