上浒充通大学 SHANGHAI JIAO TONG UNIVERSITY Phospholipase 1896 1920 1987 2006 Steroids Arachidonic acid Cyclooxygenase Lipoxygenases NSAIDs Lipoxygenase inhititors Prostaglandins PMNs PGF2a PGE2 PGL, ON Lymphokines algesic pyrexia vasodilation The events of the inflammtory response and mechanisms of anti-flammatory
Phospholipase Arachidonic acid Cyclooxygenase Lipoxygenases ----- Steroids NSAIDs ----- Prostaglandins PGF2α PGE2 PGI2 algesic pyrexia vasodilation PMNs Lymphokines ----- Lipoxygenase inhititors The events of the inflammtory response and mechanisms of anti-flammatory
上降充通大警 SHANGHAI JIAO TONG UNIVERSITY 1896 1920 1987 2006 Pharmacological Effects Diverse group of chemicals,but all inhibit cyclooxygenase. Resultant inhibition of PG synthesis is largely responsible for their therapeutic effects. But,inhibition of PG synthase in gastric mucosa>GIT damage(dyspepsia, gastritis)
Pharmacological Effects • Diverse group of chemicals, but all inhibit cyclooxygenase. • Resultant inhibition of PG synthesis is largely responsible for their therapeutic effects. • But, inhibition of PG synthase in gastric mucosa GIT damage (dyspepsia, gastritis)
上降充通大警 SHANGHAI JIAO TONG UNIVERSITY 1896 1920 1987 2006 Common Adverse Effects Platelet Dysfunction Gastritis and peptic ulceration with bleeding (inhibition of PG+other effects) Acute Renal Failure in susceptible o Sodium+water retention and edema Increase in risk of cardiovascular events Hypersensitivity(not immunologic but due to PG inhibition) ·Headache,dizziness
Common Adverse Effects • Platelet Dysfunction • Gastritis and peptic ulceration with bleeding (inhibition of PG + other effects) • Acute Renal Failure in susceptible • Sodium+ water retention and edema • Increase in risk of cardiovascular events • Hypersensitivity (not immunologic but due to PG inhibition) • Headache ,dizziness
上降充通大警 SHANGHAI JIAO TONG UNIVERSITY 1896 1920 1987 2006 Non-steroidal anti-inflammatory drugs (NSAIDs) An anti-inflammatory action: (1)The decrease in vasodilator prostaglandinds (PGE2,PGI,)means less vasodilatation and, indirectly,less edema (2)The inhibition of activity of adhesion molecule. (3)Accumulation of inflammatory cells is also reduced
Non-steroidal anti-inflammatory drugs (NSAIDs) • An anti-inflammatory action: (1) The decrease in vasodilator prostaglandinds (PGE2 , PGI2 ) means less vasodilatation and, indirectly, less edema. (2) The inhibition of activity of adhesion molecule. (3) Accumulation of inflammatory cells is also reduced
上降充通大警 SHANGHAI JIAO TONG UNIVERSITY 1896 1920 1987 2006 Non-steroidal anti-inflammatory drugs (NSAIDs) .An analgesic effect:decreased prostaglandin generation means less sensitisation of nociceptive nerve endings to inflammatory mediators such as bradykinin and 5-hydroxytryptamine Relief of headache is probably due to decreased prostaglandin-mediated vasodilatation
Non-steroidal anti-inflammatory drugs (NSAIDs) • An analgesic effect: decreased prostaglandin generation means less sensitisation of nociceptive nerve endings to inflammatory mediators such as bradykinin and 5-hydroxytryptamine. • Relief of headache is probably due to decreased prostaglandin-mediated vasodilatation