NSAIDs and glucocorticoids
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| Abnormal Immune Responses? | 1. Extensive tissue damage (Hypersensitivity)
2. Reactivity against self its own cells and tissues(antoimmunity)
*炎症: 自身免疫系統過敏,攻擊自身
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| Pharmacological Actions of NSAIDs | 1. Anti-inflammatory
- reduce vasodilation and vascular permeability
- reduce edema, swelling and redness
2. Analgesic
- reduce sensitization of pain nerve endings
3. Antipyretic
- reduce set-point of hypothalamic themoregulatory center
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| Side-effects of normal NSAIDs [ both cox-1 and cox-2 inhibitors) | 1. GI (GI disorder)
2. Platelets (prolonged bleeding,aspirin:anti-platelet)
3. Kidneys (nephropahty 腎痛)
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| Mechanism of NSAIDs | inhibit cyclooxygenase 1 and 2
-> COX catalyzes the formation of Eicosanoids e.g. prostaglandins and thromboxane from arachidonic acid (derived from phospholipid bilayer by phospholipase)
-> Prostaglandins as messenger molecules in inflammation
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| why selective cox-2 inhibitors of NSAIDs better? e.g.? disadvantage? | e.g. celecoxib [coxb]
selective COX-2 inhibitor x cause gastric problems,less effect on platelet
i.e. cox-2 is inducible which only act on the inflammatory sites, cox-1 is constitutive 固有的 (保護GI,platelet)
Bad: renal deficiency 腎虧,thrombosis (coagulatio
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| Aspirin | NSAID : salicylates
cox-1 selective salicylates 水楊酸
mainly for anti-platelet drug
cox-2 is inducible which only act on the inflammatory sites, cox-1 is constitutive 固有的 (保護GI ,platelet).
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| Ibuprofen | NSAID : propionic acid
more selective to cox-2 inhibitors
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| Diflunisal | NSAID : salicylates
more selective to cox-2 inhibitors
no antipyretic effects
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| Paracetamol / Acetaminophen | weak cox-1 n cox-2 inhibitor
NOT NSAID! non-opiod anaglestic
lack of anti-inflammatory effect!
anaglesic effect + antipyretic
SE: hepatotoxity if 8 x 500mg in a day
anti-dose: Fluimucil
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| Pharmacological Actions of Glucocorticoids 糖大白咬前列腺 | 1. cause vasoconstriction [大]and reduce capillary permeability
2. inhibit white cell [白]adhersion with endothelial cells
3.inhibit the function of macrophages [咬]and other APCs (reduce phagocytosis and T cell activation )
4. Inhibit production of prost
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| Hydrocortisone its pro-drug? | Gp: Glucocorticoids
For: anti-inflammation (short acting)
Pro-drug (inactive): cortisone
converting enzyme: 11(B)-HSD1
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| Prednisolone its pro-drug? | Gp: Glucocorticoids
For: anti-inflammation (short acting)
Pro-drug (inactive): Prednisone
converting enzyme: 11(B)-HSD1
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| Dexamethasone 爹曬米花嫂 | Gp: Glucocorticoids
For: anti-inflammation (long acting)
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| Betamethasone 病態米花嫂 | Gp: Glucocorticoids
For: anti-inflammation (long acting)
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| Side effect of Steroids | 1 . insomnia
2. peptic ulcer
3. fat gian
4. muscle wasting
5. osteoporosis
6. poor wound healing
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| Withdrawal of Steroids | *step down before withdrawal *
nd 2-12 ms for recovery of adrenal function
anohter 6-9 ms for recovery of steroids lv
or else -> cause adrenal insufficiency 腎虧
- hypoglycaemia (自己唔識出glucocorticoids
=> iatrogenic 醫源性的Addison's disease)
-> circulatory
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