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anti-inflammatory
NSAIDs and glucocorticoids
| Question | Answer |
|---|---|
| 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 |
| 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 |
| 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) |
| 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 |
| 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 |
| 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). |
| Ibuprofen | NSAID : propionic acid more selective to cox-2 inhibitors |
| Diflunisal | NSAID : salicylates more selective to cox-2 inhibitors no antipyretic effects |
| 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 |
| 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 |
| Hydrocortisone its pro-drug? | Gp: Glucocorticoids For: anti-inflammation (short acting) Pro-drug (inactive): cortisone converting enzyme: 11(B)-HSD1 |
| Prednisolone its pro-drug? | Gp: Glucocorticoids For: anti-inflammation (short acting) Pro-drug (inactive): Prednisone converting enzyme: 11(B)-HSD1 |
| Dexamethasone 爹曬米花嫂 | Gp: Glucocorticoids For: anti-inflammation (long acting) |
| Betamethasone 病態米花嫂 | Gp: Glucocorticoids For: anti-inflammation (long acting) |
| Side effect of Steroids | 1 . insomnia 2. peptic ulcer 3. fat gian 4. muscle wasting 5. osteoporosis 6. poor wound healing |
| 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 |
Created by:
kopoyeehk
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