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22 Cards in this Set
- Front
- Back
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What is the mechanism of action of NSAIDs? |
They inhibit cyclooxygenase |
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What are the indications of NSAIDs? |
- As antipyretics - As antiinflammatory drugs - As analgesics - Dysmenorrhoea - As antiplatelets (only aspirin) - To prevent CRC |
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The prostaglandins and thromboxanes produced by COX1 have which effects on the body? |
- Stimulate platelet aggregation - Protect the gastric mucosa - Vasodilate the afferent arteriole |
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The prostaglandins and thromboxanes produced by COX2 have which effects on the body? |
- Vasodilate the afferent arteriole - Induce fever - Stimulate inflammation by increasing vascular permeability - Increase pain sensitivity - Inhibit platelet aggregation and decrease coagulability (?) |
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Name some non-selective NSAIDs |
Aspirin, naproxen, indomethacin, diclofenac, ibuprofen |
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Name some COX2-preferential NSAIDs |
Paracetamol, celecoxib, meloxicam |
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Name some COX2-selective NSAIDs |
Parecoxib, etoricoxib |
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What are the adverse effects of NSAIDs? |
- Peptic ulcers - Reduced GFR - Prolonged bleeding time - Hypersensitivity reactions (aspirin asthma) - Cardiovascular events (AMI, stroke) - In utero closure of ductus arteriosus |
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What are some common pharmacokinetics of NSAIDs? |
- Most are weak acids - They have strong plasma protein binding - They are actively secreted into tubules |
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What is the main indication of aspirin? |
Aspirin is given in low dose to inhibit platelet aggregation to prevent coronary artery disease and stroke. |
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What is special for the mechanism of action of aspirin compared to other NSAIDs? |
Aspirin is the only irreversible COX inhibitor |
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Which population should never be given aspirin and why? |
Children under 16, as they can develop Rete syndrome, an encephalopathy |
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What is the mechanism of action of paracetamol? |
Paracetamol weakly inhibits COX in the CNS but not in the periphery. It might stimulate descending inhibitory pain pathways. |
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How are the effects of paracetamol different from other NSAIDs? |
Paracetamol has no anti-inflammatory effect. |
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Describe the intoxication of paracetamol. What is the antidote? |
Intoxication of paracetamol causes dangerous levels of the toxic metabolite NAPQI to build up in the liver. The antidote is N-acetylcysteine |
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What are the contraindications for NSAIDs? |
Peptic ulcer
Renal injury or impaired renal circulation Before surgery Pregnancy (except short-term aspirin or paracetamol) |
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Name some drugs NSAIDs can interact with |
Glucocorticoids (both damage the GI mucosa) RAAS-inhibiting drugs (both cause renal damage) |
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How long does the antiplatelet effect of aspirin last? |
7 - 10 days, the whole lifetime of platelets |
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What are the symptoms of aspirin intoxication?
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Tinnitus, hyperpnoea, acid-base disorderes |
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What is the antiplatelet dose of aspirin? |
300 mg saturation dose, 80 - 160 mg/day |
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What is the analgesic and antipyretic dose of aspirin?
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0,5 - 1 g/dose. Max 3 g/day.
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What is the maximum dose of paracetamol every day? |
4 g/day. |
