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25 Cards in this Set
- Front
- Back
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Molecule responsible for inflammation? |
Prostaglandins |
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Where do PG come from? |
Arachidonic acid |
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Function of prostaglandins |
Increase vasopermeability - Dilate precapillary arterioles - Promote blood clotting |
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What is the common precursor to all PGs? |
PGH2 |
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How do we prevent Arachidonic acid formation? |
Steroid inhibitors |
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How do we inhibit cyclooxygenase? (Enzyme to create PG). |
COX Inhibs |
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Which PG types have opposite effects? |
PGI2 (Dilation) TXA2 ( Constriction) |
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What is the mechanism of Aspirin? |
Acetylation of serine in the active site to block access to arachidonic acid. |
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Which COX enzyme contains a hydrophobic pocket? |
Cox 2 |
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How do NSAIDs effect COX enzymes? |
They will block the opening (Arg 120) - Reversible |
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How do COXibs effect COX enzymes? |
Will only block the opening of the COX2 enzyme - Irreversible |
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How does ASA effect COX enzymes? |
Acetylation of both COX |
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Which COXib is still on the market? |
Celecoxib |
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How do COXibs and non-selective NSAIDS produce hypertension? Mechanism 1 |
Cox helps to dilate blood vessels and balance out vasoconstriction caused by LOX enzyme. When COX is inhibited there is no vasodilation and all precursors are sent into th LOX pathway which increase vasoconstriction even further. |
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How do COXibs and non-selective NSAIDS produce hypertension? Mech. 2 |
These drugs will increase the sodium concentration and thus blood pressure. Dilated bloodvessels are needed for GFR to take place |
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NSAID effect on stomach mucosa |
NSAIDS can increase the levels of acid in the stomach by inhibiting PG since PG are inhibitory of acid secretion in the stomach. We can co-treat with Mesoprostol. |
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What drug? - Salicylate - Mild pain and inflammation |
Aspirin |
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What drugs? - Acetic Acids |
Indomethacin Sulindac |
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What drug? - Propionic acid - For RA and Dysmenorrhea - Accumulation in synovial fluid |
Ibuprofen |
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What drug? - Propionic Acid - Inflammation and RA/Gout |
Naproxen |
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What drug? - Oxicams - Prolonged half-life due to enterohepatic circulation |
Piroxicam |
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How do NSAIDS inhibit pain and fever? |
PG can use Gprotiens to polarize membrane aiding in nociception. PG also effect basal body temperatures which can lead to high temperatures during an infection |
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How does aspirin induce asthma? |
- COX 1 inhibition - Most likely related to inhibition of PGE2 prouction - NSAIDS also release cys-leukotrienes |
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Side effects of NSAIDs and COXibs? |
- GI Upset - Aspirin induced asthma - Reyes Syndrome - Dose-dependent urate accumulation - High BP - Bleeding |
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Explain acetaminophen toxicity. |
High does will lead to a saturation of conjugates preventing the expelling of toxic metabolites |
