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26 Cards in this Set
- Front
- Back
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What are the 3 main effects of NSAIDs?
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Anti inflammatory
Antipyretic Analgesic |
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Describe the arachidonic acid cycle in inflammation, pain and fever.
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Triglycerides can become Platelet activating factor or they can become arachidonic acid via phospholipase A2. Arachidonic acid is then converted to several different prostaglandins via cyclooxygenase.
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What produces PAF and when is it produced?
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Neutrophils, macrophages, basophils, eosinophils, platelets and endothelial cells in response to inflammatory (LPS, TNF-alpha) and phagocytic stimuli.
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NSAIDs inhibit COX 1 and 2. When are these two enzymes expressed?
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COX-1 - constitutively
COX-2 - induced by injury They block prostaglandin synthesis. Side effects are due to this feature. |
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Draw salicylic acid.
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Salicylic acid
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Name the 5 major classes of NSAID and an example drug for each class.
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Salicylates (aspirin)
para-Aminophenol derivatives (acetaminophen) Arylalkanoic acids (Ibuprofen) Diaryl substituted furanones (vioxx) Pyrazoles (celebrex) |
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Draw the salicylate ion and describe its structure activity relationship.
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Salicylate ion = Comes from Na, Mg, choline salts. Less acidic, Less GI problems
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Draw Salicylamide and describe its structure activity relationship.
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Salicylamide = analgesic, not anti-inflammatory, Less GI problems
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Draw benzoic acid and describe its structure activity relationship.
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Benzoic acid = weak activity
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What happens to the compounds activity if the hydroxyl group is moved to the meta or para positions?
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Not active.
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What are the therapeutic effects of acetaminophen?
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Analgesic
Antipyretic Little anti-inflammatory ability |
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Explain why acetaminophen can become hepatotoxic.
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Its hydroxyl group can be hydrolized to a quinone which is hepatotoxic especially with ethanol consumption.
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What is unique about aspirin compared to other NSAIDs?
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It is an irreversible inhibitor
Inhibits COX-1 and decreases thromboxane formation (helps forms clots) |
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What is Indomethacin?
What is it used for? What are its limitations? |
Very potent NSAID. Anti-inflammatory, anti-pyretic, analgesic.
Used in Gout and arthritis Can only be used for a short period of time. Causes GI problems |
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Draw indomethacin. Point out important structural features.
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Indomethacin
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What is Sulindac?
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A prodrug derived from indomethacin with less severe side effects but lower antipyretic and anti-inflammatory activity.
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Draw Sulindac and point out important structural features.
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Sulindac
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What is Diclofenac?
How does it work? What is it used for? |
A leading NSAID.
Inhibits COX to decrease prostaglandins, lipooxygenase to decrease leukotrienes and arachidonic acid re-uptake Used for long term treatment of arthritis More potent antipyretic and anti-inflammatory than aspirin |
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What is Etolodac?
How does it work? |
A type of Arylalkanoic acid
More selective for COX-2 than 1 so less GI problems |
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What is Nabumetone?
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Non-acidic prodrug NSAID.
Decreased GI irritation, potency, and less severe side effects |
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What is the structural difference between COX 1 and 2?
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COX-2 has a larger NSAID binding site.
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What 2 drugs are COX-2 selective?
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Celecoxib (Celebrex)
Rofecoxib (Vioxx) - pulled from market |
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Why are selective COX-2 inhibitors important?
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They are less irritating on the GI than COX-1 inhibitors.
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What 3 metabolic processes are focused on in the treatment of Gout?
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Increasing uric acid excretion
Inhibiting xanthine oxidase (uric acid biosynthesis) Reducing inflammation |
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What is Gold used for therapeutically?
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Rheumatoid arthritis
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What is the MOA glucocorticoids use to reduce inflammation?
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They inhibit Phospholipase A2 in the conversion of Diacylglyercol or phospholipids to arachidonic acid.
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