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19 Cards in this Set
- Front
- Back
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General physiological effects of the NSAIDS
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Analgesic, antipyretic, anti-inflammatory, anti-platelet
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Clinical uses for aspirin and the NSAIDS
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- Low doses: muscle aches, headaches, sprains
- Very low doses: anticoagulant - High doses: used in Tx of severe inflammatory issues (RA) |
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Pharmacokinetics of aspirin
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- Weak acid
- Hydrolyzed to salicylic acid in plasma - Binds strongly to plasma proteins - Massive doses -> "saturation" in the blood - Decomposes in-vitro to salicylic acid +acetic acid |
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Mechanism of action of aspirin
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Inhibits cyclooxygenase
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Antipyretic effects of aspirin
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- Decreases temp in ppl w/ fever; no effect in ppl w/o fever
- Bacterial pyrogens -> inc PGs (ASA blocks this) - May cause peripheral vasodilation - Tx of fever due to viral infection w/ ASA can cause Reye's syndrome (encephalopathy) in children |
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Analgesic effects of aspirin
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- Limited, not for visceral pain
- ASA may work centrally and dec PG production in periphery - Decreases PG that modulate the pain response |
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Anti-inflammatory effects of aspirin
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- Aspirin decreases PG which serve as the initial signals for inflammation
- Inhibits a number of immune cell functions |
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Anticlotting effects of aspirin
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ASA dec platelet aggregation by decreasing production of TXA2 by platelets
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Therapeutic and toxic doses of aspirin
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2 tabs = 650 mg avg dose
For RA - 4 to 6 grams/day Lethal doses: 50-60 tablets for adults (20 grams) and12 tablets in kids (4 grams) |
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Death from aspirin overdose is due to what?
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CNS depression that leads to respiratory failure
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GI effects of aspirin
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- Salicylic acid is a direct irritant
- PGs are necessary for producing GI mucous and bicarbonate |
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Misoprostol
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A PGE2 analog which can restore normal stomach protection, but is an abortifacent
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CNS effects of aspirin
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Tinnitus
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Other effects of aspirin
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Clotting, directly cause miosis, decrease kidney perfusion, bronchospasms in patients w/ nasal polyps, inhibits uterine contractions
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Acetaminophen
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- A COX inhibitor
- Little or no anti-inflammatory/platelet effects - Toxicities: less GI effects, overdose can cause irreversible liver damage due to depletion of SH groups; damage can be avoided if given a SH drug to reduce glutathione |
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Propionic Acid Derivatives- the "Pros" (7)
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1- Ibuprofen
2- Naproxyn 3- Fenoprofen 4- Ketoprofen 5- Flurbiprofen 6- Oxaprozin 7- Suprofen |
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Acetic Acid Derivatives (3)
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1- Indomethacin: very potent COX inhibitor; used to Tx patent ductus arteriosus
2- Tolmetin 3- Sulindac |
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The Other NSAIDS (6)
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1- Pyroxicam
2- Diclofenac 3- Bromfenac 4- Nepafenac 5- Etodolac 6- Nabumetone |
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COX-2 Inhibitor
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1- Celecoxib
SE: increased cardiovascular problems (stroke, MI) |
