Nsaids

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Mechanism for Aspirin

Back 1

Irreversible inhibition of COX-1 > COX-2
Rapid absorption and distribution
-Buffers (speed dissolution process, reduce GI irritation)
-Inhibits platelet aggregation TXA2 inhibition > PGI2. The TXA2 stimulates aggregation and PGI2 inhibits aggregation so inhibits more the platelet aggregation.
-Inhibition of COX is irreversible (duration of action equals 8-10 days)
-Can be diurtiec in nature.

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Indications for Aspirin

Back 2

-Analgesia – peripheral (via COX inhibition) and CNS
-Antipyresis – lowers the set point of hypothalamic thermostat; augments heat dissipation mechanisms
-Antiinflammatory – inhibits PG role in inflammation
-GI effects – due to direct irritation and COX inhibition (indigestion, nausea, gastritis, bleeding, ulcers)

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Advantages of Aspirin

Back 3

-↓ risk of colon cancer

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Disadvantages of Aspirin

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Fluid retention and renal damage
-Tinnitus
-Impaired hearing
-Vertigo
-Hypersensitivity – allergy like symptoms
-Reye’s Syndrome - Vomiting, lethargy, associated with children with viral infections.

Front 5

Mechanism of ibuprofen

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Reversible inhibtion of COX 1 and COX 2.
Inhibit platelet aggregation

Front 6

Indications of ibuprofen

Back 6

Reversible inhibition of cyclooxygenase
-Analgesic, antipyretic, and anti-inflammatory
-Half life determines dose interval; Potency determines tablet size

Front 7

Advantages of ibuprofen

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More potent and more expensive than aspirin
-Available OTC, topical gels, or patches

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Disadvantages of ibuprofen

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May cause fluid retention or overt kidney damage in compromised patients
-GI irritation and erosions
-Cross-hypersensitivity with aspirin

Front 9

Mechanism of celecoxib

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Selective COX-2 inhibitor.
Inhibits COX-2 without altering activity of COX-1

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Indications of celecoxib

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-Theory: retain anti-inflammatory efficacy with a lower incidence of side effects

Front 11

Advantages of celecoxib

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-Lower incidence of GI complaints
-Little or no inhibition of platelet aggregation

Front 12

Disadvantages of celecoxib

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-Renal and hepatic toxicity still present
-↑ risk of heart attacks and strokes

Front 13

Mechanism of acetaminophen

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-Rapid absorption and distribution
-Probably acts only in CNS
-Weak peripheral COX inhibitor

Front 14

Indications of acetaminophen

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-Aspirin substitute
-Especially indicated for children with viral infections, patients with hypersensitive to aspirin, patients with clotting abnormalities, patients with ulcers
-Analgesia and antipyresis only – no PG related effects

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Advantages of acetaminophen

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Children use it when they have infections.

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Disadvantages of acetaminophen

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-Hepatotoxicity
-Renal toxicity
-Cannot substitute for aspirin when inflammation is present

Front 17

Mechanism that is the inhibtion of the enzyme COX.

Back 17

Decrease the production of prostaglandins (PG), Postacyclin (PGI2), and thromboxanes (TX)

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COX 1: The enzyme

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Found in the gastric mucosa, kidney and platelets and is a constitutive enzyme.

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COX 2:

Back 19

Highly inducible form. The activity of it increases during the inflammatory response and the synthesis is induced by cytokinesis

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NSAID disadvantages

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Loss of PG vasodilation effects.
Can interfere with antihypertensive drugs such as diuretics and ACE inhibitors due to the prostaglandin effects.