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NSAIDS

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Name 8 other side-effects are associated with acetyl-salicylate?
1) Anorexia

2) Vomiting

3) Hemorrhage

4) GI ulceration

5) Nephrotoxicity

6) Hepatotoxicity

7) Blood dyserasia

8) Hypersensitivity
Name 10 drugs that are classified as NSAIDS.
1) Acetyl-salicylate (aspirin)

2) Acetominophen

3) Phenylbutazone

4) Carprofen

5) Flunixin (banamine)

6) Ketoprofen

7) Naproxen (alleve)

8) Piroxicam

9) Carbolic Acids (etodolac)

10) Miloxicam
What is the mechanism for acetominophen?
centrally active
What are the 2 secondary effects of NSAIDS, in general?
1) Antithrombotic: bind COX-1 in platelets, inhibiting TXA2 and clotting

2) Renal vasodilation by closing of efferent arterioles/opening of afferents
What is the indication for acetominophen?
pain relief ONLY
What 2 AMDE aspects that are related to NSAIDS, in general?
1) HUGE variation in T1/2 of elimination among species and among individuals within species

2) HIGHLY PROTEIN BOUND (phase I and II)
What are the 7 contraindications associated with acetyl-salicylate?
1) Gastric ulcers (w/ glucocorticoids)

2) Anticoagulants (compete for protein binding sites)

3) Renal/hepatic disease

4) Late pregnancy

5) GI ulcers

6) Dehydration

7) Inhibit excretion (w/ Digoxin)
What are the 4 primary effects that NSAIDS produce, in general?
1) Decrease eicosanoids (thromboxane, prostacycline, prostaglandins)

2) Inhibit pain centrally

3) Decrease peripheral "pain threshold"

4) Decrease fever (decrease PGE)
What is the primary effect of acetominophen?
inhibits pain centrally
What are the 2 mechanisms used by acetyl-salicylate?
1) Acetylates irreversibly bind COX-1

2) Affect opiate receptors (CNS)
Name 8 other effects of NSAIDS, in general.
1) Anorexia

2) Vomiting

3) Hemorrhage

4) GI ulceration

5) Nephrotoxicity

6) Hepatotoxicity

7) Blood dyserasia

8) Hypersensitivity
Name 7 contraindications for NSAIDS, in general.
1) Gastric ulcers (w/ glucocorticoids)

2) Anticoagulants (compete for protein binding sites)

3) Renal/hepatic disease

4) Late pregnancy

5) GI ulcers

6) Dehydration

7) Inhibit excretion (w/ Digoxin)
What are the 4 indications of NSAIDS, in general?
1) Reduce inflammation (eg arthritis, fever)

2)Reduce pain (eg colic)

3)Prevent pain (eg perioperative)

4) Prevent endotoxic shock
What are 3 indications for acetyl-salicylate?
1) Reduce inflammation

2) Reduce pain

3) Inhibit clotting
What are the 4 primary effects of acetyl-salicylate?
1) Decrease eicosanoids (thromboxane, prostacycline, prostaglandins)

2) Inhibit pain centrally

3) Decrease peripheral "pain threshold"

4) Decrease fever (decrease PGE)
What is the relationship of COX-1 and -2 with regards to NSAIDS, in general?
COX-2:COX-1 should be <1
What are the 3 mechanisms used by NSAIDS, in general?
1) Inhibit cyclo-oxygenase I or II

2) Affect opiate receptors (CNS)

3) Variations on these themes
Name the AMDE associated with acetyl-salicylate.
Very long T1/2 in CAT
What are the 2 secondary effects of acetyl-salicylate?
1) Antithrombotic: bind COX-1 in platelets, inhibiting TXA2 and clotting

2) Renal vasodilation by closing of efferent arterioles/opening of afferents

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