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27 Cards in this Set

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NSAIDs:

- mechanism of action
- reversibility?
Nonselective COX inhibitor, thus decreasing production of prostaglandins and thromboxanes.

Reversible
Differentiate between COX-1 and COX-2.
COX-1 is ubiquitous

COX-2 is induced by inflammation/injury
General Pharmacological Actions of NSAIDs. x8
Analgesia
Anti-pyretic
Anti-inflammatory
Anti-thrombotic

Induces closure of Ductus Arteriosus

Alleviates Dysmenorrhea

Tocolytic activity (Indomethacin)

Effective against Colorectal CA and Alzheimers
What bodily areas are affected by the side effects of NSAIDs?

List specific damages
GI
(Ulcers, GI distress, diarrhea)

Renal
(Renal necrosis, nephritis, acute renal failure)
What is Misoprostol, and what does it do?
PGE1 analog

Prevents GI damage from NSAIDs
NSAID pharmacokinetics:

- Absorption
- Distribution
- Metabolism
- Excretion
Fast and complete

Highly bound to proteins (90-95%)

By hepatic P450

Renal
Salicylates:

- mechanism of action
- reversibility
Nonselectively inhibits COX
(COX-1 and COX-2)

IRREVERSIBLE
How is salicylates absorbed?
By passive diffusion (b/c weak acid)

via ion trapping effect
What is the major excreted conjugate for salicylates?
Salicyuric acid
Describe the dose dependency of Salicylates
Low Dose - 1st order kinetics

High Dose - Saturation kinetics
Describe the pH dependency of Salicylates.
If urine pH below 7.4 -> Absorption
(b/c urine/plasma ratio is < 1)

If urine pH above 7.4 -> Excretion
(b/c urine/plasma ratio is < 1)
What are the common side effects of NSAIDs? x3
GI bleed

Stimulates respiration

Changes Acid/Base balance
(respiratory alkalosis -> increased bicarb excretion -> alkalosis compensation)
List the Salicylates derivatives. x3
Methyl Salicylate

Sodium Salicylate

Diflusinal
Which salicylate derivative is used topically to counter irritants?
Methyl Salicylate
Which salicylate derivative is least potent when compared to ASA?
Sodium Salicylate
Diflusinal:

- Derivative of what?
- Potent at?
- Weak at?
- Side effects?
Diflusinal

Analgesia + Anti-inflammatory

Anti-pyretic

Less effects on GI, auditory, thrombotic
Acetominophen:

- mechanism of action
- reversibility?
- occurs where?
Nonselective COX inhibitor
(COX-1 and COX-2)

Reversible

More at the CNS (inactive at PNS)
Acetominophen:

- Potent at?
- Weak at?
Analgesia + Anti-pyretic

Anti-inflammatory + GI effecs
(also anti-thrombotic)
Acetominophen:

- toxicity
- antidote
Hepatic Necrosis

N-acetylcysteine (NAC)
Acetominophen:

- metabolism/excretion
With glutathione -> nontoxic

Without glutathione -> hepatotoxic
List the Acetic Acid derivatives. x7
1. Indomethacin
2. Tolmetin
3. Sulindac

4. Ketolorac
5. Fenamates
6. Etodolac
7. Diclofenac
List the propionic acid derivatives. x5
1. Ketoprofen
2. Ibuprofen
3. Naproxen

4. Oxaprozin
5. Fluriprofen
Propionic acid derivatives:

- mechanism of action
- why use?
Non selective COX inhibitor

Better tolerated than ASA or indomethacin
List the enolic acid derivatives and their mechanism of action. x3
Piroxicam - (inhibits COX 1)

Meloxicam - (inhibits COX 2)

Nabumatone -
(inhibits COX 1 and COX 2)
COXIBs

- mechanism of action
- weak at?
- side effects
COX 2 inhibitors

GI and antithrombotic

may cause CV problems
Celecoxib:

- metabolized by?
- inhibited by?
CYP2 C9

CYP2 D6
What drugs only inhibit COX-2? x4
Etodolac

Diclofenac

Meloxicam

Coxibs