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Flashcards in NSAIDs - Fitz Deck (27)
1

Drug classes (w/ members) that target COX (7 total drugs)


For what injury type?

- Salicylates (Aspirin, Diflunisal)
- NSAIDs (Ibuprofen, Naproxen, Indomethacin, Diclofenac, Ketorolac)
- Coxibs (Celecoxib)

Tissue injury

2

Name the PG associated w/...
- Uterus
- Stomach
- Renal artery
- Blood vessels
- Platelets
- CNS
- PNS

Uterus = PGF2a, PGE2 (contract)
Stomach = PGE2 (protection)
Renal aa = PGE2 (patency)
Vessels = PGI2 (dilation)
Platelets = TxA2 (aggregate)
CNS = PGE2 (fever)
PNS = PGE2 (pain sensitization)

3

Salicylate - side effect

GI ulcers

4

4 similarities btwn COX-1 and COX-2

- Same substrate (AA)
- Same product (PGH2)
- Anti-inflammation effect
- Renal artery constriction effect

5

Ibuprofen vs. Naproxen

Ibuprofen = 2 hr half life
Naproxen = 14 hr half life

6

Indications for NSAIDs

- Osteoarthritis
- Arthritides
- Bursitis
- Gout FLARE
- Ankylosing spondylitis
- Dysmenorrhea
- Headaches/Migraine

7

Side effects of NSAIDs

GI ulcer (no PGE2)
Bleeding (no TxA2)
Peripheral edema, increased BP (renal artery constriction)

8

***People to be careful about when prescribing an NSAID

- HF or risk factors for HF
- Obesity, high LDL, etc.
- Renal disease
- BP medication
- Those at risk of infection (will blunt the fever response)

9

Contraindications for NSAIDs

- Asthma
- GI inflammation (gastritis, colitis, pancreatitis, hepatitis)

10

Celecoxib - MoA

COX-2 selective inhibitor

11

Celecoxib - benefit

Gastric-sparing (no ulcers)

12

Drugs that are more COX-1 selective (from most to least) (5)

Ketorolac
Indomethacin
Aspirin
Naproxen
Ibuprofen

13

Drug that acts on COX-1 and COX-2 equally

Salicylate

14

Drugs that are more COX-2 selective (2)

Celecoxib
Diclofenac

15

***Which drug is the only NSAID available for parenteral administration?

Where is it on the COX1/COX2 scale?

Ketorolac

1000x COX-1 specific (most of all of them)

16

**Which side effect is shared by traditional NSAIDs and Celecoxib?

Peripheral edema, HTN (Renal artery constriction)

17

Patient has sulfa allergy. Which NSAID is contraindicated?

Celecoxib (sulfa drug) - SJS/TEN

18

What is high dose of Aspirin?

Pro-drug of Salicylate (converted in the liver)

19

***Side effects of Salicylate (or Aspirin) - COX independent (4)

**Acid-Base disturbance (respiratory alkalosis --> metabolic acidosis)
**Tinnitus
Hypersensitivity
*Reye's syndrome (when treating viral infection)

20

Effect/Side effect of Aspirin at...
- 80-160 mg
- 325 mg - 1 g

- 1-6 g
- 6-20 g
- > 20 g

- Anti-platelet
- Analgesic, ant-pyretic, anti-inflammatory

- **Tinnitus
- **Acid-base issue
- **Shock, coma

21

Describe COX-independent side effects of Salicylate

Uncouples OxPhos, respiratory centers see low ATP, get hyperventilation, respiratory alkalosis causes bicarb wasting, accumulate acids b/c no ATP, get metabolic acidosis

22

Children w/ fever (viral illnesses, etc)...treatment?

Why?

Acetaminophen (Tylenol)

Prevent risk of Reye's syndrome

23

******What is low-dose Aspirin used for? Why/how?

Anti-thrombotic (heart dz)

ASA (before conversion to salicylate) is an IRREVERSIBLE inhibitor of COX. Aspirin sits in portal vein (prior to liver) and acts on all the platelets, causing COX inhibition. Platelets have no nucleus, so they cannot make more COX. Hence they are permanently inactive

24

How long does it take to get full anti-thrombotic effect of low-dose aspirin?

How long will clotting ability return to normal after stopping low-dose aspirin?

3 days

3 days

25

When is Aspirin given as an anti-thrombotic agent? Why then?

After an MI (improves survival)

Before = GI bleeding, etc.

26

Why were the stronger Coxibs taken off of the market?

COX-2 can sometimes have a protective/beneficial effect in inflammation by making PGI2/prostacyclin (ex. atherosclerosis). Inhibiting COX-2 only allows COX-1 to dominate, leading to higher risk for CV disease (thrombosis).

27

Why was Celecoxib NOT taken off the market?

ALL NSAIDs have what?

Confers same level of CV risk as any NSAID

Black box warning for CV risks