Exam 4 - NSAIDs

Question 1

DRUG LIST

Answer 1

Aspirin etc: Aspririn, Salicylate
NSAIDs: Ibu, Naproxen, Acetaminophen, Celecoxib
GI protectors: Omeprazole

Question 2

NSAIDs

general description

Answer 2

-organic acids, well absorbed, renal excretion,
protein bound, found in synovial fluid
-prostoglandin synth inhibitors
(block eicosanid conversion to prostaglandin, thromboxane)
-competitive COX inhibition (not aspirin)
-low dose: analgesia, antipyretic
-high dose: anti-inflamm, arthritis relief
-other: PDA closure, anti-cancer-ish

Question 3

NSAIDs

Prostanoids

Answer 3

-endogenous compounds, products of COX rxns
-synth’d vascular endothelium
COX1: TXA2 -platelet agg, vaso/bronchoconstrict
COX2: PGE1 - vasodilation, uterine contr, anti-ulcer
COX2: PGE2 - incr temp, inflammation, anti-ulcer

Question 4

NSAIDs

COX enzymes

Answer 4

• endoplasmic retic

- COX1 and 2 isoforms

Question 5

NSAIDs

COX1

Answer 5

-in most tissues

Question 6

NSAIDs

COX2

Answer 6

• expression induced by stress

- major source of inflammatory prostanoids

Question 7

NSAIDs

COX inhibiton

Answer 7

COX1 and 2: asprin, salicylate, ibu, naproxen, acetaminophen

COX2: celecoxib

Question 8

NSAIDs

analgesia

Answer 8

• inflammation-induced pain

- inhibs hyperalgesic PGs

Question 9

NSAIDs

antipyretic

Answer 9

• resets temp set-point

- inhibs PGE2 release into preoptic hypothal

Question 10

NSAIDs

antiinflamm

Answer 10

-at larger doses, sx relief (ibu, aspirin)

Question 11

NSAIDs

anti-cancer

Answer 11

inhib inflammation (PGE2)

Question 12

NSAIDs

side effects

Answer 12

• GI: nausea, diarrhea, ulcers, perforation (aspirin)
• renal: decreased PGE2 causes decreased renal bl flow
• preg (inhibs labor), lactation (weigh risks)
• hypersens (not IgE), nasal polyps; apsirin allergy contras all

Question 13

NSAIDs

drug-drug

Answer 13

• ibu impairs aspirin’s acetylation of COX
• ACE inhibitors: attenuates effects, renal tox
• Warfarin: incr bleeding, CYP2C9

Question 14

NSAIDs

aspirin tx

Answer 14

• analgesic, antipyretic, antiinflamm
• antiinflamm takes higher does, irreversible
• antiplatelet/CV protection/MI
• TXA2 synth inhib
• contra’d in children with viral fever (Reye’s)

Question 15

NSAIDs

aspirin adverse

Answer 15

• dosage adjust for renal dz
• GI effects (prevents PGE1/2)
• co-adm omeprazole PRN
• hypersensitivity (not immunological)
• respiratory alkalosis at tx dose
• resp and metabolic alkalosis high dose
• analgesic nephropathy
• HTN

Question 16

NSAIDs

ibuprofen tx

Answer 16

• most common
• recently approved for IV
• analgesia, PDA closure

Question 17

NSAIDs

ibuprofen adverse

Answer 17

• same as aspirin

- fewer GI effects than aspirin, naproxen

Question 18

NSAIDs

Naproxen tx

Answer 18

• rheumatoid arthritis
• many formulations
• co-rx with omemprazole PRN

Question 19

NSAIDs

Celecoxib tx

Answer 19

• not better than non-selective
• arthritis, familial adenomatous polyposis
• not first choice drug

Question 20

NSAIDs

Celecoxib adverse

Answer 20

• contra’d in CV and cerebrovasc dz

- sulfonamid moiety can cause allergic rxns

Question 21

NSAIDs

Acetaminophen tx

Answer 21

• analgesia, antipyretic
• metab’d to glucuronic and sulfate conjugates
• NOT GOOD FOR ANTI-INFLAMM
• weaker COX2 affinity
• No effects on: platelets, CV, Resp, acid/base, GI

Question 22

NSAIDs

Acetaminophen adverse

Answer 22

• hepatotoxicity, potentially fatal (CYP2E1)
• nausea, ab pain, anorexia
• liver enzymes peak 72-96 hrs after
• N-acetylcysteine for OD tx
• incr BP w/ CAD
• maybe causes asthma in children

Question 23

NSAIDs

tx for GI effects

Answer 23

Omeprazole, a PPI