NSAIDs

Question 1

Difference between TXA2 and TXA3

Answer 1

TXA2 is a vasoconstrictor, TXA3 is not

Question 2

Cycloxygenases convert Arachidonic Acid into what? (2 names)

Answer 2

PGG2 (Cyclic Endoperoxidases)

Question 3

Peroxidase converts what to what?

Answer 3

PGG2 to PGH2

Question 4

What is Prostaglandin synthetase:

Answer 4

enzyme complex of cyclo-oxygenase and

peroxidase

Question 5

COX-1 vs COX 2

Answer 5

COX-1 constitutive form - found in blood vessels, stomach & kidney

COX-2 inducible form
Involved in inflammation
Levels elevated by inflammation & cytokines
Decreased by administration of glucocorticoids

Question 6

What kind of receptor are Prostaglandin receptors?

Answer 6

GPCR

Question 7

Where is prostacyclin (PGI2) synthesized?

Answer 7

vascular smooth muscle cells and endothelial cells

Question 8

Prostacyclin actions on:
vasculature
platelets
airways
GI
renal
reproductive
pain

Answer 8

Tone - Vasodilator
platelets - inhibits platelet aggregation
Airways - bronchodilator
GI- Inhibits gastric acid secretion; increase mucus secretion Renal - Enhances renal excretion of sodium & water Reproductive - relaxes uterine muscle
Pain - Induces pain by lowering the threshold of nociceptors

Question 9

Prostaglandin (PGE2) actions on:
vasculature
platelets
airways
GI
renal
reproductive
pain
fever

Answer 9

Vascular - vasodilator
Platelets: low conc enhances and high conc inhibits platelet aggregation
Airway - bronchodilator
GI - Inhibits gastric acid secretion & stimulates gastric mucus secretion
Renal - Promotes renal salt and water excretion
Reproductive - Uterine smooth muscle, increases contraction
pain - Induces hyperalgesia at localized area
Fever - PGE2 IS A DIRECT PYROGEN IN HYPOTHALAMUS

Question 10

Where is TXA2 synthesized?

Answer 10

platelets, lung, kidney

Question 11

Effects of TXA2 (2)

Answer 11

Vasoconstriction

Stimulates platelet aggregation

Question 12

PGF2α actions on:
vasculature
airway
reproductive
eye

Answer 12

Vascular - Vasoconstrictor
Airway - contracts airway smooth muscle cells
Reproductive - Contracts uterine smooth muscle/dysmenorrhea
eye - decreases intraocular pressure

Question 13

Misoprostol is what kind of drug?

Answer 13

PGE1 analog

Question 14

Misoprostol clinical use

Answer 14

Inhibits gastric acid secretion, reduces risk of peptic ulcer in patients taking NSAID

Question 15

Misoprostol contraindication

Answer 15

pregnancy, women of childbearing age must use contraceptive measures

Question 16

Latanoprost is what kind of drug?

Answer 16

PGF2α analog

Question 17

Latanoprost clinical use

Answer 17

ophthalmic preparation for open angle glaucoma

Question 18

Latanoprost mechanism

Answer 18

increases outflow of aqueous humor, reduces ocular pressure

Question 19

Alprostadil is what kind of drug?

Answer 19

PGE1 analog

Question 20

Alprostadil clinical use and form given

Answer 20

maintain patency of the ductus arteriosus via IV infusion

Question 21

Which Arachidonic Acid metabolites are chemotactic?

Answer 21

LTB4 and 5-HETE

Question 22

LTC4, LTD4, and LTE4 actions (3)

Answer 22

Bronchoconstrictor
increase vascular permeability
Components of slow reacting substance of anaphylaxis

Question 23

Zafirlukast and Montelukast mechanism

Answer 23

competitive leukotriene LTD4 (CysLT1) receptor antagonist

Question 24

Zafirlukast and Montelukast

Answer 24

Prophylactic agent in treatment of asthma in adults

Montelukast - Especially good for aspirin-induced asthma.

Question 25

Zafirlukast and Montelukast interactions

Answer 25

Zafirlukast inhibits P450 isozyme CYP2C9 and CYP3A4 Warfarin | Food reduces bioavailability

Question 26

Zileuton mechanism

Answer 26

inhibitor of 5-lipoxygenase | Blocks conversion of arachidonic acid to leukotrienes

Question 27

Zileuton use

Answer 27

Prophylaxis for asthma in adults and children (12 yr and older)

Question 28

Zileuton toxicity

Answer 28

hepatotoxic

Question 29

Zileuton decreases clearance of what 3 drugs?

Answer 29

Theophylline Warfarin Propranolol

Question 30

NSAIDs mechanism (and exceptions)

Answer 30

competitive, reversible inhibitors COX1/COX2 aspirin is irreversible Celecoxib is COX2 inhibitor

Question 31

NSAIDs clinical use (3)

Answer 31

Antipyretic Analgesics for mild to moderate pain Anti-inflammatory

Question 32

NSAIDs side effects (4)

Answer 32

GI irritation and ulcers Bleeding, Inhibits platelet aggregation Inhibit uterine motility Fluid retention

Question 33

NSAIDs contraindications

Answer 33

pregnancy - last trimester | Cross sensitivity with aspirin (contraindication)

Question 34

Aspirin mechanism

Answer 34

irreversible COX inhibitor | acetylates enzyme

Question 35

Aspirin actions (3)

Answer 35

analgesic (mild to moderate pain) antipyretic anti-inflammatory

Question 36

Aspirin clinical use

Answer 36

arthritis initial therapy | low dose prevents MI

Question 37

How does Aspirin prevent MI?

Answer 37

irreversibly inhibits TXA2 production in platelets

Question 38

Aspirin side effects

Answer 38

GI pain, hemorrhage & ulcers

Question 39

Aspirin contraindication

Answer 39

viral infection due to Reye's Syndrome

Question 40

Ibuprofen (Advil), Naproxen (Aleve) mechanism

Answer 40

reversible inhibition of COX

Question 41

Ibuprofen (Advil) clinical use (4)

Answer 41

antipyretic, can be used in children Arthritis acute migraine attacks primary dysmenorrhea

Question 42

Naproxen (Aleve) clinical use (3)

Answer 42

arthritis ankylosing spondylitits acute gout

Question 43

Benefit of Ibuprofen and Naproxen over Aspirin?

Answer 43

less GI ulcers

Question 44

Naproxen contraindications

Answer 44

Naproxen clearance reduced in liver cirrhosis | increased risk of stroke/cardiovascular event

Question 45

Ketorolac mechanism of action

Answer 45

inhibits COX

Question 46

Ketorolac clinical use

Answer 46

Ophthalmic allergy and inflammation following cataract surgery Post-operative pain Only NSAID approved for moderate to severe pain

Question 47

Ketorolac side effects

Answer 47

Bleeding hepatotoxicity Lower dose in patients under 110 lbs or elderly or elevated creatinine

Question 48

Ketorolac contraindications

Answer 48

During labor/delivery or during lactation

Question 49

DICLOFENAC clinical use

Answer 49

arthritis and ankylosing spondylitits | Ophthalmic preparation for post-cataract surgery

Question 50

Arthotec contraindication?

Answer 50

Contraindicated during pregnancy

Question 51

Arthotec is a combination of what drugs and is used in what patients?

Answer 51

Diclofenac and Misoprostol patients at high risk for GI ulcer

Question 52

Indomethacin IV clinical use?

Answer 52

non-surgical closure of patent ductus arteriosus

Question 53

Indomethacin contraindications

Answer 53

renal and hyperbilirubinemia

Question 54

Celecoxib mechanism

Answer 54

selective COX-2 competitive reversible inhibitor

Question 55

Celecoxib clinical use

Answer 55

arthritis

Question 56

Celecoxib side effects

Answer 56

GI pain | increased risk of cardiovascular and stroke event with high dose for prolonged time

Question 57

Celecoxib drug interaction

Answer 57

-monitor dose carefully when given with fluconazole inhibits Cyp 2C9

Question 58

Acetaminophen mechanism

Answer 58

Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally.

Question 59

Acetaminophen clinical use

Answer 59

Antipyretic Analgesic for mild to moderate pain, osteoarthritis poor anti-inflammatory

Question 60

Acetaminophen side effects

Answer 60

Hepatotoxicity (acute) | 2. Renal toxicity with chronic use

Question 61

Auranofin (oral) and Gold Sodium Thiomalate (given IM) mechanism

Answer 61

Inhibit maturation and function of phagocytes and T cells | Decrease levels of rheumatoid factor

Question 62

Auranofin side effects and Gold Sodium Thiomalate side effects (4)

Answer 62

Can occur months after discontinuation of therapy Gray color to skin Nephrotic Syndrome Thrombocytopenia