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Flashcards in NSAIDs Deck (62):
1

Difference between TXA2 and TXA3

TXA2 is a vasoconstrictor, TXA3 is not

2

Cycloxygenases convert Arachidonic Acid into what? (2 names)

PGG2 (Cyclic Endoperoxidases)

3

Peroxidase converts what to what?

PGG2 to PGH2

4

What is Prostaglandin synthetase:

enzyme complex of cyclo-oxygenase and
peroxidase

5

COX-1 vs COX 2

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

6

What kind of receptor are Prostaglandin receptors?

GPCR

7

Where is prostacyclin (PGI2) synthesized?

vascular smooth muscle cells and endothelial cells

8

Prostacyclin actions on:
vasculature
platelets
airways
GI
renal
reproductive
pain

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

9

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

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

10

Where is TXA2 synthesized?

platelets, lung, kidney

11

Effects of TXA2 (2)

Vasoconstriction
Stimulates platelet aggregation

12

PGF2α actions on:
vasculature
airway
reproductive
eye

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

13

Misoprostol is what kind of drug?

PGE1 analog

14

Misoprostol clinical use

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

15

Misoprostol contraindication

pregnancy, women of childbearing age must use contraceptive measures

16

Latanoprost is what kind of drug?

PGF2α analog

17

Latanoprost clinical use

ophthalmic preparation for open angle glaucoma

18

Latanoprost mechanism

increases outflow of aqueous humor, reduces ocular pressure

19

Alprostadil is what kind of drug?

PGE1 analog

20

Alprostadil clinical use and form given

maintain patency of the ductus arteriosus via IV infusion

21

Which Arachidonic Acid metabolites are chemotactic?

LTB4 and 5-HETE

22

LTC4, LTD4, and LTE4 actions (3)

Bronchoconstrictor
increase vascular permeability
Components of slow reacting substance of anaphylaxis

23

Zafirlukast and Montelukast mechanism

competitive leukotriene LTD4 (CysLT1) receptor antagonist

24

Zafirlukast and Montelukast

Prophylactic agent in treatment of asthma in adults

Montelukast - Especially good for aspirin-induced asthma.

25

Zafirlukast and Montelukast interactions

Zafirlukast inhibits P450 isozyme CYP2C9 and CYP3A4 Warfarin
Food reduces bioavailability

26

Zileuton mechanism

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

27

Zileuton use

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

28

Zileuton toxicity

hepatotoxic

29

Zileuton decreases clearance of what 3 drugs?

Theophylline
Warfarin
Propranolol

30

NSAIDs mechanism (and exceptions)

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

31

NSAIDs clinical use (3)

Antipyretic
Analgesics for mild to moderate pain
Anti-inflammatory

32

NSAIDs side effects (4)

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

33

NSAIDs contraindications

pregnancy - last trimester
Cross sensitivity with aspirin (contraindication)

34

Aspirin mechanism

irreversible COX inhibitor
acetylates enzyme

35

Aspirin actions (3)

analgesic (mild to moderate pain)
antipyretic
anti-inflammatory

36

Aspirin clinical use

arthritis initial therapy
low dose prevents MI

37

How does Aspirin prevent MI?

irreversibly inhibits TXA2 production in platelets

38

Aspirin side effects

GI pain, hemorrhage & ulcers

39

Aspirin contraindication

viral infection due to Reye's Syndrome

40

Ibuprofen (Advil), Naproxen (Aleve) mechanism

reversible inhibition of COX

41

Ibuprofen (Advil) clinical use (4)

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

42

Naproxen (Aleve) clinical use (3)

arthritis
ankylosing spondylitits
acute gout

43

Benefit of Ibuprofen and Naproxen over Aspirin?

less GI ulcers

44

Naproxen contraindications

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

45

Ketorolac mechanism of action

inhibits COX

46

Ketorolac clinical use

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

47

Ketorolac side effects

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

48

Ketorolac contraindications

During labor/delivery or during lactation

49

DICLOFENAC clinical use

arthritis and ankylosing spondylitits
Ophthalmic preparation for post-cataract surgery

50

Arthotec contraindication?

Contraindicated during pregnancy

51

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

Diclofenac and Misoprostol

patients at high risk for GI ulcer

52

Indomethacin IV clinical use?

non-surgical closure of patent ductus arteriosus

53

Indomethacin contraindications

renal and hyperbilirubinemia

54

Celecoxib mechanism

selective COX-2 competitive reversible inhibitor

55

Celecoxib clinical use

arthritis

56

Celecoxib side effects

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

57

Celecoxib drug interaction

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

58

Acetaminophen mechanism

Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally.

59

Acetaminophen clinical use

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

60

Acetaminophen side effects

Hepatotoxicity (acute)
2. Renal toxicity with chronic use

61

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

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

62

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

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