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First Aid Step 1 material > NSAIDs > Flashcards

NSAIDs Flashcards

1
Q

Difference between TXA2 and TXA3

A

TXA2 is a vasoconstrictor, TXA3 is not

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2
Q

Cycloxygenases convert Arachidonic Acid into what? (2 names)

A

PGG2 (Cyclic Endoperoxidases)

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3
Q

Peroxidase converts what to what?

A

PGG2 to PGH2

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4
Q

What is Prostaglandin synthetase:

A

enzyme complex of cyclo-oxygenase and

peroxidase

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5
Q

COX-1 vs COX 2

A

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

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6
Q

What kind of receptor are Prostaglandin receptors?

A

GPCR

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7
Q

Where is prostacyclin (PGI2) synthesized?

A

vascular smooth muscle cells and endothelial cells

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8
Q 
Prostacyclin actions on:
vasculature
platelets
airways
GI
renal
reproductive
pain
A

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

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9
Q 
Prostaglandin (PGE2) actions on:
vasculature
platelets
airways
GI
renal
reproductive
pain
fever
A

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

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10
Q

Where is TXA2 synthesized?

A

platelets, lung, kidney

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11
Q

Effects of TXA2 (2)

A

Vasoconstriction

Stimulates platelet aggregation

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12
Q 
PGF2α actions on:
vasculature
airway
reproductive
eye
A

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

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13
Q

Misoprostol is what kind of drug?

A

PGE1 analog

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14
Q

Misoprostol clinical use

A

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

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15
Q

Misoprostol contraindication

A

pregnancy, women of childbearing age must use contraceptive measures

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16
Q

Latanoprost is what kind of drug?

A

PGF2α analog

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17
Q

Latanoprost clinical use

A

ophthalmic preparation for open angle glaucoma

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18
Q

Latanoprost mechanism

A

increases outflow of aqueous humor, reduces ocular pressure

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19
Q

Alprostadil is what kind of drug?

A

PGE1 analog

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20
Q

Alprostadil clinical use and form given

A

maintain patency of the ductus arteriosus via IV infusion

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21
Q

Which Arachidonic Acid metabolites are chemotactic?

A

LTB4 and 5-HETE

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22
Q

LTC4, LTD4, and LTE4 actions (3)

A

Bronchoconstrictor
increase vascular permeability
Components of slow reacting substance of anaphylaxis

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23
Q

Zafirlukast and Montelukast mechanism

A

competitive leukotriene LTD4 (CysLT1) receptor antagonist

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24
Q

Zafirlukast and Montelukast

A

Prophylactic agent in treatment of asthma in adults

Montelukast - Especially good for aspirin-induced asthma.

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25
Q

Zafirlukast and Montelukast interactions

A

Zafirlukast inhibits P450 isozyme CYP2C9 and CYP3A4 Warfarin

Food reduces bioavailability

26
Q

Zileuton mechanism

A

inhibitor of 5-lipoxygenase

Blocks conversion of arachidonic acid to leukotrienes

27
Q

Zileuton use

A

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

28
Q

Zileuton toxicity

A

hepatotoxic

29
Q

Zileuton decreases clearance of what 3 drugs?

A

Theophylline
Warfarin
Propranolol

30
Q

NSAIDs mechanism (and exceptions)

A

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

31
Q

NSAIDs clinical use (3)

A

Antipyretic
Analgesics for mild to moderate pain
Anti-inflammatory

32
Q

NSAIDs side effects (4)

A

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

33
Q

NSAIDs contraindications

A

pregnancy - last trimester

Cross sensitivity with aspirin (contraindication)

34
Q

Aspirin mechanism

A

irreversible COX inhibitor

acetylates enzyme

35
Q

Aspirin actions (3)

A

analgesic (mild to moderate pain)
antipyretic
anti-inflammatory

36
Q

Aspirin clinical use

A

arthritis initial therapy

low dose prevents MI

37
Q

How does Aspirin prevent MI?

A

irreversibly inhibits TXA2 production in platelets

38
Q

Aspirin side effects

A

GI pain, hemorrhage & ulcers

39
Q

Aspirin contraindication

A

viral infection due to Reye’s Syndrome

40
Q

Ibuprofen (Advil), Naproxen (Aleve) mechanism

A

reversible inhibition of COX

41
Q

Ibuprofen (Advil) clinical use (4)

A

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

42
Q

Naproxen (Aleve) clinical use (3)

A

arthritis
ankylosing spondylitits
acute gout

43
Q

Benefit of Ibuprofen and Naproxen over Aspirin?

A

less GI ulcers

44
Q

Naproxen contraindications

A

Naproxen clearance reduced in liver cirrhosis

increased risk of stroke/cardiovascular event

45
Q

Ketorolac mechanism of action

A

inhibits COX

46
Q

Ketorolac clinical use

A

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

47
Q

Ketorolac side effects

A

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

48
Q

Ketorolac contraindications

A

During labor/delivery or during lactation

49
Q

DICLOFENAC clinical use

A

arthritis and ankylosing spondylitits

Ophthalmic preparation for post-cataract surgery

50
Q

Arthotec contraindication?

A

Contraindicated during pregnancy

51
Q

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

A

Diclofenac and Misoprostol

patients at high risk for GI ulcer

52
Q

Indomethacin IV clinical use?

A

non-surgical closure of patent ductus arteriosus

53
Q

Indomethacin contraindications

A

renal and hyperbilirubinemia

54
Q

Celecoxib mechanism

A

selective COX-2 competitive reversible inhibitor

55
Q

Celecoxib clinical use

A

arthritis

56
Q

Celecoxib side effects

A

GI pain

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

57
Q

Celecoxib drug interaction

A

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

58
Q

Acetaminophen mechanism

A

Reversibly inhibits cyclooxygenase, mostly in CNS. Inactivated peripherally.

59
Q

Acetaminophen clinical use

A

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

60
Q

Acetaminophen side effects

A

Hepatotoxicity (acute)

2. Renal toxicity with chronic use

61
Q

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

A

Inhibit maturation and function of phagocytes and T cells

Decrease levels of rheumatoid factor

62
Q

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

A

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

First Aid Step 1 material (10 decks)

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