Chapter 74 - NSAIDs and Acetaminophen Flashcards

1
Q

How do cyclooxygenase inhibitors work?

A

inhibit COX, the enzyme that converts arachidonic acid into prostanoids

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2
Q

What does COX regulate?

A

-stomach: promote PGE2 and PGI2 synthesis that protect mucosa
-promote inflammation and sensitize receptors to pain
-stimulate platelet aggregation
-causes vasodilation via prostacyclin
-vasodilation in kidneys
-mediates fever and contributes to pain perception
-promotes uterine contractions

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3
Q

What is the benefit of inhibiting COX-1?

A

protect against MI and stroke

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4
Q

Drugs that inhibit COX-1 can cause:

A

-gastric ulcers
-bleeding
-renal impairment

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5
Q

What are the beneficial effects of COX-2 inhibition?

A

-suppress inflammation
-alleviate pain and fever
-protect against colorectal cancer

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6
Q

What are things that drugs that inhibit COX-2 can cause?

A

-renal impairment
-promotion of MI and stroke

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7
Q

What are COX inhibitors used for?

A

-suppressing inflammation
-pain relief
-fever reduction

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8
Q

NSAIDs are a class of __________

A

COX inhibitors

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9
Q

What are some NSAIDs?

A

-aspirin (ASA)
-celecoxib
-ibuprofen (advil)
-naproxen
-diclofenac
-ketoprofen
-flurbiprofen
-indomethacin
-ketorolac
-menfenamic acid

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10
Q

What are the classes of COX inhibitors?

A

-anti-inflammatory - NSAIDs
-not anti-inflammatory - acetaminophen (tylenol)

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11
Q

1st Gen NSAIDs inhibit COX ___

A

1 and 2

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12
Q

What are 1st gen NSAIDs used to treat?

A

-inflammatory disorders
-pain
-fever

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13
Q

How does ASA act?

A

non-selectively inhibits COX

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14
Q

Does ASA pass membranes?

A

yes all including fetal tissue and CNS

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15
Q

What are the uses of ASA?

A

-analgesic
-antipyretic
-anti inflammatory
-suppresses platelet aggregation
-cancer prevention

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16
Q

What are the adverse effects of ASA?

A

-GI effects
-bleeding
-renal impairment
-tinnitus
-sweating
-headache
-dizziness
-pregnancy - anemia, hemorrhage, prolong labour
-hypersensitivity

17
Q

What does ASA interact with?

A

-anticoagulants
-glucocorticoids
-alcohol
-ibuprofen
-ACEIs
-ARBs

18
Q

ASAs should not be used in people with…

A

-bleeding disorders
-peptic ulcer disease

19
Q

How are non-ASA 1st gen NSAIDs different:

A

-fewer Gi, renal, hemorrhagic effects
-have reversible inhibition
-don’t protect against MI and strok

20
Q

What are non-ASA 1st gen NSAIDs used for?

A

-rheumatoid arthritis
-osteoarthritis
-pain conditions

21
Q

What kind of drug is ibuprofen?

A

1st gen NSAID

22
Q

How does ibuprofen act?

A

COX inhibition and antiinflammatory, analgesic, antipyretic actions

23
Q

What is ibuprofen used for?

A

-fever
-mild to moderate pain
-arthritis

24
Q

What are the adverse effects of ibuprofen?

A

-GI upset
-risk of GI bleed
-confusion in elderly
-allergic rxn
-fluid retention

25
Q

What is a safety risk for 1st gen NSAIDs?

A

-risk of GI bleeding: esp with hx of ulcer, multiple NSAID use, anticoagulant, SSRI, steroid, > 60 yoa, hx of heart disease

26
Q

How do 2nd gen NSAIDs compare?

A

-just as effective
-lower risk of GI side effects
-can impair renal function
-may cause HTN and edema
-increased risk of MI and stroke
-work mainly on COX 2

27
Q

What drug class is Celecoxib?

A

a 2nd gen COX 2 inhibitor

28
Q

Why is Celecoxib the last choice drug for pain?

A

CV effects

29
Q

What is celecoxib used for?

A

-osteoarthritis
-rheumatoid arthritis
-acute pain

30
Q

What are the adverse effects of celecoxib?

A

-dyspepsia
-abdominal pain
-sulfa allergy
-CV events

31
Q

What is acetaminophen (tylenol) used for?

A

-analgesic
-antipyretic
-no anti inflammatory or antirheumatic action
-not associated with Reye’s syndrome

32
Q

How does acetaminophen act?

A

inhibits prostaglandin synthesis in CNS (not periphery)

33
Q

What does acetaminophen interact with?

A

ALCOHOL and warfarin

34
Q

How is acetaminophen metabolized?

A

-major pathway is conjugation to nontoxic metabolites
-minor pathway via CYP450 to toxic metabolite then to non-toxic metabolite via glutathione

35
Q

What are the adverse effects of acetaminophen?

A

-few at normal doses***
-Stevens-Johnson syndrome
-Toxic epidermal necrolysis
-hepatotoxicity (OD or liver failure)

36
Q

What are the signs and symptoms of hepatic necrosis?

A

-N&V
-diarrhea
-sweating
-abdominal pain

37
Q

What is the treatment for acetaminophen OD?

A

acetylcysteine via IV or oral - converts toxic metabolits to non-toxic form