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Pathopharm Final > NSAIDs (Part 1) > Flashcards

NSAIDs (Part 1) Flashcards

1
Q

Aspirin is classfied as a

A

salicylate

(Acetylsalicylic acid, ASA)

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2
Q

T/F
Ibuprofen is the prototype drug and is the standard of comparison for other anti-inflammatory agents.

A

False
Aspirin (Acetylsalicylic acid, ASA

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3
Q

Aspirin (Acetylsalicylic acid, ASA) is the agent is choice for

A

rheumatoid arthritis (RA) therapy

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4
Q

How to decrease GI concerns with aspirin

A
  • taking with food and water
  • buffered/enteric-coated forms
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5
Q

T/F
Aspirin is the agent of choice for rheumatoid arthritis. It can limit the progression of the disease.

A

False
only reduces pain and inflammation
NO effect on disease progression

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6
Q

Can we use other salicylates besides aspirin?

A

available but appear to be somewhat less effective

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7
Q

Sodium salicylate

A
  • buffered salt form ↑ gastric pH
  • less GI irritation
  • probably less potent than ASA as an analgesic and antipyretic agent
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8
Q

Salicylates besides aspirin

A

Sodium salicylate
Methyl salicylate
magnesium salicylate
Salsalate

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9
Q

Which salicylate is a counter- irritant, but also an innocent source of poisoning to children, requiring only 1 tsp to be fatal?

A

Methyl salicylate (oil of wintergreen)

“no meth for kids”

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10
Q

T/F
One tablespoon of Methyl salicylate (oil of wintergreen) can be fatal to a child.

A

False
TEAspoon

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11
Q

Methyl salicylate preparations

A
  • 50% of drug
  • 5% must be sold in childproof containers
  • must be labeled for external use only
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12
Q

Which salicylate causes less bleeding but may not be as effective as aspirin?

A

magnesium salicylate

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13
Q

mechanism of action of ASA

A
  • irreversibly inhibits COX via acetylation → inhibits PG synthesis
  • probably more selective for COX-1
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14
Q

Aspirin irreversibly inhibits COX by _____

A

acetylation

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15
Q

T/F
ASA is probably more selective for COX1 more than COX2.

A

True

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16
Q

Therapeutic Effects of ASA

A
  • Analgesia
  • Antipyresis
  • Anti-inflammatory
  • Anti-platelet
  • Uricosuric
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17
Q

ASA
-what pain is best to use for
-how does it work?

A
  • low intensity, somatic pain
  • headache, muscle and joint, toothache
  • not good for visceral pain; effects difficult to eval
  • PG-E sensitizes pain receptors, salicylates decrease PG synthesis at inflammation sites
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18
Q

ASA should not be used for (somatic/visceral) pain.

A

visceral
effects difficult to evaluate

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19
Q

ASA
Antipyresis moA

A
  • Leukocyte pyrogen enters hypothalamus and generates PG-E
  • PG-E release resets “thermostat”
  • ASA inhibits PG production in the hypothalamus
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20
Q

Which PG “resets the thermostat” as seen in fever?

A

PGE

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21
Q

T/F
ASA resets the thermoregulatory center and lowers body temperature.

A

False

  • “resets” by increasing cutaneous blood flow → heat loss and sweating
  • Doesn’t actually lower normal body temperature
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22
Q

ASA Anti-inflammatory
moA

A

Inhibits PG synthesis by blocking COX

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23
Q

ASA Anti-platelet
moA

A
  • Decreases platelet aggregation
  • valuable therapy for various thrombotic diseases
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24
Q

ASA Uricosuric
moA

A
  • High doses: increase urate excretion
  • low doses: urate retention & can worsen gout
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25
Q

T/F
Low dose Aspirin is helpful in managing gout pain.

A

FALSE
low doses cause urate retention and can worsen gout

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26
Q

Side Effects of ASA

A
  • Gastric ulceration and bleeding
  • Intolerance (asthma, nasal polyps, chronic urticaria)
  • Cross sensitivity to other NSAIDs
  • hepatotoxicity
  • Acute decrease in renal function
  • Reye’s syndrome
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27
Q

T/F
If a pt has an ASA hypersensitivity, all NSAIDS are contraindicated.

A

True

ALL NSAIDS ARE CONTRAINDICATED IN PATIENTS WITH ASA HYPERSENSITIVITY

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28
Q

ASA Cross-sensitivity
Common agents

A

indomethacin, ibuprofen

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29
Q

How does aspirin cause GI ulceration and bleeding?

A
  • local irritation
  • ↑ back diffusion of H+ & acid secretion
  • result from decreased PG synthesis & elimination of cytoprotectant effects
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30
Q

T/F
Decreasing PG synthesis will lead to increased gastric irritation.

A

True

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31
Q

How much of the general population is intolerant of aspirin?

A

0.2 to 0.9%

may be as high as 20-25% in patients with asthma, nasal polyps, and chronic urticaria

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32
Q

How common is serious bleeding from aspirin?

A

15 cases/100,000/year

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33
Q

Which attributes contribute to intolerance to ASA?

A

asthma, nasal polyps, and chronic urticaria

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34
Q

Symptoms of ASA intolerance

A
  • bronchial secretions
  • urticaria
  • angioedema
  • hypotension, shock, etc
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35
Q

T/F
Ibuprofen irreversibly prevents thromboxane synthesis for the life of the platelet.

A

False
ASA will

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36
Q

How does ASA cause bleeding?

A
  • Decreases platelet aggregation
  • acetylates platelet COX by low doses
  • irreversibly prevents thromboxane synthesis for the life of the platelet (8-11 days)
  • potentiate capillary bleeding (GIT, tonsils, tooth sockets after extraction)
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37
Q

ASA preferentially inhibits ___ more than ___ synthesis (may also get more platelet aggregation-inhibiting PG-I2).

A

inhibits TX-A2 > PG-I2

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38
Q

What dose of ASA is used in preventing cardiovascular catastrophes in high-risk patients?

A

81 mg/children’s aspirin

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39
Q

When to stop aspirin before surgery

A

1 week before surgery to avoid potential bleeding complications

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40
Q

ASA liver fx

A
  • SLE & juvenile RA may be susceptible to dose-dependent hepatotoxicity
  • Do not use in chronic liver diseases
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41
Q

ASA Renal fx

A
  • Acute decrease in renal function in certain conditions
  • CHF, renal disease, diuretic use
  • monitor renal function in at-risk patients
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42
Q

Reye’s syndrome

A
  • a/w ASA use
  • children with viral diseases (chicken pox, cold, influenza, etc.)
  • 1985: FDA required warning labels
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43
Q

Can ASA be used in pregnancy?

A

Do not use in last trimester
Risks:

  • prolong gestation and labor
  • increase blood loss at delivery
  • decrease baby’s platelet aggregation→intracranial hemorrhage.
  • close ductus arteriosus prematurely
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44
Q

The Dimer of salicylic acid

A

Salsalate

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45
Q

Salsalate
metab & absorption

A
  • Some is hydrolyzed in small intestine to two molecules of salicylic acid
  • while majority is absorbed unchanged
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46
Q

Salsalate is hydrolyzed into…

A

two molecules of salicylic acid
(in the small int)

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47
Q

Salsalate
half life

A
  • Low dose ~1 hour
  • anti-inflammatory dose: up to 16 hours due to metabolic enzyme saturation
48
Q

Salicylates + PO anticoagulants

A
  • ↓ prothrombin, ↓ platelet aggregation + GI effects: ↑ bleeding
  • displaces anticoagulants from plasma binding sites
49
Q

Drugs that Salicylates will displace

A
  • anticoagulants
  • oral hypoglycemics
  • phenytoin
  • sulfonamides
  • methotrexate
  • other NSAIDs
  • alcohol
  • ototoxic agents
  • antacids
  • penicillin
  • acetazolamide (increases salicylate intoxication).
50
Q

Which drug increases salicylate intoxication?

A

acetazolamide

51
Q

Salicylates antagonize… (2)

A

diuretics and uricosurics

52
Q

Para-Aminophenols

A

prototype is acetaminophen
(Tylenol, Datril, Tempra, Panadol)

53
Q

T/F
Para-Aminophenols are not true NSAIDS.

A

True
Tylenol, Datril, Tempra, Panadol

54
Q

Therapeutic Effects of Acetaminophen

A

Analgesia
Antipyresis
Anti-Inflammatory

55
Q

Can Tylenol be useful to RA pts or inflammatory disorders?

A

No

56
Q

Acetaminophen
Anti-Inflammatory Properties

A
  • inhibit COX only if low in H2O2 (hypothalamus)
  • inflammatory sites usually more peroxides (generated by leukocytes)

NOT useful for RA or inflammatory conditions

57
Q

T/F
Acetaminophen’s fever control is comparable to aspirin.

A

True

58
Q

Acetaminophen Antipyresis
moA

A
  • central PG synthesis inhibition may be responsible
  • not well understood
59
Q

Ofirmev US approval

A

2010

60
Q

Ofirmev dose

A
  • Normal adult dose: 1000mg (100 ml) in 15 min infusion
  • [10 mg/ml]
61
Q

Studies demonstrate Ofirmev + morphine allows…

A

lower doses and less morphine needed

62
Q

Current Max daily acetaminophen

A
  • 4000 mg by any route
  • PO: 3000 mg/day max due to first pass
63
Q

Acetaminophen
Side Effects Compared to aspirin

A

no:

  • gastric erosion
  • platelet effects
  • cross allergies with aspirin or NSAIDS
  • effects on urate excretion

less drug interactions!

64
Q

Does Tylenol affect platelets?

A

No

65
Q

Frequent Tylenol doses may increase the effect of ____

A

warfarin

66
Q

Chronic excessive Tylenol doses may cause hepatotoxicity; ____ potentiates effects.

A

alcohol

67
Q

Tylenol & Behavioral issues

A
  • Reported link (JAMA 2016)
  • hyperactive & behavioral problems in 7 year olds if mothers who used Tylenol between 18 and 32 weeks gestation
  • modest risk
  • not recommended to cease use in pregnancy
68
Q

T/F
A reported link by JAMA in 2016 between Tylenol and behavioral problems in children led to the recommendation to stop Tylenol use during pregnancy.

A

False
modest risk
did not recommend to stop using

69
Q

Acetaminophen Intoxication
-dosing
-what to avoid

A
  • Hepatic necrosis
  • 10 g causes injury
  • 25 g probably fatal
  • > 3 drinks/day enhances liver damage risk
  • DO NOT EXCEED RECOMMENDED DOSE OF 4 G/DAY
70
Q

Acetaminophen Intoxication
moA

A

(if other pathways are saturated)

  • more P-450 hydroxylation: Tylenol → quinone metabolite that conjugates with glutathione
  • glutathione runs out (depletion>regeneration)
  • metabolite binds to sulfhydryl groups of protein in liver cells instead and destroys them
  • centrilobular necrosis

Conversion may be increased by P-450 inducing agents

71
Q

Acetaminophen Intoxication
Symptoms

A

initial:
N/V, diarrhea, abdominal pain; hepatic injury
abnormal LFTs (24-48 hrs)
↑ SGOT, LDH, PT

3-6 days:
encephalopathy, jaundice, hepatic failure, renal failure (acute tubular necrosis)

72
Q

Acetaminophen t1/2 increases with liver damage. Hepatic necrosis will occur if half-life exceeds…

A

4 hr

(normal t1/2 is 2-3 hr)

73
Q

Acetaminophen Intoxication
Treatment

A
  • primary GI decontaminant: Activated charcoal
  • sulfhydryl agents (N-acetylcysteine/Mucomyst) increases glutathione production
  • PO or IV useful if treatment started early (24 – 36 hrs. after overdose)
74
Q

N-acetylcysteine
(Mucomyst)

A
  • sulfhydryl agent used in Tylenol toxicity
  • increases glutathione production
  • PO or IV
  • useful if treatment started early (24 – 36 hrs. after overdose)
75
Q

What is considered early treatment of Tylenol toxicity

A

within 24 – 36 hrs. after overdose

76
Q

Drugs for rheumatoid arthritis (RA) are also used in other inflammatory disorders such as..

A
  • osteoarthritis
  • gouty arthritis
  • ankylosing spondylitis
  • some musculoskeletal injuries
77
Q

Other NSAIDs
(not ASA or Tylenol)
moA

A
  • All reversibly inhibit COX I & II
  • effects on PGs & thromboxanes
  • Selectivity for these isoforms is variable and incomplete
  • Most are more effective in inhibiting COX I
  • ibuprofen & meclofenamate appear to equally inhibit both COX isoforms
78
Q

Which agents appear to equally inhibit both COX isoforms?

A

ibuprofen and meclofenamate

reversibly inhibit COX I and COX II

79
Q

Other NSAIDs
binding

“other NSAIDs” means not ASA or Para-aminophenols

A
  • All organic anions
  • highly bound to plasma protein
  • may compete for anion transport & plasma protein binding
80
Q

T/F
Other NSAIDs:
All can cause gastric ulceration and GI blood loss, but probably cause less GI distress than aspirin.

“other NSAIDs” means not ASA or Para-aminophenols

A

True

81
Q

Other NSAIDs
platelet aggregation

A
  • All inhibit platelet aggregation, but less than with aspirin
  • Also, effect is reversible when drug disappears.
82
Q

All NSAIDs must be suspected of causing hypersensitivity-like reactions in patients that are…

A

intolerant to aspirin

83
Q

As a group, all NSAIDs must be suspected of causing…

A

CNS, hematologic, hepatic, & renal toxicity!

  • dizziness, tinnitus, headache
  • aplastic anemia & granulocytopenia (serious!)
  • hepatotoxicity: cholestatic jaundice & necrosis
  • nephrotoxicities: Na & H2O retention, ARF, papillary necrosis, nephrotic syndrome
84
Q

T/F
All NSAIDs can cause gastric ulceration and GI blood loss, but probably less GI distress is seen with aspirin.

A

False
Other NSAIDs probably cause less GI distress than does aspirin

85
Q
A
86
Q

T/F
All NSAIDs, including ASA have only palliative effects on RA. RA will continue to progress regardless.

A

True

87
Q

Aspirin vs other NSAIDs
Which has worse acute overdose?

A

acute aspirin intoxication

88
Q

Recent studies have shown COX inhibitors to have protective effects against…

A

colon cancer and useful in treating Alzheimer’s disease.

89
Q

NSAIDs
Most common complaints

A

stomach pain, nausea and vomiting

90
Q

T/F
Most NSAIDS increase bleeding times to some degree

A

True

91
Q

Probably is the most potent of the NSAIDs

A

Indomethacin (Indocin)

92
Q

T/F
Indomethacin (Indocin) is probably the most potent NSAID and is superior to aspirin for RA.

A

False
not superior to ASA for RA

93
Q

Indomethacin (Indocin)
may be more effective for…

A
  • ankylosing spondylitis
  • osteoarthritis
  • acute gout
94
Q

Indomethacin (Indocin)
Adverse effects

A
  • 35-50% of patients
  • severe frontal headache (most common)
  • dizziness
  • confusion
  • gastric intolerance
95
Q

T/F
The most common adverse effect of Indomethacin (Indocin) is gastric intolerance.

A

False
severe frontal headache

96
Q

Indomethacin (Indocin) appears to be better tolerated and more effective if …

A

larger doses are taken HS

97
Q

Indomethacin (Indocin) appears to be more selective in inhibiting COX-___

A

1

98
Q

Sulindac

A
  • Prodrug converted to the active sulfide metabolite
  • t1/2 = 7 hr; 16-18 hr for the sulfide metabolite (due to extensive enterohepatic circulation).
99
Q

Indomethacin (Indocin) vs Sulindac
Which has lower incidence of GI toxicity?

A

Sulindac

100
Q

NSAID with lowest incidence of GI side effects

A

Etodolac

significant difference between anti-inflammatory dose and doses that cause gastric irritation

101
Q

Etodolac

A
  • Single dose provides postoperative analgesia that lasts 6-8 hr.
  • Also available as extended-release preparation for once-a-day administration.
  • More selective for COX-II than COX-I (as selective as Celebrex)
102
Q

Better tolerated than aspirin and equally effective

A

Tolmetin

103
Q

first injectable NSAID

A

Ketorolac

104
Q

⭐️
Ketorolac is a very potent analgesic & shouldnt be used…

A

for more than 5 days

105
Q

Ketorolac IM

A
  • 30-90 mg
  • short-term treatment of acute surgical pain
  • (not longer than 5 days).
  • Can replace morphine.
  • not for obstetrical pre-operative or analgesic
106
Q

T/F
Ketorolac can replace morphine

A

True

107
Q

Ketorolac PO

A

10 mg prn q 4 - 6 hr

108
Q

T/F
Ketorolac’s Side effects increase in frequency and severity if used for longer periods

A

True

109
Q

Ketorolac opthalmic solution

A

for allergic conjunctivitis (Acular)

110
Q

Sprix

A

Ketorolac metered nasal dose form for systemic absorption

111
Q

Diclofenac (Voltaren)

A
  • Very potent antiinflammatory
  • ophthalmic: cataract surgery inflammation
  • Immediate-release (Cataflam): pain & dysmenorrhea (50 mg TID)
  • with misoprostol (Cytotec), a PG-E1 analog (Arthrotec)
112
Q

Which agent may decrease concentration of free arachadonic acid?

A

Diclofenac (Voltaren)

113
Q

Diclofenac (Voltaren)
metab

A
  • t1/2 (1 - 2 hr), but accumulates in synovial fluid
  • Significant first-pass
114
Q

Diclofenac (Voltaren) has ashort half life but may accumulate in…

A

synovial fluid

115
Q

misoprostol (Cytotec)

A
  • PG-E1 analog
  • Arthrotec: miso + Diclofenac

Pathopharm Final (8 decks)

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