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Therapeutics Spring 2015 > NSAID drugs > Flashcards

NSAID drugs Flashcards

1
Q

What is the mechanism of Salicylic Acid?

A

Inhibits COX-1 and COX-2 reversibly

May suppress COX-2 induction

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2
Q

How are salicylates absorbed?

A

Ionically through the small intestine

In acid form less from the stomach

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3
Q

What are 3 kinds of salicylic acid drugs?

A

Salicin
Salicylic acid
aspirin (ASA)

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4
Q

Generic name of aspirin?

A

acetylsalicylic acid

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5
Q

what is the mechanism of aspirin?

A

irreversibly inhibits COX by acetylating a serine residue in the active site
- also has salicylate action because it is rapidly hydrolyzed

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6
Q

What kind of enzyme hydrolyzes aspirin?

A

plasma esterase

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7
Q

which is more potent, aspirin or salicylic acid?

A

asprin is 2x more potent as an analgesic and andipyretic

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8
Q

What is a an exploited side effect of aspirin?

A

it blocks platelet aggravating factor thromboxane A2

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9
Q

Is aspirin stable in solution?

A

NO

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10
Q

Brand name of salsalate?

A

Disalcid

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11
Q

What is the structure of salsalate?

A

salicylic acid dimer connected by an ester bond

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12
Q

How is salsalate absorbed?

A

hydrolyzed in the small intestine and absorbed

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13
Q

What is an advantage of salsalate?

A

it does not cause GI bleeding, less active in stomach

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14
Q

What NSAID category does salsalate belong too?

A

Salicylates

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15
Q

what is the brand name of diflunisal?

A

Dolobid

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16
Q

which is more potent, aspirin or diflunisal?

A

diflunisal is a more potent analgesic but has less antipyretic activity

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17
Q

What is the unique structural property of diflunisal?

A

diflurobenzene ring

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18
Q

Which has a longer half life, aspirin or diflunisal?

A

Diflunisal

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19
Q

which NSAID category does diflunisal belong too?

A

salicylates

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20
Q

which category does indomethacin belong too?

A

arylacetic acids

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21
Q

is indomethacin suitable for long term use?

A

No, very high incidence of side effects

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22
Q

Is indomethacin stable in solution?

A

No, amide bond hydrolyzed in solution

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23
Q

True of false, indomethacin is one of the most potent NSAIDs in use?

A

True

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24
Q

What NSAID category does sulindac belong too?

A

Arylacetic acids

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25
Q

How is sulindac activated in the body?

A

It is a prodrug

reduction of the sulfoxide group to the active sulfide intermediate activates into the circulatory system

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26
Q

what is the brand name of etodolac?

A

Lodine

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27
Q

how potent is etodolac?

A

as potent as indomethacin

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28
Q

What is an advantage of etodolac?

A

less GI bleeding

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29
Q

What is the primary use of etodolac?

A

Long term management of osteoarthritis

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30
Q

What is the unique structural property of etodolac?

A

pyranocarboxylic acid

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31
Q

What NSAID class does etodolac belong too?

A

arylacetic acids

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32
Q

What is the brand name of diclofenac?

A

Voltaren

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33
Q

How potent is diclofenac?

A

as potent as indomethacin

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34
Q

Etodolac and diclofenac are somewhat selective for which COX enzyme?

A

COX-2

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35
Q

Which two pathways does diclofenac inhibit?

A

COX and lipoxygenase pathways

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36
Q

Which NSAID class does diclofenac belong too?

A

arylacetic acid

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37
Q

Which NSAID class does ibuprofen belong too?

A

arylpropionic acids

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38
Q

What is the brand name of ibuprofen?

A

Advil, Motrin

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39
Q

How potent is ibuprofen?

A

Less potent than indomethacin but more than aspirin

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40
Q

What is the structural feature of ibuprofen?

A

alpha-methyl group enhances its activity and reduces the side effects

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41
Q

True of false, ibuprofen is a racemic mixture of bioINequivalent isomers?

A

False, the isomers are bioEQUIVALENT because the (r) enantiomer is converted to (s) in vivo

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42
Q

What is the brand name of naproxen?

A

Aleve

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43
Q

Which NSAID category does naproxen belong too?

A

Arylpropionic acid

44
Q

Which enantiomer is in naproxen?

A

Pure S-(+) enantopmer

45
Q

What is naproxen used to treat?

A

rheumatoid arthritis and osteoarthritis

46
Q

What is the brand name of ketorolac?

A

Toradol

47
Q

what NSAID class does ketorolac belong too?

A

arylpropionic acids

48
Q

Is ketorolac for short or long term management?

A

Short term management of moderate to severe pain

49
Q

How potent is ketorolac?

A

Analgesic activity similar to centrally acting analgesics

alternative to narcotics, no addiction potential

50
Q

What kind of NSAID class does nabumetone belong too?

A

Non-carboxylates

51
Q

What is the mechanism of nabumetone?

A

nonacidic prodrug that is metabolized to 6-MNA

52
Q

What is the function of 6-MNA?

A

COX inhibitor, similar structure to naproxen

53
Q

What is the advantage of nabumetone?

A

minimum GI side effects

very potent anti-inflammatory but weak analgesic

54
Q

What is the brand name of meloxicam?

A

Mobic

55
Q

What NSAID class does meloxicam belong too?

A

non-carboxylates

56
Q

What is the mechanism of meloxicam?

A

resembles the peroxy radical intermediate in COX

57
Q

Which COX enzyme is meloxicam slightly selective for?

A

COX 2

58
Q

what is the potency of meloxicam?

A

as potent as indomethacin, long acting, single daily dose

59
Q

What is the only fully selective COX-2 inhibitor on the market?

A

Celecoxib (Celebrex)

60
Q

How is celecoxib selective for COX-2?

A

has larger and rigid substituents which collide with the isoluecine of the COX 1 receptor

61
Q

What are some advantages of celecoxib?

A

less GI side effects
No antiplatelet activity
Good efficacy against pain, inflammation and fever

62
Q

How potent is celecoxib?

A

As potent as naproxen

63
Q

What is celecoxib used to treat?

A

osteoarthritis and RA

64
Q

What is the mechanism behind acetaminophen?

A

scavenges peroxynitrite which is required for PGHS activity in the CNS

65
Q

What are some advantages of acetaminophen?

A

less GI SE
Can be used in patients with coagulation disorders
Not associated with Reye’s syndrome
No cross reaction with aspirin

66
Q

What is a downside of acetaminophen?

A

Hepatotoxicity

67
Q

What is the mechanism behind acetaminophen’s hepatoxicity?

A

CYP450 concerts to ketone metabolite which reacts with glutathione in the liver

68
Q

What is the mechanism of methotrexate?

A

Decreases purine and pyrimidine synthesis

Has an anti-proliferative and pro-apoptotic effect on inflammatory cells

69
Q

Which vitamin is methotrexate structurally similar too?

A

Folic acid

70
Q

What are some side effects of methrotrexate?

A 
GI
stomatitis
rash
hair loss
myelosupression
hepatoxocicity
pulmonary toxicity
71
Q

Which condition is methotrexate contraindicated in?

A

Pregnancy

72
Q

What is the brand name of leflunomide?

A

Arava

73
Q

What is the mechanis, of leflunomide?

A

Prodrug that inhibits dihydroorotate dehydrogenase- a pyrimidine synthesis inhibitor (can’t synthesize DNA or proliferate T cells)

74
Q

What are some side effects of leflunomide?

A

hepatoxicity, diarrhea, hair loss, and rash

75
Q

What is a contraindication of leflunomide?

A

pregnancy or child bearing age

76
Q

What is the mechanism of hydroxychloroquine?

A

accumulates in lysosomes and inhibit protein secretion

77
Q

What condition should patients be monitored for with hydroxychloroquine?

A

reversible retinal toxicity

78
Q

What drug is hydroxychloroquine combined with?

A

methotrexate (reduces clearance so dose needs to be adjusted)

79
Q

What is the mechanism behind sulfasalazine?

A

It is a prodrug that is cleaved by colon bacteria into sulfapyridine and 5-aminosalicylic acid
-suppresses release of cytokines from macrophages

80
Q

What condition should patients be monitored for when using sulfasalazine?

A

rare myselosuppression

81
Q

What class of drugs does Infliximab belong too?

A

TNF Blockers, DMARDS

82
Q

What drug class does methotrexate belong too?

A

DMARDs

83
Q

What drug class does leflunomide belong too?

A

DMARDs

84
Q

What class of drugs does hydroxychloroquine belong too?

A

DMARDs

85
Q

What class of drugs does sulfasalazine belong too?

A

DMARDs

86
Q

What is the brand name of infliximab?

A

Remicade

87
Q

How is infliximab dosed?

A

IV q 8 weeks

88
Q

How do the antibody TNF alpha drugs work?

A

they bind and inhibit TNF alpha

89
Q

What is the brand of adalimumab?

A

Humira

90
Q

What kind of antibody is infliximab?

A

chimeric antibody- humanized Fc region

91
Q

What kind of antibody is adalimumab?

A

human antibody to TNF alpha

92
Q

What is the administration of adalimumab?

A

SubQ q 2 weeks

93
Q

What kind of molecule is etanercept?

A

TNF alpha receptor bound to Fc of human antibody

94
Q

What is the brand name of etanercept?

A

Enbrel

95
Q

What is the brand name of anakinra?

A

Kineret

96
Q

What is the mechanism of anakinra?

A

natural inhibitor of IL-1

97
Q

What patient population is anakinra indicated for?

A

MOderate and severe RA when they aren’t responsive to DMARDs

98
Q

What medication can not be combined with anakinra?

A

TNF alpha blockers

99
Q

What is the brand name of rituximab?

A

Rituxan

100
Q

What kind of molecule is rituximab?

A

Humanized monoclonal antibody against CD20 on B cells

101
Q

What is the mechanism behind rituximab?

A

Induces apoptosis of CD20+ cells

Reduces activation of T cells

102
Q

What is a serious side effect of rituximab?

A

Increased risk of serious infection because little antibody production

103
Q

What is the brand of abatacept?

A

Orencia

104
Q

What is the mechanism behind abatacept?

A

Binds to CTLA-4 and prevents stabilization of immune synapse with CD80 so no costimulation of T cells by APCs

105
Q

What are serious side effects of abatacept?

A

Increased risk of serious infections

Slight increase in risk of lymphomas

Therapeutics Spring 2015 (12 decks)

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