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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
How is sulindac activated in the body?
It is a prodrug | reduction of the sulfoxide group to the active sulfide intermediate activates into the circulatory system
26
what is the brand name of etodolac?
Lodine
27
how potent is etodolac?
as potent as indomethacin
28
What is an advantage of etodolac?
less GI bleeding
29
What is the primary use of etodolac?
Long term management of osteoarthritis
30
What is the unique structural property of etodolac?
pyranocarboxylic acid
31
What NSAID class does etodolac belong too?
arylacetic acids
32
What is the brand name of diclofenac?
Voltaren
33
How potent is diclofenac?
as potent as indomethacin
34
Etodolac and diclofenac are somewhat selective for which COX enzyme?
COX-2
35
Which two pathways does diclofenac inhibit?
COX and lipoxygenase pathways
36
Which NSAID class does diclofenac belong too?
arylacetic acid
37
Which NSAID class does ibuprofen belong too?
arylpropionic acids
38
What is the brand name of ibuprofen?
Advil, Motrin
39
How potent is ibuprofen?
Less potent than indomethacin but more than aspirin
40
What is the structural feature of ibuprofen?
alpha-methyl group enhances its activity and reduces the side effects
41
True of false, ibuprofen is a racemic mixture of bioINequivalent isomers?
False, the isomers are bioEQUIVALENT because the (r) enantiomer is converted to (s) in vivo
42
What is the brand name of naproxen?
Aleve
43
Which NSAID category does naproxen belong too?
Arylpropionic acid
44
Which enantiomer is in naproxen?
Pure S-(+) enantopmer
45
What is naproxen used to treat?
rheumatoid arthritis and osteoarthritis
46
What is the brand name of ketorolac?
Toradol
47
what NSAID class does ketorolac belong too?
arylpropionic acids
48
Is ketorolac for short or long term management?
Short term management of moderate to severe pain
49
How potent is ketorolac?
Analgesic activity similar to centrally acting analgesics | alternative to narcotics, no addiction potential
50
What kind of NSAID class does nabumetone belong too?
Non-carboxylates
51
What is the mechanism of nabumetone?
nonacidic prodrug that is metabolized to 6-MNA
52
What is the function of 6-MNA?
COX inhibitor, similar structure to naproxen
53
What is the advantage of nabumetone?
minimum GI side effects | very potent anti-inflammatory but weak analgesic
54
What is the brand name of meloxicam?
Mobic
55
What NSAID class does meloxicam belong too?
non-carboxylates
56
What is the mechanism of meloxicam?
resembles the peroxy radical intermediate in COX
57
Which COX enzyme is meloxicam slightly selective for?
COX 2
58
what is the potency of meloxicam?
as potent as indomethacin, long acting, single daily dose
59
What is the only fully selective COX-2 inhibitor on the market?
Celecoxib (Celebrex)
60
How is celecoxib selective for COX-2?
has larger and rigid substituents which collide with the isoluecine of the COX 1 receptor
61
What are some advantages of celecoxib?
less GI side effects No antiplatelet activity Good efficacy against pain, inflammation and fever
62
How potent is celecoxib?
As potent as naproxen
63
What is celecoxib used to treat?
osteoarthritis and RA
64
What is the mechanism behind acetaminophen?
scavenges peroxynitrite which is required for PGHS activity in the CNS
65
What are some advantages of acetaminophen?
less GI SE Can be used in patients with coagulation disorders Not associated with Reye's syndrome No cross reaction with aspirin
66
What is a downside of acetaminophen?
Hepatotoxicity
67
What is the mechanism behind acetaminophen's hepatoxicity?
CYP450 concerts to ketone metabolite which reacts with glutathione in the liver
68
What is the mechanism of methotrexate?
Decreases purine and pyrimidine synthesis | Has an anti-proliferative and pro-apoptotic effect on inflammatory cells
69
Which vitamin is methotrexate structurally similar too?
Folic acid
70
What are some side effects of methrotrexate?
``` GI stomatitis rash hair loss myelosupression hepatoxocicity pulmonary toxicity ```
71
Which condition is methotrexate contraindicated in?
Pregnancy
72
What is the brand name of leflunomide?
Arava
73
What is the mechanis, of leflunomide?
Prodrug that inhibits dihydroorotate dehydrogenase- a pyrimidine synthesis inhibitor (can't synthesize DNA or proliferate T cells)
74
What are some side effects of leflunomide?
hepatoxicity, diarrhea, hair loss, and rash
75
What is a contraindication of leflunomide?
pregnancy or child bearing age
76
What is the mechanism of hydroxychloroquine?
accumulates in lysosomes and inhibit protein secretion
77
What condition should patients be monitored for with hydroxychloroquine?
reversible retinal toxicity
78
What drug is hydroxychloroquine combined with?
methotrexate (reduces clearance so dose needs to be adjusted)
79
What is the mechanism behind sulfasalazine?
It is a prodrug that is cleaved by colon bacteria into sulfapyridine and 5-aminosalicylic acid -suppresses release of cytokines from macrophages
80
What condition should patients be monitored for when using sulfasalazine?
rare myselosuppression
81
What class of drugs does Infliximab belong too?
TNF Blockers, DMARDS
82
What drug class does methotrexate belong too?
DMARDs
83
What drug class does leflunomide belong too?
DMARDs
84
What class of drugs does hydroxychloroquine belong too?
DMARDs
85
What class of drugs does sulfasalazine belong too?
DMARDs
86
What is the brand name of infliximab?
Remicade
87
How is infliximab dosed?
IV q 8 weeks
88
How do the antibody TNF alpha drugs work?
they bind and inhibit TNF alpha
89
What is the brand of adalimumab?
Humira
90
What kind of antibody is infliximab?
chimeric antibody- humanized Fc region
91
What kind of antibody is adalimumab?
human antibody to TNF alpha
92
What is the administration of adalimumab?
SubQ q 2 weeks
93
What kind of molecule is etanercept?
TNF alpha receptor bound to Fc of human antibody
94
What is the brand name of etanercept?
Enbrel
95
What is the brand name of anakinra?
Kineret
96
What is the mechanism of anakinra?
natural inhibitor of IL-1
97
What patient population is anakinra indicated for?
MOderate and severe RA when they aren't responsive to DMARDs
98
What medication can not be combined with anakinra?
TNF alpha blockers
99
What is the brand name of rituximab?
Rituxan
100
What kind of molecule is rituximab?
Humanized monoclonal antibody against CD20 on B cells
101
What is the mechanism behind rituximab?
Induces apoptosis of CD20+ cells | Reduces activation of T cells
102
What is a serious side effect of rituximab?
Increased risk of serious infection because little antibody production
103
What is the brand of abatacept?
Orencia
104
What is the mechanism behind abatacept?
Binds to CTLA-4 and prevents stabilization of immune synapse with CD80 so no costimulation of T cells by APCs
105
What are serious side effects of abatacept?
Increased risk of serious infections | Slight increase in risk of lymphomas

Therapeutics Spring 2015 (12 decks)

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