NSAIDs & DMARDs Flashcards

1
Q

NSAIDs act through _

A

inhibition of prostoglandins

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2
Q

cyclo-oxygenases (COX1/COX2)

A

synthesize prostoglandins and thromboxanes

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3
Q

prostoglandin effects

A

pain by lowering threshold of pain receptors, fever, inflammation

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4
Q

glucorticoids

A

induce lipocortin that inhibits PLA2 for broad anti-inflammatory response

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5
Q

COX1

A

constitutive activation; production of platelet clotting factors, parturition, stomach mucosa, ion excretion

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6
Q

COX2

A

activated by inflammatory stimulus and mostly transcribed in macrophages; causes inflammation, swelling, pain, redness

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7
Q

COX1 for _

A

prevention of cardiovascular events

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8
Q

COX2 for _

A

anti-inflammatory/analgesic reasons

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9
Q

NSAIDs three therapeutic actions

A

fever, pain, inflammation

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10
Q

acetaminophen lacks _

A

anti-inflammatory effects

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11
Q

analgesic action of NSAIDs

A

PGE2 sensitizes nerve endings to action of bradykinin, histamine, and other chemical mediators released by inflammatory process –> by decreasing PGE2, pain is decreased

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12
Q

ketorolac

A

can be used in severe pain for short duration

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13
Q

dose-dependent effects of salicylates

A

lower dose has an analgesic effect while higher dose has an anti-inflammatory effect

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14
Q

antipyretic (fever) action of NSAIDs

A

cytokines (mainly IL-1) stimulate hypothalamus to release PGE2 which leads to an increase in body temp –> decreasing PGE2 will inhibit this

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15
Q

low dose aspirin

A

selectively inhibits COX1 which reduces the production of TXA2 to prevent vasoconstriction and platelet aggregation

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16
Q

salicylic acid

A

topically to treat acne, corns, calluses, warts

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17
Q

methyl salicylate

A

used externally as a cutaneous counterirritant

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18
Q

diclofenac

A

topical treatment of osteoarthritis

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19
Q

side effects associated with COX1 inhibition

A

peptic ulcers and GI bleeding

20
Q

side effects associated with COX inhibition

A

water retention, hypertension, kidney injury

21
Q

side effects associated with COX2 inhibition

A

stroke and myocardial infection

22
Q

gastrointestinal adverse effects

A

PGI2 inhibits gastric acid secretion and PGE2/PGF2 promote mucus synthesis so inhibition will cause bleeding and ulceration

23
Q

renal adverse effects

A

PGE2/PGI2 are responsible for maintaining renal blood flow so inhibition will cause retention of sodium and water

24
Q

cardiac adverse effects

A

agents with higher COX-2 selectivity can increase risk for platelet aggregation and vasoconstriction by inhibiting PGI2/TXA2

25
Q

naproxen

A

least harmful NSAIDs for patients with CV contraindications

26
Q

NSAIDs and asthma

A

inhibition of prostoglandin synthesis will shift the precursors to make leukotrienes which causes asthma, anaphylaxis, and smooth muscle contraction

27
Q

celecoxib

A

selective COX-2 inhibitor for the treatment of RA, osteoarthritis, and acute pain

28
Q

celecoxib metabolism

A

metabolized by CYP2C9

29
Q

fluconazole

A

inhibits CYP2CP, causing increased celecoxib levels

30
Q

N-acetylcysteine

A

antidote for acetaminophen OD

31
Q

DMARDs

A

disease modifying antirheumatic drugs; can suppress rheumatoid process and bring about a remission but do not have nonspecific anti-inflammatory or analgesic action

32
Q

traditional DMARDs

A

non-biologic; typical one is methotrexate

33
Q

biologic DMARDs

A

non-TNF inhibitors; monoclonal Abs; used when inadequate response with traditional DMARDs

34
Q

methotrexate

A

folic acid antagonist that inhibits cytokine production and purine NT synthesis leading to immunosuppressive and anti-inflammatory effects; for RA

35
Q

hydroxychloroquine

A

used for early, mild RA and can be combined with methotrexate

36
Q

hydroxychloroquine side effects

A

ocular toxicity

37
Q

methotrexate side effects

A

hepatic and GI; contraindicated in pregnancy

38
Q

DMARDs begin to show a response within _

A

weeks to months

39
Q

leflunomide

A

inhibits DHODH to cause cell arrest of autoimmune lymphocytes; used in patients with CI for methotrexate

40
Q

leflunomide side effects

A

flu-like symptoms, alopecia, rash; contraindicated in pregnancy

41
Q

sulfasalazine

A

similar to leflunomide

42
Q

TNF-alpha inhibitors

A

biologic DMARDs; response within 2 weeks but only used after inadequate response to traditional DMARDs

43
Q

TNF-alpha inhibitor effects

A

heart failure, increased risk of cancer

44
Q

non-TNF biologics

A

also used after inadequate response but CAN NOT be used with TNF-alpha inhibitors

45
Q

tofacitinib

A

inhibitor of janus kinase and can be used for RA if no response to methotrexate