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PHA6126 Pharmacology 2 Lecture > Drugs Used in Gout > Flashcards

Drugs Used in Gout Flashcards

1
Q

metabolic disease characterized by recurrent episodes of acute arthritis due to deposits of monosodium urate in joints and cartilage

A

gout

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2
Q

systemic disease caused by buildup of uric acid in joints, cause inflammation, swelling, and pain

A

gout

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3
Q

urate level >8mg/dL and 7mg/dL in women

A

hyperuricemia

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4
Q

most common first symptom of gout

A

pain in one joint of the lower extremity

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5
Q

end product of purine metabolism

A

uric acid

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6
Q

rate limiting step in the formation of uric acid

A

xanthine oxidase

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7
Q

serves no known biological functions, but body has content of 1.0-0.2 g

A

uric acid

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8
Q

T/F: Approximately 70-80% of uric acid is excreted via the kidneys

A

True

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9
Q

Types of gout

A

Primary and Secondary

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10
Q

result of innate defect in purine metabolism of uric acid excretion

A

primary gout

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11
Q

uric acid overproduction, impaired renal clearance of uric acid (underexcreters) or a combi of both are associated with

A

primary gout

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12
Q

hematologic disorders, drug-induced salicylates, diuretics (thiazide), ethambutol, pyrazinamide, nicotinic acid, ethanol, niacin and cyclosporine

A

secondary gout

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13
Q

tx goals for gout

A
  1. relieve pain and inflammation
  2. reduce serum uric acid conc (urate lithiasis)
  3. prevent recurrent gout attacks
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14
Q

drugs for acute gouty arthritis attack

A
  1. colchicine
  2. NSAIDs
  3. corticosteroids
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15
Q

antimitotic drug that is highly effective in relieving acute gout attack with a low-benefit to toxicity ratio

A

colchicine

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16
Q

T/F: Colchicine is used more often than NSAIDs due to its low-benefit to toxicity ratio

A

False: used less often

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17
Q

cause dose-dependent GI adverse effect (nausea, vomitin, bloating, emesis and diarrhea) that occur in up to 80% of px

A

oral colchicine

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18
Q

can be taken with or w/o food and sometimes used in combination with NSAIDs

A

colchicine

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19
Q

alkaloid isolated from autumn crocus (Colchicum autumnale)

A

colchicine

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20
Q

Colchicine relieves pain and inflammation of ___________________________________ w/o altering urate metabolism or excretion and w/o other analgesic effects

A

gouty arthritis in 12-24 hrs

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21
Q

NSAIDs are the _________________________ because of their excellent efficacy and minimal toxicity with short-term use

A

mainstay of therapy

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22
Q

most common adrs of NSAIDs involve ___________________ (gastritis, bleeding and perforation)

A

GI system

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23
Q

most extensively studied NSAID in the tx of acute gouty arthritis attack

A

indomethacin

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24
Q

Aside from inhibiting PG synthase, NSAIDs also inhibit _______________________ and reduce inflammation and pain in acute gout flare

A

urate crystal phagocytosis

25
Q

Aspirin is not used in gout because it causes _________________________ at lower doses (less than or equal to 2.6 g/d)

A

renal retention of uric acid

26
Q

All NSAIDs except ______________________________ have been successfully used to treat acute gouty episodes

A

aspirin, salicylates, and tolmetin

27
Q

lowers serum uric acid and is theoretically a good choice

A

oxaprozin

28
Q

T/F: All NSAIDs appear to be as effective and safe as older drugs like indomethacin

A

True

29
Q

equivalents to NSAIDs for tx of acute gout flares

A

corticosteroids

30
Q

Corticosteroids are effective when given ______________________________

A

intra-articularly, IV, or orally

31
Q

oral corticosteroid

A

prednisone

32
Q

long-acting corticosteroid administered through IM, intra-articular (if px is unable to take oral meds)

A

triamcinolone acetonide or methylprednisolone

33
Q

corticosteroids ___________________ (increase/decrease) activation, proliferation, and survival of various inflammatory cells

A

decrease

34
Q

corticosteroids also decrease the migration of neutrophils and inhibit __________________________ such as IL-1B

A

prostaglandins and proinflammatory cytokines

35
Q

indicated as good alternative for px in whom NSAIDs or colchicine are contraindicated and in those w/renal impairment or CKD

A

corticosteroids

36
Q

Corticosteroids are sometimes used in the tx of ______________________ by oral, intra-articular, systemic, or SC routes

A

severe symptomatic gout

37
Q

goal is to achieve and maintain serum uric acid conc of less than 6mg/dL and preferable <5mg/dL

A

urate lowering therapy

38
Q

reduction of serum urate conc can be accomplished by

A
  1. decreasing uric acid synthesis
  2. increasing renal excretion of uric acid
39
Q

decrease uric acid synthesis

A

xanthin oxidase inhibitor

40
Q

increase renal excretion of uric acid

A

uricosurics

41
Q

T/F: uric acid lowering therapy are not to be used during acute gouty arthritis attack

A

True

42
Q

xanthine oxidase inhibitors

A

allopurinol (first-line tx), febuxostat

43
Q

reduce uric acid by impairing conversion of hypoxanthine to xanthine and xanthine to uric acid

A

xanthine oxidase inhibitor

44
Q

xanthine oxidase inhibitors are effective in both _________________________________ of uric acid

A

overproducers and uncerexcretion

45
Q

most widely prescribed agents for long-term prevention of recurrent gout attacks

A

xanthine oxidase inhibitors

46
Q

a purine analog that inhibits xanthine oxidase resulting in a fall in plasma urate level and in the overall urate burden

A

allopurinol

47
Q

Allopurinol is often the first-line agent for tx of ________________ in the period between attacks

A

chronic gout

48
Q

it tends to prolong intercritical period and therapy is continued for years if not for life

A

allopurinol

49
Q

potent and selective non-purine inhibitor of xanthine oxidase

A

febuxostat

50
Q

probenecid, sulfinpyrazone, and lesinurad

A

uricosuric drugs

51
Q

uricosuric agents discontinued in the US

A

sulfinpyrazone and lesinurad

52
Q

uricosuric drugs increase renal clearance of uric acid by inhibiting the _____________________________________ of uric acid

A

postsecretory renal proximal tubular reabsorption

53
Q

should be initiated in gouty px with underexcretion of uric acid when allopurinol or febuxostat is contraindicated

A

probenecid

54
Q

probenecid can be used as monotherapy or in combination with a ____________________ (e.g., allopurinol or febuxostat)

A

xanthine oxidase inhibitor

55
Q

canakinumab, anakinra, rilonacept

A

IL-1 receptor inhibitors

56
Q

main proinflammatory cytokine responsible for the crystal-induced inflammation of gout

A

IL-1B

57
Q

not yet FDA-approved for gout

A

IL-1 inhibitors

58
Q

canakinumab, anakinra, rilonacept mode of admin

A

SC

PHA6126 Pharmacology 2 Lecture (10 decks)

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