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Drug Mech Final > Anti-Gout > Flashcards

Anti-Gout Flashcards

1
Q

Which drug is used for the treatment and prophylaxis of gout flares?

A

Colchicine

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2
Q

Does Colchicine alter the metabolism or excretion of uric acid?

A

No

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3
Q

What is Colchicine’s MOA?

A

Binds to tubulin preventing its polymerization into microtubules leading to inhibition of leukocyte migration and phagocytosis

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4
Q

What are some rare complications of Colchicine (toxicities)?

A

Myelosuppression and neuropathy

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5
Q

If Colchicine is taken with a statin or a fibrate, what can occur?

A

Myopathy or rhabdomyolysis

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6
Q

What are NSAIDs used for with patients who have gout?

A

used for their anti-inflammatory effects

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7
Q

The use of _________ is not recommended in patients with gout.

A

Aspirin

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8
Q

Why is Aspirin not recommended for gout treatment?

A

because it increases the plasma levels of uric acid

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9
Q

What do NSAIDs treat for in patients who have gout?

A

Acute gout attacks

Used for prophylaxis for gout arthritis

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10
Q

What is the MOA of NSAIDs?

A

Inhibit the phagocytosis of uric acid crystals in the joint

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11
Q

What class of drugs can be given to patients with gout for the treatment of acute flares?

A

Corticosteroids

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12
Q

Name the corticosteroids that are used to treat patients with gout

A

Prednisone
Methylprednisolone
Triamcinolone

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13
Q

Name the Interleukin-1 (IL-1) Inhibitors

A

Canakinumab

Anakinra

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14
Q

Which IL-1 Inhibitor is approved for the treatment of systemic juvenile idiopathic arthritis, but has also shown to be effective in relieving gout pain and inflammation?

A

Canakinumab

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15
Q

Which IL-1 Inhibitor is approved for use in RA, but has also been shown to reduce the pain and inflammation of gout and is widely used off-label?

A

Anakinra

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16
Q

Name the Uricosuric Agent

A

Probenecid

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17
Q

Does Probenecid (increase or decrease?) the urate pool thus decreasing the size of plasma urate levels

A

decrease

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18
Q

Does Probenecid (increase or decrease?) the urinary excretion of uric acid?

A

increase

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19
Q

What can increased urinary excretion of uric acid lead to?

A

the formation of urate calculi (stones) in the kidney

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20
Q

What is Probenecid’s MOA?

A

Compete with uric acid for the transporter inhibiting uric acid reabsorption and increasing urinary excretion

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21
Q

How is uric acid secreted?

A

glomerular filtration and active renal tubular secretion

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22
Q

Most of the excreted uric acid (~90%) is reabsorbed by the ____________

A

renal proximal tubule

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23
Q

How is urate exchanged for organic or inorganic anions?

A

by the Organic Anion Transporter (URAT-1)

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24
Q

Low dosage of uricosuric agents usually results in ___________

A

decreased urinary excretion of urate

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25
Q

Higher dosage of uricosuric agents results in _________________

A

increased urinary excretion of urate

26
Q

At high doses, uricosuric drugs compete with uric acid for the transporter. What is the result of this?

A

inhibits its reabsorption via the urate-anion exchanger system

27
Q

Inhibition of the reabsorption of uric acid in the renal proximal tubule leads to an (increase or decrease?) in its urinary excretion

A

increase

28
Q

True or False: One uricosuric agent can inhibit the action of another?

A

True

29
Q

True or False: Uricosuric drugs are not organic acids?

A

False

30
Q

True or False: Aspirin and other salicylates are also organic acids?

A

True

31
Q

What happens if you take Aspirin in low doses (1-2 g/day)?

A

decrease urinary excretion of uric acid by inhibiting the transporter

32
Q

What happens if you take Aspirin in high doses (4-5 g/day)?

A

increases urinary excretion by inhibiting the reabsorption in the PCT

33
Q

True of False: Aspirin should not be used in combination with Probenecid?

A

True

34
Q

What drugs interact with Probenecid?

A

Penicillins and Beta-lactams

35
Q

What happens if you take Probencid with Penicillins and Beta-lactams?

A

increases duration of action by inhibiting the renal tubular secretion of these drugs

36
Q

Is Probenecid effective in patients with renal insufficiency?

A

no

37
Q

What are common toxicities of Probenecid?

A

GI irritation and skin rash

38
Q

Probenecid (increases or decreases?) the rise of urate neprolithiasis?

A

increases

39
Q

Probenecid is contraindicated in patients with _______

A

kidney stones

40
Q

Allopurinol (increases or decreases?) uric acid levels in the plasma by inhibiting the biosynthesis in the body?

A

decreases

41
Q

True of False: Allopurinol is a noncompetitive inhibitor of the xanthine oxidase enzyme?

A

false- it is a competitive inhibitor

42
Q

What is Allopurinol’s MOA?

A

Competitive inhibitor of xanthine oxidase enzyme which inhibits the synthesis of uric acid by inhibiting the conversion of xanthine and hypoxanthine

43
Q

What does inhibition of the synthesis of uric acid lead to?

A

decrease in the plasma urate levels and a decrease in the size of the urate pool in the body

44
Q

Are xanthine and hypoxanthine more soluble than uric acid?

A

yes

45
Q

True or False: The action of Allopurinol leads to an increase of the more soluble xanthine and hypoxanthine?

A

True

46
Q

What is Allopurinol’s toxicities?

A

hypersensitivity reactions, liver enzyme abnormalities, and leucopenia

47
Q

What drug interacts with Allopurinol?

A

Mercaptopurine

48
Q

What effect does xanthine oxidase have on Mercaptopurine?

A

xanthine oxidase catalyzes the metabolism of Mercaptopurine and increases its plasma levels and toxicity

49
Q

What is Febuxostat’s MOA?

A

Decreases serum urate concentrations by decreasing urate synthesis

50
Q

What is Febuxostat?

A

xanthine oxidase inhibitor

51
Q

Is Febuxostat more or less effective than allopurinol for chronic treatment of hyperuricemia in patients with gout?

A

more effective

52
Q

What are some adverse effects of Febuxostat?

A

liver function abnormalities, arthralgias, and rash

53
Q

Febuxostat is contraindicated in patients being treated with ____________________

A

azathiopurine, mercaptopurine, or theophylline, which are metabolized by xanthine oxidase

54
Q

What is Pegloticase?

A

PEGylated recombinated uricase enzyme

55
Q

What is the function of the uricase enzyme?

A

converts uric acid to allantoin

56
Q

How is Pegloticase administered?

A

IV infusion

57
Q

Pegloticase has a black box warning for?

A

anaphylaxis, infusion reactions (uticaria, dyspnea, chest pain, erythmia, and pruritus), delayed-type hypersensitivity reactions and gout flares (first 3 months)

58
Q

Patients should be pre-medicated with ____________ as gout flare prophylaxis before receiving Pegloticase

A

Colchicine or NSAIDs

59
Q

Pegloticase is contraindicated in patients with?

A

glucose-6-phosphate dehydrogenase (G6PD) deficiency

60
Q

Pre-medication with ____________ minimizes black box side effects

A

antihistamines and corticosteroids

Drug Mech Final (7 decks)

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