Anti-Gout

Question 1

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

Answer 1

Colchicine

Question 2

Does Colchicine alter the metabolism or excretion of uric acid?

Answer 2

No

Question 3

What is Colchicine’s MOA?

Answer 3

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

Question 4

What are some rare complications of Colchicine (toxicities)?

Answer 4

Myelosuppression and neuropathy

Question 5

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

Answer 5

Myopathy or rhabdomyolysis

Question 6

What are NSAIDs used for with patients who have gout?

Answer 6

used for their anti-inflammatory effects

Question 7

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

Answer 7

Aspirin

Question 8

Why is Aspirin not recommended for gout treatment?

Answer 8

because it increases the plasma levels of uric acid

Question 9

What do NSAIDs treat for in patients who have gout?

Answer 9

Acute gout attacks

Used for prophylaxis for gout arthritis

Question 10

What is the MOA of NSAIDs?

Answer 10

Inhibit the phagocytosis of uric acid crystals in the joint

Question 11

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

Answer 11

Corticosteroids

Question 12

Name the corticosteroids that are used to treat patients with gout

Answer 12

Prednisone
Methylprednisolone
Triamcinolone

Question 13

Name the Interleukin-1 (IL-1) Inhibitors

Answer 13

Canakinumab

Anakinra

Question 14

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?

Answer 14

Canakinumab

Question 15

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?

Answer 15

Anakinra

Question 16

Name the Uricosuric Agent

Answer 16

Probenecid

Question 17

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

Answer 17

decrease

Question 18

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

Answer 18

increase

Question 19

What can increased urinary excretion of uric acid lead to?

Answer 19

the formation of urate calculi (stones) in the kidney

Question 20

What is Probenecid’s MOA?

Answer 20

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

Question 21

How is uric acid secreted?

Answer 21

glomerular filtration and active renal tubular secretion

Question 22

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

Answer 22

renal proximal tubule

Question 23

How is urate exchanged for organic or inorganic anions?

Answer 23

by the Organic Anion Transporter (URAT-1)

Question 24

Low dosage of uricosuric agents usually results in ___________

Answer 24

decreased urinary excretion of urate

Question 25

Higher dosage of uricosuric agents results in _________________

Answer 25

increased urinary excretion of urate

Question 26

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

Answer 26

inhibits its reabsorption via the urate-anion exchanger system

Question 27

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

Answer 27

increase

Question 28

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

Answer 28

True

Question 29

True or False: Uricosuric drugs are not organic acids?

Answer 29

False

Question 30

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

Answer 30

True

Question 31

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

Answer 31

decrease urinary excretion of uric acid by inhibiting the transporter

Question 32

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

Answer 32

increases urinary excretion by inhibiting the reabsorption in the PCT

Question 33

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

Answer 33

True

Question 34

What drugs interact with Probenecid?

Answer 34

Penicillins and Beta-lactams

Question 35

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

Answer 35

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

Question 36

Is Probenecid effective in patients with renal insufficiency?

Answer 36

no

Question 37

What are common toxicities of Probenecid?

Answer 37

GI irritation and skin rash

Question 38

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

Answer 38

increases

Question 39

Probenecid is contraindicated in patients with _______

Answer 39

kidney stones

Question 40

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

Answer 40

decreases

Question 41

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

Answer 41

false- it is a competitive inhibitor

Question 42

What is Allopurinol's MOA?

Answer 42

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

Question 43

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

Answer 43

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

Question 44

Are xanthine and hypoxanthine more soluble than uric acid?

Answer 44

yes

Question 45

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

Answer 45

True

Question 46

What is Allopurinol's toxicities?

Answer 46

hypersensitivity reactions, liver enzyme abnormalities, and leucopenia

Question 47

What drug interacts with Allopurinol?

Answer 47

Mercaptopurine

Question 48

What effect does xanthine oxidase have on Mercaptopurine?

Answer 48

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

Question 49

What is Febuxostat's MOA?

Answer 49

Decreases serum urate concentrations by decreasing urate synthesis

Question 50

What is Febuxostat?

Answer 50

xanthine oxidase inhibitor

Question 51

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

Answer 51

more effective

Question 52

What are some adverse effects of Febuxostat?

Answer 52

liver function abnormalities, arthralgias, and rash

Question 53

Febuxostat is contraindicated in patients being treated with ____________________

Answer 53

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

Question 54

What is Pegloticase?

Answer 54

PEGylated recombinated uricase enzyme

Question 55

What is the function of the uricase enzyme?

Answer 55

converts uric acid to allantoin

Question 56

How is Pegloticase administered?

Answer 56

IV infusion

Question 57

Pegloticase has a black box warning for?

Answer 57

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

Question 58

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

Answer 58

Colchicine or NSAIDs

Question 59

Pegloticase is contraindicated in patients with?

Answer 59

glucose-6-phosphate dehydrogenase (G6PD) deficiency

Question 60

Pre-medication with ____________ minimizes black box side effects

Answer 60

antihistamines and corticosteroids