GOUT MEDICINES

Question 1

Give the 9 AntiGour drugs discussed

Answer 1

Allopurinol
Febuxostat
Probenecid
Sulfinpyrazole
Colchicine
NSAIDs
Glucocorticoids
Pegloticase
Interleukin I Inhibitor

Question 2

Goals of therapy of gout

Answer 2

Relieve acute attacks

Prevent recurrent gouty episodes and urate lithiasis

Question 3

General mechanisms give

ALLOPURINOL & FEBUXOSTAT

PROBENECID & SULFINPYRAZOLE (Uricosuric)

COLCHICINE

Answer 3

A & F - decrease uric acid synthesis

S & C Increase uric acid secretion

Col - inhibition of leukocyte migration + phagocytosis into the joint (colchicine call to the scene —> that’s what you inhibit)

Question 4

MOA of Allopurinol

Answer 4

Becomes Alloxanthine that inhibits Xanthin Oxidase —> decreased Uric acid production

Question 5

Allopurinol ____% reabsorbed after oral administation

Oral half life

Dosing: how many times a day?

Answer 5

80%

2-3 hrs half life

1 a day cos long duration

Question 6

DRUG INTERACTIONS OF ALLOPURINOL (3)

1 effect on iron metab

Answer 6

Dose of MERCAPTOPURINE must be reduced to 75% when give with AP

Increase effect of cyclophosphamide

Decrease metabolism of PROBENECID & oral anticoagulants ***

Increase hepatic iron conc.

Question 7

Febuxostat MOA

Answer 7

Potent and selective inhibitor of xanthin oxidase

Question 8

Dose of febuxostat

Answer 8

40-80 mg/day

Question 9

Adverse effects of febuxostat:

Answer 9

Liver function abnormalities

Question 10

PK of Febuxostat

% absorption

t1/2

Answer 10

80% absorption after oral ad

4-18 hrs

Question 11

MOA of Probenecid and SULFINPYRAZOLE

Answer 11

Decreases net absorption of uric acid in the mid segment of the renal proximal tubule

—> decrease in urate pool, less tophaceous deposits

Question 12

Difference on the PK or Probenecid and Sulfinpyrazole

Answer 12

Probenecid - completely reabsorbed by the renal tubules

Metabolized slowly

T1/2: 5-8 hrs

SULFINPYRAZOLE - RAPIDLY EXCRETED

Question 13

Indication of Uricosurics

Answer 13

If di pwede yung mentioned earlier na xanthine oxidase inhibitors

Question 14

When is therapy initiated for Uricosurics?

Answer 14

2-3 weeks after acute attack

Question 15

Precautions when giving Uricosurics:

Answer 15

Renal Stone formation

High urine vol

Urine pH kept above 6.0 - Alkaline

Therapy 2-3 weeks after

Question 16

Adverse effect of uricosurics:

Answer 16

GI irritation

Question 17

Primary tx for ACUTE GOUT

Answer 17

Colchicine

Question 18

Nice about cochicine

Answer 18

Relieves pain and inflammation in 12-24 hrs w/o altering the metab and excretion of uric acid and w/o other analgesic effects

Question 19

MOA of COLCHICINE

Answer 19

Inhibition of leukocytes in migrating to joints

This is through:

1. IGAWID NA. BINDING to Intracellular protein tubules —> preventing it’s polymerization INTO MICROTUBULE (na need para makagalaw? Hahaha)
2. Inhibits formation of leukotriene B4 (LTB4)

Question 20

Peak plasma levels with ___ hrs of colchicine

Answer 20

2 hrs

Question 21

Half life of colchicine

Answer 21

9 hrs

Question 22

Pegloticase MOA

Answer 22

Converts acid allantoin which us highly soluble & easily excreted