RHEUM - Gout Drugs - Sweatman Flashcards Preview

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Flashcards in RHEUM - Gout Drugs - Sweatman Deck (20):

What are the drugs used to treat gout?

1) Colchicine
2) Indomethacin
3) Allopurinol
4) Probenecid
5) Febuxostat
6) Pegloticase


What are the causes of gout and which causes most cases?

Metabolic and renal --> 90% are renal


What enzymes are known to cause primary genetic metabolic gout?

PRPP synthetase (activating mutation) and HGPRT (removes hypoxanthine salvage pathway)


What is the mechanism of action of colchicine?

Depolymerization of microtubules so PMNs can't enter joint and phagocytose uric acid crystals


What si colchicine used for therapeutically?

Terminate acute gout attack and prevent gout attacks


What are some common side effect of colchicine?

1) GI disturbances2) Blood dycrasias3) Peripheral neuropathy4) Renal failure5) Proximal muscle weakness and increased CPK6) Chronic therapy can cause bone marrow suppression


What is the mechanism of action of indomethacin?

NSAID --> inhibits COX 1 and 2


What is the therapeutic use of indomethacin in gout?

Treatment of acute gout attack


What are the adverse effects of indomethacin?

1) N/V and GI ulcers --> give with antacid
2) Hematopoietic disorders


What is the mechanism of action of allopurinol?

Competitive inhibitor of xanthine oxidase


What are the therapeutic uses of allopurinol?

1) treat primary hyperuricemia in people with enzyme deficiency2) Treat secondary hyperuricemia due to hematological disorders


What are some adverse effects of using allopurinol?

1) increased incidence of acute gout due to immobilization from joints2) Increase levels of 6-mercaptopurine and 6-thioguanine


What is the mechanism of action of febuxostat?

Inhibits xanthine oxidase --> lowers blood levels of uric acid like allopurinol


What are the primary indications for febuxostat?

Used in pts who can't take allopurinol --> hypersensitivity, or people with renal insufficiency


What is the mechanism of action of probenecid?

Inhibits reabsorption of organic anion in proximal CT, which blocks reabsorption of urate


What drugs inhibit the uricosuric effect of probenecid?

Salicylates (aspirin) and HCTZ


What si the mechanism of action of pegloticase?

Enzyme found in most mammals that converts urate into allantoin --> given IV


What are the primary therapeutic uses of pegloticase?

Treat patients with severe gout that don't respond to other therapies


What is the major side effect of pegloticase?

Increased acute gout due to dissolution of tophi --> given NSAIDs, colchicine, glucocorticoids prophylactically


what is the rate limiting step of the synthesis of uric acid?

the step catalyzed by PRPP synthetase