RHEUM - Gout Drugs - Sweatman Flashcards
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
