Gout Drugs Flashcards
NSAIDs
Treatment of Acute gout
Excluding low dose Aspirin, are used to treat acute attacks of gout.
At lower doses (2-3g/day) aspirin causes uric acid retention by the kidney, whereas at higher doses, aspirin has a uricosuric effect. In most individuals, low dose aspirin that is being administered for its CV protective effects does not need to be discontinued.
Colchicine
Treatment of Acute gout
MOA: inhibits microtubule assembly. Suppresses inflammasome-driven caspase 1 activation, IL-1B processing and release, and L-selectin expression
SE: GI symptoms (diarrhea, abdominal pain, nausea, vomiting), and readily reversible peripheral neuropathy. More severe colchicine toxicity:(blood cytopenias, severe cutaneous eruption) has only rarely been reported
Cautions: Contraindication in patients with advanced renal or hepatic impairment
Notes: Used in patients who have contraindications to NSAIDs
Allopurinol
Treatment of Chronic Gout
MOA: Xanthine oxidase inhibitor-inhibits uric acid synthesis
SE: Mild rash, can cause leukopenia or thrombocytopenia; diarrhea; can precipitate acute gouty arthritis
Caution: patients with renal insufficiency
Contraindication: known hypersensitivity
Notes: Although reduced renal uric excretion is responsible for the majority of cases of hyperuricemia, allopurinol, which inhibits the production of uric acid is the first line of defense
Febuxostat
Treatment of Chronic Gout
MOA: Xanthine oxidase inhibitor
SE: incidence of liver function test abnormalities, nausea, arthralgia, and rash; increased risk of acute gouty attack
Caution: periodic monitoring of the liver function, principally hepatic transaminase enzyme levels is suggested
Notes: more expensive than allopurinol
Probenecid
Treatment of Chronic Gout
Uricosuric agent
MOA: promotes renal clearance of uric acid by inhibiting urate-anion exchangers (including URAT1) in the proximal tubule that mediates urate reabsorption. It increases urate excretion
SE: rash, precipitation of acute gouty arthritis, GI intolerance, and uric acid stone formation.
Caution: interferes with the renal transport of various drugs that are organic acids (penicillin and ampicillin) and which undergo transport int he kidney; consequently, there is a need to adjust dosage of these drugs.
Contraindication: patients in whom nephrolithiasis or uric acid nephropathy may occur
Notes: Efficacy is reduced in patients with impaired renal function, relatively short half life, multiple drug interactions due to inhibition of organic anion transporter
Lesinurad
Treatment of Chronic Gout
MOA: inhibits activity of URAT1 and OAT4 in vitro; does not inhibit GLUT9 or ABCG2; does not inhibit OAT1 or OAT3 like Probenecid
SE: headache, influenza, higher levels of blood creatinine, and GERD
Caution: patient need to be cautioned to stay well hydrated
Warning: increased risk of acute renal failure
Contraindication: patients with severe renal impairment, end stage renal disease, kidney transplant, or patients on dialysis
Notes: often administered with Allopurinol
Pegloticase
Treatment of Chronic Gout
MOA: recombinant uricase, which converts uric acid to allantoin
SE: increased risk of acute gouty attack
Caution: infusion reaction, patients may develop anti-pegloticase antibodies
Contraindication: patients with G6PD deficiency
