Sulfinpyrazone Probenecid

Drugs that may be affected by aspirin include ACE inhibitors, acetazolamide, anticoagulants, anticonvulsants (hydantoins, valproic acid), beta blockers, diuretics, methotrexate, NSAIDs, oral hypoglycemics, and uricosuric agents (probenecid, sulfinpyrazone). 

In the proximal tubule probenecid, sulfinpyrazone and benzbromarone enhance the excretion of uric acid Although they compete with uric acid for active secretion by the proximal tubules, resorption of uric acid in the proximal tubules is also inhibited with as a net effect the promotion of uric acid excretion. Indications for the use of uricosurics are repeated attacks of gout, the presence of renal impairment associated with hyperuricaemia and the presence of chronic gouty arthropathy or tophi. 

PENICILLINS PROBENECID, SULFINPYRAZONE t penicillin levels Uncertain Watch for t incidence of side-effects... 

NITROFURANTOIN ANTIGOUT DRUGS- PROBENECID, SULFINPYRAZONE i efficacy of nitrofurantoin in urinaiy tract infections L urinary excretion Watch for poor response to nitrofurantoin... 

Clinically important, potentially hazardous interactions with estrogens, methotrexate, phenindione, probenecid, sulfinpyrazone, warfarin... 

MRP5 (ABCC5) pancreas, bladder Ubiquitous Basolateral cyclic nucleotide (cAMP, cGMP), GSH, PMEA Cyclic nucleotide analogs. Probenecid, sulfinpyrazone,... 

URATl (SLC22A12) Kidney Apical Urate Probenecid, sulfinpyrazone, benzbromarone losartan loop diuretics... 

The aims of treatment are to decrease the symptoms of an acute attack, decrease the risk of recurrent attacks, and lower serum urate levels. Therapy of gout focuses on colchicine, allopurinol, and the uricosuric agents—probenecid, sulfinpyrazone, and ben7,bromarone. 

Mechanism Uricosuric agents (probenecid, sulfinpyrazone) are weak acids that compete with uric acid for reabsorption by the weak acid transport mechanism in the S2 segment of the proximal renal tubule. At low doses, these agents may also compete with uric acid for secretion by the tubule and (occasionally) can even elevate serum uric acid concentration. Elevation of uric acid levels by this mechanism occurs with aspirin (another weak acid) over much of its dose range. 

Nitrofurantoin (Macrodanrin, Furadanrin, Macrobid) [Urinary Anri-infective] WARNING Pulm Rxns possible Uses Prevendon Rx UTE Action Bacteriostatic iaterferes w/ carbohydrate metabolism. Dose Adults. Suppression 50-100 mg/d PO Rx 50-100 mg PO qid Peds. Suppression 1-2 mg/kg/d ia 1—2 + doses, max 100 mg/d Rx 5—7 mg/lcg/24 h ia 4 + doses (w/ food/milk/antacid) Caution [B, +] Avoid w/ CrCl <60 ml ymin, PRG at term Contra Renal failure, infants <1 mo Disp Cperipheral neuropathy Interactions T Effects W/ probenecid, sulfinpyrazone 4 effects w/ antacids, quinolones EMS May affect glucose (hypoglycemia) may discolor urine OD May cause N/V give IV fluids... 

The amount of urate bound in the absence of drugs was regarded as the baseline and the amounts bound in the presence of various drugs were expressed as percentages of the control values (Fig. 2). It can be seen that probenecid, sulfinpyrazone and sodium salicylate all significantly displaced urate from human albumin binding sites, while colchicine had no effect. 

Ethambutol had no effect on the urinary excretion of sodium or potassium and there was no clinical evidence of volume depletion in patients receiving this agent. The hyperuricemia of ethambutol was not reversed by salicylates in 3 patients in whom this was studied. Ethambutol did not inhibit the effect of probenecid, sulfinpyrazone or iopanoic acid in 3 additional patients. 

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