Probenecid

Chemical Name 4-[(Dipropylamino)sulfonyl] benzoic acid 

Trade Name Manufacturer Country Year Introduced 

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The thia2ides are actively secreted into the proximal tubules, where they exert their action on the luminal side of the tubules. The diuretic effect occurs within 1 h after oral adininistration, and the duration of action varies from 4 to 24 h depending on which thia2ide-type diuretic is used. The diuretic effects of the thia2ides are not influenced by acid—base conditions of the blood or urine. Probenecid, which also is secreted into the proximal tubules, may block the diuretic effects of the thia2ides. 

Di-n-propylacetyl chloride Anistropine methyl bromide Di-n-propylamine Probenecid Dipyridamole Mopidamol... 

The daily dose ofprobenecid is 0.5-3.0 g. Probenecid is well tolerated, and there are few serious side effects. In... 

The daily dose of sulfinpyrazone is 200-400 mg. The side effects of sulfinpyrazone are comparable with those of probenecid. A potential therapeutic advantage of sulfinpyrazone in patients with coronary heart disease and thromboembolic diseases is its inhibitory effect on platelet aggregation. 

The co-administration of drugs which inhibit the transporters involved in renal tubular secretion can reduce the urinaty excretion of drugs which are substrates of the transporter, leading to elevated plasma concentrations of the drugs. For example, probenecid increases the plasma concentration and the duration of effect of penicillin by inhibiting its renal tubular secretion. It also elevates the plasma concentration of methotrexate by the same mechanism, provoking its toxic effects. 

Uricosuric dtugs increase the renal excretion of uric acid by inhibiting its renal reabsorption. Therapeutically used uricosuric dtugs are benzbromarone, probenecid and sulfinpyrazone. 

In those with gout, the serum uric acid level is usually elevated. Sulfinpyrazone increases the excretion of uric acid by the kidneys, which lowers serum uric acid levels and consequently retards the deposit of urate crystals in the joints. Probenecid (Benemid) works in the same manner and may be given alone or with colchicine as combination therapy when there are frequent, recurrent attacks of gout. Probenecid also has been used to prolong the plasma levels of the penicillins and cephalosporins. 

The drugp used for gout are contraindicated in patients with known hypersensitivity. Probenecid is contraindicated in patients with blood dyscrasias or uric acid kidney stones and in children younger than 2 years. Sulfinpyrazone is contraindicated in patients with peptic ulcer disease and gastrointestinal inflammation. Colchicine is contraindicated in patients with serious gastrointestinal, renal, hepatic, or cardiac disorders and those with blood dyscrasias. 

Salicylates antagonize probenecid s uricosuric action. Concurrent administration of probenecid increases die effects of acyclovir, barbiturates, benzodiazepines, dap-sone, mediotrexate, NSAIDs, rifampin, and the sulfonamides. 

There is an increased risk of toxicity of MTX when administered with the NSAIDs, salicylates, oral antidiabetic drugs, phenytoin, tetracycline, and probenecid. There is an additive bone marrow depressant effect when administered with other drug known to depress the bone marrow or with radiation therapy. There is an increased risk for nephrotoxicity when MTX is administered with other drug that cause nephrotoxicity. When penicillamine is administered with digoxin, decreased blood levels of digoxin may occur. There is a decreased absorption of penicillamine when the dmg is administered with food, iron preparations, and antacids. 

Cinoxacin is contraindicated in patients with known hypersensitivity to the individual drug and in patients with anuria. Cinoxacin is a Pregnancy Category B drug and should be used with caution during pregnancy and lactation. Cinoxacin is used with caution in patients with hepatic impairment. When cinoxacin is administered with probenecid, there is a risk for lowered urine concentration of cinoxacin. 

Colbenemid (Merck Sharp Dohme)-comb. wfm Probenecid (IFI)... 

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