Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: EC:6.3.4.6 (urease)
 7,490 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

The formation of struvite stones is closely linked to the enzyme urease produced by certain bacteria found in urine. It has been shown that hydroxamic acids will block the activity of this enzyme. One of these, hydroxyurea, in a morning dose of 500 mg. was used in 21 patients for three months or longer. Most were then able to acidify their urine despite persistent urinary infection. After three months, treatment with nitrofurantoin (Macrodantin and hydroxyurea (Hydrea), 78.6 per cent of patients had persistently sterile urine. There are 11 patients who have been observed for one year, and no toxic effect of the drug has been found. Three patients have shown some decrease in size of their retained calculus. This experimental study has shown that hydroxyurea may be useful in the management of struvite stones and deserves further study.
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PMID:Hydroxyurea and infected stones. 63 34

A single oral administration of the urease inhibitor benurestat (2-(p-chlorobenz-amido)acetohydroxamic acid) to the human at 15 or 25 mg per kg produced, for 4 hr, mean urinary levels of inhibitory activity that were 700 to 1900 times that equivalent concentration of benurestat required to inhibit Proteus mirabilis urease by 90 per cent. In the rat these same dosage levels produced urinary inhibitory activity equivalent to 16 to 140 fold that required for 90 per cent urease inhibition. Benurestat administration, 25, 50, or 100 mg per kg, caused a decrease in the urinary excretion of ammonia from rats with experimental P. mirabilis genitourinary tract infection. The formation of struvite calculi was inhibited under these conditions. Nitrofurantoin, sulfamethoxazole, and ampicillin also slowed the formation of struvite calculi in infected rats and together with benurestat a potentiation of the inhibition of calculi formation was secured. Some combination therapies composed of benurestat plus an antibacterial agent, sulfamethoxazole or ampicillin, were effective in promoting the net dissolution of formed calculi. The number of viable bacteria present in the bladders of infected rats was significantly less after the administration of benurestat plus nitrofurantoin, sulfamethoxazole, or ampicillin than the respective numbers that were obtained from control infected rats or from rats administered either component of the combination separately.
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PMID:Benurestat, a urease inhibitor for the therapy of infected ureolysis. 108 13

Three pilot studies were performed to evaluate the efficacy of bismuth subsalicylate (BSS) and nitrofurantoin to eradicate Campylobacter pylori colonization in man. Nitrofurantoin 3 x 100 mg capsules for 10 days did not clear C. pylori in any of 13 patients, and neither did the combination of BSS and nitrofurantoin suspension (0/6 patients). Immediately after high dose BSS therapy 3 x 900 mg for 28 days, 8/17 patients (47%) had negative cultures and rapid urease tests. There was recrudescence in 5 out of 6 patients so far submitted to follow-up investigations, giving a best possible outcome estimate of 18% and a worst possible eradication rate of 6% in this study. Preliminary data indicate that triple therapy may be a more effective option, but doubts remain as to whether the puristic therapeutic goal of complete bacterial eradication can be safely and effectively achieved with presently available drugs.
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PMID:Monotherapy or polychemotherapy in the treatment of Campylobacter pylori-related gastroduodenal disease. 316 27