benzofurans and Gout

Topics: Benzbromarone; Benzofurans; Biological Availability; Chemical Phenomena; Chemistry; Gout; Half-Life; Humans; Time Factors; Uric Acid

Topics: Allopurinol; Balneology; Benzofurans; Crystallization; Diagnosis, Differential; Exercise Therapy; Glomerular Filtration Rate; Gout; Probenecid; Sulfinpyrazone; Uric Acid; Urinary Calculi

Benzbromarone1 is a benzofuran derivative which lowers serum urate and increases urinary urate excretion in normal, hyperuricaemic and gouty subjects. In open short- and long-term studies benzbromarone reduced serum uric acid levels by one-third to one-half and maintained its effectiveness for periods of up to 8 years. Single-dose experimental studies have shown benzbromarone to have a urate-lowering effect similar to that of a therapeutic dose of probenecid or sulphinpyrazone, but unlike these drugs benzbromarone can be administered in a once daily regimen. In 2 short-term comparative therapeutic trials in a small number of patients with hyperuricaemia, 80mg of micronised benzbromarone daily was at least as effective as 1000mg of probenecid or 300mg of allopurinol daily in lowering serum uric acid levels. Side-effects during benzbromarone administration are usually mild and primarily gastrointestinal in nature.

Topics: Aspirin; Benzbromarone; Benzofurans; Drug Interactions; Fasting; Gout; Humans; Kidney Diseases; Kinetics; Lipid Metabolism; Pyrazinamide; Triglycerides; Uric Acid; Xanthine Oxidase

Topics: Acute Disease; Allopurinol; Antineoplastic Agents; Benzofurans; Colchicine; Female; Gout; Humans; Phenylbutazone; Pregnancy; Probenecid; Sulfinpyrazone; Uricosuric Agents; Vasodilator Agents; Zoxazolamine

Topics: Adult; Aged; Allopurinol; Benzbromarone; Benzofurans; Dose-Response Relationship, Drug; Drug Therapy, Combination; Female; Gout; Humans; Male; Metabolic Clearance Rate; Middle Aged; Oxypurinol; Purines; Pyrimidines

Topics: Allopurinol; Benzbromarone; Benzofurans; Clinical Trials as Topic; Gout; Humans; Uric Acid

Topics: Adult; Aged; Benzbromarone; Benzofurans; Clinical Trials as Topic; Gout; Humans; Male; Middle Aged; Uric Acid

Topics: Benzbromarone; Benzofurans; Clinical Trials as Topic; Follow-Up Studies; Gout; Humans; Uric Acid

The uric-acid lowering effect was investigated in a group of 2220 patients. 1984 of these were employed for statistical evaluation purposes. On average, the uric acid level was reduced from 8,24 +/- 1,16 mg/100 ml to 5,32 +/- 1,265 mg/100 ml. In 82 % of all the cases, the uric acid level at the end of the treatment period was below 6,4 mg%, both in patients treated throughout with 50 mg benzbromarone (NarcaricinRmite) and in those changed over to 100 mg benzbromarone (NarcaricinR) after 1 to 3 weeks. The lowering of the uric acid levels was in no way related to hypertension, adiposity, hyperlipoproteinaemia, diabetes mellitus or age.

Topics: Benzbromarone; Benzofurans; Body Height; Body Weight; Clinical Trials as Topic; Female; Follow-Up Studies; Gout; Humans; Male; Uric Acid

Topics: Benzofurans; Clinical Trials as Topic; Gout; Humans; Male; Middle Aged; Uric Acid

12 hyperuremic male patients got during two comparative tests for 16 days 300 mg/die Allopurinol or 100 mg/die Benzbromarone or a combination of 100 mg Allopurinol with 20 mg Benzbromarone. During this time the renal elimination of uric acid, sodium, calcium, magnesium and citrate war measured and the renal clearance of uric acid, creatinine and sodium was determinated. Without any therapy the combination of 100 mg Allopurinol with 20 mg Benzbromarone per die reduces the elimination of uric acid significantly under the original value in the 24-hour-urine. The elimination of the uric acid increases with 300 mg/die Allopurinol. The clearance ratio of uric acid and creatinine rises 33% to 60%. With 100 mg/die Benzbromarone this value goes up to 233% compared with the results without therapy. At the same time the therapy with Brenzbromarone makes the clearance ratio of uric acid to sodium rise significantly to 257%. Under the 3 types of therapy there is no significant change in the 24-hours-urine of the clearance of creatinine and sodium, the clearance ratio of sodium to creatinine and the elimination ratio of sodium, calcium, magnesium and citrate. Hyperuremic patients with urolithic diathesis need Allopurinol therapy without any combination.

Topics: Adult; Aged; Allopurinol; Benzbromarone; Benzofurans; Calcium; Citrates; Creatinine; Glomerular Filtration Rate; Gout; Humans; Magnesium; Male; Middle Aged; Natriuresis; Sodium; Uric Acid

Topics: Adult; Allopurinol; Benzbromarone; Benzofurans; Clinical Trials as Topic; Drug Combinations; Female; Gout; Humans; Male; Metabolic Clearance Rate; Middle Aged; Uric Acid

Topics: Adolescent; Adult; Benzbromarone; Benzofurans; Fasting; Female; Gout; Humans; Male; Middle Aged; Starvation; Uric Acid

Benzbromarone, a synthetic benzofurane, was administered in a series of 23 patients with hyperuricaemia: 5 with gout, 8 with secondary forms, 6 with renal insufficiency, 4 undergoing diuresis with etacrinic acid. The drug was also given to 10 subjects with normal values. A surprisingly rapid and constant hypouricamising effect was noted, together with marked hyperuricuria. These changes were more prompt in the controls and relatively late and protracted in the diseased subjects, expecially those with gout. The drug was also active in renal insufficiency. Its effects ceased on suspension. It cannot be seen as a simple hyperuricuric preparation, since it may have some effect on the metabolic pathways that degrade purines to uric acid. The drug is similar to benziodarone. The replacement of iodine by two bromine atoms in its formula, however, ensures its freedom from side-effects.

Topics: Adult; Aged; Benzofurans; Clinical Trials as Topic; Drug Evaluation; Drug Tolerance; Ethacrynic Acid; Glomerular Filtration Rate; Gout; Humans; Ketones; Kidney Failure, Chronic; Middle Aged; Uric Acid

Topics: Acute Kidney Injury; Adult; Aged; Allopurinol; Benzofurans; Clinical Trials as Topic; Gout; Humans; Kidney Diseases; Kidney Failure, Chronic; Metabolic Clearance Rate; Middle Aged; Urea; Uric Acid

Topics: Adolescent; Adult; Aged; Benzofurans; Clinical Trials as Topic; Female; Gout; Humans; Male; Middle Aged; Uricosuric Agents

Topics: Benzofurans; Bromine; Clinical Trials as Topic; Gout; Humans; Iodine; Uric Acid; Uricosuric Agents; Xanthines

Twenty male hyperuricaemic patients with normal kidney function were studied and it was found that the serum concentrations and excretions rates in the 24-hour urine of allopurinol and oxipurinol do not differ significantly after 9 days of oral treatment with either 300 mg allopurinol or a combination of 300 mg allopurinol and 60 mg benzbromarone daily. The sum of the excretion rates of the two pyrazolopyrimidines in the 24-hour urine represents 80.9% and 77.1%, respectively of the daily dose of allopurinol given alone or in combination with benzbromarone. As expected, the hypouricaemic effect of the combined therapy turned out to be stronger than that observed after monotherapy with allopurinol, due to the uricosuric component of benzbromarone. The difference was found to be highly significant.

Topics: Adult; Aged; Allopurinol; Benzbromarone; Benzofurans; Creatinine; Drug Therapy, Combination; Glomerular Filtration Rate; Gout; Humans; Male; Middle Aged; Oxypurinol; Pyrimidines; Uric Acid

Topics: Allopurinol; Benzbromarone; Benzofurans; Drug Therapy, Combination; Fatty Liver, Alcoholic; Gout; Humans; Hypoxanthine; Hypoxanthines; Uric Acid; Xanthine; Xanthines

Topics: Allopurinol; Benzbromarone; Benzofurans; Chemical Phenomena; Chemistry; Drug Therapy, Combination; Gout; Humans; Uric Acid

Topics: Adult; Aged; Allopurinol; Benzbromarone; Benzofurans; Drug Interactions; Drug Therapy, Combination; Gout; Humans; Kidney Failure, Chronic; Male; Middle Aged; Phenylbutazone

The results over 10 years in 200 patients (103 with gout and 97 with hyperuricaemia) treated with benzbromarone 75 - 120 mg/d are reported. The average stable decrease in the serum uric acid level was 54%. The severity and incidence of articular manifestations in the patients with gout were reduced by 75% before the end of the 1st year of treatment; relapses were very uncommon in the following years. In all cases tophaceous deposits disappeared within 6 - 18 months. Adequate fluid intake and alkalinization of urine effectively contributed to a low incidence of urinary incidents (3%), although 35% of the patients were overexcretors of urate before treatment and 33% had a previous history of urolithiasis or associated urinary problems. The drug was well tolerated by 96% of the patients. Renal tolerance has been demonstrated by routine urinalysis and functional tests, as has the long-term safety of the drug with regard to the liver, nervous system and eyes. The biological and clinical results suggest that benzbromarone should be considered as the drug of choice in the majority of gouty and hyperuricaemic patients.

Topics: Adult; Aged; Benzbromarone; Benzofurans; Female; Follow-Up Studies; Gout; Humans; Male; Middle Aged; Time Factors; Uric Acid

Topics: Benzbromarone; Benzofurans; Gout; Humans; Hydrogen-Ion Concentration; Uric Acid; Urine

Topics: Adult; Aged; Benzbromarone; Benzofurans; Female; Gout; Humans; Male; Middle Aged

The effect of the uricosuric drug benzdromarone was investigated in 15 patients with hyperuricemia and renal failure. Benzbromarone micron was given in a dose of 80 mg/day for 6 days. The mean serum uric acid level fell from 8.9 to 4.24 mg/100 ml. After therapy uric acid concentrations in serum returned to 5.2 mg/100 ml. Renal urate elimination was increased from 487 mg/day to 831.3 mg/day; after medication urate elimination decreased to the initial values. Uric acid clearance was increased by benzbromarone from 3.97 to 11.1 ml/min, and even after therapy a uric acid clearance of 6.4 ml/min could be measured. A decrease of uric acid reabsorption from 4.73 to 2.3 mg/min was observed, after medication the reabsorption rate increased to 3.42 mg/min.

Topics: Adult; Aged; Benzbromarone; Benzofurans; Creatinine; Drug Evaluation; Gout; Humans; Kidney Diseases; Male; Middle Aged; Uric Acid

Topics: Adolescent; Adult; Aged; Allopurinol; Benzbromarone; Benzofurans; Drug Combinations; Drug Evaluation; Female; Gout; Humans; Male; Middle Aged; Uric Acid

Rational therapy of gout must be correlated with the two basic aetiopathogenetic factors, i.e. metabolic error and the inflammatory dysreactive moment. Due to its different action mechanism, the former is responsible for the typing of adult primary hyperuricaemia: a) hyperincorporating and hyperescretory forms; b) normo-incorporating and relatively or absolutely hypoexcretory forms; c) hyperincorporating and hyposcretory forms. It would be a mistake to treat the condition chemically without knowing the physiopathology of the metabolic error. On the basis of a preliminary typing assessment, rational chemical correction of the metabolic error in gout cases can be achieved with drugs that block the enhanced endogenous synthesis of uric acid (allopurinol, etc.) or correct the metabolite renal excretion defect. Therapy of the dysreactive-inflammatory component should involve non-steroid anti-inflammatory drugs. The disadvantages of using cortisones in gout treatment are stressed.

Topics: Allopurinol; Benzofurans; Gout; Humans; Life Style; Phenylbutazone; Probenecid; Sulfinpyrazone; Uric Acid

In a collective of 3899 out-patients, the effect of uric acid reduction of benzbromarone was tested. Ten days after beginning of treatment, a uric acid concentration of 5.1 to 5.7 mg/100 ml had been obtained. Three months after beginning of therapy, uric acid values were at 4.9 mg/100 ml, independently of age and sex. As side-effects were observed:diarrhoea in 1% (n = 41) of the treated patients, furthermore, 0,8% (n = 31) complained of gastro-intestinal trouble such as pressure over the stomach, nausea, sensation of fullness and epigastric pain. Only in 2 of the 3899 patients (0.05%) the appearance of a renal colic was observed.

Topics: Benzbromarone; Benzofurans; Diarrhea; Female; Gout; Humans; Kidney Calculi; Male; Nausea; Uric Acid

Topics: Adult; Aged; Allopurinol; Benzbromarone; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Sulfinpyrazone; Uric Acid

Topics: Benzofurans; Gout; Humans; Kidney Diseases; Probenecid

During treatment with benzbromaron in a dose of 100 mg/day a significant fall of uric acid was shown beginning on the second day. On the forth day in the evening or the fifth day in the morning a steady state for the uric acid level is reached. The morning value was 2,9 mg/100 ml, the evening value 2,6 mg/100 ml. During treatment, even when serum uric acid levels are decreased, an augmented renal uric acid elimination excists but a hyperuraturia was not found.

Topics: Benzbromarone; Benzofurans; Gout; Humans; Uric Acid

Benzbromarone, a potent uricosuric agent, is a benzofuran derivative with a bromine on the 3rd and 5th positions of the benzene ring. Readily absorbed after oral administration, it is promptly dehalogenated in the liver and excreted via the biliary system. Peak drug concentration usually precedes maximal uricosuria following a single dose of 40 mg of benzbromarone, since benzarone, one of the two metabolites, likewise has a uricosuric action. Longterm studies in 24 gouty patients indicate that the drug is well tolerated. It has not produced any skin rash or renal colic. Renal hemodynamics, blood picture, and liver enzymes were unchanged. Since it is eliminated by the biliary tract, it may cause diarrhoea in some patients. Being a very potent uricosuric agent, it is not advocated in patients with a history of uric acid lithiasis. The uricosuric effect is not liable to be counteracted when used in conjunction with hyperuricemic diuretics. The drug is particularly useful in patients with chronic gouty arthritis and tophi, either refractory or allergic to probenecid, sulfinpyrazone, or allopurinol.

Topics: Adult; Aged; Arthritis; Benzbromarone; Benzofurans; Chemical Phenomena; Chemistry; Chronic Disease; Gout; Humans; Hydrochlorothiazide; Kinetics; Middle Aged; Probenecid; Sulfinpyrazone; Uric Acid

Three patients with gout and seven with hyperuricaemia, previously untreated, took a single dose of 100 mg allopurinol and 20 mg benzbromaron (as a combined preparation) each morning. There occurred a highly significant decrease in serum uric acid concentration from 430.7 mumol/l (72.4 mg/l) to 268.6 mumol/l (45.2 mg/l), without any significant increase in urinary excretion of uric acid.

Topics: Allopurinol; Benzbromarone; Benzofurans; Drug Combinations; Gout; Humans; Time Factors; Uric Acid

Topics: Adult; Aged; Benzbromarone; Benzofurans; Diarrhea; Female; Gout; Humans; Leukopenia; Long-Term Care; Male; Middle Aged; Uric Acid

Topics: Benzofurans; Carbonates; Coronary Disease; Diabetes Complications; Gout; Humans; Hypertension; Kidney Failure, Chronic; Potassium; Uric Acid

Topics: Allopurinol; Antimetabolites; Azathioprine; Benzofurans; Chemical Phenomena; Chemistry; Erythrocytes; Folic Acid Antagonists; Glutamine; Gout; Humans; Metabolic Clearance Rate; Methotrexate; Purines; Time Factors; Transferases; Xanthine Oxidase

The hypouricemic effect of benzbromarone has been investigated in six subjects. Benzbromarone increased urate: creatinine by 371 per cent over control values at two to four hours after administration. Over a 24 hour period, the mean serum uric acid decreased from a control value of 7.8 +/- 0.8 to 4.3 +/- 0.6 mg/dl. This uricosuric effect was completely reversed by pyrazinamide, partially inhibited by acetylsalicyclic acid and sulfinpyrazone, and was not accompanied by an elevation of the creatinine clearance or an inhibition of urate binding to plasma protein. In vitro studies showed only 22 per cent inhibition of urate binding by benzbromarone five muM, a concentration which is transiently reached in man. Kinetic studies of human liver xanthine oxidase demonstrated non-competitive inhibition with variable hypoxanthine and a Ki slope of 8.5 muM. The Ki slopes for benzarone and allopurinol were 19.0 muM and 0.05 muM respectively. There was no elevation of the urinary oxypurines following benzbromarone ingestion. These observations suggest that only the renal tubular activity of benzbromarone is relevant to its hypouricemic effects in man. (J Rheumatol 2: 437-445, 1975).

Topics: Adult; Aspirin; Benzbromarone; Benzofurans; Blood Proteins; Creatinine; Female; Gout; Humans; Male; Middle Aged; Protein Binding; Pyrazinamide; Sulfinpyrazone; Uric Acid; Uricosuric Agents

Topics: Adult; Aged; Benzofurans; Cholesterol; Fatty Acids, Nonesterified; Gout; Humans; Lipids; Male; Middle Aged; Phospholipids; Triglycerides; Uric Acid; Uricosuric Agents

Topics: Adult; Allopurinol; Benzoates; Benzofurans; Bromine; Gout; Gout Suppressants; Humans; Male; Metabolic Diseases; Uric Acid

Topics: Benzoates; Benzofurans; Benzyl Compounds; Bromine; Cartilage; Chondroitin; Creatinine; Gout; Humans; Kinetics; Knee; Pentosyltransferases; Purines; Sulfates; Sulfurtransferases; Time Factors; Uric Acid

Topics: Adult; Allopurinol; Anemia; Arthritis; Benzofurans; Gout; Humans; Hyperlipidemias; Hypothyroidism; Hypoxanthines; Kidney Calculi; Male; Metabolism, Inborn Errors; Pedigree; Pentosyltransferases; Uric Acid; Uricosuric Agents

Topics: Adult; Benzofurans; Gout; Humans; Hyperthyroidism; Male; Middle Aged; Uricosuric Agents

Topics: Benzofurans; Bromine; Gout; Humans; Uric Acid; Uricosuric Agents

Topics: Austria; Benzofurans; Chemical Phenomena; Chemistry; Gout; Humans; Ketones; Kidney Failure, Chronic; Pharmaceutical Preparations; Registries; Uric Acid

Topics: Anuria; Benzofurans; Gout; Humans; Male; Middle Aged; Ureteral Calculi; Uric Acid; Uricosuric Agents; Vasodilator Agents

Topics: Adenine; Benzofurans; Gout; Guanine; Humans; Hypoxanthines; Iodobenzoates; Male; Pentosyltransferases; Purines; Uricosuric Agents

Topics: Administration, Oral; Adult; Benzofurans; Gout; Humans; Joint Diseases; Male; Psoriasis; Uric Acid

Topics: Allopurinol; Arthritis, Rheumatoid; Benzofurans; Diagnosis, Differential; Gout; Humans; Ketones; Psoriasis; Rheumatic Fever; Uric Acid

Topics: Benzofurans; Fatty Acids; Gout; Humans; Uric Acid

Topics: Adult; Aged; Benzofurans; Colchicine; Creatinine; Female; Gout; Humans; Kidney Function Tests; Male; Middle Aged; Uric Acid; Uricosuric Agents

Topics: Adult; Aged; Benzofurans; Bromine; Female; Gout; Humans; Iodine; Male; Middle Aged; Uric Acid; Uricosuric Agents

Topics: Adult; Allopurinol; Benzofurans; Colchicine; Gout; Humans; Ketones; Male; Middle Aged; Sulfinpyrazone

Topics: Aged; Allopurinol; Benzofurans; Diet Therapy; Gout; Humans; Uric Acid

Topics: Adult; Aged; Benzofurans; Female; Gout; Humans; Male; Middle Aged

Topics: Benzofurans; Gout; Humans; Purines; Uric Acid

Topics: Benzofurans; Gout; Humans; Middle Aged; Uric Acid

Topics: Benzofurans; Gout; Humans; Male; Uric Acid; Uricosuric Agents

Topics: Adult; Aged; Benzofurans; Creatinine; Female; Glomerular Filtration Rate; Gout; Humans; Kidney Function Tests; Male; Middle Aged; Uric Acid; Uricosuric Agents

Topics: Benzofurans; Gout; Humans; Uricosuric Agents

Topics: Adult; Benzofurans; Blood Glucose; Blood Sedimentation; Colchicine; Creatinine; Diabetes Mellitus; Electrocardiography; Fatty Liver; Female; Gout; Humans; Hyperlipidemias; Hypertension; Lipids; Liver Function Tests; Male; Middle Aged; Uric Acid

Topics: Adult; Aged; Arthritis; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Uric Acid

Topics: Adult; Aged; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Uric Acid

Topics: Adenine Nucleotides; Benzofurans; Fatty Acids; Gout; Guanine; Humans; Hypoxanthines; Pentosephosphates; Purines; Transferases; Uric Acid

Topics: Adult; Aged; Arthritis, Rheumatoid; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Uric Acid; Uricosuric Agents

Topics: Acute Disease; Adult; Aged; Anti-Inflammatory Agents; Benzofurans; Chronic Disease; Gout; Humans; Male; Middle Aged; Tablets; Time Factors; Uric Acid

Topics: Benzofurans; Female; Gout; Humans; Male; Middle Aged; Phenylbutazone; Purine-Pyrimidine Metabolism, Inborn Errors; Uric Acid

Topics: Adult; Allopurinol; Benzofurans; Depression, Chemical; Female; Gout; Humans; Male; Middle Aged; Uric Acid; Uricosuric Agents

Topics: Adult; Arthritis, Rheumatoid; Benzofurans; Female; Gout; Humans; Male; Rheumatic Diseases; Sulfinpyrazone; Uric Acid; Vasodilator Agents

Topics: Adult; Aged; Benzofurans; Colchicine; Female; Gout; Humans; Male; Metabolism, Inborn Errors; Middle Aged; Uric Acid

Topics: Allopurinol; Benzofurans; Colchicine; Diet Therapy; Gout; Humans; Orotic Acid; Urate Oxidase; Uricosuric Agents

Topics: Adult; Aged; Benzofurans; Female; Gout; Humans; Joint Diseases; Male; Middle Aged; Uric Acid

Topics: Adult; Aged; Benzofurans; Gout; Humans; Middle Aged; Uric Acid; Uricosuric Agents

Topics: Adult; Aged; Benzofurans; Female; Gout; Humans; Male; Middle Aged

Topics: Adolescent; Adult; Aged; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Uricosuric Agents

Topics: Benzofurans; Gout; Humans; Uric Acid

Topics: Adult; Aged; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Uric Acid; Vasodilator Agents

Topics: Benzofurans; Gout; Humans; Kidney Calculi; Uricosuric Agents; Vasodilator Agents

Topics: Allopurinol; Benzofurans; Colchicine; Diuretics; Gout; Humans; Mineral Waters; Oxalates; Tromethamine; Uric Acid; Uricosuric Agents; Vasodilator Agents

Topics: Benzofurans; Gout; Humans; Uric Acid; Xanthines

Topics: Adult; Aged; Allopurinol; Benzofurans; Female; Gout; Humans; Male; Middle Aged; Uric Acid

Topics: Adrenal Cortex Hormones; Adrenocorticotropic Hormone; Anticoagulants; Benzofurans; Colchicine; Gout; Griseofulvin; Humans; Indomethacin; Oxyphenbutazone; Phenylbutazone; Probenecid; Salicylates; Sulfinpyrazone

Topics: Benzofurans; Female; Gout; Humans; Middle Aged; Uricosuric Agents