Uricosuric that acts by increasing uric acid clearance. It is used in the treatment of gout.
Gout suppressants that act directly on the renal tubule to increase the excretion of uric acid, thus reducing its concentrations in plasma.
A xanthine oxidase inhibitor.
Agents that increase uric acid excretion by the kidney (URICOSURIC AGENTS), decrease uric acid production (antihyperuricemics), or alleviate the pain and inflammation of acute attacks of gout.
An oxidation product, via XANTHINE OXIDASE, of oxypurines such as XANTHINE and HYPOXANTHINE. It is the final oxidation product of purine catabolism in humans and primates, whereas in most other mammals URATE OXIDASE further oxidizes it to ALLANTOIN.
A uricosuric drug that is used to reduce the serum urate levels in gout therapy. It lacks anti-inflammatory, analgesic, and diuretic properties.
Hereditary metabolic disorder characterized by recurrent acute arthritis, hyperuricemia and deposition of sodium urate in and around the joints, sometimes with formation of uric acid calculi.
An anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.
Excessive URIC ACID or urate in blood as defined by its solubility in plasma at 37 degrees C; greater than 0.42mmol per liter (7.0mg/dL) in men or 0.36mmol per liter (6.0mg/dL) in women. This condition is caused by overproduction of uric acid or impaired renal clearance. Hyperuricemia can be acquired, drug-induced or genetically determined (LESCH-NYHAN SYNDROME). It is associated with HYPERTENSION and GOUT.
A XANTHINE OXIDASE inhibitor that decreases URIC ACID production. It also acts as an antimetabolite on some simpler organisms.
The prototypical uricosuric agent. It inhibits the renal excretion of organic anions and reduces tubular reabsorption of urate. Probenecid has also been used to treat patients with renal impairment, and, because it reduces the renal tubular excretion of other drugs, has been used as an adjunct to antibacterial therapy.
A pyrazine that is used therapeutically as an antitubercular agent.
A family of proteins involved in the transport of organic cations. They play an important role in the elimination of a variety of endogenous substances, xenobiotics, and their metabolites from the body.
Proteins involved in the transport of organic anions. They play an important role in the elimination of a variety of endogenous substances, xenobiotics and their metabolites from the body.

Vinblastine and sulfinpyrazone export by the multidrug resistance protein MRP2 is associated with glutathione export. (1/40)

The multidrug resistance proteins MRP1 and MRP2 are members of the same subfamily of ATP-binding cassette transporters. Besides organic molecules conjugated to negatively charged ligands, these proteins also transport cytotoxic drugs for which no negatively charged conjugates are known to exist. In polarized MDCKII cells, MRP1 routes to the lateral plasma membrane, and MRP2 to the apical plasma membrane. In these cells MRP1 transports daunorubicin, and MRP2 vinblastine; both transporters export reduced glutathione (GSH) into the medium. We demonstrate that glutathione transport in MDCKII-MRP1 cells is inhibited by the inhibitors of organic anion transporters sulfinpyrazone, indomethacin, probenecid and benzbromarone. In MDCKII-MRP2 cells, GSH export is stimulated by low concentrations of sulfinpyrazone or indomethacin, whereas export is inhibited down to control levels at high concentrations. We find that unmodified sulfinpyrazone is a substrate for MRP2, also at concentrations where GSH export is inhibited. We also show that GSH export in MDCKII-MRP2 cells increases in the presence of vinblastine, and that the stoichiometry between drug and GSH exported is between two and three. Our data indicate that transport of sulfinpyrazone and vinblastine is associated with GSH export. However, at high sulfinpyrazone concentrations this compound is transported without GSH. Models of MRP action are discussed that could explain these results.  (+info)

Effect of urate-lowering therapy on the velocity of size reduction of tophi in chronic gout. (2/40)

OBJECTIVE: The optimal serum urate levels necessary for elimination of tissue deposits of monosodium urate in patients with chronic gout is controversial. This observational, prospective study evaluates the relationship between serum urate levels during therapy and the velocity of reduction of tophi in patients with chronic tophaceous gout. METHOD: Sixty-three patients with crystal-confirmed tophaceous gout were treated with allopurinol, benzbromarone, or combined therapy to achieve serum uric acid levels less than the threshold for saturation of urate in tissues. The tophi targeted for evaluation during followup were the largest in diameter found during physical examination. RESULTS: Patients taking benzbromarone alone or combined allopurinol and benzbromarone therapy achieved faster velocity of reduction of tophi than patients taking allopurinol alone. The velocity of tophi reduction was linearly related to the mean serum urate level during therapy. The lower the serum urate levels, the faster the velocity of tophi reduction. CONCLUSION: Serum urate levels should be lowered enough to promote dissolution of urate deposits in patients with tophaceous gout. Allopurinol and benzbromarone are equally effective when optimal serum urate levels are achieved during therapy. Combined therapy may be useful in patients who do not show enough reduction in serum urate levels with single-drug therapy.  (+info)

Effects of aspirin and/or salicylate on hydrolysis and glucuronidation of indomethacin in rat erythrocytes and hepatocytes. (3/40)

This study was conducted to explore the mechanism of the pharmacokinetic interaction between aspirin (ASP) and indomethacin (IND) using rat erythrocytes (RBCs) and hepatocytes. ASP was hydrolyzed to salicylic acid (SA) in both the RBCs and hepatocytes. Within RBCs, aspirin and/or salicylate (ASP/SA) increased the concentration of IND, accompanied by a constant hydrolysis of IND. In hepatocytes, a low dose of IND was subjected to glucuronidation rather than hydrolysis, and ASP/SA inhibited both the acylglucuronidation of IND and hydrolysis of IND glucuronide. A high dose of IND underwent hydrolysis with about double the glucuronidation, and ASP/SA decreased the ratio of hydrolysis to glucuronidation, accompanied by a loss of ASP, IND and their metabolites from the medium. Collectively, the results provide metabolic insight into the mechanism of drug-drug interaction between ASP/SA and IND in the hepatocytes and RBCs.  (+info)

A new class of CYP2C9 inhibitors: probing 2C9 specificity with high-affinity benzbromarone derivatives. (4/40)

Noncovalent forces, other than hydrophobic interactions, are important determinants of substrate bias exhibited by some cytochromes P450. The CYP2C9 pharmacophore is proposed to include either an anionic group or hydrogen bond donor in addition to its hydrophobic groups. By constructing analogs of benzbromarone, evidence supporting the existence of a 2C9 anion-binding site was revealed. A nonsubstituted phenol analog was determined to have a pKa of 8.4 and a Ki of 414 nM whereas those with dihalogenated benzoyl phenols had pKa values between 4.2 to 5.2 and Ki values as low as 1 nM. The nonhalogenated, nonionizable analog is the poorest binder at 796 nM. The Ki range covers around three orders of magnitude with even the weakest binder being a more potent inhibitor than 2C9 substrate phenytoin. Thus, benzbromarone derivatives represent a class of molecules with the potential to reveal more structural details of the 2C9 active site.  (+info)

A case of exercise-induced acute renal failure in a patient with idiopathic renal hypouricemia developed during antihypertensive therapy with losartan and trichlormethiazide. (5/40)

Exercise-induced acute renal failure (ARF) developed in a 45-year-old man during antihypertensive therapy with losartan and trichlormethiazide. The antihypertensive therapy was stopped and marked hypouricemia became apparent during improvement of his renal function. The daily urinary excretion of uric acid was normal and an increased fractional excretion of uric acid was observed. Renal biopsy revealed that the kidney was recovering from acute tubular necrosis with interstitial fibrosis. Based on the results of pyrazinamide and benzbromarone tests, we classified this case as one of presecretory reabsorption defect of uric acid. Antihypertesive therapy with benidipine and candesartan was initiated, and the patient has not had any ARF episodes since. Because idiopathic renal hypouricemia can be associated with exercise-induced ARF and chronic renal dysfunction, careful antihypertensive therapy and follow-up evaluation of renal function might be necessary for hypertensive patients with idiopathic renal hypouricemia.  (+info)

Circadian rhythm of plasma uric acid and handling stress-induced hyperuricemia in conscious cebus monkeys. (6/40)

An apparent circadian rhythm of plasma uric acid and the effect of handling stress on plasma uric acid level in conscious cebus monkeys were demonstrated. The lowest level of plasma uric acid in the circadian rhythm occurred early in the morning and the highest, before bedtime at night. With experimental handling stress, the plasma uric acid level rose to much more than the maximum level of the circadian rhythm. Stress-induced hyperuricemia could be inhibited without an increase of urinary uric acid excretion by the minor tranquilizer diazepam at doses of more than 1 mg/kg, p.o. On the other hand, benzbromarone at 20 mg/kg, p.o. significantly inhibited the hyperuricemia with a hyperuricosuric effect, while probenecid at 50 mg/kg, p.o. had no effect on either the increased plasma uric acid or urinary uric acid excretion. Accordingly, it is concluded that the plasma uric acid level in conscious cebus monkeys easily fluctuates with experimental conditions and that the animals can be utilized to evaluate the hypouricemic and hyperuricosuric property of benzbromarone-like agents.  (+info)

CYP2C9 genotype-dependent effects on in vitro drug-drug interactions: switching of benzbromarone effect from inhibition to activation in the CYP2C9.3 variant. (7/40)

The CYP2C9.3 variant exhibits marked decreases in substrate turnover compared with the wild-type enzyme, but little is known regarding the effect this variant form may have on the occurrence of drug-drug interactions. To examine this possibility, the effect of the potent CYP2C9 inhibitor, benzbromarone, was studied with regard to CYP2C9.1- and CYP2C9.3-mediated flurbiprofen metabolism to evaluate whether the variant enzyme exhibits differential inhibition kinetics. Although benzbromarone inhibited CYP2C9.1 activity as expected, CYP2C9.3-mediated flurbiprofen 4'-hydroxylation was activated in the presence of benzbromarone. T1 relaxation studies revealed little change in distances of flurbiprofen protons from the heme iron of either CYP2C9.1 or CYP2C9.3 in the presence of benzbromarone compared with flurbiprofen alone. Spectral binding studies were also performed to investigate whether benzbromarone affected substrate binding, with the addition of benzbromarone having little effect on flurbiprofen-binding affinity in both CYP2C9.1 and CYP2C9.3. Docking studies with the 2C9.1 structure crystallized with a closed active site identified multiple but overlapping subsites with sufficient space for benzbromarone binding in the enzyme when flurbiprofen was positioned closest to the heme. If the closed conformation of 2C9.3 is structurally similar to 2C9.1, as expected for the conservative I359L mutation, then the dynamics of benzbromarone binding may account for the switching of drug interaction effects. In conclusion, the I359L amino acid substitution found in CYP2C9.3 not only reduces metabolism compared with CYP2C9.1 but can also dramatically alter inhibitor effects, suggesting that differential degrees of drug inhibition interactions may occur in individuals with this variant form of CYP2C9.  (+info)

Prediction of CYP2C9-mediated drug-drug interactions: a comparison using data from recombinant enzymes and human hepatocytes. (8/40)

The IC50 values of 14 drugs were determined in recombinantly expressed CYP2C9 (rCYP2C9) and human hepatocytes and the data used to simulate clinical area under the plasma concentration-time curve (AUC) changes upon coadministration with prototypic CYP2C9 substrates. There was an excellent correlation between IC(50, apparent) values determined using diclofenac and naproxen as CYP2C9 substrates (r2 = 0.82, p < 0.0001), with values being generally higher in the naproxen assay. After correcting for nonspecific binding, the IC(50, unbound) values were similar between the assays, for the majority of compounds. Two compounds, amiodarone and benzbromarone, demonstrated substrate-specific differences, activating naproxen O-demethylase to approximately 250% of control activity at 1 mM and 1 microM, respectively, while inhibiting diclofenac 4'-hydroxylation with IC(50, apparent) values of 3 microM and 0.04 microM, respectively. CYP2C9 IC(50, apparent) values generated in human hepatocytes were systematically higher than those determined with rCYP2C9. After correcting for nonspecific binding, there was an excellent correlation of IC(50, unbound) values generated in the different milieu (r2 = 0.88, p < 0.0001). The ratio of inhibitor concentration at the entrance to the liver to the inhibition constant ([I]in/Ki) was used to simulate clinical deltaAUC changes and compared with that observed in vivo. Where [I]in, total/Ki, apparent) was used, there were zero false negatives (observed deltaAUC >or=2, predicted deltaAUC <2), eight correct assignations, and seven false positives (observed deltaAUC 2. Where [I]in, unbound/Ki, unbound was used, there was one false negative, 14 correct assignations, and zero false positives. In summary, the data presented here suggest that for CYP2C9 interactions, the use of total liver inhibitor concentrations may indeed avoid false negatives, but more realistic predictions may be achieved using unbound liver inhibitor concentrations and unbound in vitro inhibition parameters.  (+info)

Benzbromarone is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially when allopurinol, a first-line treatment, fails or produces intolerable adverse effects. It is structurally related to the antiarrhythmic amiodarone. Benzbromarone is highly effective and well tolerated, and clinical trials as early as 1981 and as recently as April 2008 have suggested it is superior to both allopurinol, a xanthine oxidase inhibitor but not uricosuric, and probenecid, another uricosuric drug.
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Benzbromarone (BBR) is a uricosuric agent that has been used as a treatment for chronic gout. Although never approved in the United States, BBR was recently withdrawn from European markets due to several clinical cases linking the drug to an idiosyncratic hepatotoxicity that is sometimes fatal. We r …
This study shows that benzbromarone is very useful for the control of hyperuricaemia using doses ranging from 50 to 100 mg/day. It also shows that 47% of our patients taking allopurinol did not achieve optimal Pur concentrations with 300 mg/day despite alcohol abstinence and weight reduction. Previous studies showed that poor control of uricaemia is common,23-27 and it may result in radiological progression of bony lesions,23 increased size of tophi,23 and frequent recurrence of gouty bouts and tophi after withdrawal of urate lowering treatment.24 25 27 Although most standard sources of information recommend uricosurics to correct hyperuricaemia in underexcretors,5-8 29 30this approach is not a common practice in more recent studies.23-26 Epidemiological studies show that only 2-15% of patients with gout were taking uricosuric drugs.30-32 It may be because uricosurics such as probenecid or sulphinpyrazone have to be given in a twice daily regimen and have little efficacy in patients with low ...
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In the present study we identified a novel compound, UR-1102, as a potent URAT1 inhibitor that is selective over OAT1 and OAT3. In the monkey model, UR-1102 showed a better PK profile and reduced the levels of urate in plasma to a greater extent through its stronger uricosuric effect compared with benzbromarone, even when the plasma exposures were comparable, and achieved a maximum efficacy twice that of benzbromarone at a lower dose. Additionally, UR-1102 showed lower in vitro toxic potential in every mechanism that has been proposed for the hepatic toxicity of benzbromarone.. OAT1 and OAT3 are nonspecific anion transporters reported to be involved in urate excretion. Because they are both expressed in the basolateral membrane of renal proximal tubules and transport urate from the blood to inside the cells (Bakhiya et al., 2003; Ichida et al., 2003; Choi et al., 2005), inhibiting these transporters would decrease the secretion of urate into the urine. As mentioned earlier, the inability of ...
Ramark: For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20 ℃ for several month.PubMed ID:http://www.ncbi.nlm.nih.gov/pubmed/27500836?dopt=Abstract. ...
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Results. In total, 3206 references were recovered. Of these, 72 articles were selected based on our inclusion criteria. This included 1 report of 2 randomized controlled trials, 2 nonrandomized studies, and 69 case series and reports. The study with 2 randomized controlled trials looked at pegloticase. This showed improvement in tophi with treatment. One observational prospective trial looked at allopurinol and benzbromarone individually and in combination. It noted that achieving lower serum urate levels was associated with a faster reduction of tophi. An open-label extension trial noted that longterm maintenance of serum uric acid , 6.0 mg/dl with febuxostat led to a reduction in tophi. The case series and reports looked at surgical, pharmacological, and other interventions, as well as combination therapies. All surgical interventions reported improvement in pain and/or function. No report had objective measures of outcome. ...
A study published in PLOS One found that uric acid-lowering therapy improved renal outcomes and lowered the risk of cardiovascular (CV) events in adult pat
CCCadvanced FN1 motifs consumables are classical Eppendorf Cell Culture Consumables, additionally coated with a defined synthetic animal- and human-component-free substrate. The substrate (fibronectin-derived motifs with optimized steric configuration) is designed to mimic the cell attachment site of native ECM.. Learn more about cultivation of human iPSCs and MSCs on FN1 motifs and smart features of our cultureware below.. ...
The new RAFT enables the production of reproducible 3D cell cultures in a standard 96-well plate format designed for compound screening and cell biology research. It uses collagen to create a realistic cellular environment to study complex cell behavior and gives scientists complete control over their experimental parameters.
The iaxsys™ is a unique in vitro mechanobiology actuator that is compatible with established cell culture methods, consumables and incubators.. This versatile bioreactor platform facilitates near-physiologic strain of 2D membranes and scaffolds, thick 3D scaffolds (variotis™), ex vivo tissues, and soft tissue implants (eg bovine pericardium xenograft heart valve materials) within standard cell culture plates and flasks.. Quasi-static strain or cyclic strain can be applied uniformly to 6 samples simultaneously within a 6 well cell plate with a specified rate and number of cycles. Depending on the configuration, tensile or compression stresses are imparted.. When the iaxsys™ is used to actuate variotis™ scaffolds for mechanobiology studies in standard 6 well cell culture plates, the quality of RNA sampled is of a very high level. Unlike biologically derived gels and scaffolds, the fully synthetic variotis™ with b-glass™ avoids any contamination. The use of standard cell well plates ...
Below is a procedure for adherent cells (ie A431, A549, Hela, NIH3T3) I) Remove culture medium and rinse a subconfluent, 100 mm cell culture plate (80% confluent plate yields ~600-1000 microg protein total) with PBS at room temperature. The following steps should be performed on ice or at 4° C using fresh, ice cold buffers. II) Add 0.8 ml of ice cold fresh RIPA buffer to the 100 mm cell culture plates OR 0.5 ml per 5 x 10e6 cells/60 mm dish. III) Gently rock plates for 15 minutes at 4° C or let the plates set on ice. This step will allow the lysis buffer to act on the cells and will increase the total yield of soluble protein. IV) For monolayer cells, do a trypsin treatment to lift cells off the flasks prior to cell lysis, instead of scraping the cells for a more gentle approach. OR Scrape the adherent cells with a cell scraper and then transfer the scraped lysate into a sterile microcentrifuge tube. Place the tube on ice. Optional: wash the plate once with 0.2 ml of RIPA buffer and combine ...
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Cell or tissue culture experimentations should not be carried out in the regular laboratory space where other laboratory investigations are undertaken. This is critical to avoid contamination of cells in the cell culture plates and also to ensure that all the physiochemical environmental factors that encourage optimal growth of the cells are provided. Thus, cell culture experimentations should be carried out in a specialized laboratory or an area in the regular laboratory that is secluded from the usual laboratory area in order to achieve optimal result. Some key environmental conditions (i.e. the physiochemical or physico-chemical environmental growth factors) must be met in order to achieve optimum cell/tissue culture technique.. The microenvironment in which cell culture technique is basically carried out is unique and quite different from the traditional microbial cultures that also occur in vitro in the sense that tissue culture support the growth of living cells or cultures derived from ...
Do you use all wells of your 96 well plate including the outer ones? Usually, these wells are not used for a good reason: Increased evaporation in the outer wells reduces reproducibility and comparability between all wells (edge effect). Therefore, more than a third of a plate is not used. More experiments are necessary which mean higher costs. With Eppendorf Cell Culture Plates, the surrounding moat can be filled. This significantly reduces the edge effect and all wells become comparable. Learn more by reading our Application Notes 326 and 384. ...
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It really does sound like a bad batch of plates. Perhaps you could post the lot number and people with the same lot could compare notes? Peter French wrote: , , angelpet wrote: , ,Rusnak is EXACTLY right. Its an evaporation problem. I use a lot of , ,96-well plates and no longer use any of the outer wells . . . I fill them , ,with sterile water. So, I only get 60 wells, but I grow things long-term , ,so . . . .. , , , ,Dont be fooled by the name . . . Im not a bimbo, but I play one on the , ,net! , , , EXACTLY WRONG! , Sloppy thinking. Can we all get back to the original question (I reproduce , it here): , Thomas Kreuzer wrote: , , , , Hello fellow netters, , , , , I have been faced with a problem recently , for which I can find no solution , , altough it may be trivial. , , I seed HeLa - cells on standard 6-well cell culture plates (Costar) in 1 ml , , DMEM plus 5 % FCS , let them attach to the bottom overnight and then change , , the medium according to the tests I want to perform ...
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Here in the micro-space of cancellous bone, we can see microarchitectural deterioration due to osteoclasts breaking down trabeculae. This destruction leads to bone fragility and vulnerability to fracture.
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The algorithm based on the ACR guidelines for escalation of urate-lowering therapy recommends that, in patients not achieving target sUA after upward titration of an initial XO inhibitor, another should be substituted.5 ,6 This may also be combined with a uricuretic agent that provides a therapeutic increase in UA excretion from the kidney.14 Further reduction to sUA ,5 mg/dL is recommended for severe gout, polyarticular gout and tophaceous gout.5 ,6 Patients refractory to or intolerant of such options are candidates for pegloticase.5 Pegloticase is associated with infusion-related reactions, including anaphylaxis, and requires pretreatment with antihistamines and corticosteroids.16 ,17 Probenecid may be ineffective in patients with chronic renal disease, has associated drug-drug interactions, and requires twice-daily or four-times-daily dosing.18 Benzbromarone has limited availability worldwide and is associated with safety issues. Thus, a safe, effective, and potent URAT1 inhibitor would ...
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Hyperuricemia in Dalmatians (as in all breeds) is inherited, but unlike other breeds, the normal gene for a uric acid transporter that allows for uric acid to enter liver cells and be subsequently broken down is not present in the breeds gene pool. Therefore, there is no possibility of eliminating hyperuricemia among pure-bred Dalmatians. The only possible solution to this problem must then be crossing Dalmatians with other breeds to reintroduce the normal uric acid transporter gene. This led to the foundation of the Dalmatian-Pointer Backcross Project, which aims to reintroduce the normal uric acid transporter gene into the Dalmatian breed. The backcross used a single English Pointer; subsequent breedings have all been to purebred Dalmatians. This project was started in 1973 by Dr. Robert Schaible. The first cross (F1) hybrids did not resemble Dalmatians very closely. The F1s were then crossed back to purebreds. This breeding produced puppies of closer resemblance to the pure Dalmatian. By ...
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Cell migration is a highly integrated, multi-step process that plays an important role in the progression of various diseases including cancer, atherosclerosis and arthritis. There are various types and definitions of cell migration. Cell invasion is related to, and encompasses, cell migration, except that cells do more than migrate. Invasive cells move through the extracellular matrix into neighboring tissues in a process that involves ECM degradation and proteolysis. We offer cell migration assays in two formats: Boyden Chamber Assays consist of a cell culture insert nested in the well of cell culture plate. Cells are seeded into the insert and migrate through the pores of the membrane at the bottom of the insert. Gap Closure Assays create a defined area across which cells migrate. Cell migration can be monitored in real time by microscopy. These assays include our new proprietary Radius™ technology which uses a biocompatible hydrogel to create a circular area across which cells can
High field gradient targeting of magnetic nanoparticle PNAS. Jan 15, 2008 loaded with magnetic nanoparticles or the field gradient, but not both, making highgradient magnetic fields are produced by the magnetizable wires of a .. on a magnetic separator adapted for cell culture plates by using a magnetic the Alamar blue assay as described by the manufacturer (Biosource).. Get Price ...
The present invention is directed to pharmaceutical compositions, and method for preparing pharmaceutical compositions, comprising a cross-linked matrix physically entrapping at least one therapeutic agent. The matrix may comprise one or more phases in addition to an aqueous phase, such as a solid and/or oil phase. The matrix of the invention has at least one controlled release in-vivo kinetic profile, and may have additional profiles for the same agent. The matrix may also comprise more than one therapeutic agent, and each additional therapeutic agent may have one or more controlled release in-vivo kinetic profile.
Background: what are tophi and what interventions are used? Gout is caused by urate crystals forming either within or around joints. Inflammation can lead to pain, redness, warmth and swelling of the affected joints, making the area difficult to touch or move. Some of the reasons why people get gout include their genetic make-up, being overweight, ingesting certain medications (e.g. cyclosporine), impaired kidney function and lifestyle habits such as drinking excessive amounts of alcohol and sugar-sweetened drinks. Tophi are nodules that develop in people with poorly treated or uncontrolled chronic gout. Tophi can become infected, cause pain and lead to a decrease in function. Tophi can be treated with urate-lowering drugs (e.g. benzbromarone, probenecid, allopurinol, febuxostat, pegloticase), surgical removal or other interventions such as haemodialysis. Surgical interventions can be used where urgent removal is required, for example, for relief of nerve compression.. Study characteristics This ...
TY - JOUR. T1 - Loss of ATP-dependent transport activity in pseudoxanthoma elasticum-associated mutants of human ABCC6 (MRP6). AU - Iliás, Attila. AU - Urbán, Zsolt. AU - Seidl, Thomas L.. AU - Saux, Olivier Le. AU - Sinkó, Emese. AU - Boyd, Charles D.. AU - Sarkadi, B.. AU - Váradi, A.. PY - 2002/5/10. Y1 - 2002/5/10. N2 - Mutations in the ABCC6 (MRP6) gene cause pseudoxanthoma elasticum (PXE), a rare heritable disorder resulting in the calcification of elastic fibers. In the present study a cDNA encoding a full-length normal variant of ABCC6 was amplified from a human kidney cDNA library, and the protein was expressed in Sf9 insect cells. In isolated membranes ATP binding as well as ATP-dependent active transport by ABCC6 was demonstrated. We found that glutathione conjugates, including leukotriene C4 and N-ethylmaleimide S-glutathione (NEM-GS), were actively transported by human ABCC6. Organic anions (probenecid, benzbromarone, indomethacin), known to interfere with glutathione conjugate ...
Although regenerative medicine products are at the forefront of scientific research, technological innovation, and clinical translation, their reproducibility and large-scale production are compromised by automation, monitoring, and standardization issues. To overcome these limitations, new technologies at software (e.g., algorithms and artificial intelligence models, combined with imaging software and machine learning techniques) and hardware (e.g., automated liquid handling, automated cell expansion bioreactor systems, automated colony-forming unit counting and characterization units, and scalable cell culture plates) level are under intense investigation. Automation, monitoring and standardization should be considered at the early stages of the developmental cycle of cell products to deliver more robust and effective therapies and treatment plans to the bedside, reducing healthcare expenditure and improving services and patient care.
2465-59-0 - HXNFUBHNUDHIGC-UHFFFAOYSA-N - Oxypurinol [USAN] - Similar structures search, synonyms, formulas, resource links, and other chemical information.
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Ganoderma applanatum (G. applanatum) dispels wind to eliminate dampness and exhibited nephron- and liver-protective effects as noted in Chinese herbal classic literature; it might also affect hyperuricemia. Therefore, we examined the hypouricemia effects and mechanisms underlying G. applanatum on chemical-induced hyperuricemia in mice. Ethanol (GAE) and water (GAW) extracts were prepared by extracting G. applanatum in ethanol (GAE), followed by bathing the remains in water to yield GAW. GAE and GAW were administered orally at different doses to hyperuricemia mice, while allopurinol and benzbromarone served as positive controls. Both GAE and GAW showed remarkable hypouricemia activities, rendering a substantial decline in the SUA (serum uric acid) level in hyperuricemia control (P
ANTICONVULSANTS PSYCHOSEDATIVES BENTIROMIDE BENTOCID BENTONITE BENTYL BENTYLOL BENURESTAT BENURON BENURYL BENZ(A)ANTHRACENE BENZAFLAVIN BENZALAZINE BENZALDEHYDE BENZALIN BENZALKONIUM BROMIDE BENZALKONIUM CHLORIDE BENZAMIDE BENZAMIDE-RIBOSIDE BENZAMIDINE BENZAMIDOSALICYLATE CALCIUM BENZAMIL benzamine BENZANTHRIN-A BENZANTHRIN-B BENZANTHRONE BENZAPRINOXIDE BENZARONE BENZASAL BENZASTATIN-A BENZASTATIN-B BENZASTATIN-C BENZASTATIN-D BENZATHINE BENZATHINE-BENZYLPENICILLIN BENZATHINE-CEFAPIRIN BENZATHINE-CHLORTETRACYCLINE BENZATHINE-CLOXACILLIN TRANQUILIZERS Page 102 п98 SECTION B BENZATHINE- PHENOXYMETHYLPENICILLIN BENZATROPINE BENZBROMARONE BENZEDREX BENZEDRINE BENZELMIN BENZENE BENZENEARSONATE BENZENESULFOHYDROXAMATE benzenesulfonylphenytoin-1 BENZESTROL BENZETHIDINE BENZETHONIUM CHLORIDE BENZETIMIDE benzhexol BENZHYDRAZONE BENZIDINE BENZIL BENZILATE BENZILONIUM BROMIDE BENZILYLCHOLINE BENZIMIDAZOLE BENZIMIDAZOLYL-UREA-2 BENZINDOPYRINE BENZIODARONE BENZMALECENE BENZMETANIDE BENZNIDAZOLE BENZO(A)PYRENE
The angiotensin II (AII) antagonist, losartan, increases uric acid excretion when administered to humans. However, the active metabolite of losartan, EXP 3174, and other nonpeptide AII antagonists such as eprosartan and SB 203220 are devoid of uricosuric activity. To investigate the mechanism of losartan-induced uricosuria, we examined the effects of losartan, EXP 3174, eprosartan and SB 203220 on OH- -dependent [14C]urate uptake into rat proximal tubule brush-border membrane vesicles. Losartan (10 microM) inhibited [14C]urate uptake at all time points examined, except at equilibrium (2 hr). Losartan had no effect on urate uptake in the absence of an OH- gradient. The inhibitory effect of losartan on urate uptake was concentration dependent (IC50 = 9.5 +/- 1.4 microM) and competitive in nature. The other AII antagonists also inhibited urate uptake but were 6-8-fold less potent than losartan with IC50 values of EXP 3174 (65 +/- 13 microM), eprosartan (60 +/- 7.0 microM) and SB 203220 (74 +/- 12.5 ...
Background & Rationale:. Convergent epidemiological and clinical observations have identified urate - a major antioxidant and the end product of purine metabolism in humans - as the first molecular predictor of both the risk and the progression of typical Parkinsons disease (PD). Among some 1600 early PD patients enrolled in prior clinical trials, those with baseline serum urate levels in the highest quintile (i.e., in the upper normal range) displayed a 40% slower rate of clinical (disability) progression compared to those with baseline urate at or below the median (with p,0.000001 for trend across quintiles). Similarly, amongst those who underwent serial SPECT brain scans for changes in dopamine transporter (DAT) binding, those with higher baseline serum urate levels displayed a slower rate of radiographic progression (loss of striatal DAT). Moreover, urate levels in baseline cerebrospinal fluid (CSF) samples also correlate inversely with rates of clinical progression. Although this link ...
The system consists of a mini-microscope, the CytoSMART™ Device (roughly the size of a cell culture plate), and an accompanying tablet which is linked to the device and can be fixed outside the incubator. With the CytoSMART™ Connect Cloud Service you can view your images and create time-lapse movies of your cell culture. As a cloud-based system, it enables you to access and download your cell culture data from any browser-capable system, whether it is your computer, laptop, smartphone or your personal tablet device. With the CytoSMART™ System your cells can remain in their defined conditions in the incubator, while you monitor the culture remotely online. Moreover, you can set automatic alerts - meaning you only need to physically tend to your cells once they have reached a certain confluency.. Applications for the CytoSMART™ System. With the CytoSMART™ System, both cell culture monitoring and the morphological read-out of a multitude of cell-based assays become routine tasks that can ...
Influenza, one of the most common infectious diseases, is a highly contagious airborne disease that occurs in seasonal epidemics and manifests as an acute febrile illness with variable degrees of systemic symptoms, ranging from mild fatigue to respiratory failure and death. Influenza causes significant loss of workdays, human suffering, and m...
Introduction Adherence to urate-lowering drugs (ULDs) has not been well evaluated among those with gout. Our aim was to assess the level and determinants of non-adherence with ULDs prescribed for gout.
RESULTS: Of 23,371,362 beneficiaries in 2010, there were 1,458,569 prevalent and 56,595 incident cases of gout, giving a prevalence of 6.24% (95% confidence interval (CI), 6.23% to 6.25%) and an incidence of 2.74 (95% CI, 2.72 to 2.76) per 1,000 person-years. The annual percentage change (APC) of the standardised prevalence was −0.7% (95% CI, −1.7% to 0.3%; P = 0.14), suggesting that the prevalence of gout was essentially the same throughout the study period. However, The APC of incidence was −13.4 (95% CI, −16.1 to −10.6) between 2005 and 2007 and −2.1 (95% CI, −10.4 to 7.1) between 2007 and 2010. Regions with the highest prevalence and incidence were eastern coastal counties and offshore islets, where indigenous people are clustered. Among prevalent gout cases in 2010, only 22.93% (95% CI, 22.87% to 23.00%) were prescribed urate-lowering treatment (ULT), which remained unchanged between 2005 and 2010 at an APC of 0.0 (95% CI, −3.8 to 4.0). Uricosuric agents were more commonly ...
Buy Sulfinpyrazone, CAS number: 57-96-5, online for pharmaceutical analytical testing. The highest quality reference standards for reliable results.
DESCRIPTION Probenecid and Colchicine contains probenecid, which is a uricosuric agent, and colchicine, which has antigout activity, the mechanism of which is unknown. Probenecid is the generic name for 4-[(dipropylamino)sulfonyl] benzoic ac...
Urate levels increased (urine) information including symptoms, causes, diseases, symptoms, treatments, and other medical and health issues.
Oliverio, A and Castellano, C, Genotype-dependent sensitivity and tolerance to morphine and heroin. Dissociation between opiate-induced running and analgesia in the mouse. (1974). Subject Strain Bibliography 1974. 795 ...
Trabucchi, M; Spano, P F.; Racagni, G; and Oliverio, A, Genotype-dependent sensitivity to morphine. Dopamine involvement in morphine-induced running in the mouse. (1976). Subject Strain Bibliography 1976. 3228 ...
Although the above phenomena are commonly seen in kinetic profiles, they are not always appreciated by the investigators, and several examples exist of standard Michaelis-Menten hyperbolic curves forced through the data rather than the adoption of more suitable models. In other cases the paucity of data points precludes any meaningful selection of an alternative model. What will the consequences be of ignoring the nonhyperbolic nature of a kinetic profile and fitting the Michaelis-Menten equation? The extent of error and the consequences when scaled for in vivo prediction can be considered for three situations:. 1. For substrate inhibition, the consequences are clear in Fig. 1B. Substantial underestimation of Vmax will occur by merely ignoring the high concentration data points and forcing a standard Michaelis-Menten model through the remaining lower substrate concentration data. Also, Km would be poorly estimated. Thus there is a need for full description of the profile to allow for the impact ...
The National Institute of Standards and Technology (NIST) uses its best efforts to deliver a high quality copy of the Database and to verify that the data contained therein have been selected on the basis of sound scientific judgment. However, NIST makes no warranties to that effect, and NIST shall not be liable for any damage that may result from errors or omissions in the Database ...
Probenecid is a uricosuric and branch blocking agent. It inhibits the re-absorption of uric acerbic in the kidneys, appropriately accretion the elimination of uric acerbic in urine and abbreviating urate levels in the blood. This stops new crystals forming, and helps old clear deposits to deliquesce . It is a lot of advantageous to under-excreters…
DI-fusion, le Dépôt institutionnel numérique de lULB, est loutil de référencementde la production scientifique de lULB.Linterface de recherche DI-fusion permet de consulter les publications des chercheurs de lULB et les thèses qui y ont été défendues.
Amiodarone Benzbromarone Benziodarone Budiodarone Dronedarone Gautier, P; Guillemare, E; Djandjighian, L; Marion, A; ...
In some persons with loss-of-function mutations of URAT1, the uricosurics benzbromarone and losartan had no effect, suggesting ... The primary uricosuric drugs include probenecid, benzbromarone and sulfinpyrazone. Drugs with other primary uses, that have ...
... benzbromarone, and colchicine. Long term medications are not recommended until a person has had two attacks of gout, unless ...
... benzbromarone". Drug Metabolism and Disposition. 33 (12): 1791-5. doi:10.1124/dmd.105.006056. PMID 16135657. S2CID 16377221. ...
Amiodarone Benzbromarone, the brominated analogue of benziodarone, used as an uricosuric Dronedarone Pizzichini M, Aleo MF, ...
... benzbromarone MeSH D03.438.127.125 - cantharidin MeSH D03.438.127.187 - citalopram MeSH D03.438.127.250 - fura-2 MeSH D03.438. ...
... benzbromarone, benziodarone, probenecid, lesinurad, sulfinpyrazone, ethebencid, zoxazolamine, and ticrynafen) increase the ...
... combinations M04AB01 Probenecid M04AB02 Sulfinpyrazone M04AB03 Benzbromarone M04AB04 Isobromindione M04AB05 Lesinurad M04AC01 ...
Amiodarone Benzbromarone Benziodarone Celivarone Dronedarone Roy D, Talajic M, Dorian P, Connolly S, Eisenberg MJ, Green M, Kus ...
Benzbromarone (INN) Benzedrex Benzestrol (INN) Benzethidine (INN) Benzethonium chloride (INN) Benzetimide (INN) Benzfetamine ( ...
... is highly effective and well tolerated, and clinical trials as early as 1981 and as recently as April 2008 have ... Benzbromarone is a very potent inhibitor of CYP2C9. Several analogues of the drug have been developed as CYP2C9 and CYP2C19 ... Benzbromarone was introduced in the 1970s and was viewed as having few associated serious adverse reactions. It was registered ... Benzbromarone is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially ...
The most frequent adverse reactions are nausea, vomiting, diarrhea, abdominal pain, and a feeling of general discomfort. It is also common to experience various sensations in the skin, from crawling or tingling sensations, tenderness of palms and the soles, and numbness of hands, arm, legs or feet.[10] Other skin reactions include skin rash, swelling and stinging sensation.[10] Suramin can also cause loss of appetite and irritability.[10] Suramin causes non-harmful changes in urine during use, specifically making the urine cloudy.[10] It may exacerbate kidney disease.[11] Less common side effects include extreme fatigue, ulcers in the mouth, and painful tender glands in the neck, armpits and groin.[10] Suramin uncommonly affects the eyes causing watery eyes, swelling around the eyes, photophobia, and changes or loss of vision.[10] Rare side effects include hypersensitivity reactions causing difficulty breathing. Other rare systemic effects include decreased blood pressure, fever, rapid heart ...
1/C10H15N5O10P2/c11-8-5-9(13-2-12-8)15(3-14-5)10-7(17)6(16)4(24-10)1-23-27(21,22)25-26(18,19)20/h2-4,6-7,10,16-17H,1H2,(H,21,22)(H2,11,12,13)(H2,18,19,20)/t4-,6-,7-,10-/m1/ ...
Benzbromarone is highly effective and well tolerated, and clinical trials as early as 1981 and as recently as April 2008 have ... Benzbromarone is a very potent inhibitor of CYP2C9. Several analogues of the drug have been developed as CYP2C9 and CYP2C19 ... Benzbromarone was introduced in the 1970s and was viewed as having few associated serious adverse reactions. It was registered ... Benzbromarone is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially ...
Acute intermittent porphyria (AIP) is one of the porphyrias, a group of diseases involving defects in heme metabolism and that results in excessive secretion of porphyrins and porphyrin precursors. AIP manifests itself by abdomen pain, neuropathies, and constipation, but, unlike most types of porphyria, patients with AIP do not have a rash.
Acute intermittent porphyria (AIP) is one of the porphyrias, a group of diseases involving defects in heme metabolism and that results in excessive secretion of porphyrins and porphyrin precursors. AIP manifests itself by abdomen pain, neuropathies, and constipation, but, unlike most types of porphyria, patients with AIP do not have a rash.
Benzbromarone Tops Febuxostat for Gout? In countries where available, low-dose benzbromarone may warrant stronger consideration ...
Efficacy of allopurinol and benzbromarone for the control of hyperuricaemia. A pathogenic approach to the treatment of primary ... febuxostat or benzbromarone and increased frequency of visits until the target SUA concentration was achieved.14 Other urate- ...
Frequency of CYP2C9 polymorphisms in Polynesian people and potential relevance to management of gout with benzbromarone. Joint ...
Similar effects were observed with benzbromarone (a uricosuric agent). Allopurinol also prevented weight gain in fructose-fed ...
medicines used to treat gout (such as probenecid, sulfinpyrazone or benzbromarone). *fluconazole or voriconazole (used to treat ...
In the profiling of an in vivo single dose, benzbromarone and aspirin were located in the same cluster of the three PPARα ... The clustering of in vitro data revealed that benzbromarone, three NSAIDs (aspirin, indomethacin and diclofenac sodium) and ... benzbromarone- and aspirin-treated rat livers as well as rat hepatocytes, and for glutathione deficiency-related genes were ... valproic acid belonged to the same cluster of PPARα agonists, supporting the reports that benzbromarone,valproic acid and some ...
... benzbromarone, thiazide diuretics, aspirin, pyrazinamide, nifedipine or other drugs that may have affected uric acid metabolism ... benzbromarone, and lesinurad), and recombinant uricase (pegloticase), which breaks down urate to water-soluble allantoin. ...
Benzbromarone withdrawn from the European market: Another case of absence of evidence is evidence of absence ?. T.L.Th.A. ...
Acute intermittent porphyria (AIP) is one of the porphyrias, a group of diseases involving defects in heme metabolism and that results in excessive secretion of porphyrins and porphyrin precursors. AIP manifests itself by abdomen pain, neuropathies, and constipation, but, unlike most types of porphyria, patients with AIP do not have a rash.
Acute intermittent porphyria (AIP) is one of the porphyrias, a group of diseases involving defects in heme metabolism and that results in excessive secretion of porphyrins and porphyrin precursors. AIP manifests itself by abdomen pain, neuropathies, and constipation, but, unlike most types of porphyria, patients with AIP do not have a rash.
Product containing benzbromarone (medicinal product). Code System Preferred Concept Name. Product containing benzbromarone ( ... Product containing benzbromarone (medicinal product) {703372005 , SNOMED-CT } Parent/Child (Relationship Type) Product ...
Acute intermittent porphyria (AIP) is one of the porphyrias, a group of diseases involving defects in heme metabolism and that results in excessive secretion of porphyrins and porphyrin precursors. AIP manifests itself by abdomen pain, neuropathies, and constipation, but, unlike most types of porphyria, patients with AIP do not have a rash.
中文品名 別他生錠 英文品名 Betashin Tablets 主要成份 Betamethasone 成份含量 Betamethasone 0.5mg+ Lactose 75mg+ Starch 51.5mg+ Magnesium Stearate 3mg ...
Frequency of CYP2C9 polymorphisms in Polynesian people and potential relevance to management of gout with benzbromarone. Joint ...
Required for efficient urate re-absorption in the kidney. Regulates blood urate levels. Mediates saturable urate uptake by facilitating the exchange of urate against organic anions. The protein encoded by this gene is a member of the organic anion transporter (OAT) family, and it acts as a urate transporter to regulate urate levels in blood. This protein is an integral membrane protein primarily found in epithelial cells of the proximal tubule of the kidney. An elevated level of serum urate, hyperuricemia, is associated with increased incidences of gout, and mutations in this gene cause renal hypouricemia type 1. Alternative splicing results in multiple transcript variants. [provided by RefSeq, Jan 2013]
Benzbromarone_Middle, Benzbromarone_High, Clofibrate_Middle, Clofibrate_High, WY14643_Low, WY14643_High, WY14643_Middle, ...
The most frequent adverse reactions are nausea, vomiting, diarrhea, abdominal pain, and a feeling of general discomfort. It is also common to experience various sensations in the skin, from crawling or tingling sensations, tenderness of palms and the soles, and numbness of hands, arm, legs or feet.[10] Other skin reactions include skin rash, swelling and stinging sensation.[10] Suramin can also cause loss of appetite and irritability.[10] Suramin causes non-harmful changes in urine during use, specifically making the urine cloudy.[10] It may exacerbate kidney disease.[11] Less common side effects include extreme fatigue, ulcers in the mouth, and painful tender glands in the neck, armpits and groin.[10] Suramin uncommonly affects the eyes causing watery eyes, swelling around the eyes, photophobia, and changes or loss of vision.[10] Rare side effects include hypersensitivity reactions causing difficulty breathing. Other rare systemic effects include decreased blood pressure, fever, rapid heart ...
... is definitely a C-ring methoxy analog of benzbromarone 1.11 Compound 16 was a much weaker inhibitor, ~47-fold (1.2 M versus 26 ...
痛風、高尿酸血症。 藥物的主要成分是什麼? BENZBROMARONE. 這
Allopurinol, benzbromarone and risk of coronary heart disease in gout patients: A population-based study. Lin, H. C., Daimon, M ...
Benzbromarone .. Acifugan .. Benzbromaron .. Benzbromaron AL .. Benzbromaron-Ratiopharm .. Besuric .. Desuric .. Narcaricin .. ... D03.633.100.127.110 Benzbromarone .. D04 Polycyclic Compounds .. D04.615 Polycyclic Aromatic Hydrocarbons .. D04.615.638 ...
Efficacy and tolerability of urate-lowering drugs in gout: a randomised controlled trial of benzbromarone versus probenecid ... Biochemical effectiveness of allopurinol and allopurinol-probenecid in previously benzbromarone-treated gout patients.. 2007 ...
Drugs (such as benzbromarone or probenecid). Pregnancy. Intractable diarrhea. 2. Underproduction-type hypouricemia. ...
Effect of benzbromarone on body fat in patients with gout / 中华内分泌代谢杂志 ... After 2 weeks of washout, all patients were treated with benzbromarone for consecutive 12 weeks. The data of blood biochemical ...
  • Benzbromarone is a uricosuric agent and non-competitive inhibitor of xanthine oxidase used in the treatment of gout, especially when allopurinol, a first-line treatment, fails or produces intolerable adverse effects. (wikipedia.org)
  • Benzbromarone is highly effective and well tolerated, and clinical trials as early as 1981 and as recently as April 2008 have suggested it is superior to both allopurinol, a non-uricosuric xanthine oxidase inhibitor, and probenecid, another uricosuric drug. (wikipedia.org)
  • Efficacy of allopurinol and benzbromarone for the control of hyperuricaemia. (wikipedia.org)
  • These urate lowering therapies (ULTs) include the xanthine oxidase inhibitors (allopurinol, febuxostat), medications that increase urate excretion (probenecid, benzbromarone, and lesinurad), and recombinant uricase (pegloticase), which breaks down urate to water-soluble allantoin. (hindawi.com)
  • Ten years' experience with benzbromarone in the management of gout and hyperuricaemia" (PDF). (wikipedia.org)
  • Frequency of CYP2C9 polymorphisms in Polynesian people and potential relevance to management of gout with benzbromarone. (cdc.gov)
  • Benzbromarone, a uricosuric medicine which is currently unapprovedin New Zealand, is to become available, fully subsidised, under Special Authority criteria from 1 voltaren w kapsulkach April, 2013. (kr.ua)
  • Benzbromarone is a very potent inhibitor of CYP2C9. (wikipedia.org)
  • therefore, (16) is definitely a C-ring methoxy analog of benzbromarone 1.11 Compound 16 was a much weaker inhibitor, ~47-fold (1.2 M versus 26 nM). (woofahs.com)
  • A benefit-risk assessment of benzbromarone in the treatment of gout. (wikipedia.org)
  • Benzbromarone Tops Febuxostat for Gout? (medscape.com)
  • In countries where available, low-dose benzbromarone may warrant stronger consideration in gout with renal uric acid underexcretion, researchers say. (medscape.com)
  • Further antihyperuricemic-guided purification of the fraction afforded three lignans, phyllanthin (1), hypophyllanthin (2) and phyltetralin (3), of which 1 significantly reversed the plasma uric acid level of hyperuricemic animals to its normal level in a dose-dependent manner, comparable to that of allopurinol, benzbromarone and probenecid which are used clinically for the treatment of hyperuricemia and gout. (nih.gov)
  • Benzbromarone, probenecid, pravastatin, and diclofenac were able to inhibit both apical and basolateral calcein efflux. (ncl.ac.uk)
  • Here, we performed a cross-sectional survey of the implementation status of liver function tests in patients who were newly prescribed benzbromarone, using the Japanese large claims database. (elsevier.com)
  • Male patients who were newly prescribed benzbromarone from January 2010 to December 2016 were included. (elsevier.com)
  • We targeted patients who continued benzbromarone during the observation period (up to 180d from the start of administration). (elsevier.com)
  • This graph shows the total number of publications written about "Benzbromarone" by people in Harvard Catalyst Profiles by year, and whether "Benzbromarone" was a major or minor topic of these publication. (harvard.edu)
  • A major adverse effect of benzbromarone is hepatotoxicity. (elsevier.com)
  • Results from a randomized controlled trial conducted in China found low-dose benzbromarone to be more effective in lowering serum urate levels than low-dose febuxostat (Uloric), with a similar safety profile, in gout with renal uric acid underexcretion. (medscape.com)
  • A total of 196 relatively young healthy men with gout and uric acid underexcretion were randomly assigned to receive low-dose benzbromarone (25 mg/d) or low-dose febuxostat (20 mg/d) for 12 weeks. (medscape.com)
  • For most patients, benzbromarone is effective for those who have failed to achieve serum uric acid goals with allopurinol treatment. (medscape.com)
  • There are many studies on the effect of uric acid lowering therapy on CV risk in gout patients, but few studies have compared allopurinol and benzbromarone. (acrabstracts.org)
  • During the study period, patients who used uric acid lowering agents other than allopurinol and benzbromarone or who used both drugs in combination were also excluded from the study. (acrabstracts.org)
  • Inhibitor of the renal urate transporter URAT1 with high selectivity to URAT1 over OAT1 and OAT3 in vitro (Ki values 0.057 µM, 7.2 µM, and 2.4 µM, respectively), capable of increasing the fractional excretion of urinary uric acid, and reducing plasma uric acid more effectively than Benzbromarone. (axonmedchem.com)
  • The drug for excreting uric acid is benzbromarone. (zgxkx.org)
  • We did not find severe hepatotoxicity with low-dose benzbromarone, but ethnic background may affect drug responses, and severe hepatotoxicity of benzbromarone has rarely been reported in Asia," the authors write. (medscape.com)
  • Benzbromarone is severely hepatotoxic in some individuals and unlikely to ever gain approval in the United States," one of the study's investigators, Robert Terkeltaub, MD, professor of medicine, University of California San Diego, told Medscape Medical News . (medscape.com)
  • Using known hepatotoxic compounds (usnic acid, benzbromarone, tamoxifen, and acetaminophen) and compounds that have no reported human cases of liver toxicity (dimethyl sulfoxide, theophylline, and aminohippurate) the platform's performance was evaluated. (pubfacts.com)
  • If there is only hyperuricemia, benzbromarone and febuxostat can be used. (zgxkx.org)
  • Therefore, this phenylalanine may be important in the high potency and specificity of benzbromarone and verinurad for hURAT1 (Tan et al . (iecnc.org)
  • However, if there are urinary stones, benzbromarone can not be used for treatment, so we should also communicate with your doctor to fully improve the examination. (zgxkx.org)
  • Benzbromarone is not approved in the United States because of concerns of acute liver injury but is approved in several other countries, including China, Brazil, and New Zealand. (medscape.com)