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An Overview of Drug-Induced Nephropathies *
Published in Robin S. Goldstein, Mechanisms of Injury in Renal Disease and Toxicity, 2020
Jean Paul Fillastre, Michel Godin
Sulfinpyrazone is a uricosuric analgesic used in treating gout and an antiplatelet agent prescribed after myocardial infarction. Many reversible cases of renal failure are due to this drug and in some patients a typical acute interstitial nephritis with eosinophilic infiltration of the interstitium was noted. Renal function improved in all patients with discontinuation of the drug.
Effects of Antithrombotic and Results of Drug Screening
Published in Josef Hladovec, Antithrombotic Drugs in Thrombosis Models, 2020
Renaud et al.150 used a relatively complicated method with endotoxin DIC in hyperlipemic rats. Oral administration of sulfinpyrazone was effective at extremely high doses (100 mg/kg). Endotoxin shock and generalized Shwartzman reaction were also inhibited in rabbits in the study of Evans and Mustard.151 Many attempts to use DIC models for testing sulfinpyrazone appeared later, particularly those with arachidonic acid injection causing a pulmonary distress with subsequent death of animals of various species. This model was supposed to be specific for TXA2 production,152 but considerable objections have been raised.153 The model may reflect bronchoconstricting and vasoconstricting activity as well as a mediation by products of the lipoxygenase pathway. It was used for testing sulfinpyrazone e.g., by Rüegg,37 Kohler et al., 154 Philp et al., 82 and Vigdahl.155 The drug orally administered was effective at doses between 10 and 30 mg/kg.
Acquired Bleeding Disorders Associated with Disease and Medications
Published in Harold R. Schumacher, William A. Rock, Sanford A. Stass, Handbook of Hematologic Pathology, 2019
William A. Rock, Sue D. Walker
Sulfinpyrazone is a pyrazolidine derivative, and is a potent uricosuric agent which also has antithrombotic and platelet inhibitory effects. It lacks anti-inflammatory and analgesic properties. Sulfinpyrazone competitively inhibits prostaglandin synthesis and thereby prevents platelet aggregation (134).
Novel urate transporter 1 (URAT1) inhibitors: a review of recent patent literature (2016–2019)
Published in Expert Opinion on Therapeutic Patents, 2019
Yue Dong, Tong Zhao, Wei Ai, Waleed A. Zalloum, Dongwei Kang, Ting Wu, Xinyong Liu, Peng Zhan
URAT1 (encoded by SLC22A12) is a member of the organic anion transporter (OAT) family. This protein contains 553 amino acids and 12 transmembrane domains, and it is specifically localized to the apical membrane of epithelial cells of proximal tubules. It is commonly accepted that URAT1 plays a key role in urate reabsorption in kidney. Accordingly, inhibition of URAT1 blocks reabsorption of urate anion, which enhances renal urate excretion [11,12]. However, the currently approved URAT1 inhibitors in clinical use are limited and can cause severe adverse effects. Of the four main uricosuric drugs (Figure 1), probenecid (1) can induce gastrointestinal tract irritation and hemolytic anemia [13], sulfinpyrazone (2) may cause nausea, vomiting, loss of appetite, joint pain, redness, or swelling [14], benzbromarone (3) has serious hepatotoxicity and bone marrow suppression [15], lesinurad (4) has cardiovascular toxicity and can induce liver and kidney injuries. Moreover, the recommended dosage of oral lesinurad is high and it is only approved as combination therapy with an XOD inhibitor for the treatment of hyperuricemia associated with gout in patients who have not achieved serum urate target levels with an XOD inhibitor alone [16]. Therefore, there is an urgent need for new drugs to control urate serum levels and the discovery of novel inhibitors targeting URAT1 has become a research hotspot in recent years.
Safety and tolerability of available urate-lowering drugs: a critical review
Published in Expert Opinion on Drug Safety, 2019
Larysa Strilchuk, Federica Fogacci, Arrigo Fg Cicero
The most often side effects of allopurinol include mild skin rash; to avoid more serious adverse reactions it is recommended to start at the lowest effective dose and then titrate it. Febuxostat seems to be a safe alternative to allopurinol, however, there is a need of further studies to evaluate its effect on cardiovascular events and death. Topiroxostat has been poorly studied yet so that we cannot draw any clear conclusion. Probenecid has a very wide spectrum of pharmacological interactions so that it is supposed to be carefully prescribed especially to polimorbidity patients undergoing complex drug therapies. Despite its withdrawal from some pharmaceutical markets, benzbromarone can be administered together with regular liver function monitoring and slow dose titration. Combination therapy with lesinurad or verinurad and XOI is well tolerated too, whereas monotherapy or its usage at high doses is not recommended. Arhalofenate is well tolerated, as it emerges from the existing studies. Tranilast has been well studied in patients with asthma and allergic diseases, even if evidence in gout is limited. Renal adverse effects of sulfinpyrazone have been described quite long ago so that before recommending it we need to have new studies estimating its efficacy and safety. Rasburicase is usually well tolerated, but all African, South-East Asian, Middle Eastern, and Mediterranean patients have to be screened for G6PD deficiency. When administering rasburicase the physician must also consider pre-medication with antihistamines and corticosteroids. Pegloticase can be used for treatment of severe refractory gout, but there is a need to measure SU level twice before infusion, in order to avoid infusion-related reactions.
Management of hyperuricemia and gout in obese patients undergoing bariatric surgery
Published in Postgraduate Medicine, 2018
Claudio Tana, Luca Busetto, Angelo Di Vincenzo, Fabrizio Ricci, Andrea Ticinesi, Fulvio Lauretani, Antonio Nouvenne, Maria Adele Giamberardino, Francesco Cipollone, Roberto Vettor, Tiziana Meschi
Uricosuric agents such as probenecid and sulfinpyrazone can be used in alternative. These drugs are contraindicated in the presence of urolithiasis or severe renal impairment. Benzbromarone is a potent uricosuric drug whose use is limited by the risk of hepatotoxicity. In case of coexistence of hyperuricemia and urolithiasis, allopurinol is the treatment of choice, with a proven reduction of the risk of recurrent renal colics [133,134]. Febuxostat seems also a valid alternative for urolithiasis prevention [135].