部份中文托匹司他处方资料（仅供参考）
英文名：Topiroxostat
商品名：Uriadec Tablets
中文名：托匹司他片
生产商：三和化学研究所
药品简介 托匹司他（ウリアデック）是由日本三和化学研究所(Sanwa Kagaku Kenkyusho)和日本富士药品(Fuji Yakuhin)联合研发，2013年6月28日获日本PMDA批准上市，商品名为Uriadec®（ウリアデック）或Topiloric®（トピロリック®錠）；托匹司他是一种黄嘌呤氧化酶抑制剂，通过抑制黄嘌呤氧化酶，进而降低尿素在体内的产生；该药适用于痛风和高尿素血症的治疗。 ウリアデック錠20mg/ウリアデック錠40mg/ウリアデック錠60mg
药效分类名称
非嘌呤选择性黄嘌呤氧化酶抑制剂
-高尿酸血症治疗剂-
批准日期：2013年9月
商品名
URIADEC Tablets
一般的名称
トピロキソスタット（Topiroxostat）
化学名
4-[5-(Pyridin-4-yl)-1H-1,2,4-triazol-3-yl]pyridine-2-carbonitrile
分子式
C13H8N6
分子量
248.24
性状
它是白色至浅黄色的结晶性粉末。微溶于N，N-二甲基甲酰胺，微溶于0.1mol/L盐酸TS，微溶于甲醇和乙醇（99.5），几乎不溶于水。
化学構造式
融点
約329℃（分解）
药效药理
作用机理
拓扑洛司他竞争性地抑制黄嘌呤氧化还原酶（Ki值：5.1nmol/L）并抑制尿酸的产生。它对其他嘌呤/嘧啶代谢酶没有抑制作用，并选择性抑制黄嘌呤氧化还原酶。
降低血尿酸的作用
在小鼠，大鼠和黑猩猩（高尿酸血症模型）中，托朴司他通过单次口服给药显示出降低血尿酸的作用。
尿酸排泄降低作用
在黑猩猩（高尿酸血症模型）中，托朴司他通过单次口服减少尿酸的尿排泄。
适应症
痛风、高尿酸血症
用法与用量
托吡司他的成人剂量通常为20mg，每天早晚两次口服。之后，根据需要逐渐增加剂量，同时检查血尿酸水平。维持剂量通常为每天两次60mg，并且可以根据患者的病情进行调整，但最大剂量应为每天两次80mg。
包装
片
20mg：100片（PTP 10片x 10），500片（PTP 10片x 50）
40mg：100片（PTP 10片x 10），500片（PTP 10片x 50，散装）
60mg：100片（10 PTP片x 10）
制造商和分销商
三和化学研究所
Sanwa Kagaku Kenkensho Co.Ltd. 注：以上中文处方资料不够完整，使用者以原处方资料为准。
完整说明资料附件： https://www.info.pmda.go.jp/go/pack/3949004F1028_1_06/
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Topistat (ウリアデック) product advantages
Gout is a kind of crystal arthritis caused by purine metabolism disorder and/or uric acid excretion disorder. The clinical characteristics are hyperuricemia and the resulting recurrent gouty arthritis, tophi deposits, and chronic joints caused by tophi Inflammation and joint deformities often involve the kidneys and can cause chronic interstitial nephritis and uric acid kidney stones. In recent years, the incidence of gout has been on the rise and has gradually become younger.Hyperuricemia has also become a common disease.
There are not many types of anti-gout drugs at present, and clinical treatment is mainly based on colchicine, non-steroidal anti-inflammatory drugs, hormones, drugs that promote uric acid excretion, and drugs that inhibit uric acid synthesis (allopurinol). These drugs are all flawed in treatment. Poor curative effect and large side effects have become the bottleneck of its clinical application.
From the pharmacology, toxicology and clinical efficacy of Topiroxostat(Topiroxostat), this product has the advantages of strong uric acid reduction effect, few adverse reactions, and good safety:
1. This product is a non-purine xanthine oxidase inhibitor. It has inhibitory effect on both oxidized and reduced xanthine oxidase and inhibits the production of uric acid. Traditional drugs only have an inhibitory effect on the reduced form, so this product has a stronger effect on reducing uric acid.
2. Selective inhibitor with better safety: This product is a non-purine xanthine oxidase selective inhibitor. Compared with the traditional drug allopurinol (purine analog), it will not affect the metabolism of purine and pyridine and its enzymes The activity does not require repeated high-dose administration to maintain a higher drug level, with relatively fewer adverse reactions and better safety.
Topistat (ウリアデック) was jointly developed by Sanwa Kagaku Kenkyusho and Fuji Yakuhin. It was approved for marketing by Japan PMDA on June 28, 2013. The product name is Uriadec® (ウリアデック). ) Or Topiloric® (トピロリック® tablets); Topipristat is a xanthine oxidase inhibitor, which reduces the production of urea in the body by inhibiting xanthine oxidase; this drug is suitable for gout and hyperureaemia treatment.
