【分类名称】
一级分类：内分泌系统药物 二级分类：痛风及高尿酸血症用药物 
 
【药品英文名】 Sulfinpyrazone
 
【药品别名】 苯磺唑酮、苯磺保泰松、硫氧唑酮、磺吡拉宗、磺胺吡啶二酮、亚磺基吡唑酮、亚硫吡拉宗、Anturane
 
【药物剂型】 片剂：100mg， 0.2g。
 
【药理作用】 本品为保泰松的衍生物。在体内具有抑制血小板聚集和释放的作用，能可逆性地抑制血小板前列腺合成酶。本品可竞争性抑制尿酸盐在近曲小管的主动重吸收，增加尿酸的排泄，降低血中尿酸的浓度，减缓或预防痛风结节形成和关节的痛风病变。本品还可抑制血小板聚集，增加血小板存活时间。还具有微弱的抗炎和镇痛作用。
 
【药动学】本品口服吸收良好，健康人每次口服200mg，服后1h达峰值，t1/23.3h，AUC每分钟3.0mg/ml，每分钟CL70ml，Vd18L。大部分以原形从肾脏排泄。
 
【适应证】主要用于缺血性心脏病和脑血管疾病的防治，如冠状动脉粥样硬化性心脏病、心肌梗死、暂时性脑缺血发作和脑梗死等；也用于防止瓣膜性心脏病动脉栓塞并发症及手术后静脉血栓形成的预防。用于慢性痛风的治疗。也可用于高尿酸血症。
【禁忌证】有严重肝肾功能不全者禁用。
 
【注意事项】
1.血液病、溃疡病和肾结石者慎用。
2.服药初期宜加用苏打片，服药期间应忌酒和多饮水。
3.定期随访血象、血尿酸和肾功能。个别患者用药期间可引起肾功能衰竭。
4.孕妇、肾功能不全者慎用。
 
【不良反应】
主要为胃肠反应，如恶心、呕吐、腹泻等，发生率10%～15%。偶见溃疡发生，也有报道发生血小板和粒细胞减少。
 
【用法用量】口服，每天2次，每次100～200mg，逐渐增加剂量至每次200～400mg，持续1周。维持量每天2次，每次100～400mg。进餐时或与牛奶同时服用。
 
【药物相应作用】
1.与阿司匹林等水杨酸类药物：
(1)阿司匹林等可抑制尿酸排泄，故合用可降低磺吡酮的排尿酸作用。用于治疗痛风时，两药不宜合用；
(2)两药合用抗血小板聚集作用可增强。磺吡酮可通过抑制环氧化酶，激发阿司匹林诱发哮喘患者的支气管痉挛。
2.与吲哚美辛合用可增强吲哚美辛作用。
3.与噻嗪类利尿药氢氯噻嗪、苄氟噻嗪等噻嗪类利尿药能提高尿酸的血浆浓度，因而对抗磺吡酮的抗痛风效果。
4.与糖皮质激素合用使磺吡酮的作用增强。
5.与丙磺舒合用增加对治疗慢性痛风的疗效。
6.与青霉素类及头孢菌素类抗生素合用可增加青霉素G、邻氯西林、萘夫西林等青霉素类抗生素以及头孢氨苄、头孢拉定等头孢菌素类抗生素的作用。
7.可增强香豆素类抗凝药的作用，合用时需减少后者的剂量。
8.可降低青霉素、甲苯磺丁脲的清除率，后者的血药浓度被增高并延长其作用持续时间。
 
【专家点评】本品是保泰松衍生物。具有类似阿司匹林的作用，抑制血小板的环氧化酶，能延长血小板存活期，减慢血小板更新、抑制血小板黏附和聚集，因此具有较强的抗栓性能。主要用于急性心肌梗死的二级预防，可降低猝死的危险，降低再梗死率。也用于脑血管患者。临床用于慢性痛风，能减慢或强防痛风结节的形成和关节的痛风病变。现本品也用于缺血性心脏病，临床研究表明，它能显著减少新近发生心肌梗死患者在第一年内病死率，减少心绞痛及心肌梗死的发病率。也用于脑血管疾病，防止血栓形成。
【原产地英文商品名】SULFINPYRAZONE 100mg/pill 100pills/box
【原产地英文药品名】SULFINPYRAZONE
【中文参考商品译名】
注：以下产品是不同的价格和不同的规格，购买时请以电话咨询为准！
·苯磺唑酮 200毫克/丸 100丸/盒
·苯磺唑酮 100毫克/丸 100丸/盒

·ANTURANE 200毫克/丸 100丸/盒 （厂家：诺华NOVARTIS）
【中文参考药品译名】苯磺唑酮
【生产厂家中文参考译名】诺华
【生产厂家英文名】NOVARTIS

Anturane®

sulfinpyrazone USP

Tablets Capsules

Prescribing Information

DESCRIPTION

Anturane, sulfinpyrazone USP, is a uricosuric agent available as 100-mg tablets and 200-mg capsules for oral administration. Its chemical name is 1,2-diphenyl-4-[2-(phenylsulfinyl) ethyl]-3,5-pyrazolidinedione, and its structural formula is

Sulfinpyrazone USP is a white to off-white powder practically insoluble in water and in solvent hexane, soluble in alcohol and in acetone, and sparingly soluble in dilute alkali. Its molecular weight is 404.48.

Inactive Ingredients. Anturane tablets: Colloidal silicon dioxide, gelatin, lactose, magnesium stearate, cornstarch, stearic acid, and talc.

Anturane capsules: D&C Red No. 33, D&C Yellow No. 10, FD&C Blue No. 1, gelatin, lactose, magnesium stearate, methylparaben, propylparaben, silicon dioxide, sodium lauryl sulfate, cornstarch, stearic acid, talc, and titanium dioxide.

CLINICAL PHARMACOLOGY

Its pharmacologic activity is the potentiation of the urinary excretion of uric acid. It is useful for reducing the blood urate levels in patients with chronic tophaceous gout and acute intermittent gout, and for promoting the resorption of tophi.

INDICATIONS

Anturane is indicated for the treatment of:

Chronic gouty arthritis

1. Intermittent gouty arthritis

CONTRAINDICATIONS

Patients with an active peptic ulcer or symptoms of gastrointestinal inflammation or ulceration should not receive the drug.

The drug is contraindicated in patients with a history or the presence of:

Hypersensitivity to phenylbutazone or other pyrazoles

Blood dyscrasias

WARNINGS

Studies on the teratogenicity of pyrazole compounds in animals have yielded inconclusive results. Up to the present time, however, there have been no reported cases of human congenital malformation proved to be due to the use of the drug.

It is suggested that Anturane be used with caution in pregnant women, weighing the potential risks against the possible benefits.

PRECAUTIONS

As with all pyrazole compounds, patients receiving Anturane should be kept under close medical supervision and periodic blood counts are recommended. It may be administered with care to patients with a history of healed peptic ulcer.

Recent reports have indicated that Anturane potentiates the action of certain sulfonamides, such as sulfadiazine and sulfisoxazole. In addition, other pyrazole compounds (phenylbutazone) have been observed to potentiate the hypoglycemic sulfonylurea agents, as well as insulin. In view of these observations, it is suggested that Anturane be used with caution in conjunction with sulfa drugs, the sulfonylurea hypoglycemic agents and insulin.

Because Anturane is a potent uricosuric agent, it may precipitate urolithiasis and renal colic, especially in the initial stages of therapy. For this reason, an adequate fluid intake and alkalinization of the urine are recommended. In cases with significant renal impairment, periodic assessment of renal function is indicated. Occasional cases of renal failure have been reported; but a cause-and-effect relationship has not always been clearly established.

Salicylates antagonize the uricosuric action of Anturane and for this reason their concomitant use is contraindicated in gouty arthritis.

Anturane may accentuate the action of coumarin-type anticoagulants and further depress prothrombin activity when these medications are employed simultaneously.

PEDIATRIC USE

Safety and effectiveness in pediatric patients have not been established.

NOTE

Anturane has minimal anti-inflammatory effect and is not intended for the relief of an acute attack of gout.

In the initial stages of therapy, because of the marked ability of Anturane to mobilize urates, acute attacks of gouty arthritis may be precipitated.

ADVERSE REACTIONS

The most frequently reported adverse reactions with Anturane have been upper gastrointestinal disturbances. In these patients it is advisable to administer the drug with food, milk, or antacids. Despite this precaution, Anturane may aggravate or reactivate peptic ulcer.

Rash has been reported. In most instances, this reaction did not necessitate discontinuance of therapy. In general, Anturane has not been observed to affect electrolyte balance.

Blood dyscrasias (anemia, leukopenia, agranulocytosis, thrombocytopenia, and aplastic anemia) have rarely been reported. There has also been a published report associating Anturane, administered concomitantly with other drugs including colchicine, with leukemia following long-term treatment of patients with gout. However, the circumstances involved in the two cases reported are such that a cause-and-effect relationship to Anturane has not been clearly established.

OVERDOSAGE

Symptoms

Nausea, vomiting, diarrhea, epigastric pain, ataxia, labored respiration, convulsions, coma. Possible symptoms, seen after overdosage with other pyrazolone derivatives: anemia, jaundice, ulceration.

Treatment

No specific antidote. Induce emesis; gastric lavage, supportive treatment (intravenous glucose infusions, analeptics).

DOSAGE AND ADMINISTRATION

Initial

200-400 mg daily in two divided doses, with meals or milk, gradually increasing when necessary to full maintenance dosage in one week.

Maintenance

400 mg daily, given in two divided doses, as above. This dosage may be increased to 800 mg daily, if necessary, and may sometimes be reduced to as low as 200 mg daily after the blood urate level has been controlled. Treatment should be continued without interruptian even in the presence of acute exacerbations, which can be concomitantly treated with phenylbutazone or colchicine. Patients previously controlled with other uricosuric therapy may be transferred to Anturane at full maintenance dosage.

HOW SUPPLIED

Tablets 100 mg – round, white, scored (imprinted CIBA 41)

Bottles of 100 ....................................... NDC 0083-0041-30

Capsules 200 mg – green (imprinted Anturane 200 CIBA 168)

Bottles of 100 ....................................... NDC 0083-0168-30

Do not store above 86°F (30°C).

Dispense in tight container (USP).

C96-18 (Rev. 4/96