Krystexxa（pegloticase,聚乙二醇重组尿酸酶注射液)
制造商：
Savient药厂

药理分类：
聚乙二醇尿酸特定的酶。

活性成分：
Pegloticase 8mg/mL（如尿酸酶蛋白）的磷酸盐缓冲液，稀释后用于静脉输液。

指示：
慢性痛风治疗成人难治常规治疗。

药理作用：
Pegloticase是一种重组，修改尿酸氧化酶结合到哺乳动物的聚乙烯二醇的形式。 Pegloticase催化尿囊素尿酸氧化，从而降低血清尿酸。它表明在谁没有正常化血清尿酸，其标志，并与黄嘌呤氧化酶抑制剂不足或对他们来说，这些药物控制症状的病人禁忌使用的。
Pegloticase不应给予葡萄糖六磷酸脱氢酶（G6PD）缺乏症的病人，因为他们有较高的溶血和高铁血红蛋白血症的危险性增加。为了更好地管理痛风耀斑，患者应开始治疗前的类固醇消炎药或秋水仙碱治疗pegloticase至少一个星期，至少6个月的时候可行的​​继续。这是没有必要停止在一个事件pegloticase治疗痛风急性发作。

临床试验：
两个双盲，安慰剂控制的6个月进行审判，以评估疗效和安全性pegloticase治疗慢性，难治性痛风成人（每2周或每4周一次给予）。患者口服抗组织胺与预处理，静脉注射皮质类固醇，以及对乙酰氨基酚，他们还获得治疗前NSAIDs和/或秋水仙碱开始一周，除非有禁忌，防止痛风弹。在这两项研究的主要终点是谁取得患者血浆尿酸水平“至少80％的时间6mg/dL比例在3到6个月。基准的标准包括：血清尿酸≥8mg/dL和至少3个前18个月痛风耀斑或至少一个痛风痛风石或痛风性关节炎。一个更大的患者比例显着治疗pegloticase每两周取得尿酸降至<比那些服​​用安慰剂6mg/dL。好处：风险是与双周剂量更好。
Pegloticase上痛风石的作用是次要终点。双周方案显着优于安慰剂的痛风石完全缓解（100％≥1的目标痛风石分辨率，无新的或累进痛风石）率。

成人：
“18岁：与抗组胺药和皮质类固醇Premedicate。静脉输注给受了至少2小时。 8mg每2周一次。速度缓慢，或停止并重新启动率较低，如果发生输液反应，观察至少1小时后输液。

儿童：
<18年：不推荐。

禁忌：
G6PD缺乏症。

警告/注意事项：
不适用于治疗无症状高尿酸血症。在为G6PD缺乏（非洲或地中海裔）的风险屏幕患者。管理在医疗保健管理的准备输液反应和过敏反应的临床医生设置。密切监控过敏反应/输液反应，尤指。患者接受药物后，无间隔> 4周再治疗。瑞士法郎。在每次输液监测血清尿酸水平;考虑停止时的水平> 6mg/dL，尤其是连续2个级别> 6mg/dL（过敏反应和输液反应的风险增加）。妊娠（Cat.C）。哺乳母亲：不推荐。

不良反应：
痛风耀斑（prophylax与NSAIDs或秋水仙碱），输液反应，胃肠不适，挫伤，淤血，鼻咽炎，便秘，胸口疼痛，过敏反应，心衰加重，抗体的形成。

如何提供：
单用小瓶- 1

The gout is a form of arthritis defined by secondary painful episodes affecting the joints inflammations. The disease can be characterized by pain, edema, redness and warmth, as well as the functional impotence of the joints. Without the proper treatment, the gout is the type of disease that presents frequent acute episodes, resulting in severe wounds of the joints. It usually affects men, but this doesn’t mean that women are immune to it. One of the most efficient treatments for gout is Krystexxa (pegloticase). Its active substance is an enzyme called pegloticase. The pegloticase transforms the uric acid into a useless and harmless acid that has no role at all. It is finally eliminated through the patient’s urine.
Krystexxa (pegloticase) is a very powerful treatment. It is part of that special category of drugs that are given only when similar, yet less aggressive medications are ineffective. Just like most other drugs, it comes with side effects that are more severe compared with its alternatives. The patient must be carefully reevaluated after the previous treatments and can take this drug only with a medical prescription. It is a new name on the market, FDA approved since 2010 only. This aspect makes the medical prescription even more important, since many tests are not conclusive enough yet.

WARNING: ANAPHYLAXIS and INFUSION REACTIONS
See full prescribing information for complete boxed warning.
•Anaphylaxis and infusion reactions have been reported to occur during and after administration of KRYSTEXXA.
•KRYSTEXXA should be administered in healthcare settings and by healthcare providers prepared to manage anaphylaxis and infusion reactions.
•Patients should be pre-medicated with antihistamines and corticosteroids.
•Patients should be closely monitored for an appropriate period of time for anaphylaxis after administration of KRYSTEXXA.
•Monitor serum uric acid levels prior to infusions and consider discontinuing treatment if levels increase to above 6 mg/dL, particularly when 2 consecutive levels above 6 mg/dL are observed.

CONTRAINDICATIONS
•Glucose-6-phosphate dehydrogenase (G6PD) Deficiency: Before starting KRYSTEXXA, patients at higher risk for G6PD deficiency (e.g., those of African and Mediterranean ancestry) should be screened due to the risk of hemolysis and methemoglobinemia.、

WARNINGS AND PRECAUTIONS
•Anaphylaxis: Anaphylaxis occurred in patients treated with KRYSTEXXA. Anaphylaxis may occur with any infusion, including a first infusion, and generally manifests within 2 hours of the infusion. However, delayed-type hypersensitivity reactions have also been reported. KRYSTEXXA should be administered in healthcare settings and by healthcare providers prepared to manage anaphylaxis. Patients should be pre-medicated with antihistamines and corticosteroids. Patients should be closely monitored for an appropriate period of time for anaphylaxis after administration of KRYSTEXXA.
•Infusion Reactions: Infusion reactions occurred in patients treated with KRYSTEXXA. KRYSTEXXA should be administered in a healthcare setting and by healthcare providers prepared to manage infusion reactions. Patients should be pre-medicated with antihistamines and corticosteroids. Monitor patients closely for signs and symptoms of infusion reactions. In the event of an infusion reaction, the infusion should be slowed, or stopped and restarted at a slower rate. If a severe infusion reaction occurs, discontinue infusion and institute treatment as needed. The risk of an infusion reaction is higher in patients who have lost therapeutic response.
•Gout Flares: An increase in gout flares is frequently observed upon initiation of anti-hyperuricemic therapy, including treatment with KRYSTEXXA. If a gout flare occurs during treatment, KRYSTEXXA need not be discontinued. Gout flare prophylaxis (i.e., non-steroidal anti-inflammatory drugs [NSAIDs] or colchicine upon initiation of treatment) is recommended for at least the first 6 months of therapy unless medically contraindicated or not tolerated.
•Congestive Heart Failure: KRYSTEXXA has not been formally studied in patients with congestive heart failure, but some patients in clinical trials experienced exacerbation. Exercise caution when using KRYSTEXXA in patients who have congestive heart failure and monitor patients closely following infusion.

ADVERSE REACTIONS
The most common adverse reactions (occurring in at least 5% of KRYSTEXXA-treated patients) are gout flares, infusion reactions, nausea, contusion or ecchymosis, nasopharyngitis, constipation, chest pain, anaphylaxis and vomiting.

FDA批准治疗痛风的新药Krystexxa (pegloticase)

2010年9月14日，FDA批准治疗痛风的新药Krystexxa(pegloticase)，用于常规治疗无效或常规治疗无法耐受的成年痛风患者。
痛风为嘌呤代谢紊乱和(或)尿酸排泄障碍所致血尿酸增高的一组异质性疾病。过多的尿酸最终以针状结晶存留在关节或软组织中,引起间歇性肿胀、发红、发热、疼痛和关节僵硬。常规疗法是服用能够降低血液中尿酸含量的药物，例如黄嘌呤氧化酶抑制剂别嘌醇(别嘌呤醇)和Uloric(非布司他，febuxostat)。
Krystexxa是一种酶，能够通过将尿酸代谢成无害物质并通过尿液排出体外来降低痛风患者体内的尿酸水平。该药物的给药方式为静脉注射，每两周注射一次。
FDA药品审评与研究中心相关专家表示:“在3 000 000成年痛风患者中，大约有3%的人群无法从常规治疗中获益。本次批准的这一新药物能够为这患者提供一种重要的新选择。”
该药临床试验中曾出现不良反应包括过敏、痛风发作、恶心、注射部位青肿、鼻道刺激、便秘、胸痛、呕吐。
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原产地英文商品名:
KRYSTEXXA 8mg/ml/vial
原产地英文药品名:
PEGLOTICASE
中文参考商品译名:
KRYSTEXXA 8毫克/毫升/瓶
中文参考药品译名:
聚乙二醇重组尿酸酶
生产厂家中文参考译名:
SAVIENT PHARMS
生产厂家英文名:
SAVIENT PHARMS