硫唑嘌呤

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依木兰

薄膜衣片Imuran

制造商 葛兰素史克

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性状

片剂 为圆形,双凸,黄色薄膜衣片。注射粉剂 粉末为黄至琥珀色,无菌冰冻干燥剂,含钠量约为4.5 mg。  

目录

药理作用

本药是6-硫基嘌呤的咪唑衍生物,为具有免疫抑制作用的抗代谢剂。可产生烷基化作用阻断SH组群,抑制核酸生物合成,防止细胞增生,并可引起DNA的损害。动物实验证实,本药可使胸腺、脾内DNA、RNA减少,影响DNA、RNA,以及蛋白质的合成,主要抑制T-淋巴细胞而影响免疫,所以可抑制迟发过敏反应器官移植的排斥反应。本药的疗效需于治疗数周或数月后才出现。在上消化道内吸收较佳。血浆中的硫唑嘌呤及6-硫基嘌呤水平与本药的疗效及毒性无相互关系。  

毒理研究

本药可致染色体异常,动物实验表明可致不同程度的胎儿异常,并具有明显的致畸性,不能排除本药对人体的致癌性。  

适应症

本药与其它药物联合应用于器官移植病人的抗排斥反应,例如肾移植心脏移植肝移植,亦减少肾移植受者对皮质激素的需求。本药也可单独使用于严重的风湿性关节炎系统性红斑狼疮皮肌炎/多发性肌炎,自体免疫性慢性活动性肝炎,寻常天疱疮结节性多动脉炎,自体免疫性溶血性贫血,慢性顽固自发性血小板减少性紫癜。  

用法用量

注射剂只有在无法口服时才由静脉给药,且当口服疗法可以耐受时即应停用。器官移植 第1日给予5 mg/kg体重,口服或静注。维持剂量要根据临床需要和血液系统的耐受性而调整,通常为1-4 mg/kg体重/日。维持治疗应无限期地进行。因为如果治疗中断,就有排斥的危险。其它疾病 开始剂量为1-3 mg/kg体重/日。应根据临床反应和血液学指标所示耐受程度而定。治疗效果明显时,应减少维持量至可保持此治疗效果的最低水平。如3个月内病人情况无改善,应考虑停用。所需维持量从1 mg/kg体重/日至3 mg/kg体重/日不等,取决于临床治疗需要和病人个体反应,包括血液学指标所示的耐受程度。兼有肝和/或肾功能不全者,剂量酌减。老年人用药的副作用发生率较其他病人高,应采用推荐剂量范围的低限值。  

不良反应

过敏反应:如全身不适头晕恶心呕吐腹泻发热寒战肌痛关节痛肝功能异常低血压。应立即停药和给予支持疗法,可使大部分病例恢复。造血功能 :可能产生剂量相关性、可逆性骨髓抑制,常见白细胞减少症,偶见贫血血小板减少性紫癜感染 :使用本药和肾上腺皮质激素的器官移植受者对病毒真菌细菌感染易感性增加。胃肠道反应 :偶有恶心,餐后服药可缓解。罕见胰腺炎。肺部反应 :罕见可逆性肺炎。  

禁忌症

对本药及6-疏基嘌呤过敏者禁用。  

注意事项

在治疗的首8周内,至少每周检查1次全血象,包括血小板。如使用大剂量或病人有肝和/或肾功能不全时,血象检查的次数应该更多。此后每月或最少每3个月重复进行全血象的检查。对肾和/或肝功能不全者,应使用推荐剂量的低限值及小心地监察血液学及肝肾功能。若出现肝或血液学毒性时,更应再减剂量。用药期间不要进行活疫苗免疫接种

孕妇及哺乳期妇女用药

临床上证明本药对胎儿有不良影响,只有对孕妇的益处大于对胎儿产生的危险时,才可考虑使用。本药可分泌入乳汁,故哺乳妇女慎用。  

药物相互作用

别嘌呤醇氧嘌呤醇和/或硫嘌呤醇与6-硫基嘌呤或硫唑嘌呤联用时,6-硫基唑嘌呤和硫唑嘌呤的剂量应减至原剂量的?。本药可增强去极化药物,如瑚珀酰胆碱神经肌肉阻滞作用,减弱非去极化药物如筒箭毒碱的神经肌肉阻滞作用。阻碍华法林抗凝作用。本药可增强骨髓抑制剂作用,导致严重的血液学异常,还可加强西咪替叮及吲哚美辛的骨髓抑制作用。  

药物过量

症状 无法解释的感染、喉部溃疡紫癜出血,通常是用药9-14天达到最大的骨髓抑制而引起。一次性用药过量后,可出现恶心、呕吐及腹泻,接着是轻微的白血球减少和肝功能异常。治疗 目前尚无特效解毒药,进行胃灌洗后,可予对症支持治疗及密切监察血象。  

用药须知

每瓶注射剂应加入5-15 mL注射用水重组,(重组液pH值为10-12)并在使用前现配,未用完的药物要废弃。重组溶液贮存于15-25°C之间时可保存5天。5 mL重组溶液加入20-200 mL下列任一输注溶液稀释(稀释液pH值为8-9.5) :0.18%/0.45%/0.9%的氯化钠注射液+4%葡萄糖,该稀释液在室温下(15-25°C)可保存24小时。如重组或稀释液中可见混浊或结晶物沉淀,该溶液即应废弃。静脉注射时应注意不要将本药注射至血管周围,因为可可导致组织损伤。本药片剂不应被切开。配制注射剂应在无菌室或专设的房间中进行,操作人员应戴防护用具(手套,面罩,护目镜,一次性工作服),如皮肤接触到药液,应用肥皂和大量清水清洗,如果溅到眼中,应用氯化钠溶液或大量清水清洗。

通用名称:硫唑嘌呤

英文名称:Azathioprine

中文别名:硝基咪唑硫嘌呤、义美仁、咪唑硫嘌呤

英文别名:Imurek、Imurel  

英文说明

【药理作用】

Classification: Immunosuppressant

Action/Kinetics: Antimetabolite that is quickly split to form mercaptopurine. To be effective, the drug must be given during the induction period of the antibody response. The precise mechanism in depressing the immune response is unknown, but it suppresses cell-mediated hypersensitivities and alters antibody production. Inhibits synthesis of DNA, RNA, and proteins and may interfere with meiosis and cellular metabolism. The mechanism for its effect on autoimmune diseases is not known. Is readily absorbed from the GI tract. The anuric client manifests increased effectiveness and toxicity (up to twofold). Onset: 6-8 weeks for rheumatoid arthritis. t1/2: 3 hr.

【适应症】

As an adjunct to prevent rejection in renal homotransplantation. In adult clients meeting criteria for classic or definite rheumatoid arthritis as defined by the American Rheumatism Association. Restrict use to clients with severe, active, and erosive disease that is not responsive to conventional therapy. Investigational: Chronic ulcerative colitis, generalized myasthenia gravis, to control the progression of Behet's syndrome (especially eye disease), Crohn's disease (low doses).

【用法用量】

Tablets, IV Use in renal homotransplantation. Adults and children, initial: 3-5 mg/kg (120 mg/m2), 1-3 days before or on the day of transplantation; maintenance: 1-3 mg/kg (45 mg/m2) daily. Rheumatoid arthritis, SLE. Adults and children, tablets, initial: 1 mg/kg (50-100 mg); then, increase dose by 0.5 mg/kg/day after 6-8 weeks and thereafter q 4 weeks, up to maximum of 2.5 mg/kg/day; maintenance: lowest effective dose. Dosage should be reduced in clients with renal dysfunction. Myasthenia gravis. 2-3 mg/kg/day. However, side effects occur in more than 35% of clients. To control progression of Behet's syndrome. 2.5 mg/kg/day. To treat Crohn's disease. 75-100 mg/day.

【注意事项】

Pregnancy Category: D

Contraindications: Treatment of rheumatoid arthritis in pregnancy or in clients previously treated with alkylating agents. Pregnancy and lactation.

Special Concerns: Hematologic toxicity is dose-related and may occur late in the course of therapy; may be more severe in renal transplant clients undergoing rejection. Although used in children, safety and efficacy have not been established.

【不良反应】

Hematologic: Leukopenia, thrombocytopenia, macrocytic anemia, severe bone marrow depression selective erythrocyte aplasia. GI: N&V, diarrhea, abdominal pain, steatorrhea. CNS: Fever, malaise. Other: Increased risk of carcinoma severe infections (fungal, viral, bacterial, and protozoal), and hepatotoxicity are major side effects. Also, skin rashes, alopecia, myalgias, increase in liver enzymes, hypotension, negative nitrogen balance.

【相互作用】

ACE inhibitors / ↑ Risk of severe leukopenia Allopurinol / ↑ Pharmacologic effect of azathioprine R/T ↓ liver breakdown Anticoagulants / ↓ Anticoagulant effect Corticosteroids / With azathioprine, may cause muscle wasting after prolonged therapy Cyclosporine / ↑ Plasma cyclosporine levels Echinacea / Do not give with azathioprine Methotrexate / ↑ Plasma levels of the active metabolite, 6-mercaptopurine Tubocurarine / ↓ Tubocurarine effect and other nondepolarizing neuromuscular blocking agents

【药物过量】

Symptoms: Large doses may result in bone marrow hypoplasia bleeding, infection, and death. Treatment: Approximately 45% can be removed from the body following 8 hr of hemodialysis.

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