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  药店国别: 德国药房
产地国家: 德国
所属类别: 心血管系统药物->降胆固醇
处方药:处方药
包装规格: 1克/片 198片/盒
计价单位:
   
生产厂家英文名:
Mitsubishi Pharma
该药品相关信息网址1:
http://beta.medicines.org.uk/emc/medicine/28348
原产地英文商品名:
BindRen 1g 198tabs
原产地英文药品名:
Colestilan
中文参考商品译名:
BindRen 1克/片 198片/盒
中文参考药品译名:
考来替兰
原产地国家批准上市年份:
0000/00/00
英文适应病症1:
Hypercholesterolemia
临床试验期:
完成
中文适应病症参考翻译1:
高胆固醇血症
药品信息:
药品英文名 Colestilan 药品别名 可来替兰 药理作用 本品可影响胆汁酸以及胆固醇的吸收。其作用机制为在消化道内吸附胆汁酸,抑制胆汁酸和胆固醇的再吸收,从而促进胆汁酸以及胆固醇的排泄,并增加肝内UDL受体促使血中LDL进入肝脏,从而也降低血中LDL。本品与同类药物消胆胺比较,显示与大多数胆汁酸类有较大的吸附量和亲和性,本品可有效降低门静脉血中的总胆汁酸量以及腹部淋巴管内的总胆固醇浓度,有效增加排泄物中的胆汁酸以及胆固醇。反复给予本品可使大白鼠肝微粒体中的胆固醇7α-羟基化酶活性上升,使肝中的胆固醇向胆汁酸转化加剧。因此,本品主要是通过吸附消化管内胆汁酸以及胆固醇从而抑制其吸收,同时可促进肝中LDL的摄取以及异化,从而导致血中胆固醇浓度的降低。小鼠、大白鼠以及狗口服本品,进行急性毒性实验。小鼠、大白鼠的LD50值超过1000mg/kg,狗的LD50值则超过5000mg/kg。大自鼠以及狗口服本品,进行亚急性和慢性毒性实验。发现对大白鼠的主要毒性为GOT、GPT上升,体重增加受到抑制;对狗的主要毒性为体重增加受到抑制,呕吐等。未进行依赖性和抗原性试验,致突变性试验以及致癌性试验结果为阴性。对大白鼠以及家兔口服给药进行致畸性试验,表明对于大白鼠在妊娠前以及初期,胎儿器官形成期,产期和哺乳期给药,出现毒性的最小剂量分别为600mg/(kg·d)、800mg/(kg·d)、800mg/(kg·d)以上。对于家兔在胎儿器官形成期给药时出现毒性的最小剂量600mg/(kg·d)以上。 药动学 口服给予大白鼠和狗200mg/kg用14C标记的本品,血液和血浆中均未能检测出放射能。同样,1次/d,连续21d反复给予大白鼠本品,在血液中亦未能检测出放射能。而且,在反复给药5d后消化道内容物以及组织中也未能检测出放射能,也未发现本品的体内残留。狗单剂量以及大白鼠21d反复给14C标记的本品后,粪便中未发现代谢物,尿液中也未发现放射能,全部药物在粪便中被排泄。表明:口服给予本品后,本品不能被吸收,消化道内亦未能代谢分解,全部经粪便排除。 适应证 高胆固醇血症;家族性高胆固醇血症。 禁忌证 注意事项 1.对本品有既往过敏史的病人慎用。2.由于本品主要是通过与肠管中的胆汁酸结合,促进胆汁酸在粪便中的排泄从而降低血清中的胆固醇,因此胆道完全闭塞的病人疗效不佳。3.有便秘、痔疮、消化道溃疡、有出血倾向、肝疾病、肝功能障碍病人使用本品有可能使症状加剧,因此应慎用。4.使用本品前应确认为高胆固醇血症病人方可使用,同时要明确LDL-胆固醇值,因为根据三酰甘油值的不同,LDL-胆固醇的值亦不同。5.长期使用本品有可能会影响脂溶性维生素A、D、E、K的吸收,因此应适当予以补充。6.使用本品期间应定期检测血中脂值,如无治疗作用应立即停止用药。此外用药期间,会引起三酰甘油的上升,因此应定期检测血中的三酰甘油值,如发现该值异常上升,应立即停止给药。7.高龄病人中出现不良反应的种类和频率与非高龄病人之间没有显著差别。但是高龄病人的生理功能低下,因此应注意其消化道的不良反应。 不良反应 在642例病人中,150例病人(23.4%)出现不同程度的不良反应。主要为便秘82例(12.8%)、腹胀42例(6.5%)、呕吐9例(1.4%)、腹痛7例(1.1%)等。偶见其他不良反应为:口干、消化不良、便血、痔疮出血、肝功能损害(GOT、GPT、γ-GTP、Al-P上升)、瘙痒、丘疹、心悸、(CPK上升、关节痛、头痛、胸痛、乏力、末梢性浮肿、红细胞以及白细胞减少等。 用法用量 通常成人给予2次/d,每次1.5g,早晚饭前口服。但是,也可根据症状以及服用状况,早、晚饭后口服(但原则上仍应早、晚饭前给药)。 4.1 Therapeutic indications BindRen is indicated for the treatment of hyperphosphataemia in adult patients with Chronic Kidney Disease (CKD) Stage 5 receiving haemodialysis or peritoneal dialysis. 4.2 Posology and method of administration Posology The recommended starting dose is 6-9 g per day (2-3 g three times daily). Patients previously on other phosphate binders who are switched to BindRen should start taking 6-9 g per day (2-3 g three times daily). Dose titration Serum phosphorus concentrations should be monitored. If an acceptable serum phosphorus concentration is not achieved, the dose may be increased by 3 g per day (1 g three times daily) in 2-3 weekly intervals. The maximum daily dose of BindRen tested in clinical trials was 15 g per day (5 g three times daily). Special populations Elderly population Experience from clinical studies in patients above the age of 75 years is very limited. Renal impairment BindRen is indicated for use in patients with Chronic Kidney Disease (CKD) Stage 5 receiving haemodialysis or peritoneal dialysis. No data on the use of BindRen in pre-dialysis patients are available. Severe hepatic impairment Patients with severe hepatic impairment were excluded from clinical studies. Therefore, the use of BindRen is not recommended in patients with severe hepatic impairment (see also section 4.4). No data are available. Paediatric population The safety and efficacy of BindRen in children and adolescents aged under 18 years has not yet been established. No data are available. Method of administration BindRen is for oral use. Granules should be taken whole as one dose from the sachet. The daily dose of BindRen granules should be taken in three equally divided doses with or immediately after meals with a sufficient amount of water to aid swallowing. The division of the daily dose may be adjusted on a physician's advice taking into account the dietary intake of phosphate. Patients should be encouraged to adhere to their prescribed low phosphate diets. Treatment of high blood phosphorus levels usually requires long-term treatment. 4.3 Contraindications • Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. • Bowel obstruction. 4.4 Special warnings and precautions for use The safety and efficacy of BindRen has not been studied in patients with: • Dysphagia or swallowing disorders • Severe gastrointestinal disorders such as chronic or severe constipation, intestinal stenosis, intestinal diverticulum, sigmoid colitis, gastrointestinal ulcers, or recent major gastrointestinal surgery • Biliary obstruction • Severe hepatic impairment (see also section 4.2) • Seizure disorders • Recent history of peritonitis in peritoneal dialysis patients • Serum albumin <30 g/L Therefore, the use of BindRen is not recommended in patients with these disorders. Hyperparathyroidism BindRen alone is not indicated for the control of hyperparathyroidism. Intestinal obstruction and ileus/subileus In very rare cases, intestinal obstruction and ileus/subileus have been observed in patients during treatment with BindRen. Constipation may be a preceding symptom. Patients who are constipated should be monitored carefully while being treated with BindRen. In patients who develop severe constipation or other severe gastrointestinal symptoms, alternative treatment may need to be considered. Gastrointestinal haemorrhage Caution should be exercised when treating patients with conditions which predispose to gastrointestinal haemorrhage, such as recent history of gastrointestinal haemorrhage, gastrointestinal ulcers, gastritis, diverticulosis, colitis and haemorrhoids. Hypocalcaemia/hypercalcaemia Patients with renal insufficiency may develop hypocalcaemia or hypercalcaemia. BindRen does not contain calcium, and has no effect on serum calcium concentrations on treatment for up to one year. Serum calcium concentrations should be monitored as a normal follow-up of a dialysis patient. Elemental calcium should be given as a supplement in case of hypocalcaemia. Fat-soluble vitamins BindRen did not induce any clinically relevant reduction in the absorption of vitamins A, D, E or K during clinical studies of up to one year. However, caution should be exercised when treating patients with a susceptibility to vitamin K or fat-soluble vitamin deficiencies, such as patients with malabsorption syndromes and patients treated with coumarin anticoagulants (e.g. warfarin). In these patients, monitoring of vitamin A, D and E concentrations or assessing vitamin K status through the measurement of coagulation parameters is recommended and the vitamins should be supplemented if necessary. Folate deficiency BindRen did not induce a clinically relevant reduction in folate absorption during clinical studies of up to one year. However, intestinal folate absorption may be impaired during long-term treatment of BindRen. In these patients, monitoring serum folate status and supplementation with folic acid should be considered. Hypothyroidism Close monitoring of patients with hypothyroidism is recommended when levothyroxine is co-administered with BindRen (see section 4.5). Systemic ion balance BindRen binds phosphate and bile acid, with the release of chloride which is available for systemic absorption. Changes in systemic ion balance with an increase in chloride and decrease in bicarbonate are therefore possible. However, BindRen did not induce any clinically relevant change in chloride and bicarbonate on treatment for up to one year. 4.5 Interaction with other medicinal products and other forms of interaction BindRen is not absorbed from the gastrointestinal tract but may affect the bioavailability or absorption rate of other medicinal products. In addition, reduced bioavailability of other medicinal products by changes in enterohepatic circulation, for example, steroid hormones with potential impairment of the effectiveness of oral contraceptives, have been reported for medicinal products with a similar mechanism of action to BindRen. When administering any medicinal product where a reduction in the bioavailability could have a clinically relevant effect on safety or efficacy, the medicinal product should be administered at least 1 hour before, or 3 hours after taking BindRen. Concomitant treatment with medicinal products with a narrow therapeutic window requires close monitoring of drug concentrations or adverse reactions, on initiation or dose-adjustment of either BindRen or the concomitant medicinal product. Interaction studies have been conducted in healthy volunteers. Interactions have not been studied at doses >9 g daily, and greater interaction effects at higher doses of BindRen cannot be excluded. Single dose interaction studies demonstrated that the bioavailability of ciprofloxacin, warfarin and enalapril were not affected when co-administered with BindRen (6-9 g/day). BindRen lowered the bioavailability of digoxin by 16% and Cmax by 17%, and the Cmax of enalapril by 27%. Due to the high in vitro binding potential between BindRen and levothyroxine, closer monitoring of thyroid stimulating hormone (TSH) levels in patients receiving BindRen and levothyroxine is recommended. No in vivo data are available on the possible interaction of BindRen on the absorption of the immunosuppressant medicinal products mycophenolate mofetil, ciclosporin or tacrolimus. However, decreased blood concentrations have been reported for medicinal products with a similar mechanism of action to BindRen. Caution should be exercised when prescribing BindRen to patients receiving immunosuppressants. Patients with seizure disorders were excluded from clinical trials with BindRen. Caution should be exercised when prescribing BindRen to patients also taking anti-seizure medicinal products. 4.6 Fertility, pregnancy and lactation BindRen is not absorbed and is not systemically available. No direct effects of BindRen are thus anticipated. However, other effects of BindRen may affect pregnant and breast-feeding women or influence fertility, see sections 4.4 and 4.5. Pregnancy No data are available to assess the safety and efficacy in pregnant women. Patients that become pregnant and where a benefit/risk assessment confirms continued treatment with BindRen, supplementation of vitamins may be required, see section 4.4. Breast-feeding No data are available to assess the safety and efficacy in breast-feeding women. Patients that breast-feed and where a benefit/risk assessment confirms continued treatment with BindRen, supplementation of vitamins may be required, see section 4.4. Fertility No data are available to assess the potential influence of BindRen on fertility. 4.7 Effects on ability to drive and use machines BindRen has no or negligible influence on the ability to drive and use machines. 4.8 Undesirable effects Summary of the safety profile The Phase II and III clinical studies involving 1,410 patients with CKD Stage 5 on dialysis treated with BindRen for up to one year constituted the safety population. Patients received doses of up to 15 g per day, in three divided doses of 5 g. Approximately 30% of patients experienced at least one adverse reaction. The most serious adverse reactions were gastrointestinal haemorrhage (uncommon) and constipation (common). The most frequently reported adverse reactions were nausea, dyspepsia and vomiting (all common). The frequency of adverse reactions increased with dose.
更新日期: 2014-09-29
附件:
201412723561833.pdf    

 
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