贝沙罗汀1%软膏TARGRETIN(bexarotene capsules)

产地国家美国

处方药

所属类别 75毫克/胶囊, 100胶囊/瓶

包装规格 75毫克/胶囊, 100胶囊/瓶

计价单位

生产厂家英文名Ligand Pharmaceuticals

原产地英文商品名TARGRETIN  100 x 75mg

原产地英文药品名bexarotene capsules中文参考商品译名TARGRETIN 75毫克/胶囊, 100胶囊/瓶中文参考药品译名蓓萨罗丁

简介:

Targretin (Cephalon)[bexaroteen]caps.100 x 75mg(leukopenie, hyperlipidemie, hypothyreose, huidreacties, hoofdpijn, inductor van CYP2C9 en CYP3A4【商品名】Targretin

【通用名】Bexarotene

【化学名】4-[1-(5,6,7,8-四氢-3,5,5,8,8-五甲基-2-萘基)乙烯基]苯甲酸

【上市厂商】由美国Ligand制药公司研制,2000年1月15日在美国首次上市。

【适应证】用于口服治疗顽固性皮肤T-细胞淋巴瘤的皮肤症状。TARGRETIN

【药理作用】本品可选择性地结合并激活视黄酸类(retinoid)X受体亚型(RXRα,RXRβ,RXRγ)。RXR可与多种受体[如维A酸受体(RAR)、维生素D受体、甲状腺素受体,以及过氧化物酶体增生物激活受体(PPAR)]形成异二聚体。这些受体一旦被激活可控制基因的表达,控制细胞分化和增生。在体外试验中,本品可抑制某些肿瘤细胞系的生长;在动物模型体内试验中,本品可诱使乳腺瘤消退。本品口服后,约2小时达血浆峰浓度,半衰期约为7小时。含脂食物可增加本品吸收,较之葡萄糖溶液,含脂食物可使300mg本品的AUC及Cmax分别上升35%和48%;本品可与血浆蛋白高度结合(99%)。在血浆中能测得本品的四种代谢产物:6-和7-羟基bexarotene以及6-和7-氧代bexarotene。体外试验显示细胞色素P450 3A4是对氧化产物形成及氧化产物葡糖醛酸化起主要作用的酶。经对Ⅱ型糖尿病患者进行本品及本品代谢物肾消除过程的检测,目前认为本品主要大部分随胆汁消除,基本不随尿液排出。

【临床评价】两项开放性研究显示本品对早期及晚期难治性皮肤T-细胞淋巴瘤有效。在第一项研究中,对至少两种治疗方法无反应或不能耐受的早期皮肤T-细胞淋巴瘤病人服用本品一日300mg/m2后,28例病人中有15例(54%)获得全部或部分反应(改善至少达50%以上),而更高剂量组反应率为10例/15例(67%),此外,一日300mg/m2组中有2例病人在25周内复发。在第二项研究中,94例至少一种全身性治疗方法无效的晚期皮肤T-细胞淋巴瘤病人中,56例接受本品一日300mg/m2后有25例(45%)获得反应,另外35例接受较高剂量本品,有21例(55%)获得瓜;低剂量组有反应的病人中有9例经中位时间19周复发。在两项研究中,共有84例病人接受本品一日300mg/m2,其中3例(4%)获得完全反应,40例(48%)获得部分瓜;在高剂量组中,完全反应率为9例/53例(17%)。

【不良反应】本品的多数不良反应与剂量有关,使用本品后大部分病人会出现高甘油三酯血症、高胆固醇血症及高密度脂蛋白水平低下,通常需要对症治疗或减少本品的用药剂量;此外,尚易发生中枢性甲状腺机能减退并需要治疗,还常发生头痛、虚弱、白细胞减少、贫血、感染、皮疹、光敏反应和脱发。临床研究中约30%的病人停药;亦有转氨酶升高、致命性胰腺炎和致命性胆汁郁积的报道。

【注意事项】本品可对胎儿造成伤害,故孕妇禁用。在动物试验中本品可致睾丸萎缩。本品理论上与P450 3A4诱导剂或抑制剂可发生相互作用;已发现经P450 3A4代谢的吉非贝齐(gemfibrozil)可升高本品血浆浓度,这至少部分归因于吉非贝剂能抑制细胞色素P4503A4;本品与胰岛素、磺酰脲类、二甲双胍、曹格列奈或噻唑烷二酮(格列酮)类药物合用时可致低血糖。由于本品是一种VA衍生物,与VA合用可增加药物的毒性作用。对bexarotene或该产品的其他成分过敏者禁用。

【用法与用量】治疗皮肤T-细胞淋巴瘤的推荐剂量为一日300mg/m2,与食物同服;若8周后尚未见疗效,则可增加剂量至一日400mg/m2,最佳治疗时间目前尚未确定。

【剂型规格】本品为75mg口服明胶软胶囊制剂;软膏药100 x 75mg/盒TARGRETIN胶囊。

英文版说明书:

Generic Name for TARGRETINBexarotene 75mg; caps.Legal Classification:RxPharmacological Class for TARGRETINRetinoid.Manufacturer of TARGRETINEisai PharmaceuticalsIndications for TARGRETINCutaneous manifestations of cutaneous T-cell lymphoma in patients who are refractory to at least one prior systemic therapy.Adult dose for TARGRETINTake with food. Initially 300mg/m2 once daily; may increase after 8 weeks to 400mg/m2 once daily if no tumor response and if well tolerated; monitor carefully. If toxicity occurs, reduce to 200mg/m2 then 100mg/m2 once daily, or suspend therapy.Children’s dosing for TARGRETINNot recommended.Contraindications for TARGRETINPregnancy (Cat.X).Warnings/Precautions for TARGRETINBe fully familiar with this drug’s toxicity before use. Pancreatitis or risk of pancreatitis (eg, history of pancreatitis, uncontrolled hyperlipidemia, excess alcohol consumption, uncontrolled diabetes, biliary tract disease, drugs that can cause pancreatitis). Counsel patients monthly about need for contraception. Women of childbearing potential: obtain reliable negative pregnancy test within 1 week of start; repeat monthly. Start therapy on 2nd or 3rd day of normal menstrual period. Use two effective forms of contraception 1 month prior to, during, and for 1 month after therapy. Max 1 month/℞. Men with partners who are or may become pregnant: use condoms during and for at least 1 month after therapy. Monitor lipids before treatment, weekly until stable, then every 8 weeks; try to keep triglycerides <400mg/dL; treat hyperlipidemia, or reduce or suspend bexarotene if needed. Hepatic or renal insufficiency. Monitor liver function at baseline, 1, 2, and 4 weeks after start, then (if stable) at least every 8 weeks during therapy; consider suspending or discontinuing treatment if SGOT/AST, SGPT/ALT, or bilirubin >3xULN occurs. Monitor WBC with differential and thyroid function at baseline and during treatment; treat hypothyroidism if needed. Avoid sun and UV light. Nursing mothers: not recommended.Interactions for TARGRETINConcomitant gemfibrozil: not recommended. Levels may be increased by CYP3A4 inhibitors (eg, ketoconazole, itraconazole, erythromycin, grapefruit juice). Levels may be reduced by CYP3A4 inducers (eg, rifampin, phenobarbital, phenytoin). May potentiate antihyperglycemics (eg, insulin, sulfonylureas, thiazolidinediones); monitor. May potentiate or be potentiated by protein-bound drugs. May antagonize tamoxifen, hormonal contraceptives, other CYP3A4 substrates. Limit Vit. A supplements to avoid toxicity. May increase CA125 assay values.Adverse Reactions for TARGRETINLipid abnormalities, headache, hypothyroidism, asthenia, leukopenia, anemia, rash, GI disturbances, peripheral edema, dry skin, exfoliative dermatitis, alopecia, insomnia, fatigue, abnormal liver function tests, pancreatitis, pruritus, photosensitivity.How is TARGRETIN supplied?Caps—100Related Disease:Lymphoma, cutaneous T-cell.

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