英文药名:KYTRIL(Granisetron Hydrochloride Tablet)
中文药名:盐酸格拉司琼片
生产厂家:中外制药
カイトリル錠1mg/カイトリル錠2mg/カイトリル細粒0.4%
治疗类别名称 5-HT3受体拮抗剂的止吐药 商標名 KYTRIL 一般名 グラニセトロン塩酸塩(Granisetron Hydrochloride)(JAN) 化学名 1-Methyl-N-(endo-9-methyl-9-azabicyclo[3.3.1]non-3-yl)-1H-indazole-3-carboxamide hydrochloride 構造式
分子式 C18H24N4O・HCl 分子量 348.87 性 状 它是用白色粉末或质量的粉末。易溶于水,微溶于甲醇,乙醇(95)非常微溶,并在乙醚中几乎不溶。 熔点 约291℃(分解) 适应症 用于防治化疗和放疗引起的恶心与呕吐。 用法用量 成人,每天一次,每次一片(2毫克),此外,增加或减少取决于患者的年龄和症状。 药效药理 1. 抗恶性肿瘤引起的呕吐的抑制 (1) 顺铂引起的呕吐抑制试验 在盐酸格拉司琼经口给药,静脉内给药后,其中的顺铂10毫克/公斤15分钟雪貂,观察到显著延长显著降低和呕吐在盐酸格拉司琼0.005/ kg以上呕吐次数的延迟时间这是。 (2) 在感应作用,阿霉素和环磷酰胺联合呕吐 口服施用盐酸格拉司琼为0.5mg/ kg的阿霉素为6mg/ kg和环磷酰胺80毫克/公斤至15分钟静脉内施用之前,在呕吐次显著减少和呕吐孵育时间显著延长据观察。 2. 研究的作用机制 (1) 各种亲和力受体 使用大鼠或豚鼠脑样品,它进行了检查盐酸格拉司琼对各种受体的亲和性,但这种药物表现出非常高的亲和力对5-HT 3受体的5(Ki值= 0.26纳米),5-HT(5-HT1A,5-HT1B/℃,5-HT1C),5-HT 2,多巴胺D2,肾上腺素α1,α2和β,苯二氮,印防己毒素和组胺H1,阿片类μ,每个κ和δ的为受体的亲和力,几乎看不到(比其他受体5 HT1C受体:Ki值>为1000nm,5 HT1C受体:IC50值>10000nM)。 (2) 在感应心动过缓5-HT的作用 在麻醉大鼠中研究了5-HT 3的瞬态心动过缓受体介导的(冯的Bezold-Jarisch反射)的5对5-HT的作用,盐酸格拉司琼抑制反射的剂量依赖性。 包装规格 片剂 1毫克:20片(PTP)
2毫克:10片(PTP)
細粒0.4% 0.5克×10包
制造厂商 中外制药有限公司 完整处方资料附件:http://www.info.pmda.go.jp/go/pack/2391002C1037_1_07/ KYTRIL Tablet 1mg(カイトリル錠1mg) Brand name : KYTRIL Tablet 1mg Active ingredient: Granisetron hydrochloride Dosage form: triangle-shaped, white tablet (perpendicular: approx. 7.1mm, thickness: approx. 2.7mm) Print on wrapping: カイトリル1mg KYTRIL Tablet 2mg(カイトリル錠2mg) Brand name : KYTRIL Tablet 2mg Active ingredient: Granisetron hydrochloride Dosage form: triangle-shaped, white tablet (perpendicular: approx. 8.5mm, thickness: approx. 3.7mm) Print on wrapping: カイトリル2mg Effects of this medicine This medicine exerts antagonistic inhibition on serotonin-its receptor combination, and prevents nausea and vomiting caused by taking anticancer drugs and radiation therapy. It is usually used to treat digestive symptoms (nausea and vomiting) caused by taking anticancer drugs or radiation therapy. Before using this medicine, be sure to tell your doctor and pharmacist •If you ever experienced any allergic reaction (itch, rash etc.) to any medicine. •If you are pregnant or breastfeeding. •If you are taking any other medicinal products. (Some medicines may interact to enhance or diminish medicinal effects. Beware of over-the-counter medicines and dietary supplements as well as other prescription medicines.) Dosing schedule (How to take this medicine) •Your dosing schedule prescribed by your doctor is << to be written by a healthcare professional>> •General dosage regimen: For adults, take 1 tablet (2mg of granisetron) once a day. It should be adjusted according to your age and symptoms. Strictly follow the instructions of your doctor/pharmacist. •Contact your doctor/pharmacist. If you do not take this medicine for a while, you may throw up or feel nauseous. DO NOT take double doses to make up for the missed dose. •If you took too much of this medicine (more than ordered), check with your doctor/pharmacist. •Do not stop taking this medicine without the instructions of your doctor. Precautions while taking this medicine • Possible adverse reactions to this medicine Common side effects are reported as below. If any of them occurs, check with your doctor/pharmacist: constipation, rash, etc. The symptoms described below are rarely seen as initial symptoms of the adverse reactions indicated in brackets. If any of these symptoms occur, stop taking this medicine and see your doctor immediately. •chills, cold sweat, numbness in the limbs, dizziness on standing up, breathing difficulty, chest pressured feeling, rash, urticaria, itch, swelling, decreased blood pressure [shock, anaphylactoid symptoms] The above symptoms do not describe all the adverse reactions to this medicine. Consult with your doctor or pharmacist if you notice any symptoms of concern other than those listed above. Storage conditions and other information •Keep out of the reach of children. Store at room temperature (1-30℃), away from direct sunlight and moisture. •Discard the remainder. Do not store them. Ask the pharmacist how to discard. Chugai Pharmaceutical Co., Ltd.Internal Revised: 12/2011 The information on this sheet is based on approvals granted by the Japanese regulatory authority. Approval details may vary by country. Medicines have adverse reactions (risks) as well as efficacies (benefits). It is important to minimize adverse reactions and maximize efficacy. To obtain a better therapeutic response, patients should understand their medication and cooperate with the treatment.
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