英文药名：PROTECADIN OD tablet（Lafutidine）

中文药名：拉呋替丁口腔崩解片

生产厂家：大鹏制药
类别名称
H2受体拮抗剂
商標名
PROTECADIN OD tablet
一般名
ラフチジン（Lafutidine）
**化学名
2-［（RS）-Furan-2-ylmethylsulfinyl］-N-{4-［4-（piperidin-1-ylmethyl）pyridin-2-yl］oxy-（2Z）-but-2-en-1-yl}acetamide
分子式
C22H29N3O4S
分子量
431.55
分配係数（log P）
-3.36（pH2）、0.39（pH6）、2.37（pH10）
（1-オクタノール/Britton-Robinson Buffer（20±1℃））
**構造式

**性状
白是一种浅黄色结晶性粉末。易溶于乙酸（100），微溶于甲醇，稍少溶于乙醇（99.5），并且几乎不溶于水。甲醇溶液（1→100）示出了没有旋光性。水晶多态性观察。
操作注意事项
<注>
(1) 开封后应存放，避免受潮。
(2) 30℃，相对湿度75％，白色荧光灯（500 LX）贮存条件下，稍微观察到色素，注意保存开盘后
药理作用
本品具有持续的抗分泌作用和潜在的胃黏膜保护作用。呈剂量依赖性地减少由组胺、四肽胃泌素、氯甲酰甲胆碱和乙-脱氧-D-葡萄糖刺激引起胃酸分泌
适应证
○胃溃疡，十二指肠溃疡，吻合口溃疡，反流性食道炎
○下列疾病胃粘膜病变（糜烂，出血，发红，肿胀）改善
急性胃炎，慢性胃炎急性发作
○麻醉前用药
用法用量
○胃溃疡，十二指肠溃疡，吻合口溃疡，反流性食道炎
成人:
每天口服二次，每次口服一次10毫克（早饭后，晚饭后或睡前）。此外，将根据年龄和症状调整。
○下列疾病胃粘膜病变（糜烂，出血，发红，肿胀）改善
急性胃炎，慢性胃炎急性发作
成人:
每天口服二次，每次口服10毫克（早饭后，晚饭后或睡前）。此外，将根据年龄和症状调整。
○麻醉前用药
通常口服两次10毫克单一手术前一天睡前和手术麻醉的一天推出前2个小时的拉呋替丁成人。
包装规格
OD片：5mg
PTP包装：100片（10片×10），1000片（10片×10×10）

OD片：10mg
PTP包装：100片（10片×10），1000片（10片×10×10）

生产商：大鹏制药
Brand name : PROTECADIN OD Tablet 5
　Active ingredient: Lafutidine
　Dosage form: yellowish white tablet (φ: 6.0mm, thickness: 3.1mm)
　Print on wrapping: (face) プロテカジンOD 5mg口腔内崩壊錠 (back) プロテカジン OD 5mg 口腔内崩壊錠 TC23
-------------------------------------
Brand name : PROTECADIN OD Tablet 10
　Active ingredient: Lafutidine
　Dosage form: white tablet (φ: 8.0mm, thickness: 3.7mm)
　Print on wrapping: (Face) プロテカジンOD 10mg 口腔内崩壊錠,(back) プロテカジンOD 10mg 口腔内崩壊錠 TC24 
Effects of this medicine
This medicine reduces acid production in the stomach by histamine H2 receptor antagonism. It increases gastric mucus, too.
It is usually used to treat gastric/duodenal/anastomotic ulcer, reflux oesophagitis and to improve gastric mucosal lesion caused by acute gastritis/acutely exacerbated chronic gastritis. It is also used for anesthetic premedication.
Before using this medicine, be sure to tell your doctor and pharmacist
•If you have previously experienced any allergic reactions (itch, rash, etc.) to any medicines.
If you are a patient with renal or liver damage.
If you are receiving dialysis.
•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>>
•For the treatment of gastric/duodenal/anastomotic ulcer, reflux oesophagitis, For adults, take 2 tablets (10mg as active ingredient) at a time, twice a day, after breakfast and after dinner or at bedtime. The dose may be adjusted according to your disease, age and symptoms.
For the improvement of gastric mucosal lesion caused by acute gastritis or acutely exacerbated chronic gastritis, For adults, take 2 tablets (10mg as active ingredient) once a day, after dinner or at bedtime. The dose may be adjusted according to your disease, age and symptoms.
For anesthetic premedication, For adults, take 2 tablets (10mg as active ingredient) at a time, 2 times; at bedtime of the day before the operation day, and 2 hours before anesthesia induction on the operation day. In each case, strictly follow the instructions of your doctor/pharmacist.
•This medicine is designed to be dissolved after soaking it with saliva on the tongue so it can be swallowed with saliva. It may be taken with water like usual drugs.
•Do not take the tablet without water when you are lying down.
•If you miss a dose, take the missed dose as soon as possible. However, if it is almost time for the next dose, skip the missed dose. You should never take two doses at one time.
•If you accidentally take more than your prescribed dose, consult with your doctor or pharmacist.
•Do not stop taking this medicine unless your doctor instructs you to do so.
Precautions while taking this medicine
• Possible adverse reactions to this medicine
The most commonly reported adverse reactions include rash, constipation and diarrhea. If any of these symptoms occur, consult with your doctor or pharmacist.
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.
•facial pallor, decrease in blood pressure, breathing difficulty [shock, anaphylactoid symptoms]
•lassitude, appetite loss, yellowness in the skin and the white of the eye [liver dysfunction, jaundice]
•sore throat, lassitude, bleeding tendency (blue spot) [agranulocytosis, thrombocytopenia]
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 away from heat, moisture and direct sunlight.
•Discard the remainder. Do not store them.
http://www.info.pmda.go.jp/go/pack/2325006F3020_1_03/
临床研究
拉呋替丁是日本富士（ Fujirebio）公司和大鹏（Taiho）公司联合开发的一种抗溃疡药，该产品为强效、长效的第二代组胺H2受体拮抗剂，具有独特的胃保护作用。已于2000年4月在日本上市。 本品为第二代H2受体拮抗剂，主要用于治疗消化性溃疡，本品可减少胃酸的基础分泌量，抑制组胺、胃泌素、乌拉坦刺激的胃酸分泌。相比其它同类药物（如西咪替丁和法莫替丁），本品对H2受体的阻断作用更有效、持久，所以具有抗胃酸分泌作用更加持续的优点。 胃溃疡和十二指肠溃疡 。
药理作用
拉呋替丁能持续地抑制人胃酸、胃蛋白酶的基础分泌、夜间分泌及四肽胃泌素等刺激因子引起的分泌，对胃酸的抑制作用与法莫替丁和西咪替丁相比，作用更有效、更持久。拉呋替丁还具有很强的黏膜保护作用，在低于抗胃酸分泌剂量下就可产生抗溃疡活性。而法莫替丁和西咪替丁只有在高于抗分泌剂量下才能发挥抗溃疡活性。动物实验中，拉呋替丁可使胃黏膜损伤加速愈合，包括恢复变薄的胃黏膜厚度和减少的壁细胞数量，而法莫替丁和西咪替丁在产生相同程度的抗胃酸分泌作用的同时没有这些形态学作用。以奥美拉唑为代表的现有的质子泵抑制剂也无胃黏膜保护作用。另外，接受拉呋替丁治疗后的复发率低。与法莫替丁和雷尼替丁在实验性胃溃疡愈合率相当的剂量下，三者的溃疡复发率分别为4%、40.9%和31.3%，拉呋替丁与后二者差异有显着性。
临床作用
1) 治疗消化性溃疡
临床试验中，采用多中心、随机、双盲、阳性药物平行对照的临床研究。对不同中心进行区组随机分配，分为两组，一组为试验药拉呋替丁片，另一组为对照药法莫替丁片。本试验共入组患者207例，拉呋替丁组103例，法莫替丁组104例，全部患者均使用了研究药物并进行了至少一次安全性评价和有效性评价，202例被纳入PPS分析，其中拉呋替丁组102例，法莫替丁组100例，所有入组患者被纳入FAS分析与安全性分析数据集（SS）分析；试验中有5例患者脱落，脱落率为2.42%。无剔除病例。内镜检查溃疡愈合率：PPS人群中拉呋替丁组溃疡愈合率为85.1%,法莫替丁组溃疡愈合率为75%，两组溃疡治愈率差异无显着性（P>0.05）。总有效率：PPS人群中拉呋替丁组溃疡总有效率为93.1%,法莫替丁组溃疡总有效率为82%，两组总有效率差异有显着性（P<0.05）。
2) 治疗急性胃炎
临床报道，在治疗急性胃炎时，服用拉呋替丁10mg/次，2次/d，连续用药6天，结果治愈率为96.8%。机制：胃炎急性期胃黏膜充血、水肿、胃酸分泌过多等造成一系列临床刺激症状，应用拉呋替丁将H2受体阻断，减少胃酸分泌，控制和改善黏膜充血、水肿，使疼痛、恶心及呕吐症状消失。
3) 在胃泌素瘤中的应用
胃泌素瘤好发于十二指肠和胰腺，亦可见于脾门、胃或肝脏，高胃泌素血症是诊断胃泌素瘤有价值的依据之一。大多数胃泌素瘤病人未刺激胃酸分泌超过18mmol/L。拉呋替丁是被证明治疗胃泌素瘤有效的H2受体阻断剂，可缓解症状、减少酸分泌和治疗溃疡。拉呋替丁经安全性评价，均未证明有致癌性、致突变性和致畸性。根据临床观察，本药不良反应甚微，少数患者有口干、头晕、失眠、便秘、腹泻等症状。