【成分】醋酸奥曲肽 octreotide acetate(妊娠分级: B)

【药物分类】脑垂体激素和相关药物

【性状】
　　醋酸奥曲肽的分子式 ： C49H66N10O10S2，nCH3COOH，分子量 ：1019.3，按游离肽计。
　　本品为白色或类白色粉末，装在5 mL I型硼硅酸盐管状玻璃瓶内，丁基橡胶塞。每个包装还包括 ：2 瓶（1支储备）溶剂，用于将药物溶解为2 mL溶液、以及1支5 mL注射器和两个针头（0.9×40 mm） ；注射器 CE0123。

【适应症】
　　已证实的使用 ：肢端肥大症 用于下列肢端肥大症患者的治疗 ：在皮下注射标准剂量的善宁后，病情已充分控制 ；不适合外科手术、放疗或治疗无效的患者，或在放疗充分发挥疗效前，处于潜在反应阶段的患者。
　　胃肠胰内分泌肿瘤伴有功能性胃肠胰内分泌肿瘤相关症状的患者，已经用皮下注射善宁治疗得到充分控制。
　　伴有类癌综合征特征的类癌 。
　　血管活性肠肽瘤。
　　胰高糖素瘤。
　　胃泌素瘤/卓－艾综合征。
　　胰岛素瘤（用于术前低血糖的预防和维持）。
　　生长激素释放因子腺瘤。

【用法用量】
　　本品仅能通过臀部肌肉深部注射给药，而决不能静脉注射。如果穿入血管要更换注射部位。反复注射应当轮流选择左侧或右侧不同的臀部肌肉注射。
　　肢端肥大症 对使用标准剂量皮下注射善宁已完全控制的患者，本品的推荐初始 剂量为20 mg，每隔4周给药1次，共3月。治疗可以在最后一次皮下注射善宁后1天开始。此后剂量应当根 据血清GH和生长因子C（IGF-1）的浓度以及临床症状和体征决定。
　　如果3月后临床症状和体征以及生化参数（GH和IGF-1）尚未完全控制（GH>2.5 ug/L）时，剂 量应当增至30 mg，每隔4周给药1次。如GH≤ (smaller than or equal to) 2.5 ug/L，则继续使用20 mg治疗，每4周给药1次。
　　如果使用20 mg治疗3月后，GH的浓 度持续低于1 ug/L，IGF-1的浓度正常以及临床上肢端肥大症的可逆的症状和体征消失，本品的剂量可降至10 mg。鉴于如此低的剂量，要密切观察监测血清GH和IGF-1的浓度以及临床症状和 体征。
　　对于不适合外科手术、放疗、多巴胺激动剂治疗或治疗无效的患者，或在放疗发挥充分疗效前病情处于潜在反应阶段的患者，建议在开始上述使用本品治疗 前，先短期使用皮下注射善宁以评估奥曲肽治疗的耐受性和疗效。
　　胃肠胰内分 泌肿瘤 已使用皮下注射善宁治疗的患者 ：对于症状已完全由皮下注射善宁控制的患者，建议本品的初始剂量为20 mg，每隔4周给药1次。原有的皮下注射善宁的有效剂量治疗应当维续到第一次注射本品后至少2周（有的患者则需维持3-4周）。
　　从未使用皮下注射善宁治疗的患者 ：建议开始使用本品治疗前，应短期（约2周）每日3次皮下注射善宁0.1 mg，以评估奥曲肽治疗反应和全身耐受性。
　　剂量调整 使用本品治疗3个月后，对于症状和生化 指标已完全控制的患者，本品剂量应当降至10 mg，每隔4周给药1次。
　　使用本品治疗3个月症状仅部分控制的患者，剂量应当增至30 mg，每隔4周给药1次。
　　使用本品治疗胃肠胰肿瘤期间，患者的症状会一度更明显。此时建议加用皮下注射 善宁，其剂量与使用本品之前相同。这对于治疗的最初2月使血奥曲肽达到治疗水平尤为重要。
　　肾功能损害患者的使用 ：当皮下注射善宁治疗时，肾功能损害不会影响血奥曲肽的曲线下面积（AUC）。因此本品的剂量不必调整。
　　肝功能损 害患者的使用 ：通过皮下和静脉途径给予善宁的研究发现肝硬化患者的清除力可能下降，而脂肪肝患者 则不然。鉴于奥曲肽较宽的治疗窗，肝硬化患者的本品的剂量不需调整。

【不良反应】
　　最常见的不良反应为局部反应和胃肠道症状。
　　局部反应 ：注射部位可能出现对本品的局部反应（疼痛、罕见的水肿和 皮疹）。这些通常很轻微且短暂。
　　胃肠道症状 ：胃肠道反应包括食欲减退、恶心、呕吐、腹部痉挛、腹胀、胀气、稀便、腹泻和脂肪泻。虽然大便脂肪排出量可能 增加，但目前无资料证实使用奥曲肽治疗（包括长期治疗）会由于吸收不良导致营养缺乏。个别罕见病例胃肠道反应类似急性肠梗阻，伴有进行性腹部膨胀、严重的上腹痛、肌紧张和腹胀。
　　胆石形成 ：长期使用本品可能会造成胆囊结石形成。
　　全身反应 ：有报道个别罕见病例使用本品治疗后出现暂时的脱发以及过敏反应。
　　胰腺 ：由于可以抑制GH、胰高糖素和胰岛素的分泌，本品可能影响葡萄糖的调节，可能损伤餐后糖耐量。个别使用皮下注射本品治疗的罕见病例，长期用药可能有 永久性的高血糖，也观察到有低血糖的发生。有报道少数患者在接受治疗后的最初的几小时或几天发生急性胰腺炎。也有报道长期使用善宁的患者会因胆石症导致胰腺炎的发生。
　　肝脏 ：有个别报道在使用奥曲肽后出现肝功受损。它们包括 ：非胆汁淤积性急性肝 炎，停用皮下注射善宁后转氨酶恢复正常。
　　缓慢发生的高胆红素血症伴碱性磷 酸酶、γ-谷氨酰转移酶的增高，以及转氨酶的轻度增高。
　　其它 ：同时给予奥曲肽及溴隐亭，可以增加溴隐亭的生物利用度。

【禁忌症】对于奥曲肽或制剂中任何成分过敏者。

【注意事项】
　　由于分泌GH的垂体瘤有增大的可能，从而导致严重的并发症（如视野受限），因此要密切监察所有的患者，一旦发现有肿瘤增大的证据，建议改用其 它的治疗方法。
　　已报道长期皮下注射善宁治疗的患者中有15-30%的患者有胆石 形成，一般人群（40-60岁）的患者病率为5-20%。长期使用本品治疗的肢端肥大症和胃肠胰肿瘤患者的资料显示 ：与皮下注射善宁的患者相比，使用本品治疗没有导致胆囊结石发生率的增加。然而仍建议在使用本品治疗前和治疗后约每隔6月进行胆囊超声检查。治疗期间发生的胆囊结石通 常是无症状的 ；有症状的结石应当使用药物（胆酸）或手术治疗。
　　对于胰岛素依赖的I型糖尿病患者，本品可能影响机体对血糖的调节功能，所需治疗量的胰岛素 可能会有所降低。皮下注射本品治疗，对于非糖尿病患者和有部分胰岛素受损的II型糖尿病患者，可能导致餐后血糖升高，因此建议注意监测糖耐量以及相应降糖治疗。
　　胰岛素瘤患者 ：由于奥曲肽抑制生长激素和胰高糖素的作用强于对胰岛素的抑制，且对胰岛素的抑制时间较短，因此奥曲肽有可能加重并延长低血糖的发作。应密 切观察此类患者。

【孕妇及哺乳期妇女用药】
　　动物生殖研究显示对胎儿无任何危害。但目前尚无使用本品治疗妊娠和哺乳妇女的经验。此类患者仅在绝对需要的情况下方可使用。

【儿童用药】目前尚无儿童使用本品的经验。
　　老年患者用药: 皮下注射善宁的研究发现，65岁以上的患者的剂量不需要调整。因此这些患者也不须调整本品的剂量。

【药物相互作用】
　　已发现奥曲肽可降低肠道对环孢素的吸收，也可减慢对西咪替丁的吸收。
　　同时使用奥曲肽及溴隐亭，可以增加溴隐亭的生物 利用度。
　　有限发表的数据显示，生长抑素类似物由于对生长激素的抑制作用可能减慢通过细胞色素P450酶代谢的物质的清除。虽然尚不能断言奥曲肽具有这样的效 应，但对同时使用主要通过CYP3A4代谢且治疗指数窄的药物，如奎尼丁和特非那定等时，应特别注意。

【药物过量】
　　目前没有过量使用本品的资料，但癌症患者每隔2周使用剂量达90 mg的本品后没有出现未预料的反应。曾经报道一成年患者在单剂 静脉推注1.0 mg后的症状和体征 ：短暂的心率下降、面部潮红、腹部痉挛、腹泻、胃内空虚感及恶心。以上所有症状及体征于24小时内消失。如有过量，须进行对症治疗。

【用药须知】
　　本品仅能通过臀部肌肉深部注射给药。重复注射应轮流选择左、右臀部肌肉。
　　本品肌肉注射的使用方法指导 仅用于臀部肌 肉深部注射，仅在立即注射前准备，须由有经验的医务人员严格按下列指导操作。
　　将本品置于室温下，使其温度与室温相同。揭开本品小瓶的小帽。
　　轻敲小瓶以确保粉末在小瓶的底部。
　　打开一支溶剂安瓿。如果开瓶时安瓿破损，丢弃并使用包装中的备用安瓿。
　　给5 mL注射器（包装内）安装上针头。
　　将1支安瓿内的溶剂吸入注射器，并调整至2 mL。
　　将针头从本品小瓶的橡皮塞中心插入。
　　小心地将溶剂沿小瓶内壁注入小瓶，抽出小瓶内多余的空气。
　　不要晃动小瓶直到本品粉末完全被溶剂浸湿（大约2-5分钟）。一旦完全浸 湿，轻旋小瓶直到形成均一悬浮液。不要猛烈地摇动小瓶。不要倒置药瓶，避免形成絮状凝结物，否则不可使用。
　　立即将2 mL空气吸入注射器，将针头从橡皮塞插 入。将2毫升空气注入小瓶，针头朝下，小瓶呈45度角斜置，缓慢将瓶内所有的溶液吸入注射器。
　　立即更换针头（包装内提供）。
　　轻轻倒 置注射器以保证悬浮液的均一。注射前应迅速倒置注射器一次，排出空气，消毒注射部位。将针头扎入左侧或右侧臀部肌肉并回抽以确保没有穿入血管。立即深部肌肉注射。

【配伍】注射用本品微球仅能单剂使用，而不能用其他物质稀释或混合。因此没有与其他溶液和物质的配伍数据记录。

【贮藏/有效期】
　　为延长贮存期，本品小瓶应当保存在2-8°C的冰箱内并避免冻结和光照。注射前约24小时，本品应放置在室温下。配制后的本品溶液应当立即使用。

【原产地英文商品名】SANDOSTATIN LAR 30mg/kit
【原产地英文药品名】OCTREOTIDE ACETATE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·善龙LAR 20毫克/套
·善龙LAR 10毫克/套
·善龙LAR 20毫克/套
【中文参考药品译名】醋酸奥曲肽
【生产厂家中文参考译名】诺华
【生产厂家英文名】Novartis

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【原产地英文商品名】SANDOSTATIN 0.5MG/ML/VIAL 10VIALS/BOX
【原产地英文药品名】OCTREOTIDE ACETATE
【中文参考商品译名】
注：以下产品不同规格和不同价格，购买时请以电话咨询为准！
·善龙 0.05毫克/毫升/瓶 10瓶/盒
·善龙 0.2毫克/毫升/瓶 5瓶/盒
·善龙 1毫克/毫升/瓶 5瓶/盒
·善龙 0.5毫克/毫升/瓶 10瓶/
【中文参考药品译名】醋酸奥曲肽
【生产厂家中文参考译名】诺华
【生产厂家英文名】Novartis

GENERIC NAME: OCTREOTIDE - INJECTION (ok-TREE-oh-tide)

BRAND NAME(S): Sandostatin

USES: Octreotide is used to treat severe watery diarrhea and sudden reddening of the face and neck caused by certain types of tumors (e.g., carcinoid tumors, vasoactive intestinal peptide tumors) that are found usually in the intestines and pancreas. The symptoms occur when these tumors make too much of certain natural substances (hormones). This medication works by blocking the production of these hormones. By decreasing watery diarrhea, octreotide helps to reduce the loss of body fluids and minerals.Octreotide is also used to treat a certain condition (acromegaly) that occurs when the body makes too much of a certain natural substance called growth hormone. Treating acromegaly helps reduce the risk of serious problems such as diabetes and heart disease. Octreotide works by decreasing the amount of growth hormone to normal levels.This drug is not a cure for these conditions. This medication is usually used with other treatment (e.g., surgery, radiation, other drugs).

HOW TO USE: This medication is usually given by injection under the skin, usually 2 to 3 times a day or as directed by your doctor. Depending on your condition, it may be given by injection into a vein by a health care professional.If your doctor directs you to inject this medication under the skin yourself, learn all preparation and usage instructions from your health care professional. Learn how to store and discard needles and medical supplies safely. If you have questions, ask your health care professional.Before using, check this product visually for particles or discoloration. If either is present, do not use the liquid. Before injecting each dose, clean the injection site with rubbing alcohol. Change the location of the injection site each time to avoid problem areas under the skin.Dosage is based on your medical condition and response to treatment.Use this medication regularly to get the most benefit from it. To help you remember, use it at the same times each day.Tell your doctor if your condition does not improve or if it worsens.

SIDE EFFECTS: Nausea, vomiting, loose/oily stools, constipation, stomach upset, gas, bloating, dizziness, or headache may occur. Pain and irritation at the injection site may also occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.Tell your doctor immediately if any of these unlikely but serious side effects occur: signs of gallbladder/liver problems (e.g., fever, stomach/abdominal pain, severe nausea/vomiting, yellowing eyes/skin, unexplained pain in the back/right shoulder), signs of underactive thyroid (e.g., unexplained weight gain, cold intolerance, slow heartbeat, severe constipation, unusual/extreme tiredness, growth/lump/swelling on the front of the neck), worsening heart condition symptoms (e.g., trouble breathing, slow/fast/irregular heartbeat), numbness/tingling of the arms/legs.This medication may infrequently cause changes in blood sugar, especially if you have diabetes. Symptoms of high blood sugar include increased thirst and urination. Symptoms of low blood sugar include nervousness, shakiness, sweating, fast heartbeat, and hunger. Follow your doctor's instructions to treat low blood sugar (e.g., eat a quick source of sugar such as glucose gel/tablets, table sugar, or honey, or drink fruit juice or non-diet soda). Tell your doctor immediately if you experience symptoms of high or low blood sugar while taking this medication. Monitor your blood sugar levels as directed by your doctor.A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.In the US -Call your doctor for medical advice about side effects.

PRECAUTIONS: Before using octreotide, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.Before using this medication, tell your doctor or pharmacist your medical history, especially of: kidney disease, liver disease (e.g., cirrhosis), diabetes, thyroid problems, gallbladder problems (e.g., gallstones), nutrition problems (e.g., decreased fat absorption, vitamin B12 deficiency).This drug may make you dizzy. Do not drive, use machinery, or do any activity that requires alertness until you are sure you can perform such activities safely. Limit alcoholic beverages.Caution is advised when using this drug in children. Use of this medication for long periods (e.g., longer than 1 year) may slow a child's growth rate. However, the growth rate catches up after treatment with the drug is stopped. Consult your doctor for more information.This medication may restore the normal ability to become pregnant in females with acromegaly who have infertility. Females of childbearing age should discuss reliable forms of birth control with the doctor. During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.It is not known whether this drug passes into breast milk. Consult your doctor before breast-feeding.

DRUG INTERACTIONS: Your doctor or pharmacist may already be aware of any possible drug interactions and may be monitoring you for them. Do not start, stop, or change the dosage of any medicine before checking with them first.Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: beta-blockers (e.g., metoprolol, propranolol), calcium channel blockers (e.g., diltiazem, verapamil), cyclosporine, drugs to treat diabetes (e.g., glyburide, insulin), nutritional solutions given by vein (e.g., total parenteral nutrition-TPN), pegvisomant, "water pills" (diuretics such as furosemide, hydrochlorothiazide).This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, contact your local poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others.Laboratory and/or medical tests (e.g., blood glucose tests, thyroid function tests, hormone levels, vitamin B12 levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store this medication in the refrigerator between 36-46 degrees F (2-8 degrees C) away from light. Allow the medication to come to room temperature before using. This medication is good for 2 weeks if stored at room temperature between 68-86 degrees F (20-30 degrees C) away from light. Multi-use vials should be discarded 2 weeks after opening. Ampules should be opened just before each dose, and any unused portion should be discarded. Do not store in the bathroom. Keep all medicines away from children and pets.Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.