【药理毒理】 本药转移到胃粘膜壁细胞的酸分泌细管后,在酸性条件下,转变为活性体结构,此种活性物与质子泵((H++K+)-ATPase)的SH基结合,从而抑制该酶的活性,故能抑制胃酸的分泌。 1.(H++K+)-ATPase活性抑制作用,兰索拉唑可抑制狗胃粘膜内微粒体的(H++K+)-ATPase活性(体外实验)。 2.壁细胞酸生成抑制作用,兰索拉唑对狗胃粘膜离体壁细胞由组胺、乙酰胆碱及胃泌素的刺激所产生的酸分泌,皆具有抑制作用(体外实验)。 3.胃酸分泌抑制作用, 1)对胃泌素刺激引起的酸分泌:于健康成人,1天1次兰索拉唑30mg口服给药,连续7天,可明显地抑制由胃泌素引起的酸分泌,且此作用能持续24小时。 2)对胰岛素刺激引起的酸分泌:于健康成人,1天1次兰索拉唑30mg口服给药,连续7天,可明显地抑制由胰岛素引起的酸分泌。 3)对夜间的酸分泌:于健康成人,1天1次兰索拉唑30mg口服给药,连续7天,具有明显地抑制夜间胃酸分泌的作用。 4)对24小时的酸分泌:于健康成人24小时胃液采样试验,以1天1次兰索拉唑30mg口服给药连续7天,24小时的胃酸分泌明显地受到抑制。 5)24小时胃内pH值的监测:对健康成人以及十二指肠溃疡患者,以1天1次兰索拉唑30mg口服给药连续7天,24小时的胃酸分泌皆明显地受到抑制。 6)24小时下部食道pH值的监测:于反流性食管炎患者,以1天1次兰索拉唑30mg口服给药连续7天~9天,对胃食管反流现象,有明显地抑制作用。 7)对大白鼠及胃pouch狗的胃酸分泌:本药对于大白鼠的基础酸分泌和因组胺、胃泌素、氨基甲酰基胆碱、2-脱氧-D-葡萄糖或水浸应激试验(water immersion stress)所引起的酸分泌均能明显且持续地抑制(在十二指肠内)。对胃pouch狗因各种刺激所引起的酸分泌,本药亦有明显且持续地抑制作用,在反复给药期间,均能显示稳定的酸分泌抑制作用(经口给药)。 4.慢性溃疡的治愈促进作用,于大白鼠的实验,兰索拉唑能明显地促进由醋酸引起的慢性胃及十二指肠溃疡的愈合(经口给药)。 5.溃疡形成的抑制作用,于大白鼠的实验,对因水浸应激试验、阿司匹林或乙醇引起的胃溃疡,及因mepirisol或半胱胺引起的十二指肠溃疡,和反流性食管炎皆有明显的抑制作用(经口或十二指肠内给药)。
【药代动力学】 1.血中浓度 兰索拉唑的生物利用度具有个体差异性。于空腹或餐后对健康成人(6例)经口给予1次30mg的药量时,血中主要检测到药物原形,其代谢物亦可测得。空腹服药的Tmax为2.2± 0.4h,Cmax为1038± 323ng/ml,T1/2为1.44± 0.94h,AUC为3890± 2484 ng· h/ml。餐后服药的Tmax为3.5± 0.8h,Cmax为679± 359ng/ml,T1/2为1.60± 0.90h,AUC为 3319± 2651ng· h/ml。尿中未能检出兰索拉唑的原形,只检出其代谢物,至服用后24小时为止,其尿中排泄率为13.1~14.3%。此外,对健康成人(6例),晨间空腹时,经口给予兰索拉唑30mg1天1次,连续7天,由血中浓度的变化及尿中排泄率来观察,体内无蓄积性。
【适应症】 胃溃疡、十二指肠溃疡、反流性食管炎、卓-艾综合征(Zollinger-Ellison症候群)、吻合口部溃疡。
【用法用量】 十二指肠溃疡,通常成人每日一次,口服兰索拉唑15mg~30mg,连续服用4~6周;胃溃疡、反流性食管炎、卓-艾综合征(Zollinger-Ellison症候群)、吻合口部溃疡,通常成人每日一次,口服兰索拉唑30mg,连续服用6~8周。但用做维持治疗、高龄者、有肝功能障碍、肾功能低下的患者,每日一次,口服兰索拉唑15mg。
【不良反应】 1)过敏症:偶有皮疹、瘙痒等症状,如出现上述症状时请停止用药。 2)肝脏:偶有GOT、GPT、ALP、LDH、γ-GTP上升等现象,所以须细心观察,如有异常现象应采取停药等适当的处置。 3)血液:偶有贫血、白细胞减少,嗜酸球增多等症状,血小板减少之症状极少发生。 4)消化器:偶有便秘,腹泻,口渴,腹胀等症状。 5)精神神经系统:偶有头痛、嗜睡等症状。失眠,头晕等症状极少发生。 6)其它:偶有发热,总胆固醇上升,尿酸上升等症状。
【禁忌】 对本品过敏者禁用
【注意事项】 1.在治疗过程中,应充分观察,按其症状使用治疗上所需最小剂量。 2.下列患者慎重用药 1)曾发生药物过敏症的患者 2)肝功能障碍的患者 3.其它 对大白鼠经口给药52周的实验,50mg/kg/日组(约为临床用量的100倍),发现1例有良性精巢间细胞瘤。于大白鼠经口给药24个月的实验,15mg及50mg/kg/日组中,精巢间细胞瘤发生率会增加,在50mg/kg/日组中发现1例雌大白鼠有胃部类癌(carcinoid)出现。 因本药会掩盖胃癌的症状,所以须先排除胃癌,方可给药。
【孕妇及哺乳期妇女用药】 1.已确认兰索拉唑在大白鼠胎仔的血浆浓度比在母鼠中高。又在兔子(经口给药30mg/kg)的实验发现胎仔死亡率增加,故对孕妇或有可能怀孕的妇女,需事先判断治疗上的益处超过危险性时,方可用药。 2.曾有报告指出,在动物实验中药品会转移到乳汁中。所以本药品不适合用于正在哺乳中的妇女。如不得已需服药时,应避免哺乳。
【儿童用药】 对儿童用药的安全性尚未确立(由于在小儿的临床经验极少)。
【老年患者用药】 一般而言,老年患者的胃酸分泌能力和其他生理机能均会降低,故用药期间请注意观察。
【药物相互作用】 会延迟安定(diazepam)及苯妥英钠(phenytoin)的代谢与排泄,资料已被发表于类似药物奥美拉唑的报告中。
【贮藏】 密封,在干燥处保存
【原产地英文商品名】PREVACID SOLUTAB DR 30mg/tablet 100tablets/box 【原产地英文药品名】LANSOPRAZOLE 【中文参考商品译名】 注:以下产品不同的规格不同的价格,购买时请以电话咨询为准! ·PREVACID口服缓释分散片 30毫克/片 100片/盒 ·PREVACID口服缓释分散片 15毫克/片 100片/盒 【中文参考药品译名】兰索拉唑 【生产厂家中文参考译名】武田 【生产厂家英文名】TAKEDA PHARMS NA
Prevacid Generic Name: lansoprazole (lan SOE pra zol) Brand Names: Prevacid, Prevacid SoluTab
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What is Prevacid? Prevacid decreases the amount of acid produced in the stomach.
Prevacid is used to treat and prevent stomach and intestinal ulcers, erosive esophagitis (damage to the esophagus from stomach acid), and other conditions involving excessive stomach acid such as Zollinger-Ellison syndrome.
Prevacid may also be used for other purposes not listed in this medication guide.
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Important information about Prevacid Before taking Prevacid, tell your doctor if you are allergic to any drugs, or if you have any type of liver disease. You may need a dose adjustment or special tests to safely take this medication.
Some conditions are treated with a combination of Prevacid and antibiotics. To best treat your condition, use all of your medications as directed by your doctor. Be sure to read the medication guide or patient instructions provided with each of your medications. Do not change your doses or medication schedule without advice from your doctor.
If you also take sucralfate (Carafate), avoid taking it at the same time you take Prevacid. Sucralfate can make it harder for your body to absorb Prevacid. Wait at least 30 minutes after taking this medicine before you take sucralfate.
Take Prevacid for the entire length of time prescribed by your doctor. Your symptoms may get better before your treatment is completed. Some forms of this medication may contain phenylalanine. Tell your doctor if you have phenylketonuria.
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What should I discuss with my healthcare provider before taking Prevacid? You should not use Prevacid if you are allergic to lansoprazole. Before taking this medication, tell your doctor if you are allergic to any drugs, or if you have any type of liver disease. You may need a dose adjustment or special tests to safely take Prevacid.
Some conditions are treated with a combination of Prevacid and antibiotics. To best treat your condition, use all of your medications as directed by your doctor. Be sure to read the medication guide or patient instructions provided with each of your medications. Do not change your doses or medication schedule without advice from your doctor.
FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment. It is not known whether Prevacid passes into breast milk or if it could harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.
Some forms of Prevacid may contain phenylalanine. Tell your doctor if you have phenylketonuria.
Do not give this medication to a child younger than 1 year old.
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How should I take Prevacid? Take Prevacid exactly as it was prescribed for you. Do not take the medication in larger amounts, or take it for longer than recommended by your doctor. Follow the directions on your prescription label.
Take each dose with a full glass (8 ounces) of water. Prevacid should be taken before eating. Do not crush or open a delayed-release capsule. Swallow the pill whole. It is specially made to release medicine slowly in the body. Breaking or opening the pill would cause too much of the drug to be released at one time.
If you are unable to swallow a delayed-release capsule whole: Open the capsule and sprinkle the medicine into a spoonful of pudding, applesauce, yogurt, cottage cheese, strained pears, or a nutritional drink such as Ensure. Swallow this mixture right away without chewing. Do not save the mixture for later use. Discard the empty capsule.
You may also dissolve the medicine from a Prevacid capsule in 2 ounces (1/4 cup) of apple juice, orange juice, or tomato juice. Stir this mixture and drink all of it right away. To make sure you get the entire dose, add a little more juice to the same glass, swirl gently and drink right away.
Dissolve the oral granules in 2 tablespoons of water. Use only water when mixing lansoprazole oral granules. Stir this mixture and drink all of it right away. To make sure you get the entire dose, add a little more water to the same glass, swirl gently and drink right away.
To take Prevacid orally disintegrating tablet: Use dry hands to remove the tablet and place it
in your mouth. It will begin to dissolve right away. Allow the tablet to dissolve in your mouth without chewing, swallowing several times as it dissolves.
The Prevacid orally disintegrating tablet may be taken with an oral syringe as follows: Place the dry tablet into a 15-milliliter oral syringe and draw 10 milliliters of water into the syringe. Shake until the tablet is dissolved and then empty the syringe into your mouth. Refill the syringe with water, shake gently, and empty into your mouth.
The disintegrating tablet can also be given through a nasogastric (NG) feeding tube as follows:
Place a 15-milligram tablet in a syringe and draw up 4 milliliters of water (or 10 milliliters of water if using a 30-milligram tablet). Shake until the tablet is dissolved. Attach the syringe to the NG tube and push the plunger down to empty the syringe into the tube. Then flush the tube with more water to wash the contents down.
It is important to use Prevacid regularly to get the most benefit. Get your prescription refilled before you run out of medicine completely.
Take this medication for the entire length of time prescribed by your doctor. Your symptoms may get better before your treatment is completed. Store Prevacid at room temperature away from moisture and heat.
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What happens if I miss a dose? Take the missed dose as soon as you remember. If it is almost time for your next dose, skip the missed dose and take the medicine at the next regularly scheduled time. Do not take extra medicine to make up the missed dose.
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What happens if I overdose? Seek emergency medical attention if you think you have used too much of this medicine. An overdose of Prevacid is not expected to produce life-threatening symptoms.
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What should I avoid while taking Prevacid? If you also take sucralfate (Carafate), avoid taking it at the same time you take Prevacid.
Sucralfate can make it harder for your body to absorb Prevacid. Wait at least 30 minutes after taking this medication before you take sucralfate.
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Prevacid side effects Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.
Less serious Prevacid side effects may include: headache; nausea, stomach pain; diarrhea; or constipation.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
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What other drugs will affect Prevacid? Before taking Prevacid, tell your doctor if you are using any of the following drugs: ampicillin (Omnipen, Principen); atazanavir (Reyataz); clopidogrel (Plavix); digoxin (Lanoxin, Lanoxicaps); ketoconazole (Nizoral); a blood thinner such as warfarin (Coumadin); iron (Feosol, Mol-Iron, Fergon, Femiron, others); or theophylline (such as Elixophyllin, Respbid, Slo-Bid, Theobid, Theoclear, Theo-Dur, Uniphyl).
This list is not complete and there may be other drugs that can interact with Prevacid. Tell your doctor about all the prescription and over-the-counter medications you use. This includes vitamins, minerals, herbal products, and drugs prescribed by other doctors. Do not start using a new medication without telling your doctor.
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Where can I get more information? Your pharmacist can provide more information about Prevacid.
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What does my medication look like? Lansoprazole is available with a prescription under the brand name Prevacid. Other brand or generic formulations may also be available. Ask your pharmacist any questions you have about this medication, especially if it is new to you. Prevacid 15 mg - pink/green, delayed-release capsules Prevacid 30 mg - pink/black, delayed-release capsules Prevacid for Delayed-Release Oral Suspension-white to pale brownish granules Prevacid SoluTab Delayed-Release Orally Disintegrating Tablets - white to yellowish tablets with orange or brown specks
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.
Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist. |