近日，美国FDA批准即释型质子泵抑制剂ZEGERID（omeprazole/sodium bicarbonate）的新药申请，Zegerid胶囊用于治疗胃酸过多、胃食管反流病、糜烂性食道炎（4-8周短期治疗，经内窥镜检查）、良性活动性胃溃疡和活动性十二指肠溃疡等疾病。
ZEGERID在空腹（至少餐前1小时）服用，一天只需服用一次，能迅速达到最大血药浓度（约30分钟以内），强效控制胃酸，其中抗酸剂碳酸氢钠能提高胃内pH值从而保护质子泵抑制剂奥美拉唑被酸降解。
目前上市的ZEGERID有口服混悬剂和胶囊两个剂型。ZEGERID胶囊分奥美拉唑/碳酸氢钠：40mg/1100mg和20mg/1100mg两个规格。
批准日期：2006年2月27日 公司：桑塔茹斯（Santarus）
ZEGERID（奥美拉唑/碳酸氢钠[omeprazole/sodium bicarbonate]）粉末用于口服混悬液
ZEGERID（奥美拉唑/碳酸氢钠[omeprazole/sodium bicarbonate]）胶囊用于口服
美国最初批准：2004年
最近的重大变化
警告和注意事项，基底腺体息肉：06/2018
作用机制
奥美拉唑属于一类抗分泌化合物，取代苯并咪唑，不具有抗胆碱能或H2组胺拮抗特性，但通过特异性抑制胃壁细胞分泌表面的H+/K+ATP酶系统来抑制胃酸分泌。因为这种酶系统被认为是胃粘膜内的酸（质子）泵，所以奥美拉唑已被定性为胃酸泵抑制剂，因为它阻断了酸生成的最后步骤。这种作用与剂量有关，并且不管刺激如何都会导致基础和受刺激的酸分泌受到抑制。动物研究表明，在血浆迅速消失后，可在胃粘膜内发现奥美拉唑一天或更长时间。
奥美拉唑是酸不稳定的，因此被胃酸迅速降解。ZEGERID胶囊和口服悬浮液粉末是含有碳酸氢钠的速释制剂，可提高胃液pH值，从而保护奥美拉唑免受酸降解。
适应症和用法
ZEGERID是一种质子泵抑制剂（PPI），适用于：
•短期治疗活动性十二指肠溃疡。
•短期治疗活动性良性胃溃疡。
•治疗胃食管反流病（GERD）。
•维持糜烂性食管炎的愈合。
•降低重症患者上消化道出血的风险。
ZEGERID在儿科患者（<18岁）中的安全性和有效性尚未确定。
剂量和给药
•活动性十二指肠溃疡的短期治疗：每天一次，每次20毫克，持续4周（一些患者可能需要额外的4周治疗。
•胃溃疡：每日一次40毫克，持续4-8周。
•胃食管反流病（GERD）
•症状性GERD（无食管糜烂）：每日20mg，最长4周
•糜烂性食管炎：每日一次20毫克，持续4-8周
•维持糜烂性食管炎的治疗：每日20毫克*
•降低重症患者上消化道出血的风险:(仅40mg口服混悬液）40mg，最初接着40mg，6-8小时后，每天40mg，持续14天
*研究了12个月
剂量形式和强度
•ZEGERID可作为胶囊和口服悬浮液的粉末，含量为20毫克和40毫克。
禁忌症
•已知对制剂的任何组分过敏。
警告和注意事项
•胃部恶性：在成人中，症状反应并不排除胃恶性肿瘤的存在。考虑额外的后续和诊断测试。
•在服用PPI的患者中观察到急性间质性肾炎。
•缓冲液含量：含有碳酸氢钠。
•PPI治疗可能与艰难梭菌相关性腹泻的风险增加有关。
•骨折：长期和多次每日剂量PPI治疗可能与骨质疏松相关的髋部，腕部或脊柱骨折风险增加有关。
•皮肤和系统性红斑狼疮：主要是皮肤;现有疾病的新发作或恶化;停止ZEGERID并咨询专家进行评估。
•氰钴胺素（维生素B-12）缺乏症：每日长期使用（例如，超过3年）可能导致吸收不良或氰钴胺素缺乏。
•长期使用PPI治疗很少报告低镁血症。
•避免同时使用ZEGERID与圣约翰草或利福平，因为奥美拉唑浓度可能会降低。
•与神经内分泌肿瘤诊断调查的相互作用：胃内pH升高可能导致高胃泌素血症和肠嗜铬细胞样细胞增生，并增加嗜铬粒蛋白A水平，这可能会干扰神经内分泌肿瘤的诊断调查。
•与甲氨蝶呤的相互作用：与PPI同时使用可能会升高和/或延长甲氨蝶呤和/或其代谢物的血清浓度，可能导致毒性。对于高剂量甲氨蝶呤给药，考虑暂时停用ZEGERID。
•基底腺体息肉：长期使用会增加风险，尤其是超过一年。使用最短的治疗时间。
不良反应
最常见的不良反应（发生率≥2％）是：头痛，腹痛，恶心，腹泻，呕吐和胃肠胀气。
要报告疑似不良反应，请致电1-800-321-4576联系Valeant Pharmaceuticals North America LLC或1-800-FDA-1088或WWW.FDA.GOV/MEDWATCH联系FDA。
药物相互作用
•可能会干扰胃液pH值影响生物利用度的药物（如酮康唑，氨苄西林酯，铁盐，厄洛替尼，地高辛和霉酚酸酯）。
•由细胞色素P450代谢的药物（例如，地西泮，华法林，苯妥英，环孢菌素，双硫仑，苯二氮卓类）：ZEGERID可延长其消除。使用ZEGERID进行监测以确定是否需要进行可能的剂量调整。
•伴随质子泵抑制剂和华法林治疗的患者可能需要监测INR和凝血酶原时间的增加。
•伏立康唑：可能会增加奥美拉唑的血药浓度。
•沙奎那韦：ZEGERID可增加沙奎那韦的血浆水平。
•ZEGERID可降低阿扎那韦和奈非那韦的血药浓度。
•氯吡格雷：ZEGERID可降低氯吡格雷活性代谢物的暴露。
•他克莫司：ZEGERID可能会增加他克莫司的血清水平。
用于特定人群
•怀孕：根据动物数据，可能会导致胎儿伤害。
•尚未确定ZEGERID在18岁以下儿童患者中的安全性和有效性。
•肝功能损害：考虑减少剂量，特别是维持糜烂性食管炎的愈合。
包装提供/存储和处理
ZEGERID 20毫克胶囊：每个不透明的硬明胶，白色胶囊，印有Santarus标志和“20”，含有20毫克奥美拉唑和1,100毫克碳酸氢钠。
NDC 68012-102-30瓶装30粒胶囊
ZEGERID 40毫克胶囊：每个不透明的硬明胶，深蓝色和白色胶囊，印有Santarus标志和“40”，含有40毫克奥美拉唑和1,100毫克碳酸氢钠。
NDC 68012-104-30瓶装30粒胶囊
ZEGERID口服悬浮液粉末是一种白色调味粉末，以单位剂量包装包装。 每个包含20毫克或40毫克奥美拉唑和1,680毫克碳酸氢钠。
NDC 68012-052-30纸箱30：20mg单位剂量包装
NDC 68012-054-30纸箱30：40mg单位剂量包装
存储
储存在25°C（77°F）; 允许偏移15°至30°C（59°至86°F）[见USP受控室温]。
保持容器密闭。 避免光照，避免潮湿。
完整说明书附件：https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cd6868b9-5824-442b-8d65-4db29ecb70a4 
Indication for ZEGERID
ZEGERID® (omeprazole/sodium bicarbonate) is a prescription medicine called a proton pump inhibitor (PPI). ZEGERID reduces the amount of acid in your stomach.
ZEGERID is used in adults for:
•short term to heal ulcers in the first part of the small bowel (duodenal ulcers).
•short term healing of stomach ulcers.
•treatment of heartburn and other symptoms that happen with gastroesophageal reflux disease (GERD).
•healing of acid-related damage to the lining of the esophagus (called erosive esophagitis or EE).
•maintenance of healing of the esophagus. It is not known if ZEGERID is safe and effective if used longer than 12 months (1 year).
•reduction of the risk of stomach bleeding in critically ill people.
Important Safety Information about ZEGERID
Do not take ZEGERID® (omeprazole/sodium bicarbonate) if you are allergic to omeprazole or any of the other ingredients in ZEGERID, or are allergic to any other proton pump inhibitor (PPI) medicine.
Before you take ZEGERID, tell your doctor if you have been told that you have low magnesium, calcium, or potassium levels in your blood, liver problems, heart failure, or have Bartter’s syndrome (a rare kidney disorder).
Tell your doctor about all the medicines you take, including prescription and non-prescription drugs, anti-cancer drugs, vitamins and herbal supplements. ZEGERID may affect how other medicines work, and other medicines may affect how ZEGERID works. This can cause serious side effects. Be sure to tell your doctor if you are taking:
•Mycophenolate mofetil (Cellcept)
•diazepam (Valium®)
•warfarin (Coumadin® Jantoven)
•phenytoin (Dilantin®)
•cyclosporine (Gengraf, Neoral, Sandimmune)
•disulfiram (Antabuse®)
•a benzodiazepine medicine
•ketoconazole (Nizoral®)
•an antibiotic that contains ampicillin
•products that contain irondigoxin (Lanoxin®)
•voriconazole (Vfend®)
•atazanavir (Reyataz®)
•nelfinavir (Viracept®)
•tacrolimus (Prograf®)
•saquinavir (Fortovase®)
•clarithromycin (Biaxin®, Biaxin XL)
•clopidogrel (Plavix®)
•St. John's Wort (Hypericum perforatum)
•rifampin (Rifater, Rifamate, Rimactane, Rifadin)
•methotrexate
Do not substitute two 20 mg capsules for one 40 mg capsule of ZEGERID because you will receive twice the amount of sodium bicarbonate. Do not substitute two 20 mg packets for one 40 mg packet of ZEGERID Powder for Oral Suspension because you will receive twice the amount of sodium bicarbonate.
Taking ZEGERID for a long period of time may increase the risk of inflammation to your stomach lining (atrophic gastritis). You may or may not have symptoms. Tell your doctor if you have stomach pain, nausea, vomiting, or weight loss.
ZEGERID may cause vitamin B-12 deficiency. ZEGERID reduces the amount of acid in your stomach. Stomach acid is needed to absorb vitamin B-12 properly. Talk with your doctor about the possibility of vitamin B-12 deficiency if you have been on ZEGERID for a long time (more than 3 years).
Your doctor may stop ZEGERID if you have low magnesium levels in your body. This problem can be serious. Low magnesium can happen in some people who take a proton pump inhibitor medicine for at least 3 months. If low magnesium levels happen, it is usually after a year of treatment. You may or may not have symptoms of low magnesium.
People who are taking multiple daily doses of proton pump inhibitor medicines for a long period of time may have an increased risk of fractures of the hip, wrist, or spine.
If you are on a low-sodium diet or at risk of developing congestive heart failure (CHF), you and your doctor should decide if you will take ZEGERID.
It is not known if ZEGERID is safe and effective in children and adolescents less than 18 years of age.
If you are pregnant, planning to become pregnant, or nursing, talk to your healthcare provider before taking ZEGERID. It is unknown if ZEGERID can harm your unborn baby.
The most common side effects with ZEGERID include headache, abdominal pain, nausea, diarrhea, vomiting, and gas. However, tell your doctor right away if you develop the following symptoms: seizures, dizziness, abnormal or fast heartbeat, jitteriness, jerking movements or shaking (tremors), muscle weakness, spasms of the hands and feet, cramps or muscle aches, spasm of the voice box.
You are encouraged to report negative side effects of prescription drugs to the FDA. Visit www.fda.gov/medwatch/ or call 1-800-FDA-1088.
ZEGERID ® (omeprazole / sodium bicarbonate) is the first and only immediate-release oral PPIs. Santarus has received FDA approval of ZEGERID for Capsules® and Powder for Oral Suspension dosage forms. Santarus obtain FDA approval of ZEGERID ® capsules and bulk oral suspension dosage forms. These products are intended to treat or prevent a variety of upper GI diseases and disorders. The purpose of these products is the treatment or prevention of various diseases and upper gastrointestinal diseases. PPIs are used widely due to their potent acid suppression, demonstrated safety and once-a-day dosing. The producer price index is widely used due to its strong acid suppression, indicating that safety and once-daily dose.
Santarus received FDA approval for ZEGERID Capsules in February of 2006, ZEGERID Powder for Oral Suspension 40 mg in December of 2004, and ZEGERID Powder for Oral Suspension 20 mg in June of 2004. Santarus received FDA approval ZEGERID capsules in February 2006, ZEGERID Powder for Oral Suspension 40 mg, in December 2004, and ZEGERID Powder for Oral Suspension 20 mg in June 2004.
ZEGERID Capsules and Powder for Oral Suspension dosage forms are immediate-release formulations, providing rapid absorption of omeprazole and continued acid control. ZEGERID capsules and powder for oral suspension dosage form is an immediate release formulation of omeprazole and continue to be able to quickly absorb acid control . The immediate-release formulation of ZEGERID is unique. ZEGERID immediate release formulation is unique. Except for ZEGERID, all other oral PPIs are delayed release, and require enteric coatings to protect against acid degradation. In addition ZEGERID, all other oral PPIs are delayed release, and asked intestinal coating to prevent acid degradation. These enteric coatings delay absorption and initial acid suppression. These coatings delay intestinal absorption and initial acid suppression.
Santarus has licensed exclusive, worldwide rights to patents and patent applications covering specific formulations of immediate-release PPIs and antacids for treating upper GI diseases and disorders from the University of Missouri. Santarus exclusive license in the world, enjoy specific formulation patents and patent applications related to the the immediate release of the University of gastrointestinal diseases and disorders of Missouri on price index and producer antacid treatment. The initially issued US patents on which our ZEGERID products are based, expire in U.S. Patent ZEGERID July 2016. Originally released on the basis of our products, expires in July 2016.
ZEGERID (omeprazole / sodium bicarbonate) is indicated for: ZEGERID (omeprazole / sodium bicarbonate) is applicable to:
Short-term treatment of active duodenal ulcer short-term treatment of active duodenal ulcer
Short-term treatment (4-8 weeks) of active benign gastric ulcer short-term treatment (4-8 weeks) of active benign gastric ulcer
Heartburn and other symptoms associated with gastroesophageal reflux disease (GERD) heartburn and other symptoms associated with gastroesophageal reflux disease (GERD)
Short-term treatment (4-8 weeks) of erosive esophagitis which has been diagnosed in endoscopy short-term treatment (4-8 weeks) of erosive esophagitis had endoscopic diagnosis
Maintenance of healing of erosive esophagitis (controlled studies do not extend beyond 12 months) to maintain healing of erosive esophagitis (controlled studies no more than 12 months)
Reduction of critically ill patients on the risk of upper GI bleeding in critically ill patients (powder for oral suspension only) to reduce the risk of gastrointestinal bleeding (powder for oral suspension only)
On ZEGERID Powder for Oral Suspension 40 mg / 1680 mg is the only FDA approved PPI for reduction of risk of upper GI bleeding in critically ill patients. ZEGERID Powder for Oral Suspension 40 mg / 1680 mg is the only FDA approved to reduce the risk of prices upper gastrointestinal bleeding in critically ill patients.
Product Description Product Description
ZEGERID® (omeprazole / sodium bicarbonate) contains omeprazole, a proton pump inhibitor (PPI), and sodium bicarbonate, an antacid, which raises the gastric pH and thus protects omeprazole from acid degradation. ZEGERID ® (omeprazole / sodium bicarbonate ) contains omeprazole, a proton pump inhibitor (PPI), and sodium bicarbonate antacids, which raises the gastric pH, thereby protecting the omeprazole acid degradation.
Indications and Dosing for ZEGERID flag and ingredients ZEGERID
ZEGERID is indicated for heartburn and other symptoms associated with gastroesophageal reflux disease (GERD) (20 mg); for the short-term treatment (4-8 weeks) of erosive esophagitis diagnosed by endoscopy (20 mg); for maintenance of healing of erosive esophagitis (20 mg) (controlled studies do not extend beyond 12 months); for short-term treatment (4-8 weeks) of active duodenal ulcer (20 mg); for short-term treatment (4-8 weeks) of active benign gastric ulcer (40 mg); and for reduction of risk of upper gastrointestinal bleeding in critically ill patients (only powder for oral suspension 40 mg / 1680 mg; use beyond 14 days has not been eva luated). ZEGERID for heartburn and other symptoms and gastroesophageal reflux disease (GERD) (20 mg) for short-term treatment (4-8 weeks) of erosive esophagitis endoscopic diagnosis (20 mg); for maintenance of healing of erosive esophagitis (20 mg) (Control Study no more than 12 months); the short-term treatment (4-8 weeks) of active duodenal ulcer (20 mg) for short-term treatment (4-8 weeks) of active benign gastric ulcer (40 mg) ; on critically ill patients and reduce the risk of gastrointestinal bleeding (only powder for oral suspension 40 mg / 1680 mg; using more than 14 days have not been eva luated).
Important Safety Information about ZEGERID important safety information ZEGERID
The most frequently reported adverse events with ZEGERID are headache, diarrhea, and abdominal pain. ZEGERID adverse events most frequently reported were headache, diarrhea, abdominal pain. In 178 critically ill patients treated with ZEGERID Powder for Oral Suspension, adverse events generally reflected the serious, underlying medical condition of the patients, but some adverse events occurred with more frequency in patients treated with ZEGERID Powder for Oral Suspension than in those treated with the comparator (acid-controlling) drug. 178 个 critically ill patients ZEGERID Powder for Oral Suspension, adverse events generally reflected the serious, underlying medical conditions of patients, but some of the frequency of adverse events in patients with more ZEGERID Powder treatment than those who compare oral suspension (acid control) of the drug. For more information about these and other events, please see Table 13 of the full Prescribing Information. For more information on these and other activities, see Table 13 of the full prescribing information. Symptomatic response to therapy does not preclude the presence of gastric malignancy. Symptomatic response to therapy does not preclude the presence of gastric malignancy. Atrophic gastritis has been noted occasionally in gastric corpus biopsies from patients treated long term with omeprazole. Atrophic gastritis has been noted occasionally in gastric corpus biopsies from the patients with long-term omeprazole.
ZEGERID Capsules contain 304 mg of sodium per dose. ZEGERID capsules containing 304 milligrams of sodium per dose. ZEGERID Powder for Oral Suspension contains 460 mg of sodium per dose. ZEGERID Powder for Oral Suspension contains 460 mg of sodium per dose. This should be taken into consideration for patients on a sodium-restricted diet. It should take into account the patient's sodium-restricted diet.
Sodium bicarbonate is contraindicated in patients with metabolic alkalosis and hypocalcemia. Sodium bicarbonate in patients with metabolic alkalosis and hypocalcemia. ZEGERID is contraindicated in any part of the patients with known hypersensitivity to any component of the formulation. Patients ZEGERID known allergy formulation.
Since both 20 mg and 40 mg ZEGERID contain the same amount of sodium bicarbonate (1100 mg in capsules, 1680 mg in packets of powder for oral suspension), two 20 mg capsules are not equivalent to, and should not be substituted for, one 40 mg capsule, and two 20 mg packets are not equivalent to, and should not be substituted for, one 40 mg packet. Because both 20 mg and 40 mg ZEGERID contain the same amount of sodium bicarbonate (1100 mg capsules, 1680 mg packet powder for oral suspension), two 20 mg capsules is not equal to, and should not be substituted, a 40 mg capsule, and the two packages is not equal to 20 mg, and should not be substituted, a pack 40 mg.