خواص دارویی و گیاهی
اس امپرازول Esomeprazole
قرص های 20 و 40 میلی گرمی
نکسیوم حاوی دارویی است به نام اس امپرازول که متعلق به گروه دارویی مهارکننده های پمپ پروتون (ترشح اسید) می باشد که موجب کاهش تولید اسید معده می شوند.
نکسیوم برای درمان موارد زیر به کار می رود:
قرص nexium چیست
در بزرگسالان و کودکان بالای 12 سال
در بزرگسالان
در صورت وجود هر یک از موارد زیر از مصرف دارو خودداری نمایید:
مانند هر دارویی مصرف نکسیوم نیز ممکن است تعدادی عارضه جانبی در پی داشته باشد، اگرچه این عوارض در تمام افراد بروز نمی کنند.
در صورت بروز هر یک از عوارض زیر مصرف نکسیوم را متوقف و فوراً به پزشک مراجعه نمایید:
عوارض ذکر شده نادر هستند و در کمتر از یک مورد به ازای هر هزار نفر بروز می کنند.
محتویات نکسیوم:
ماده فعال در این دارو اس امپرازول می باشد. قرص های نکسیوم مقاوم به اسید معده در دو شکل 20 و 40 میلی گرمی در دسترس هستند.
نکسیوم (Nexium) نام تجاری داروی (اسموپرازول) , یک مهارکننده پمپ پروتونی است که مقدار اسید تولید شده در معده را کاهش می‌دهد.
قرص نکسیوم برای درمان علائم بیماری ریفلاکس معده (GERD) و سایر وضعیت‌های دیگر که به خاطر تولید بیش‌ازحد اسید معده مانند سندرم زولینگر- الیسون رخ می دهد و همچنین برای پیشگیری از التهاب فرسایشی مری که ناشی از اسید معده مورد استفاده قرار می‌گیرد.
این دارو با مهار انتخابی پمپ k/h- ATPase در سلول های پاریتال معده، از ترشح اسید جلوگیری میکند.
قرص nexium چیست
فارماکوکینتیک: فراهمی زیستی دارو 90 % می باشد و غذا باعث کاهش جذب آن می گردد. اس- امپرازول تا 97 % به پروتئین های پلاسما باند می شود. از طریق سیستم آنزیمی سیتوکروم P450 در کبد به متابولیتهای غیر فعال تبدیل میگردد.
دفع این دارو عمدتا از راه ادرار میباشد که حدود 80 ٪ آن به صورت متابولیت غیرفعال و کمتر از 1% دارو بصورت دست نخورده دفع میگردد، حدود 20 ٪ دارو نیز از راه مدفوع دفع میشود. نیمه عمر دارو بین 1 تا 1.5 ساعت می باشد.
ازوفاژیت اروزیو، ریفلاکس معده به مری علامت دار ، عفونت هلیکوباکتر پیلوری (کاهش خطر عود زخم دوازدهه)، کاهش خطر زخم معده ناشی از مصرف ضدالتهابهای غیراستروئیدی، سندروم زولینجر- الیسون
بزرگسالان: ۴۰ میلی گرم همراه 1 گرم آموکسی سیلین و ۵۰۰ میلی گرم کلاریترومایسین هر ۱۲ ساعت به مدت ۱۰ روز
بزرگسالان: ۲۰ تا ۴۰ میلی گرم به مدت حداکثر 6 ماه
بزرگسالان: ۴۰ میلی گرم دو بار در روز، دوز دارو بر اساس شرایط بیمار تنظیم می شود و ممکن است تا ۲۴۰ میلی گرم در روز هم افزایش یابد.
نکسیوم را باید یک ساعت قبل از صبحانه میل کرد.
در صورتی که بیمار قادر به بلع کپسول نباشد، می تواند محتویات کپسول را با آب سیب یا پرتقال یا در غذای نرم مخلوط نموده و بلافاصله میل کند. لازم به ذکر است که گرانولهای این دارو به علت اینکه باید در محیط روده باز شوند، داخل مایعات خوراکی، انحلال ناپذیر بوده و به صورت ذرات معلق در مایعات باقی میماند و باید به همین صورت مصرف گردد.
نکسیوم را می‌توان از طریق لوله تغذیه بینی (NG) استفاده کرد. کپسول را بازکنید و دارو را به یک سرنگ با ظرفیت ۶۰ میلی‌لیتر اضافه کنید. سپس آن را با ۵۰ میلی‌لیتر آب مخلوط‌کنید. محلول پیستون را داخل سرنگ قرار داده و مخلوط را کاملاً تکان دهید.
اطمینان حاصل کنید که هیچ دانه گرانولی از دارو در نوک سرنگ وجود ندارد. سرنگ را به لوله NG وصل کرده و میله پیستونی را پایین بیاورید تا سرنگ را داخل لوله قرار دهید. سپس لوله را با آب بیشتر همراه کنید تا محتویات را بشوید.
اگر از این دارو برای مدت بیش از ۳ سال استفاده کنید، ممکن است این میزان مصرف در شما کمبود ویتامین B12 ایجاد کند. در مورد چگونگی مدیریت این وضعیت اگر در شما رو به وخیم شدن است، با پزشک خود صحبت کنید.
اگر علائم شما بهبود نیافته باشد یا در صورت استفاده از این دارو بدتر شوند، با پزشک خود تماس بگیرید.
نکسیوم می‌تواند نتایج غیرمعمولی را در آزمایش‌های پزشکی خاصی ایجاد کند و ممکن است لازم باشد از مصرف دارو برای مدت کوتاهی قبل از آزمایش خودداری کنید. با هر پزشکی که شمارا تحت درمان قرار می‌دهد، در مورد اینکه شما از این دارو استفاده می‌کنید صحبت کنید.
مصرف در دوران بارداری و شیردهی FDA رده بندی بارداری : گروه B
انتظار نمی رود که نکسیوم برای کودک شما مضر باشد٬ اما اگر باردار هستید یا قصد بچه دار شدن را دارید حتما در استفاده از این دارو با پزشک خود مشورت نمایید.
معلوم نیست که آیا نکسیوم یا اسموپرازول از طریق خون به شیر مادر وارد می شود و یا می تواند به کودک شیرخوار آسیب برساند. اما اگر شما نوزاد شیرخوار دارید حتما پزشک خود را در مصرف این دارو مطلع سازید.
این دارو به مقدار زیادی به پروتئین‌های پلاسما پیوند می‌یابد، بنابراین نمی‌توان دارو را با دیالیز برداشت نمودو درمان حمایتی است.
برای اینکه مطمئن شوید نکسیوم برای شما بی خطر است٬ در مورد سابقه ها و حساسیت های زیر حتما پزشک خود را در جریان قرار دهید :
چه اتفاقی می افتد اگر شما یک دوز از این دارو را فراموش کنید؟
به محض اینکه شما دوز فراموش شده را به یاد آوردید، آن را مصرف کنید. اگر تقریباً موقع نوبت بعدی مصرف دوز بعدی است، از مصرف دوز فراموش شده اجتناب کنید. برای جبران دوز از دست رفته قبلی در دوز بعدی از داروی اضافه استفاده نکنید.
اگر نکسیوم را بیش از حد مصرف کنید، چه اتفاقی می افتد؟
با مراقبت‌های پزشکی اورژانس و یا کمک‌های اضطراری برای مسمومیت، تماس بگیرید.
این دارو می تواند اسهال را ایجاد کند که ممکن است نشانه عفونتی جدید در بدن شما باشد. اگر اسهال آبکی یا خونریزی دارید، با پزشک خود تماس بگیرید. از داروهای ضد اسهال استفاده نکنید، مگر اینکه پزشک شما به شما توصیه کند.
اگر موارد زیر را مشاهده کردید به پزشک خود اطلاع دهید:
قرص nexium چیست
بیشتر بخوانید:
فواید مصرف مکمل گیاهی رافویه برای مشکلات معده
9دلیل قانع کننده برای مصرف روغن زیتون با معده خالی
علائم و نشانه های میکروب هلیکوباکتری معده و درمان این بیماری
© تمامی حقوق این سایت برای شرکت آرادپرداز محفوظ است ؛ هر گونه استفاده از مطالب دلگرم با رعایت شرایط بازنشر امکان پذیر است.
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قرص nexium چیست
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Brand name
Nexium Hp7
Active ingredient
Clarithromycin; Esomeprazole; Amoxicillin
Schedule
S4
Please read this leaflet carefully before you start using Nexium Hp7 [8944].
This leaflet answers some of the common questions people ask about NEXIUM Hp7. It does not contain all the available information about NEXIUM Hp7.
It does not take the place of talking to your doctor or pharmacist.
All medicines have risks and benefits. Your doctor will have weighed the risks of you taking NEXIUM Hp7 against the benefits they expect it will have for you.
If you have any concerns about taking these medicines, ask your doctor or pharmacist.
قرص nexium چیست
Keep this leaflet with the medicines.
You may need to read it again.
NEXIUM Hp7 is a combination pack, which contains three different medicines. When taken together in the right doses, they will kill the bacteria in your stomach called Helicobacter pylori and let your peptic ulcer heal.
Depending on the position of the ulcer it is called a gastric or duodenal ulcer. A gastric ulcer occurs in the stomach. A duodenal ulcer occurs in the duodenum which is the tube leading out from the stomach.
Most people who have a peptic ulcer also have a bacterium called Helicobacter pylori in their stomach. If the bacteria are killed it is unlikely that your ulcer will come back.
NEXIUM is the brand name of esomeprazole (E), and it is given with amoxicillin (A), brand name Amoxil and clarithromycin (C), brand name Klacid. Amoxil and Klacid are both types of antibiotic.
NEXIUM is a type of medicine called a proton-pump inhibitor.
NEXIUM works by decreasing the amount of acid made by the stomach, to give relief of symptoms and allow healing to take place. This does not stop food being digested in the normal way.
Amoxicillin and clarithromycin are both antibiotics that help kill Helicobacter pylori. NEXIUM also helps kill the bacteria. When all three are taken together they are more effective than taken one or two at a time. It is possible that the antibiotics may not always kill Helicobacter pylori.
Ask your doctor if you have any questions about why this medicine has been prescribed for you.
Your doctor may prescribe this medicine for another use.
There is no evidence that NEXIUM Hp7 is addictive.
This medicine is available only with a doctor’s prescription.
Do not take NEXIUM Hp7 if you have an allergy to:
Some of the symptoms of an allergic reaction may include shortness of breath, wheezing or difficulty breathing; swelling of the face, lips, tongue or other parts of the body; rash, itching or hives on the skin.
Do not take NEXIUM Hp7 if you are taking any of the following medicines:
Please check with your doctor or pharmacist if you are taking any of these medicines. These medicines will be affected by the medicines in NEXIUM Hp7 and it is more likely you will get side effects.
Do not take NEXIUM Hp7 if you have a history of heart conditions such as QT prolongation or ventricular cardiac arrhythmia.
Do not take NEXIUM Hp7 if you have low potassium levels.
Do not take NEXIUM Hp7 if you have both liver and kidney problems.
NEXIUM Hp7 is not recommended for use in children.
There is no information about the use of NEXIUM Hp7 in children.
Do not take this medicine after the use by (expiry) date printed on the pack or if the packaging is torn or shows signs of tampering
If it has expired or is damaged, return it to your pharmacist for disposal.
If you are not sure whether you should start taking this medicine, talk to your doctor.
Tell your doctor if you have allergies to any other medicines, foods, preservatives or dyes.
You must tell your doctor if you have:
Tell your doctor if you are pregnant or plan to be pregnant, are breast-feeding or plan to breast-feed.
It is not known if it is safe for you to take NEXIUM Hp7 if you are pregnant. The medicines in NEXIUM Hp7 may affect the developing baby.
Your baby can take in all the medicines in NEXIUM Hp7 from breast milk if you are breast-feeding. NEXIUM Hp7 is not recommended when breast-feeding.
Your doctor can discuss with you the risks and benefits of using NEXIUM Hp7 if you are pregnant or breast-feeding.
If you have not told your doctor about any of the above, tell them before you start taking NEXIUM Hp7.
Do not take NEXIUM Hp7 if you are taking the following medicines:
Tell your doctor if you are taking any other medicines, including any that you buy without a prescription from a pharmacy, supermarket or health food shop.
Some medicines and NEXIUM Hp7 may interfere with each other. These include:
These medicines may affect NEXIUM Hp7 or may affect how well it works. You may need different amounts of your medicines or you may need to take different medicines.
Your doctor and pharmacist have more information on medicines to be careful with or avoid while taking this medicine.
If you have not told your doctor about any of these things, tell them before you take any NEXIUM Hp7.
Follow all directions given to you by your doctor or pharmacist carefully.
They may differ from the information contained in this leaflet.
If you do not understand the instructions on the box, ask your doctor or pharmacist for help.
There are three different medicines in NEXIUM Hp7. It is very important that you take NEXIUM Hp7 exactly as follows:
NEXIUM (esomeprazole) = E
Take one 20 mg tablet in the morning and at night.
Amoxil (amoxicillin) = A
Take two 500 mg capsules in the morning and at night.
Klacid (clarithromycin) = C
Take one 500 mg tablet in the morning and at night.
Morning1 E, 2 A, 1 C
Night1 E, 2 A, 1 C
Swallow the NEXIUM tablets whole with a glass of water. For patients with swallowing difficulties, the tablet can be placed in half a glass of non-carbonated water (mineral water is not suitable). The tablet may be gently mixed and care should be taken not to crush the tablet. Rinse the glass with half a glass of fluid and drink.
NEXIUM tablets may also be administered, dispersed in non-carbonated water, through a gastric tube.
Do not crush or chew the tablets as they will not work properly.
Take medicines in NEXIUM Hp7 during or after meals.
Continue taking the capsules and tablets until you finish the course or until your doctor tells you to stop.
If you do not complete the full course prescribed by your doctor, the Helicobacter pylori may not clear completely and your symptoms may return.
Tell your doctor if your symptoms return.
It is possible that the antibiotics may not kill Helicobacter pylori. You may need treatment with more antibiotics.
If you forget to take any of the medicines in NEXIUM Hp7 take it as soon as you remember, as long as it is more than four hours before the next dose of that medicine is due.
Do not take a double dose to make up for any dose that you miss.
If you are unsure what to do ask your doctor or pharmacist.
If you have trouble remembering when to take your medicine, ask your pharmacist for some hints.
Immediately telephone your doctor, the Poisons Information Centre (13 11 26) or go to Accident and Emergency at your nearest hospital if you think that you or anyone else may have taken too much NEXIUM Hp7 even if there are no signs of discomfort or poisoning.
If you take too much NEXIUM Hp7 you may vomit and have severe stomach problems.
Take NEXIUM Hp7 exactly as your doctor has prescribed.
If you are about to be started on any new medicine, tell your doctor and pharmacist that you are taking NEXIUM Hp7.
If you become pregnant while you are taking NEXIUM Hp7, tell your doctor.
If you get severe diarrhoea, tell your doctor, pharmacist or nurse immediately. Do this even if it occurs several weeks after NEXIUM Hp7 has been stopped.
Diarrhoea may mean that you have a serious condition affecting your bowel. You may need urgent medical care. Do not take medicine to stop the diarrhoea without first checking with your doctor.
If you get a sore, white mouth or tongue while taking, or soon after stopping NEXIUM Hp7, tell your doctor. Also tell your doctor if you get vaginal itching or discharge.
This may mean you have a fungal infection called thrush. Sometimes the use of NEXIUM Hp7 allows fungi to grow and the above symptoms to occur. NEXIUM Hp7 does not work against fungal infections.
Tell any other doctors, dentists and pharmacists who are treating you that you are taking NEXIUM Hp7.
If you need to have any medical tests while you are taking NEXIUM Hp7, tell your doctor.
It may affect the results of some tests.
Drink plenty of water or fluids while taking NEXIUM Hp7
Do not take NEXIUM Hp7 to treat any other complaints unless your doctor tells you to.
Do not stop taking NEXIUM Hp7, or change any of the doses, unless you have discussed it with your doctor.
You need to take all the capsules and tablets in the pack for it to work properly. If you stop taking it, your ulcer may come back and be harder to treat next time.
Do not give NEXIUM Hp7 to anyone else, even if they have the same condition as you.
Be careful driving or operating machinery until you know how NEXIUM Hp7 affects you.
NEXIUM Hp7 may cause dizziness in some people. Make sure you know how you react to NEXIUM Hp7 before you do anything that may be dangerous if you are dizzy.
Please talk to your doctor or pharmacist about these possibilities if you think they may bother you.
Tell your doctor or pharmacist as soon as possible if you do not feel well while you are taking NEXIUM Hp7.
NEXIUM Hp7 helps most people with peptic ulcer and Helicobacter pylori infection, but it may have unwanted side effects in a few people.
All medicines can have side effects. Sometimes they are serious, most of the time they are not. You may need medical treatment if you get some of the side effects.
Ask your doctor or pharmacist to answer any questions you may have.
Tell your doctor if you notice any of the following and they worry you:
These side effects are usually mild.
Tell your doctor immediately or go to Accident and Emergency at your nearest hospital if you notice the following:
These may be serious side effects. You may need urgent medical attention.
If any of the following happen, stop taking NEXIUM Hp7 and tell your doctor immediately or go to Accident and Emergency at your nearest hospital:
Do not take any medicine to stop the diarrhoea unless advised by your doctor.
These are very serious side effects. If you have them, you may have had a serious reaction to one of the medicines in NEXIUM Hp7. You may need urgent medical attention or hospitalisation.
Tell your doctor if you notice anything else that is making you feel unwell.
Some people may get other side effects while taking NEXIUM Hp7.
Do not be alarmed by this list of possible side effects.
You may not experience any of them.
Keep the three medicines in NEXIUM Hp7 in their separate blisters until it is time to take them.
Keep it in a cool dry place where the temperature stays below 25°C.
Do not store it or any other medicine in the bathroom or near a sink.
Do not leave it in the car on hot days.
Heat and dampness can destroy some medicines.
Keep it where young children cannot reach it.
A locked cupboard at least one-and-a-half metres above the ground is a good place to store medicines.
If your doctor tells you to stop taking them, or the expiry date has passed, ask your pharmacist what to do with any medicine that is left over.
NEXIUM tablets 20 mg are light pink, oblong shaped, marked with ’20 mg’ on one side and ‘A/EH’ on the other side.
AMOXIL capsules 500 mg are red and yellow capsules, marked with ‘AM500’.
KLACID tablets 500 mg are pale yellow, oval, film coated tablets.
Each NEXIUM tablet contains esomeprazole 20 mg as the active ingredient, plus:
NEXIUM is provided in a blister wallet of 14 tablets.
The tablets are coloured with titanium dioxide (CI77891), iron oxide red (CI77491) and iron oxide yellow (CI77492).
Each AMOXIL capsule contains amoxicillin trihydrate 500 mg, plus:
Amoxil is provided in blister packs of 28 capsules.
The hard gelatin capsule is coloured with titanium dioxide (CI77891), iron oxide yellow (CI77492), erythrosine (CI45430), indigo carmine (CI73015) and Tek Product – Tek Print SW-0012- White Ink.
Each KLACID tablet contains clarithromycin 500 mg as the active ingredient, plus:
KLACID is provided in blister packs of 14 tablets.
NEXIUM Hp7 does not contain gluten.
AstraZeneca Pty Ltd
ABN 54 009 682 311
66 Talavera Road
Macquarie Park NSW 2113
Telephone: 1800 805 342
Aspen Pharmacare Australia Pty Ltd
34-36 Chandos Street
St Leonards NSW 2065
Mylan Health Pty Ltd
Level 1, 30 The Bond
30-34 Hickson Road
Millers Point NSW 2000
Australian Registration Number:
NEXIUM Hp7 – 281690
This leaflet was prepared in March 2019.
NEXIUM is a registered trade mark of the AstraZeneca group of companies.
AMOXIL is a registered trade mark of the Aspen Global Inc. group of companies.
KLACID is a registered trade mark of Mylan Health Pty Ltd.
Doc ID-002262136 V12.0
Published by MIMS May 2019
Reasonable care is taken to provide accurate information at the time of creation. This information is not intended as a substitute for medical advice and should not be exclusively relied on to manage or diagnose a medical condition. NPS MedicineWise disclaims all liability (including for negligence) for any loss, damage or injury resulting from reliance on or use of this information. Read our full disclaimer. This website uses cookies. Read our privacy policy.
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Esomeprazole, sold under the brand names Nexium among others,[1] is a medication which reduces stomach acid.[3] It is used to treat gastroesophageal reflux disease, peptic ulcer disease, and Zollinger–Ellison syndrome.[3][4] Effectiveness is similar to other proton pump inhibitors (PPIs).[5] It is taken by mouth or injection into a vein.[3]
Common side effects include headache, constipation, dry mouth, and abdominal pain.[3] Serious side effects may include angioedema, Clostridium difficile infection, and pneumonia.[3] Use in pregnancy appear to be safe while safety during breastfeeding is unclear.[6] Esomeprazole is the (S)-(−)-isomer of omeprazole.[3] It works by blocking H+/K+-ATPase in the parietal cells of the stomach.[3]
It was patented in 1993 and approved for medical use in 2000.[7] It is available as a generic medication and sold over the counter in a number of countries.[8][4] A month supply in the United Kingdom costs the NHS about £3 per month as of 2019.[4] In the United States the wholesale cost of this amount is about 10 USD.[9] In 2016 it was the 69th most prescribed medication in the United States with more than 11 million prescriptions.[10]
The primary uses of esomeprazole are gastroesophageal reflux disease, treatment and maintenance of erosive esophagitis, treatment of duodenal ulcers caused by H. pylori, prevention of gastric ulcers in those on chronic NSAID therapy, and treatment of gastrointestinal ulcers associated with Crohn’s disease.[11][12]
قرص nexium چیست
Gastroesophageal reflux disease (GERD) is a condition in which the digestive acid in the stomach comes in contact with the esophagus. The irritation caused by this disorder is known as heartburn. Long-term contact between gastric acids and the esophagus can cause permanent damage to the esophagus. Esomeprazole reduces the production of digestive acids, thus minimizing their effect on the esophagus.
Esomeprazole is combined with the antibiotics clarithromycin and amoxicillin (or metronidazole instead of amoxicillin in penicillin-hypersensitive patients) in a 10-day eradication triple therapy for Helicobacter pylori. Infection by H. pylori is a causative factor in the majority of peptic and duodenal ulcers.
A 2006 meta analysis concluded that compared to other proton pump inhibitors, esomeprazole confers a modest overall benefit in esophageal healing and symptom relief. When broken down by disease severity, the benefit of esomeprazole relative to other proton pump inhibitors was negligible in people with mild disease (number needed to treat 50), but appeared more in those with severe disease (number needed to treat 8).[13] A second meta analysis also found increases in erosive esophageal healing (>95% healing rate) when compared to standardized doses in broadly selected patient populations.[14] A 2017 study found esomeprazole to be among a number of effective doses of PPIs.[15]
Common side effects include headache, diarrhea, nausea, flatulence, decreased appetite, constipation, dry mouth, and abdominal pain. More severe side effects are severe allergic reactions, chest pain, dark urine, fast heartbeat, fever, paresthesia, persistent sore throat, severe stomach pain, unusual bruising or bleeding, unusual tiredness, and yellowing of the eyes or skin.[16]
Proton pump inhibitors may be associated with a greater risk of hip fractures[17] and Clostridium difficile-associated diarrhoea.[18] Patients are frequently administered the drugs in intensive care as a protective measure against ulcers, but this use is also associated with a 30% increase in occurrence of pneumonia.[19]
Long-term use of PPIs in patients treated for Helicobacter pylori has been shown to dramatically increase the risk of gastric cancer.[20]
Esomeprazole is a competitive inhibitor of the enzyme CYP2C19, and may therefore interact with drugs that depend on it for metabolism, such as diazepam and warfarin; the concentrations of these drugs may increase if they are used concomitantly with esomeprazole.[21] Conversely, clopidogrel (Plavix) is an inactive prodrug that partially depends on CYP2C19 for conversion to its active form; inhibition of CYP2C19 blocks the activation of clopidogrel, thus reducing its effects.[22][23]
Drugs that depend on stomach pH for absorption may interact with omeprazole; drugs that depend on an acidic environment (such as ketoconazole or atazanavir) will be poorly absorbed, whereas drugs that are broken down in acidic environments (such as erythromycin) will be absorbed to a greater extent than normal.[21]
Single 20 to 40 mg oral doses generally give rise to peak plasma esomeprazole concentrations of 0.5-1.0 mg/l within 1–4 hours, but after several days of once-daily administration, these levels may increase by about 50%. A 30-minute intravenous infusion of a similar dose usually produces peak plasma levels on the order of 1–3 mg/l. The drug is rapidly cleared from the body, largely by urinary excretion of pharmacologically inactive metabolites such as 5-hydroxymethylesomeprazole and 5-carboxyesomeprazole. Esomeprazole and its metabolites are analytically indistinguishable from omeprazole and the corresponding omeprazole metabolites unless chiral techniques are employed.[24]
Esomeprazole is available as delayed-release capsules in the United States or as delayed-release tablets in Australia, the United Kingdom, and Canada (containing esomeprazole magnesium) in strengths of 20 and 40 mg, as delayed-release capsules in the United States (containing esomeprazole strontium) in a 49.3 mg strength (delivering the equivalent of 40 mg of esomeprazole,[25] and as esomeprazole sodium for intravenous injection/infusion. Oral esomeprazole preparations are enteric-coated, due to the rapid degradation of the drug in the acidic conditions of the stomach. This is achieved by formulating capsules using the multiple-unit pellet system.
The combination naproxen/esomeprazole magnesium (brand name Vimovo) is used for the prevention of gastric ulcers associated with chronic NSAID therapy. Vimovo is available in two dosage strengths: 500/20 mg and 375/20 mg. Clinical trials of naproxen/esomeprazole demonstrated an incidence of GI ulcer in 24% of patients on naproxen (alone) versus 7% on naproxen/esomeprazole.[26] The FDA has added warnings to the label for Vimovo concerning acute interstitial nephritis and risk of kidney problems in some patients.[27]
Esomeprazole capsules, as well as Losec/Prilosec tablets, are formulated as a “multiple-unit pellet system” (MUPS). Essentially, the capsule consists of extremely small enteric-coated granules (pellets) of the esomeprazole formulation inside an outer shell. When the capsule is immersed in an aqueous solution, as happens when the capsule reaches the stomach, water enters the capsule by osmosis. The contents swell from water absorption, causing the shell to burst, and releasing the enteric-coated granules. For most patients, the multiple-unit pellet system is of no advantage over conventional enteric-coated preparations.[citation needed] Patients for whom the formulation is of benefit include those requiring nasogastric tube feeding and those with difficulty swallowing (dysphagia).[citation needed]
In 2010, AstraZeneca announced a co-promotion agreement with Daiichi Sankyo to distribute Nexium in Japan.[28] In September 2011, Nexium was approved for sale and was launched by Daiichi Sankyo in Japan.[29] Nexium is also sold online with a prescription via Nexium direct.[citation needed]
Between the launch of esomeprazole in 2001 and 2005, the drug netted AstraZeneca about $14.4 billion.[30]
There has been some controversy about AstraZeneca’s behaviour in creating, patenting, and marketing of the drug. Esomeprazole’s successful predecessor, omeprazole, is a mixture of two mirror-imaged molecules (esomeprazole which is the S-enantiomer, and R-omeprazole); critics said the company was trying to “evergreen” its omeprazole patent by patenting the pure esomeprazole and aggressively marketing to doctors that it is more effective than the mixture.[31]
Thomas A. Scully, head of the Centers for Medicare and Medicaid Services (CMS), also criticized AstraZeneca for their aggressive marketing of Nexium. At a conference of the American Medical Association (AMA), he said that Astra was using the new drug to overcharge consumers and insurance companies.[citation needed]
Generic versions of esomeprazole magnesium are available worldwide.[1] It is available over-the-counter under the brand name Nexium in the United States[32] and in the UK.[citation needed]