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نشرة الممارس الصحي نشرة معلومات المريض بالعربية نشرة معلومات المريض بالانجليزية صور الدواء بيانات الدواء
  SFDA PIL (Patient Information Leaflet (PIL) are under review by Saudi Food and Drug Authority)

Esomeprazole Sodium for Injection contains a medicine called Esomeprazole Sodium for Injection esomeprazole. This belongs to a group of medicines called ‘proton pump inhibitors’. They work by reducing the amount of acid that your stomach produces.

Esomeprazole Sodium for Injection is used for the short-term treatment of certain conditions, when you are unable to have treatment by mouth. It is used to treat the following conditions:

Adults

·       Gastroesophageal reflux disease’ (GERD). This is where acid from the stomach escapes into the gullet (the tube which connects your throat to your stomach) causing pain, inflammation and heartburn.

·       Stomach ulcers caused by medicines called NSAIDs (Non-Steroidal Anti-Inflammatory Drugs). Esomeprazole Sodium for Injection can also be used to stop stomach ulcers from forming if you are taking NSAIDs.

·       Prevention of rebleeding following therapeutic endoscopy for acute bleeding gastric or

 

duodenal ulcers.

 

Children and adolescents aged 1-18 years

 

·       ‘Gastroesophageal reflux disease’ (GERD). This is where acid  from  the stomach escapes into the gullet (the tube which connects your throat to your stomach) causing pain, inflammation and heartburn.

 


You must not be given Esomeprazole Sodium for Injection:

 

·       If you are allergic to Esomeprazole Sodium for Injection eprazole or any of the other ingredients of this medicine (listed in section 6).

·       If you are allergic to other proton pump inhibitor medicines (e.g. pantoprazole, lansoprazole, rabeprazole, omeprazole).

·       If you are taking a medicine containing nelfinavir (used to treat HIV infection).

 

You must not be given Esomeprazole Sodium for Injection if any of the above apply to you. If you are not sure, talk to your doctor or nurse before you are given this medicine.

Warnings and precautions

Talk to your doctor or nurse before you are given Esomeprazole Sodium for Injection if:

 

·       You have severe liver problems.

·       You have severe kidney problems.

·       You have ever had a skin reaction after treatment with a medicine similar to Esomeprazole Sodium for Injection that reduces stomach acid.

·       You are due to have a specific blood test (Chromogranin A).

·       Esomeprazole Sodium for Injection may hide the symptoms of other diseases. Therefore, if any of the following happen to you before you are given Esomeprazole Sodium for Injection or after you are given it, talk to your doctor straight away:

·       You lose a lot of weight for no reason and have problems swallowing.

·       You get stomach pain or indigestion.

·       You begin to vomit food or blood.

·       You pass black stools (blood-stained faeces).

 

Taking a proton pump inhibitor like Esomeprazole Sodium for Injection, especially over a period of

 

more than one year, may slightly increase your risk of fracture in the hip, wrist or spine. Tell  your  doctor if you have osteoporosis or if you are taking corticosteroids (which can increase the risk of osteoporosis). If you get a rash on your skin, especially in areas exposed to the sun tell your doctor as soon as you can, as you may need to stop your treatment with Esomeprazole Sodium for Injection. Remember to also mention any other ill effects like pain in your joints.

Other medicines and Esomeprazole Sodium for Injection

Tell your doctor or nurse if you are taking, have recently taken, or might take any other medicines. This includes medicines that you buy without a prescription. This is because Esomeprazole Sodium for Injection can affect the way some medicines work and some medicines can have an effect on Esomeprazole Sodium for Injection.

You must not be given Esomeprazole Sodium for Injection if you are taking a medicine containing nelfinavir (used to treat HIV infection).

Tell your doctor or nurse if you are taking any of the following medicines:

·       Atazanavir (used to treat HIV infection).

·       Clopidogrel (used to prevent blood clots).

·       Ketoconazole, itraconazole or voriconazole (used to treat infections caused by a fungus).

·       Erlotinib (used to treat cancer).

·       Citalopram, imipramine or clomipramine (used to treat depression).

·       Diazepam (used to treat anxiety, relax muscles or in epilepsy).

·       Phenytoin (used in epilepsy). If you are taking phenytoin, your doctor will need to monitor you when you start or stop having Esomeprazole Sodium for Injection.

·       Medicines that are used to thin your blood, such as warfarin. Your doctor may need to monitor you when you start or stop having Esomeprazole Sodium for Injection.

·       Cilostazol (used to treat intermittent claudication – a pain in your legs when you walk which is caused by an insufficient blood supply).

·       Cisapride (used for indigestion and heartburn).

·       Digoxin (used for heart problems).

·       Methotrexate (a chemotherapy medicine used in high doses to treat cancer) – if you are taking a high dose of methotrexate, your doctor may temporarily stop your Esomeprazole Sodium for Injection treatment.

·       Tacrolimus (organ transplantation).

·       Rifampicin (used for treatment of tuberculosis).

·       St. John’s wort (Hypericum perforatum) (used to treat depression).

 

 

 

Pregnancy, breast-feeding and fertility

 

If you are pregnant, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before you are given this medicine. Your doctor will decide whether  you  can  take Esomeprazole Sodium for Injection during this time. It is not known if Esomeprazole Sodium for Injection passes into breast milk. Therefore, you should not be given Esomeprazole Sodium  for Injection if you are breastfeeding.

Driving and using machines

Esomeprazole Sodium for Injection is not likely to affect you being able to drive or use any tools or machines. However, side effects such as dizziness and blurred vision may uncommonly  occur  (see  section 4). If affected, you should not drive or use machines.


Esomeprazole Sodium for Injection can be given to children and adolescents aged 1-18 years and adults, including the elderly.

Being given Esomeprazole Sodium for Injection

Use in adults

 

·       Esomeprazole Sodium for Injection will be given to you by your doctor who will decide how much you need.

·       The recommended dose is 20 mg or 40 mg once a day.

·       If you have severe liver problems, the maximum dose is 20 mg a day (GERD).

·       The medicine will be given to you as an injection  or infusion into one of  your veins. This will  last for up to 30 minutes.

·       The recommended dose for prevention of re-bleeding of gastric or duodenal ulcer is 80 mg administered as intravenous infusion over 30 minutes followed by a continuous infusion of 8 mg/hr given over 3 days. If you have severe liver problems, a continuous infusion of 4 mg/hr  given over 3 days may be sufficient.

Use in children and adolescents

·       Esomeprazole Sodium for Injection will be given by your doctor who will decide how much you need.

·       For children 1-11 years, the recommended dose is 10 or 20 mg given once a day.

·       For children 12-18 years, the recommended dose is 20 or 40 mg given once a day.

·       The medicine will be given as an injection or infusion into a vein. This will last up to 30

 

minutes.

If you are given more Esomeprazole Sodium for Injection than you should

 

If you think you have been given too much Esomeprazole Sodium for Injection, talk to your doctor straight away

 


If you notice any of the following serious side effects, stop taking Esomeprazole Sodium for Injection and contact a doctor immediately:

 

·       Sudden wheezing, swelling of your lips, tongue and throat or body, rash, fainting or difficulties in swallowing (severe allergic reaction).

·       Reddening of the skin with blisters or peeling. There may also be severe blisters and bleeding in the lips, eyes, mouth, nose and genitals. This could be ‘Stevens-Johnson syndrome’  or  ‘toxic  epidermal necrolysis’.

Yellow skin, dark urine and tiredness which can be symptoms of liver problems.

 

Like all medicines, this medicine can cause side effects, although not everybody gets them. These effects are rare, and may affect up to 1 in 1,000 people. Other side effects include:

Common (may affect up to 1 in 10 people)

·       Headache.

·       Effects on your stomach or gut: diarrhoea, stomach pain, constipation, wind (flatulence).

·       Feeling sick (nausea) or being sick (vomiting).

·       Injection site reaction.

·       Benign polyps in the stomach.

Uncommon (may affect up to 1 in 100 people)

·       Swelling of the feet and ankles.

·       Disturbed sleep (insomnia).

·       Dizziness, tingling feelings such as “pins and needles”, feeling sleepy.

·       Spinning feeling (vertigo).

·       Eyesight problems such as blurred vision.

·       Dry mouth.

·       Changes in blood tests that check how the liver is working.

·       Skin rash, lumpy rash (hives) and itchy skin.

·       Fracture of the hip, wrist or spine (if Esomeprazole Sodium for Injection is used in high doses

 

and over long duration).

Rare (may affect up to 1 in 1,000 people)

·       Blood problems such as a reduced number of white cells or platelets. This can cause weakness, bruising or make infections more likely.

·       Low levels of sodium in the blood. This may cause weakness, being sick (vomiting) and cramps.

·       Feeling agitated, confused or depressed.

·       Taste changes.

·       Suddenly feeling wheezy or short of breath (bronchospasm).

·       An inflammation of the inside of the mouth.

·       An infection called “thrush” which can affect the gut and is caused by a fungus.

·       Liver problems, including jaundice which can cause yellow skin, dark urine, and tiredness.

·       Hair loss (alopecia).

·       Skin rash on exposure to sunshine.

·       Joint pains (arthralgia) or muscle pains (myalgia).

·       Generally feeling unwell and lacking energy.

·       Increased sweating.

Very rare (may affect up to 1 in 10,000 people)

·       Changes in blood count including agranulocytosis (lack of white blood cells)

·       Aggression.

·       Seeing, feeling or hearing things that are not there (hallucinations).

·       Severe liver problems leading to liver failure and inflammation of the brain.

·       Sudden onset of a severe rash or blistering or peeling skin. This may be  associated  with  a high fever and joint pains (Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal  necrolysis).

·       Muscle weakness.

·       Severe kidney problems.

·       Enlarged breasts in men.

Not known (frequency cannot be estimated from the available data)

 

·            If you are on Esomeprazole Sodium for Injection  for more than three months it is possible that  the levels of magnesium in your  blood  may  fall.  Low  levels  of  magnesium  can  be  seen  as  fatigue, involuntary muscle contractions, disorientation, convulsions, dizziness or increased heart rate.  If you get any of these symptoms, please tell your doctor promptly. Low levels of magnesium

 

can also lead to a reduction in potassium or calcium levels in the blood. Your doctor may decide to perform regular blood tests to monitor your levels of magnesium.

·       Inflammation in the gut (leading to diarrhoea).

·       Rash, possibly with pain in the joints.

Esomeprazole Sodium for Injection may in very rare cases affect the white blood cells leading to immune deficiency. If you have an infection with symptoms such as fever with a severely reduced general condition or fever with symptoms of a local infection such as pain in the neck, throat or mouth or difficulties in urinating, you must consult your doctor as soon as possible so that a lack of white blood cells (agranulocytosis) can be ruled out by a blood test. It is important for you to give information about your medication at this time.

Reporting of side effects

 

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. You can also report side effects directly (see details below). By reporting side effects you can help provide more information on the safety of this medicine.

 • Saudi Arabia:

 

The National Pharmacovigilance and Drug Safety Centre (NPC)

o Fax: +966-11-205-7662

o Call NPC at +966-11-2038222, Exts: 2317-2356-2353-2354-2334-2340.

o Toll free phone: 8002490000

o E-mail: npc.drug@sfda.gov.sa

o Website: www.sfda.gov.sa/npc

 

 

 

 

 

 

 

o Other GCC States:

         Please contact the relevant competent authority.


Keep this medicine out of the sight and reach of children.

Do not use this medicine after the expiry date which is stated on the vial and on the box. The expiry date refers to the last day of that month.

Store below 30ºC. Protect from light.

 

 

 

 


What Esomeprazole Sodium for Injection contains?

The active substance is Esomeprazole Sodium for Injection esomeprazole Sodium.

 

Esomeprazole Sodium for Injection 40mg/Vial

Each vial contains Esomeprazole Sodium equivalent to Esomeprazole 40mg.

 

The other ingredients are: Disodium edetate, Sodium hydroxide and water for injection.

 


What Esomeprazole Sodium for Injection looks like?   Esomeprazole Sodium for Injection 40mg/Vial A white to off-white lyophilized cake in 5 mL clear, Type-I Tubular glass vial with 13 mm neck with grey bromo butyl double slotted rubber stopper with flip-off seal (13mm). How supplied: Esomeprazole Sodium for Injection 40mg/Vial is supplied in glass Vials. Direction for use: Esomeprazole Sodium for Injection 40 mg/vial: Intravenous Infusion: After reconstitution in 50 mL of 0.9% Sodium chloride Injection USP, Lactose Ringer's Injection USP or 5% Dextrose Injection USP, the resulting solution will contain Esomeprazole 0.8 mg/mL.

Marketing Authorisation Holder and Manufacturer

Saudi Amarox Industrial Company

Aljameah Street, Malaz quarter, Riyadh 11441 Saudi Arabia

Tel: +966 11 477 2215

 


October, 2018
  نشرة الدواء تحت مراجعة الهيئة العامة للغذاء والدواء (اقرأ هذه النشرة بعناية قبل البدء في استخدام هذا المنتج لأنه يحتوي على معلومات مهمة لك)

يحتوي ایسوبول للحقن على دواء يسمى إيسوميبرازول الصوديوم . ينتمي هذا الدواء إلى مجموعة من الأدوية تسمى "مثبطات مضخة البروتون" . حيث أنها تعمل عن طريق تقليل كمية الأحماض التي تفرزها المعدة .

يستخدم ایسوبول للحقن كعلاج قصير الأمد لحالات معينة ، عندما تكون غير قادر على تناول العلاج عن طريق الفم ويتم استخدامه لعلاج الحالات التالية:

البالغين

·       مرض الإرتجاع المريئي المعدي (GERD) . والذي يحدث فيه إرتجاع الحمض من المعدة إلى المريء (الأنبوب الذي يربط الحلق بالمعدة) مسبباً الألم والالتهابات والحرقة .

·       قرحات المعدة التي تسببها الأدوية التي تسمى مضادات الالتهاب غير الستيرودية (NSAID). يمكن أيضا استخدام ایسوبول للحقن لوقف قرحة المعدة من التكون إذا كنت تتناول مضادات الالتهاب غير الستيرودية .

·       منع عودة النزيف بعد حالات التنظير العلاجي للنزيف الحاد في المعدة أو الاثني عشر .

الأطفال والمراهقون الذين تتراوح أعمارهم بين 1-18 سنة

·       مرض الإرتجاع المريئي المعدي (GERD) . والذي يحدث فيه إرتجاع الحمض من المعدة إلى المريء (الأنبوب الذي يربط الحلق بالمعدة) مسبباً الألم والالتهابات والحرقة .


 

لا تقم باستعمال ایسوبول للحقن  :

·       إذا كنت تعاني من حساسية من ایسوبول للحقن أو أي من المكونات الأخرى لهذا الدواء (المذكورة في القسم 6).

·       إذا كنت تعاني من حساسية من أدوية مثبطات مضخة البروتون الأخرى (مثل بانتوبرازول ، لانسوبرازول ، والرايبرازول ، أوميبرازول) .

·       إذا كنت تتناول دواء يحتوي على نيلفينافير (يستخدم لعلاج عدوى فيروس نقص المناعة البشري) .

·       يجب عدم إعطائك ایسوبول للحقن إذا كان أي مما سبق ينطبق عليك . إذا لم تكن متأكداً ، تحدث مع طبيبك أو الممرضة قبل إعطاؤك هذا الدواء .

التحذيرات والاحتياطات

أخبر الطبيب المعالج قبل تناول ایسوبول للحقن خاصة إذا كنت تعاني من:

·       لديك مشاكل حادة في الكبد .

·       لديك مشاكل حادة في الكلى .

·       سبق أن عانيت من حساسية في الجلد بعد العلاج بتناول دواء مشابه لایسوبول للحقن الذي يقلل من حامض المعدة .

·       من المقرر إجراء اختبار دم محدد (كروموجرانين أ) .

ایسوبول للحقن قد يخفي أعراض الأمراض الأخرى . لذلك ، إذا حدث لك أي مما يلي قبل تناول ایسوبول للحقن أو بعد تناوله ، تحدث إلى طبيبك على الفور:

·       إذا كنت تفقد الكثير من الوزن بدون سبب ولديك مشاكل في البلع .

·       الشعور بألم في المعدة أو عسر الهضم .

·       إذا كنت تبدأ في تقيؤ الطعام أو الدم .

·       إذا كان لديك اﻟﺒﺮاز اﻷﺳﻮد (اﻟﺒﺮاز اﻟﻤﻠﻮن ﺑﺎﻟﺪم) .

قد يؤدي استخدام مثبط لمضخة البروتون مثل ایسوبول للحقن ، خاصة خلال فترة تزيد عن عام واحد ، إلى زيادة خطر حدوث الكسر بشكل طفيف في الورك أو الرسغ أو العمود الفقري . أخبر طبيبك إذا كان لديك هشاشة العظام أو إذا كنت تتناول الكورتيزون (التي يمكن أن تزيد من خطر الإصابة بهشاشة العظام) . إذا عانيت من طفح جلدي على بشرتك ، خاصة في المناطق المعرضة للشمس ، أخبر طبيبك بأسرع ما يمكن ، لأنك قد تحتاج إلى إيقاف علاجك باستخدام ایسوبول للحقن . تذكر أيضا أن تذكر أي آثار سيئة أخرى مثل ألم في المفاصل .

تناول الأدوية الأخرى و ایسوبول للحقن

أخبر طبيبك أو الممرضة إذا كنت تتناول ، أو تناولت مؤخرًا ، أو ربما تتناول أي أدوية أخرى . وهذا يشمل الأدوية التي تشتريها دون وصفة طبية . وذلك لأن ایسوبول للحقن يمكن أن يؤثر على طريقة عمل بعض الأدوية وقد يكون لبعض الأدوية تأثير على ایسوبول للحقن .

يجب عدم تناول ایسوبول للحقن إذا كنت تتناول دواء يحتوي على نلفينافير (يستخدم لعلاج عدوى فيروس نقص المناعة البشري) .

أخبر طبيبك أو الممرضة إذا كنت تتناول أي من الأدوية التالية:

·       أتازانافير (يستخدم لعلاج عدوى فيروس نقص المناعة البشرية) .

·       كلوبيدوجريل (يستخدم لمنع تجلط الدم) .

·       كيتوكونازول ، إيتراكونازول أو فورونيكونازول (يستخدم لعلاج الالتهابات التي تسببها الفطريات) .

·       إيرلوتينيب (يستخدم لعلاج السرطان) .

·       سيتالوبرام ، إيميبرامين أو كلوميبرامين (يستخدم لعلاج الاكتئاب) .

·       الديازيبام (يستخدم لعلاج القلق أو استرخاء العضلات أو الصرع) .

·       الفينيتوين (يستخدم في الصرع) . إذا كنت تتناول الفينيتوين ، فسوف يحتاج طبيبك لمتابعتك عند البدء أو التوقف عن تناول ایسوبول للحقن .

·       الأدوية التي تستخدم لأمراض الدم ، مثل الوارفارين . قد يحتاج طبيبك لمتابعتك عند البدء أو إيقاف استخدام ایسوبول للحقن .

·       سيلوستازول (يستخدم لعلاج العرج المتقطع - ألم في ساقيك عند المشي الذي يحدث بسبب عدم كفاية إمدادات الدم) .

·       سيسابريد (يستخدم لعسر الهضم والحرقة) .

·       الديجوكسين (يستخدم لعلاج مشاكل القلب) .

·       ميثوتريكسات (دواء علاج كيميائي يستخدم في جرعات عالية لعلاج السرطان) - إذا كنت تتناول جرعة كبيرة من الميثوتريكسيت ، قد يقوم طبيبك بإيقاف تناول ایسوبول للحقن .

·       تاكروليموس (زرع الأعضاء) .

·       ريفامبيسين (يستخدم لعلاج السل) .

·       نبتة سانت جونز (هايبيريكم بيرفراتم (العرن المثقوب)) (تستخدم لعلاج الاكتئاب) .

الحمل والرضاعة الطبيعية والخصوبة

إذا كنتِ حاملاً ، أو قد تكونين حاملاً أو تخططين لإنجاب طفل ، اسأل طبيبك أو الصيدلي للحصول على المشورة قبل تناول هذا الدواء . سيقرر طبيبك ما إذا كان بإمكانك تناول ایسوبول للحقن خلال هذا الوقت . ليس من المعروف ما إذا كان ایسوبول للحقن يمر إلى حليب الثدي . لذلك ، يجب عدم تناول ایسوبول للحقن إذا كنت ترضعين طفلك رضاعة طبيعية .

القيادة واستخدام الآلات

 

من غير المحتمل أن يؤثر ایسوبول للحقن على قدرتك على القيادة أو استخدام أي أدوات أو آلات . ومع ذلك ، قد تحدث تأثيرات جانبية مثل الدوخة وعدم وضوح الرؤية (انظر القسم 4) . إذا تأثرت ، يجب ألا تقود السيارة أو تستخدم الآلات .

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يمكن استخدام ایسوبول للحقن للأطفال والمراهقين الذين تتراوح أعمارهم بين 1-18 سنة والبالغين ، بما في ذلك كبار السن .

استخدام ایسوبول للحقن

استخدامها في البالغين

 

·       سيُعطى ایسوبول للحقن من قبل الطبيب والذي سيحدد الكمية التي تحتاجها .

·       الجرعة الموصى بها هي 20 ملغم أو 40 ملغم مرة واحدة في اليوم .

·       إذا كنت تعاني من مشاكل خطيرة في الكبد ، فإن الجرعة القصوى هي 20 ملغم في اليوم (GERD).

·       سيتم إعطاؤك الدواء كحقن أو بالتقطير الوريدي في أحد عروقك . سيستمر هذا لمدة تصل إلى 30 دقيقة .

·       الجرعة الموصى بها للوقاية من إعادة النزيف من قرحة المعدة أو الاثني عشر هي 80 ملغم يتم تناولها عن طريق الحقن في الوريد على مدى 30 دقيقة تليها تسريب مستمر من 8 ملغم / ساعة على مدى 3 أيام . إذا كنت تعاني من مشاكل خطيرة في الكبد ، يكون التسريب المستمر 4 ملغم / ساعة خلال 3 أيام .

 

استخدامها في الأطفال والمراهقين

 

·       سيُعطى ایسوبول للحقن من قبل الطبيب والذي سيحدد الكمية التي تحتاجها .

·       بالنسبة للأطفال من 1 إلى 11 سنة ، تكون الجرعة الموصى بها 10 أو 20 ملغم مرة واحدة في اليوم .

·       بالنسبة للأطفال الذين تتراوح أعمارهم بين 12 و 18 سنة ، تكون الجرعة الموصى بها 20 أو 40 ملغم مرة واحدة في اليوم .

·       سيتم إعطاء الدواء كحقن أو بالتقطير الوريدي . هذا سوف يستمر حتى 30 دقيقة .

تناول جرعة زائدة من ایسوبول للحقن

إذا كنت تعتقد أنك قد تناولت الكثير من ایسوبول للحقن ، تحدث إلى طبيبك على الفور

مثل جميع الأدوية ، من الممكن أن يسبب ایسوبول للحقن بعض الآثار الجانبية الخطيرة .

إذا لاحظت أيًا من الآثار الجانبية الخطيرة التالية ، فتوقف عن تناول ایسوبول للحقن واتصل بالطبيب على الفور:

·       أزيز الصدر المفاجئ وتورم الشفاه واللسان والحلق أو الجسم والطفح الجلدي والإغماء أو صعوبات في البلع (رد فعل تحسسي شديد) .

·        احمرار الجلد بثور أو تقشير . قد يكون هناك أيضا بثور شديدة ونزيف في الشفتين والعيون والفم والأنف والأعضاء التناسلية . يمكن أن يكون هذا "متلازمة ستيفنز جونسون" أو "انحلال البشرة السمي" .

·       البشرة الصفراء والبول الداكن والتعب والتي يمكن أن تكون من أعراض مشاكل الكبد .

هذه التأثيرات نادرة وقد تؤثر على 1 من كل 1000 شخص .

تشمل الآثار الجانبية الأخرى:

عام (قد يؤثر على شخص واحد من كل 10 أشخاص)

·       صداع الراس .

·       آثار على المعدة أو القناة الهضمية: الإسهال ، آلام في المعدة ، والإمساك ، والرياح (انتفاخ البطن) .

·       الشعور بالمرض (الغثيان) أو الإعياء (التقيؤ) .

·       رد فعل تحسسي في موقع الحقن .

·       الاورام الحميدة في المعدة .

غير شائع (قد يؤثر على شخص واحد من بين كل 100 شخص)

·        تورم القدمين والكاحلين .

·       اضطراب النوم (الأرق) .

·       دوار ، شعور بالوخز مثل "الدبابيس والإبر" ، الشعور بالنعاس .

·       الشعور بالدوخة (الدوار) .

·       مشاكل في البصر مثل عدم وضوح الرؤية .

·       جفاف بالفم .

·       التغييرات في نتائج اختبارات الدم التي تتحقق من كيفية عمل الكبد .

·       الطفح الجلدي (الشرى) والحكة الجلدية .

·       كسر في الورك أو المعصم أو العمود الفقري (إذا تم استخدام ایسوبول للحقن بجرعات عالية ولمدة طويلة) .

نادر (قد يؤثر على 1 من كل 1000 شخص)

·       مشاكل الدم مثل انخفاض عدد الخلايا البيضاء أو الصفائح الدموية . هذا يمكن أن يسبب الضعف ، وكدمات أو جعل العدوى أكثر احتمالا .

·       مستويات منخفضة من الصوديوم في الدم . قد يتسبب ذلك في الضعف ، والمرض (التقيؤ) والمغص .

·       الشعور بالتهيج أو الارتباك أو الاكتئاب .

·       تغيرات التذوق .

·       الشعور المفاجئ بأزيز الصدر أو ﻗﺼﺮ اﻟﺘﻨﻔﺲ (التشنج القصبي).

·       التهاب داخل الفم .

·       عدوى تسمى "القلاع" يمكن أن تؤثر على القناة الهضمية وينتج عن فطر .

·       مشاكل الكبد ، بما في ذلك اليرقان الذي يمكن أن يسبب الجلد الأصفر والبول الداكن والتعب.

·       تساقط الشعر .

·       الطفح الجلدي عند التعرض لأشعة الشمس .

·       آلام المفاصل (ألم مفصلي) أو آلام في العضلات (ألم عضلي) .

·       الشعور عمومًا بالإعياء ونقص الطاقة .

·       زيادة التعرق .

نادر جدًا (قد يؤثر على شخص واحد من بين كل 10000 شخص)

·       التغييرات في عدد خلايا الدم بما في ذلك ندرة المحببات (نقص خلايا الدم البيضاء)

·       العدوانية .

·       رؤية أو الشعور أو سماع أشياء غير موجودة (الهلوسة) .

·       مشاكل الكبد الحادة التي تؤدي إلى فشل الكبد والتهاب الدماغ .

·       ظهور مفاجئ للطفح الجلدي الشديد أو تقرحات الجلد أو تقشير الجلد . قد يكون هذا مرتبطًا بحمى مرتفعة وآلام في المفاصل (الحمامي متعددة الاشكال ، متلازمة ستيفنس جونسون ، تقشر الانسجة المتموتة البشروية التسممي) .

·       ضعف العضلات .

·       مشاكل حادة بالكلى .

·       تضخم الثديين عند الرجال .

غير معروف (لا يمكن تقدير معدلاتها من البيانات المتاحة)

·       إذا كنت تتناول ایسوبول للحقن لأكثر من ثلاثة أشهر فمن الممكن أن تنخفض مستويات الماغنيسيوم في دمك . المستويات المنخفضة من الماغنيسيوم  تظهر على هيئة التعب ، وتقلصات العضلات اللاإرادية ، والارتباك ، والتشنجات ، والدوخة أو زيادة معدل ضربات القلب . إذا عانيت من  أي من هذه الأعراض ، فالرجاء إخبار طبيبك على الفور . قد يؤدي انخفاض مستوى الماغنيسيوم أيضًا إلى انخفاض مستويات البوتاسيوم أو الكالسيوم في الدم . قد يقرر طبيبك إجراء اختبارات دم منتظمة لمراقبة مستويات الماغنسيوم .

·       التهاب في القناة الهضمية (مما يؤدي إلى الإسهال) .

·       الطفح ، ربما مع ألم في المفاصل .

 

في حالات نادرة جدا يؤثر تناول ایسوبول للحقن على خلايا الدم البيضاء مما يؤدي إلى نقص المناعة . إذا كان لديك عدوى مع أعراض مثل الحمى مع إنخفاض شديد في الحالة العامة أو حمى مع أعراض العدوى الموضعية مثل ألم في الرقبة أو الحلق أو الفم أو صعوبات في التبول ، يجب عليك استشارة الطبيب في أقرب وقت ممكن حتى يمكن استبعاد نقص خلايا الدم البيضاء (ندرة المحببات) عن طريق فحص الدم . من المهم بالنسبة لك إعطاء معلومات عن الدواء الخاص بك في هذا الوقت .

 

الإبلاغ عن الآثار الجانبية:

إذا زادت حدة أي من هذه الأعراض الجانبية ، أو لاحظت ظهور أعراض جانبية غير ما تم ذكره في هذه النشرة ، يرجى إبلاغ الطبيب المعالج أو الصيدلي . وهذا يشمل أي آثار جانبية محتملة غير مدرجة في هذه النشرة . يمكنك أيضا الإبلاغ عن الآثار الجانبية مباشرة (انظر التفاصيل أدناه) . بالإبلاغ عن الآثار الجانبية يمكنك المساعدة في توفير مزيد من المعلومات حول أمان هذا الدواء .

للإبلاغ عن الأعراض الجانبية

-        المركز الوطني للتيقظ والسلامة الدوائية

o     فاكس 7662-205-1-966+

o     الاتصال على المركز الوطني للتيقظ والسلامة الدوائية +966-11-2038222 ، تحويلة: 2317-2356-2353-2354-2334-2340

o     الهاتف المجاني: 8002490000

o     البريد الإلكتروني : npc .drug@sfda .gov .sa

o     الموقع الإلكتروني: www .sfda .gov .sa/npc

 

دول مجلس التعاون الخليجي الأخرى:

   يرجى الاتصال بالسلطة الصحية المختصة .

·         يحفظ بعيدا عن متناول أيدي الأطفال أو على مرأى منهم .

·         يجب الحفظ في درجة حرارة أقل من 30 ° مئوية . وبعيدا عن الضوء .

·         لا تستخدم ایسوبول للحقن بعد تاريخ انتهاء الصلاحية الموجود على العبوة . تاريخ انتهاء الصلاحية يشير إلى اليوم الأخير من ذلك الشهر .

ما تحتويه ایسوبول للحقن ؟

ایسوبول للحقن 20 ملغم / قارورة:

المادة الفعالة هي إيسوميبرازول .

تحتوي كل قارورة من ایسوبول للحقن على إيسوميبرازول الصوديوم ما يكافئ 20 ملغم من إيسوميبرازول .

الصواغات الأخرى هي: ثنائي صوديوم الإيديتات ، هيدروكسيد الصوديوم والماء للحقن .

ایسوبول للحقن 40 ملغم / قارورة:

المادة الفعالة هي إيسوميبرازول .

تحتوي كل قارورة من ایسوبول للحقن على إيسوميبرازول الصوديوم ما يكافئ 40 ملغم من إيسوميبرازول .

الصواغات الأخرى هي: ثنائي صوديوم الإيديتات ، هيدروكسيد الصوديوم والماء للحقن .

ما هو شكل ایسوبول للحقن ومحتويات العلبة ؟

ایسوبول للحقن 20 ملغم / قارورة

مسحوق مجفف بالتجميد لونه أبيض إلى الأبيض القاتم معبأ في قارورة زجاجية أنبوبية الشكل من النوع I سعة 5 مل ، بقطر 13 ملم مغطاة بسدادة مطاطية من البرومو بيوتيل ثنائية التجويف باللون الرمادي الفاتح مع غطاء حماية لونه أزرق فاتح (13 مم) .

ایسوبول للحقن 40 ملغم / قارورة

مسحوق مجفف بالتجميد لونه أبيض إلى الأبيض القاتم معبأ في قارورة زجاجية أنبوبية الشكل من النوع I سعة 5 مل ، بقطر 13 ملم مغطاة بسدادة مطاطية من البرومو بيوتيل ثنائية التجويف باللون الرمادي الفاتح مع غطاء حماية (13 مم) .

توافر ایسوبول للحقن:

تتوافر ایسوبول للحقن 20 ملغم على هيئة قارورة زجاجية .

تتوافر ایسوبول للحقن 40 ملغم على هيئة قارورة زجاجية .

 

تعليمات للاستخدام:

20 ملغم / قارورة:

التسريب الوريدي: بعد إعادة الحل في 50 مل من محلول كلوريد الصوديوم 0.9 % أو محلول الرينجر اللاكتوزي أو محلول الديكستروز 5 % المتوافقين مع دستور الأدوية الأمريكي ، سيصبح تركيز إيسوميبرازول 0.4 ملغم / مل .

 

 

 

 

  40 ملغم / قارورة:

التسريب الوريدي: بعد إعادة الحل في 50 مل من محلول كلوريد الصوديوم 0.9 % أو محلول الرينجر اللاكتوزي أو محلول الديكستروز 5 % المتوافقين مع دستور الأدوية الأمريكي ، سيصبح تركيز إيسوميبرازول 0.8 ملغم / مل .

 

اسم وعنوان مالك رخصة التسویق والمصنع
المصنع:
شركة اسبیرو فارما
حیدر اباد – تیلانقا – الھند
هاتف : ٠٠٩١٨٤٥٨٢٧٥٣١٤

صاحب حق التسويق:

شركة أماروكس السعودية للصناعة

شارع الجامعة – الملز - الرياض

المملكة العربية السعودية .  

هاتف : 00966114772215

     

مایو /٢٠١٨
 Read this leaflet carefully before you start using this product as it contains important information for you

Esomeprazole Sodium for Injection 40mg/Vial

Esomeprazole Sodium for Injection 40mg/Vial: Each vial contains Esomeprazole sodium equivalent to Esomeprazole 40mg

Esomeprazole Sodium for Injection 40mg/Vial: A white to off-white lyophilized cake in 5 mL clear, Type-I Tubular glass vial with 13 mm neck with grey bromo butyl double slotted rubber stopper with flip-off seal (13mm).

EsomeprazoleSodiumforInjectionandinfusionisindicatedinadultsfor:

 

• Gastric ant secretory treatment when the oral route is not possible, such as:

 

-         gastroesophageal reflux disease (GERD) in patients with esophagitis and/or severe symptoms of reflux.

-         healing of gastric ulcers associated with NSAID therapy.

 

-         prevention of gastric and duodenal ulcers associated with NSAID therapy, in patients at risk.

 

•          Prevention  of  rebleeding  following  therapeutic  endoscopy  for  acute  bleeding  gastric  or duodenal ulcers.                                                                                                               

EsomeprazoleSodiumforInjectionandinfusionisindicatedinchildrenandadolescentsaged1-18       yearsfor:

•          Gastric antisecretory treatment when the oral route is not possible, such as:

 

- gastroesophageal reflux disease (GERD) in patients with erosive reflux esophagitis and/or severe symptoms of reflux.


Posology

Adults

Gastric ant secretory treatment when the oral route is not possible

Patients who cannot take oral medication may be treated parenterally with 20–40 mg once daily. Patients with reflux esophagitis should be treated with 40 mg once daily. Patients treated symptomatically for reflux disease should be treated with 20 mg once daily.

For healing of gastric ulcers associated with NSAID therapy the usual dose is 20 mg once daily. For prevention of gastric and duodenal ulcers associated with NSAID therapy, patients at risk should be treated with 20 mg once daily.

Usually the intravenous treatment duration is short and transfer to oral treatment should be made as soon as possible.

Prevention of rebleeding of gastric and duodenal ulcers

Following therapeutic endoscopy for acute bleeding gastric or duodenal ulcers, 80 mg should be administered as a bolus infusion over 30 minutes, followed by a continuous intravenous infusion of 8 mg/h given over 3 days (72 hours).

The parenteral treatment period should be followed by oral acid-suppression therapy.

Methodofadministration

For instructions on reconstitution of the medicinal product before administration, see section 6.6.

 Injection

40mgdose

5 ml of the reconstituted solution (8 mg/ml) should be given as an intravenous injection over a

period of at least 3 minutes.

20mgdose

2.5 ml or half of the reconstituted solution (8 mg/ml) should be given as an intravenous injection over a period of at least 3 minutes. Any unused solution should be discarded. Infusion

40mgdose

The reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes.

20mgdose

Half of the reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes. Any unused solution should be discarded.

80mgbolusdose

The reconstituted solution should be given as a continuous intravenous infusion over 30 minutes.

8mg/hdose

The reconstituted solution should be given as a continuous intravenous infusion over a period of

71.5 hours (calculated rate of infusion of 8 mg/h. See section 6.3 for shelf-life of the reconstituted solution).

SpecialPopulations

Renal impairment

Dose adjustment is not required in patients with impaired renal function. Due to limited experience in patients with severe renal insufficiency, such patients should be treated with caution (see section

5.2).

Hepatic impairment

GERD: Dose adjustment is not required in patients with mild to moderate liver impairment. For patients with severe liver impairment, a maximum daily dose of 20 mg Esomeprazole Sodium for Injection I.V. should not be exceeded (see section 5.2).

Bleeding ulcers: Dose adjustment is not required in patients with mild to moderate liver impairment. For patients with severe liver impairment, following an initial bolus dose of 80 mg Esomeprazole Sodium for Injection for infusion, a continuous intravenous infusion dose of 4 mg/h for 71.5 hours may be sufficient (see section 5.2).

Elderly

Dose adjustment is not required in the elderly.

Paediatric population

Posology                                     

Childrenandadolescentsaged1-18 years

Gastric ant secretory treatment when the oral route is not possible

Patients who cannot take oral medication may be treated parenterally once daily, as a part of a full treatment period for GERD (see doses in table below).

Usually the intravenous treatment duration should be short and transfer to oral treatment should be made as soon as possible.

Recommended intravenous doses of esomeprazole

 

Age group

Treatment of erosive reflux esophagitis

Symptomatic     treatment

GERD

of

1-11 Years

Weight <20 kg: 10 mg once daily

 

Weight ≥20 kg: 10 mg or 20 mg once daily

10 mg once daily

 

12-18 Years

40 mg once daily

20 mg once daily

 

Methodofadministration

For instructions on reconstitution of the medicinal product before administration, see section 6.6. Injection

40mgdose

5 ml of the reconstituted solution (8 mg/ml) should be given as an intravenous injection over a period of at least 3 minutes.

20mgdose

2.5 ml or half of the reconstituted solution (8 mg/ml) should be given as an intravenous injection over a period of at least 3 minutes. Any unused solution should be discarded.

10mgdose

1.25 ml of the reconstituted solution (8 mg/ml) should be given as an intravenous injection over a

period of at least 3 minutes. Any unused solution should be discarded. Infusion

40mgdose

The reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes.

20mgdose

Half of the reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes. Any unused solution should be discarded.

10mgdose

A quarter of the reconstituted solution should be given as an intravenous infusion over a period of 10 to 30 minutes. Any unused solution should be discarded.


Hypersensitivity to the active substance, to substituted benzimidazoles or to any of the excipients listed in section 6.1. Esomeprazole should not be used concomitantly with nelfinavir (see section 4.5).

In the presence of any alarm symptom (e.g. significant unintentional weight loss, recurrent vomiting, dysphagia, haematemesis or melaena) and when gastric ulcer is suspected or present, malignancy should be excluded, as treatment with Esom may alleviate symptoms and delay diagnosis.

Gastrointestinalinfections

Treatment  with  proton  pump  inhibitors may lead  to  slightly increased  risk  of  gastrointestinal infections such as Salmonella and Campylobacter (see section 5.1).

AbsorptionofvitaminB12

Esomeprazole,  as  all  acid-blocking  medicines,  may  reduce  the  absorption  of  vitamin  B12 (cyanocobalamin) due to hypo- or achlorhydria. This should be considered in patients with reduced body stores or risk factors for reduced vitamin B12 absorption on long-term therapy.

Hypomagnesaemia

Severe hypomagnesaemia has been reported in patients treated with proton pump inhibitors (PPIs) like esomeprazole for at least three months, and in most cases for a year. Serious manifestations of hypomagnesaemia such as fatigue, tetany, delirium, convulsions, dizziness and ventricular arrhythmia can occur but they may begin insidiously and be overlooked. In most affected patients, hypomagnesaemia improved after magnesium replacement and discontinuation of the PPI. For patients  expected  to  be  on  prolonged  treatment  or  who  take  PPIs  with  digoxin  or  medicinal products that may cause hypomagnesaemia (e.g. diuretics), healthcare professionals should consider measuring magnesium levels before starting PPI treatment and periodically during treatment.    

Riskoffracture

Proton pump inhibitors, especially if used in high doses and over long durations (>1 year), may modestly increase the risk of hip, wrist and spine fracture, predominantly in the elderly or in presence of other recognised risk factors. Observational studies suggest that proton pump inhibitors may increase the overall risk of fracture by 10-40%. Some of this increase may be due to other risk factors. Patients at risk of osteoporosis should receive care according to current clinical guidelines and they should have an adequate intake of vitamin D and calcium.                                      

Subacutecutaneouslupuserythematosus(SCLE)

Proton pump inhibitors are associated with very infrequent cases of SCLE. If lesions occur, especially in sun-exposed areas of the skin, and if accompanied by arthralgia, the patient should seek medical help promptly and the health care professional should consider stopping Esomeprazole Sodium for Injection. SCLE after previous treatment with a proton pump inhibitor may increase the risk of SCLE with other proton pump inhibitors.

Combinationwithothermedicines

Co-administration of esomeprazole with atazanavir is not recommended (see section 4.5). If the combination of atazanavir with a proton pump inhibitor is judged unavoidable, close clinical monitoring is recommended in combination with an increase in the dose of atazanavir to 400 mg with 100 mg of ritonavir; esomeprazole 20 mg should not be exceeded.

Esomeprazole is a CYP2C19 inhibitor. When starting or ending treatment with esomeprazole, the potential for interactions with medicinal products metabolised through CYP2C19 should be considered. An interaction is observed between clopidogrel and esomeprazole (see section 4.5). The clinical relevance of this interaction is uncertain. As a precaution, concomitant use of esomeprazole and clopidogrel should be discouraged.

Interferencewithlaboratorytests

Increased Chromogranin A (CgA) level may interfere with investigations for neuroendocrine tumours. To avoid this interference, esomeprazole treatment should be stopped for at least 5 days before CgA measurements (see section 5.1). If CgA and gastrin levels have not returned to reference range after initial measurement, measurements should be repeated 14 days after cessation of proton pump inhibitor treatment.


Effectsofesomeprazoleonthepharmacokineticsofothermedicinalproducts     

Proteaseinhibitors

Omeprazole has been reported to interact with some protease inhibitors. The clinical importance and the mechanisms behind these reported interactions are not always known. Increased gastric pH during omeprazole treatment may change the absorption of the protease inhibitors. Other possible interaction mechanisms are via inhibition of CYP 2C19.

For atazanavir and nelfinavir, decreased serum levels have been reported when given together with omeprazole and concomitant administration is not recommended. Co-administration of omeprazole (40 mg once daily) with atazanavir 300 mg/ritonavir 100 mg to healthy volunteers resulted in a substantial reduction in atazanavir exposure (approximately 75% decrease in AUC, Cmax and Cmin). Increasing the atazanavir dose to 400 mg did not compensate for the impact of omeprazole on atazanavir exposure. The co-administration of omeprazole (20 mg qd) with atazanavir 400 mg/ritonavir 100 mg to healthy volunteers resulted in a decrease of approximately 30% in the atazanavir exposure as compared with the exposure observed with atazanavir 300mg/ritonavir 100 mg qd without omeprazole 20 mg qd. Co-administration of omeprazole (40 mg qd) reduced mean

nelfinavir AUC, Cmax and Cmin by 36–39 % and mean AUC, Cmax and Cmin for the pharmacologically active metabolite M8 was reduced by 75-92%. Due to the similar pharmacodynamic effects and pharmacokinetic properties of omeprazole and esomeprazole, concomitant administration with esomeprazole and atazanavir is not recommended (see section 4.4) and concomitant administration with esomeprazole and nelfinavir is contraindicated (see section

4.3).

For saquinavir (with concomitant ritonavir), increased serum levels (80-100%) have been reported during concomitant omeprazole treatment (40 mg qd). Treatment with omeprazole 20 mg qd had no effect on the exposure of darunavir (with concomitant ritonavir) and amprenavir (with concomitant ritonavir). Treatment with esomeprazole 20 mg qd had no effect on the exposure of amprenavir (with and without concomitant ritonavir). Treatment with omeprazole 40 mg qd had no effect on the exposure of lopinavir (with concomitant ritonavir).

Methotrexate

When given together with PPIs, methotrexate levels have been reported to increase in some patients. In high-dose methotrexate administration a temporary withdrawal of esomeprazole may need to be considered.

Tacrolimus

Concomitant administration of esomeprazole has been reported to increase the serum levels of tacrolimus.  A  reinforced  monitoring  of  tacrolimus  concentrations  as  well  as  renal  function (creatinine clearance) should be performed, and dosage of tacrolimus adjusted if needed.  

MedicinalproductswithpHdependentabsorption

Gastric acid suppression during treatment with esomeprazole and other PPIs might decrease or increase the absorption of medicinal products with a gastric pH dependent absorption. As with other medicinal products that decrease intragastric acidity, the absorption of medicinal products such as ketoconazole, itraconazole and erlotinib can decrease and the absorption of digoxin can increase during treatment with esomeprazole. Concomitant treatment with omeprazole (20 mg daily) and digoxin in healthy subjects increased the bioavailability of digoxin by 10% (up to 30% in two out of ten subjects). Digoxin toxicity has been rarely reported. However, caution should be exercised when esomeprazole is given at high doses in elderly patients. Therapeutic medicinal product monitoring of digoxin should then be reinforced.                                                    

MedicinalproductsmetabolisedbyCYP2C19

Esomeprazole inhibits CYP2C19, the major esomeprazole-metabolising enzyme. Thus, when esomeprazole is combined with medicinal products metabolised by CYP2C19, such as diazepam, citalopram, imipramine, clomipramine, phenytoin etc., the plasma concentrations of these medicinal products may be increased and a dose reduction could be needed. No in vivo interaction studies have been performed with the high dose intravenous regimen (80 mg+8 mg/h). The effect of esomeprazole on medicinal products metabolised by CYP2C19 may be more pronounced during this regimen, and patients should be monitored closely for adverse effects, during the 3 day intravenous treatment period.

Diazepam

Concomitant oral administration of 30 mg esomeprazole resulted in a 45% decrease in clearance of the CYP2C19 substrate diazepam.

Phenytoin

Concomitant oral administration of 40 mg esomeprazole and phenytoin resulted in a 13% increase in trough plasma levels of phenytoin in epileptic patients. It is recommended to monitor the plasma concentrations of phenytoin when treatment with esomeprazole is introduced or withdrawn.

Voriconazole

Omeprazole (40 mg once daily) increased voriconazole (a CYP2C19 substrate) Cmax and AUC by

15% and 41%, respectively.

Cilostazol

Omeprazole as well as esomeprazole act as inhibitors of CYP2C19. Omeprazole, given in doses of

40 mg to healthy subjects in a cross-over study, increased Cmax and AUC for cilostazol by 18% and 26% respectively, and one of its active metabolites by 29% and 69% respectively.

Cisapride

In healthy volunteers, concomitant oral administration of 40 mg esomeprazole and cisapride resulted in a 32% increase in area under the plasma concentration-time curve (AUC) and a 31% prolongation of elimination half-life(t1/2) but no significant increase in peak plasma levels of cisapride. The slightly prolonged QTc interval observed after administration of cisapride alone, was not further prolonged when cisapride was given in combination with esomeprazole.

Warfarin

Concomitant oral administration of 40 mg esomeprazole to warfarin-treated patients in a clinical trial showed that coagulation times were within the accepted range. However, post-marketing of oral esomeprazole, a few isolated cases of elevated INR of clinical significance have been reported during concomitant treatment. Monitoring is recommended when initiating and ending concomitant esomeprazole treatment during treatment with warfarin or other coumarine derivatives.

Clopidogrel

Results from studies in healthy subjects have shown a pharmacokinetic (PK)/ pharmacodynamic (PD) interaction between clopidogrel (300 mg loading dose/75 mg daily maintenance dose) and esomeprazole (40 mg p.o.daily) resulting in decreased exposure to the active metabolite of clopidogrel by an average of 40% and resulting in decreased maximum inhibition of (ADP induced) platelet aggregation by an average of 14%.

When clopidogrel was given together with a fixed dose combination of esomeprazole 20 mg + ASA 81 mg compared to clopidogrel alone in a study in healthy subjects there was a decreased exposure by almost 40% of the active metabolite of clopidogrel. However, the maximum levels of inhibition of (ADP induced) platelet aggregation in these subjects were the same in the clopidogrel and the clopidogrel + the combined (esomeprazole + ASA) product groups.

Inconsistent data on the clinical implications of a PK/PD interaction of esomeprazole in terms of major cardiovascular events have been reported from both observational and clinical studies. As a precaution concomitant use of clopidogrel should be discouraged.                                   

Investigatedmedicinalproductswithnoclinicallyrelevantinteraction

Amoxicillin or quinidine

Esomeprazole has been shown to have no clinically relevant effects on the pharmacokinetics of amoxicillin or quinidine.

Naproxen or rofecoxib

Studies evaluating concomitant administration of esomeprazole and either naproxen or rofecoxib did not identify any clinically relevant pharmacokinetic interactions during short-term studies.

Effectsofothermedicinalproductsonthepharmacokineticsofesomeprazole                             

MedicinalproductswhichinhibitCYP2C19and/orCYP3A4

Esomeprazole is metabolised by CYP2C19 and CYP3A4. Concomitant oral administration of esomeprazole and a CYP3A4 inhibitor, clarithromycin (500 mg b.i.d.), resulted in a doubling of the exposure (AUC) to esomeprazole. Concomitant administration of esomeprazole and a combined inhibitor of CYP2C19 and CYP 3A4 may result in more than doubling of the esomeprazole exposure. The CYP2C19 and CYP3A4 inhibitor voriconazole increased omeprazole AUC by 280%. A dose adjustment of esomeprazole is not regularly required in either of these situations. However, dose adjustment should be considered in patients with severe hepatic impairment and if long-term treatment is indicated.

Medicinal products which induce CYP2C19 and/or CYP3A4

Medicinal products known to induce CYP2C19 or CYP3A4 or both (such as rifampicin and St. John's wort) may lead to decreased esomeprazole serum levels by increasing the esomeprazole metabolism.

Paediatricpopulation

Interaction studies have only been performed in adults.


Pregnancy

Clinical data on exposed pregnancies with Esomeprazole Sodium for Injection are insufficient. With the racemic mixture, omeprazole data on a larger number of exposed pregnancies from epidemiological studies indicate no malformative nor foeto toxic effect. Animal studies with esomeprazole do not indicate direct or indirect harmful effects with respect to embryonal/foetal development. Animal studies with the racemic mixture do not indicate direct or indirect harmful effects with respect to pregnancy, parturition or postnatal development. Caution should be exercised when prescribing Esomeprazole Sodium for Injection to pregnant women.

A moderate amount of data on pregnant women (between 300-1000 pregnancy outcomes) indicates no malformative or foeto/neonatal toxicity of esomeprazole.

Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity (see section 5.3).

Breast-feeding

It is not known whether esomeprazole is excreted in human breast milk, there is insufficient information on the effects of esomeprazole in newborns/infants. Esomeprazole should not be used during breast-feeding.

Fertility

Animal studies with the racemic mixture omeprazole, given by oral administration, do not indicate effects with respect to fertility.


Esomeprazole has minor influence on the ability to drive and use machines. Adverse reactions such as dizziness (uncommon) and blurred vision (uncommon) have been reported (see section 4.8). If affected patients should not drive or use machines.


Summaryofthesafetyprofile

 

Headache, abdominal pain, diarrhoea and nausea are among those adverse reactions that have been most commonly reported in clinical trials (and also from post-marketing use). In addition, the safety profile  is  similar  for  different  formulations,  treatment  indications,  age  groups  and  patient populations. No dose-related adverse reactions have been identified.                                   

Tabulatedlistofadversereactions

The following adverse medicinal product reactions have been identified or suspected in the clinical trials programme for esomeprazole administered orally or intravenously and post-marketing when administered orally. The reactions are classified according to frequency: very common >1/10; common >1/100 to <1/10; uncommon >1/1,000 to <1/100; rare >1/10,000 to <1/1,000; very rare

<1/10,000; not known (cannot be estimated from the available data).

 

System Organ Class

 

Frequency

Undesirable Effect

Blood       and       lymphatic

disorders

system

Rare

Leukopenia, thrombocytopenia

Very rare

Agranulocytosis, pancytopenia

Immune system disorders

 

Rare

Hypersensitivity reactions e.g. fever, angioedema and anaphylactic reaction/shock

 

 

Metabolism and nutrition disorders

Uncommon

Peripheral oedema

Rare

Hyponatraemia

Not known

Hypomagnesaemia (see section 4.4); severe hypomagnesaemia can correlate with hypocalcaemia. Hypomagnesaemia may also be associated with hypokalaemia.

Psychiatric disorders

Uncommon

Insomnia

Rare

Agitation, confusion, depression

Very rare

Aggression, hallucinations

Nervous system disorders

Common

Headache

Uncommon

Dizziness, paraesthesia, somnolence

Rare

Taste disturbance

Eye disorders

Uncommon

Blurred vision

Ear and labyrinth disorders

Uncommon

Vertigo

Respiratory, thoracic and mediastinal disorders

Rare

Bronchospasm

Gastrointestinal disorders

Common

Abdominal pain, constipation, diarrhoea, flatulence, nausea/vomiting, fundic gland polyps (benign)

Uncommon

Dry mouth

Rare

Stomatitis, gastrointestinal candidiasis

Not known

Microscopic colitis

Hepatobiliary disorders

Uncommon

Increased liver enzymes

Rare

Hepatitis with or without jaundice

Very rare

Hepatic  failure,  encephalopathy  in  patients

 

 

 

 

with pre-existing liver disease

Skin    and      subcutaneous   tissue disorders

 Common

Administration site reactions*

Uncommon

Dermatitis, pruritus, rash, urticaria

Rare

Alopecia, photosensitivity

Very rare

Erythema multiforme, Stevens-Johnson syndrome, toxic epidermal necrolysis (TEN)

Not known

Subacute cutaneous lupus erythematosus (see section 4.4)

Musculoskeletal       and       connective

tissue disorders

Uncommon

Fracture of the hip, wrist or spine (see section

4.4)

Rare

Arthralgia, myalgia

Very rare

Muscular weakness

Renal and urinary disorders

Very rare

Interstitial  nephritis:  in  some  patients,  renal failure has been reported concomitantly

Reproductive system             and             breast disorders

Very rare

Gynaecomastia

General disorders and administration site conditions

Rare

Malaise, increased sweating

*Administration site reactions have mainly been observed in a study with high-dose exposure over

 

3 days (72 hours) (see section 5.3).

 

Irreversible visual impairment has been reported in isolated cases of critically ill patients who have received omeprazole (the racemate) intravenous injection, especially at high doses, but no causal relationship has been established.

Reportingofsuspectedadversereactions

If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. You can also report side effects directly (see details below). By reporting side affects; you can help provide more information on the safety of this medicine.

Saudi Arabia:

The National Pharmacovigilance and Drug Safety Centre (NPC)
o Fax: +966-11-205-7662
o Call NPC at +966-11-2038222, Exts: 2317-2356-2353-2354-2334-2340.
o Toll free phone: 8002490000
o E-mail: npc.drug@sfda.gov.sa
o Website: www.sfda.gov.sa/npc

 o Other GCC States:

Please contact the relevant competent authority.


 

There is very limited experience to date with deliberate overdose. The symptoms described in connection with an oral dose of 280 mg were gastrointestinal symptoms and weakness. Single oral doses of 80 mg esomeprazole and intravenous doses of 308 mg esomeprazole over 24 hours were uneventful. No specific antidote is known. Esomeprazole is extensively plasma protein bound and is therefore not readily dialyzable. As in any case of overdose, treatment should be symptomatic and general supportive measures should be utilised.


Pharmacotherapeutic group: Drugs for acid-related disorders, proton pump inhibitor

ATC code: A02BC05

Esomeprazole is the S-isomer of omeprazole and reduces gastric acid secretion through a specific targeted mechanism of action. It is a specific inhibitor of the acid pump in the parietal cell. Both the R- and S-isomer of omeprazole have similar pharmacodynamic activity.

Mechanismofaction

Esomeprazole is a weak base and is concentrated and converted to the active form in the highly acidic environment of the secretory canaliculi of the parietal cell, where it inhibits the enzyme

H+K+-ATPase – the acid pump and inhibits both basal and stimulated acid secretion. Pharmacodynamiceffects

After 5 days of oral dosing with 20 mg and 40 mg of esomeprazole, intragastric pH above 4 was maintained for a mean time of 13 hours and 17 hours respectively, over 24 hours in symptomatic GERD patients. The effect is similar irrespective of whether esomeprazole is administered orally or intravenously.

Using AUC as a surrogate parameter for plasma concentration, a relationship between inhibition of acid secretion and exposure has been shown after oral administration of esomeprazole.

During intravenous administration of 80 mg esomeprazole as a bolus infusion over 30 minutes followed by a continuous intravenous infusion of 8 mg/h for 23.5 hours, intragastric pH above 4, and pH above 6 was maintained for a mean time of 21 hours and 11-13 hours, respectively, over 24 hours in healthy subjects.

Healing of reflux esophagitis with esomeprazole 40 mg occurs in approximately 78% of patients after 4 weeks, and in 93% after 8 weeks of oral treatment.

In a randomised, double blind, placebo-controlled clinical study, patients with endoscopically confirmed peptic ulcer bleeding characterised as Forrest Ia, Ib, IIa or IIb (9%, 43%, 38% and 10% respectively) were randomised to receive Esomeprazole Sodium for Injection solution for infusion (n=375) or placebo (n=389). Following endoscopic haemostasis, patients received either 80 mg esomeprazole as an intravenous infusion over 30 minutes followed by a continuous infusion of 8 mg per hour or placebo for 72 hours. After the initial 72 hour period, all patients received open- label 40 mg oral Esomeprazole Sodium for Injection for 27 days for acid suppression. The occurrence of rebleeding within 3 days was 5.9% in the Esomeprazole Sodium for Injection treated group compared to 10.3% for the placebo group. At 30 days post-treatment, the occurrence of rebleeding in the Esomeprazole Sodium for Injection treated versus the placebo treated group was

7.7% vs 13.6%.

During treatment with antisecretory medicinal products, serum gastrin increases in response to the decreased acid secretion. Also CgA increases due to decreased gastric acidity. The increased CgA level may interfere with investigations for neuroendocrine tumours. Available published evidence suggests that proton pump inhibitors should be discontinued between 5 days and 2 weeks prior to CgA measurements. This is to allow CgA levels that might be spuriously elevated following PPI treatment to return to reference range.

An increased number of ECL cells possibly related to the increased serum gastrin levels, have been observed in both children and adults during long-term treatment with esomeprazole. The findings are considered to be of no clinical significance.

During long-term oral treatment with antisecretory medicinal products, gastric glandular cysts have been reported to occur at a somewhat increased frequency. These changes are a physiological consequence of pronounced inhibition of acid secretion, are benign and appear to be reversible. Decreased gastric acidity due to any means including proton pump inhibitors, increases gastric counts of bacteria normally present  in the  gastrointestinal tract.  Treatment with proton pump inhibitors may lead to slightly increased risk of gastrointestinal infections such as Salmonella and Campylobacter and, in hospitalised patients, possibly also Clostridium difficile.                 

Paediatricpopulation

In a placebo-controlled study (98 patients aged 1-11 months) efficacy and safety in patients with signs and symptoms of GERD were evaluated. Esomeprazole 1 mg/kg once daily was given orally for 2 weeks (open-label phase) and 80 patients were included for an additional 4 weeks (doubleblind, treatment-withdrawal phase). There was no significant difference between esomeprazole and placebo for the primary endpoint time to discontinuation due to symptom worsening.

In a placebo-controlled study (52 patients aged < 1 month) efficacy and safety in patients with symptoms of GERD were evaluated. Esomeprazole 0.5 mg/kg once daily was given orally for a minimum of 10 days. There was no significant difference between esomeprazole and placebo in the primary endpoint, change from baseline of number of occurrences of symptoms of GERD.

Results from the paediatric studies further show that 0.5 mg/kg and 1.0 mg/kg esomeprazole in < 1 month old and 1 to 11 month old infants, respectively, reduced the mean percentage of time with intra-oesophageal pH < 4.

The safety profile appeared to be similar to that seen in adults.

In a study in paediatric GERD patients (<1 to 17 years of age) receiving long-term PPI treatment, 61% of the children developed minor degrees of ECL cell hyperplasia with no known clinical significance and with no development of atrophic gastritis or carcinoid tumours


Distribution

The apparent volume of distribution at steady state in healthy subjects is approximately 0.22 l/kg body weight. Esomeprazole is 97% plasma protein bound.

Biotransformation

Esomeprazole is completely metabolised by the cytochrome P450 system (CYP). The major part of the metabolism of esomeprazole is dependent on the polymorphic CYP2C19, responsible for the formation of the hydroxy- and desmethyl metabolites of esomeprazole. The remaining part is dependent on another specific isoform, CYP3A4, responsible for the formation of esomeprazole sulphone, the main metabolite in plasma.

Elimination

The parameters below reflect mainly the pharmacokinetics in individuals with a functional CYP2C19 enzyme, extensive metabolisers.

Total plasma clearance is about 17 l/h after a single dose and about 9 l/h after repeated administration. The plasma elimination half-life is about 1.3 hours after repeated once daily dosing. Esomeprazole is completely eliminated from plasma between doses with no tendency for accumulation during once daily administration.

The major metabolites of esomeprazole have no effect on gastric acid secretion. Almost 80% of an oral dose of esomeprazole is excreted as metabolites in the urine, the remainder in the faeces. Less than 1% of the parent medicinal product is found in urine.

Linearity/non-linearity

Total exposure (AUC) increases with repeated administration of esomeprazole. This increase is dose-dependent and results in a non-linear dose-AUC relationship after repeated administration. This time- and dose-dependency is due to a decrease of first pass metabolism and systemic clearance probably caused by inhibition of the CYP2C19 enzyme by esomeprazole and/or its sulphone metabolite.

Following repeated doses of 40 mg administered as intravenous injections, the mean peak plasma concentration is approx. 13.6 micromol/l. The mean peak plasma concentration after corresponding oral doses is approx. 4.6 micromol/l. A smaller increase (of approx 30%) can be seen in total exposure after intravenous administration compared to oral administration. There is a dose-linear increase in total exposure following intravenous administration of esomeprazole as a 30-minute infusion (40 mg, 80 mg or 120 mg) followed by a continuous infusion (4 mg/h or 8 mg/h) over 23.5 hours.

Specialpatientpopulations

Poormetabolisers

Approximately 2.9 ±1.5% of the population lacks a functional CYP2C19 enzyme and is called poor metabolisers. In these individuals, the metabolism of esomeprazole is probably mainly catalysed by CYP3A4. After repeated once daily administration of 40 mg oral esomeprazole, the mean total exposure was approximately 100% higher in poor metabolisers than in subjects with a functional CYP2C19 enzyme (extensive metabolisers). Mean peak plasma concentrations were increased by about 60%. Similar differences have been seen for intravenous administration of esomeprazole.

These findings have no implications for the posology of esomeprazole.

Gender

Following a single oral dose of 40 mg esomeprazole the mean total exposure is approximately 30% higher  in  females  than  in  males.  No  gender  difference  is  seen  after  repeated  once  daily administration.   Similar   differences   have   been   observed   for   intravenous   administration   of esomeprazole. These findings have no implications for the posology of esomeprazole.          

Hepaticimpairment

The metabolism of esomeprazole in patients with mild to moderate liver dysfunction may be impaired. The metabolic rate is decreased in patients with severe liver dysfunction resulting in a doubling of the total exposure of esomeprazole. Therefore, a maximum dose of 20 mg should not be exceeded in GERD patients with severe dysfunction. For patients with bleeding ulcers and severe liver impairment, following an initial bolus dose of 80 mg, a maximum continuous intravenous infusion dose of 4 mg/h for 71.5 hours may be sufficient. Esomeprazole or its major metabolites do not show any tendency to accumulate with once daily dosing.

Renalimpairment

No studies have been performed in patients with decreased renal function. Since the kidney is responsible for the excretion of the metabolites of esomeprazole but not for the elimination of the parent compound, the metabolism of esomeprazole is not expected to be changed in patients with impaired renal function.

Elderly

The metabolism of esomeprazole is not significantly changed in elderly subjects (71-80 years of age).

Paediatricpopulation

In a randomised, open-label, multi-national, repeated dose study, esomeprazole was given as a once-daily 3-minute injection over four days. The study included a total of 59 paediatric patients 0 to 18 years old of which 50 patients (7 children in the age group 1 to 5 years) completed the study and were evaluated for the pharmacokinetics of esomeprazole.

The table below describes the systemic exposure to esomeprazole following the intravenous administration as a 3-minute injection in paediatric patients and adult healthy subjects. The values in the table are geometric means (range). The 20 mg dose for adults was given as a 30-minute infusion. The Css, max was measured 5 minutes post-dose in all paediatric groups and 7 minutes post- dose in adults on the 40 mg dose, and after stop of infusion in adults on the 20 mg dose.

Age group

Dose group

AUC (µmol*h/l)

Css,max (µmol/l)

0-1 month*

0.5 mg/kg (n=6)

7.5 (4.5-20.5)

3.7 (2.7-5.8)

1-11 months*

1.0 mg/kg (n=6)

10.5 (4.5-22.2)

8.7 (4.5-14.0)

 

 

1-5 years

10 mg (n=7)

7.9 (2.9-16.6)

9.4 (4.4-17.2)

6-11 years

10 mg (n=8)

6.9 (3.5-10.9)

5.6 (3.1-13.2)

20 mg (n=8)

 

20 mg (n=6)**

14.4 (7.2-42.3)

 

10.1 (7.2-13.7)

8.8 (3.4-29.4)

 

8.1 (3.4-29.4)

12-17 years

20 mg (n=6)

8.1 (4.7-15.9)

7.1 (4.8-9.0)

40 mg (n=8)

17.6 (13.1-19.8)

10.5 (7.8-14.2)

Adults

20 mg (n=22)

5.1 (1.5-11.8)

3.9 (1.5-6.7)

40 mg (n=41)

12.6 (4.8-21.7)

8.5 (5.4-17.9)

* A patient in the age group 0 up to 1 month was defined as a patient with a corrected age of ≥32

complete weeks and <44 complete weeks, where corrected age was the sum of the gestational age and the age after birth in complete weeks. A patient in the age group 1 to 11 months had a corrected age of ≥44 complete weeks.

** Two patients excluded, 1 most likely a CYP2C19 poor metaboliser and 1 on concomitant treatment with a CYP3A4 inhibitor.

Model based predictions indicate that Css,max following intravenous administration of esomeprazole as a 10 minute, 20 minute and 30 minute infusions will be reduced by on average 37% to 49%, 54% to 66% and 61% to 72%, respectively, across all age and dose groups compared to when the dose is administered as a 3 minute injection.


Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction and development. Adverse reactions not observed in clinical studies, but seen in animals at exposure levels similar to clinical exposure levels and with possible relevance to clinical use were as follows:

Oral carcinogenicity studies in the rat with the racemic mixture have shown gastric ECL-cell hyperplasia and carcinoids. These gastric effects are the result of sustained, pronounced hypergastrinaemia secondary to reduced production of gastric acid, and are observed after long- term treatment in the rat with inhibitors of gastric acid secretion. In the non-clinical program for esomeprazole intravenous formulation there was no evidence of vaso-irritation but a slight tissue inflammatory reaction at the injection site after subcutaneous (paravenous) injection was noted (see section 4.8).


Disodium Edetate, Sodium hydroxide and water for injection.


This medicinal product must not be used with other medicinal products except 0.9% Sodium

Chloride.


2 Years in all climate zones. Shelf-life after reconstitution Chemical and physical in-use stability has been demonstrated for 12°hours at 30°C. From a microbiological point of view, the product should be used immediately.

Store below 30ºC. Protect from Light.


Glass vials 


NA


Saudi Hetero Lab Aljameah Street, Malaz quarter, Riyadh 11441 Saudi Arabia Tel: +966 11 477 2215 Manufacture: Aspiro Pharma, Hyderabad, India

14/10/2019
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