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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)

MONTEK is a leukotriene receptor antagonist that blocks substances called leukotrienes. Leukotrienes cause narrowing and swelling of airways in your lungs.

By blocking leukotrienes, MONTEK improves asthma symptoms and helps control asthma.

Your doctor has prescribed MONTEK to treat your child’s asthma, preventing asthma symptoms during the day and night.

·         MONTEK is used for the treatment patients who are not adequately controlled on their medication and need additional therapy.

·         MONTEK may also be used as an alternative treatment to be inhaled corticosteroids for patients who have not recently taken oral corticosteroids for their asthma and have shown that they are unable to use inhaled corticosteroids.

·         MONTEK also helps prevent the narrowing of airways triggered by exercise for patients 2 years of age and older.

Your doctor will determine how MONTEK should be used depending on the symptoms and severity of your child's asthma.

What is asthma?

Asthma is a long-term disease.

Asthma includes:

·         Difficulty breathing because of narrowed airways. This narrowing of airways worsens and improves in response to various conditions.

·         Sensitive airways that react to many things, such as cigarette smoke, pollen, cold air, or exercise.

·         Swelling (inflammation) in the lining of the airways.

Symptoms of asthma include coughing, wheezing, and chest tightness.


Tell your doctor about any medical problems or allergies your child has now or has had.

Do not give MONTEK to your child if he/she

·         Is allergic (hypersensitive) to montelukast or any of the other ingredients of MONTEK (see 6. Further information).

Warning and precautions

·         If your child’s asthma or breathing gets worse, tell your doctor immediately.

·         MONTEK is not meant to treat acute asthma attacks. If an attack occurs, follow the instructions your doctor has given you for your child. Always have your child’s inhaled rescue medicine for asthma attacks with you.

·         It is important that your child take all asthma medications prescribed by your doctor. MONTEK should not be used instead of other asthma medications your doctor has prescribed for your child.

·         Any patient on anti-asthma medicines, be aware that if he/she develops a combination of symptoms such as flu-like illness, pins and needles or numbness of arms or legs, worsening of pulmonary symptoms, and/or rash, you should consult your doctor.

·         You or your child should not take acetyl-salicylic acid (aspirin) or other anti-inflammatory medicines (also known as non-steroidal anti-inflammatory drugs or NSAIDs) if they make his/her asthma worse.

Children and adolescents

Do not give this medicine to children less than 2 years of age.

Taking other medicines

Please tell your doctor or pharmacist if your child is taking or has recently taken other medicines, including those obtained without a prescription.

Some medicines may affect how these tablets works, or these tablets may affect how your child’s other medicines work.

Tell your doctor if your child is taking the following medicines before starting this medicine:

·         Phenobarbital (used for treatment of epilepsy)

·         Phenytoin (used for treatment of epilepsy)

·         Rifampicin (used to treat tuberculosis and some other infections)

Taking MONTEK with food and drink

These tablets should not be taken immediately with food; they should be taken at least 1 hour before or two hours after food.

Pregnancy and breast-feeding

Use in pregnancy

Women who are pregnant or intend to become pregnant should consult their doctor before taking this medicine. Your doctor will assess whether you can take this medicine during this time.

Use in breast-feeding

It is not known if montelukast appears in breast milk. You should consult your doctor before taking this medicine if you are breast-feeding or intend to breast-feed.

Driving and using machines

This subsection is not applicable for the MONTEK 4mg chewable tablets since they are intended for use in children 2 to 5 years of age, however the following information is relevant to the active ingredient, montelukast.

This medicine is not expected to affect your ability to drive a car or operate machinery. However, individual responses to medication may vary. Certain side effects (such as dizziness and drowsiness) that have been reported very rarely with these tablets may affect some patients’ ability to drive or operate machinery.

Important information about some of the ingredients of MONTEK

MONTEK 4 mg chewable tablets contain aspartame, a source of phenylalanine. If your child has phenylketonuria (a rare, hereditary disorder of the metabolism) you should take this into account that each 4 mg chewable tablet contains phenylalanine.


Always have your child take this medicine as your doctor has told you. You should check with your child’s doctor or pharmacist if you are not sure.

·         Your child should take only one tablet of this tablets once a day as prescribed by your doctor.

·         It should be taken even when your child has no symptoms or if he/she has an acute asthma attack.

·         This medicine is for oral use.

·         The tablets are to be chewed before swallowing.

For children 2 to 5 years of age:

One MONTEK 4 mg chewable tablet daily to be taken in the evening. The tablet should not be taken immediately with food; it should be taken at least 1 hour before or 2 hours after food.

For children 6 to 14 years old

MONTEK 5 mg chewable tablets are available. The tablet should not be taken immediately with food; it should be taken at least 1 hour before or 2 hours after food. If your child is taking this medicine, be sure that he/she does not take any other medicines that contain the same active ingredient, montelukast.

If your child takes more MONTEK than he/she should

Contact your child’s doctor immediately for advice. There were no side effects reported in the majority of overdose reports.

The most frequently occurring symptoms reported with overdose in adults and children included abdominal pain, sleepiness, thirst, headache, vomiting, and hyperactivity.

If you forget to give MONTEK to your child

Try to take this medicine as prescribed. However, if your child misses a dose, just resume the usual schedule of one tablet once daily. Do not give a double dose to make up for a forgotten dose.

If your child stops taking MONTEK

This medicine can treat your child’s asthma only if your child continues taking it. It is important for your child to continue taking MONTEK for as long as your doctor prescribes. It will help control your child’s asthma.

If you have any further questions on the use of this product, ask your child’s doctor or pharmacist.


Like all medicines, this medicine can cause side effects, although not everybody gets them.

In clinical studies with montelukast 4 mg chewable tablets, the most reported side effects (occurring in up to 1 in 10 children) thought to be related to montelukast chewable tablets were:

·          Abdominal pain

·          Thirst

Additionally, the following side effect was reported in clinical studies with montelukast 10 mg film-coated tablets and montelukast 5 mg chewable tablets:

·          Headache

These were usually mild and occurred at a greater frequency in patients treated with montelukast tablets than placebo (a pill containing no medication).

Serious side effects

Talk with your doctor immediately if you notice any of the following side effects, which may be serious, and for which you may need urgent medical treatment.

Uncommon (may affect up to 1 in 100 people)

·          Allergic reactions including swelling of the face, lips, tongue, and/or throat which may cause difficulty in breathing or swallowing

·          Behavior and mood related changes: agitation including aggressive behavior or hostility, depression

·          Seizure

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

·          Increased bleeding tendency

·          Tremor

·          Fast or irregular heartbeats (Palpitations)

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

•          Combination of symptoms such as flu-like illness, pins and needles or numbness of arms and legs, worsening of pulmonary symptoms and/or rash (Churg-Strauss syndrome).

•          Low blood platelet count.

•          Behavior and mood related changes: hallucinations, disorientation, suicidal thoughts and actions.

•          Swelling (inflammation) of the lungs.

•          Severe skin reactions (erythema multiforme) that may occur without warning.

•          Inflammation of the liver (hepatitis).

Other side effects while montelukast has been in the market

Very common: (may affect more than 1 in 10 people)

·          Upper respiratory infection

Common (may affect up to 1 in 10 people)

·          Diarrhea, nausea, vomiting

·          Rash

·          Fever

·          Elevated liver enzymes

Uncommon (may affect up to 1 in 100 people)

•          Behavior and mood related changes: dream abnormalities, including nightmares, trouble sleeping, sleepwalking, irritability, feeling anxious, restlessness.

•          Dizziness, drowsiness, pins and needles/numbness.

•          Nosebleed.

•          Dry mouth, indigestion.

•          Bruising, itching, hives.

•          Joint or muscle pain, muscle cramps.

•          Bedwetting in children.

•          Weakness/tiredness, feeling unwell, swelling.

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

•          Behavior and mood related changes: disturbance in attention, memory impairment, uncontrolled muscle movements.

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

•          Tender red lumps under the skin, most commonly on your shins (erythema nodosum).

Ask your doctor or pharmacist for more information about side effects. If any of the side effects gets serious, or if you notice any side effects not listed, please tell your doctor or pharmacist.

To report any side effect(s):

•  Saudi Arabia:

-      The National Pharmacovigilance Centre (NPC)

o  Fax: +966-11-205-7662

o  SFDA Call Center: 19999

o  E-mail: npc.drug@sfda.gov.sa

o  Website: https://ade.sfda.gov.sa

•  Other GCC States:

Please contact the relevant competent authority.


Keep out of the reach and sight of children.

Do not store above 30ºC

Do not use MONTEK after the expiry date which is stated on the carton and on the blister after EXP. The expiry date refers to the last day of that month.

Medicines should not be disposed of via wastewater or household waste. Ask your pharmacist how to dispose of medicines no longer required. These measures will help to protect the environment.


•          The active substance is montelukast. Each tablet contains montelukast sodium which corresponds to 4 mg of montelukast.

•          The other ingredients are mannitol, microcrystalline cellulose, hydroxypropyl cellulose, iron oxide red, croscarmellose sodium, cherry flavor, aspartame (E 951) and magnesium stearate.


MONTEK 4 mg chewable tablets are pink, flat, round, with bevel edges, engraved with ‘M4’ on one side and plain on the other. Available in packages of 30 chewable tablets

AJA Pharmaceutical Industries Company, Ltd.

Hail Industrial City MODON, Street No 32

PO Box 6979, Hail 55414

Kingdom of Saudi Arabia


04/2021
  نشرة الدواء تحت مراجعة الهيئة العامة للغذاء والدواء (اقرأ هذه النشرة بعناية قبل البدء في استخدام هذا المنتج لأنه يحتوي على معلومات مهمة لك)

مونتك هو مضاد لمستقبل ليوكوتراين الذي يعمل على حصر مواد تدعى ليوكوتراينات. تؤدي الليوكوتراينات إلى تضيّق وتورم المجاري الهوائية في الرئة، عن طريق حصر الليوكوتراينات، يخفف مونتك من أعراض الربو ويساعد في السيطرة عليه.

وصف الطبيب مونتك لعلاج الربو لدى طفلك ومنع [HAM1] حدوث اعراض هذا المرض خلال النهار والليل. 

•          يستخدم هذا الدواء لعلاج المرضى الذين لم يتم السيطرة على الربو لديهم باستخدام أدويتهم الحالية وبحاجة إلى علاج إضافي.

•          قد يستخدم هذا الدواء أيضا كعلاج بديل عن الستيرويدات القشرية المستنشقة للمرضى الذين لم يتناولوا مؤخراً الستيرويدات القشرية عن طريق الفم لعلاج الربو وأظهروا عدم قدرتهم على استخدام الستيرويدات القشرية المستنشقة.

•          يساعد هذا الدواء أيضا للوقاية من حدوث تضيق المجاري الهوائية الناتج عن القيام بالتمارين الرياضية. 

سيحدد طبيبك كيفية استخدام هذا الدواء وذلك اعتماداً على الأعراض وشدة حالة الربو الذي تعاني منه [HAM2] أنت وطفلك. 

ما هو الربو؟ 

الربو هو عبارة مرض طويل الأمد.

يتضمن الربو:

•          صعوبة في التنفس نتيجة لتضيق المجاري الهوائية. يزداد تضيق المجاري الهوائية سوءاً ويتحسن استجابةً لظروف متعددة.

•          المجاري الهوائية الحساسة التي تتأثر بعوامل عدة، مثل دخان السجائر، غبار الطلع، الهواء البارد، أو التمارين الرياضية.

•          تورم (التهاب) في بطانة المجاري الهوائية.

تتضمن أعراض الربو: السعال، أزيز تنفسي، الإحساس بضيق في الصدر.

 [HAM1]لقد وصف الطبيب مونتك لعلاج الربو لدى طفلك ولمنع

 [HAM2]التي تعاني منها

ابلغ طبيبك عن أي مشاكل صحية او حساسيه يعاني منها طفلك حاليا او سبق ان عانى منها.

موانع تناول مونتك

•          إذا كان الطفل يعاني من الحساسية لمونتيلوكاست أو أي من مكونات مونتك (المذكورة في الفقرة رقم-6)

التحذيرات والاحتياطات

•          إذا أصبح مرض الربو أو التنفس اسوأ، يجب عليك ابلاغ الطبيب فوراً.

•          مونتك غير مخصص لعلاج نوبات الربو الحادة. فإذا حصلت نوبة حادة فعليك اتباع تعليمات الطبيب الذي حددها لطفلك. ويجب عليك الاحتفاظ بالدواء البخاخ للحلق في متناولك من اجل استخدامه عند تعرض الطفل للنوبات الحادة.

•          من المهم أن تعطي لطفلك جميع أدوية الربو التي وصفها له الطبيب. ويجب عدم تناول مونتك كبديل عن أي أدوية أخرى وصفها الطبيب لطفلك لعلاج الربو.

•          أي مريض يتناول ادوية لعلاج الربو يجب أن يكون حذراً في حالة الإصابة بمجموعة من الأعراض مثل مرض يشبه الإنفلونزا، الإحساس بوخز خفيف، أو تنمل في الذراعين أو القدمين، زيادة حالة الأعراض التنفسية سوءاً، و/أو طفح، يجب عليك استشارة الطبيب.

•          يجب ان لا يتناول طفلك حامض الأستيل سالساليك (الأسبرين) او الأدوية المضادة للالتهابات الأخرى (التي تسمى أيضا العقاقير غير السترويدية المضادة للإلتهاب "NSAID") إذا كانت تجعل مرض الربو أسوأ

الأطفال والمراهقين

لا تقم بإعطاء هذا الدواء للأطفال الذين تقل أعمارهم عن سنتين.

تناول أدوية أخرى مع مونتك

  الرجاء أن تخبر طبيبك أو الصيدلاني إذا كنت أنت أو طفلك تتناولان حالياً أو تناولتما مؤخراً أو قد تتناولان أدوية أخرى، بما في ذلك الأدوية التي يتم الحصول عليها دون وصفة طبية.

قد تؤثر بعض الأدوية على آلية عمل هذه الأقراص، أو قد تؤثر الأقراص على آلية عمل الأدوية الأخرى.

أخبر الطبيب إذا كنت أنت أو طفلك تتناولان حالياً إحدى الأدوية التالية قبل البدء بتناول هذا الدواء:

·         فينوباربيتال (يستخدم لعلاج الصرع).

·         فينيتوين (يستخدم لعلاج الصرع).

·         ريفامبيسين (يستخدم لعلاج مرض الدرن وبعض انواع العدوى الأخرى).

تناول مونتك مع الأطعمة والمشروبات

يجب عدم تناول مونتك مع الطعام مباشرة ويجب ان يؤخذ قبل ساعة واحدة من الطعام او بعده بساعتين.

الحمل والإرضاع

الاستخدام اثناء الحمل:

النساء الحوامل أو اللاتي يشتبه أنهن حوامل أو يخططن لحدوث الحمل يجب عليهن استشارة الطبيب قبل استخدام مونتك. والطبيب هو الذي يقرر ما إذا كانت المرأة يمكن ان تستخدم مونتك خلال ذلك.

الاستخدام اثناء الإرضاع:

لا يعرف ما إذا كان مونتيلوكاست يفرز في حليب الثدي. ويجب استشارة الطبيب قبل تناول هذا الدواء إذا كنت مرضع أو سوف تقومين بذلك.

قيادة المركبات واستخدام الآلات

هذا الجزء لا ينطبق على أقراص مونتك 4 ملجم القابلة للمضغ حيث إنها مخصصه لاستخدام من قبل الأطفال من سنتين إلى خمسة سنوات، ولكن تتعلق المعلومات التالية بالمادة الفعالة مونتيلوكاست.

لا يتوقع أن يؤثر هذا الدواء على قدرتك على قيادة المركبات او استخدام الآلات. ولكن قد تختلف الاستجابة لهذا الدواء من شخص لآخر. وقد ذكرت بعض التقارير حدوث أعراض جانبية معينة (مثل الدوار والنعاس) في حالات نادرة جداً عند تناول هذا الدواء فقد يؤثر في قدرة بعض المرضى على قيادة المركبات استخدام الآلات.

معلومات هامة عن بعض مكونات مونتك

أقراص مونتك 4 ملجم القابلة للمضغ تحتوي على اسبارتام وهو مصدر لمادة الفنيل آلانين فإذا كان طفلك يعاني من مشكلة نزول الفنيل كيتون في البول (وهي مشكلة وراثية في الاستقلاب الغذائي أو "الأيض") فيجب عليك أن تأخذ بعين الاعتبار أن كل قرص 4 ملجم قابل للمضغ يحتوي على الفنيل آلانين.

https://localhost:44358/Dashboard

يجب أن يتناول طفلك هذا الدواء حسب تعليمات الطبيب. لذا فيجب التواصل مع الطبيب أو الصيدلي في حال لم تكن متأكد.

•          يجب إعطاء قرص واحد للطفل في اليوم حسب تعليمات الطبيب.

•          ويجب ان يعطى طفلك الدواء، حتى لو لم تكن لديه أعراض أو نوبة ربو حادة.

•          يتم تناول هذا الدواء عن طريق الفم.

•          يتم مضغ الأقراص قبل البلع.

للأطفال من عمر 2 إلى 5 سنة

يعطى قرص واحد مونتك 4 ملجم القابل للمضغ للطفل في المساء. يجب عدم تناول مونتك مع الطعام مباشرة ويجب ان يؤخذ قبل ساعة واحدة من الطعام او بعده بساعتين.

للأطفال من عمر 6 إلى 14 سنة

قرص واحد مونتك 5 ملجم القابلة للمضغ. يجب عدم تناول مونتك مع الطعام مباشرة ويجب ان يؤخذ قبل ساعة واحدة من الطعام او بعده بساعتين. وإذا كان طفلك يتناول هذا الدواء فيجب عليك التحقق من أنه لا يستخدم أي ادوية أخرى تحتوي على نفس المادة الفعالة، مونتيلوكاست.

إذا تناول طفلك جرعة زائدة من مونتك

إذا تناول الطفل جرعة زائدة فيجب عليك الاتصال بالطبيب فوراً. لا توجد هناك أعراض جانبية لدى معظم حالات زيادة الجرعة التي وردت في التقارير.

الأعراض الأكثر شيوعاً المبلغ عنها والناتجة عن الجرعات الزائدة لدى البالغين والأطفال تشمل الألم في البطن، والنعاس، والعطش والصداع، والتقيؤ، وفرط النشاط الحركي.

إذا نسيت أن تعطي مونتك لطفلك

حاول دائما اعطاء هذا الدواء حسب التعليمات تماماً. ولكن إذا نسيت ان تعطي طفلك الجرعة المعتادة في وقتها فيجب عليك استئناف إعطائه الجرعات حسب الجدول المعتاد (مرة واحدة يوميا). ويجب ان لا تعطي الطفل أبداً جرعة مضاعفة لتعويض الجرعة التي نسيتها.

إذا توقف طفلك عن تناول مونتك

هذا الدواء يقوم بعلاج مرض الربو الذي يعاني منه طفلك إذا استمر على تناوله. فمن المهم ان يستمر الطفل في تناول مونتك إذا لم ينصح الطبيب بعكس ذلك، فهذا سيساعد في السيطرة على مرض الربو لدى الطفل.

وإذا كانت لديك أي اسئلة حول استخدام هذا المنتج عليك الاتصال بالطبيب أو الصيدلي.

كغيره من الأدوية يمكن أن يسبب بعض التأثيرات الجانبية مع انها لا تحدث لدى جميع الأشخاص.

في دراسات سريرية اجريت على مونتيلوكاست 4 ملجم أقراص القابلة للمضغ، كانت الأعراض الجانبية الأكثر شيوعاً التي تم الإبلاغ عنها (حدثت على الأقل لدى 1 من بين كل 10 مريض) والتي يعتقد أنها متعلقة بمونتيلوكاست كانت كما يلي:

•          ألم في البطن

•          عطش

كما وقد تم الإبلاغ عن العرض الجانبي التالي في دراسات سريرية على أقراص مونتيلوكاست 10 ملجم المغلفة وأقراص 5 ملجم القابلة للمضغ:

•          صداع

وكانت تلك الأعراض غالبا خفيفة وحدثت لدى مرضى الذين تم علاجهم باستخدام مونتيلوكاست بمعدلات اكبر مما كانت لدى مرضى تم علاجهم بلاسيبو (اقراص مشابهة لا تحتوي على أي دواء).

أعراض جانبية خطيرة

غير شائع (يؤثر على 1 من 100 أشخاص)

•          ردود فعل حساسية بما فيها ظهور طفح جلدي، تورم بالوجه، الشفتين، اللسان و/أو الحلق مما قد يتسبب في صعوبة التنفس أو البلع.

•          تغيرات ذات علاقة بالسلوك والمزاج: التهيج بما في ذلك السلوك العدواني، الارتعاش، الاكتئاب.

•          تشنجات (صرع).

نادر (يؤثر على 1 من 1,000 أشخاص)

•          زيادة القابلية للنزف.

•          رعشة.

•          خفقان بالقلب.

نادر جدا (يؤثر على 1 من 10,000 أشخاص)

•          مجموعة من الأعراض تشبه مرض الإنفلونزا، الإحساس بوخز خفيف أو تنمل في الذراعين والقدمين، ازدياد حالة الأعراض التنفسية سوءاً و/أو طفح (متلازمة شورج-ستروس).

•          نقص في تعداد الصفائح الدموية.

•          تغيرات مرتبطة بالسلوك والمزاج: هلوسة، ارتباك، التفكير في الانتحار والإقدام عليه.

•          تورم (التهاب) الرئتين.

•          تفاعلات جلدية خطيرة (حمامى متعددة الأشكال) التي قد تحدث دون سابق إنذار.

•          التهاب الكبد.

تم تسجيل أعراض جانبية أخرى بعد تسويق لمونتيلوكاست

شائعة جداً (قد تؤثر على أكثر من 1 من كل 10 أشخاص)

•          التهاب الجهاز التنفسي العلوي.

شائعة (قد تؤثر على 1 من كل 10 أشخاص)

•          إسهال، غثيان، قيء.

•          طفح جلدي.

•          حمّى.

•          ارتفاع مستوى إنزيمات الكبد.

غير شائعة (قد تؤثر على 1 من كل 100 شخص)

•          تغيرات مرتبطة بالسلوك والمزاج: أحلام غير طبيعية، تشمل كوابيس، مشاكل في النوم، المشي أثناء النوم، هياج، الشعور بالقلق، الشعور بعدم الراحة.

•          الشعور بالدوار، النعاس، الإحساس بوخز خفيف/تنمل.

•          نزيف الأنف.

•          جفاف الفم، عسر الهضم.

•          كدمات، حكة، شرى.

•          ألم المفاصل أو العضلات، معص عضلي.

•          تبول الأطفال في الفراش.

•          الشعور بضعف/تعب، الشعور بالمرض، تورم.

نادرة (قد تؤثر على شخص أو أقل من كل 1,000 شخص)

•          تغيرات مرتبطة بالسلوك والمزاج: اضطرابات التركيز، قصور الذاكرة، حركات لا إرادية في العضلات.

نادرة جداً (قد تؤثر على شخص أو أقل من كل 10,000 شخص)

•          بروز كتل حمراء تحت الجلد على الساقين (الحمامى العقدة).

اسأل طبيبك أو الصيدلي لمعلومات إضافية عن الأعراض الجانبية. إذا ازدادت أي من هذه الأعراض سوءًا أو لاحظت أعراض أخرى لم تذكر في هذه النشرة، تواصل مع طبيبك أو الصيدلي.

للإبلاغ عن الأعراض الجانبية:

•         المملكة العربية السعودية:

-       المركز الوطني للتيقظ الدوائي

o        فاكس 7662-205-11-966+

o        الهاتف الموحد: 19999

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

o        الموقع الإلكتروني: https://ade.sfda.gov.sa  

 

•         دول مجلس التعاون الخليجي الأخرى:

الرجاء الاتصال بالمؤسسات والهيئات الوطنية لكل دولة.

احفظ هذا الدواء بعيدا عن مرأى ومتناول الأطفال.

يحفظ في درجة حرارة لا تزيد عن 30 درجة مئوية.

لا تتناول مونتك بعد تاريخ انتهاء صلاحيته المطبوع على العلبة وهو يشير إلى آخر يوم في ذلك الشهر.

يجب عدم إلقاء أي أدوية في مياه الصرف الصحي او في النفايات المنزلية. وعليك ان تسأل الصيدلي عن كيفية التخلص من الأدوية التي لا تحتاجها. وهذه التدابير تساعد على حماية البيئة.

•   المادة الفعالة هي مونتيلوكاست. كل قرص يحتوي على مونتيلوكاست صوديوم ما يعادل 4 ملجم من "مونتيلوكاست".

•  المكونات الأخرى هي مانيتول، سيليولوز مبلور دقيق، هيدروكسي بروبيل سيليولوز، اكسيد الحديد الأحمر، كروسكارميلوز صوديوم، نكهة الكرز، اسبارتام (E951)، ستيارات المغنيسيوم.

أقراص مونتك 4 ملجم القابلة للمضغ هي اقراص بلون وردي مستديرة ومسطحة وذات حواف مشطوفه، منقوش على أحد جانبها ’4M’ والجانب الآخر سادة.

تتوفر بعبوة من 30 قرص قابل للمضغ.

شركة آجا للصناعات الصيدلانية

المدينة الصناعية مدن بحائل، شارع رقم 32

حائل 55414، ص.ب. 6979

المملكة العربية السعودية

04/2021
 Read this leaflet carefully before you start using this product as it contains important information for you

MONTEK 4 mg chewable Tablets

Each chewable tablet contains montelukast sodium, which is equivalent to 4 mg montelukast. Excipients with known effect: This medicine contains aspartame (E 951). For the full list of excipients, see section 6.1.

Chewable tablet. Pink, flat, round, with bevel edges, engraved with ‘4’ on one side and plain on the other.

MONTEK is indicated in the treatment of asthma as add-on therapy in those 2- to 5-year- old patients with mild to moderate persistent asthma who are inadequately controlled on inhaled corticosteroids and in whom “as-needed” short-acting β-agonists provide inadequate clinical control of asthma.

MONTEK may also be an alternative treatment option to low-dose inhaled corticosteroids for 2- to 5-year-old patients with mild persistent asthma who do not have a recent history of serious asthma attacks that required oral corticosteroid use, and who have demonstrated that they are not capable of using inhaled corticosteroids (see section 4.2).

MONTEK is also indicated in the prophylaxis of asthma from 2 years of age and older in which the predominant component is exercise-induced bronchoconstriction.


Posology

This medicinal product is to be given to a child under adult supervision. The recommended dose for pediatric patients 2-5 years of age is one 4 mg chewable tablet daily to be taken in the evening. If taken in connection with food, MONTEK should be taken 1 hour before or 2 hours after food. No dosage adjustment within this age group is necessary.

General recommendations

The therapeutic effect of MONTEK on parameters of asthma control occurs within one day. Patients should be advised to continue taking MONTEK even if their asthma is under control, as well as during periods of worsening asthma.

 

No dosage adjustment is necessary for patients with renal insufficiency, or mild to moderate hepatic impairment. There are no data on patients with severe hepatic impairment. The dosage is the same for both male and female patients.

MONTEK as an alternative treatment option to low-dose inhaled corticosteroids for mild, persistent asthma

Montelukast is not recommended as monotherapy in patients with moderate persistent asthma. The use of montelukast as an alternative treatment option to low-dose inhaled corticosteroids for children with mild persistent asthma should only be considered for patients who do not have a recent history of serious asthma attacks that required oral corticosteroid use and who have demonstrated that they are not capable of using inhaled corticosteroids (see section 4.1). Mild persistent asthma is defined as asthma symptoms more than once a week but less than once a day, nocturnal symptoms more than twice a month but less than once a week, normal lung function between episodes. If satisfactory control of asthma is not achieved at follow-up (usually within one month), the need for an additional or different anti-inflammatory therapy based on the step system for asthma therapy should be evaluated. Patients should be periodically evaluated for their asthma control.

MONTEK as prophylaxis of asthma for 2 to 5 years old patients in whom the predominant component is exercise-induced bronchoconstriction

In 2 to 5 years old patients, exercise-induced bronchoconstriction may be the predominant manifestation of persistent asthma that requires treatment with inhaled corticosteroids. Patients should be evaluated after 2 to 4 weeks of treatment with montelukast. If satisfactory response is not achieved, an additional or different therapy should be considered.

Therapy with MONTEK in relation to other treatments for asthma

When treatment with MONTEK is used as add-on therapy to inhaled corticosteroids, MONTEK should not be abruptly substituted for inhaled corticosteroids (see section 4.4). 10 mg film-coated tablets are available for adults and adolescents 15 years of age and older.

Pediatric population

Do not give MONTEK 4 mg chewable tablets to children less than 2 years of age. The safety and efficacy of MONTEK 4 mg chewable tablets in children less than 2 years of age has not been established.

MONTEK 5 mg chewable tablets are available for pediatric patients 6 to 14 years of age. Method of administration

Oral use.

The tablets are to be chewed before swallowing.

 


Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.

Patients should be advised never to use oral montelukast to treat acute asthma attacks and to keep their usual appropriate rescue medication for this purpose readily available. If an acute attack occurs, a short-acting inhaled β-agonist should be used. Patients should seek their doctors' advice as soon as possible if they need more inhalations of short-acting β- agonists than usual.

Montelukast should not be abruptly substituted for inhaled or oral corticosteroids.

There are no data demonstrating that oral corticosteroids can be reduced when montelukast is given concomitantly.

In rare cases, patients on therapy with anti-asthma agents including montelukast may present with systemic eosinophilia, sometimes presenting with clinical features of vasculitis consistent with Churg-Strauss syndrome, a condition which is often treated with systemic corticosteroid therapy. These cases have been sometimes associated with the reduction or withdrawal of oral corticosteroid therapy. Although a causal relationship with leukotriene receptor antagonism has not been established, physicians should be alert to eosinophilia, vasculitic rash, worsening pulmonary symptoms, cardiac complications, and/or neuropathy presenting in their patients. Patients who develop these symptoms should be reassessed and their treatment regimens evaluated.

Treatment with montelukast does not alter the need for patients with aspirin-sensitive asthma to avoid taking aspirin and other non-steroidal anti-inflammatory drugs.

MONTEK contains aspartame, a source of phenylalanine. Patients with phenylketonuria should take into account that each 4 mg chewable tablet contains phenylalanine in an amount equivalent to 0.674 mg phenylalanine per dose.

Neuropsychiatric Events

Serious neuropsychiatric (NP) events have been reported with use of montelukast. These post-marketing reports have been highly variable and included, but were not limited to, agitation, aggressive behavior or hostility, anxiousness, depression, disorientation, disturbance in attention, dream abnormalities, dysphemia (stuttering), hallucinations, insomnia, irritability, memory impairment, obsessive-compulsive symptoms, restlessness, somnambulism, suicidal thoughts and behavior (including suicide), tic, and tremor. NP events have been reported in adult, adolescent, and pediatric patients with and without a previous history of psychiatric disorder. NP events have been reported mostly during montelukast treatment, but some were reported after montelukast discontinuation. Animal studies showed that montelukast distributes into the brain in rats [see Clinical Pharmacology (12.3)]; however, the mechanisms underlying montelukast -associated NP events are currently not well understood. Based upon the available data, it is difficult to identify risk factors for or quantify the risk of NP events with montelukast use.

Because of the risk of NP events, the benefits of montelukast may not outweigh the risks in some patients, particularly when the symptoms of disease may be mild and adequately treated with alternative therapies. Reserve use of montelukast for patients with allergic rhinitis who have an inadequate response or intolerance to alternative therapies [see

 

Indications and Usage (1.3)]. In patients with asthma or exercise-induced bronchoconstriction, consider the benefits and risks before prescribing montelukast.

Discuss the benefits and risks of montelukast use with patients and caregivers when prescribing montelukast. Advise patients and/or caregivers to be alert for changes in behavior or for new NP symptoms when taking montelukast. If changes in behavior are observed, or if new NP symptoms or suicidal thoughts and/or behavior occur, advise patients to discontinue montelukast and contact a healthcare provider immediately. In many cases, symptoms resolved after stopping montelukast therapy; however, in some cases symptoms persisted after discontinuation of montelukast. Therefore, continue to monitor and provide supportive care until symptoms resolve. Re-evaluate the benefits and risks of restarting treatment with montelukast if such events occur.


Montelukast may be administered with other therapies routinely used in the prophylaxis and chronic treatment of asthma. In drug-interactions studies, the recommended clinical dose of montelukast did not have clinically important effects on the pharmacokinetics of the following medicinal products: theophylline, prednisone, prednisolone, oral contraceptives (ethinyl estradiol/norethindrone 35/1), terfenadine, digoxin and warfarin.

The area under the plasma concentration curve (AUC) for montelukast was decreased approximately 40% in subjects with co-administration of phenobarbital. Since montelukast is metabolized by CYP 3A4, 2C8, and 2C9, caution should be exercised, particularly in children, when montelukast is co-administered with inducers of CYP 3A4, 2C8, and 2C9, such as phenytoin, phenobarbital and rifampicin.

In vitro studies have shown that montelukast is a potent inhibitor of CYP 2C8. However, data from a clinical drug-drug interaction study involving montelukast and rosiglitazone (a probe substrate representative of medicinal products primarily metabolized by CYP 2C8) demonstrated that montelukast does not inhibit CYP 2C8 in vivo. Therefore, montelukast is not anticipated to markedly alter the metabolism of medicinal products metabolized by this enzyme (e.g., paclitaxel, rosiglitazone, and repaglinide).

In vitro studies have shown that montelukast is a substrate of CYP 2C8, and to a less significant extent, of 2C9, and 3A4. In a clinical drug-drug interaction study involving montelukast and gemfibrozil (an inhibitor of both CYP 2C8 and 2C9) gemfibrozil increased the systemic exposure of montelukast by 4.4-fold. No routine dosage adjustment of montelukast is required upon co-administration with gemfibrozil or other potent inhibitors of CYP 2C8, but the physician should be aware of the potential for an increase in adverse reactions.

Based on in vitro data, clinically important drug interactions with less potent inhibitors of CYP 2C8 (e.g., trimethoprim) are not anticipated. Co-administration of montelukast with itraconazole, a strong inhibitor of CYP 3A4, resulted in no significant increase in the systemic exposure of montelukast.


Pregnancy

Animal studies do not indicate harmful effects with respect to effects on pregnancy or embryonal/fetal development.

Available data from published prospective and retrospective cohort studies with montelukast use in pregnant women evaluating major birth defects have not established a drug-associated risk. Available studies have methodologic limitations, including small sample size, in some cases retrospective data collection, and inconsistent comparator groups.

MONTEK may be used during pregnancy only if it is considered to be clearly essential. Breast-feeding

Studies in rats have shown that montelukast is excreted in milk (see section 5.3). It is unknown whether montelukast/metabolites are excreted in human milk.

MONTEK may be used in breast-feeding mothers only if it is considered to be clearly essential.


MONTEK has no or negligible influence on the ability to drive and use machines. However, individuals have reported drowsiness or dizziness.


Montelukast has been evaluated in clinical studies in patients with persistent asthma as follows:

•   10 mg film-coated tablets in approximately 4,000 adult and adolescent patients 15 years of age and older

•  5 mg chewable tablets in approximately 1,750 pediatric patients 6 to 14 years of age, and

•  4 mg chewable tablets in 851 pediatric patients 2 to 5 years of age.

Montelukast has been evaluated in a clinical study in patients with intermittent asthma as follows:

The following drug-related adverse reactions in clinical studies were reported commonly (≥1/100 to <1/10) in patients treated with montelukast and at a greater incidence than in patients treated with placebo:

 

 

 

Body System Class

 

Adult and Adolescent Patients 15 years and older (two 12-week studies; n=795)

Pediatric Patients 6 to 14 years old

(one 8-week study; n=201)

(two 56-week studies; n=615)

Pediatric Patients 2 to 5 years old

(one 12-week study; n=461)

(one 48-week study; n=278)

 

Nervous system disorders

headache

headache

 

Gastro-intestinal disorders

abdominal pain

 

abdominal pain

General disorders and administration site conditions

 

 

 

thirst

With prolonged treatment in clinical trials with a limited number of patients for up to 2 years for adults, and up to 12 months for pediatric patients 6 to 14 years of age, the safety profile did not change.

Cumulatively, 502 pediatric patients 2 to 5 years of age were treated with montelukast for at least 3 months, 338 for 6 months or longer, and 534 patients for 12 months or longer. With prolonged treatment, the safety profile did not change in these patients either.

Tabulated list of Adverse Reactions

Adverse reactions reported in post-marketing use are listed, by System Organ Class and specific Adverse Reactions, in the table below. Frequency Categories were estimated based on relevant clinical trials.

System Organ Class

Adverse Reactions

Frequency Category*

Infections and infestations

upper respiratory infection†

Very Common

Blood      and      lymphatic      system disorders

increased bleeding tendency

Rare

 

thrombocytopenia

Very Rare

 

Immune system disorders

hypersensitivity reactions including anaphylaxis

Uncommon

hepatic eosinophilic infiltration

Very Rare

 

 

 

 

 

Psychiatric disorders

dream abnormalities including nightmares,                          insomnia, somnambulism, anxiety, agitation including aggressive behavior or hostility, depression, psychomotor hyperactivity (including irritability, restlessness, tremor§)

 

 

 

Uncommon

disturbance   in    attention,   memory impairment, tic

Rare

hallucinations,              disorientation, suicidal     thinking     and     behavior

Very Rare

     

 

 

(suicidality),     obsessive-compulsive symptoms, dysphemia

 

Nervous system disorders

dizziness,                          drowsiness, paraesthesia/hypoesthesia, seizure

Uncommon

Cardiac disorders

palpitations

Rare

 

Respiratory,     thoracic mediastinal disorders

 

and

epistaxis

Uncommon

Churg-Strauss Syndrome (CSS) (see section 4.4)

Very Rare

pulmonary eosinophilia

Very Rare

Gastro-intestinal disorders

diarrhea‡, nausea‡, vomiting‡

Common

dry mouth, dyspepsia

Uncommon

 

 

Hepatobiliary disorders

elevated        levels        of transaminases (ALT, AST)

serum

Common

hepatitis (including cholestatic, hepatocellular, and mixed-pattern liver injury).

 

Very Rare

 

 

Skin and subcutaneous tissue disorders

rash‡

Common

bruising, urticaria, pruritus

Uncommon

angioedema

Rare

erythema        nodosum, multiforme

erythema

Very Rare

Musculoskeletal                 and connective tissue disorders

arthralgia, myalgia including muscle cramps

Uncommon

Renal and urinary disorders

enuresis in children

Uncommon

General        disorders        and administration site conditions

pyrexia‡

Common

asthenia/fatigue, malaise, edema

Uncommon

*Frequency Category: Defined for each Adverse Reaction by the incidence reported in the clinical trials data base: 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).

†This adverse experience, reported as Very Common in the patients who received

montelukast, was also reported as Very Common in the patients who received placebo in clinical trials.

‡This adverse experience, reported as Common in the patients who received montelukast,

was also reported as Common in the patients who received placebo in clinical trials.

§ Frequency Category: Rare

Reporting of suspected adverse reactions

 

Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system.

To report any side effect(s):

•         Saudi Arabia:

-      The National Pharmacovigilance Centre (NPC)

o Fax: +966-11-205-7662

o  SFDA Call Center: 19999

o  E-mail: npc.drug@sfda.gov.sa

o  Website: https://ade.sfda.gov.sa

 

 
  

•         Other GCC states:

Please contact the relevant competent authority.


In chronic asthma studies, montelukast has been administered at doses up to 200 mg/day to adult patients for 22 weeks and in short-term studies, up to 900 mg/day to patients for approximately one week without clinically important adverse experiences.

There have been reports of acute overdose in post-marketing experience and clinical studies with montelukast. These include reports in adults and children with a dose as high as 1,000 mg (approximately 61 mg/kg in 42 months old child). The clinical and laboratory findings observed were consistent with the safety profile in adults and pediatric patients. There were no adverse experiences in the majority of overdose reports.

Symptoms of overdose

The most frequently occurring adverse experiences were consistent with the safety profile of montelukast and included abdominal pain, somnolence, thirst, headache, vomiting, and psychomotor hyperactivity.

Management of overdose

No specific information is available on the treatment of overdose with montelukast. It is not known whether montelukast is dialysable by peritoneal- or haemo-dialysis.


Pharmacotherapeutic group: Leukotriene receptor antagonist ATC-Code: R03D C03

Mechanism of action

The cysteinyl leukotrienes (LTC4, LTD4, LTE4) are potent inflammatory eicosanoids released from various cells including mast cells and eosinophils. These important pro- asthmatic mediators bind to cysteinyl leukotriene receptors (CysLT) found in the human

 

airway and cause airway actions, including bronchoconstriction, mucous secretion, vascular permeability, and eosinophil recruitment.

Pharmacodynamic effects

Montelukast is an orally active compound which binds with high affinity and selectivity to the CysLT1 receptor. In clinical studies, montelukast inhibits bronchoconstriction due to inhaled LTD4 at doses as low as 5 mg. Bronchodilation was observed within 2 hours of oral administration. The bronchodilation effect caused by a β-agonist was additive to that caused by montelukast. Treatment with montelukast inhibited both early- and late-phase bronchoconstriction due to antigen challenge. Montelukast, compared with placebo, decreased peripheral blood eosinophils in adult and pediatric patients. In a separate study, treatment with montelukast significantly decreased eosinophils in the airways (as measured in sputum). In adult and pediatric patients 2 to 14 years of age, montelukast, compared with placebo, decreased peripheral blood eosinophils while improving clinical asthma control.

Clinical efficacy and safety

In studies in adults, montelukast, 10 mg once daily, compared with placebo, demonstrated significant improvements in morning FEV1 (10.4% vs 2.7% change from baseline), AM peak expiratory flow rate (PEFR) (24.5 L/min vs 3.3 L/min change from baseline), and significant decrease in total β-agonist use (-26.1% vs -4.6% change from baseline). Improvement in patient-reported daytime and nighttime asthma symptoms scores was significantly better than placebo.

Studies in adults demonstrated the ability of montelukast to add to the clinical effect of inhaled corticosteroid (% change from baseline for inhaled beclomethasone plus montelukast vs beclomethasone, respectively for FEV1: 5.43% vs 1.04%; β-agonist use: - 8.70% vs 2.64%). Compared with inhaled beclomethasone (200 μg twice daily with a spacer device), montelukast demonstrated a more rapid initial response, although over the 12-week study, beclomethasone provided a greater average treatment effect (% change from baseline for montelukast vs beclomethasone, respectively for FEV1: 7.49% vs 13.3%; β-agonist use: -28.28% vs -43.89%). However, compared with beclomethasone, a high percentage of patients treated with montelukast achieved similar clinical responses (e.g., 50% of patients treated with beclomethasone achieved an improvement in FEV1 of approximately 11% or more over baseline while approximately 42% of patients treated with montelukast achieved the same response).

In a 12-week, placebo-controlled study in pediatric patients 2 to 5 years of age, montelukast

4 mg once daily improved parameters of asthma control compared with placebo irrespective of concomitant controller therapy (inhaled/nebulized corticosteroids or inhaled/nebulized sodium cromoglycate). Sixty percent of patients were not on any other controller therapy. Montelukast improved daytime symptoms (including coughing, wheezing, trouble breathing and activity limitation) and nighttime symptoms compared with placebo. Montelukast also decreased “as needed” β-agonist use and corticosteroid rescue for worsening asthma compared with placebo. Patients receiving montelukast  had

 

more days without asthma than those receiving placebo. A treatment effect was achieved after the first dose.

In a 12-month, placebo-controlled study in pediatric patients 2 to 5 years of age with mild asthma and episodic exacerbations, montelukast 4 mg once daily significantly (p≤0.001) reduced the yearly rate of asthma exacerbation episodes (EE) compared with placebo (1.60 EE vs. 2.34 EE, respectively), [EE defined as ≥3 consecutive days with daytime symptoms requiring β-agonist use, or corticosteroids (oral or inhaled), or hospitalization for asthma]. The percentage reduction in yearly EE rate was 31.9%, with a 95% CI of 16.9, 44.1.

In a placebo-controlled study in pediatric patients 6 months to 5 years of age who had intermittent asthma but did not have persistent asthma, treatment with montelukast was administered over a 12-month period, either as a once-daily 4 mg regimen or as a series of 12-day courses that each were started when an episode of intermittent symptoms began. No significant difference was observed between patients treated with montelukast 4 mg or placebo in the number of asthma episodes culminating in an asthma attack, defined as an asthma episode requiring utilization of health-care resources such as an unscheduled visit to a doctor's office, emergency room, or hospital; or treatment with oral, intravenous, or intramuscular corticosteroid.

In an 8-week study in pediatric patients 6 to 14 years of age, montelukast 5 mg once daily, compared with placebo, significantly improved respiratory function (FEV1 8.71% vs 4.16% change from baseline; AM PEFR 27.9 L/min vs 17.8 L/min change from baseline) and decreased “as-needed” β-agonist use (-11.7% vs +8.2% change from baseline).

In a 12-month study comparing the efficacy of montelukast to inhaled fluticasone on asthma control in pediatric patients 6 to 14 years of age with mild persistent asthma, montelukast was non-inferior to fluticasone in increasing the percentage of asthma rescue- free days (RFDs), the primary endpoint. Averaged over the 12-month treatment period, the percentage of asthma RFDs increased from 61.6 to 84.0 in the montelukast group and from

60.9 to 86.7 in the fluticasone group. The between group difference in LS mean increase in the percentage of asthma RFDs was statistically significant (-2.8 with a 95% CI of -4.7,

-0.9), but within the limit pre-defined to be clinically not inferior. Both montelukast and fluticasone also improved asthma control on secondary variables assessed over the 12 months treatment period:

FEV1 increased from 1.83 L to 2.09 L in the montelukast group and from 1.85 L to 2.14 L in the fluticasone group. The between-group difference in LS mean increase in FEV1 was

-0.02 L with a 95% CI of -0.06, 0.02. The mean increase from baseline in % predicted FEV1 was 0.6% in the montelukast treatment group, and 2.7% in the fluticasone treatment group. The difference in LS means for the change from baseline in the %  predicted  FEV1 was significant: -2.2% with a 95% CI of -3.6, -0.7.

The percentage of days with β-agonist use decreased from 38.0 to 15.4 in the montelukast group, and from 38.5 to 12.8 in the fluticasone group. The between group difference in LS means for the percentage of days with β-agonist use was significant: 2.7 with a 95% CI of 0.9, 4.5.

 

The percentage of patients with an asthma attack (an asthma attack being defined as a period of worsening asthma that required treatment with oral steroids, an unscheduled visit to the doctor's office, an emergency room visit, or hospitalization) was 32.2 in the montelukast group and 25.6 in the fluticasone group; the odds ratio (95% CI) being significant: equal to 1.38 (1.04, 1.84).

The percentage of patients with systemic (mainly oral) corticosteroid use during the study period was 17.8% in the montelukast group and 10.5% in the fluticasone group. The between group difference in LS means was significant: 7.3% with a 95% CI of 2.9; 11.7.

Significant reduction of exercise-induced bronchoconstriction (EIB) was demonstrated in a 12-week study in adults (maximal fall in FEV1 22.33% for montelukast vs 32.40% for placebo; time to recovery to within 5% of baseline FEV1 44.22 min vs 60.64 min). This effect was consistent throughout the 12-week study period. Reduction in EIB was also demonstrated in a short-term study in pediatric patients 6 to 14 years of age (maximal fall in FEV1 18.27% vs 26.11%; time to recovery to within 5% of baseline FEV1 17.76 min vs

27.98 min). The effect in both studies was demonstrated at the end of the once-daily dosing interval.

In aspirin-sensitive asthmatic patients receiving concomitant inhaled and/or oral corticosteroids, treatment with montelukast, compared with placebo, resulted in significant improvement in asthma control (FEV1 8.55% vs -1.74% change from baseline and decrease in total β-agonist use -27.78% vs 2.09% change from baseline).


Absorption

Montelukast is rapidly absorbed following oral administration. For the 10 mg film-coated tablet, the mean peak plasma concentration (Cmax) is achieved 3 hours (Tmax) after administration in adults in the fasted state. The mean oral bioavailability is 64%. The oral bioavailability and Cmax are not influenced by a standard meal. Safety and efficacy were demonstrated in clinical trials where the 10 mg film-coated tablet was administered without regard to the timing of food ingestion.

For the 5 mg chewable tablet, the Cmax is achieved in 2 hours after administration in adults in the fasted state. The mean oral bioavailability is 73% and is decreased to 63% by a standard meal.

After administration of the 4 mg chewable tablet to pediatric patients 2 to 5 years of age in the fasted state, Cmax is achieved 2 hours after administration. The mean Cmax is 66% higher while mean Cmin is lower than in adults receiving a 10 mg tablet.

Distribution

Montelukast is more than 99% bound to plasma proteins. The steady-state volume of distribution of montelukast averages 8-11 liters. Studies in rats with radiolabelled montelukast indicate minimal distribution across the blood-brain barrier. In addition, concentrations of radiolabelled material at 24 hours post-dose were minimal in all other tissues.

 

Biotransformation

Montelukast is extensively metabolized. In studies with therapeutic doses, plasma concentrations of metabolites of montelukast are undetectable at steady state in adults and children.

Cytochrome P450 2C8 is the major enzyme in the metabolism of montelukast. Additionally, CYP 3A4 and 2C9 may have a minor contribution, although itraconazole, an inhibitor of CYP 3A4, was shown not to change pharmacokinetic variables of montelukast in healthy subjects that received 10 mg montelukast daily. Based on in vitro results in human liver microsomes, therapeutic plasma concentrations of montelukast do not inhibit cytochromes P450 3A4, 2C9, 1A2, 2A6, 2C19, or 2D6. The contribution of metabolites to the therapeutic effect of montelukast is minimal.

Elimination

The plasma clearance of montelukast averages 45 ml/min in healthy adults. Following an oral dose of radiolabelled montelukast, 86% of the radioactivity was recovered in 5-day faecal collections and <0.2% was recovered in urine. Coupled with estimates of montelukast oral bioavailability, this indicates that montelukast and its metabolites are excreted almost exclusively via the bile.

Characteristics in Patients

No dosage adjustment is necessary for the elderly or mild to moderate hepatic insufficiency. Studies in patients with renal impairment have not been undertaken. Because montelukast and its metabolites are eliminated by the biliary route, no dose adjustment is anticipated to be necessary in patients with renal impairment. There are no data on the pharmacokinetics of montelukast in patients with severe hepatic insufficiency (Child-Pugh score >9).

With high doses of montelukast (20- and 60-fold the recommended adult dose), a decrease in plasma theophylline concentration was observed. This effect was not seen at the recommended dose of 10 mg once daily.


In animal toxicity studies, minor serum biochemical alterations in ALT, glucose, phosphorus and triglycerides were observed which were transient in nature. The signs of toxicity in animals were increased excretion of saliva, gastro-intestinal symptoms, loose stools and ion imbalance. These occurred at dosages which provided >17-fold the systemic exposure seen at the clinical dosage. In monkeys, the adverse effects appeared at doses from 150 mg/kg/day (>232-fold the systemic exposure seen at the clinical dose). In animal studies, montelukast did not affect fertility or reproductive performance at systemic exposure exceeding the clinical systemic exposure by greater than 24-fold. A slight decrease in pup body weight was noted in the female fertility study in rats at 200 mg/kg/day (>69-fold the clinical systemic exposure). In studies in rabbits, a higher incidence of incomplete ossification, compared with concurrent control animals, was seen at systemic exposure >24-fold the clinical systemic exposure seen at the clinical dose. No

 

abnormalities were seen in rats. Montelukast has been shown to cross the placental barrier and is excreted in breast milk of animals.

No deaths occurred following a single oral administration of montelukast sodium at doses up to 5,000 mg/kg in mice and rats (15,000 mg/m2 and 30,000 mg/m2 in mice and rats, respectively), the maximum dose tested. This dose is equivalent to 25,000 times the recommended daily adult human dose (based on an adult patient weight of 50 kg).

Montelukast was determined not to be phototoxic in mice for UVA, UVB or visible light spectra at doses up to 500 mg/kg/day (approximately >200-fold based on systemic exposure).

Montelukast was neither mutagenic in in vitro and in vivo tests nor tumorigenic in rodent species.

 


  Mannitol

Microcrystalline cellulose

Hydroxypropyl cellulose

Iron oxide red

Croscarmellose sodium

Cherry flavor

Aspartame (E 951)

Magnesium stearate


Not applicable.


2 years.

Do not store above 30°C


Alu/Alu blister packs, each containing 30 chewable tablets


Any unused medicinal product or waste material should be disposed of in accordance with local requirements.


AJA Pharmaceutical Industries Company, Ltd. Hail Industrial City MODON, Street No 32 PO Box 6979, Hail 55414 Kingdom of Saudi Arabia Tel: +966 11 268 7900

04 April 2021
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