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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)

Bucaine contains a medicine called bupivacaine hydrochloride. It belongs to a group of medicines called local anaesthetics.

Bucaine is used to numb (anaesthetise) parts of the body. It is used to stop pain happening or to provide pain relief. It can be used to:

  • Numb parts of the body during surgery in adults and children above 12 years.
  • Relieve pain in adults, infants and children above 1 year of age.

You must not be given Bucaine

  • If you are allergic to bupivacaine hydrochloride or any of the other ingredients of this medicine (listed in section 6).
  • If you are allergic to any other local anaesthetics of the same class (such as lidocaine or ropivacaine).
  • If you have a skin infection near to where the injection will be given.
  • If you have something called cardiogenic shock (a condition where the heart is unable to supply enough blood to the body).
  • If you have something called hypovolaemic shock (very low blood pressure leading to collapse).
  • If you have problems with clotting of your blood.
  • If you have diseases of the brain or spine such as meningitis, polio or spondylitis.
  • If you have a severe headache caused by bleeding inside the head (intracranial haemorrhage).
  • If you have problems with your spinal cord due to anaemia.
  • If you have blood poisoning (septicaemia).
  • If you have had a recent trauma, tuberculosis or tumours of the spine.

You must not be given Bucaine if any of the above apply to you. If you are not sure, talk to your doctor or nurse before you are given Bucaine.

Warnings and precautions
Talk to your doctor or nurse before having Bucaine:

  • If you have heart, kidney or liver problems. This is because your doctor may need to adjust the dose of Bucaine. Problems with your liver enzymes. This may happen if you have long-term treatment with this medicine.
  • If you have a swollen stomach due to more fluid than normal.
  • If you have a stomach tumour.
  • If you have been told that you have decreased volume of blood (hypovolaemia).
  • If you have fluid in your lungs.

Children
In children aged less than 12 years as some injections of bupivacaine in order to numb parts of the body during surgery are not established in younger children. The use of bupivacaine is not established in children less than 1 year of age.

If you are not sure if any of the above apply to you, talk to your doctor or nurse before you are given Bucaine.

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

In particular, tell your doctor if you are taking any of the following medicines:

  • Medicines used to treat an uneven heart beat (arrhythmia) such as lidocaine, mexiletine or amiodarone.
  • Medicines used to stop blood clots (anti-coagulants).

Your doctor needs to know about these medicines to be able to work out the correct dose of Bucaine for you.

Pregnancy and breast-feeding
If you are pregnant or breast-feeding, think that you may be pregnant or are planning to have a baby, ask your doctor for advice before taking this medicine.

Driving and using machines
Bucaine may make you feel sleepy and affect the speed of your reactions. After you have been given Bucaine, you should not drive or use tools or machines until the next day.

Bucaine contains sodium
Bucaine contains sodium. Each ml of Bucaine 0.25 % and 0.5% Solution for Injection contains 0.137 mmol (3.151 mg) sodium (main component of cooking/table salt). This is equivalent to 0.15% of the recommended maximum daily dietary intake of sodium for an adult.


Bucaine will be given to you by a doctor. Your doctor will know the correct way to give you this medicine.

The dose that your doctor gives you will depend on the type of pain relief that you need and the part of your body that the medicine will be injected into. It will also depend on your body size, age, and physical condition. Usually one dose will last long enough but more doses may be given if the surgery takes a long time.

Bucaine will be given to you as an injection. The part of the body where you are injected will depend on why you are being given Bucaine. Your doctor will give you Bucaine in one of the following places:

  • Near to the part of the body that needs to be numbed.
  • In an area away from the part of the body that needs to be numbed. This is the case if you are given an epidural injection (an injection around the spinal cord).

When Bucaine is injected into the body in one of these ways, it stops the nerves from being able to pass pain messages to the brain. It will slowly wear off when the medical procedure is over.

If you have been given too much Bucaine
Serious side effects from getting too much bupivacaine are unlikely. They need special treatment and the doctor treating you is trained to deal with these situations. The first signs of being given too much bupivacaine are usually as follows:

  • Feeling dizzy or light-headed
  • Numbness of the lips and around the mouth.
  • Numbness of the tongue.
  • Hearing problems.
  • Problems with your sight (vision).

To reduce the risk of serious side effects, your doctor will stop giving you Bucaine as soon as these signs appear. This means that if any of these happen to you, or you think you have received too much Bucaine, tell your doctor immediately.

More serious side effects from being given too much bupivacaine include twitching of your muscles, fits (seizures), and loss of consciousness.

If you have any further questions on the use of this medicine, ask your doctor, pharmacist or nurse.


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

Severe allergic reactions (rare, may affect up to 1 in 1,000 people)
If you have a severe allergic reaction, tell your doctor immediately. The signs may include sudden onset of:

  • Swelling of your face, lips, tongue or throat. This may make it difficult to swallow.
  • Severe or sudden swelling of your hands, feet and ankles.
  • Difficulty breathing.
  • Severe itching of the skin (with raised lumps).

Other possible side effects:
Very common (may affect more than 1 in 10 people)

  • Low blood pressure. This might make you feel dizzy or light-headed.
  • Feeling sick (nausea).

Common (may affect up to 1 in 10 people)

  • Being sick (vomiting).
  • Feeling dizzy.
  • Pins and needles.
  • High blood pressure (hypertension).
  • Slow heartbeat.
  • Problems passing water.

Uncommon (may affect up to 1 in 100 people)

  • Feeling light-headed.
  • Fits (seizures).
  • Numbness of the tongue or around the mouth.
  • Ringing in the ears or being sensitive to sound.
  • Difficulty speaking.
  • Blurred sight (vision).
  • Loss of consciousness.
  • Shaking (tremors).
  • Twitching of your muscles.

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

  • Double vision.
  • Nerve damage that may cause changes in sensation or muscle weakness (neuropathy). This may include peripheral nerve damage.
  • A condition called arachnoiditis (inflammation of the membrane that surrounds the spinal cord). The signs include a stinging or burning pain in the lower back or legs and tingling, numbness or weakness in the legs.
  • Weak or paralysed legs.
  • Uneven heart beat (arrhythmias). This could be life-threatening.
  • Slowed or stopped breathing or stopped heartbeat. This could be life-threatening.

Possible side effects seen with other local anaesthetics which might also be caused by bupivacaine include:

  • Problems with your liver enzymes. This may happen if you have long-term treatment with this medicine.
  • Damaged nerves. Rarely this may cause permanent problems.
  • Blindness which is not permanent or problems with the muscles of the eyes that are long-lasting. This may happen with some injections given around the eyes.

Do not be concerned by this list of possible side effects. You may not get any of them.


Keep out of the sight and reach of children.

Store below 30°C. Avoid freeze.

Store in the original package.

For single use only.

Discard any unused solution.

Do not use this medicine after the expiry date which is stated on the package after “EXP”. The expiry date refers to the last day of that month.

Do not use this medicine if you notice any visible signs of deterioration.

Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to throw away medicines you no longer use. These measures will help protect the environment.


The active substance is bupivacaine hydrochloride.

Each 20 ml of Bucaine 0.25% Solution for Injection contains 50 mg bupivacaine hydrochloride.

Each 20 ml of Bucaine 0.5% Solution for Injection contains 100 mg bupivacaine hydrochloride.

The other ingredients are sodium chloride, sodium hydroxide solution and/or hydrochloric acid solution and water for injection.


Bucaine 0.25% is a clear colorless solution in 20 ml clear glass vials sealed with white flip-off caps. Bucaine 0.5% is a clear colorless solution in 20 ml clear glass vials sealed with green flip-off caps. Pack size: 1 Vial (20 ml).

Marketing Authorization Holder
Jazeera Pharmaceutical Industries
Al-Kharj Road
P.O. Box 106229
Riyadh 11666, Saudi Arabia
Tel: + (966-11) 8107023, + (966-11) 2142472
Fax: + (966-11) 2078170
e-mail: SAPV@hikma.com

Manufacturer
Hikma Farmaceutica (Portugal), S.A.
Estrada do Rio Da Mó,
n.°8, 8A e 8B, Fervença
2705-906 Terrugem
Sintra, Portugal
Tel: + (351-2) 19608410
Fax: + (351-2) 19615102

Reporting of side effects
If you get any side effects, talk to your doctor, pharmacist or nurse. 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 also help provide more information on the safety of this medicine.

  • Saudi Arabia

The National Pharmacovigilance Centre (NPC)
SFDA Call Center: 19999
E-mail: npc.drug@sfda.gov.sa
Website: https://ade.sfda.gov.sa

  • Other GCC States

Please contact the relevant competent authority.


This leaflet was last revised in 06/2023; version number SA3.1.
  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 بيوكين على دواء يُسمى هيدروكلوريد البوبيفاكايين. وينتمي إلى مجموعة أدوية تُسمى أدوية التخدير الموضعية.

يُستخدم بيوكين لتخدير أجزاء من الجسم. حيث يُستخدم لإيقاف الألم أو لتخفيفه. ويمكن استخدامه في:

  • تخدير أجزاء من الجسم أثناء الجراحة للبالغين والأطفال فوق 12 سنة.
  • تخفيف الألم لدى البالغين، الرُضَّع والأطفال فوق عمر السنة.

يجب أن لا تعطى بيوكين

  • إذا كنت تعاني من حساسية اتجاه هيدروكلوريد البوبيفاكايين أو أي من المكونات الأخرى في هذا الدواء (المذكورة في القسم 6).
  • إذا كنت تعاني من حساسية اتجاه أي مخدر موضعي آخر من الفئة نفسها (مثل ليدوكايين أو روبيفاكايين).
  • إذا كنت تعاني من عدوى في الجلد قرب الموضع الذي ستعطى فيه الحقنة.
  • إذا كنت تعاني من حالة تُسمى الصدمة القلبية (حالة يكون القلب فيها غير قادر على إمداد الجسم بما يكفي من الدم).
  • إذا كنت تعاني من حالة تُسمى صدمة نقص حجم الدم (انخفاض شديد جدًا في ضغط الدم يؤدي إلى الإعياء).
  • إذا كنت تعاني من مشاكل في تجلط الدم.
  • إذا كنت تعاني من أمراض في الدماغ أو العمود الفقري مثل التهاب السحايا، شلل الأطفال أو التهاب الفقار.
  • إذا كنت تعاني من صداع شديد بسبب وجود نزيف داخل الرأس (نزيف داخل الجمجمة).
  • إذا كنت تعاني من مشاكل في الحبل الشوكي بسبب فقر الدم.
  • إذا كنت تعاني من تسمم في الدم (إنتان دمويّ).
  • إذا عانيت مؤخرًا من صدمة، مرض السل أو أورام العمود الفقري.

ينبغي أن لا تعطى بيوكين إذا كانت أي من الحالات المذكورة أعلاه تنطبق عليك. إذا لم تكن متأكدًا، فاستشر طبيبك أو الممرض قبل أن تعطى بيوكين.

الاحتياطات والتحذيرات
 تحدث مع طبيبك أو الممرض قبل أخذ بيوكين:

  • إذا كان لديك مشاكل في القلب، الكلى أو الكبد. وذلك لأن طبيبك قد يحتاج إلى تعديل جرعة بيوكين. مشاكل في إنزيمات الكبد. قد يحدث هذا إذا كان لديك علاج طويل الأمد مع هذا الدواء. 
  • إذا كنت تعاني من انتفاخ في المعدة بسبب وجود سوائل بالمعدة أكثر من الطبيعي.
  • إذا كنت تعاني من ورم في المعدة.
  • إذا علمت أن حجم الدم لديك منخفض (نقص حجم الدم).
  • إذا كنت تعاني من وجود سوائل في الرئتين.

الأطفال
لدى الأطفال بعمر أقل من 12 سنة حيث لم يتم إثبات استخدام بعض حُقن بوبيفاكايين لتخدير أجزاء الجسم أثناء الجراحة لدى الأطفال صغيري السن. لم يتم إثبات استخدام بوبيفاكايين لدى الأطفال بعمر أقل من سنة.

إذا لم تكن متأكدًا من أن أي من المذكور أعلاه ينطبق عليك، فتحدث إلى طبيبك أو الممرض قبل إعطائك بيوكين.

 الأدوية الأخرى وبيوكين
يرجى إبلاغ طبيبك إذا كنت تتناول، تناولت مؤخرًا أو قد تتناول أية أدوية أخرى. يشمل ذلك الأدوية التي تشتريها بدون وصفة علاجية والأدوية العشبية. وذلك لأن بيوكين يمكن أن يؤثر على مفعول الأدوية الأخرى، كما أنه يمكن لبعض الأدوية أن تؤثر على مفعول بيوكين.

أبلغ الطبيب إذا كنت تتناول أيًّ من الأدوية التالية على وجه الخصوص:

  • الأدوية التي تُستخدم لعلاج نبضات القلب غير المنتظمة (اضطراب النظم) مثل ليدوكايين، ميكسيليتين أو أميودارون.
  • الأدوية المستخدمة لإيقاف الجلطات الدموية (مضادات التخثر).

يجب أن يكون طبيبك على علم بهذه الأدوية حتى يتمكن من تحديد الجرعة الصحيحة لك من بيوكين.

 الحمل والرضاعة
إذا كنتِ حاملاً أو ترضعين، تعتقدين بأنكِ قد تكونين حاملاً أو تخططين لإنجاب طفل، فاستشيري طبيبكِ قبل أخذ هذا الدواء.

القيادة واستخدام الآلات
قد يجعلك بيوكين تشعر بالنعاس ويؤثر على سرعة ردود أفعالك. بعد أن يتم إعطاؤك بيوكين، يجب عليك تجنب القيادة أو استخدام الأدوات أو الآلات حتى اليوم التالي.

يحتوي بيوكين على الصوديوم
يحتوي بيوكين على الصوديوم. يحتوي كل مللتر من بيوكين 0,25% و0,5% محلول للحقن على 0,137 ملمول (3,151 ملغم) صوديوم (المكون الرئيسي لملح الطبخ/الطعام). هذا يكافئ 0,15% من القيمة الغذائية اليومية القصوى المسموح بها من الصوديوم للشخص البالغ.

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سوف تعطى بيوكين عن طريق الطبيب. سيحدد طبيبك الطريقة الصحيحة لإعطائك هذا الدواء.

سيعتمد مقدار الجرعة التي يعطيها لك طبيبك على نوع الألم المراد تخفيفه والجزء من جسمك الذي سيتم حقن الدواء فيه. كما سيعتمد أيضًا على حجم جسمك، عمرك، وحالتك البدنية. عادة يستمر مفعول الجرعة الواحدة لمدة كافية، إلا أنه يمكن إعطاء جرعات أكثر إذا استغرقت الجراحة مدة طويلة.

سوف يعطيك الطبيب بيوكين عن طريق الحقن. يعتمد اختيار الجزء من الجسم الذي سيتم الحقن فيه على سبب إعطائك بيوكين. سيعطيك طبيبك حقنة بيوكين في أحد الأماكن التالية:

  • قرب الجزء المراد تخديره من جسمك.
  • في منطقة بعيدة عن الجزء المراد تخديره من جسمك. وهذا في حالة حقنك بحقنة فوق الجافية (حقنة يتم حقنها حول الحبل الشوكي).

عندما يتم حقن بيوكين داخل الجسم بإحدى هذه الطرق، تتوقف قدرة الأعصاب على نقل رسائل الألم إلى المخ. وسيزول مفعول الحقنة ببطء عند انتهاء الإجراء الطبي.

إذا تم إعطاؤك بيوكين أكثر من اللازم
من غير المرجح حدوث آثار جانبية خطيرة عند أخذ بوبيفاكايين أكثر مما ينبغي. تتطلب هذه الاثار علاجًا خاصًا، حيث يكون الطبيب المعالج لك مدربًا على التعامل مع تلك الحالات. عادةً، تكون العلامات الأولى التي تدل على أخذ قدر كبير من بوبيفاكايين كالتالي:

  • الشعور بالدوخة أو بالدوار.
  • خدر في الشفتين وحول الفم.
  • خدر في اللسان.
  • وجود مشاكل في السمع.
  • وجود مشاكل في البصر (الرؤية).

للحد من خطورة هذه الآثار الجانبية الخطيرة، سيتوقف طبيبك عن إعطائك بيوكين بمجرد ظهور هذه العلامات. وهذا يعني أنه في حال حدوث أي منها لديك، أو في حال اعتقادك أنك أخذت أكثر مما ينبغي من بيوكين، يتوجب عليك إخبار طبيبك على الفور.

تشمل الآثار الجانبية الأكثر خطورة الناتجة من تلقي بوبيفاكايين بجرعة أكبر مما ينبغي ارتعاش العضلات، النوبات (النوبات التشنجية)، وفقدان الوعي.

إذا كانت لديك أي أسئلة إضافية عن استخدام هذا الدواء، استشر طبيبك، الصيدلي أو الممرض.

مثل جميع الأدوية، قد يسبب هذا الدواء آثارًا جانبيةً، إلا أنه ليس بالضرورة أن تحدث لدى جميع مستخدمي هذا الدواء.

ردود فعل تحسسية شديدة (نادرة، وقد تصيب ما يصل إلى شخص واحد من كل 1000 شخص)

إذا كنت تعاني من رد فعل تحسسي شديد، فيتوجب عليك إخبار طبيبك على الفور. قد تشمل العلامات حدوث مفاجئ لما يلي:

  • تورم الوجه، الشفتين، اللسان أو الحلق. الأمر الذي قد يسبب صعوبة البلع.
  • تورم يديك، قدميك، وكاحليك بشكل شديد أو مفاجئ.
  • صعوبة في التنفس.
  • حدوث حكة شديدة في الجلد (مع وجود كتل متورمة).

الآثار الجانبية المحتملة الأخرى:
شائعة جدًا (قد تصيب أكثر من شخص واحد من كل 10 أشخاص)

  • انخفاض ضغط الدم. قد يجعلك هذا تشعر بالدوخة أو الدوار.
  • الغثيان.

شائعة (قد تصيب ما يصل إلى شخص واحد من كل 10 أشخاص)

  • القيء.
  • الشعور بالدوخة.
  • الإحساس بالوخز (كالإبر والدبابيس).
  • ارتفاع ضغط الدم.
  • بطء نبضات القلب.
  • مشاكل في التبول.

غير شائعة (قد تصيب ما يصل إلى شخص واحد من كل 100 شخص)

  • الشعور بالدوار.
  • النوبات (النوبات التشنجية).
  • الشعور بخدر في اللسان وحول الفم.
  • طنين في الأذنين أو الحساسية تجاه الصوت.
  • صعوبة التحدث.
  • تغيم الرؤية.
  • فقدان الوعي.
  • ارتعاش (ارتجاف).
  • انتفاض العضلات.

نادرة (قد تصيب ما يصل إلى شخص واحد من كل 1000 شخص)

  • ازدواج الرؤية.
  • تلف الأعصاب الذي قد يسبب تغيرات في الإحساس أو ضعف العضلات (اعتلال عصبي). قد يشمل ذلك تلف الأعصاب المحيطية.
  • حدوث حالة تُسمى بالتهاب العنكبوتية (التهاب الغشاء الذي يحيط بالحبل الشوكي). تشمل العلامات الشعور بلسع أو ألم حارق في أسفل الظهر أو الساقين والشعور بوخز، خدر أو ضعف في الساقين.
  • ضعف الساقين أو إصابتهما بالشلل.
  • عدم انتظام نبضات القلب (اضطراب نظم القلب). وقد يكون هذا مهددًا للحياة.
  • بطء التنفس أو توقفه أو توقف نبضات القلب. وقد يكون هذا مهددًا للحياة.

الآثار الجانبية المحتملة التي شُوهدت مع مواد التخدير الموضعية الأخرى والتي قد يسببها أيضًا بوبيفاكايين والتي تشمل:

  • وجود مشاكل متعلقة بإنزيمات الكبد. قد يحدث هذا إذا كنت تُعالج بهذا الدواء على المدى الطويل.
  • تلف الأعصاب. نادرًا ما يسبب هذا مشاكل دائمة.
  • العمى والذي يكون غير دائم أو وجود مشاكل في عضلات العينين تدوم طويلاً. قد يحدث هذا مع بعض الحقن التي يتم حقنها حول العينين.

لا تقلق من قائمة الآثار الجانبية هذه. قد لا تصاب بأي من هذه الأعراض.

احفظ هذا الدواء بعيدًا عن مرأى ومتناول الأطفال.

يحفظ عند درجة حرارة أقل من 30° مئوية. تجنب التجميد.

يحفظ داخل العبوة الأصلية.

للاستخدام لمرة واحدة فقط.

تخلص من أي محلول غير مستخدم.

لا تستخدم هذا الدواء بعد تاريخ انتهاء الصلاحية المذكور على العبوة الخارجية بعد "EXP". يشير تاريخ انتهاء الصلاحية إلى اليوم الأخير من ذلك الشهر.

لا تستخدم هذا الدواء إذا لاحظت أي علامات تلف واضحة عليه.

لا تتخلص من أي أدوية عن طريق مياه الصرف الصحي أو النفايات المنزلية. اسأل الصيدلي عن كيفية التخلص من الأدوية التي لم تعد بحاجة إليها. هذه الإجراءات ستساعد في الحفاظ على سلامة البيئة.

المادة الفعالة هي هيدروكلوريد البوبيفاكايين.

يحتوي كل 20 مللتر من بيوكين 0,25% محلول للحقن على 50 ملغم هيدروكلوريد البوبيفاكايين.

يحتوي كل 20 مللتر من بيوكين 0,5% محلول للحقن على 100 ملغم هيدروكلوريد البوبيفاكايين.

المواد الأخرى المستخدمة في التركيبة التصنيعية هي كلوريد الصوديوم، محلول هيدروكسيد الصوديوم و/أو محلول حمض الهيدروكلوريك وماء معد للحقن.

بيوكين 0,25% محلول للحقن هو محلول صاف عديم اللون في زجاجات بحجم 20 مللتر شفافة، محكمة الإغلاق بأغطية بيضاء قابلة للفتح لأعلى.

بيوكين 0,5% محلول للحقن هو محلول صاف عديم اللون في زجاجات بحجم 20 مللتر شفافة، محكمة الإغلاق بأغطية خضراء قابلة للفتح لأعلى.

حجم العبوة: زجاجة واحدة (20 مللتر).

مالك رخصة التسويق
شركة الجزيرة للصناعات الدوائية
طريق الخرج
صندوق بريد 106229
الرياض 11666، المملكة العربية السعودية
هاتف: 8107023 (11-966) +، 2142472 (11-966) +
فاكس: 2078170 (11-966) +
البريد الإلكتروني: SAPV@hikma.com

الشركة المصنعة
شركة أدوية الحكمة (البرتغال)، المساهمة العامة المحدودة
إسترادا دو ريو دا مو،

2705-906 تيروجيم
سنترا، البرتغال
هاتف: 19608410 (2-351) +
فاكس: 19615102 (2-351) +

للإبلاغ عن الآثار الجانبية
تحدث إلى الطبيب، الصيدلي، أو الممرض إذا عانيت من أية آثار جانبية. وذلك يشمل أي آثار جانبية لم يتم ذكرها في هذه النشرة. كما أنه يمكنك الإبلاغ عن هذه الآثار مباشرةً (انظر التفاصيل المذكورة أدناه). من خلال الإبلاغ عن الآثار الجانبية، يمكنك المساعدة بتوفير معلومات مهمة عن سلامة الدواء.

  • المملكة العربية السعودية

المركز الوطني للتيقظ الدوائي
مركز الاتصال الموحد: 19999
البريد الإلكتروني: npc.drug@sfda.gov.sa
الموقع الإلكتروني:  https://ade.sfda.gov.sa

  • دول الخليج العربي الأخرى

الرجاء الاتصال بالجهات الوطنية في كل دولة.

تمت مراجعة هذه النشرة بتاريخ 06/2023؛ رقم النسخة SA3.1.
 Read this leaflet carefully before you start using this product as it contains important information for you

Bucaine 0.5% (100 mg/20 ml) Solution for Injection

Each ml contains 5 mg bupivacaine hydrochloride. Each 20 ml contains 100 mg bupivacaine hydrochloride. Excipient with known effect: Sodium. For the full list of excipients, see section 6.1.

Solution for injection. Clear colorless solution.

Bucaine 0.25% and 0.5% solutions are used for the production of local anaesthesia by percutaneous infiltration, peripheral nerve block(s) and central neural block (caudal or epidural), that is, for specialist use in situations where prolonged anaesthesia is required. Because sensory nerve block is more marked than motor block, Bucaine is especially useful in the relief of pain, e.g. during labour.

Bucaine is indicated for:

  • Surgical anaesthesia in adults and children above 12 years of age.
  • Acute pain management in adults, infants and children above 1 year of age.

The suggested dose and strength of solution appropriate for each indication are provided in Section 4.2.


Posology
Adults and children above 12 years of age
The following table is a guide to dosage for the more commonly used techniques in the average adult. The figures reflect the expected average dose range needed. Standard textbooks should be consulted for factors affecting specific block techniques and for individual patient requirements.

N.B. When prolonged blocks are used, either by continuous infusion or by repeated bolus administration, the risks of reaching a toxic plasma concentration or inducing a local neural injury must be considered.

The clinician's experience and knowledge of the patient's physical status is important in calculating the required dose. The lowest dose required for adequate anaesthesia should be used. Individual variations in onset and duration occur.

Table 1 Dosage recommendations for adults

 

Conc

mg/ml

Volume

ml

Dose

mg

Onset

min

Duration of effect

hours 7)

SURGICAL ANAESTHESIA

     

Lumbar Epidural Administration 1)

     

Surgery

5.0

15-30

75-150

15-30

2-3

Lumbar Epidural Administration 1)

     

Caesarean Section

5.0

15-30

75-150

15-30

2-3

Thoracic Epidural Administration 1)

     

Surgery

2.5

5.0

5-15

5-10

12.5-37.5

25-50

10-15

10-15

1.5-2

2-3

Caudal Epidural Block 1)

     
 

2.5

5.0

20-30

20-30

50-75

100-150

20-30

15-30

1-2

2-3

Major Nerve Block 2)

     

(e.g. brachial plexus, femoral, sciatic)

5.0

10-35

50-175

15-30

4-8

Field block

     

(e.g. minor nerve blocks and infiltration)

2.5

5.0

<60

≤ 30

<150

≤ 150

1-3

1-10

3-4

3-8

 

ACUTE PAIN MANAGEMENT

Conc

mg/ml

Volume

ml

Dose

mg

Onset

min

Duration of effect

hours 7)

Lumbar Epidural Administration

     

Intermittent injections 3)

(e.g. post-operative pain relief)

2.5

6-15;

minimum interval 30 minutes

15-37.5;

minimum interval 30 minutes

2-5

1-2

Lumbar Epidural Administration

     

Continuous infusion 4)

1.25

2.5

10-15/h

5-7.5/h

12.5-18.8/h

12.5-18.8/h

-

-

-

-

Lumbar Epidural Administration

     

Continuous infusion, labour pain relief 4)

1.25

5-10/h

6.25-12.5/h

-

-

Thoracic Epidural Administration

     

Continuous infusion 4)

1.25

2.5

5-10/h

4-7.5/h

6.3-12.5/h

10-18.8/h

-

-

-

-

Intra-Articular Block 6)

     

(e.g. single injection following knee arthroscopy)

2.5

≤40

≤1005)

5-10

2-4 h after wash out

Field Block

     

(e.g. minor nerve blocks and infiltration)

2.5

≤60

≤150

1-3

3-4

1) Dose includes test dose

2) The dose for a major nerve block must be adjusted according to site of administration and patient status. Interscalene and supraclavicular brachial plexus blocks may be associated with a higher frequency of serious adverse reactions, regardless of the local anaesthetic used, see also section 4.4.

3) In total ≤400 mg/24 h.

4) This solution is often used for epidural administration in combination with a suitable opioid for pain management. In total ≤400 mg/24 h.

5) If additional bupivacaine is used by any other techniques in the same patient, an overall dose limit of 150 mg should not be exceeded.

6) There have been post-marketing reports of chondrolysis in patients receiving post-operative intra-articular continuous infusion of local anaesthetics. Bupivacaine is not approved for this indication (see also section 4.4).

7) Bupivacaine without adrenaline.

In general, surgical anaesthesia (e.g. epidural administration) requires the use of higher concentrations and doses. When a less intense block is required (e.g. in the relief of labour pain), the use of a lower concentration is indicated. The volume of drug used will affect the extent of spread of anaesthesia.

In order to avoid intravascular injection, aspiration should be repeated prior to and during administration of the main dose, which should be injected slowly or in incremental doses, at a rate of 25-50 mg/min, while closely observing the patient's vital functions and maintaining verbal contact. An inadvertent intravascular injection may be recognised by a temporary increase in heart rate and an accidental intrathecal injection by signs of a spinal block. If toxic symptoms occur, the injection should be stopped immediately. (See section 4.8.1).

Experience to date indicates that 400 mg administered over 24 hours is well tolerated in the average adult.

Paediatric population 1 to 12 years of age
Paediatric regional anaesthetic procedures should be performed by qualified clinicians who are familiar with this population and the technique.

The doses in the table should be regarded as guidelines for use in paediatrics. Individual variations occur. In children with a high body weight a gradual reduction of the dosage is often necessary and should be based on the ideal body weight. Standard textbooks should be consulted for factors affecting specific block techniques and for individual patient requirements.

The lowest dose required for adequate analgesia should be used.

Table 2 Dosage recommendations for children 1 to 12 years of age

 

Conc.

mg/ml

Volume

ml/kg

Dose

mg/kg

Onset

min

Duration of effect

hours

ACUTE PAIN MANAGEMENT (per- and postoperative)

Caudal Epidural Administration

2.5

0.6-0.8

1.5-2

20-30

2-6

Lumbar Epidural Administration

2.5

0.6-0.8

1.5-2

20-30

2-6

Thoracic Epidural Administration a)

2.5

0.6-0.8

1.5-2

20-30

2-6

Field Block (e.g. minor nerve blocks and infiltration)

2.5

 

0.5-2.0

  
 

5.0

 

0.5-2.0

  

Peripheral Nerve Blocks (e.g. ilioinguinal – iliohypogastric)

2.5

 

0.5-2.0 b

  
 

5.0

 

0.5-2.0 b

  

a) Thoracic epidural blocks need to be given by incremental dosage until the desired level of anaesthesia is achieved.

b) The onset and duration of peripheral nerve blocks depend on the type of block and the dose administered.

In children the dosage should be calculated on a weight basis up to 2 mg/kg.

In order to avoid intravascular injection, aspiration should be repeated prior to and during administration of the main dose. This should be injected slowly in incremental doses, particularly in the lumbar and thoracic epidural routes, constantly and closely observing the patient's vital functions.

Peritonsillar infiltration has been performed in children above 2 years of age with bupivacaine 2.5 mg/ml at a dose of 7.5-12.5 mg per tonsil.

Ilioinguinal-iliohypogastric blocks have been performed in children aged 1 year or older with bupivacaine 2.5 mg/ml at a dose of 0.1-0.5 ml/kg equivalent to 0.25-1.25 mg/kg. Children aged 5 years or older have received bupivacaine 5 mg/ml at a dose of 1.25-2 mg/kg.

For penile blocks bupivacaine 5 mg/ml has been used at total doses of 0.2-0.5 ml/kg equivalent to 1-2.5 mg/kg.

The safety and efficacy of bupivacaine with and without adrenaline in children aged < 1 year of age have not been established. Only limited data are available.

Safety and efficacy of intermittent epidural bolus injection or continuous infusion have not been established. Only limited data is available.


Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. Bupivacaine hydrochloride solutions are contra-indicated in patients with hypersensitivity to local anaesthetic agents of the amide type. Solutions of bupivacaine hydrochloride are contra-indicated for intravenous regional anaesthesia (Bier's-block). Epidural anaesthesia, regardless of the local anaesthetic used, has its own contra-indications which include: Active disease of the central nervous system such as meningitis, poliomyelitis, intracranial haemorrhage, sub-acute combined degeneration of the cord due to pernicious anaemia and cerebral and spinal tumours; tuberculosis of the spine; pyogenic infection of the skin at or adjacent to the site of lumbar puncture; cardiogenic or hypovolaemic shock; coagulation disorders or ongoing anticoagulation treatment. Bucaine contains sodium Bucaine contains sodium. Each ml of Bucaine 0.5% (100 mg/20 ml) Solution for Injection contains 0.137 mmol (3.151 mg) sodium, equivalent to 0.15% of the WHO recommended maximum daily intake of 2 g sodium for an adult.

There have been reports of cardiac arrest during the use of bupivacaine for epidural anaesthesia or peripheral nerve blockade where resuscitative efforts have been difficult, and were required to be prolonged before the patient responded. However, in some instances resuscitation has proven impossible despite apparently adequate preparation and appropriate management.

Like all local anaesthetic drugs, bupivacaine may cause acute toxicity effects on the central nervous and cardiovascular systems if utilised for local anaesthetic procedures resulting in high blood concentrations of the drug. This is especially the case after unintentional intravascular administration or injection into highly vascular areas. Ventricular arrhythmia, ventricular fibrillation, sudden cardiovascular collapse and death have been reported in connection with high systemic concentrations of bupivacaine.

Adequate resuscitation equipment should be available whenever local or general anaesthesia is administered. The clinician responsible should take the necessary precautions to avoid intravascular injection (see section 4.2).

Before any nerve block is attempted, intravenous access for resuscitation purposes should be established. Clinicians should have received adequate and appropriate training in the procedure to be performed and should be familiar with the diagnosis and treatment of side effects, systemic toxicity or other complications (see sections 4.9 & 4.8).

Major peripheral nerve blocks may require the administration of a large volume of local anaesthetic in areas of high vascularity, often close to large vessels where there is an increased risk of intravascular injection and/or systemic absorption. This may lead to high plasma concentrations.

Overdosage or accidental intravenous injection may give rise to toxic reactions.

Injection of repeated doses of bupivacaine hydrochloride may cause significant increases in blood levels with each repeated dose due to slow accumulation of the drug. Tolerance varies with the status of the patient.

Although regional anaesthesia is frequently the optimal anaesthetic technique, some patients require special attention in order to reduce the risk of dangerous side effects:

  • The elderly and patients in poor general condition should be given reduced doses commensurate with their physical status.
  • Patients with partial or complete heart block – due to the fact that local anaesthetics may depress myocardial conduction.
  • Patients with advanced liver disease or severe renal dysfunction.
  • Patients in the late stages of pregnancy.
  • Patients treated with anti-arrhythmic drugs class III (e.g. amiodarone) should be under close surveillance and ECG monitoring, since cardiac effects may be additive.

Patients allergic to ester-type local anaesthetic drugs (procaine, tetracaine, benzocaine, etc.) have not shown cross-sensitivity to agents of the amide type such as bupivacaine.

Certain local anaesthetic procedures may be associated with serious adverse reactions, regardless of the local anaesthetic drug used.

  • Local anaesthetics should be used with caution for epidural anaesthesia in patients with impaired cardiovascular function since they may be less able to compensate for functional changes associated with the prolongation of A-V conduction produced by these drugs.
  • The physiological effects generated by a central neural blockade are more pronounced in the presence of hypotension. Patients with hypovolaemia due to any cause can develop sudden and severe hypotension during epidural anaesthesia. Epidural anaesthesia should therefore be avoided or used with caution in patients with untreated hypovolaemia or significantly impaired venous return.
  • Retrobulbar injections may very rarely reach the cranial subarachnoid space causing temporary blindness, cardiovascular collapse, apnoea, convulsions etc.
  • Retro- and peribulbar injections of local anaesthetics carry a low risk of persistent ocular muscle dysfunction. The primary causes include trauma and/or local toxic effects on muscles and/or nerves. The severity of such tissue reactions is related to the degree of trauma, the concentration of the local anaesthetic and the duration of exposure of the tissue to the local anaesthetic. For this reason, as with all local anaesthetics, the lowest effective concentration and dose of local anaesthetic should be used.
  • Vasoconstrictors may aggravate tissue reactions and should be used only when indicated.
  • Small doses of local anaesthetics injected into the head and neck, including retrobulbar, dental and stellate ganglion blocks, may produce systemic toxicity due to inadvertent intra-arterial injection.
  • Paracervical block may have a greater adverse effect on the foetus than other nerve blocks used in obstetrics. Due to the systemic toxicity of bupivacaine special care should be taken when using bupivacaine for paracervical block.
  • There have been post-marketing reports of chondrolysis in patients receiving post-operative intra-articular continuous infusion of local anaesthetics. The majority of reported cases of chondrolysis have involved the shoulder joint. Due to multiple contributing factors and inconsistency in the scientific literature regarding mechanism of action, causality has not been established. Intra-articular continuous infusion is not an approved indication for bupivacaine.

Epidural anaesthesia with any local anaesthetic can cause hypotension and bradycardia which should be anticipated and appropriate precautions taken. The risk of such effects can be reduced, e.g. by injecting a vasopressor. Hypotension should be treated promptly with a sympathomimetic intravenously, repeated as necessary. Severe hypotension may result from hypovolaemia due to haemorrhage or dehydration, or aorto-caval occlusion in patients with massive ascites, large abdominal tumours or late pregnancy. Marked hypotension should be avoided in patients with cardiac decompensation.

Patients with hypovolaemia due to any cause can develop sudden and severe hypotension during epidural anaesthesia.

Epidural anaesthesia can cause intercostal paralysis and patients with pleural effusions may suffer respiratory embarrassment. Septicaemia can increase the risk of intraspinal abscess formation in the postoperative period.

When bupivacaine is administered as intra-articular injection, caution is advised when recent major intra-articular trauma is suspected or extensive raw surfaces within the joint have been created by the surgical procedure, as that may accelerate absorption and result in higher plasma concentrations.

Hepatic dysfunction, with reversible increases of alanine aminotransferase (ALT), alkaline phosphates (AlkP) and bilirubin, has been observed following repeated injections or long-term infusions of bupivacaine. Association between bupivacaine use and the development of drug-induced liver injury (DILI) has been reported in a small number of literature reports especially with prolonged use. While the pathophysiology of this reaction remains unclear, immediate withdrawal of bupivacaine has shown rapid clinical improvement. If signs of hepatic dysfunction are observed during administration with bupivacaine, the medicinal product should be discontinued.

Paediatric population
The safety and efficacy of bupivacaine in children < 1 year of age have not been established. Only limited data are available.

The use of bupivacaine for intra-articular block in children 1 to 12 years of age has not been documented.

The use of bupivacaine for major nerve block in children 1 to 12 years of age has not been documented.

For Epidural anaesthesia children should be given incremental doses commensurate with their age and weight as especially epidural anaesthesia at a thoracic level may result in severe hypotension and respiratory impairment.


Bupivacaine should be used with caution in patients receiving other local anaesthetics or agents structurally related to amide-type local anaesthetics, e.g. certain anti-arrhythmics, such as lidocaine and mexiletine, since the systemic toxic effects are additive. Specific interaction studies with bupivacaine and anti-arrhythmic drugs class III (e.g. amiodarone) have not been performed, but caution should be advised. (See section 4.4).


Pregnancy
There is no evidence of untoward effects in human pregnancy. In large doses there is evidence of decreased pup survival in rats and an embryological effect in rabbits if bupivacaine is administered in pregnancy. Bupivacaine should not therefore be given in early pregnancy unless the benefits are considered to outweigh the risks.

Foetal adverse effects due to local anaesthetics, such as foetal bradycardia, seem to be most apparent in paracervical block anaesthesia. Such effects may be due to high concentrations of anaesthetic reaching the foetus. (See section 4.4).

Breast-feeding
Bupivacaine enters the mother's milk, but in such small quantities that there is no risk of affecting the child at therapeutic dose levels.


Bupivacaine has minor influence on the ability to drive and use machines. Besides the direct anaesthetic effect, local anaesthetics may have a very mild effect on mental function and co-ordination even in the absence of overt CNS toxicity, and may temporarily impair locomotion and alertness.


Accidental sub-arachnoid injection can lead to very high spinal anaesthesia possibly with apnoea and severe hypotension.

The adverse reaction profile for bupivacaine is similar to those for other long acting local anaesthetics. Adverse reactions caused by the drug per se are difficult to distinguish from the physiological effects of the nerve block (e.g. decrease in blood pressure, bradycardia), events caused directly (e.g. nerve trauma) or indirectly (e.g. epidural abscess) by needle puncture.

Neurological damage is a rare but well recognised consequence of regional and particularly epidural and spinal anaesthesia. It may be due to several causes, e.g. direct injury to the spinal cord or spinal nerves, anterior spinal artery syndrome, injection of an irritant substance, or an injection of a non-sterile solution. These may result in localised areas of paraesthesia or anaesthesia, motor weakness, loss of sphincter control and paraplegia. Occasionally these are permanent.

Tabulated list of adverse reactions
The adverse reactions considered at least possibly related to treatment with bupivacaine from clinical trials with related products and post-marketing experience are listed below by body system organ class and absolute frequency. Frequencies are defined as 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) or not known (cannot be estimated from the available data).

Table of Adverse Drug Reactions (ADR)

System Organ Class

Frequency Classification

Adverse Drug Reaction

Immune system disorders

Rare

Allergic reactions, anaphylactic reaction/shock (see section 4.4)

Nervous system disorders

Common

Paraesthesia, dizziness

 

Uncommon

Signs and symptoms of CNS toxicity (convulsions, circumoral paraesthesia, numbness of the tongue, hyperacusis, visual disturbances, loss of consciousness, tremor, light headedness, tinnitus, dysarthria, muscle twitching)

 

Rare

Neuropathy, peripheral nerve injury, arachnoiditis, paresis and paraplegia

Eye disorders

Rare

Diplopia

Cardiac disorders

Common

Bradycardia (see section 4.4)

 

Rare

Cardiac arrest (see section 4.4), cardiac arrhythmias

Vascular disorders

Very Common

Hypotension (see section 4.4)

 

Common

Hypertension (see section 4.5)

Respiratory, thoracic and mediastinal disorders

Rare

Respiratory depression

Gastrointestinal disorders

Very Common

Nausea

 

Common

Vomiting

Renal and urinary disorders

Common

Urinary retention

Hepatic dysfunction, with reversible increases of SGOT, SGPT, alkaline phosphates and bilirubin, has been observed following repeated injections or long-term infusions of bupivacaine. If signs of hepatic dysfunction are observed during treatment with bupivacaine, the drug should be discontinued.

Acute systemic toxicity
Systemic toxic reactions primarily involve the central nervous system (CNS) and the cardiovascular system. Such reactions are caused by high blood concentrations of a local anaesthetic, which may appear due to (accidental) intravascular injection, overdose or exceptionally rapid absorption from highly vascularised areas (see section 4.4). CNS reactions are similar for all amide local anaesthetics, while cardiac reactions are more dependent on the drug, both quantitatively and qualitatively.

  • Central nervous system toxicity is a graded response with symptoms and signs of escalating severity. The first symptoms are usually light-headedness, circumoral paraesthesia, numbness of the tongue, hyperacusis, tinnitus and visual disturbances. Dysarthria, muscular twitching or tremors are more serious and precede the onset of generalised convulsions. These signs must not be mistaken for neurotic behaviour. Unconsciousness and grand mal convulsions may follow, which may last from a few seconds to several minutes. Hypoxia and hypercarbia occur rapidly following convulsions due to the increased muscular activity, together with the interference with respiration and possible loss of functional airways. In severe cases apnoea may occur. Acidosis, hyperkalaemia and hypoxia increase and extend the toxic effects of local anaesthetics.

Recovery is due to redistribution of the local anaesthetic drug from the central nervous system and subsequent metabolism and excretion. Recovery may be rapid unless large amounts of the drug have been injected.

  • Cardiovascular system toxicity may be seen in severe cases and is generally preceded by signs of toxicity in the central nervous system. In patients under heavy sedation or receiving a general anaesthetic, prodromal CNS symptoms may be absent. Hypotension, bradycardia, arrhythmia and even cardiac arrest may occur as a result of high systemic concentrations of local anaesthetics, but in rare cases cardiac arrest has occurred without prodromal CNS effects.
  • Paediatric population
    Adverse drug reactions in children are similar to those in adults, however in children, early signs of local anaesthetic toxicity may be difficult to detect in cases where the block is given during general anaesthesia.

Treatment of acute toxicity
If signs of acute systemic toxicity appear, injection of the local anaesthetic should be immediately stopped.

Treatment of a patient with systemic toxicity consists of arresting convulsions and ensuring adequate ventilation with oxygen, if necessary by assisted or controlled ventilation (respiration).

Once convulsions have been controlled and adequate ventilation of the lungs ensured, no other treatment is generally required.

If cardiovascular depression occurs (hypotension, bradycardia) appropriate treatment with intravenous fluids, vasopressor, inotropic agents and/or lipid emulsion should be considered. Children should be given doses commensurate with age and weight.

If circulatory arrest should occur, immediate cardiopulmonary resuscitation should be instituted. Optimal oxygenation and ventilation and circulatory support as well as treatment of acidosis are of vital importance.

Cardiac arrest due to bupivacaine can be resistant to electrical defibrillation and resuscitation must be continued energetically for a prolonged period.

High or total spinal blockade causing respiratory paralysis and hypotension during epidural anaesthesia should be treated by ensuring and maintaining a patent airway and giving oxygen by assisted or controlled ventilation.

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:

  • Saudi Arabia

The National Pharmacovigilance Centre (NPC)
SFDA Call Center: 19999
E-mail: npc.drug@sfda.gov.sa
Website: https://ade.sfda.gov.sa

  • Other GCC States

Please contact the relevant competent authority.


Accidental intravascular injections of local anaesthetics may cause immediate (within seconds to a few minutes) systemic toxic reactions. In the event of overdose, systemic toxicity appears later (15-60 minutes after injection) due to the slower increase in local anaesthetic blood concentration. (See section 4.8).


Phamacotherapeutic group (ATC code): N01B B51

Bupivacaine hydrochloride is a long acting local anaesthetic of the amide type with both anaesthetic and analgesic effects. At high doses it produces surgical anaesthesia, while at lower doses it produces sensory block (analgesia) with less pronounced motor block.

Onset and duration of the local anaesthetic effect of bupivacaine depends on the dose and site of administration.

Bupivacaine, like other local anaesthetics, causes a reversible blockade of impulse propagation along nerve fibres by preventing the inward movement of sodium ions through the cell membrane of the nerve fibres. The sodium channels of the nerve membrane are considered a receptor for local anaesthetic molecules.

Local anaesthetics may have similar effects on other excitable membranes e.g. in the brain and myocardium. If excessive amounts of drug reach the systemic circulation, symptoms and signs of toxicity may appear, emanating from the central nervous and cardiovascular systems.

Central nervous system toxicity (see section 4.8.1) usually precedes the cardiovascular effects as central nervous system toxicity occurs at lower plasma concentrations. Direct effects of local anaesthetics on the heart include slow conduction, negative inotropism and eventually cardiac arrest.

Indirect cardiovascular effects (hypotension, bradycardia) may occur after epidural administration depending on the extent of the concomitant sympathetic block.


Bupivacaine has a pKa of 8.2 and a partition coefficient of 346 (25°C n-octanol/ phosphate buffer pH 7.4). The metabolites have a pharmacological activity that is less than that of bupivacaine.

The plasma concentration of bupivacaine depends upon the dose, the route of administration and the vascularity of the injection site.

Bupivacaine shows complete and biphasic absorption from the epidural space with half-lives in the order of 7 min and 6 h respectively. The slow absorption is rate-limiting in the elimination of bupivacaine, which explains why the apparent half-life after epidural administration is longer than that after intravenous administration.

Bupivacaine has a total plasma clearance of 0.58 l/min, a volume of distribution at steady state of 73 l, a terminal half-life of 2.7 h and an intermediate hepatic extraction ratio of 0.38 after IV administration (ref.). It is mainly bound to alpha-l-acid glycoprotein with plasma binding of 96%. Clearance of bupivacaine is almost entirely due to liver metabolism and more sensitive to changes in intrinsic hepatic enzyme function that to liver perfusion.

Paediatric population
In children the pharmacokinetics are similar to that in adults.

An increase in total plasma concentration has been observed during continuous epidural infusion. This is related to a postoperative increase in alpha 1-acid glycoprotein. The unbound, i.e. pharmacologically active, concentration is similar before and after surgery.

Bupivacaine readily crosses the placenta and equilibrium with regard to the unbound concentration is rapidly reached. The degree of plasma protein binding in the foetus is less than in the mother, which results in lower total plasma concentrations in the foetus.

Bupivacaine is extensively metabolised in the liver, predominately by aromatic hydroxylation to 4-hydroxy-bupivacaine and N-dealkylation to PPX, both mediated by cytochrome P4503A4. About 1% of bupivacaine is excreted in the urine as unchanged drug in 24 h and approximately 5% as PPX. The plasma concentrations of PPX and 4-hydroxy-bupivacaine during and after continuous administration of bupivacaine are low as compared to the parent drug.

 


Bupivacaine hydrochloride is a well established active ingredient.


-    Sodium chloride

-    Sodium hydroxide solution and/or hydrochloric acid

-    Water for injection


Not applicable.


36 months.

Store below 30°C. Avoid freeze.

 Store in the original package.


20 ml clear glass vials sealed with green flip-off caps.

 Pack size: 1 Vial (20 ml)


For single use only. Discard any unused solution. Any unused medicinal product or waste material should be disposed of in accordance with local requirements.


Jazeera Pharmaceutical Industries Al-Kharj Road P.O. Box 106229 Riyadh 11666, Saudi Arabia Tel: + (966-11) 8107023, + (966-11) 2142472 Fax: + (966-11) 2078170 e-mail: SAPV@hikma.com

31 August 2023
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