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• Levocetirizine dihydrochloride is the active ingredient of Levozin.
• Levozin is an anti-allergic medication.
• For the treatment of signs of illness (symptoms) associated with:
• Allergic rhinitis (including persistent allergic rhinitis);
• Nettle rash (urticaria).
Do not take Levozin
• if you are allergic (hypersensitive) to levocetirizine dihydrochloride or any of the other ingredients of Levozin (see ‘What Levozin contains’)
• if you have a severe impairment of kidney function (severe renal failure with creatinine clearance below 10 ml/min) take special care with Levozin
• The use of Levozin is not recommended in children less than 6 years since the film coated tablets do not allow for dose adaptation.
• If you are likely to be unable to empty your bladder (with conditions such as spinal cord injury or enlarged prostate), please ask your doctor for advice.
Taking other medicines
• Please tell your doctor or pharmacist if you are taking or have recently taken any other medicines, including medicines obtained without a prescription.
Taking Levozin with food and drink
• Caution is advised if Levozin is taken at the same time with alcohol.
• In sensitive patients, the simultaneous use of cetirizine or levocetirizine and alcohol or other centrally acting agents may have effects on the central nervous system, Although the racemate cetirizine has been shown not to increase the effect of alcohol.
Pregnancy and breast-feeding
• Ask your doctor or pharmacist for advice before taking any medicine.
• Tell your doctor if you are pregnant, trying to get pregnant or breast-feeding.
Driving and using machines
• Some patients being treated with Levozin may experience somnolence/ drowsiness, tiredness and exhaustion.
• Use caution when driving or operating machinery until you know how this medicine affects you. However, special tests have revealed no impairment of mental alertness, the ability to react or the ability to drive in healthy test persons after taking levocetirizine in the recommended dosage.
Important information about some of the ingredients of Levozin
• These tablets contain lactose, if you have been told by your doctor that you have intolerance to some sugars you should contact your doctor before taking them.
• Always take Levozin exactly as your doctor has told you. You should check with your doctor or pharmacist if you are not sure.
Dosage:
• The usual dose for adults and children aged 6 years and over is one tablet daily.
Special dosage instructions for specific populations:
• Patients with impaired kidney function may be given a lower dose according to the severity of their kidney disease, and in children the dose will also be chosen on the basis of body weight; the dose will be determined by your doctor.
• Patients who have severe impairment of kidney function must not take Levozin.
• Patients who only have impaired liver function should take the usual prescribed dose.
• Patients who have both impaired liver and kidney function may be given a lower dose depending on the severity of the kidney disease, and in children the dose will also be chosen on the basis of body weight; the dose will be determined by your doctor.
• Levozin is not recommended for children under 6 years of age.
• No adaptation of the dose is necessary in elderly patients, provided their renal function is normal.
How and when should you take Levozin?
• The tablets should be swallowed whole with water and may be taken with or without food.
If you take more Levozin than you should
• If you take more Levozin than you should, somnolence can occur in adults, Children may initially show excitation and restlessness followed by somnolence.
• If you think you have taken an overdose of Levozin, please tell your doctor who will then decide what action should be taken.
If you forget to take Levozin
• If you forget to take Levozin or if you take a dose lower than that prescribed by your doctor, do not take a double dose to compensate; just wait for the foreseen time for intake of the next dose, and take a normal dose as prescribed by your doctor.
If you stop taking Levozin
• Stopping treatment should have no negative effects. Symptoms may return, but they should not be any worse than they were prior to the treatment.
• If you have any further questions on the use of this product, ask your doctor or pharmacist.
• Like all medicines, Levozincan cause side effects, although not everybody gets them:
Common: may affect up to 1 in 10 people
Dry mouth, headache, tiredness and somnolence/drowsiness
Uncommon: may affect up to 1 in 100 people
Exhaustion and abdominal pain
Not known: frequency cannot be estimated from the available data
• Other side effects such as palpitations, increased heart rate, fits, pins and needles, dizziness, syncope, tremor, dysgeusia (distortion of the sense of taste), sensation of rotation or movement, visual disturbances, blurred vision, painful or difficult urination, inability to completely empty the bladder, oedema, pruritus (itchiness), rash, urticaria (swelling, redness and itchiness of the skin), skin eruption, shortness of breath, weight increase, muscular pain, aggressive or agitated behavior, hallucination, depression, insomnia, recurring thoughts of or preoccupation with suicide, hepatitis, abnormal liver function, vomiting, increased appetite and nausea, have also been reported.
• At the first signs of a hypersensitivity reaction, stop taking Levozin and tell your doctor.
Hypersensitivity reaction symptoms may include: swelling of the mouth, tongue, face and/or throat, breathing or swallowing difficulties (chest tightness or wheezing) hives, sudden fall in blood pressure leading to collapse or shock, which may be fatal.
• If any of the side effects gets serious, or if you notice any side effects not listed in this leaflet, please tell your doctor or pharmacist.
• Keep out of the reach and sight of children.
• Store below 30 °C
• Do not use Levozin after the expiry date which is stated on the label and carton after {abbreviation used for expiry date}. The expiry date refers to the last day of that month.
• This medicinal product does not require any special storage conditions.
– The active substance is levocetirizine dihydrochloride
Each film-coated tablet contains 5 mg levocetirizine dihydrochloride.
– The other ingredients are silicified microcrystalline cellulose, lactose monohydrate, magnesium stearate, opadry white 03F48937
SAJA Pharmaceuticals
Saudi Arabian Japanese pharmaceutical company limited
Jeddah – Saudi Arabia
To report any side effect(s)
• Saudi Arabia
- The National Pharmacovigilance Centre (NP):
- Fax: +966-11-205-7662
- SFDA Call Center: 19999
- E-mail: npc.drug@sfda.gov.sa
- Website: https://ade.sfda.gov.sa
• Other GCC states /other countries
-Please contact the relevant competent authority
• ثنائي هيدروكلوريد الليفوسيتيريزين هي المادة الفعَّالة الموجودة بـ "ليفوزين".
• ليفوزين هو دواء مضاد للحساسية.
• لعلاج علامات المرض (الأعراض) المصاحبة لـ:
• التهاب الأنف التحسسي (بما في ذلك التهاب الأنف التحسسي المستمر)؛
• طفح القراص (أرتكاريا).
لا تتناول ليفوزين في الحالات الآتية:
• إذا كنت تعاني من الحساسية "الحساسية المفرطة" تجاه ثنائي هيدروكلوريد الليفوسيتيريزين أو أيٍّ من مكونات ليفوزين الأخرى.
• إذا كنت تُعاني من قصور شديد في وظائف الكُلى (فشل كُلوي شديد مع معدل تصفية كرياتينين أقل من ۱۰ مللي لتر/دقيقة) فتوخ حذرًا خاصًا مع ليفوزين
• لا يُوصى باستخدام ليفوزين في الأطفال الذين تقل أعمارهم عن ٦ سنوات لأن الأقراص المُغلَّفة لا تسمح بتعديل (موائمة) الجرعة.
• إذا كان من المُحتَمَل ألا تتمكن من تفريغ المثانة (مع حالات مثل إصابة النُّخاعِ الشوكي أو تضخم البروستاتا)، فيُرجى استشارة طبيبك.
تناوُل ليفوزين مع أدوية أخرى
• يُرجى إبلاغ الطبيب أو الصيدلي الخاص بك إذا كنت تتناول أو تناولت مؤخرًا أية أدوية أخرى، بما في ذلك الأدوية التي حصلت عليها دون وصفة طبية.
تناوُل ليفوزين مع الأغذية والمشروبات
• يُنصَح بتوخي الحذر إذا تم تناوُل ليفوزين في الوقت نفسه مع الكحوليات.
• في المرضى الذين لديهم حساسية، قد يؤثر الاستخدام المتزامن لسيتيريزين أو ليفوسيتيريزين مع الكحوليات أو الأدوية الأخرى التي تعمل مركزيًا على الجهاز العصبي المركزي، على الرغم من أنّه اتضح أن راسيمات السيتيريزين لا تُزيد من تأثير الكحوليات.
الحمل والرضاعة الطبيعية
• استشيري طبيبك أو الصيدلي قبل تناول أيّ دواء.
• اخبري طبيبك إذا كنتِ حاملًا أو ترغبين في الحمل أو تمارسين الرضاعة الطبيعية.
القيادة واستخدام الآلات
• قد يتعرَّض بعض المرضى الذين يُعالجون ب"ليفوزين" لنيمومة/ نعاس وتعب وإنهاك.
• توخ الحذر عند القيادة أو تشغيل الآلات حتى تعرف مدى تأثير هذا الدّواء عليك. مع ذلك، لم تكشف الاختبارات الخاصة أيّ قصور في اليقظة الذهنية أو القدرة على الاستجابة أو القدرة على القيادة في الاختبارات التي أُجريَّت على أشخاص أصحاء بعد تناوُل ليفوسيتيريزين بالجرعات المُوصى بها.
معلومات هامة عن بعض مكونات ليفوزين
• تحتوي هذه الأقراص على لاكتوز، إذا كان طبيبك قد أخبرك بأنك لا تتحمل بعض أنواع السكريات، فاتصل به قبل تناولها.
• تناوَل ليفوزين دائمًا كما اخبرك طبيبك بالضبط. كما يجب مراجعة الطبيب أو الصيدلي الخاص بك إذا لم تكن متأكدًا من كيفية التناول.
الجرعة:
• الجرعة المعتادة للبالغين والأطفال ممن تتراوح أعمارهم من ٦ سنوات فأكثر هي قرص واحد يوميًا.
تعليمات الجرعة الخاصة لشرائح مُحَددة من المرضى:
• قد يتم إعطاء المرضى الذين يُعانون من قصور بوظائف الكُلى جرعة أقل وفقًا لشدة المرض الموجود بالكُلى لديهم، وفي الأطفال سيتم أيضًا اختيار الجرعة على أساس وزن الجسم؛ وسيقوم طبيبك بتحديد الجرعة.
• يجب ألا يتناول المرضى المصابين بقصور شديد في وظائف الكُلى ليفوزين.
• يجب على المرضى الذين يُعانون من قصور بوظائف الكبد فقط تناوُل الجرعة المُعتادة الموصوفة.
• قد يتم إعطاء المرضى الذين يُعانون من قصور بوظائف الكبد والكُلى جرعة أقل وفقًا لشدة المرض الموجود بالكُلى لديهم، وفي الأطفال سيتم أيضًا اختيار الجرعة على أساس وزن الجسم؛ وسيقوم طبيبك بتحديد الجرعة.
• لا ينصح بـ "ليفوزين" للأطفال دون سن ٦ سنوات من العمر.
• لا يستلزم الأمر تعديل الجرعة في المرضى من كبار السن، شريطة أن تكون وظائف الكُلى لديهم طبيعية.
كيف ومتى يجب تناوُل ليفوزين؟
• يجب بلع الأقراص كاملة مع بعض الماء ويُمكن تناولها مع أو بدون طعام.
إذا تناولت كمية من ليفوزين أكثر مما يجب
• إذا تناولت كمية أكثر مما يجب من ليفوزين، فقد تحدث نيمومة لدى البالغين، قد يُظهر الأطفال في البداية إثارة وتململ (شعور بعدم الارتياح) ثم نيمومة.
• إذا كنت تعتقد أنك قد تناولت جرعة زائدة من ليفوزين، فيُرجى إخبار طبيبك والذي بدوره سيقوم حينها بتحديد الإجراء الواجب اتخاذه.
إذا أغفلت تناوُل ليفوزين
• إذا أغفلت تناوُل ليفوزين أو إذا تناولت جرعة أقل من تلك التي وصفها لك طبيبك، فلا تتناول جرعة مضاعفة لتعويض الجرعة التي أغفلتها؛ فقط انتظر حتى الوقت المُقدَّر لتناوُل الجرعة التالية، وتناول الجرعة المعتادة على النحو الذي وصفه لك طبيبك.
إذا توقفت عن تناوُل ليفوزين
• لا يكون لإيقاف العلاج أيّ آثار سلبي، ولكن قد تعود الأعراض، لكنها لا تكون أسوأ مما كانت عليه قبل العلاج.
• إذا كانت لديك أيّة أسئلة إضافية حول استخدام هذا المنتج، فاستشر الطبيب أو الصيدلي الخاص بك.
• مثله مثل كافة الأدوية، فقد يُسبب ليفوزين أعراضًا جانبية، على الرغم من عدم حدوثها لدى الجميع وهى:
شائعة: قد تؤثر في ما يصل إلى ۱ من بين كل ۱۰ أشخاص
جُفافُ الفَم وصداع وتعب ونيمومة/ نعاس
غير شائعة: قد تؤثر في ما يصل إلى ۱ من بين كل ۱۰۰ شخص.
إنهاك وألم بالبطن
غير معروفة: لا يمكن تقدير معدل التكرار من واقع البيانات المتاحة
• تم الإبلاغ أيضًا عن آثار جانبية أخرى مثل الخَفَقان وزيادة معدل ضربات القلب وتشنجات ووخز "الإبر والمسامير"، دوخة، غشي (إغماء) وارتعاش واضطراب بحاسة التذوق (تغيُّر حاسة التذوق) وإحساس بالدوران أو الحركة واضطرابات بصرية وعدم وضوح الرؤية وألم أو صعوبة عند التبوُّل وعدم القدرة على تفريغ المثانة ووذمة وحكة وطفح جلدي وأرتكاريا (تورُّم الجلد واحمراره والشعور بحكة به) وطفح جلدي وضيق في التنفس وزيادة الوزن، وألم بالعضلات وسلوك عدواني أو هياج وهَلْوَسَة واكتئاب وأَرَق وأفكار متكررة في الانتحار أو الانشغال به والتهاب الكبد ووظائف الكبد غير طبيعية وقيء وزيادة الشهية وغثيان.
• عند ظهور أول علامات تفاعلات فرط الحساسية، توقف عن تناوُل ليفوزين واخبر طبيبك.
أعراض تفاعلات فرط الحساسية قد تشمل: تورُّم الفم واللسان والوجه أو الحَلْق وصعوبات في التنفس أو البلع (ضيق أو أزيز بالصدر) شرى (ارتكاريا)، وهبوط مفاجئ في ضغط الدَّم يؤدي إلى سقوط أو صدمة، مما قد يكون مميتًا.
• إذا أصبح أيٌّ من الآثار الجانبية خطيرًا، أو إذا لاحظت أيَّة آثار جانبية غير المدّرجة بهذه النشرة، فيُرجى إبلاغ الطبيب.
• يُحفظ بعيدًا عن مُتناوَل ورؤية الأطفال.
• يُحفظ في درجة حرارة أقل من ۳۰ درجة مئوية.
• لا تستعمل ليفوزين بعد انتهاء تاريخ الصلاحية المدون على الملصق والعبوة بعد كلمة " EXP" (انتهاء الصلاحية). يُشير تاريخ انتهاء الصلاحية إلى اليوم الأخير من ذلك الشهر.
• هذا المنتج الدّوائي لا يحتاج لظروف تخزين خاصة.
- المادة الفعّالة هي ثنائي هيدروكلوريد الليفوسيتيريزين
يحتوي كل قرص على ٥ ملج ثنائي هيدروكلوريد الليفوسيتيريزين.
- المكونات الأخرى هي سليلوز دقيق التَّبلور مُتَسَلِّك (تحول إلى سليكا)، لاكتوز أحادي الهيدرات، ستيرات الماغنيسيوم، أوبادري أبيض 03F48937
ليفوزين ٥ ملج أقراص مغلَّفة هو عبارة عن أقراص مغلَّفة ذات لون أبيض وبيضاوية الشكل وثنائية التحدُّب ومنقوش على أحد جانبيها الكود "SJ572" وملساء من الجانب الآخر.
يتوفر ليفوزين ٥ ملج في عبوة بها ۲۰ قرصًا مغلفاً.
مصنع ساجا للصناعات الدوائية
الشركة العربية السعودية اليابانية للمنتجات الصيدلانية المحدودة
جدة – المملكة العربية السعودية
للإبلاغ عن أية آثار جانبية
• المملكة العربية السعودية
- المركز الوطني للتيقظ والسامة الدوائية
- فاكس: 7662-205-11-966+
- مركز اتصالات الهيئة العامة للغذاء والدواء السعودية : 19999
npc.drug@sfda.gov.sa :- البريد الإلكتروني
https://ade.sfda.gov.sa :- الموقع الإلكتروني
• دول الخليج الأخرى/ الدول الأخرى
- الرجاء الاتصال بالمؤسسات و الهيئات الوطنية في كل دولة
| Symptomatic treatment of allergic rhinitis (including persistent allergic rhinitis) and nettle rash (urticarial). |
| The film-coated tablet must be taken orally, swallowed whole with liquid and may be taken with or without food. It is recommended to take the daily dose in one single intake. For children aged 2 to 6 years no adjusted dosage is possible with the film-coated tablet formulation. It is recommended to use a pediatric formulation of levocetirizine. Due to the lack of data in this population, the administration of levocetirizine to infants and toddlers aged less than 2 years is not recommended. Children aged 6 to 12 years: The daily recommended dose is 5 mg (1 film-coated tablet). Adults and adolescents 12 years and above: The daily recommended dose is 5 mg (1 film-coated tablet). Elderly: Adjustment of the dose is recommended in elderly patients with moderate to severe renal impairment (see Patients with renal impairment below). Adult patients with renal impairment: The dosing intervals must be individualized according to renal function. Refer to the following table and adjust the dose as indicated. To use this dosing table, an estimate of the patient's creatinine clearance (CLcr) in ml/min is needed. The CLcr (ml/min) may be estimated from serum creatinine (mg/dl) determination using the following formula: |
| In pediatric patients suffering from renal impairment, the dose will have to be adjusted on an individual basis taking into account the renal clearance of the patient and his body weight. There are no specific data for children with renal impairment. Patients with hepatic impairment: No dose adjustment is needed in patients with solely hepatic impairment. In patients with hepatic impairment and renal impairment, adjustment of the dose is recommended (see Patients with renal impairment above). Duration of use: Intermittent allergic rhinitis (symptoms <4days/week or during less than 4 weeks) has to be treated according to the disease and its history; it can be stopped once the symptoms have disappeared and can be restarted again when symptoms reappear. In case of persistent allergic rhinitis (symptoms >4days/week and during more than 4 weeks), continuous therapy can be proposed to the patient during the period of exposure to allergens. Clinical experience with 5 mg levocetirizine as a film-coated tablet formulation is currently available for a 6-month treatment period. For chronic urticaria and chronic allergic rhinitis, up to one year's clinical experience is available for the racemate. |
| The use of the film-coated tablet formulation is not recommended in children aged less than 6 years since this formulation does not allow for appropriate dose adaptation. It is recommended to use a paediatric formulation of levocetirizine. Precaution is recommended with intake of alcohol (see Interactions). Caution should be taken in patients with predisposing factors of urinary retention (e.g. spinal cord lesion, |
| prostatic hyperplasia) as levocetirizine may increase the risk of urinary retention. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose galactose malabsorption should not take this medicine. |
| No interaction studies have been performed with levocetirizine (including no studies with CYP3A4 inducers); studies with the racemate compound cetirizine demonstrated that there were no clinically relevant adverse interactions (with antipyrine, pseudoephedrine, cimetidine, ketoconazole, erythromycin, azithromycin, glipizide and diazepam). A small decrease in the clearance of cetirizine (16%) was observed in a multiple dose study with theophylline (400 mg once a day); while the disposition of theophylline was not altered by concomitant cetirizine administration. In a multiple dose study of ritonavir (600 mg twice daily) and cetirizine (10 mg daily), the extent of exposure to cetirizine was increased by about 40% while the disposition of ritonavir was slightly altered (- 11%) further to concomitant cetirizine administration. The extent of absorption of levocetirizine is not reduced with food, although the rate of absorption is decreased. In sensitive patients the simultaneous administration of cetirizine or levocetirizine and alcohol or other CNS depressants may have effects on the central nervous system, although it has been shown that the racemate cetirizine does not potentiate the effect of alcohol. |
| Pregnancy Category: B For levocetirizine no clinical data on exposed pregnancies are available. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development. Caution should be exercised when prescribing to pregnant or lactating women |
| Comparative clinical trials have revealed no evidence that levocetirizine at the recommended dose impairs mental alertness, reactivity or the ability to drive. Nevertheless, some patients could experience somnolence, fatigue and asthenia under therapy with Levozin. Therefore, patients intending to drive, engage in potentially hazardous activities or operate machinery should take their response to the medicinal product into account |
| a) Summary of safety profile: Use of levocetirizine has been associated with somnolence, fatigue, asthenia, and urinary retention. Clinical studies: |
| In therapeutic studies in women and men aged 12 to 71 years, 15.1% of the patients in the levocetirizine 5 mg group had at least one adverse drug reaction compared to 11.3% in the placebo group. 91.6 % of these adverse drug reactions were mild to moderate. In therapeutic trials, the dropout rate due to adverse events was 1.0% (9/935) with levocetirizine 5 mg and 1.8% (14/771) with placebo. Clinical therapeutic trials with levocetirizine included 935 subjects exposed to the drug at the recommended dose of 5 mg daily. From this pooling, following incidence of adverse drug reactions were :reported at rates of 1 % or greater (common: ≥1/100 to <1/10) under levocetirizine 5 mg or placebo: |
| a) Symptoms Symptoms of overdose may include drowsiness in adults and initially agitation and restlessness, followed by drowsiness in children. b) Management of overdoses There is no known specific antidote to levocetirizine. Should overdose occur, symptomatic or supportive treatment is recommended. Gastric lavage should be considered following short-term ingestion. Levocetirizine is not effectively removed by haemodialysis |
| Pharmacotherapeutic group: antihistamine for systemic use, piperazine derivative, ATC code: R06A E09. Levocetirizine, the (R) enantiomer of cetirizine, is a potent and selective antagonist of peripheral H1- |
| receptors. Binding studies revealed that levocetirizine has high affinity for human H1-receptors (Ki = 3.2 nmol/l). Levocetirizine has an affinity 2-fold higher than that of cetirizine (Ki = 6.3 nmol/l). Levocetirizine dissociates from H1-receptors with a half-life of 115 ± 38 min. After single administration, levocetirizine shows a receptor occupancy of 90% at 4 hours and 57% at 24 hours. Pharmacodynamic studies in healthy volunteers demonstrate that, at half the dose, levocetirizine has comparable activity to cetirizine, both in the skin and in the nose. The pharmacodynamic activity of levocetirizine has been studied in randomised, controlled trials: In a study comparing the effects of levocetirizine 5mg, desloratadine 5mg, and placebo on histamine induced wheal and flare, levocetirizine treatment resulted in significantly decreased wheal and flare formation which was highest in the first 12 hours and lasted for 24 hours, (p<0.001) compared with placebo and desloratadine. The onset of action of levocetirizine 5 mg in controlling pollen-induced symptoms has been observed at 1 hour post drug intake in placebo controlled trials in the model of the allergen challenge chamber. In vitro studies (Boyden chambers and cell layers techniques) show that levocetirizine inhibits eotaxin induced eosinophil transendothelial migration through both dermal and lung cells. A pharmacodynamic experimental study in vivo (skin chamber technique) showed three main inhibitory effects of levocetirizine 5 mg in the first 6 hours of pollen-induced reaction, compared with placebo in 14 adult patients: inhibition of VCAM-1 release, modulation of vascular permeability and a decrease in eosinophil recruitment. The efficacy and safety of levocetirizine has been demonstrated in several double-blind, placebo controlled, clinical trials performed in adult patients suffering from seasonal allergic rhinitis, perennial allergic rhinitis, or persistent allergic rhinitis. Levocetirizine has been shown to significantly improve symptoms of allergic rhinitis, including nasal obstruction in some studies. A 6-month clinical study in 551 adult patients (including 276 levocetirizine-treated patients) suffering from persistent allergic rhinitis (symptoms present 4 days a week for at least 4 consecutive weeks) and sensitized to house dust mites and grass pollen demonstrated that levocetirizine 5 mg was clinically and statistically significantly more potent than placebo on the relief from the total symptom score of allergic rhinitis throughout the whole duration of the study, without any tachyphylaxis. During the whole duration of the study, levocetirizine significantly improved the quality of life of the patients. The paediatric safety and efficacy of levocetirizine tablets has been studied in two placebo controlled clinical trials including patients aged 6 to 12 years and suffering from seasonal and perennial allergic rhinitis, respectively. In both trials, levocetirizine significantly improved symptoms and increased health related quality of life. In children below the age of 6 years, clinical safety has been established from several short- or long -term therapeutic studies: - one clinical trial in which 29 children 2 to 6 years of age with allergic rhinitis were treated with levocetirizine 1.25 mg twice daily for 4 weeks - one clinical trial in which 114 children 1 to 5 years of age with allergic rhinitis or chronic idiopathic |
| urticaria were treated with levocetirizine 1.25 mg twice daily for 2 weeks - one clinical trial in which 45 children 6 to 11 months of age with allergic rhinitis or chronic idiopathic urticaria were treated with levocetirizine 1.25 mg once daily for 2 weeks - one long-term (18 months) clinical trial in 255 levocetirizine - treated atopic subjects aged 12 to 24 months at inclusion The safety profile was similar to that seen in the short-term studies conducted in children 1 to 5 years of age. In a placebo-controlled clinical trial including 166 patients suffering from chronic idiopathic urticaria, 85 patients were treated with placebo and 81 patients with levocetirizine 5mg once daily over six weeks. Treatment with levocetirizine resulted in significant decrease in pruritus severity over the first week and over the total treatment period as compared to placebo. Levocetirizine also resulted in a larger improvement of health-related quality of life as assessed by the Dermatology Life Quality Index as compared to placebo. Chronic idiopathic urticaria was studied as a model for urticarial conditions. Since histamine release is a causal factor in urticarial diseases, levocetirizine is expected to be effective in providing symptomatic relief for other urticarial conditions, in addition to chronic idiopathic urticaria. Pharmacokinetic / pharmacodynamic relationship: The action on histamine-induced skin reactions is out of phase with the plasma concentrations. ECGs did not show relevant effects of levocetirizine on QT interval. |
| The pharmacokinetics of levocetirizine are linear with dose- and time-independent with low inter-subject variability. The pharmacokinetic profile is the same when given as the single enantiomer or when given as cetirizine. No chiral inversion occurs during the process of absorption and elimination. Absorption: Levocetirizine is rapidly and extensively absorbed following oral administration. Peak plasma concentrations are achieved 0.9 h after dosing. Steady state is achieved after two days. Peak concentrations are typically 270 ng/ml and 308 ng/ml following a single and a repeated 5 mg o.d. dose, respectively. The extent of absorption is dose-independent and is not altered by food, but the peak concentration is reduced and delayed. Distribution: No tissue distribution data are available in humans, neither concerning the passage of levocetirizine through the blood-brain-barrier. In rats and dogs, the highest tissue levels are found in liver and kidneys, the lowest in the CNS compartment. In Human, levocetirizine is 90% bound to plasma proteins. The distribution of levocetirizine is restrictive, as the volume of distribution is 0.4 l/kg. |
| Biotransformation: The extent of metabolism of levocetirizine in humans is less than 14% of the dose and therefore differences resulting from genetic polymorphism or concomitant intake of enzyme inhibitors are expected to be negligible. Metabolic pathways include aromatic oxidation, N- and O- dealkylation and taurine conjugation. Dealkylation pathways are primarily mediated by CYP 3A4 while aromatic oxidation involved multiple and/or unidentified CYP isoforms. Levocetirizine had no effect on the activities of CYP isoenzymes 1A2, 2C9, 2C19, 2D6, 2E1 and 3A4 at concentrations well above peak concentrations achieved following a 5 mg oral dose. Due to its low metabolism and absence of metabolic inhibition potential, the interaction of levocetirizine with other substances, or vice-versa, is unlikely. Elimination: The plasma half-life in adults is 7.9 ± 1.9 hours. The mean apparent total body clearance is 0.63 ml/min/kg. The major route of excretion of levocetirizine and metabolites is via urine, accounting for a mean of 85.4% of the dose. Excretion via faeces accounts for only 12.9% of the dose. Levocetirizine is excreted both by glomerular filtration and active tubular secretion. Renal impairment: The apparent body clearance of levocetirizine is correlated to the creatinine clearance. It is therefore recommended to adjust the dosing intervals of levocetirizine, based on creatinine clearance in patients with moderate and severe renal impairment. In anuric end stage renal disease subjects, the total body clearance is decreased by approximately 80% when compared to normal subjects. The amount of levocetirizine removed during a standard 4-hour hemodialysis procedure was < 10%. Paediatric population: Data from a paediatric pharmacokinetic study with oral administration of a single dose of 5 mg levocetirizine in 14 children age 6 to 11 years with body weight ranging between 20 and 40 kg show that Cmax and AUC values are about 2-fold greater than that reported in healthy adult subjects in a cross-study comparison. The mean Cmax was 450 ng/ml, occurring at a mean time of 1.2 hours, weight-normalized, total body clearance was 30% greater, and the elimination half-life 24% shorter in this paediatric population than in adults. Dedicated pharmacokinetic studies have not been conducted in paediatric patients younger than 6 years of age. A retrospective population pharmacokinetic analysis was conducted in 324 subjects (181 children 1 to 5 years of age, 18 children 6 to 11 years of age, and 124 adults 18 to 55 years of age) who received single or multiple doses of levocetirizine ranging from 1.25 mg to 30 mg. Data generated from this analysis indicated that administration of 1.25 mg once daily to children 6 months to 5 years of age is expected to result in plasma concentrations similar to those of adults receiving 5 mg once daily. Geriatric Patients: Limited pharmacokinetic data are available in elderly subjects. Following once daily repeat oral administration of 30 mg levocetirizine for 6 days in 9 elderly subjects (65–74 years of age), the total body clearance was approximately 33% lower compared to that in younger adults. The disposition of racemic cetirizine has been shown to be dependent on renal function rather than on age. This finding would also be applicable for levocetirizine, as levocetirizine and cetirizine are both predominantly excreted in urine. Therefore, the levocetirizine dose should be adjusted in accordance with renal function in elderly patients. |
| Gender: Pharmacokinetic results for 77 patients (40 men, 37 women) were evaluated for potential effect of gender. The half-life was slightly shorter in women (7.08 ± 1.72 hr) than in men (8.62 ± 1.84 hr); however, the body weight-adjusted oral clearance in women (0.67 ± 0.16 ml/min/kg) appears to be comparable to that in men (0.59 ± 0.12 ml/min/kg). The same daily doses and dosing intervals are applicable for men and women with normal renal function. Race: The effect of race on levocetirizine has not been studied. As levocetirizine is primarily renally excreted, and there are no important racial differences in creatinine clearance, pharmacokinetic characteristics of levocetirizine are not expected to be different across races. No race-related differences in the kinetics of racemic cetirizine have been observed. Hepatic impairment: The pharmacokinetics of levocetirizine in hepatically impaired subjects have not been tested. Patients with chronic liver diseases (hepatocellular, cholestatic, and biliary cirrhosis) given 10 or 20 mg of the racemic compound cetirizine as a single dose had a 50% increase in half life along with a 40% decrease in clearance compared to healthy subjects. |
| Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, toxicity to reproduction. |
| Core: Silicified microcrystalline cellulose Lactose monohydrate Magnesium stearate Coating: Opadry white 03F48937 |
| Not applicable |
| Store below 30°C |
| Al/Al blister packs: 20 film coated tablets |
| No special requirements |
