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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)

TADALO 20mg is a treatment for adult men with erectile dysfunction. This is when a man cannot get, or keep a hard, erect penis suitable for sexual activity. TADALO 20mg has been shown to significantly improve the ability of obtaining a hard erect penis suitable for sexual activity.
TADALO 20mg contains the active substance tadalafil which belongs to a group of medicines called phosphodiesterase type 5 inhibitors. Following sexual stimulation TADALO 20mg works by helping the blood vessels in your penis to relax, allowing the flow of blood into your penis. The result of this is improved erectile function. TADALO 20mg will not help you if you do not have erectile dysfunction.
It is important to note that TADALO 20mg does not work if there is no sexual stimulation. You and your partner will need to engage in foreplay, just as you would if you were not taking a medicine for erectile dysfunction.


Do not take TADALO 20mg if you:
• Are allergic to Tadalafil or any of the other ingredients of this medicine (listed in section 6).
• Are taking any form of organic nitrate or nitric oxide donors such as amyl nitrite. This is a group of medicines (“nitrates”) used in the treatment of angina pectoris (“chest pain”). TADALO 20mg has been shown to increase the effects of these medicines. If you are taking any form of nitrate or are unsure tell your doctor.
• Have serious heart disease or recently had a heart attack within the last 90 days.
• Recently had a stroke within the last 6 months.
• Have low blood pressure or uncontrolled high blood pressure.
• Ever had loss of vision because of non-arteritic anterior ischemic optic neuropathy (naion), a condition described as “stroke of the eye”.
• Are taking riociguat. This drug is used to treat pulmonary arterial hypertension (i.e., high blood pressure in the lungs) and chronic thromboembolic pulmonary hypertension (i.e., high blood pressure in the lungs secondary to blood clots). Pde5 inhibitors, such as TADALO 20mg, have been shown to increase the hypotensive effects of this medicine. If you are taking riociguat or are unsure tell your doctor.
Warnings and precautions
Talk to your doctor before taking TADALO 20mg.
Be aware that sexual activity carries a possible risk to patients with heart disease because it puts an extra strain on your heart. If you have a heart problem you should tell your doctor.
Before taking the tablets, tell your doctor if you have:
- Sickle cell anaemia (an abnormality of red blood cells).
- Multiple myeloma (cancer of the bone marrow).
- leukaemia (cancer of the blood cells).
- Any deformation of your penis.
- A serious liver problem.
- A severe kidney problem.
It is not known if TADALO 20mg is effective in patients who have had:
- Pelvic surgery.
- Removal of all or part of the prostate gland in which nerves of the prostate are cut (radical non-nerve-sparing prostatectomy).
If you experience sudden decrease or loss of vision, stop taking TADALO 20mg and contact your doctor immediately.
Decreased or sudden hearing loss has been noted in some patients taking Tadalafil. Although it is not known if the event is directly related to Tadalafil, if you experience decreased or sudden hearing loss, stop taking TADALO 20mg and contact your doctor immediately.
TADALO 20mg is not intended for use by women.
Children and adolescents
TADALO 20mg is not intended for use by children and adolescents under the age of 18.
Other medicines and TADALO 20mg
Tell your doctor if you are taking, have recently taken or might take any other medicines
Do not take TADALO 20mg if you are already taking nitrates.
Some medicines may be affected by TADALO 20mg or they may affect how well TADALO 20mg will work. Tell your doctor or pharmacist if you are already taking:
- An alpha blocker (used to treat high blood pressure or urinary symptoms associated with benign prostatic hyperplasia).
- Other medicines to treat high blood pressure.
- Riociguat.
- A 5- alpha reductase inhibitor (used to treat benign prostatic hyperplasia).
- Medicines such as ketoconazole tablets (to treat fungal infections) and protease inhibitors for treatment of AIDS or HIV infection.
- Phenobarbital, phenytoin and carbamazepine (anticonvulsant medicines).
- Rifampicin, erythromycin , clarithromycin or itraconazole.
- Other treatments for erectile dysfunction.
TADALO 20mg with drink and alcohol
Information on the effect of alcohol is in section 3. Grapefruit juice may affect how well TADALO 20mg will work and should be taken with caution. Talk to your doctor for further information.
Fertility
When dogs were treated there was reduced sperm development in the testes. A reduction in sperm was seen in some men. These effects are unlikely to lead to a lack of fertility.
Driving and using machines
Some men taking TADALO 20mg in clinical studies have reported dizziness. Check carefully how you react to the tablets before driving or using machines.
TADALO 20mg contains lactose:
If you have an intolerance to some sugars, contact your doctor before taking this medicine.


Always take this medicine exactly as your doctor has told you. Check with your doctor or pharmacist if you are not sure.
TADALO 20mg tablets are for oral use in men only. Swallow the tablet whole with some water. The tablets can be taken with or without food.
The recommended starting dose is one 10 mg tablet before sexual activity. However, you have been given the dose of one 20mg tablet as your doctor has decided that the recommended dose of 10mg is too weak.

You may take a TADALO 20mg tablet at least 30 minutes before sexual activity.

TADALO 20mg may still be effective up to 36 hours after taking the tablet.
Do not take TADALO 20mg more than once a day. TADALO 20mg is intended for use prior to anticipated sexual activity and is not recommended for continuous daily use.
It is important to note that TADALO 20mg does not work if there is no sexual stimulation. You and your partner will need to engage in foreplay, just as you would if you were not taking a medicine for erectile dysfunction.
Drinking alcohol may affect your ability to get an erection and may temporarily lower your blood pressure. If you have taken or are planning to take TADALO 20mg, avoid excessive drinking (blood alcohol level of 0.08 % or greater), since this may increase the risk of dizziness when standing up.
If you take more TADALO 20mg than you should
Contact your doctor. You may experience side effects described in section 4.
If you have any further questions on the use of this medicine, ask your doctor or pharmacist.


Like all medicines, this medicine can cause side effects, although not everybody gets them. These effects are normally mild to moderate in nature.
If you experience any of the following side effects stop using the medicine and seek medical help immediately:
- Allergic reactions including rashes (frequency uncommon).
- Chest pain - do not use nitrates but seek immediate medical assistance (frequency uncommon).
- Priapism, a prolonged and possibly painful erection after taking TADALO 20mg (frequency rare). If you have such an erection, which lasts continuously for more than 4 hours you should contact a doctor immediately.
- Sudden loss of vision (frequency rare).
Other side effects have been reported:
Common (seen in 1 to 10 in every 100 patients):
- Headache, back pain, muscle aches, pain in arms and legs, facial flushing, nasal congestion, and indigestion.
Uncommon (seen in 1 to 10 in every 1,000 patients):
- Dizziness, stomach ache, feeling sick, being sick (vomiting), reflux, blurred vision, eye pain, difficulty in breathing, presence of blood in urine, prolonged erection, pounding heartbeat sensation, a fast heart rate, high blood pressure, low blood pressure, nose bleeds, ringing in the ears, swelling of the hands, feet or ankles and feeling tired.
Rare (seen in 1 to 10 in every 10,000 patients):
- Fainting, seizures and passing memory loss, swelling of the eyelids, red eyes, sudden decrease or loss of hearing, hives (itchy red welts on the surface of the skin), penile bleeding, presence of blood in semen and increased sweating.
- Heart attack and stroke have also been reported rarely in men taking TADALO 20mg. Most of these men had known heart problems before taking this medicine.
- Partial, temporary, or permanent decrease or loss of vision in one or both eyes has been rarely reported.
Some additional rare side effects have been reported in men taking TADALO 20mg that were not seen in clinical trials. These include:
- Migraine, swelling of the face, serious allergic reaction which causes swelling of the face or throat, serious skin rashes, some disorders affecting blood flow to the eyes, irregular heartbeats, angina and sudden cardiac death.
- The side effect dizziness has been reported more frequently in men over 75 years of age taking TADALO 20mg. Diarrhea has been reported more frequently in men over 65 years of age taking TADALO 20mg.


Keep this medicine out of the sight and reach of children.
Do not use this medicine after the expiry date which is stated on the carton and blister after ‘exp’. The expiry date refers to the last day of that month.
Do not store above 30°c. Store in the original package in order to protect from moisture.
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 tadalafil. Each tablet contains 20 mg of tadalafil.
-the other ingredients are:
tablet core: lactose monohydrate (see end of section 2), croscarmellose sodium, hydroxypropyl cellulose, colloidal silicon dioxide, sodium laurilsulfate, magnesium stearate.
Film-coat: lactose monohydrate, hypromellose, triacetin, titanium dioxide, iron oxide yellow, talc.


TADALO 20mg is a yellow film-coated tablet in the shape of an almond and has "T20" marked on one side. TADALO 20mg is available in blister packs containing 4 tablets.

Al Razi pharma industries 2nd industrial city – street no. 67 cross 110
Building no. 3992 Dammam kingdom of Saudi Arabia “KSA”.
Tel: +966 13 8281919
Fax: +966 13 8251313
Website: www.alrazi-pharma.com


03/2022
  نشرة الدواء تحت مراجعة الهيئة العامة للغذاء والدواء (اقرأ هذه النشرة بعناية قبل البدء في استخدام هذا المنتج لأنه يحتوي على معلومات مهمة لك)

تادالو هو علاج للرجال الذين يعانون من مشاكل في الانتصاب. وذلك عندما لا يستطيع الرجل الحصول على أو الاحتفاظ بثبات القضيب منتصبا بشكل مناسب للنشاط
الجنسي وقد تبين أن تادالو يحسِّن بشكل ملحوظ القدرة على الحصول على قضيب منتصب وثابت مناسب للنشاط الجنسي.
يحتوي تادالو على المادة الفعالة تادالافيل والتي تنتمي إلى مجموعة من الأدوية تسمى مثبطات فوسفوديستريس من النوع الخامس. عقب التحفيز الجنسي يعمل تادالو
عن طريق مساعدة الأوعية الدموية في قضيبك على الاسترخاء، ممّا يسمح للدم بالتدفق إلى القضيب. ونتيجة لهذا يتم تحسين عملية الانتصاب. لن يساعدك تادالو إذا لم
يكن لديك مشاكل في الانتصاب.
ومن المهم أن تلاحظ أن تادالو لا يعمل إذا لم يكن هناك تحفيز جنسي. يجب أن تبدأ أنت وشريكتك بالمداعبة، تماما كما تفعل لو كنت لا تتناول دواء لضعف الانتصاب .

لا تتناول تادالو إذا:

- كنت تأخذ أي شكل من أشكال النترات العضوية أو الأدوية المانحة لأكسيد النيتريك مثل نتريت الأميل. هذه مجموعة من الأدوية ("النترات") المستخدمة في علاج الذبحة الصدرية ("ألم في الصدر"). تبين أن تادالو يزيد من تأثير هذه الأدوية. إذا كنت تأخذ أي شكل من أشكال النترات أو غير متأكد فاستشر طبيبك.
- كان لديك مرض خطير في القلب أو تعرضت مؤخرا لنوبة قلبية في غضون 90 يوما الماضية .
- تعرضت مؤخرا لجلطة في المخ في غضون 6 شهور الماضية .
- كان لديك انخفاض أو ارتفاع في ضغط الدم لم تتم السيطرة عليه .
- سبق وتعرضت في أي وقت مضى لفقدان البصر بسبب اعتلال الأعصاب الدماغية الأمامية البصرية غير الشريانية وهي حالة توصف بأنها "جلطة العين NAION
-

يستخدم هذا الدواء لعلاج ارتفاع ضغط الدم الشرياني الرئوي (أي ارتفاع ضغط الدم في الرئتين)، ارتفاع ضغط الدم الرئوي نتيجة: Ricoiguat - إذا كنت تستخدم
مثل تادالو، تزيد من آثار انخفاض الضغط ، PDE الانسداد التجلطي المزمن (أي ارتفاع ضغط الدم في الرئتين الثانوية لتجلط الدم). وقد ثبت أنّ مثبطات 5
لهذا الدواء. إذا كنت تأخذ أو غير متأكد أخبر طبيبك


تحذيرات واحتياطات:
تحدث مع طبيبك قبل أن تتناول تادالو.
عليك أن تدرك أن النشاط الجنسي ينطوي على خطر محتمل بالنسبة للمرضى الذين يعانون من أمراض القلب لأنه يضيف جهد آخر على قلبك. إذا كان لديك مشكلة في
القلب يجب إخبار طبيبك بذلك.
قبل أن تتناول أقراص تادالو، أخبر طبيبك إذا: -
- كنت مصابا بفقر الدم المنجلي (شذوذ في خلايا الدم الحمراء) .
- كنت مصابا بسرطان النخاع الشوكي المتعدد (سرطان نخاع العظم) .
- كنت مصابا بسرطان الدم (سرطان خلايا الدم) .
- كان لديك اي تشوه في القضيب .
- كان لديك مشكلة خطيرة في الكبد.
- كان لديك مشكلة حادة في الكلى
ومن غير المعروف ما إذا كان تادالو فعالاً في المرضى الذين خضعو ا :
- لجراحة في الحوض .
- جراحة لاستئصال جذري أو جزئي لغدّة البروستات والتي يتم بها قطع أعصاب البروستات (استئصال جذري للبروستات مع عدم المحافظة على ا لأعصاب المغذية لها).
إذا واجهت تدني مفاجئ أو فقدان البصر، أوقف تناول تادالو واتّصل بطبيبك على الفو ر.
لقد لوحظ انخفاض أو فقدان السمع المفاجئ لدى بعض المرضى الذين يتناولون تادالو. على الرغم من أنه ليس من المعروف ما إذا كان هذا مرتبطا مباشرة بتادالافيل،
إذا عانيت من انخفاض أو فقدان السمع المفاجئ، توقف عن تناول تادالو واتصل بطبيبك على الفور .
ولا يستخدم تادالو من قبل النساء .
الأطفال والمراهقين
لا يستخدم تادال و من قبل الأطفال والمراهقين تح ت سن 18 سن ة .
استخدام أدوية أخرى مع تادالو
يرجى إخبار الطبيب إذا كنت تتناول أو تناولت في الآونة الأخيرة، أو قد تتناول أي أدوية أخرى .
لا تتناول تادالو إذا كنت تتناول حاليا النيترات .
بعض الأدوية قد تتأثر بتناولك تادالو أو قد تؤثر على كيفية عمل تادالو .
أخبر طبيبك أو الصيدلي إذا كنت تتناول :
- حاصرات الألفا (يستخدم لعلاج ارتفاع ضغط الدم وأعراض القناة البولية المصاحبة لتضخم البروستاتا الحميد).
- أدوية أخرى لعلاج ارتفاع ضغط الدم .
- Riociguat
- مثبطات مختزلات الفا - 5 (المستخدمة لعلاج تضخم البروستاتا الحميد)
- أدوية مثل أقراص الكيتوكونازول (المستخدمة لعلاج الإنتان الفطري) ومثبطات الأنزيم البروتيني لعلاج الإيدز أو فيروس نقص المناعة البشرية .
- فينوباربيتال، فينايتوين وكاربامازيبين (دواء مضاد للتشنجات) .
- ريفامبيسين، إريثرومايسين، كلاريثرومايسين أو إتراكونازول.
- علاج آخر لعجز الإنتصا ب
تناول تادالو مع الشراب والكحو ل
المعلومات حول أثر الكحول متوفرة في الفقرة 3. عصير الجريب فروت قد يؤثر على طريقة عمل تادالو ويجب تناوله بحذر. تحدث مع طبيبك للحصول على معلومات إضافية .
الخصوبة
عندما تم معالجة الكلاب لوحظ تدني نمو الحيوانات المنوية في الخصيتين. وقد لوحظ تدني عدد الحيوانات المنوية لدى بعض الرجال. ونادرا ما تؤدي هذه التأثيرات إلى تدني مستوى الخصوبة.
 القيادة واستخدام الآلات
ذكر بعض الرجال الذين يتناولون تادلافيل في الدراسات السريرية حدوث الدوخة. تحقّق بعناية حول كيفية استجابتك للأقراص قبل قيادة السيارات أو استخدام الآلات.
يحتوي تادالو على اللاكتوز
إذا كنت تعاني من عدم تحمل بعض السكريات، فعليك الاتصال بطبيبك قبل تناول هذا الدوا ء

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تناول تادالو دائما تماما كما ذكر لك طبيبك. يجب عليك استشار ة طبيبك أو الصيدلي إذا لم تكن متأكدا.
تستخدم أقراص تادالو عن طريق الفم للرجال فقط. ابتلع القرص بأكمله مع بعض الماء. يمكن تناول القرص مع أو بدون الطعام .
الجرعة الابتدائية الموصى بها هي قرص واحد تركيز 10 ملجم قبل النشاط الجنسي. وعموما إذا قرر لك الطبيب تناول جرعة 20 ملجم فهذا يعني أن جرعة 10 ملجم
ضعيفة جدا بالنسبة ل ك .
يمكنك تناول قرص تادالو قبل النشاط الجنسي بثلاثين دقيقة على الأقل .
قد تستمر فعالية تادالو حتى 36 ساعة بعد تناول القرص.
لا تتناول تادال و أكثر من مرة واحدة يوميا. تادال و 20 ملجم يقصد تناوله قبل النشاط الجنسي المتوقع ولا يوصى بتناوله للاستعمال اليومي المستمر .
من المهم ملاحظة أن تادالو لا يعمل في غياب المحفز الجنسي. عليك أنت وشريكتك الشروع في المداعبة، تماما كما تفعل إذا كنت لا تتناول دواء لعدم القدرة على الانتصاب.
قد يؤثر شرب الكحول على القدرة على الانتصاب وقد يخفض ضغط الدم لديك بصورة مؤقتة. إذا كنت قد تناولت، أو تخطط لتناول تادالو، عليك تجنب الإفراط في شرب الكحول (مستوى الكحول في الدم من 0.08 ٪ أو أكثر)، لأن ذلك قد يزيد من خطر الدوخة عند الوقوف.
إذا تناولت تادالو أكثر مما يجب أخبر طبيبك بذلك. قد تعاني من الآثار الجانبيّة المذكورة في الفقرة 4
إذا كان لديك أي أسئلة إضافية حول هذا الدواء، فاسأل طبيبك أو الصيدلي.

مثل جميع الأدوية، يمكن أن يتسبب هذا الدواء في حدوث آثار جانبية، على الرغم من عدم حدوثها لدى الجميع. تكون هذه الآثار عادة خفيفة الى معتدلة في طبيعتها .
إذا حصلت لديك الآثار الجانبية التالية فتوقف عن تناول هذا الدواء و اسعى للحصول على المساعدة الطبية فورا:
- تفاعلات الحساسية وتشمل الطفح (التكرارية غير شائعة ).
- ألم في الصدر.
- لا تتناول النيترات والجأ للمساعدة الطبية الفورية (التكرارية غير شائعة ).
- انتصاب لمدة طويلة ومن المحتمل ان يصحبه ألم عقب تناول تادال و (التكرارية نادرة). إذا اصبت بانتصاب كهذا، والذي يدوم لمدة أكثر من 4 ساعات فعليك الاتصا ل بالطبيب مباشرة.
- الفقدان المفاجئ للبصر (التكرارية نادرة ).
الآثار الجانبية الأخرى التي تم ذكرها :
شائع (لوحظ في 1-10 مرضى من بين 100 مريض)
- صداع، آلام الظهر، آلام في العضلات، ألم في الذراعين والساقين، توهج الوجه، احتقان الأنف، وعسر الهضم.
غير شائع (لوحظ في 1-10 مرضى من بين 1000 مريض)
- الدوخة، ألم المعدة، الشعور بالمرض، القيء، ارتجاع، زغللة النظر، ألم العين، صعوبة التنفس، ظهور دم مع البول، الانتصاب لفترات طويلة، الإحساس بضربات القلب، تسارع معدل ضربات القلب، ارتفاع ضغط الدم، هبوط ضغط الدم، رعاف، طنين بالأذن، تورم في اليدين والقدمين والكاحلين والشعور بالتعب.
نادر(لوحظ في 1-10 مرضى من بين 10000 مريض)
- إغماء، تشنجات، ومرور فقدان للذاكرة، تورم الجفون، احمرار العينين، تدني مفاجئ أو فقدان للسمع والإصابة بحمى القش (كدمات حمراء حاكة على سطح الجلد)، نزيف القضيب، وجود الدم في السائل المنوي وزيادة التعر ق .
- سجل أيضاً بصورة نادرة حدوث نوبات قلبية وسكتات دماغية لدى الرجال الذين يتناولون تادالافيل. معظم هؤلاء الرجال تعرّضوا لمشاكل في القلب قبل تناول هذا الدواء
- ذكر أيضاً وبصورة نادرة حدوث تدني أو فقدان للبصر في أحد أو كلا العينين بشكل جزئي، مؤقت أو دائم.
تم الإبلاغ عن بعض الآثار الجانبية الإضافية النادرة لدى الرجال الذين يتناولون تادالافيل والتي لم تلحظ في التجارب السّريريّة، وتشمل :
- الصداع النصفي، تورم في الوجه، تفاعلات حساسية خطيرة والتي تسبب تورم الوجه أو الحلق، طفح جلدي خطير، بعض الاضطرابات التي تؤثر على تدفق الدم للعيون، اضطراب ضربات القلب، الذبحة الصدرية، وموت القلب المفاجئ

تم الإبلاغ عن حدوث الأثر الجانبي، الدوخة، بشكل أكبر لدى الرجال الذين تتجاوز أعمارهم 75 سنة من العمر ويتناولون تادالافيل. تمّ الإبلاغ عن حدوث الإسهال
بشكل متكرّر لدى الرجال الذين تتجاوز أعمارهم 65 سنة من العمر ويتناولون تادالافيل.
الإبلاغ عن الآثار الجانبيّة
إذا لاحظت حدوث أي آثار جانبية، فتحدث إلى طبيبك أو الصيدلي. هذا يشمل أي أثر جانبي محتمل غير مدرج في هذه النشرة. كما أنّ بإمكانك الإبلاغ عن الآثار الجانبية مباشرة من خلال نظام الإبلاغ الوطني المذكور في الفقرة 6.

إن الإبلاغ عن الآثار الجانبية يساعد في توفير معلومات إضافية حول سلامة هذا الدواء .

احفظ هذا الدواء بعيدا عن نظر ومتناول الأطفا ل.
لا تستخدم تادالو بعد تاريخ انتهاء الصلاحية المدون على العلبة أو الشريط بعد كلم ة EXP” تاريخ الانتهاء يعود لآخر يوم من الشهر المحد د.
لا تخزنه في درجة حرارة أعلى من 30 ° درجة مئوي ة. احفظه في العبوة الأصلية لتحفظه من الرطوبة.
لا ينبغي التخلص من الأدوية في مياه الصرف الصحي أو مع النفايات المنزلية. اسأل الصيدلي حول كيفية التخلص من الأدوية التي لم تعد تستعملها. ومن شأن هذه
التدابير أن تساعد على حماية البيئة .

المادة الفعالة هي تادالافيل. كل قرص يحتوي على 20 ملجم من تادالافيل
المكونات الأخرى هي :
لب القر ص: مونوهيدرات اللاكتوز (انظر نهاية الفقرة 2)، كروسكارميلوز الصوديوم، هيدروكسي بروبايل سيليلوز، ثاني أكسيد السيليكون الغروي، صوديوم لاورايل سلفيت، ستيرات المغنيسيوم .
غشاء القرص: مونوهيدرات اللاكتوز، هايبرميللوز، تراياسيتين، وثاني أكسيد التيتانيوم، وأكسيد الحديد الأصفر، التالك

ب.كيف يبدو شكل هذا المستحضر وماهي محتويات العلبة:
تادالو تركيز 20 ملجم يوجد بأقراص صفراء مغلفة بغشاء رقيق على شكل اللوز وعلى أحد الأوجه توجد علامة T20
تادالو 20 ملجم متوفّر في علبة تحتوي على 4 أقراص .

مصنع شركة الرازي للصناعات الدوائية
المدينة الصناعية الثانية شارع رقم 67 تقاطع 110
رقم المبنى 3992
المملكة العربية السعودية الدما م.
+ 966 13 تليفون: 8281919
+ 966 13 فاك س: 8251313
www.alrazi-pharma.com : الموقع الإكتروني

03/2022
 Read this leaflet carefully before you start using this product as it contains important information for you

Tadalafil 20 mg film-coated tablets.

Tadalafil 20 mg: Each film-coated tablet contains 20 mg tadalafil. Excipient with known effect: Each 20 mg tablet contains: lactose monohydrate 261.90 mg For the full list of excipients, see section 6.1.

Film-coated tablet Tadalafil 20 mg: yellow colored, caplet shaped, biconvex, film coated tablet, debossed with “T 20” on one side and plain on the other.

Treatment of erectile dysfunction in adult males.
In order for tadalafil to be effective, sexual stimulation is required.
Tadalafil is not indicated for use by women.


Posology
Adult men
In general, the recommended dose is 10 mg taken prior to anticipated sexual activity and with or without food.
In those patients in whom tadalafil 10 mg does not produce an adequate effect, 20 mg might be tried.
It may be taken at least 30 minutes prior to sexual activity.
The maximum dose frequency is once per day.
Tadalafil 10 and 20 mg is intended for use prior to anticipated sexual activity and it is not recommended for continuous daily use.
In patients who anticipate a frequent use of Tadalafil (i.e., at least twice weekly) a once daily regimen with the lowest doses of Tadalafil might be considered suitable, based on patient choice and the physician’s judgement.

In these patients the recommended dose is 5 mg taken once a day at approximately the same time of day.
The dose may be decreased to 2.5 mg once a day based on individual tolerability.
The appropriateness of continued use of the daily regimen should be reassessed periodically.
Special populations
Elderly men
Dose adjustments are not required in elderly patients.
Men with renal impairment
Dose adjustments are not required in patients with mild to moderate renal impairment. For patients with severe renal impairment 10 mg is the maximum recommended dose. Once-a-day dosing of tadalafil is not recommended in patients with severe renal impairment. (See sections 4.4 and 5.2).
Men with hepatic impairment
The recommended dose of Tadalafil is 10 mg taken prior to anticipated sexual activity and with or without food. There is limited clinical data on the safety of tadalafil in patients with severe hepatic impairment (Child-Pugh Class C); if prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician. There are no available data about the administration of doses higher than 10 mg of tadalafil to patients with hepatic impairment. Once-a-day dosing has not been evaluated in patients with hepatic impairment; therefore, if prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician (see sections 4.4 and 5.2).
Men with diabetes Dose adjustments are not required in diabetic patients.
Paediatric population
There is no relevant use of tadalafil in the paediatric population with regard to the treatment of erectile dysfunction.
Method of administration
TADALAFIL is available as 20 mg film-coated tablets for oral use.


Hypersensitivity to the active substance or to any of the excipients listed in section 6.1. In clinical studies, tadalafil was shown to augment the hypotensive effects of nitrates. This is thought to result from the combined effects of nitrates and tadalafil on the nitric oxide/cGMP pathway. Therefore, administration of Tadalafil to patients who are using any form of organic nitrate is contraindicated. (See section 4.5). Tadalafil must not be used in men with cardiac disease for whom sexual activity is inadvisable. Physicians should consider the potential cardiac risk of sexual activity in patients with pre-existing cardiovascular disease. The following groups of patients with cardiovascular disease were not included in clinical trials and the use of tadalafil is therefore contraindicated:  Patients with myocardial infarction within the last 90 days.  Patients with unstable angina or angina occurring during sexual intercourse.  Patients with New York Heart Association Class 2 or greater heart failure in the last 6 months.  Patients with uncontrolled arrhythmias, hypotension (< 90/50 mm Hg), or uncontrolled hypertension.  Patients with a stroke within the last 6 months. Tadalafil is contraindicated in patients who have loss of vision in one eye because of non-arteritic anterior ischaemic optic neuropathy (NAION), regardless of whether this episode was in connection or not with previous PDE5 inhibitor exposure (See section 4.4). The co-administration of PDE5 inhibitors, including tadalafil, with guanylate cyclase stimulators, such as riociguat, is contraindicated as it may potentially lead to symptomatic hypotension (see section 4.5).

Before treatment with Tadalafil
A medical history and physical examination should be undertaken to diagnose erectile dysfunction and determine potential underlying causes, before pharmacological treatment is considered.
Prior to initiating any treatment for erectile dysfunction, physicians should consider the cardiovascular status of their patients, since there is a degree of cardiac risk associated with sexual activity. Tadalafil has vasodilator properties, resulting in mild and transient decreases in blood pressure (see section 5.1) and as such potentiates the hypotensive effect of nitrates (see section 4.3).
The evaluation of erectile dysfunction should include a determination of potential underlying causes and the identification of appropriate treatment following an appropriate medical assessment. It is not known if Tadalafil is effective in patients who have undergone pelvic surgery or radical non-nervesparing prostatectomy.
Cardiovascular
Serious cardiovascular events, including myocardial infarction, sudden cardiac death, unstable angina pectoris, ventricular arrhythmia, stroke, transient ischemic attacks, chest pain, palpitations and tachycardia, have been reported either post marketing and/or in clinical trials. Most of the patients in
whom these events have been reported had pre-existing cardiovascular risk factors. However, it is not possible to definitively determine whether these events are related directly to these risk factors, to tadalafil, to sexual activity, or to a combination of these or other factors.

In patients who are taking alpha1 blockers, concomitant administration of Tadalafil may lead to symptomatic hypotension in some patients (see section 4.5). The combination of tadalafil and doxazosin is not recommended.
Vision
Visual defects and cases of NAION have been reported in connection with the intake of tadalafil and other PDE5 inhibitors. The patient should be advised that in case of sudden visual defect, he should stop taking Tadalafil and consult a physician immediately (see section 4.3).
Hepatic impairment
There is limited clinical data on the safety of single-dose administration of tadalafil in patients with severe hepatic insufficiency (Child-Pugh Class C). If Tadalafil is prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician.
Priapism and anatomical deformation of the penis Patients who experience erections lasting 4 hours or more should be instructed to seek immediate medical assistance. If priapism is not treated immediately, penile tissue damage and permanent loss of potency may result.
Tadalafil, should be used with caution in patients with anatomical deformation of the penis (such as angulation, cavernosal fibrosis or Peyronie's disease), or in patients who have conditions which may predispose them to priapism (such as sickle cell anemia, multiple myeloma or leukemia).
Use with CYP3A4 inhibitors
Caution should be exercised when prescribing Tadalafil to patients using potent CYP3A4 inhibitors (ritonavir, saquinavir, ketoconazole, itraconazole, and erythromycin) as increased tadalafil exposure (AUC) has been observed if the medicinal products are combined (see section 4.5).
Tadalafil and other treatments for erectile dysfunction
The safety and efficacy of combinations of tadalafil and other PDE5 inhibitors or other treatments for erectile dysfunction have not been studied. The patients should be informed not to take Tadalafil in such combinations.
Lactose
Tadalafil contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicinal product.


Interaction studies were conducted with 10 mg and/or 20 mg tadalafil, as indicated below. With regard to those interaction studies where only the 10 mg tadalafil dose was used, clinically relevant interactions at higher doses cannot be completely ruled out.

Effects of other substances on tadalafil
Cytochrome P450 inhibitors
Tadalafil is principally metabolized by CYP3A4. A selective inhibitor of CYP3A4, ketoconazole (200 mg daily), increased tadalafil (10 mg) exposure (AUC) 2-fold and Cmax by 15 %, relative to the AUC and Cmax values for tadalafil alone. Ketoconazole (400 mg daily) increased tadalafil (20 mg) exposure (AUC) 4-
fold and Cmax by 22 %.
Ritonavir, a protease inhibitor (200 mg twice daily), which is an inhibitor of CYP3A4, CYP2C9, CYP2C19, and CYP2D6, increased tadalafil (20 mg) exposure (AUC) 2- fold with no change in Cmax.
Although specific interactions have not been studied, other protease inhibitors, such as saquinavir, and other CYP3A4 inhibitors, such as erythromycin, clarithromycin, itraconazole and grapefruit juice should be co-administered with caution as they would be expected to increase plasma concentrations of tadalafil (see section 4.4).
Consequently the incidence of the adverse reactions listed in section 4.8 might be increased.
Transporters
The role of transporters (for example p-glycoprotein) in the disposition of tadalafil is not known.
Therefore there is the potential of drug interactions mediated by inhibition of transporters.
Cytochrome P450 inducers
A CYP3A4 inducer, rifampicin, reduced tadalafil AUC by 88 %, relative to the AUC values for tadalafil alone (10 mg). This reduced exposure can be anticipated to decrease the efficacy of tadalafil; the magnitude of decreased efficacy is unknown.
Other inducers of CYP3A4 such as phenobarbital, phenytoin and carbamazepine, may also decrease plasma concentrations of tadalafil.
Effects of tadalafil on other medicinal products
Nitrates
In clinical studies, tadalafil (5, 10 and 20 mg) was shown to augment the hypotensive effects of nitrates.
Therefore, administration of Tadalafil to patients who are using any form of organic nitrate is contraindicated (see section 4.3). Based on the results of a clinical study in which 150 subjects receiving daily doses of tadalafil 20 mg for 7 days and 0.4 mg sublingual nitroglycerin at various times, this interaction lasted for more than 24 hours and was no longer detectable when 48 hours had elapsed after the last tadalafil dose. Thus, in a patient prescribed any dose of Tadalafil (2.5 mg-20 mg), where nitrate administration is deemed medically necessary in a life-threatening situation, at least 48 hours should have elapsed after the last dose of Tadalafil before nitrate administration is considered. In such circumstances, nitrates should only be administered under close medical supervision with appropriate haemodynamic monitoring.

Anti-hypertensives (including calcium channel blockers)
The co-administration of doxazosin (4 and 8 mg daily) and tadalafil (5 mg daily dose and 20 mg as a single dose) increases the blood pressure-lowering effect of this alpha-blocker in a significant manner.
This effect lasts at least twelve hours and may be symptomatic, including syncope. Therefore this combination is not recommended (see section 4.4).
In interaction studies performed in a limited number of healthy volunteers, these effects were not reported with alfuzosin or tamsulosin. However, caution should be exercised when using tadalafil in patients treated with any alpha-blockers, and notably in the elderly. Treatments should be initiated at minimal
dosage and progressively adjusted.
In clinical pharmacology studies, the potential for tadalafil to augment the hypotensive effects of antihypertensive medicinal products was examined. Major classes of antihypertensive medicinal products were studied, including calcium channel blockers (amlodipine), angiotensin converting enzyme (ACE) inhibitors (enalapril), beta-adrenergic receptor blockers (metoprolol), thiazide diuretics (bendrofluazide), and angiotensin II receptor blockers (various types and doses, alone or in combination with thiazides, calcium channel blockers, beta-blockers, and/or alpha-blockers).
Tadalafil (10 mg except for studies with angiotensin II receptor blockers and amlodipine in which a 20 mg dose was applied) had no clinically significant interaction with any of these classes. In another clinical pharmacology study tadalafil (20 mg) was studied in combination with up to 4 classes of antihypertensives. In subjects taking multiple antihypertensives, the ambulatory-blood-pressure changes appeared to relate to the degree of blood-pressure control. In this regard, study subjects whose blood pressure was well controlled, the reduction was minimal and similar to that seen in healthy subjects. In study subjects whose blood pressure was not controlled, the reduction was greater although this reduction was not associated with hypotensive symptoms in the majority of subjects. In patients receiving concomitant antihypertensive medicinal products, tadalafil 20 mg may induce a blood pressure decrease, which (with the exception of alpha blockers -see above-) is, in general, minor and not likely to be clinically relevant. Analysis of phase 3 clinical trial data showed no difference in adverse events in patients taking tadalafil with or without antihypertensive medicinal products. However, appropriate clinical advice should be given to patients regarding a possible decrease in blood pressure when they are treated with antihypertensive medicinal products.
Riociguat
Preclinical studies showed an additive systemic blood pressure lowering effect when PDE5 inhibitors were combined with riociguat. In clinical studies, riociguat has been shown to augment the hypotensive effects of PDE5 inhibitors. There was no evidence of favourable clinical effect of the combination in the
population studied. Concomitant use of riociguat with PDE5 inhibitors, including tadalafil, is contraindicated (see section 4.3).
5- Alpha reductase inhibitors
In a clinical trial that compared tadalafil 5 mg co-administered with finasteride 5 mg to placebo plus finasteride 5 mg in the relief of BPH symptoms, no new adverse reactions were identified. However, as a formal drug-drug interaction study evaluating the effects of tadalafil and 5-alpha reductase inhibitors (5- ARIs) has not been performed, caution should be exercised when Tadalafil is co-administered with 5- ARIs. CYP1A2 substrates (e.g. theophylline) When tadalafil 10 mg was administered with theophylline (a non-selective phosphodiesterase inhibitor) in a clinical pharmacology study, there was no pharmacokinetic interaction. The only pharmacodynamic effect was a small (3.5 bpm) increase in heart rate. Although this effect is minor and was of no clinical significance in this study, it should be considered when co-administering these medicinal products.
Ethinylestradiol and terbutaline
Tadalafil has been demonstrated to produce an increase in the oral bioavailability of ethinylestradiol; a similar increase may be expected with oral administration of terbutaline, although the clinical consequence of this is uncertain.
Alcohol
Alcohol concentrations (mean maximum blood concentration 0.08 %) were not affected by coadministration with tadalafil (10 mg or 20 mg). In addition, no changes in tadalafil concentrations were seen 3 hours after co-administration with alcohol.
Alcohol was administered in a manner to maximize the rate of alcohol absorption (overnight fast with no food until 2 hours after alcohol).
Tadalafil (20 mg) did not augment the mean blood pressure decrease produced by alcohol (0.7 g/kg or approximately 180 ml of 40 % alcohol [vodka] in an 80-kg male) but in some subjects, postural dizziness and orthostatic hypotension were observed.
When tadalafil was administered with lower doses of alcohol (0.6 g/kg), hypotension was not observed and dizziness occurred with similar frequency to alcohol alone. The effect of alcohol on cognitive function was not augmented by tadalafil (10 mg).
Cytochrome P450 metabolized medicinal products
Tadalafil is not expected to cause clinically significant inhibition or induction of the clearance of medicinal products metabolized by CYP450 isoforms. Studies have confirmed that tadalafil does not inhibit or induce CYP450 isoforms, including CYP3A4, CYP1A2, CYP2D6, CYP2E1, CYP2C9 and
CYP2C19.

CYP2C9 substrates (e.g. R-warfarin)
Tadalafil (10 mg and 20 mg) had no clinically significant effect on exposure (AUC) to S-warfarin or Rwarfarin (CYP2C9 substrate), nor did tadalafil affect changes in prothrombin time induced by warfarin. 
Aspirin
Tadalafil (10 mg and 20 mg) did not potentiate the increase in bleeding time caused by acetyl salicylic acid.
Antidiabetic medicinal products
Specific interaction studies with antidiabetic medicinal products were not conducted.


Tadalafil is not indicated for use by women.
Pregnancy
There are limited data from the use of tadalafil in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to pregnancy, embryonal/fetal development, parturition or postnatal development (see section 5.3). As a precautionary measure, it is preferable to avoid the use of Tadalafil during pregnancy.
Breastfeeding
Available pharmacodynamic/toxicological data in animals have shown excretion of tadalafil in milk.
A risk to the suckling child cannot be excluded. Tadalafil should not be used during breast feeding.
Fertility
Effects were seen in dogs that might indicate impairment of fertility. Two subsequent clinical studies suggest that this effect is unlikely in humans, although a decrease in sperm concentration was seen in some men (see sections 5.1 and 5.3).


Tadalafil has negligible influence on the ability to drive or use machines.
Although the frequency of reports of dizziness in placebo and tadalafil arms in clinical trials was
similar, patients should be aware of how they react to Tadalafil, before driving or using machines.


Summary of the safety profile
The most commonly reported adverse reactions in patients taking tadalafil for the treatment of erectile dysfunction or benign prostatic hyperplasia were headache, dyspepsia, back pain and myalgia, in which the incidences increase with increasing dose of tadalafil. The adverse reactions reported were transient, and generally mild or moderate. The majority of headaches reported with tadalafil once-a day dosing are experienced within the first 10 to 30 days of starting treatment.

Tabulated summary of adverse reactions
The table below lists the adverse reactions observed from spontaneous reporting and in placebocontrolled clinical trials (comprising a total of 8022 patients on tadalafil and 4422 patients on placebo) for on-demand and once-a-day treatment of erectile dysfunction and the once-a-day treatment of benign prostatic hyperplasia.
Frequency convention: very common (≥1/10), common (≥1/100 to <1/10), uncommon (≥1/1000 to <1/100), rare (≥1/10,000 to <1/1,000) and very rare (<1/10,000) and not known (cannot be estimated from the available data).

System organ classFrequencyPreferred Term
Immune system disordersUncommonHypersensitivity reactions
RareAngioedema2
Nervous system disordersCommonHeadache
UncommonDizziness
RareStroke1 (including haemorrhagic events), Syncope, Transient ischaemic attacks1, Migraine2, Seizures, Transient amnesia
Eye disordersUncommonBlurred vision, Sensations described as eye pain.
RareVisual field defect, swelling of eyelids, Conjunctival hyperaemia, Non-arteritic anterior ischemic optic neuropathy (NAION) 2, Retinal vascular occlusion2.
Ear and labyrinth disordersUncommonTinnitus
RareSudden hearing loss
Cardiac disorders1UncommonTachycardia, Palpitations
RareMyocardial infarction, unstable angina pectoris2, Ventricular arrhythmia2
Vascular disordersCommonFlushing
UncommonHypotension3, Hypertension
Respiratory, thoracic and mediastinal disordersCommonNasal congestion
UncommonDyspnoea, Epistaxis
Gastrointestinal disordersCommonDyspepsia
UncommonAbdominal pain, Vomiting, Nausea, Gastro-oesophageal reflux
Skin and subcutaneous tissue disordersUncommonRash
RareUrticaria, Stevens-Johnson syndrome2, Exfoliative dermatitis2, Hyperhydrosis (sweating)
Musculoskeletal, connective tissue and bone disordersUncommonBack pain, Myalgia, Pain in extremity
Renal and urinary disordersUncommonHaematuria
Reproductive system and breast disordersUncommonProlonged erections
RarePriapism2, Penile haemorrhage, Haematospermia
General disorders and administration site conditionsUncommonChest pain1, Peripheral oedema, Fatigue
Rare

Facial oedema2, Sudden cardiac death1,2

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

 

(1) Most of the patients had pre-existing cardiovascular risk factors (see section 4.4).
(2) Post marketing surveillance reported adverse reactions not observed in placebo controlled clinical trials.
(3) More commonly reported when tadalafil is given to patients who are already taking antihypertensive medicinal products.


Description of selected adverse reactions
A slightly higher incidence of ECG abnormalities, primarily sinus bradycardia, has been reported in patients treated with tadalafil once a day as compared with placebo.
Most of these ECG abnormalities were not associated with adverse reactions.
Other special populations
Data in patients over 65 years of age receiving tadalafil in clinical trials, either for the treatment of erectile dysfunction or the treatment of benign prostatic hyperplasia, are limited. In clinical trials with tadalafil taken on demand for the treatment of erectile dysfunction, diarrhea was reported more frequently in patients over 65 years of age.
In clinical trials with tadalafil 5mg taken once a day for the treatment of benign prostatic hyperplasia, dizziness and diarrhea were reported more frequently in patients over 75 years of age.

Reporting of suspected adverse reactions
To report any side effects please contact;
National Pharmacovigilance and Drug Safety Centre (NPC)
SFDA Call Center: 19999
E-mail: npc.drug@sfda.gov.sa
Website: https://ade.sfda.gov.sa/


Single doses of up to 500 mg have been given to healthy subjects, and multiple daily doses up to 100 mg have been given to patients. Adverse events were similar to those seen at lower doses.
In cases of overdose, standard supportive measures should be adopted as required.
Hemodialysis contributes negligibly to tadalafil elimination.


Pharmacotherapeutic group: Urologicals, Drugs used in erectile dysfunction, ATC Code: G04BE08.
Mechanism of action
Tadalafil is a selective, reversible inhibitor of cyclic guanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5). When sexual stimulation causes the local release of nitric oxide, inhibition of PDE5 by tadalafil produces increased levels of cGMP in the corpus cavernosum. This results in smooth muscle relaxation and inflow of blood into the penile tissues, thereby producing an erection. Tadalafil has no effect in the absence of sexual stimulation.
Pharmacodynamic effects
Studies in vitro have shown that tadalafil is a selective inhibitor of PDE5. PDE5 is an enzyme found in corpus cavernosum smooth muscle, vascular and visceral smooth muscle, skeletal muscle, platelets, kidney, lung, and cerebellum. The effect of tadalafil is more potent on PDE5 than on other phosphodiesterases. Tadalafil is > 10,000-fold more potent for PDE5 than for PDE1, PDE2, and PDE4 enzymes which are found in the heart, brain, blood vessels, liver, and other organs. Tadalafil is > 10,000- fold more potent for PDE5 than for PDE3, an enzyme found in the heart and blood vessels.
This selectivity for PDE5 over PDE3 is important because PDE3 is an enzyme involved in cardiac contractility. Additionally, tadalafil is approximately 700-fold more potent for PDE5 than for PDE6, an enzyme which is found in the retina and is responsible for phototransduction. Tadalafil is also > 10,000 fold more potent for PDE5 than for PDE7 through PDE10.

Clinical efficacy and safety
Three clinical studies were conducted in 1054 patients in an at-home setting to define the period of responsiveness to tadalafil. Tadalafil demonstrated statistically significant improvement in erectile function and the ability to have successful sexual intercourse up to 36 hours following dosing, as well as patients’ ability to attain and maintain erections for successful intercourse compared to placebo as early as 16 minutes following dosing.
Tadalafil administered to healthy subjects produced no significant difference compared to placebo in supine systolic and diastolic blood pressure (mean maximal decrease of 1.6/0.8 mm Hg, respectively), in standing systolic and diastolic blood pressure (mean maximal decrease of 0.2/4.6 mm Hg, respectively), and no significant change in heart rate.
In a study to assess the effects of tadalafil on vision, no impairment of color discrimination (blue/green) was detected using the Farnsworth-Munsell 100-hue test.
This finding is consistent with the low affinity of tadalafil for PDE6 compared to PDE5. Across all clinical studies, reports of changes in color vision were rare (< 0.1 %).
Three studies were conducted in men to assess the potential effect on spermatogenesis of tadalafil 10 mg (one 6-month study) and 20 mg (one 6-month and one 9-month study) administered daily. In two of these studies decreases were observed in sperm count and concentration related to tadalafil treatment of unlikely clinical relevance. These effects were not associated with changes in other parameters such as motility, morphology and FSH.
Tadalafil at doses of 2 to 100 mg has been evaluated in 16 clinical studies involving 3250 patients, including patients with erectile dysfunction of various severities (mild, moderate, severe), etiologies, ages (range 21-86 years), and ethnicities. Most patients reported erectile dysfunction of at least 1 year in duration. In the primary efficacy studies of general populations, 81 % of patients reported that tadalafil improved their erections as compared to 35 % with placebo. Also, patients with erectile dysfunction in all severity categories reported improved erections whilst taking tadalafil (86 %, 83 %, and 72 % for mild, moderate, and severe, respectively, as compared to 45 %, 42 %, and 19 % with placebo). In the primary efficacy studies, 75 % of intercourse attempts were successful in tadalafil treated patients as compared to 32 % with placebo.
In a 12-week study performed in 186 patients (142 tadalafil, 44 placebo) with erectile dysfunction secondary to spinal cord injury, tadalafil significantly improved the erectile function leading to a mean per-subject proportion of successful attempts in patients treated with tadalafil 10 or 20 mg (flexible-dose, on demand) of 48 % as compared to 17 % with placebo.

Paediatric population
The European Medicines Agency has waived the obligation to submit the results of studies in all subsets of the paediatric population in the treatment of the erectile dysfunction. See section 4.2 for information on paediatric use.


Absorption
Tadalafil is readily absorbed after oral administration and the mean maximum observed plasma concentration (Cmax) is achieved at a median time of 2 hours after dosing. Absolute bioavailability of tadalafil following oral dosing has not been determined.
The rate and extent of absorption of tadalafil are not influenced by food, thus Tadalafil may be taken with or without food. The time of dosing (morning versus evening) had no clinically relevant effects on the rate and extent of absorption.
Distribution
The mean volume of distribution is approximately 63 l, indicating that tadalafil is distributed into tissues.
At therapeutic concentrations, 94 % of tadalafil in plasma is bound to proteins. Protein binding is not affected by impaired renal function.
Less than 0.0005 % of the administered dose appeared in the semen of healthy subjects.
Biotransformation
Tadalafil is predominantly metabolized by the cytochrome P450 (CYP) 3A4 isoform. The major circulating metabolite is the methyl catechol glucuronide. This metabolite is at least 13,000 fold less potent than tadalafil for PDE5. Consequently, it is not expected to be clinically active at observed metabolite concentrations.
Elimination
The mean oral clearance for tadalafil is 2.5 l/h and the mean half-life is 17.5 hours in healthy subjects. Tadalafil is excreted predominantly as inactive metabolites, mainly in the faeces (approximately 61 % of the dose) and to a lesser extent in the urine (approximately 36 % of the dose).
Linearity/non-linearity
Tadalafil pharmacokinetics in healthy subjects are linear with respect to time and dose. Over a dose range of 2.5 to 20 mg, exposure (AUC) increases proportionally with dose. Steady-state plasma concentrations are attained within 5 days of once-daily dosing.
Pharmacokinetics determined with a population approach in patients with erectile dysfunction are similar to pharmacokinetics in subjects without erectile dysfunction.

Special populations
Elderly
Healthy elderly subjects (65 years or over), had a lower oral clearance of tadalafil, resulting in 25 % higher exposure (AUC) relative to healthy subjects aged 19 to 45 years. This effect of age is not clinically significant and does not warrant a dose adjustment.
Renal insufficiency
In clinical pharmacology studies using single-dose tadalafil (5 to 20 mg), tadalafil exposure (AUC) approximately doubled in subjects with mild (creatinine clearance 51 to 80 ml/min) or moderate (creatinine clearance 31 to 50 ml/min) renal impairment and in subjects with end-stage renal disease on dialysis. In haemodialysis patients, Cmax was 41 % higher than that observed in healthy subjects. Haemodialysis contributes negligibly to tadalafil elimination.
Hepatic insufficiency
Tadalafil exposure (AUC) in subjects with mild and moderate hepatic impairment (Child-Pugh Class A and B) is comparable to exposure in healthy subjects when a dose of 10 mg is administered. There is limited clinical data on the safety of tadalafil in patients with severe hepatic insufficiency (Child-Pugh Class C). If Tadalafil is prescribed, a careful individual benefit/risk evaluation should be undertaken by the prescribing physician. There are no available data about the administration of doses higher than 10 mg of tadalafil to patients with hepatic impairment.
Patients with diabetes
Tadalafil exposure (AUC) in patients with diabetes was approximately 19 % lower than the AUC value for healthy subjects. This difference in exposure does not warrant a dose adjustment.


Non-clinical data reveal no special hazard for humans based on conventional studies of safety pharmacology, repeated dose toxicity, genotoxicity, carcinogenic potential, and toxicity to reproduction.
There was no evidence of teratogenicity, embryo toxicity or foetotoxicity in rats or mice that received up to 1000 mg/kg/day tadalafil. In a rat prenatal and postnatal development study, the no observed effect dose was 30 mg/kg/day. In the pregnant rat the AUC for calculated free drug at this dose was approximately 18 times the human AUC at a 20 mg dose.
There was no impairment of fertility in male and female rats. In dogs given tadalafil daily for 6 to 12 months at doses of 25 mg/kg/day (resulting in at least a 3-fold greater exposure [range 3.7 – 18.6] than seen in humans given a single 20 mg dose) and above, there was regression of the seminiferous tubular epithelium that resulted in a decrease in spermatogenesis in some dogs. See also section 5.1.


Tablet core
Lactose monohydrate
Croscarmellose sodium
Sodium laurilsulfate
Hydroxypropylcellulose
Colloidal silicon dioxide
Magnesium stearate
Coating
Hypromellose 2910 (E464)
Lactose monohydrate
Titanium dioxide (E171)
Triacetin
Talc (E553b)
Iron oxide yellow (E172)


Not applicable


24 months

Do not store above 30°c. Store in the original package in order to protect from moisture.


PVC/PVDC/ Aluminum blisters
Pack of: 4 film-coated tablets.


No special requirements.
Any unused medicinal product or waste material should be disposed of in accordance with local requirements.


AL RAZI PHARMA INDUSTRIES 2nd Industrial City – Street No. 67 Cross 110 Building No. 3992 Dammam Kingdom of Saudi Arabia “KSA” . Tel: +966 13 8281919 Fax: +966 13 8281313 Website: www.alrazi-pharma.com

05/2021
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