خواص دارویی و گیاهی
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قرص ibuprofen چیست
کاربر جدید هستم!
1
موضوعات داغ
قرص ایبوپروفن (Ibuprofen) چیست و چه کاربردهایی دارد؟ در چه شرایطی و به چه صورت مصرف می‌شود؟ عوارض جانبی آن کدامند؟ مصرف این قرص در دوران بارداری یا شیردهی مجاز است؟ چه داروهایی را نباید به طور همزمان با قرص ایبوپروفن (Ibuprofen) مصرف کرد؟ این سوالات، به همراه نکات و اطلاعات مهم درباره‌ی این دارو، در مطلب پیش‌رو بررسی خواهد شد.
ایبوپروفن (Ibuprofen) که با نام های تجاری ادویل (Advil)، جنپریل (Genpril)، میدل آی بی ( Midol IB)، مورتین آی بی (Motrin IB)، پروپرینال (Proprinal) و غیره، نیز شناخته می‌شود، یک داروی ضد التهابی غیر استروئیدی است. نحوه‌ی کارکرد آن بدین شکل است که هورمون‌هایی را که در بدن باعث التهاب و درد می‌شوند را کاهش می‌دهد.
ایبوپروفن برای کاهش تب، بهبود درد یا التهابی که توسط شرایط مختلفی (از جمله سردرد، دندان درد، کمردرد، آرتریت، گرفتگی عضلات در هنگام قاعدگی زنان، یا جراحت‌های خفیف) ایجاد شده باشد، مورد استفاده قرار می‌گیرد.
ایبوپروفن برای افراد بزرگسال و نوزادانی که بیشتر از ۶ ماه دارند، می‌تواند مورد استفاده قرار بگیرد.
مصرف ایبوپروفن، خطر حمله‌ی قلبی کُشنده یا سکته‌ی مغزی را در افراد افزایش می‌دهد. مخصوصاً اگر شما این دارو را به صورت طولانی مدت و یا دوز مصرفی زیاد استفاده کنید و یا مشکلات قلبی داشته باشید.
این دارو را بلافاصله قبل یا بعد از عمل بای پسِ قلب (پیوند عروق کرونر یا CABG) مصرف نکنید.
ایبوپروفن همچنین ممکن است باعث ایجاد خونریزی معده یا روده شود که می‌تواند خطرناک و کُشنده باشد. این وضعیت ممکن است در دوره مصرف ایبوپروفن، بدون هیچ‌گونه هشداری و مخصوصاً در افراد مُسن‌تر، اتفاق بیفتد.
بیشتر از دوز مصرفی که برای شما تجویز شده، ایبوپروفن را مصرف نکنید. مصرف بیش از حد این دارو می‌تواند باعث ایجاد آسیب در معده یا روده‌ی شما شود. صرفاً از کمترین میزانی از ایبوپروفن که باعث تسکین درد، التهاب یا تب می‌شود، استفاده کنید.
یادآوری می‌شود که مصرف ایبوپروفن، خطر حمله‌ی قلبی کُشنده یا سکته‌ی مغزی را در افراد افزایش می‌دهد. مخصوصاً اگر شما این دارو را به صورت طولانی مدت و یا دوز مصرفی زیاد استفاده کنید و یا مشکلات قلبی داشته باشید. حتی افرادی که مشکلات قلبی یا وضعیت ریسک‌داری ندارند، ممکن است در دوره مصرف این دارو دچار حمله‌ی قلبی یا سکته‌ی مغزی بشوند.
مجدداً یادآوری می‌شود که این دارو را بلافاصله قبل یا بعد از عمل بای پسِ قلب (پیوند عروق کرونر یا CABG) مصرف نکنید. ایبوپروفن همچنین ممکن است باعث ایجاد خونریزی معده یا روده شود که می‌تواند خطرناک و کُشنده باشد. این وضعیت ممکن است در دوره مصرف ایبوپروفن، بدون هیچ‌گونه هشداری و مخصوصاً در افراد مُسن‌تر، اتفاق بیفتد.
در صورتی که نسبت به داروی ایبوپروفن حساسیت دارید، یا اینکه تا به حال حمله‌ی آسم یا واکنش‌های آلرژیکی شدید پس از مصرف آسپرین یا یک داروی ضد التهابی غیر استروئیدی داشته‌اید، نباید ایبوپروفن را استفاده کنید.
اگر موارد زیر را دارید، قبل از مصرف این دارو از دکتر یا مسئول داروخانه بپرسید که آیا مصرف ایبوپروفن برای شما خطری ایجاد می‌کند یا خیر:
– بیماری قلبی، فشار خون بالا، کلسترول بالا، دیابت، یا اگر سیگار می‌کشید؛
– سابقه‌ی حمله‌ی قلبی، سکته‌ی مغزی یا لخته شدن خون؛
– سابقه‌ی خونریزی معده یا زخم معده؛
– آسم؛
– بیماری کبدی یا کلیوی؛
– حبس مایعات در بدن؛
– یک بیماری بافت همبند مانند سندرم مارفان، سندرم سوگرون یا لوپوس؛
مصرف این دارو در سه ماهه‌ی آخر بارداری ممکن است باعث ایجاد آسیب در جنین شود. اگر باردار هستید، ایبوپروفن را بدون تجویز پزشک و اجازه‌ی او مصرف نکنید.
هنوز مشخص نیست که آیا مصرف داروی ایبوپروفن در شیر مادر نفوذ پیدا کرده و روی نوزاد تاثیراتی دارد یا خیر؛ اگر در دوران شیردهی قرار دارید، قبل از مصرف این دارو با دکتر خود مشورت نمائید.
ایبوپروفن را بدون تجویز پزشک، به کودکان زیر ۲ سال ندهید.
ایبوپروفن را حتماً با تجویز پزشک مصرف کنید. این دارو را به همان صورتی که روی جعبه‌ی آن یا برگه‌ی راهنمای مصرف نوشته شده و یا دکتر برای شما تجویز کرده، مصرف کنید. همچنین از مصرف دوز بیشتر یا طولانی‌تر این دارو خودداری کنید. از کمترین میزانی از این دارو که باعث بهبود وضعیت فعلی‌تان می‌شود، استفاده کنید.
از مصرف بیش از میزانی که برای شما تجویز شده، خودداری نمائید. مصرف بیش از حد ایبوپروفن می‌تواند باعث ایجاد آسیب در معده یا روده‌ی شما شود. بیشتری میزان مصرف مجاز این دارو در بزرگسالان، در هر دوز ۸۰۰ میلی‌گرم و یا در هر روز، ۳۲۰۰ میلی‌گرم (۴ دوز مصرفی) می‌باشد. فقط به کمترین میزانی از این دارو استفاده کنید که باعث بهبود درد، تورم یا تب شما می‌شود.
میزان مصرف ایبوپروفن در کودکان، به وزن و سن آن‌ها بستگی دارد. به دقت مواردی را که در مورد میزان مصرف ایبوپروفن برای کودکان، نوشته شده مد نظر قرار بدهید. اگر سوالی در این مورد دارید، از دکتر یا مسئول داروخانه سوال کنید.
برای اینکه معده درد را به هنگام مصرف این دارو به حداقل برسانید، آن را به همراه غذا یا با شیر مورد استفاده قرار بدهید.
نوع مایع این دارو را قبل از مصرف به خوبی تکان دهید. همچنین آن را از یخ‌زدگی محافظت کنید.
نوع جویدینیِ ایبوپروفن را قبل از قورت دادن باید به خوبی بجوید.
اگر این دارو را به مدت طولانی مورد استفاده قرار می‌دهید، ممکن است نیاز باشد تا به صورت دوره‌ای، آژمایشاتی را برای بررسی سلامت خود انجام بدهید.
دارو را در دمای اتاق نگهداری کرده و دور از گرما و رطوبت قرار دهید.
قرص ibuprofen چیست
تمامی دستورالعمل‌ها، راهنماها و نکات مورد نظر برای مصرف این دارو را به دقت مطالعه نموده و در صورتی که هر سوال داشتید، فقط از مسئول داروخانه یا دکتر (نه فامیل و دوست و آشنا که تخصصی ندارند!) بپرسید.
به دلیل اینکه ایبوپروفن، زمانی که مورد نیاز است مصرف می‌شود، بنابراین در اغلب موارد احتمالاً یک برنامه‌ی زمانی برای مصرف آن ندارید. در صورتی که یک برنامه‌ی زمانی مشخص برای مصرف این دارو دارید، اگر یک بار مصرف ایبوپروفن را فراموش کردید، به محض اینکه به یاد آوردید، آن را مصرف کنید. اما چنانچه زمانِ به یادآوری شما، بسیار نزدیک به زمانِ مصرفِ بعدی بود، دوز فراموش شده را مصرف نکنید. فقط در نوبت بعدی، ایبوپروفن را مصرف کنید. توجه داشته باشید که برای جبران دوز مصرفی فراموش شده، داروی اضافی مصرف نکنید.
چنانچه بیشتر از میزان مورد نیاز، این دارو را مصرف کردید، به موارد اورژانسی در مورد مصرف زیاد این دارو مراجعه کنید و یا از پزشک کمک بگیرید. علائم مصرف بیش از حد این دارو عبارتند از:
حالت تهوع، استفراغ، دل درد، خواب‌آلودگی، مدفوع سیاه یا خونی، سرفه به همراه بالا آوردن خون، تنفس سطحی و کم عمق، غش کردن یا بیهوش شدن.
از نوشیدن الکل خودداری کنید؛ زیرا ممکن است خطر خونریزی معده را در شما افزایش دهد.
از مصرف آسپرین در دوره مصرف ایبوپروفن خودداری کنید. اگر در حال مصرف آسپرین برای پیشگیری از سکته‌ی مغزی یا حمله‌ی قلبی هستید، از مصرف ایبوپروفن خودداری نمائید؛ زیرا ایبوپروفن باعث کاهش تاثیر آسپرین در محافظت از قلب و رگ‌های خونی، می‌شود. در صورتی که مجبورید که هر دو دارو را مصرف کنید، ایبوپروفن را حداقل ۸ ساعت قبل یا ۳۰ دقیقه بعد از آسپرین، مصرف کنید.
قبل از مصرف هر گونه داروی سرماخوردگی، آلرژی یا مسکن، از دکتر یا مسئول داروخانه در مورد امکان مصرف همزمان این داروها بپرسید. زیرا بسیاری از داروهایی که به صورت آزاد به فروش می‌روند، حاوی آسپرین هستند و یا بسیار به ایبوپروفن شبیه می‌باشند. مصرف این داروها به همراه هم، می‌تواند باعث شود که شما یک ماده‌ی دارویی را به میزان زیاده از حد وارد بدن خود کنید. قبل از مصرف این داروها بررسی کنید که آیا حاوی آسپرین، ایبوپروفن، کتوپروفن یا ناپروکسن هستند یا خیر.
اگر هر گونه علائم آلرژیکی نسبت به این دارو – شامل عطسه، آبریزش از بینی، خس خس قفسه‌ی سینه یا به دشواری نفس کشیدن، کهیر، التهاب صورت، لب ها، زبان یا گلو – در خود مشاهده کردید، حتماً سریعاً به دکتر اطلاع دهید.
اگر علائم سکته‌ی مغزی یا حمله‌ی قلبی را داشتید، سریعاً به فوریت‌های پزشکی اطلاع دهید. این علائم عبارتند از: درد قفسه‌ی سینه که تا آرواره یا شانه‌های شما امتداد پیدا کند، بی‌حسی یا ضعف ناگهانی در یک سمت از بدن، لکنت زبان، ورم پا، احساس تنگی نفس؛
اگر موارد زیر را دارید، مصرف ایبوپروفن را متوقف کرده و بلافاصله به دکتر اطلاع دهید:
– تغییرات در دید؛
– تنگی نفس (حتی به صورت خفیف)؛
– تورم یا افزایش وزن ناگهانی؛
– علائم خونریزی معده – شامل: مدفوع تیره‌رنگ یا خونی، سرفه به همراه بالا آوردن خون، استفراغی که شبیه دانه‌های قهوه باشد؛
– مشکلات کبدی – علائم: حالت تهوع، درد در قسمت بالای شکم، خارش، احساس خستگی، علائمی شبیه آنفولانزا، کاهش اشتها، ادرار تیره‌رنگ، مدفوع به رنگ خاک رس، یرقان (زرد شدن پوست یا چشم‌ها)؛
– مشکلات کلیوی – علائم: ادرار ناچیز یا عدم ادرار، ادرار دردناک یا به سختی ادرار کردن، تورم در پا یا مچ پا، احساس خستگی یا تنگی نفس؛
– کم شدن گلبول‌های قرمز خون (آنمی) – علائم: رنگ‌پریدگی، احساس سبکی در سر یا تنگی نفس، ضربان قلب تند، مشکلات در تمرکز کردن؛
– واکنش‌های پوستی شدید – علائم: تب، گلودرد، تورم در صورت یا زبان، قرمزی و سوزش چشم ها، درد پوست به همراه ایجاد جوش‌های پوستی به رنگ قرمز یا ارغوانی که به خصوص تا صورت یا قسمت بالاییِ بدن گسترش پیدا کنند و باعث ایجاد تاول یا پوسته‌پوسته شدن شوند؛
عوارض جانبی متداول در اثر مصرف داروی ایبوپروفن عبارت است از:
– معده درد، سوزش قلب، حالت تهوع، استفراغ؛
– نفخ، اسهال، یبوست؛
– سرگیجه، سردرد، عصبانیت؛
– خارش خفیف یا جوش؛
– وز وز گوش؛
البته لازم است ذکر شود که ممکن است عوارض جانبی دیگری نیز در صورت استفاده از این دارو رخ دهد. چنانچه موارد دیگری را مشاهده نمودید، به دکتر مراجعه کنید.
اگر شما از داروهای ضد افسردگی مانند سیتالوپرام، اس سیتالوپرام، فلوکستین (Prozac)، فلووکسامین، پاروکستین، سرترالین (زولوفت)، ترازودون یا ویلازودون استفاده می‌کنید، قبل از مصرف ایبوپروفن به دکتر خود اطلاع دهید و بپرسید که آیا مصرف همزمان این داروها برای شما ایجاد مشکل می‌کند یا خیر؛
مصرف هر داروی دیگری به همراه یک داروی ضد التهابی غیر استروئیدی، می‌تواند باعث شود که به راحتی دچار کبودی یا خونریزی شوید.
اگر هر گونه از داروهای زیر را مصرف می‌کنید، از دکترتان یا مسئول داروخانه در مورد امکان مصرف ایبوپروفن به همراه این داروها، سوال کنید:
– لیتیوم؛
– متوترکسات؛
– رقیق کننده‌های خون (مانند وارفارین، کومادین، جانتووین)؛
– داروهای قلب یا فشار خون (شامل داروهای مُدِر یا قرص آب)؛
– داروهای استروئیدی (مانند: پِرِدنیزون)؛
البته لیست بالا همه‌ی داروهایی که با ایبوپروفن تداخل دارند را در بر ندارد و سایر داروها نیز ممکن است با این دارو تداخل داشته باشند؛ اعم از داروهای با نسخه و بدون نسخه (آزاد)، ویتامین ها و داروهای گیاهی.
به یاد داشته باشید که این دارو و در کل همه‌ی داروها را از دسترس کودکان دور نگه دارید.
هرگز داروهای خودتان را به دیگران ندهید.
داروی ایبوپروفن را فقط برای وضعیتی که برای شما تجویز شده، مصرف کنید.
همواره در مورد صحت اطلاعاتی که در این مطلب برای شما گرد آورده‌ایم، با دکترتان صحبت کنید که آیا در مورد شما نیز صدق می‌کند یا خیر؛ زیرا این اطلاعات، عمومی هستند و ممکن است برای برخی افراد صدق نکند.
ترجمه ی اختصاصی مجله قرمز / با اندک تصرف و تلخیص
منبع : drugs.com
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کلیه حقوق مادی و معنوی متعلق به وب سایت مجله قرمز می‌باشد. بازنشر مطالب فقط با ذکر لینک مستقیم مجاز است.
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.7 The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.8 Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.9
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.24
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
قرص ibuprofen چیست
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.11
The use of ibuprofen and its enantiomer Dexibuprofen in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.12
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labor.10
As ibuprofen is a widely used medication, the main therapeutic indications are:
Patent Ductus Arteriosus – it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.13
Rheumatoid- and osteo-arthritis – ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.14
Cystic fibrosis – the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.15
Orthostatic hypotension – ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.1
Dental pain – ibuprofen is used to manage acute and chronic orofacial pain.16
Minor pain – ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea. It is very commonly used for the relief of acute indications such as fever and tension headaches.10
Investigational uses – efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer’s disease, Parkinson disease, and breast cancer.10
Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.23
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.23
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.23
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.10
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.17 As well, it has been reported to reduce significantly the fever and the pain caused by migraines.18,19 This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.23
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.20 On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.21 The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.22
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.27
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.25
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.10
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.23 The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.23
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.25
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.10
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.10 As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.24
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives. From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.23
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.23
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.10 The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.23
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.10
قرص ibuprofen چیست
The serum half-life of ibuprofen is 1.2-2 hours.10 In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.23
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.23
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).26
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
Extended description of the mechanism of action and particular properties of each drug interaction.
A severity rating for each drug interaction, from minor to major.
A rating for the strength of the evidence supporting each drug interaction.
An effect category for each drug interaction. Know how this interaction affects the subject drug.
The date on which a patent was filed with the relevant government.
There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.
Drug created on June 13, 2005 07:24 / Updated on July 13, 2019 00:37
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.7 The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.8 Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.9
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.24
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
قرص ibuprofen چیست
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.11
The use of ibuprofen and its enantiomer Dexibuprofen in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.12
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labor.10
As ibuprofen is a widely used medication, the main therapeutic indications are:
Patent Ductus Arteriosus – it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.13
Rheumatoid- and osteo-arthritis – ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.14
Cystic fibrosis – the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.15
Orthostatic hypotension – ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.1
Dental pain – ibuprofen is used to manage acute and chronic orofacial pain.16
Minor pain – ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea. It is very commonly used for the relief of acute indications such as fever and tension headaches.10
Investigational uses – efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer’s disease, Parkinson disease, and breast cancer.10
Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.23
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.23
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.23
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.10
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.17 As well, it has been reported to reduce significantly the fever and the pain caused by migraines.18,19 This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.23
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.20 On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.21 The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.22
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.27
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.25
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.10
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.23 The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.23
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.25
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.10
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.10 As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.24
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives. From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.23
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.23
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.10 The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.23
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.10
قرص ibuprofen چیست
The serum half-life of ibuprofen is 1.2-2 hours.10 In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.23
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.23
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).26
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
Extended description of the mechanism of action and particular properties of each drug interaction.
A severity rating for each drug interaction, from minor to major.
A rating for the strength of the evidence supporting each drug interaction.
An effect category for each drug interaction. Know how this interaction affects the subject drug.
The date on which a patent was filed with the relevant government.
There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.
Drug created on June 13, 2005 07:24 / Updated on July 13, 2019 00:37
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.7 The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.8 Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.9
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.24
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
قرص ibuprofen چیست
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.11
The use of ibuprofen and its enantiomer Dexibuprofen in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.12
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labor.10
As ibuprofen is a widely used medication, the main therapeutic indications are:
Patent Ductus Arteriosus – it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.13
Rheumatoid- and osteo-arthritis – ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.14
Cystic fibrosis – the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.15
Orthostatic hypotension – ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.1
Dental pain – ibuprofen is used to manage acute and chronic orofacial pain.16
Minor pain – ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea. It is very commonly used for the relief of acute indications such as fever and tension headaches.10
Investigational uses – efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer’s disease, Parkinson disease, and breast cancer.10
Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.23
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.23
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.23
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.10
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.17 As well, it has been reported to reduce significantly the fever and the pain caused by migraines.18,19 This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.23
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.20 On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.21 The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.22
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.27
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.25
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.10
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.23 The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.23
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.25
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.10
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.10 As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.24
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives. From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.23
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.23
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.10 The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.23
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.10
قرص ibuprofen چیست
The serum half-life of ibuprofen is 1.2-2 hours.10 In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.23
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.23
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).26
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
Extended description of the mechanism of action and particular properties of each drug interaction.
A severity rating for each drug interaction, from minor to major.
A rating for the strength of the evidence supporting each drug interaction.
An effect category for each drug interaction. Know how this interaction affects the subject drug.
The date on which a patent was filed with the relevant government.
There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.
Drug created on June 13, 2005 07:24 / Updated on July 13, 2019 00:37
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.7 The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.8 Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.9
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.24
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
قرص ibuprofen چیست
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.11
The use of ibuprofen and its enantiomer Dexibuprofen in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.12
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labor.10
As ibuprofen is a widely used medication, the main therapeutic indications are:
Patent Ductus Arteriosus – it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.13
Rheumatoid- and osteo-arthritis – ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.14
Cystic fibrosis – the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.15
Orthostatic hypotension – ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.1
Dental pain – ibuprofen is used to manage acute and chronic orofacial pain.16
Minor pain – ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea. It is very commonly used for the relief of acute indications such as fever and tension headaches.10
Investigational uses – efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer’s disease, Parkinson disease, and breast cancer.10
Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.23
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.23
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.23
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.10
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.17 As well, it has been reported to reduce significantly the fever and the pain caused by migraines.18,19 This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.23
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.20 On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.21 The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.22
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.27
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.25
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.10
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.23 The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.23
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.25
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.10
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.10 As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.24
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives. From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.23
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.23
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.10 The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.23
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.10
قرص ibuprofen چیست
The serum half-life of ibuprofen is 1.2-2 hours.10 In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.23
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.23
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).26
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
Extended description of the mechanism of action and particular properties of each drug interaction.
A severity rating for each drug interaction, from minor to major.
A rating for the strength of the evidence supporting each drug interaction.
An effect category for each drug interaction. Know how this interaction affects the subject drug.
The date on which a patent was filed with the relevant government.
There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.
Drug created on June 13, 2005 07:24 / Updated on July 13, 2019 00:37
Ibuprofen is a non-steroidal anti-inflammatory drug (NSAID) derived from propionic acid and it is considered the first of the propionics.7 The formula of ibuprofen is 2-(4-isobutylphenyl) propionic acid and its initial development was in 1960 while researching for a safer alternative for aspirin.8 Ibuprofen was finally patented in 1961 and this drug was first launched against rheumatoid arthritis in the UK in 1969 and USA in 1974. It was the first available over-the-counter NSAID.9
On the available products, ibuprofen is administered as a racemic mixture. Once administered, the R-enantiomer undergoes extensive interconversion to the S-enantiomer in vivo by the activity of the alpha-methylacyl-CoA racemase. In particular, it is generally proposed that the S-enantiomer is capable of eliciting stronger pharmacological activity than the R-enantiomer.24
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
قرص ibuprofen چیست
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
A unique ID assigned by the FDA when a product is submitted for approval by the labeller.
A governmentally-recognized ID which uniquely identifies the product within its regulatory market.
Ibuprofen is the most commonly used and prescribed NSAID. It is very common over the counter medication widely used as an analgesic, anti-inflammatory and antipyretic.11
The use of ibuprofen and its enantiomer Dexibuprofen in a racemic mix is common for the management of mild to moderate pain related to dysmenorrhea, headache, migraine, postoperative dental pain, spondylitis, osteoarthritis, rheumatoid arthritis, and soft tissue disorder.12
Due to its activity against prostaglandin and thromboxane synthesis, ibuprofen has been attributed to alteration of platelet function and prolongation of gestation and labor.10
As ibuprofen is a widely used medication, the main therapeutic indications are:
Patent Ductus Arteriosus – it is a neonatal condition wherein the ductus arteriosus (blood vessel that connects the main pulmonary artery to the proximal descending aorta) fails to close after birth causing severe risk of heart failure. The prostaglandin inhibition of ibuprofen has been studied for the treatment of this condition as it is known that prostaglandin E2 is responsible for keeping the ductus arteriosus open.13
Rheumatoid- and osteo-arthritis – ibuprofen is very commonly used in the symptomatic treatment of inflammatory, musculoskeletal and rheumatic disorders.14
Cystic fibrosis – the use of high dosages of ibuprofen has been proven to decrease inflammation and decreasing polymorphonuclear cell influx in the lungs.15
Orthostatic hypotension – ibuprofen can induce sodium retention and antagonize the effect of diuretics which has been reported to be beneficial for patients with severe orthostatic hypotension.1
Dental pain – ibuprofen is used to manage acute and chronic orofacial pain.16
Minor pain – ibuprofen is widely used to reduce minor aches and pains as well as to reduce fever and manage dysmenorrhea. It is very commonly used for the relief of acute indications such as fever and tension headaches.10
Investigational uses – efforts have been put into developing ibuprofen for the prophylaxis of Alzheimer’s disease, Parkinson disease, and breast cancer.10
Ibuprofen has multiple actions in different inflammatory pathways involved in acute and chronic inflammation. The main effects reported in ibuprofen are related to the control of pain, fever and acute inflammation by the inhibition of the synthesis of prostanoids by COX-1 and COX-2. Pain relief is attributed to peripheral affected regions and central nervous system effects in the pain transmission mediated by the dorsal horn and higher spinothalamic tract. Some reports have tried to link the pain regulation with a possible enhancement on the synthesis of endogenous cannabinoids and action on the NMDA receptors. The effect on pain has been shown to be related to the cortically evoked potentials.23
The antipyretic effect is reported to be linked to the effect on the prostanoid synthesis due to the fact that the prostanoids are the main signaling mediator of pyresis in the hypothalamic-preoptic region.23
The use of ibuprofen in dental procedures is attributed to the local inhibition of prostanoid production as well as to anti-oedemic activity and an increase of plasma beta-endorphins. Some reports have suggested a rapid local reduction of the expression of COX-2 in dental pulp derived by the administration of ibuprofen.23
The administration of ibuprofen in patients with rheumatic diseases has shown to control joint symptoms.10
Ibuprofen is largely used in OTC products such as an agent for the management of dysmenorrhea which has been proven to reduce the amount of menstrual prostanoids and to produce a reduction in the uterine hypercontractility.17 As well, it has been reported to reduce significantly the fever and the pain caused by migraines.18,19 This effect is thought to be related to the effect on platelet activation and thromboxane A2 production which produces local vascular effects in the affected regions. This effect is viable as ibuprofen can enter in the central nervous system.23
In the investigational uses of ibuprofen, it has been reported to reduce neurodegeneration when given in low doses over a long time.20 On the other hand, its use in Parkinson disease is related to the importance of inflammation and oxidative stress in the pathology of this condition.21 The use of ibuprofen for breast cancer is related to a study that shows a decrease of 50% in the rate of breast cancer.22
The exact mechanism of action of ibuprofen is unknown. However, ibuprofen is considered an NSAID and thus it is a non-selective inhibitor of cyclooxygenase, which is an enzyme involved in prostaglandin (mediators of pain and fever) and thromboxane (stimulators of blood clotting) synthesis via the arachidonic acid pathway.27
Ibuprofen is a non-selective COX inhibitor and hence, it inhibits the activity of both COX-1 and COX-2. The inhibition of COX-2 activity decreases the synthesis of prostaglandins involved in mediating inflammation, pain, fever, and swelling while the inhibition of COX-1 is thought to cause some of the side effects of ibuprofen including GI ulceration.25
Comprehensive structured data on known drug adverse effects with statistical prevalence. MedDRA and ICD10 ids are provided for adverse effect conditions and symptoms.
Structured data covering drug contraindications. Each contraindication describes a scenario in which the drug is not to be used. Includes restrictions on co-administration, contraindicated populations, and more.
Structured data representing warnings from the black box section of drug labels. These warnings cover important and dangerous risks, contraindications, or adverse effects.
It is very well absorbed orally and the peak serum concentration can be attained in 1 to 2 hours after extravascular administration. When ibuprofen is administered immediately after a meal there is a slight reduction in the absorption rate but there is no change in the extent of the absorption.10
When orally administered, the absorption of ibuprofen in adults is very rapidly done in the upper GI tract.23 The average Cmax, Tmax and AUC ranges around 20 mcg/ml, 2 h and 70 mcg.h/ml. These parameters can vary depending on the enantiomer form, route, and dose of administration.23
The apparent volume of distribution of ibuprofen is of 0.1 L/kg.25
Ibuprofen dosage is more than 99% bound to plasma proteins and site II of purified albumin, binding appears to be saturable and becomes non-linear at concentrations exceeding 20 mcg/ml.10
Ibuprofen is rapidly metabolized and biotransformed in the liver to the formation of major metabolites which are the hydroxylated and carboxylated derivatives.10 As soon as it is absorbed, the R-enantiomer undergoes extensive enantiomeric conversion (53-65%) to the more active S-enantiomer in vivo by the activity of alpha-methylacyl-CoA racemase.24
Ibuprofen metabolism can be divided in phase I which is represented by the hydroxylation of the isobutyl chains for the formation of 2 or 3-hydroxy derivatives followed by oxidation to 2-carboxy-ibuprofen and p-carboxy-2-propionate. These oxidative reactions are performed by the activity of the cytochrome P450 isoforms CYP 2C9, CYP 2C19 and CYP 2C8. Therefore, these enzymes participate in the oxidation of the alkyl side chain to hydroxyl and carboxyl derivatives. From this enzymes, the major catalyst in the formation of oxidative metabolites is the isoform CYP 2C9.23
The metabolic phase I is followed by a phase II in which the oxidative metabolites may be conjugated to glucuronide prior to excretion. This activity forms phenolic and acyl glucuronides.23
Ibuprofen is rapidly metabolized and eliminated in the urine thus, this via accounts for more than 90% of the administered dose. It is completely eliminated in 24 hours after the last dose and almost all the administered dose goes through metabolism, representing about 99% of the eliminated dose.10 The biliary excretion of unchanged drug and active phase II metabolites represents 1% of the administered dose.23
In summary, ibuprofen is excreted as metabolites or their conjugates. The elimination of ibuprofen is not impaired by old age or the presence of renal impairment.10
قرص ibuprofen چیست
The serum half-life of ibuprofen is 1.2-2 hours.10 In patients with a compromised liver function, the half-life can be prolonged to 3.1-3.4 hours.23
The clearance rate ranges between 3-13 L/h depending on the route of administration, enantiomer type and dosage.23
The symptoms of overdose are presented in individuals that consumed more than 99 mg/kg. Most common symptoms of overdose are abdominal pain, nausea, vomiting, lethargy, vertigo, drowsiness (somnolence), dizziness and insomnia. Other symptoms of overdose include headache, loss of consciousness, tinnitus, CNS depression, convulsions and seizures. May rarely cause metabolic acidosis, abnormal hepatic function, hyperkalemia, renal failure, dyspnea, respiratory depression, coma, acute renal failure, and apnea (primarily in very young pediatric patients).26
The reported LD50 of ibuprofen is of 636 mg/kg in rat, 740 mg/kg in mouse and 495 mg/kg in guinea pig.MSDS
Extended description of the mechanism of action and particular properties of each drug interaction.
A severity rating for each drug interaction, from minor to major.
A rating for the strength of the evidence supporting each drug interaction.
An effect category for each drug interaction. Know how this interaction affects the subject drug.
The date on which a patent was filed with the relevant government.
There is additional data available for commercial users including Adverse Effects, Contraindications, and Blackbox Warnings. Contact us to learn more about these and other features.
Drug created on June 13, 2005 07:24 / Updated on July 13, 2019 00:37
InChI=۱S/C13H18O۲/c۱-9(2)۸-۱۱-۴-۶-۱2(7-5-11)۱0(3)۱3(14)۱۵/h۴-۷٬۹-۱۰H,8H2,۱-۳H3,(H,14,15) YKey:HEFNNWSXXWATRW-UHFFFAOYSA-N Y
ایبوپروفن (به انگلیسی: Ibuprofen)
رده درمانی: مسکن، ضد التهاب
اشکال دارویی: قرص ، شربت
ایبوپروفن یا بروفن داروی ضدالتهاب غیراستروئیدی است که برای تسکین علائم آرتریت (التهاب مفصل)، دیسمنوره (قاعدگی دردناک)، حملات نقرس و آسیب‌های حین ورزش و نیز به عنوان تب‌بر و ضد درد به ویژه در دردهای ناشی از التهاب استفاده می‌شود.
قرص ibuprofen چیست
این دارو بیشتر با نام ژنریک بروفن (Brufen) شناخته می‌شود. ادویل (ایبوپروفن)، موترین (Motrin) و نورفن (Nurofen) از دیگر نام‌های تجاری آن هستند.
سازمان بهداشت جهانی بروفن را در فهرست داروهای اساسی قرار داده است. این فهرست داروهایی را در بر می‌گیرد که باید در هر مرکز درمانی موجود باشند[۱].
فرمول شیمیایی بروفن C۱۳H۱۸O۲ است. نقطه ذوب آن ۷۶ درجه سانتی‌گراد و درصد چسبندگی آن به پروتئین پلاسما ۹۹٪ است. از طریق ادرار دفع می‌شود و نیمه عمر (داروشناسی) آن حدود ۲ ساعت است. در سه فرم خوراکی، موضعی (پماد) و مقعدی (شیاف) موجود است. پماد بروفن برای آسیب‌دیدگی‌های هنگام ورزش استفاده می‌شود.
بروفن در دههٔ ۱۹۶۰ توسط گروهی به سرپرستی استوارت آدامز در انگلیس اختراع[۲] و در سال ۱۹۶۹ به عنوان علاجی برای آرتریت روماتوئید وارد داروخانه‌های بریتانیا و آمریکا شد. گروه بوتس[۳] شرکت سازندهٔ بروفن در سال ۱۹۸۷ جایزهٔ ملکه برای دستاوردهای فنی[۴] را برای ساخت این دارو دریافت کرد.[۵]
بروفن در دوز ۲۰۰ تا ۴۰۰ میلی‌گرم در بیشتر کشورها بدون نسخه فروخته می‌شود. مدت تأثیر آن با توجه به مقدار از ۴ تا ۸ ساعت متغیر است. مقدار مصرف با توجه به شدت علائم بیماری و وزن بدن تعیین می‌شود؛ معمولاً ۲۰۰ تا ۴۰۰ میلی‌گرم (کودکان ۵-۱۰ م. گک. گ) در ۴ تا ۶ ساعت و تا حداکثر ۸۰۰ تا ۱۲۰۰ میلی‌گرم در روز. با تجویز پزشک حد نهایی مصرف روزانه ممکن است تا ۳۲۰۰ م. گ افزایش یابد.
بر پایه تحقیقی بروفن در کاهش دردهای پس از جراحی از ترامادول مؤثرتر است.[۶]
بروفن به دلیل خصوصیات ضدالتهابی‌اش گاهی برای درمان آکنه نیز استفاده می‌شود. برخی تحقیقات نشان می‌دهد که مصرف طولانی مدت آن احتمال ابتلا به پارکینسون را کاهش می‌دهد. همچنین ممکن است در هیپوتانسیون اورتواستاتیک (افت ناگهانی فشار خون در هنگام ایستادن) نیز مفید باشد.
مصرف دراز مدت بروفن مانند سایر ضدالتهاب‌های غیراستروئیدی خطر حمله قلبی را بالا می‌برد[۷][۸]. پژوهش‌‌ها نشان می‌دهد ایبوپروفن ممکن است موجب ناباروری در مردان شود[۹].
بروفن در ایران به شکل قرص‌های 200 و 400 میلی‌گرمی موجود است. در برخی کشورها مانند اسپانیا قرص‌های 600mg و در مکزیک 800mg آن نیز فروخته می‌شود. در آلمان نیز کپسول‌های 600mg و 800mg با نسخه فروخته می‌شود، در حالی‌که قرص‌های 400mg نیاز به نسخه ندارد. در ایالات متحده نیز از ۱۹۸۴ تاکنون بدون نسخه در دسترس است.
InChI=۱S/C13H18O۲/c۱-9(2)۸-۱۱-۴-۶-۱2(7-5-11)۱0(3)۱3(14)۱۵/h۴-۷٬۹-۱۰H,8H2,۱-۳H3,(H,14,15) YKey:HEFNNWSXXWATRW-UHFFFAOYSA-N Y
ایبوپروفن (به انگلیسی: Ibuprofen)
رده درمانی: مسکن، ضد التهاب
اشکال دارویی: قرص ، شربت
ایبوپروفن یا بروفن داروی ضدالتهاب غیراستروئیدی است که برای تسکین علائم آرتریت (التهاب مفصل)، دیسمنوره (قاعدگی دردناک)، حملات نقرس و آسیب‌های حین ورزش و نیز به عنوان تب‌بر و ضد درد به ویژه در دردهای ناشی از التهاب استفاده می‌شود.
قرص ibuprofen چیست
این دارو بیشتر با نام ژنریک بروفن (Brufen) شناخته می‌شود. ادویل (ایبوپروفن)، موترین (Motrin) و نورفن (Nurofen) از دیگر نام‌های تجاری آن هستند.
سازمان بهداشت جهانی بروفن را در فهرست داروهای اساسی قرار داده است. این فهرست داروهایی را در بر می‌گیرد که باید در هر مرکز درمانی موجود باشند[۱].
فرمول شیمیایی بروفن C۱۳H۱۸O۲ است. نقطه ذوب آن ۷۶ درجه سانتی‌گراد و درصد چسبندگی آن به پروتئین پلاسما ۹۹٪ است. از طریق ادرار دفع می‌شود و نیمه عمر (داروشناسی) آن حدود ۲ ساعت است. در سه فرم خوراکی، موضعی (پماد) و مقعدی (شیاف) موجود است. پماد بروفن برای آسیب‌دیدگی‌های هنگام ورزش استفاده می‌شود.
بروفن در دههٔ ۱۹۶۰ توسط گروهی به سرپرستی استوارت آدامز در انگلیس اختراع[۲] و در سال ۱۹۶۹ به عنوان علاجی برای آرتریت روماتوئید وارد داروخانه‌های بریتانیا و آمریکا شد. گروه بوتس[۳] شرکت سازندهٔ بروفن در سال ۱۹۸۷ جایزهٔ ملکه برای دستاوردهای فنی[۴] را برای ساخت این دارو دریافت کرد.[۵]
بروفن در دوز ۲۰۰ تا ۴۰۰ میلی‌گرم در بیشتر کشورها بدون نسخه فروخته می‌شود. مدت تأثیر آن با توجه به مقدار از ۴ تا ۸ ساعت متغیر است. مقدار مصرف با توجه به شدت علائم بیماری و وزن بدن تعیین می‌شود؛ معمولاً ۲۰۰ تا ۴۰۰ میلی‌گرم (کودکان ۵-۱۰ م. گک. گ) در ۴ تا ۶ ساعت و تا حداکثر ۸۰۰ تا ۱۲۰۰ میلی‌گرم در روز. با تجویز پزشک حد نهایی مصرف روزانه ممکن است تا ۳۲۰۰ م. گ افزایش یابد.
بر پایه تحقیقی بروفن در کاهش دردهای پس از جراحی از ترامادول مؤثرتر است.[۶]
بروفن به دلیل خصوصیات ضدالتهابی‌اش گاهی برای درمان آکنه نیز استفاده می‌شود. برخی تحقیقات نشان می‌دهد که مصرف طولانی مدت آن احتمال ابتلا به پارکینسون را کاهش می‌دهد. همچنین ممکن است در هیپوتانسیون اورتواستاتیک (افت ناگهانی فشار خون در هنگام ایستادن) نیز مفید باشد.
مصرف دراز مدت بروفن مانند سایر ضدالتهاب‌های غیراستروئیدی خطر حمله قلبی را بالا می‌برد[۷][۸]. پژوهش‌‌ها نشان می‌دهد ایبوپروفن ممکن است موجب ناباروری در مردان شود[۹].
بروفن در ایران به شکل قرص‌های 200 و 400 میلی‌گرمی موجود است. در برخی کشورها مانند اسپانیا قرص‌های 600mg و در مکزیک 800mg آن نیز فروخته می‌شود. در آلمان نیز کپسول‌های 600mg و 800mg با نسخه فروخته می‌شود، در حالی‌که قرص‌های 400mg نیاز به نسخه ندارد. در ایالات متحده نیز از ۱۹۸۴ تاکنون بدون نسخه در دسترس است.
InChI=۱S/C13H18O۲/c۱-9(2)۸-۱۱-۴-۶-۱2(7-5-11)۱0(3)۱3(14)۱۵/h۴-۷٬۹-۱۰H,8H2,۱-۳H3,(H,14,15) YKey:HEFNNWSXXWATRW-UHFFFAOYSA-N Y
ایبوپروفن (به انگلیسی: Ibuprofen)
رده درمانی: مسکن، ضد التهاب
اشکال دارویی: قرص ، شربت
ایبوپروفن یا بروفن داروی ضدالتهاب غیراستروئیدی است که برای تسکین علائم آرتریت (التهاب مفصل)، دیسمنوره (قاعدگی دردناک)، حملات نقرس و آسیب‌های حین ورزش و نیز به عنوان تب‌بر و ضد درد به ویژه در دردهای ناشی از التهاب استفاده می‌شود.
قرص ibuprofen چیست
این دارو بیشتر با نام ژنریک بروفن (Brufen) شناخته می‌شود. ادویل (ایبوپروفن)، موترین (Motrin) و نورفن (Nurofen) از دیگر نام‌های تجاری آن هستند.
سازمان بهداشت جهانی بروفن را در فهرست داروهای اساسی قرار داده است. این فهرست داروهایی را در بر می‌گیرد که باید در هر مرکز درمانی موجود باشند[۱].
فرمول شیمیایی بروفن C۱۳H۱۸O۲ است. نقطه ذوب آن ۷۶ درجه سانتی‌گراد و درصد چسبندگی آن به پروتئین پلاسما ۹۹٪ است. از طریق ادرار دفع می‌شود و نیمه عمر (داروشناسی) آن حدود ۲ ساعت است. در سه فرم خوراکی، موضعی (پماد) و مقعدی (شیاف) موجود است. پماد بروفن برای آسیب‌دیدگی‌های هنگام ورزش استفاده می‌شود.
بروفن در دههٔ ۱۹۶۰ توسط گروهی به سرپرستی استوارت آدامز در انگلیس اختراع[۲] و در سال ۱۹۶۹ به عنوان علاجی برای آرتریت روماتوئید وارد داروخانه‌های بریتانیا و آمریکا شد. گروه بوتس[۳] شرکت سازندهٔ بروفن در سال ۱۹۸۷ جایزهٔ ملکه برای دستاوردهای فنی[۴] را برای ساخت این دارو دریافت کرد.[۵]
بروفن در دوز ۲۰۰ تا ۴۰۰ میلی‌گرم در بیشتر کشورها بدون نسخه فروخته می‌شود. مدت تأثیر آن با توجه به مقدار از ۴ تا ۸ ساعت متغیر است. مقدار مصرف با توجه به شدت علائم بیماری و وزن بدن تعیین می‌شود؛ معمولاً ۲۰۰ تا ۴۰۰ میلی‌گرم (کودکان ۵-۱۰ م. گک. گ) در ۴ تا ۶ ساعت و تا حداکثر ۸۰۰ تا ۱۲۰۰ میلی‌گرم در روز. با تجویز پزشک حد نهایی مصرف روزانه ممکن است تا ۳۲۰۰ م. گ افزایش یابد.
بر پایه تحقیقی بروفن در کاهش دردهای پس از جراحی از ترامادول مؤثرتر است.[۶]
بروفن به دلیل خصوصیات ضدالتهابی‌اش گاهی برای درمان آکنه نیز استفاده می‌شود. برخی تحقیقات نشان می‌دهد که مصرف طولانی مدت آن احتمال ابتلا به پارکینسون را کاهش می‌دهد. همچنین ممکن است در هیپوتانسیون اورتواستاتیک (افت ناگهانی فشار خون در هنگام ایستادن) نیز مفید باشد.
مصرف دراز مدت بروفن مانند سایر ضدالتهاب‌های غیراستروئیدی خطر حمله قلبی را بالا می‌برد[۷][۸]. پژوهش‌‌ها نشان می‌دهد ایبوپروفن ممکن است موجب ناباروری در مردان شود[۹].
بروفن در ایران به شکل قرص‌های 200 و 400 میلی‌گرمی موجود است. در برخی کشورها مانند اسپانیا قرص‌های 600mg و در مکزیک 800mg آن نیز فروخته می‌شود. در آلمان نیز کپسول‌های 600mg و 800mg با نسخه فروخته می‌شود، در حالی‌که قرص‌های 400mg نیاز به نسخه ندارد. در ایالات متحده نیز از ۱۹۸۴ تاکنون بدون نسخه در دسترس است.
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قرص ibuprofen چیست
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It is a non-steroidal anti-inflammatory drug (NSAID) and also has an antiplatelet effect, which means it protects from blood clots.
Ibuprofen brand names include Brufen, Calprofen, Genpril, Ibu, Midol, Nuprin, Cuprofen, Nurofen, Advil, and
Motrin, among others.
When buying medication at a pharmacy, the packaging will state whether a product contains ibuprofen.
Here are some key points about ibuprofen. More detail is in the main article.
Ibuprofen is an NSAID, a type of medication with analgesic, fever-reducing, and, in higher doses, anti-inflammatory effects.
The World Health Organization (WHO) includes ibuprofen in a list of the minimum medical needs for a basic healthcare system known as its “Essential Drugs List.”
A non-steroidal drug is not a steroid. Steroids often have similar effects, but long-term use can cause severe adverse effects. Most NSAIDs are non-narcotic, so they do not cause insensibility or stupor.
Ibuprofen, aspirin, and naproxen are all well-known NSAIDs, partly because they are available over the counter (OTC) from pharmacies.
Ibuprofen works by blocking the production of prostaglandins, substances that the body releases in response to illness and injury.
Prostaglandins cause pain and swelling, or inflammation. They are released in the brain, and they can also cause fever.
Ibuprofen’s painkilling effects begin soon after taking a dose. The anti-inflammatory effects can take longer, sometimes several weeks.
Ibuprofen is not suitable for people who:
In 2015, the United States Food and Drug Administration (FDA) strengthened their warning about the increased risk of heart attack or stroke when taking higher doses of ibuprofen.
They call on people to be aware of this possible problem and to seek medical attention at once if they experience chest pain, breathing problems, sudden weakness in one part or one side of the body, or sudden slurred speech.
It should be used with caution if a person has, or has had:
Patients should check with a doctor or a qualified pharmacist if they are unsure.
The most common adverse effects of ibuprofen include:
Also possible, but less common, are:
Anyone who feels dizzy after taking ibuprofen should not drive or operate machinery.
Very rarely, a person may experience bleeding in the stomach, signs of which are:
Long-term use can lead to reduced fertility in some women, but this problem should stop soon after finishing treatment.
The United States (U. S.) Food and Drug Administration (FDA) warns that some people may be allergic to the ingredients of ibuprofen.
Allergic symptoms include:
Anyone experiencing these symptoms should stop using the drug.
In severe cases, anaphylactic shock may occur. The person will have difficulty breathing. This is life-threatening and needs immediate medical attention.
قرص ibuprofen چیست
Ibuprofen should not be used in the last 3 months of pregnancy unless definitely directed to do so by a doctor, as it may affect the fetus or lead to problems during delivery.
Ask a health professional before using any medication while pregnant or breast-feeding.
Some reports that suggest routine use of many pain relievers like Advil for migraine headaches may cause a rebound headache after the pain reliever wears off.
While this is not considered an addiction, it can create an annoying cycle that can be hard to break. Regular users of ibuprofen should be mindful of this.
Sometimes, one medication can interfere with the effects of another. This is known as drug interaction.
Drugs that may interact with ibuprofen include:
Antihypertensive medications: Drugs taken for high blood pressure, or hypertension. Ibuprofen can sometimes lead to a rise in blood pressure if used alongside antihypertensives.
Anti-inflammatory painkillers: Ibuprofen should not be taken with diclofenac (Voltarol), indometacin, or naproxen because there is an increased risk of stomach bleeding. Ibuprofen should not be necessary with these drugs, as they are already painkillers.
Aspirin: Ibuprofen and aspirin taken together significantly raise the risk of stomach bleeding. Patients taking low-dose aspirin for blood thinning should not take ibuprofen because the blood thinning effect will be diminished.
Digoxin: This is often used to treat atrial fibrillation. Ibuprofen and digoxin together can raise blood pressure levels.
Lithium: This drug is used for some mental disorders. Ibuprofen can make it harder for the body to eliminate lithium, resulting in potentially dangerous levels of lithium in the body.
Methotrexate: This is used to treat cancer and some auto-immune diseases. Ibuprofen can make it harder for the body to eliminate methotrexate. Potentially hazardous levels of methotrexate may build up in the body.
Tacrolimus: This drug is mainly used after an organ transplant, to stop the body’s immune system rejecting the new organ. Ibuprofen with tacrolimus can cause kidney damage.
Selective serotonin reuptake inhibitors (SSRIs): This type of antidepressant drugs, such as citalopram, fluoxetine, paroxetine and sertraline, taken with ibuprofen can increase the risk of bleeding.
Warfarin: An anticoagulant drug, or blood thinner, that stops the blood from clotting. Ibuprofen taken with warfarin can reduce the drug’s anticoagulant effects.
Anyone who is taking these or other medications should ask their doctor or pharmacist if it is safe to use ibuprofen.
As long as users adhere to the guidelines, ibuprofen can be used safely in a number of settings. It is not habit-forming or addictive.
Severe adverse effects normally occur only with long-term use.
In the face of the current opioid overdose epidemic, the Centers for Disease Control and Prevention (CDC) urge doctors and patients to consider non-opioid drugs, such as ibuprofen, before moving on to opioids as a treatment for pain.
Ibuprofen is available as gels, sprays, tablets or mousses, and it is used to relieve a variety of symptoms.
These include:
For a headache, usage is short term. For anti-inflammatory effects related to chronic conditions, such as arthritis, long-term use is necessary.
Some medications, such as decongestants, have ibuprofen added, to create, for example, a combined cold or flu remedy.
Ibuprofen is available in tablet form, in syrups, and as an intravenous (IV) preparation. Taking the correct dosage is important for avoiding or reducing any side effects.
Dosage depends on the reason for taking ibuprofen and the age of the user.
For adults using it for rheumatoid or osteoarthritis, the dosage is 1,200 milligrams (mg) to 3,200 mg orally per day in divided doses.
The patient must be monitored for adverse effects, and the dose should be adjusted so that the patient takes the smallest possible amount to meet their treatment goals.
The usual adult dose for pain is 200 mg to 400 mg by mouth, every 4 to 6 hours, or 400 to 800 mg IV every 6 hours as needed. The maximum dose in one day is 3,200 mg.
Pediatric ibuprofen can be given for pain relief, inflammation, and to control fever, as well as for juvenile idiopathic arthritis.
Children’s doses are lower than those for adults. The dose will depend on the weight and age of the child, and the severity of the fever or other symptoms.
The child must be over 6 months of age and weigh at least 5 kilograms (kg).
Parents should consult the instructions in the packaging or check with a pharmacist or health care provider before giving ibuprofen or other drugs to children.
Ibuprofen is available for purchase online.
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Article last updated by Yvette Brazier on Wed 21 June 2017.Visit our Pain / Anesthetics category page for the latest news on this subject, or sign up to our newsletter to receive the latest updates on Pain / Anesthetics.All references are available in the References tab.
CDC. (n.d.). CDC guidelines for prescribing opioids for chronic pain [Fact sheet]. Retrieved from https://www.cdc.gov/drugoverdose/pdf/guidelines_at-a-glance-a.pdf
Essential drugs. (2016). Retrieved from http://refbooks.msf.org/msf_docs/en/essential_drugs/ed_en.pdf
FDA strengthens warning of heart attack and stroke risk for non-steroidal anti-inflammatory drugs. (2016, September 28). Retrieved from https://www.fda.gov/ForConsumers/ConsumerUpdates/ucm453610.htm
Ibuprofen dosage. (n.d.). Retrieved from https://www.drugs.com/dosage/ibuprofen.html
Ibuprofen drug facts label. (2016, April 6). Retrieved from https://www.fda.gov/Drugs/DrugSafety/ucm125225.htm
11 things you should know about common pain relievers. (2015, October 9). Retrieved from http://www.health.harvard.edu/pain/12-things-you-should-know-about-pain-relievers
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Generic Name: ibuprofen (EYE bue PROE fen)Brand Names: Advil, Midol, Motrin, Motrin IB, Motrin Migraine Pain, Proprinal, Smart Sense Children’s Ibuprofen, PediaCare Children’s Pain Reliever/Fever Reducer, PediaCare Infant’s Pain Reliever/Fever Reducer
Medically reviewed by Kaci Durbin, MD Last updated on Dec 22, 2018.
Ibuprofen is a nonsteroidal anti-inflammatory drug (NSAID). It works by reducing hormones that cause inflammation and pain in the body.
Ibuprofen is used to reduce fever and treat pain or inflammation caused by many conditions such as headache, toothache, back pain, arthritis, menstrual cramps, or minor injury.
Ibuprofen is used in adults and children who are at least 6 months old.
قرص ibuprofen چیست
Ibuprofen can increase your risk of fatal heart attack or stroke, especially if you use it long term or take high doses, or if you have heart disease. Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABG).
Ibuprofen may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using ibuprofen, especially in older adults.
Do not take more than your recommended dose. An ibuprofen overdose can damage your stomach or intestines. Use only the smallest amount of medication needed to get relief from your pain, swelling, or fever.
Do not use this medicine just before or after heart bypass surgery (coronary artery bypass graft, or CABG).
Ibuprofen may also cause stomach or intestinal bleeding, which can be fatal. These conditions can occur without warning while you are using ibuprofen, especially in older adults.
You should not use ibuprofen if you are allergic to it, or if you have ever had an asthma attack, hives, or severe allergic reaction after taking aspirin or an NSAID (including acetaminophen, naproxen, or others).
Ask a doctor or pharmacist if it is safe for you to take this medicine if you have:
heart disease, high blood pressure, high cholesterol, diabetes, or if you smoke;
a history of heart attack, stroke, or blood clot;
a history of stomach ulcers or bleeding;
asthma;
liver or kidney disease;
fluid retention; or
a connective tissue disease such as Marfan syndrome, Sjogren’s syndrome, or lupus.
Taking ibuprofen during the last 3 months of pregnancy may harm the unborn baby.Do not use this medicine without a doctor’s advice if you are pregnant.
It is not known whether ibuprofen passes into breast milk or if it could affect a nursing baby. Ask a doctor before using this medicine if you are breast-feeding.
Do not give ibuprofen to a child younger than 2 years old without the advice of a doctor.
Use ibuprofen exactly as directed on the label, or as prescribed by your doctor. Do not use in larger amounts or for longer than recommended. Use the lowest dose that is effective in treating your condition.
Do not take more than your recommended dose. An ibuprofen overdose can damage your stomach or intestines. The maximum amount of ibuprofen for adults is 800 milligrams per dose or 3200 mg per day (4 maximum doses). Use only the smallest amount needed to get relief from your pain, swelling, or fever.
A child’s dose of ibuprofen is based on the age and weight of the child. Carefully follow the dosing instructions provided with your child’s medicine for the age and weight of your child. Ask a doctor or pharmacist if you have questions.
Take ibuprofen with food or milk to lessen stomach upset.
Shake the oral suspension (liquid) well just before you measure a dose. Measure liquid medicine with the dosing syringe provided, or with a special dose-measuring spoon or medicine cup. If you do not have a dose-measuring device, ask your pharmacist for one.
The ibuprofen chewable tablet must be chewed before you swallow it.
If you use this medicine long-term, you may need frequent medical tests.
Store at room temperature away from moisture and heat. Do not allow the liquid medicine to freeze.
Read all patient information, medication guides, and instruction sheets provided to you. Ask your doctor or pharmacist if you have any questions.
Ibuprofen dosage information (in more detail)
Since ibuprofen is used when needed, you may not be on a dosing schedule. If you are on a schedule, use the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not use extra medicine to make up the missed dose.
Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Overdose symptoms may include nausea, vomiting, stomach pain, drowsiness, black or bloody stools, coughing up blood, shallow breathing, fainting, or coma.
Avoid drinking alcohol. It may increase your risk of stomach bleeding.
Avoid taking aspirin while you are taking ibuprofen.
Avoid taking ibuprofen if you are taking aspirin to prevent stroke or heart attack. Ibuprofen can make aspirin less effective in protecting your heart and blood vessels. If you must use both medications, take the ibuprofen at least 8 hours before or 30 minutes after you take the aspirin (non-enteric coated form).
Ask a doctor or pharmacist before using any cold, allergy, or pain medicine. Many medicines available over the counter contain aspirin or other medicines similar to ibuprofen. Taking certain products together can cause you to get too much of this type of medication. Check the label to see if a medicine contains aspirin, ibuprofen, ketoprofen, or naproxen.
Get emergency medical help if you have signs of an allergic reaction to ibuprofen: rash or hives; sneezing, runny or stuffy nose; wheezing or trouble breathing; swelling of your face, lips, tongue, or throat.
Get emergency medical help if you have signs of a heart attack or stroke: chest pain spreading to your jaw or shoulder, sudden numbness or weakness on one side of the body, slurred speech, leg swelling, feeling short of breath.
قرص ibuprofen چیست
Stop using ibuprofen and call your doctor at once if you have:
changes in your vision;
shortness of breath (even with mild exertion);
swelling or rapid weight gain;
the first sign of any skin rash, no matter how mild;
signs of stomach bleeding – bloody or tarry stools, coughing up blood or vomit that looks like coffee grounds;
liver problems – nausea, upper stomach pain, itching, tired feeling, flu-like symptoms, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes);
kidney problems – little or no urinating, painful or difficult urination, swelling in your feet or ankles, feeling tired or short of breath;
low red blood cells (anemia) – pale skin, feeling light-headed or short of breath, rapid heart rate, trouble concentrating; or
severe skin reaction – fever, sore throat, swelling in your face or tongue, burning in your eyes, skin pain followed by a red or purple skin rash that spreads (especially in the face or upper body) and causes blistering and peeling.
Common ibuprofen side effects may include:
upset stomach, mild heartburn, nausea, vomiting;
bloating, gas, diarrhea, constipation;
dizziness, headache, nervousness;
decreased appetite;
mild itching or rash; or
ringing in your ears.
This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Ibuprofen side effects (in more detail)
Usual Adult Dose for Dysmenorrhea:
200-400 mg orally every 4 to 6 hours as needed.
Usual Adult Dose for Osteoarthritis:
Initial dose: 400 to 800 mg orally every 6 to 8 hours.
Maintenance dose: May be increased to a maximum daily dose of 3200 mg based on patient response and tolerance.
Usual Adult Dose for Rheumatoid Arthritis:
Initial dose: 400 to 800 mg orally every 6 to 8 hours.
Maintenance dose: May be increased to a maximum daily dose of 3200 mg based on patient response and tolerance.
Usual Adult Dose for Pain or Fever:
Oral: Mild to moderate pain:
200 to 400 mg orally every 4 to 6 hours as needed. Doses greater than 400 mg have not been proven to provide greater efficacy.
IV: (Patients should be well hydrated before IV ibuprofen administration):
Pain: 400 to 800 mg intravenously over 30 minutes every 6 hours as needed.
Fever: Initial: 400 mg intravenously over 30 minutes
Maintenance: 400 mg every 4 to 6 hours or 100 to 200 mg every 4 hours as needed.
Usual Pediatric Dose for Fever or Pain:
Greater than 6 months to 12 years:
5 mg/kg/dose for temperature less than 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed.
10 mg/kg/dose for temperature greater than or equal to 102.5 degrees F (39.2 degrees C) orally every 6 to 8 hours as needed.
The recommended maximum daily dose is 40 mg/kg.
OTC pediatric labeling (analgesic, antipyretic): 6 months to 11 years: 7.5 mg/kg/dose every 6 to 8 hours; Maximum daily dose: 30 mg/kg
Ask your doctor before using ibuprofen if you take an antidepressant such as citalopram, escitalopram, fluoxetine (Prozac), fluvoxamine, paroxetine, sertraline (Zoloft), trazodone, or vilazodone. Taking any of these medicines with an NSAID may cause you to bruise or bleed easily.
Ask a doctor or pharmacist if it is safe for you to use ibuprofen if you are also using any of the following drugs:
lithium;
methotrexate;
a blood thinner (warfarin, Coumadin, Jantoven);
heart or blood pressure medication, including a diuretic or “water pill” as well as “ACE-inhibitor” medications; or
steroid medicine (such as prednisone).
This list is not complete. Other drugs may interact with ibuprofen, including prescription and over-the-counter medicines, vitamins, and herbal products. Not all possible interactions are listed in this medication guide.
Ibuprofen drug interactions (in more detail)
Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use ibuprofen only for the indication prescribed.
Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.
Copyright 1996-2019 Cerner Multum, Inc. Version: 18.01.
Medical Disclaimer
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Use these dosage charts for infants and children under 12 years old:
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Ibuprofen is one of a group of drugs called non-steroidal anti-inflammatory drugs (NSAIDs). It’s widely used for its pain-relieving and anti-inflammatory effects.
It’s available over the counter as tablets or capsules in doses of 200–400 mg and can be taken up to three times a day after food. Some tablets are designed to release the drug slowly over a period of time, and some people find these helpful for night-time pain relief.
Higher doses of ibuprofen are available on prescription and can be used if you have rheumatoid arthritis or another type of inflammatory arthritis.
If ibuprofen doesn’t give enough relief from pain, or if you need pain relief over a long period of time, then you should speak to your doctor, who may be able to prescribe a stronger type of NSAID or a combination of drugs that will be more effective.
Ibuprofen can usually be used in combination with paracetamol or a compound analgesic.
قرص ibuprofen چیست
As with other NSAIDS, ibuprofen can cause stomach-related side-effects, so you should speak to your doctor if you tend to have problems such as heartburn or indigestion. Your doctor may suggest a different type of NSAID and/or prescribe a drug called a proton pump inhibitor (PPI) to help protect your stomach.
Long-term use of NSAIDs, including ibuprofen, can also increase the risk of problems with your heart or circulation – especially if you have other risk factors for these conditions. Therefore you shouldn’t take ibuprofen for long-term pain relief without seeing your doctor first, and you shouldn’t take ibuprofen if you’re also being prescribed another type of NSAID tablet.
Find out more about other NSAIDs that are available.
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