لیدوکائین
Lidocaine Patch 5% (Lidoderm)
لیدوکائین

نام ژنریک

Lidocaine (Mucosal - Local )

شکل دارویی

اشكال دارويي:


Solution: 4%


Spray, solution: 6.5%


Gel: 2%


Ointment: Lidocaine 5%+Hydrocortisone Acetate 0.5%

موارد مصرف

موارد و مقدار مصرف


پماد: بزرگسالان: براي ايجاد بيحسي در غشاي مخاطي:


در دندانپزشكي: به طور سطحي از پماد پنج درصد به مخاط دهاني كه از قبل خشك شده باشد ، ماليده مي‌شود.


در حلق دهاني: به طور سطحي از پماد پنج درصد به ناحيه مورد نظر ، و يا به دستگاه مورد استفاده قبل از كاربرد آن، ماليده مي‌شود.


کودکان: مقدار مصرف اين شكل دارو در كودكان تعيين نشده است.


افشانه (Spray) :


بزرگسالان و نوجوانان: به طور سطحي مقدار 20 ميلي‌گرم در ربع لثه و مخاط دهاني استعمال مي‌شود. حداكثر
مقدار مصرف 30 ميلي‌گرم در هر ربع لثه و مخاط دهاني طي نيم ساعت است.


کودکان: مقدار مصرف اين شكل دارو در كودكان تعيين نشده است.


ژل:


بزرگسالان و نوجوانان: براي ايجاد بيحسي در غشاي مخاطي.


مري، حنجره، ناي: پيش از كاربرد دستگاه مورد نظر ، از ژل دو درصد بر روي آن ماليده مي‌شود.


مجاري ادراري: زنان ، مقدار 5-3 ميلي‌ليتر از ژل دو درصد، چند دقيقه قبل از معاينه، در داخل مجراي ادراري استعمال مي‌شود.


مردان: قبل از گذاشتن كاتتر، مقدار 200-100 ميلي‌گرم (10-5 ميلي ليتر ) از ژل دو درصد در پيشابراه استعمال مي‌شود.


قبل از سوند گذاري يا سيستوسكوپي: مقدار 600 ميلي‌گرم (30 ميلي ليتر ) معمولاً در دو مقدار منقسم مصرف مي‌شود. حداكثر مقدار مصرف 600 ميلي گرم (30 ميلي‌گرم ) در طي 12 ساعت است.


كودكان: در زنان مي‌توان ژل را به وسيله سواب در پيشابراه به كار برد.


محلول ويسكوز: بزرگسالان و نوجوانان.


اختلالات حفره دهان: 300 ميلي‌گرم (15 ميلي‌ليتر) از محلول را بايد در دهان چرخاند و سپس بيرون ريخت در صورت لزوم، هر سه ساعت اين كار تكرار مي‌شود.


درد حلقي: 300 ميلي‌گرم (15 ميلي‌ليتر ) در دهان غرغره مي‌شود. در صورت لزوم مي‌توان آن را بلعيد. حداكثر مقدار مصرف به صورت مقدار واحد mg/Kg 5 و 4 يا 300 ميلي‌گرم (15 ميلي‌ليتر) مي‌باشد.


حداكثر مقدار مصرف در موارد مصرف متعدد، تا هشت مقدار (4 و 2 گرم يا 12 ميلي‌ليتر) در 24 ساعت است.


كودكان: مقدار مصرف اين شكل دارو براي هر كودك به طور جداگانه تعيين مي‌شود.


توجه: براي نوزادان و كودكان تا سن 3 سال توصيه مي‌شود كه مقدار مصرف به طور دقيق اندازه‌گيري شود و به وسيله يك اپليكاتور نخي در ناحيه يا ضايعه اختصاصي مصرف شود. اگر مقدار مصرف به خوبي كنترل نشده، و يا بيمار مقادير زيادي از دارو را ببلعد، خطر مسموميت سيستميك، بخصوص تشنجات، افزايش مي‌يابد.


بزرگسالان و نوجوانان: براي ايجاد بيحسي در غشاي مخاطي:


براي فرونشاني رفلكس حلقي به منظور معاينات دنداني ، اعمال جراحي دهان، آندوسكوپي يا لوله گذاري در ناي mg/Kg 3-6/0 يا 200-40 ميلي‌گرم به صورت موضعي مصرف مي‌شود.


توجه: اين شكل دارو را مي‌توان به صورت افشانه، توسط اپليكاتورهاي نخي مصرف كرد و يا به صورت مستقيم در داخل حفره چكاند.


مجاري ادراري براي قرار دادن دستگاه در پيشابراه يا معاينه آن، يا درمان التهاب دردناك پيشابراه:


زنان : مقدار 20 ميلي‌گرم به وسيله يك سواب نخي به مدت 5-2 دقيقه در محل قرار داده مي‌شود،


مردان:
مقدار 300-100 ميلي‌گرم به مدت 5-2 دقيقه در موضع قرار داده
مي‌شود.


مكانيسم اثر


بيحس كننده‌هاي موضعي از طريق كاهش نفوذپذيري غشاي سلولهاي عصبي به يون سديم شروع و هدايت تكانه‌هاي عصبي را مسدود مي‌كند. اين عمل به طور برگشت پذير موجب تثبيت غشاء و مهار دپولاريزاسيون شده و به نارسايي در انتشار پتانسيل عمل و انسداد هدايت بعدي تكانه عصبي منجر مي‌شود.


ساير اثرها: در صورت جذب مقادير كافي اين داروها از طريق مخاط ، فعاليت آنها بر روي سيستم اعصاب مركزي (CNS) ممكن است موجب تحريك و يا تضعيف CNS شود. فعاليت اين دارو بر سيستم قلبي - عروقي ممكن است سبب تضعيف هدايت و تهييج پذيري قلبي ، و موجب گشاد شدن عروق محيطي شود.

موارد منع مصرف

تداخل دارويي


در صورت مصرف همزمان با داروهاي مسدود كننده گيرنده بتا - آدرنرژيك ، سرعت متابوليسم ليدوكائين كاهش مي‌يابد و در صورت جذب قابل توجه ليدوكائين ممكن است به بروز مسموميت با اين دارو منجر شود.


در صورت مصرف همزمان با سايمتيدين، متابوليسم كبدي ليدوكائين مهار مي‌شود، و در صورت جذب قابل توجه ليدوكائين ممكن است مسموميت با اين دارو عارض شود.

موارد قابل توجه

-

تداخل دارویی

عوارض جانبي


واكنش‌هاي آلرژيك (با شيوع كمتر): آنژيوادم (تورم پوست، دهان با گلو) سوزش، گزش، تورم، يا حساسيت پوست به لمس كه قبل از درمان با اين دارو وجود نداشته است، درماتيت تماسي و آلرژيك (بثورات پوستي، قرمزي، خارش، كهير).


ادراري - تناسلي (نادر ): التهاب پيشابراه (وجود خون در ادرار - افزايش دفعات دفع ادرار ، درد يا سوزش طي ادرار كردن) اين عوارض در صورت مصرف دارو در پيشابراه ممكن است بروز كنند.


مسموميت و درمان


تظاهرات باليني: تضعيف دستگاه قلبي - عروقي (افزايش تعريق ، كاهش فشار خون، رنگ پريدگي پوست، ضربان نامنظم يا آهسته قلب) كه ممكن است به ايست قلبي منجر شود، تضعيف (CNS) (خواب آلودگي)، تحريك CNS (تاري ديد يا دوبيني ، تشنج، سرگيجه، زنگ زدن يا همهمه در گوش، لرزش يا لرزش، اضطراب، هيجان، عصبانيت يا بي قراري غير معمول).


توجه: معمولاً ابتدا تحريك CNS ممكن است گذرا بوده يا بروز نكند ، و به اين ترتيب، خواب آلودگي ممكن است اولين علامت مسموميت در بعضي از بيماران باشد. ضعف CNS ممكن است به بيهوشي و ايست تنفسي منجر شود .


درمان: براي درمان واكنشهاي سيستماتيك، از باز بودن راه تنفسي بايد اطمينان حاصل كرد، اكسيژن 100 درصد تجويز، و در صورت لزوم تنفس مصنوعي به بيمار داده شود. در بعضي از بيماران قرار دادن لوله داخل ناي ممكن است ضروري باشد.


براي درمان ضعف دستگاه گردش خون، بايد يك داروي تنگ كننده عروق و مايعات از طريق وريد تجويز شود. اگر تشنجات به حمايت تنفسي پاسخ ندهند، تزريق وريدي بنزوديازپينها، مانند ديازپام (كه هر بار 5/2 ميلي‌گرم به مقدار آن افزوده مي‌شود) و يا يك باربيتورات بسيار كوتاه اثر، مانند تيوپنتال (كه هر بار 100-50 ميلي‌گرم به مقدار اوليه افزوده مي‌شود) هر 3-2 دقيقه توصيه مي‌شود. تضعيف دستگاه گردش خون به وسيله اين داروها، بخصوص باربيتوراتها، بايد در نظر گرفته شود. در صورت لزوم مي‌توان يك داروي مسدود كننده عصبي - عضلاني استفاده كرد تا تظاهرات عضلاني تشنجات مقاوم را كاهش دهد. در صورت لزوم مصرف چنين دارويي ، تنفس مصنوعي ضروري است.

مکانیزم اثر

عوارض جانبي


واكنش‌هاي آلرژيك (با شيوع كمتر): آنژيوادم (تورم پوست، دهان با گلو) سوزش، گزش، تورم، يا حساسيت پوست به لمس كه قبل از درمان با اين دارو وجود نداشته است، درماتيت تماسي و آلرژيك (بثورات پوستي، قرمزي، خارش، كهير).


ادراري - تناسلي (نادر ): التهاب پيشابراه (وجود خون در ادرار - افزايش دفعات دفع ادرار ، درد يا سوزش طي ادرار كردن) اين عوارض در صورت مصرف دارو در پيشابراه ممكن است بروز كنند.


مسموميت و درمان


تظاهرات باليني: تضعيف دستگاه قلبي - عروقي (افزايش تعريق ، كاهش فشار خون، رنگ پريدگي پوست، ضربان نامنظم يا آهسته قلب) كه ممكن است به ايست قلبي منجر شود، تضعيف (CNS) (خواب آلودگي)، تحريك CNS (تاري ديد يا دوبيني ، تشنج، سرگيجه، زنگ زدن يا همهمه در گوش، لرزش يا لرزش، اضطراب، هيجان، عصبانيت يا بي قراري غير معمول).


توجه: معمولاً ابتدا تحريك CNS ممكن است گذرا بوده يا بروز نكند ، و به اين ترتيب، خواب آلودگي ممكن است اولين علامت مسموميت در بعضي از بيماران باشد. ضعف CNS ممكن است به بيهوشي و ايست تنفسي منجر شود .


درمان: براي درمان واكنشهاي سيستماتيك، از باز بودن راه تنفسي بايد اطمينان حاصل كرد، اكسيژن 100 درصد تجويز، و در صورت لزوم تنفس مصنوعي به بيمار داده شود. در بعضي از بيماران قرار دادن لوله داخل ناي ممكن است ضروري باشد.


براي درمان ضعف دستگاه گردش خون، بايد يك داروي تنگ كننده عروق و مايعات از طريق وريد تجويز شود. اگر تشنجات به حمايت تنفسي پاسخ ندهند، تزريق وريدي بنزوديازپينها، مانند ديازپام (كه هر بار 5/2 ميلي‌گرم به مقدار آن افزوده مي‌شود) و يا يك باربيتورات بسيار كوتاه اثر، مانند تيوپنتال (كه هر بار 100-50 ميلي‌گرم به مقدار اوليه افزوده مي‌شود) هر 3-2 دقيقه توصيه مي‌شود. تضعيف دستگاه گردش خون به وسيله اين داروها، بخصوص باربيتوراتها، بايد در نظر گرفته شود. در صورت لزوم مي‌توان يك داروي مسدود كننده عصبي - عضلاني استفاده كرد تا تظاهرات عضلاني تشنجات مقاوم را كاهش دهد. در صورت لزوم مصرف چنين دارويي ، تنفس مصنوعي ضروري است.

فارماكوكینتیك

موارد منع مصرف و احتياط


موارد احتياط: وجود عفونت موضعي (تغيير در pH ممكن است به كاهش يا از بين رفتن اثر دارو منجر شود )، اختلالهاي شديد يا وسيع پوستي (جذب دارو افزايش مي‌يابد)، آسيب مخاطي (افزايش جذب دارو به مسموميت سيستميك منجر مي‌شود) كودكان، سالخوردگان و بيماران ناتوان(ممكن است به مسموميت سيستميك با اين دارو حساس تر باشند).

سایر اطلاعات

طبقه‌بندي فارماكولوژيك: مشتق آميدي.


طبقه‌بندي درماني: بيحس كننده موضعي.


طبقه‌بندي مصرف در بارداري: رده B


نکات قابل توصيه به بيمار


1- از مصرف اين دارو در نواحي وسيعي از پوست يا مخاط (بخصوص در صورت آسيب ديدگي) و نيز از مصرف طولاني مدت يا مقادير زياد آن بدون دستور پزشك يا دندانپزشك خودداري نماييد.


2- از تماس دارو با چشم خودداري كنيد. براي استفاده شكل افشانه دارو در صورت، از دست يا يك اپليكاتور مناسب استفاده نماييد.


3- در صورت عدم بهبود يا بدتر شدن بيماري، وجود عفونت در موضع و يا بروز خارش، و ساير علائمي كه از قبل وجود نداشته است، مصرف دارو را قطع كرده و به پزشك يا دندانپزشك مراجعه نماييد.


4- در صورت استفاده از افشانه، از استنشاق دارو خودداري كنيد. افشانه را در انتهاي گلو يا دهان به كار نبريد مگر آنكه پزشك يا دندانپزشك تجويز كرده باشد.


5- تا يك ساعت بعد از مصرف دارو در دهان يا گلو از خوردن غذا خودداري نماييد، زيرا ممكن است موجب اختلال در بلع شده و به آسپيراسيون منجر شود. در صورت ادامه بيحسي دهان، از جويدن آدامس يا غذا خودداري كنيد، زيرا خطر گاز گرفتن زبان يا مخاط دهان وجود دارد.


6- در صورت مصرف اين دارو براي تسكين دندان درد از آن به طور موقت استفاده كنيد و هر چه زودتر به دندانپزشك مراجعه نماييد.


7- اين دارو را مي‌توان به طور مستقيم بر روي موضع و يا به وسيله يك اپليكاتور (مانند گاز استريل يا تكه‌اي پنبه) استفاده كرد.


8- از بلعيدن دارو خودداري كنيد، مگر آنكه پزشك يا دندانپزشك تجويز كرده باشد.


مصرف در سالمندان: احتمال بروز مسموميت سيستميك در بيماران سالخورده كه به مقادير كمتر دارو، بخصوص براي روشهاي آندوسكوپيك، احتياج دارند، بيشتر از ديگران است.


مصرف در كودكان: كودكان ممكن است نسبت به مسموميت سيستميك با اين دارو حساس تر باشند.


مصرف در شيردهي: عوارضي براي انسان درا ين مورد اثبات نشده است.


توجه: براي كسب آگاهي بيشتر درباره اين دارو، به تك نگار Hcl Lidocaine مراجعه كنيد.


ملاحظات اختصاصي


1- بي ضرري و اثربخشي مصرف اين دارو در معاينات يا به كار بردن وسايل پزشكي، به مقدار مصرف صحيح، روش مناسب، و رعايت احتياطهاي لازم و آمادگي جهت مقابله با مواد اضطراري بستگي دارد. در هنگام مصرف اين دارو، بايد وسايل احياي بيمار و ساير داروهاي ضروري در دسترس باشند.


2- بيماراني كه نسبت به يك داروي بيحس كننده موضعي آميدي تحمل نشان نمي‌دهند، به ندرت ممكن است داروي ديگر از دسته آميدها را نيز تحمل كنند.

Lidocaine Patch 5% (Lidoderm)

LIDODERM®
(lidocaine) Patch 5%

DRUG DESCRIPTION

LIDODERM (lidocaine patch 5%) is comprised of an adhesive material containing 5% lidocaine, which is applied to a non-woven polyester felt backing and covered with a polyethylene terephthalate (PET) film release liner. The release liner is removed prior to application to the skin. The size of the patch is 10 cm × 14 cm.

Lidocaine is chemically designated as acetamide, 2-(diethylamino)-N-(2,6-dimethylphenyl), has an octanol: water partition ratio of 43 at pH 7.4, and has the following structure:

LIDODERM®
  (Lidocaine) Structural Formula Illustration

Each adhesive patch contains 700 mg of lidocaine (50 mg per gram adhesive) in an aqueous base. It also contains the following inactive ingredients: dihydroxyaluminum aminoacetate, disodium edetate, gelatin, glycerin, kaolin, methylparaben, polyacrylic acid, polyvinyl alcohol, propylene glycol, propylparaben, sodium carboxymethylcellulose, sodium polyacrylate, D-sorbitol, tartaric acid, and urea.

What are the possible side effects of lidocaine topical?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using lidocaine topical and call your doctor at once if you have any of these serious side effects:

  • uneven heartbeats;
  • drowsiness, confusion;
  • tremors, seizure (convulsions); or
  • blurred vision.

Less serious side effects include:

  • mild irritation, redness, or swelling where the medication is applied; or
  • numbness in places where the medicine is accidentally...

Read All Potential Side Effects and See Pictures of Lidoderm »

What are the precautions when taking lidocaine patch 5% (Lidoderm)?

Before using lidocaine, tell your doctor or pharmacist if you are allergic to it; or to other local anesthetics; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: severe liver disease.

While wearing your patch, avoid exposing it to direct heat sources such as heating pads, electric blankets, heat lamps, saunas, hot tubs, heated waterbeds, or prolonged direct sunlight. Heat may cause more drug to be released into your body, increasing the chance of side effects.

This medication should be used only when clearly needed during pregnancy. Discuss...

Read All Potential Precautions of Lidoderm »

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

INDICATIONS

LIDODERM (lidocaine patch 5%) is indicated for relief of pain associated with post-herpetic neuralgia. It should be applied only to intact skin.

DOSAGE AND ADMINISTRATION

Apply LIDODERM (lidocaine patch 5%) to intact skin to cover the most painful area. Apply up to three patches, only once for up to 12 hours within a 24-hour period. Patches may be cut into smaller sizes with scissors prior to removal of the release liner. (See Handling And Disposal) Clothing may be worn over the area of application. Smaller areas of treatment are recommended in a debilitated patient, or a patient with impaired elimination.

If irritation or a burning sensation occurs during application, remove the patch(es) and do not reapply until the irritation subsides.

When LIDODERM (lidocaine patch 5%) is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered.

Handling And Disposal

Hands should be washed after the handling of LIDODERM (lidocaine patch 5%) , and eye contact with LIDODERM (lidocaine patch 5%) should be avoided. Do not store patch outside the sealed envelope. Apply immediately after removal from the protective envelope. Fold used patches so that the adhesive side sticks to itself and safely discard used patches or pieces of cut patches where children and pets cannot get to them. LIDODERM (lidocaine patch 5%) should be kept out of the reach of children.

HOW SUPPLIED

LIDODERM (lidocaine patch 5%) is available as the following:

Carton of 30 patches, packaged into individual child-resistant envelopes.
NDC
63481-687-06

Store at 25°C (77°F); excursions permitted to 15°-30°C (59°-86°F). [See USP Controlled Room Temperature].

Manufactured for: Endo Pharmaceuticals Inc. Chadds Ford, Pennsylvania 19317.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

SIDE EFFECTS

Application Site Reactions

During or immediately after treatment with LIDODERM (lidocaine patch 5%), the skin at the site of application may develop blisters, bruising, burning sensation, depigmentation, dermatitis, discoloration, edema, erythema, exfoliation, irritation, papules, petechia, pruritus, vesicles, or may be the locus of abnormal sensation. These reactions are generally mild and transient, resolving spontaneously within a few minutes to hours.

Allergic Reactions

Allergic and anaphylactoid reactions associated with lidocaine, although rare, can occur. They are characterized by angioedema, bronchospasm, dermatitis, dyspnea, hypersensitivity, laryngospasm, pruritus, shock, and urticaria. If they occur, they should be managed by conventional means. The detection of sensitivity by skin testing is of doubtful value.

Other Adverse Events

Due to the nature and limitation of spontaneous reports in postmarketing surveillance, causality has not been established for additional reported adverse events including:

Asthenia, confusion, disorientation, dizziness, headache, hyperesthesia, hypoesthesia, lightheadedness, metallic taste, nausea, nervousness, pain exacerbated, paresthesia, somnolence, taste alteration, vomiting, visual disturbances such as blurred vision, flushing, tinnitus, and tremor.

Systemic (Dose-Related) Reactions

Systemic adverse reactions following appropriate use of LIDODERM (lidocaine patch 5%) are unlikely, due to the small dose absorbed (see CLINICAL PHARMACOLOGY, Pharmacokinetics). Systemic adverse effects of lidocaine are similar in nature to those observed with other amide local anesthetic agents, including CNS excitation and/or depression (light headedness, nervousness, apprehension, euphoria, confusion, dizziness, drowsiness, tinnitus, blurred or double vision, vomiting, sensations of heat, cold or numbness, twitching, tremors, convulsions, unconsciousness, respiratory depression and arrest). Excitatory CNS reactions may be brief or not occur at all, in which case the first manifestation may be drowsiness merging into unconsciousness. Cardiovascular manifestations may include bradycardia, hypotension and cardiovascular collapse leading to arrest.

Read the Lidoderm (lidocaine patch 5%) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

Antiarrhythmic Drugs: LIDODERM (lidocaine patch 5%) should be used with caution in patients receiving Class I antiarrhythmic drugs (such as tocainide and mexiletine) since the toxic effects are additive and potentially synergistic.

Local Anesthetics: When LIDODERM (lidocaine patch 5%) is used concomitantly with other products containing local anesthetic agents, the amount absorbed from all formulations must be considered.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

WARNINGS

Accidental Exposure in Children

Even a used LIDODERM patch contains a large amount of lidocaine (at least 665 mg). The potential exists for a small child or a pet to suffer serious adverse effects from chewing or ingesting a new or used LIDODERM (lidocaine patch 5%) patch, although the risk with this formulation has not been evaluated. It is important for patients to store and dispose of LIDODERM (lidocaine patch 5%) out of the reach of children, pets and others. (See Handling And Disposal)

Excessive Dosing

Excessive dosing by applying LIDODERM (lidocaine patch 5%) to larger areas or for longer than the recommended wearing time could result in increased absorption of lidocaine and high blood concentrations, leading to serious adverse effects (see ADVERSE REACTIONS, Systemic Reactions). Lidocaine toxicity could be expected at lidocaine blood concentrations above 5 µg/mL. The blood concentration of lidocaine is determined by the rate of systemic absorption and elimination. Longer duration of application, application of more than the recommended number of patches, smaller patients, or impaired elimination may all contribute to increasing the blood concentration of lidocaine. With recommended dosing of LIDODERM (lidocaine patch 5%) , the average peak blood concentration is about 0.13 µg/mL, but concentrations higher than 0.25 µg/mL have been observed in some individuals.

PRECAUTIONS

General

Hepatic Disease: Patients with severe hepatic disease are at greater risk of developing toxic blood concentrations of lidocaine, because of their inability to metabolize lidocaine normally.

Allergic Reactions: Patients allergic to para-aminobenzoic acid derivatives (procaine, tetracaine, benzocaine, etc.) have not shown cross sensitivity to lidocaine. However, LIDODERM (lidocaine patch 5%) should be used with caution in patients with a history of drug sensitivities, especially if the etiologic agent is uncertain.

Non-intact Skin: Application to broken or inflamed skin, although not tested, may result in higher blood concentrations of lidocaine from increased absorption. LIDODERM (lidocaine patch 5%) is only recommended for use on intact skin.

External Heat Sources: Placement of external heat sources, such as heating pads or electric blankets, over LIDODERM (lidocaine patch 5%) patches is not recommended as this has not been evaluated and may increase plasma lidocaine levels.

Eye Exposure: The contact of LIDODERM (lidocaine patch 5%) with eyes, although not studied, should be avoided based on the findings of severe eye irritation with the use of similar products in animals. If eye contact occurs, immediately wash out the eye with water or saline and protect the eye until sensation returns.

Carcinogenesis, Mutagenesis, Impairment of Fertility

Carcinogenesis: A minor metabolite, 2,6-xylidine, has been found to be carcinogenic in rats. The blood concentration of this metabolite is negligible following application of LIDODERM.

Mutagenesis: Lidocaine HCl is not mutagenic in Salmonella/mammalian microsome test nor clastogenic in chromosome aberration assay with human lymphocytes and mouse micronucleus test.

Impairment of Fertility: The effect of LIDODERM (lidocaine patch 5%) on fertility has not been studied.

Pregnancy

Teratogenic Effects: Pregnancy Category B. LIDODERM (lidocaine patch 5%) has not been studied in pregnancy. Reproduction studies with lidocaine have been performed in rats at doses up to 30 mg/kg subcutaneously and have revealed no evidence of harm to the fetus due to lidocaine. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, LIDODERM (lidocaine patch 5%) should be used during pregnancy only if clearly needed.

Labor and Delivery

LIDODERM has not been studied in labor and delivery. Lidocaine is not contraindicated in labor and delivery. Should LIDODERM be used concomitantly with other products containing lidocaine, total doses contributed by all formulations must be considered.

Nursing Mothers

LIDODERM has not been studied in nursing mothers. Lidocaine is excreted in human milk, and the milk:plasma ratio of lidocaine is 0.4. Caution should be exercised when LIDODERM (lidocaine patch 5%) is administered to a nursing woman.

Pediatric Use

Safety and effectiveness in pediatric patients have not been established.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

OVERDOSE

Lidocaine overdose from cutaneous absorption is rare, but could occur. If there is any suspicion of lidocaine overdose (see ADVERSE REACTIONS, Systemic Reactions), drug blood concentration should be checked. The management of overdose includes close monitoring, supportive care, and symptomatic treatment. Dialysis is of negligible value in the treatment of acute overdose with lidocaine.

In the absence of massive topical overdose or oral ingestion, evaluation of symptoms of toxicity should include consideration of other etiologies for the clinical effects, or overdosage from other sources of lidocaine or other local anesthetics.

The oral LD50 of lidocaine HCl is 459 (346-773) mg/kg (as the salt) in non-fasted female rats and 214 (159-324) mg/kg (as the salt) in fasted female rats, which are equivalent to roughly 4000 mg and 2000 mg, respectively, in a 60 to 70 kg man based on the equivalent surface area dosage conversion factors between species.

CONTRAINDICATIONS

LIDODERM (lidocaine patch 5%) is contraindicated in patients with a known history of sensitivity to local anesthetics of the amide type, or to any other component of the product.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

CLINICAL PHARMACOLOGY

Pharmacodynamics

Lidocaine is an amide-type local anesthetic agent and is suggested to stabilize neuronal membranes by inhibiting the ionic fluxes required for the initiation and conduction of impulses.

The penetration of lidocaine into intact skin after application of LIDODERM (lidocaine patch 5%) is sufficient to produce an analgesic effect, but less than the amount necessary to produce a complete sensory block.

Pharmacokinetics

Absorption: The amount of lidocaine systemically absorbed from LIDODERM (lidocaine patch 5%) is directly related to both the duration of application and the surface area over which it is applied. In a pharmacokinetic study, three LIDODERM (lidocaine patch 5%) patches were applied over an area of 420 cm2 of intact skin on the back of normal volunteers for 12 hours. Blood samples were withdrawn for determination of lidocaine concentration during the application and for 12 hours after removal of patches. The results are summarized in Table 1.

Table 1: Absorption of lidocaine from LIDODERM (lidocaine patch 5%)
Normal volunteers (n = 15, 12-hour wearing time)

LIDODERM Patch Application Site Area (cm2) Dose Absorbed (mg) Cmax (µg/mL) Tmax (hr)
3 patches
(2100 mg)
Back 420 64 ± 32 0.13 ± 0.06 11 hr

When LIDODERM (lidocaine patch 5%) is used according to the recommended dosing instructions, only 3 ± 2% of the dose applied is expected to be absorbed. At least 95% (665 mg) of lidocaine will remain in a used patch. Mean peak blood concentration of lidocaine is about 0.13 µg/mL (about 1/10 of the therapeutic concentration required to treat cardiac arrhythmias). Repeated application of three patches simultaneously for 12 hours (recommended maximum daily dose), once per day for three days, indicated that the lidocaine concentration does not increase with daily use. The mean plasma pharmacokinetic profile for the 15 healthy volunteers is shown in Figure 1.

Figure 1: Mean lidocaine blood concentrations after three consecutive daily applications of three LIDODERM (lidocaine patch 5%) patches simultaneously for 12 hours per day in healthy volunteers (n = 15).

Mean lidocaine blood concentrations - Illustration

Distribution: When lidocaine is administered intravenously to healthy volunteers, the volume of distribution is 0.7 to 2.7 L/kg (mean 1.5 ± 0.6 SD, n = 15). At concentrations produced by application of LIDODERM, lidocaine is approximately 70% bound to plasma proteins, primarily alpha-1-acid glycoprotein. At much higher plasma concentrations (1 to 4 µg/mL of free base), the plasma protein binding of lidocaine is concentration dependent. Lidocaine crosses the placental and blood brain barriers, presumably by passive diffusion.

Metabolism: It is not known if lidocaine is metabolized in the skin. Lidocaine is metabolized rapidly by the liver to a number of metabolites, including monoethylglycinexylidide (MEGX) and glycinexylidide (GX), both of which have pharmacologic activity similar to, but less potent than that of lidocaine. A minor metabolite, 2,6-xylidine, has unknown pharmacologic activity but is carcinogenic in rats. The blood concentration of this metabolite is negligible following application of LIDODERM (lidocaine patch 5%). Following intravenous administration, MEGX and GX concentrations in serum range from 11 to 36% and from 5 to 11% of lidocaine concentrations, respectively.

Excretion: Lidocaine and its metabolites are excreted by the kidneys. Less than 10% of lidocaine is excreted unchanged. The half-life of lidocaine elimination from the plasma following IV administration is 81 to 149 minutes (mean 107 ± 22 SD, n = 15). The systemic clearance is 0.33 to 0.90 L/min (mean 0.64 ± 0.18 SD, n = 15).

Clinical Studies

Single-dose treatment with LIDODERM was compared to treatment with vehicle patch (without lidocaine), and to no treatment (observation only) in a double-blind, crossover clinical trial with 35 post-herpetic neuralgia patients. Pain intensity and pain relief scores were evaluated periodically for 12 hours. LIDODERM (lidocaine patch 5%) performed statistically better than vehicle patch in terms of pain intensity from 4 to 12 hours.

Multiple-dose, two-week treatment with LIDODERM was compared to vehicle patch (without lidocaine) in a double-blind, crossover clinical trial of withdrawal-type design conducted in 32 patients, who were considered as responders to the open-label use of LIDODERM (lidocaine patch 5%) prior to the study. The constant type of pain was evaluated but not the pain induced by sensory stimuli (dysesthesia). Statistically significant differences favoring LIDODERM (lidocaine patch 5%) were observed in terms of time to exit from the trial (14 versus 3.8 days at p-value < 0.001), daily average pain relief, and patient's preference of treatment. About half of the patients also took oral medication commonly used in the treatment of post-herpetic neuralgia. The extent of use of concomitant medication was similar in the two treatment groups.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

PATIENT INFORMATION

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

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PATIENT INFORMATION

No information provided. Please refer to the WARNINGS and PRECAUTIONS sections.

Last reviewed on RxList: 1/24/2011
This monograph has been modified to include the generic and brand name in many instances.

Disclaimer

Lidoderm Consumer

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

LIDOCAINE PATCH - TOPICAL

(LIE-doh-cane)

COMMON BRAND NAME(S): Lidoderm

USES: This medication is used to relieve nerve pain after shingles (infection with the herpes zoster virus). This type of pain is called post-herpetic neuralgia. Lidocaine helps to reduce sharp/burning/aching pain as well as discomfort caused by skin areas that are overly sensitive to touch. Lidocaine belongs to a class of drugs known as local anesthetics. It works by causing a temporary loss of feeling in the area where you apply the patch.

HOW TO USE: This product should only be applied to healthy, normal skin. Do not apply to skin that is broken or irritated. Dosage is based on your medical condition and response to therapy.

Remove the protective liner and apply the patch to the skin area that is most painful. Apply the prescribed number of patches, usually only once a day for up to 12 hours or as directed by your doctor. Do not apply more than 3 patches once a day or leave any patch on for longer than 12 hours in any 24-hour period. If a smaller patch is needed, it may be cut with scissors before the liner is removed.

Wash your hands well after each application. Avoid getting this medication in your eyes or mucous membranes (e.g., nose, mouth). If contact with the eyes accidentally occurs, wash your eyes immediately with water and protect them until normal feeling returns.

Inform your doctor if your condition does not improve or worsens.

Used patches still contain some medication. However, do not reuse them. Fold the used patch with the sticky sides together and discard it out of the reach of children and pets to prevent accidental swallowing or application.

Disclaimer

Lidoderm Consumer (continued)

SIDE EFFECTS: Redness, swelling, blisters, or changes in skin color at the site of application may occur. These effects usually disappear within a few minutes or hours. If any of these effects persist or worsen, notify your doctor or pharmacist promptly.

If irritation or a burning feeling occurs, remove the patch(es) and do not reapply until the irritation is gone.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

Tell your doctor immediately if any of these unlikely but serious side effects occur: blurred vision, mental/mood changes (e.g., nervousness, confusion), drowsiness, dizziness, unusually slow heartbeat.

A very serious allergic reaction to this drug is unlikely, but seek immediate medical attention if it occurs. Symptoms of a serious allergic reaction may include: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

Read the Lidoderm (lidocaine patch 5%) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before using lidocaine, tell your doctor or pharmacist if you are allergic to it; or to other local anesthetics; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: severe liver disease.

While wearing your patch, avoid exposing it to direct heat sources such as heating pads, electric blankets, heat lamps, saunas, hot tubs, heated waterbeds, or prolonged direct sunlight. Heat may cause more drug to be released into your body, increasing the chance of side effects.

This medication should be used only when clearly needed during pregnancy. Discuss the risks and benefits with your doctor.

This medication passes into breast milk. While there have been no reports of harm to nursing infants, consult your doctor before breast-feeding.

Disclaimer

Lidoderm Consumer (continued)

DRUG INTERACTIONS: Your healthcare professionals (e.g., doctor or pharmacist) may already be aware of any possible drug interactions and may be monitoring you for it. Do not start, stop or change the dosage of any medicine before checking with them first.

Before using this medication, tell your doctor or pharmacist of all prescription and nonprescription/herbal products you may use, especially of: certain drugs used to treat irregular heart rhythm (Class I anti-arrhythmic drugs such as mexiletine, tocainide), other local anesthetic products.

This document does not contain all possible interactions. Therefore, before using this product, tell your doctor or pharmacist of all the products you use. Keep a list of all your medications with you, and share the list with your doctor and pharmacist.

OVERDOSE: If overdose is suspected, remove the patch. This medicine may be harmful if swallowed. Contact your local poison control center or emergency room immediately. US residents can call the US national poison hotline at 1-800-222-1222. Canadian residents should call their local poison control center directly. Symptoms of overdose may include severe drowsiness, seizures, slowed breathing, slow/fast/irregular heartbeat.

NOTES: Do not share this medication with others.

MISSED DOSE: If you miss a dose, use it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

STORAGE: Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59-86 degrees F (15-30 degrees C) is permitted. Do not store in the bathroom. Keep the patch sealed in its protective envelope until ready to use. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed (See How to Use section).

Information last revised June 2010. Copyright(c) 2010 First Databank, Inc.

Lidoderm Patient Information Including Side Effects

Brand Names: AneCream, AneCream with Tegaderm, Anestacon, Bactine, LidaMantle, Lidocream, Lidoderm, Lidosense5, LMX 4, LMX 4 with Tegaderm, LMX 5, Medi-Quik Spray, Senatec, Solarcaine Aloe Extra Burn Relief, Solarcaine Cool Aloe, Uro-Jet, Uro-Jet AC, Xylocaine Jelly, Xylocaine Topical

Generic Name: lidocaine topical (Pronunciation: LYE doe kane TOP i kal)

What is lidocaine topical (Lidoderm)?

Lidocaine is a local anesthetic (numbing medication). It works by blocking nerve signals in your body.

Lidocaine topical (for use on the skin) is used to reduce pain or discomfort caused by skin irritations such as sunburn, insect bites, poison ivy, poison oak, poison sumac, and minor cuts, scratches, hemorrhoids, and burns.

Lidocaine topical may also be used for purposes not listed in this medication guide.

What are the possible side effects of lidocaine topical?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop using lidocaine topical and call your doctor at once if you have any of these serious side effects:

  • uneven heartbeats;
  • drowsiness, confusion;
  • tremors, seizure (convulsions); or
  • blurred vision.

Less serious side effects include:

  • mild irritation, redness, or swelling where the medication is applied; or
  • numbness in places where the medicine is accidentally applied.

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.

Read the Lidoderm (lidocaine patch 5%) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about lidocaine topical?

Your body may absorb more of this medication if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cut or irritated may also absorb more topical medication than healthy skin.

Use the smallest amount of this medication needed to numb the skin or relieve pain. Do not use large amounts of lidocaine topical, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.

Keep both used and unused lidocaine skin patches out of the reach of children or pets. The amount of lidocaine in the skin patches could be harmful to a child or pet who accidentally sucks on or swallows the patch. Seek emergency medical attention if this happens.

Side Effects Centers

Lidoderm Patient Information including How Should I Take

What should I discuss with my healthcare provider before using lidocaine topical?

Overdose is more likely to occur when using a numbing medicine without the advice of a medical doctor (such as during a cosmetic procedure like laser hair removal). However, overdose has also occurred in women treated with a numbing medicine before having a mammography. Symptoms may include uneven heartbeats, seizure (convulsions), coma, slowed breathing, or respiratory failure (breathing stops).

You should not use lidocaine topical if you are allergic to any other type of numbing medicine.

To make sure you can safely use lidocaine topical, tell your doctor if you have any of these other conditions:

  • liver disease; or
  • broken, swollen, or damaged skin.

FDA pregnancy category B. This medication is not expected to be harmful to an unborn baby. Tell your doctor if you are pregnant or plan to become pregnant during treatment.

Lidocaine topical can pass into breast milk and may harm a nursing baby. Do not use this medication without telling your doctor if you are breast-feeding a baby.

How should I use lidocaine topical?

Use exactly as prescribed by your doctor. Do not use in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Lidocaine topical comes in many different forms for different uses. Lidocaine topical cream, lotion, spray, solution, film, and transdermal patch are generally for use on the skin only.

If your medication comes with patient instructions for safe and effective use, follow these directions carefully. Ask your doctor or pharmacist if you have any questions.

Your body may absorb more of this medication if you use too much, if you apply it over large skin areas, or if you apply heat, bandages, or plastic wrap to treated skin areas. Skin that is cut or irritated may also absorb more topical medication than healthy skin.

Use the smallest amount of this medication needed to numb the skin or relieve pain. Do not use large amounts of lidocaine topical, or cover treated skin areas with a bandage or plastic wrap without medical advice. Be aware that many cosmetic procedures are performed without a medical doctor present.

Lidocaine topical may be applied with your finger tips or a cotton swab. Follow your doctor's instructions.

Do not apply this medication to swollen skin areas or deep puncture wounds. Avoid using the medicine on skin that is raw or blistered, such as a severe burn or abrasion.

Store at room temperature away from moisture and heat.

Keep both used and unused lidocaine topical patches out of the reach of children or pets. The amount of lidocaine in the skin patches could be harmful to a child or pet who accidentally sucks on or swallows the patch. Seek emergency medical attention if this happens.

Side Effects Centers

Lidoderm Patient Information including If I Miss a Dose

What happens if I miss a dose?

Since lidocaine is used as needed, you may not be on a dosing schedule. If you are using the medication regularly, 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.

What happens if I overdose?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222. Lidocaine topical applied to the skin is not likely to cause an overdose unless you apply more than the recommended dose. Overdose may also occur if you apply heat, bandages, or plastic wrap to treated skin areas.

Improper use of lidocaine topical may result in death.

Overdose symptoms may include drowsiness, confusion, nervousness, ringing in your ears, blurred vision, feeling hot or cold, numbness, muscle twitches, uneven heartbeats, seizure (convulsions), slowed breathing, or respiratory failure (breathing stops).

What should I avoid while using lidocaine topical?

Do not allow this medication to come into contact with your eyes. If it does, rinse with water. Avoid touching the sticky side of a lidocaine skin patch while applying it.

Avoid using other topical medications on the affected area unless your doctor has told you to.

What other drugs will affect lidocaine topical?

Tell your doctor about all other medicines you use, especially:

  • quinidine (Quin-G);
  • disopyramide (Norpace);
  • flecainide (Tambocor);
  • mexiletine (Mexitil);
  • procainamide (Procan, Pronestyl);
  • tocainide (Tonocard); or
  • propafenone (Rythmol).

This list is not complete and other drugs may interact with lidocaine. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist has information about lidocaine topical.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2012 Cerner Multum, Inc. Version: 6.02. Revision date: 3/27/2011.

Your use of the content provided in this service indicates that you have read,understood and agree to the End-User License Agreement,which can be accessed by clicking on this link.

Healthwise

Side Effects Centers

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