مکسیلتین (زاوسکا)
Mexiletine HCl (Mexitil)
مکسیلتین (زاوسکا)

نام ژنریک

Mexiletine HCl

شکل دارویی

اشكال دارويي:


Capsule: 100 ,200mg

موارد مصرف

موارد و مقدار مصرف


آريتمي‌هاي بطني خطرناك ثابت شده، از جمله تاكيكاردي بطني.


بزرگسالان: مقدار 200 ميلي‌گرم خوراکي هر هشت ساعت مصرف مي‌شود. در صورت لزوم، مقدار مصرف را مي‌توان در مقادير 100-50 ميلي‌گرم هر 8 ساعت هر 2 تا 3 روز افزايش يا كاهش داد. روش ديگر، تجويز مقدار سرشار 400 ميلي‌گرم، سپس مقدار نگهدارنده 200 ميلي‌گرم هر هشت ساعت است. بعضي از بيماران ممكن است به 450 ميلي‌گرم هر 12 ساعت به خوبي پاسخ‌ دهند. حداكثر مقدار مصرف mg/day 1200 در صورت مصرف هر 8 ساعت يا 900 ميلي‌گرم در صورت مصرف هر 12 ساعت مي‌باشد.


نوروپاتي ديابتي


بزرگسالان: ابتدا مقدار mg/day 150 خوراکي به مدت سه روز، سپس mg/day 300 به مدت سه روز و به دنبال آن mg/kg/day 10 مصرف‌ مي‌شود.

موارد منع مصرف

موارد منع مصرف و احتياط


موارد منع مصرف: شوك كارديوژنيك يا وجود بلوك درجه دوم يا سوم AV در غياب يك ضربان‌ساز مصنوعي.


موارد احتياط: نارسايي کبدي بويژه اگر ثانويه به نارسايي قلبي باشد، كمي فشارخون، CHF، بلوك قلبي درجه اول، ضربان‌ساز بطني، سابقه اختلال عملكرد گره سينوسي، اختلالات تشنجي.

عوارض جانبی دارو

عوارض جانبي


اعصاب مرکزي: ترمور، سرگيجه، تاري ديد، دوبيني، اغتشاش شعور، منگي، عدم هماهنگي اندامها، تغيير در عادت خواب، پارستزي، ضعف، خستگي، اشكال در تكلم، وزوز گوش، افسردگي، عصبانيت، سردرد.


قلبي ـ عروقي: آريتمي جديد يا تشديد آريتمي قلبي، تپش قلب، درد قفسة سينه، ادم غير اختصاصي، آنژين.


دستگاه گوارش: تهوع، استفراغ، ناراحتي بخش فوقاني دستگاه گوارش، سوزش سردل، اسهال، يبوست، خشكي دهان، تغيير اشتها، درد شكم.


پوست: بثورات پوستي.


مسموميت و درمان


تظاهرات باليني: اثرات باليني عمدتاً به صورت افزايش ميزان عوارض CNS دارو است. وخيمترين عارضه، حملات تشنجي مي‌باشد.


درمان: معمولاً علامتي و حمايتي است. هنگام مصرف بيش از حد حاد، بيمار را بايد وادار به استفراغ كرد يا لاواژ معده انجام داد. اسيدي كردن ادرار ممكن است دفع دارو را سرعت بخشد. در صورت بروز براديكاردي و كمي فشارخون مي‌توان آتروپين تجويز كرد.

موارد قابل توجه

-

تداخل دارویی

تداخل دارويي


مصرف همزمان با داروهاي تغيير دهنده زمان تخليه معده (مانند داروهاي مخدر، ضد اسيدهاي حاوي آلومينيم يا هيدروكسيد منيزيم، و آتروپين) ممكن است جذب مگزيلتين را به تأخير اندازد. دوز داروها از يکديگر جدا شوند.


مصرف همزمان با متوكلوپراميد ممكن است جذب متوکلوپراميد را افزايش دهد.


مصرف همزمان با داروهاي تغيير دهنده عملكرد آنزيم كبدي (مانند ريفامپين، فنوباربيتال، و فني‌توئين) ممكن است متابوليسم كبدي مگزيلتين را برانگيخته و سبب كاهش غلظت سرمي دارو شوند.


مصرف همزمان با سايمتيدين ممكن است متابوليسم مگزيلتين را كاهش يا افزايش داده و به تغيير غلظت سرمي آن منجر شود.


مصرف همزمان با داروهايي كه ادرار را اسيدي مي‌كنند (مانند كلرور آمونيم) دفع مگزيلتين را افزايش مي‌دهد.


مصرف همزمان با داروهايي كه PH ادرار را افزايش مي‌دهند(مانند مقدار زياد ضد اسيدها، مهاركننده‌هاي كربنيك انيدراز، و بيكربنات سديم).دفع مگزيلتين را كاهش مي‌دهد.


در صورت مصرف همزمان با تئوفيلين، مگزيلتين ممكن است غلظت سرمي تئوفيلين را افزايش دهد.


تداخل دارو ـ غذا: مصرف همزمان با کافئين ممکن است متابوليسم کافئين را تا 50% کاهش دهد. بيمار بايد از مصرف زياد کافئين خودداري کند.


تداخل دارو ـ روش زندگي: مصرف همزمان با سيگار ممکن است کارايي مگزيلتين را کاهش دهد. از مصرف سيگار خودداري شود.

مکانیزم اثر

تداخل دارويي


مصرف همزمان با داروهاي تغيير دهنده زمان تخليه معده (مانند داروهاي مخدر، ضد اسيدهاي حاوي آلومينيم يا هيدروكسيد منيزيم، و آتروپين) ممكن است جذب مگزيلتين را به تأخير اندازد. دوز داروها از يکديگر جدا شوند.


مصرف همزمان با متوكلوپراميد ممكن است جذب متوکلوپراميد را افزايش دهد.


مصرف همزمان با داروهاي تغيير دهنده عملكرد آنزيم كبدي (مانند ريفامپين، فنوباربيتال، و فني‌توئين) ممكن است متابوليسم كبدي مگزيلتين را برانگيخته و سبب كاهش غلظت سرمي دارو شوند.


مصرف همزمان با سايمتيدين ممكن است متابوليسم مگزيلتين را كاهش يا افزايش داده و به تغيير غلظت سرمي آن منجر شود.


مصرف همزمان با داروهايي كه ادرار را اسيدي مي‌كنند (مانند كلرور آمونيم) دفع مگزيلتين را افزايش مي‌دهد.


مصرف همزمان با داروهايي كه PH ادرار را افزايش مي‌دهند(مانند مقدار زياد ضد اسيدها، مهاركننده‌هاي كربنيك انيدراز، و بيكربنات سديم).دفع مگزيلتين را كاهش مي‌دهد.


در صورت مصرف همزمان با تئوفيلين، مگزيلتين ممكن است غلظت سرمي تئوفيلين را افزايش دهد.


تداخل دارو ـ غذا: مصرف همزمان با کافئين ممکن است متابوليسم کافئين را تا 50% کاهش دهد. بيمار بايد از مصرف زياد کافئين خودداري کند.


تداخل دارو ـ روش زندگي: مصرف همزمان با سيگار ممکن است کارايي مگزيلتين را کاهش دهد. از مصرف سيگار خودداري شود.

فارماكوكینتیك

فارماكوكينتيك


جذب: حدود 90 درصد دارو ازدستگاه گوارش جذب مي‌شود. سرعت جذب در حالاتي كه تخليه معده را تسريع مي‌كنند، كاهش مي‌يابد.


پخش: به طور گسترده در سرتاسر بدن انتشار مي‌يابد. حدود 60-50 درصد به پروتئين‌هاي پلاسما پيوند مي‌يابد. غلظت معمول درماني mcg/ml 2-5/0 است. اگرچه مسموميت ممكن است در همين محدوده درماني عارض شود، ولي غلظت بالاي mcg/ml 2 سمي درنظر گرفته شده است كه با افزايش شيوع عوارض CNS همراه است، و در اين صورت مقدار مصرف بايد كاهش يابد.


متابوليسم: در كبد به متابوليت‌هاي نسبتاً غيرفعال متابوليزه مي‌شود. متابوليسم تحت تأثير جريان خون كبدي قرار مي‌گيرد که ممكن است در دوران نقاهت انفاركتوس ميوكارد و در CHF كاهش يابد. بيماري كبدي نيز متابوليسم را محدود مي‌كند.


دفع: در بيماران سالم، نيمه‌ عمر دارو 12-10 ساعت است. نيمه‌ عمر دفع ممكن است در CHF يا بيماري كبدي طولاني شود. حدود 10% به صورت داروي تغيير نيافته در ادرار ترشح مي‌شود. دفع ادراري با اسيدي كردن ادرار افزايش و با افزايش PH ادرار كاهش مي‌يابد.





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روش مصرف




شروع اثر




پيک اثر




مدت اثر




خوراکي




5/0 تا 2 ساعت




2 تا 3 ساعت




نامشخص


سایر اطلاعات

طبقه‌بندي فارماكولوژيك:آنتاگونيست كانال سديم، آنالوگ ليدوكائين.


طبقه‌بندي درماني: ضد آريتمي بطني.


طبقه‌بندي مصرف در بارداري: رده C


ملاحظات اختصاصي


1- در صورت امكان، دارو با غذا مصرف شود.


2- به دليل اثرات آريتمي‌زا، دارو به طور كلي براي آريتمي‌هاي بي‌خطر توصيه نمي‌شود.


3- در صورت تغيير دارو از ليدوكائين به مگزيلتين، به هنگام تجويز اولين مقدار مگزيلتين بايد انفوزيون متوقف شود، با اين وجود، تا كنترل مطلوب آريتمي خط انفوزيون بايد باز باشد.


4- بيماراني كه به رژيم درماني هر هشت ساعت پاسخ نمي‌دهند، ممكن است به رژيم درماني هر شش ساعت پاسخ دهند.


5- بسياري از بيماراني را كه به رژيم درماني 300 ميلي‌گرم يا كمتر در هر 8 ساعت به‌خوبي پاسخ مي‌دهند، مي‌توان روي رژيم درماني هر 12 ساعت گذاشت (همان مقدار مصرف در دو مقدار منقسم). اين امر به همكاري بيمار مي‌افزايد.


6- رعشه (معمولاً رعشه خفيف دست) در بيماراني شايع است كه مقادير زياد مگزيلتين مصرف مي‌كنند.


7- در صورت تغيير دارو از يک آنتي آريتمي ديگر خوراکي کلاس I، مگزيلتين با دوز 200 ميلي‌گرم 6 تا 12 ساعت پس از آخرين دوز کينيدين، 3 تا 6 ساعت پس از آخرين دوز پروکائيناميد، 6 تا 12 ساعت پس از آخرين دوز ديسوپيراميد و 8 تا 12 ساعت پس از آخرين دوز توکائينايد شروع مي‌شود.


نكات قابل توصيه به بيمار


به جهت کمتر شدن ميزان تهوع، دارو با غذا مصرف شود.


كبودي ياخونريزي غيرعادي، علائم عفونت (تب، گلودرد، استوماتيت، يا لرز) يا خستگي را اطلاع دهيد.


مصرف در سالمندان: به دليل كاهش جريان خون كبدي و در نتيجه كاهش متابوليسم، مقدار مصرف در اكثر سالخوردگان بايد كاهش يابد. بيماران سالخورده ممكن است نسبت به عوارض جانبي CNS دارو نيز مستعدتر باشند.


مصرف در شيردهي: مگزيلتين در شير ترشح مي‌شود. شيردهي در دوران مصرف اين دارو توصيه نمي‌شود.


اثر بر آزمايشهاي تشخيصي


ممکن است سطح AST افزايش يابد.

Mexiletine HCl (Mexitil)

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

MEXITIL
(mexiletine hydrochloride) Capsule

Capsules of 150 mg, 200 mg and 250 mg

Oral Antiarrhythmic

DRUG DESCRIPTION

MEXITIL® (mexiletine hydrochloride, USP) is an orally active antiarrhythmic agent available as 150 mg, 200 mg and 250 mg capsules. 100 mg of mexiletine hydrochloride is equivalent to 83.31 mg of mexiletine base. It is a white to off-white crystalline powder with slightly bitter taste, freely soluble in water and in alcohol. MEXITIL (mexiletine hcl) has a pKa of 9.2.

Chemically, MEXITIL (mexiletine hcl) is 1-methyl-2-(2, 6-xylyloxy) ethylamine hydrochloride and has the following structural formula:

MEXITIL - mexiletine hydrochloride capsule  Structural Formula Illustration

MEXITIL (mexiletine hcl) capsules contain the following excipients: colloidal silicon dioxide, corn starch, magnesium stearate, titanium dioxide, gelatin, pharmaceutical glaze, simethicone, FD&C Red No. 40, and FD&C Blue No. 1; the MEXITIL (mexiletine hcl) 150 mg and 250 mg capsules also contain FD&C Yellow No. 10 and D&C Red No. 28. MEXITIL (mexiletine hcl) capsules may contain one or more of the following components: sodium lauryl sulfate, lecithin, shellac, and FD&C Blue No. 1 Aluminum Lake.

What are the possible side effects of mexiletine (Mexitil)?

If you experience any of the following serious side effects, stop taking mexiletine and seek emergency medical attention:

  • an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives);
  • a new or a worsening irregular heartbeat pattern;
  • wheezing, coughing, chest pain, or chest discomfort;
  • unusual bruising or bleeding; or
  • fever, sore throat, a sore mouth, mouth ulcers, or an infection.

Other, less serious side effects may be more likely to occur. Continue to take mexiletine and talk to...

Read All Potential Side Effects and See Pictures of Mexitil »

What are the precautions when taking mexiletine hcl (Mexitil)?

Before taking mexiletine, tell your doctor or pharmacist if you are allergic to it; 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: other heart problems (such as heart failure, slow heartbeat, previous heart attack), liver problems, seizure disorder.

This drug may make you dizzy or cause blurred vision. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.

During pregnancy, this medication should be used only when clearly...

Read All Potential Precautions of Mexitil »

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

INDICATIONS

MEXITIL (mexiletine hydrochloride, USP) is indicated for the treatment of documented ventricular arrhythmias, such as sustained ventricular tachycardia, that, in the judgement of the physician, are life-threatening. Because of the proarrhythmic effects of MEXITIL (mexiletine hcl) , its use with lesser arrhythmias is generally not recommended. Treatment of patients with asymptomatic ventricular premature contractions should be avoided.

Initiation of MEXITIL (mexiletine hcl) treatment, as with other antiarrhythmic agents used to treat life-threatening arrhythmias, should be carried out in the hospital.

Antiarrhythmic drugs have not been shown to enhance survival in patients with ventricular arrhythmias.

DOSAGE AND ADMINISTRATION

The dosage of MEXITIL (mexiletine hydrochloride, USP) must be individualized on the basis of response and tolerance, both of which are dose-related. Administration with food or antacid is recommended. Initiate MEXITIL (mexiletine hcl) therapy with 200 mg every eight hours when rapid control of arrhythmia is not essential. A minimum of two to three days between dose adjustments is recommended. Dose may be adjusted in 50 or 100 mg increments up or down.

As with any antiarrhythmic drug, clinical and electrocardiographic evaluation (including Holter monitoring if necessary for evaluation) are needed to determine whether the desired antiarrhythmic effect has been obtained and to guide titration and dose adjustment.

Satisfactory control can be achieved in most patients by 200 to 300 mg given every eight hours with food or antacid. If satisfactory response has not been achieved at 300 mg q8h, and the patient tolerates MEXITIL (mexiletine hcl) well, a dose of 400 mg q8h may be tried. As the severity of CNS side effects increases with total daily dose, the dose should not exceed 1200 mg/day.

In general, patients with renal failure will require the usual doses of MEXITIL (mexiletine hcl) . Patients with severe liver disease, however, may require lower doses and must be monitored closely. Similarly, marked right-sided congestive heart failure can reduce hepatic metabolism and reduce the needed dose. Plasma level may also be affected by certain concomitant drugs (see PRECAUTIONS: DRUG INTERACTIONS).

Loading Dose

When rapid control of ventricular arrhythmia is essential, an initial loading dose of 400 mg of MEXITIL (mexiletine hcl) may be administered, followed by a 200 mg dose in eight hours. Onset of therapeutic effect is usually observed within 30 minutes to two hours.

Q12H Dosage Schedule

Some patients responding to MEXITIL (mexiletine hcl) may be transferred to a 12-hour dosage schedule to improve convenience and compliance. If adequate suppression is achieved on a MEXITIL (mexiletine hcl) dose of 300 mg or less every eight hours, the same total daily dose may be given in divided doses every 12 hours while carefully monitoring the degree of suppression of ventricular ectopy. This dose may be adjusted up to a maximum of 450 mg every 12 hours to achieve the desired response.

Transferring to Mexitil (mexiletine hcl)

The following dosage schedule, based on theoretical considerations rather than experimental data, is suggested for transferring patients from other Class I oral antiarrhythmic agents to MEXITIL (mexiletine hcl) : MEXITIL (mexiletine hcl) treatment may be initiated with a 200 mg dose, and titrated to response as described above, 6-12 hours after the last dose of quinidine sulfate, 3-6 hours after the last dose of procainamide, 6-12 hours after the last dose of disopyramide or 8-12 hours after the last dose of tocainide.

In patients in whom withdrawal of the previous antiarrhythmic agent is likely to produce life-threatening arrhythmias, hospitalization of the patient is recommended.

When transferring from lidocaine to MEXITIL (mexiletine hcl) , the lidocaine infusion should be stopped when the first oral dose of MEXITIL (mexiletine hcl) is administered. The infusion line should be left open until suppression of the arrhythmia appears to be satisfactorily maintained.

Consideration should be given to the similarity of the adverse effects of lidocaine and MEXITIL (mexiletine hcl) and the possibility that they may be additive.

HOW SUPPLIED

MEXITIL (mexiletine hydrochloride, USP) is supplied in bottles of 100 hard gelatin capsules containing 150 mg, 200 mg or 250 mg of mexiletine hydrochloride:

MEXITIL (mexiletine hcl) 150 mg capsules are red and caramel with the marking Bl 66 (NDC 0597-0066-01).

MEXITIL (mexiletine hcl) 200 mg capsules are red with the marking Bl 67 (NDC 0597-0067-01).

MEXITIL (mexiletine hcl) 250 mg capsules are red and aqua green with the marking Bl 68 (NDC 0597-0068-01).

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

Distributed by: Boehringer Ingelheim Pharmaceuticals, Inc. Ridgefield, Connecticut 06877 USA. Rev: 05/30/03

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

SIDE EFFECTS

MEXITIL (mexiletine hydrochloride, USP) commonly produces reversible gastrointestinal and nervous system adverse reactions but is otherwise well tolerated. MEXITIL (mexiletine hcl) has been evaluated in 483 patients in one-month and three-month controlled studies and in over 10,000 patients in a large compassionate use program. Dosages in the controlled studies ranged from 600-1200 mg/day; some patients (8%) in the compassionate use program were treated with higher daily doses (1600-3200 mg/day). In the three-month controlled trials comparing MEXITIL (mexiletine hcl) to quinidine, procainamide and disopyramide, the most frequent adverse reactions were upper gastrointestinal distress (41%), lightheadedness (10.5%), tremor (12.6%) and coordination difficulties (10.2%). Similar frequency and incidence were observed in the one-month placebo-controlled trial. Although these reactions were generally not serious, and were dose-related and reversible with a reduction in dosage, by taking the drug with food or antacid or by therapy discontinuation, they led to therapy discontinuation in 40% of patients in the controlled trials. Table 1 presents the adverse events reported in the one-month placebo-controlled trial.

Table 1 : Comparative Incidence (%) of Adverse Events Among Patients Treated with Mexiletine and Placebo in the 4- Week, Double-blind Crossover Trial

  Mexiletine
N=53
Placebo
N=49
Cardiovascular
  Palpitations 7.5 10.2
  Chest Pain 7.5 4.1
  Increased Ventricular Arrhythmia /PVC's 1.9 -
Digestive
  Nausea/Vomiting/Heartburn 39.6 6.1
Central Nervous System
  Dizziness/ 26.4 14.3
Lightheadedness
  Tremor 13.2
  Nervousness 11.3 6.1
  Coordination Difficulties 9.4
  Changes in Sleep Habits 7.5 16.3
  Paresthesias/Numbness 3.8 2.0
  Weakness 1.9 4.1
  Fatigue 1.9 2.0
  Tinnitus 1.9 4.1
  Confusion/Clouded Sensorium 1.9 2.0
Other
  Headache 7.5 6.1
  Blurred Vision/Visual Disturbances 7.5 2.0
  Dyspnea/Respiratory 5.7 10.2
  Rash 3.8 2.0
  Non-specific Edema 3.8

Table 2 presents the adverse reactions occurring in one percent or more of patients in the three-month controlled studies.

Table 2: Comparative Incidence (%) of Adverse Events Among Patients Treated with Mexiletine or Control Drugs in the 12-Week Double-blind Trials

  Mexiletine
N = 430
Quinidine
N = 262
Procainamide
N = 78
Cardiovascular
  Palpitations 4.3 4.6 1.3
  Chest Pain 2.6 3.4 1.3
  Angina/Angina-like Pain 1.7 1.9 2.6
  Increased Ventricular Arrhythmias/PVC's 1.0 2.7 2.6
Digestive
  Nausea/Vomiting/Heartburn 39.3 21.4 33.3
  Diarrhea 5.2 33.2 2.6
  Constipation 4.0 6.4
  Changes in Appetite 2.6 1.9
  Abdominal Pain/Cramps/Discomfort 1.2 1.5
Central Nervous System
  Dizziness/Lightheadedness 18.9 14.1 14.1
  Tremor 13.2 2.3 3.8
  Coordination Difficulties 9.7 1.1 1.3
  Changes in Sleep Habits 7.1 2.7 11.5
  Weakness 5.0 5.3 7.7
  Nervousness 5.0 1.9 6.4
  Fatigue 3.8 5.7 5.1
  Speech Difficulties 2.6 0.4
  Confusion/Clouded Sensorium 2.6 3.8
  Paresthesias/Numbness 2.4 2.3 2.6
  Tinnitus 2.4 1.5
  Depression 2.4 1.1 1.3
Other
  Blurred Vision/Visual Disturbances 5.7 3.1 5.1
  Headache 5.7 6.9 7.7
  Rash 4.2 3.8 10.3
  Dyspnea/ Respiratory 3.3 3.1 5.1
  Dry Mouth 2.8 1.9 5.1
  Arthralgia 1.7 2.3 5.1
  Fever 1.2 3.1 2.6

Less than 1%: Syncope, edema, hot flashes, hypertension, short-term memory loss, loss of consciousness, other psychological changes, diaphoresis, urinary hesitancy/retention, malaise, impotence/decreased libido, pharyngitis, congestive heart failure.

An additional group of over 10,000 patients has been treated in a program allowing administration of MEXITIL (mexiletine hydrochloride, USP) under compassionate use circumstances. These patients were seriously ill with the large majority on multiple drug therapy. Twenty-four percent of the patients continued in the program for one year or longer. Adverse reactions leading to therapy discontinuation occurred in 15 percent of patients (usually upper gastrointestinal system or nervous system effects). In general, the more common adverse reactions were similar to those in the controlled trials. Less common adverse events possibly related to MEXITIL (mexiletine hcl) use include:

Cardiovascular System: Syncope and hypotension, each about 6 in 1000; bradycardia, about 4 in 1000; angina/angina-like pain, about 3 in 1000; edema, atrioventricular block/conduction disturbances and hot flashes, each about 2 in 1000; atrial arrhythmias, hypertension and cardiogenic shock, each about 1 in 1000.

Central Nervous System: Short-term memory loss, about 9 in 1000 patients; hallucinations and other psychological changes, each about 3 in 1000; psychosis and convulsions/seizures, each about 2 in 1000; loss of consciousness, about 6 in 10,000.

Digestive: Dysphagia, about 2 in 1000; peptic ulcer, about 8 in 10,000; upper gastrointestinal bleeding, about 7 in 10,000; esophageal ulceration, about 1 in 10,000. Rare cases of severe hepatitis/acute hepatic necrosis.

Skin: Rare cases of exfoliative dermatitis and Stevens-Johnson Syndrome with MEXITIL (mexiletine hydrochloride, USP) treatment have been reported.

Laboratory:Abnormal liver function tests, about 5 in 1000 patients; positive ANA and thrombocytopenia, each about 2 in 1000; leukopenia (including neutropenia and agranulocytosis), about 1 in 1000; myelofibrosis, about 2 in 10,000 patients.

Other: Diaphoresis, about 6 in 1000; altered taste, about 5 in 1000; salivary changes, hair loss and impotence/decreased libido, each about 4 in 1000; malaise, about 3 in 1000; urinary hesitancy/retention, each about 2 in 1000; hiccups, dry skin, laryngeal and pharyngeal changes and changes in oral mucous membranes, each about 1 in 1000; SLE syndrome, about 4 in 10,000.

Hematology

Blood dyscrasias were not seen in the controlled trials but did occur among 10,867 patients treated with mexiletine in the compassionate use program (see PRECAUTIONS).

Myelofibrosis was reported in two patients in the compassionate use program: one was receiving long-term thiotepa therapy and the other had pretreatment myeloid abnormalities.

In post-marketing experience, there have been isolated, spontaneous reports of pulmonary changes including pulmonary infiltration and pulmonary fibrosis during MEXITIL (mexiletine hcl) therapy with or without other drugs or diseases that are known to produce pulmonary toxicity. A causal relationship to MEXITIL (mexiletine hcl) therapy has not been established. In addition, there have been isolated reports of drowsiness, nystagmus, ataxia, dyspepsia, hypersensitivity reaction, and exacerbation of congestive heart failure in patients with pre-existing compromised ventricular function. There have been rare reports of pancreatitis associated with MEXITIL (mexiletine hcl) treatment.

Read the Mexitil (mexiletine hcl) Side Effects Center for a complete guide to possible side effects »

DRUG INTERACTIONS

Since MEXITIL (mexiletine hcl) is a substrate for the metabolic pathways involving CYP2D6 and CYP1A2 enzymes, inhibition or induction of either of these enzymes would be expected to alter mexiletine plasma concentrations. In a formal, single-dose interaction study (n = 6 males) the clearance of mexiletine was decreased by 38% following the coadministration of fluvoxamine, an inhibitor of CYP1A2. In another formal study (n = 8 extensive and n = 7 poor metabolizers of CYP2D6), coadministration of propafenone did not alter the kinetics of mexiletine in the poor CYP2D6 metabolizer group. However, the metabolic clearance of mexiletine in the extensive metabolizer phenotype decreased by about 70% making the poor and extensive metabolizer groups indistinguishable. In this crossover steady state study, the pharmacokinetics of propafenone were unaffected in either phenotype by the coadministration of mexiletine. Addition of mexiletine to propafenone did not lead to further electrocardiographic parameters changes of QRS, QTc, RR, and PR intervals than propafenone alone. When concomitant administration of either of these two drugs with mexiletine is initiated, the dose of mexiletine should be slowly titrated to desired effect.

In a large compassionate use program MEXITIL (mexiletine hcl) has been used concurrently with commonly employed antianginal, antihypertensive, and anticoagulant drugs without observed interactions. A variety of antiarrhythmics such as quinidine or propranolol were also added, sometimes with improved control of ventricular ectopy. When phenytoin or other hepatic enzyme inducers such as rifampin and phenobarbital have been taken concurrently with MEXITIL (mexiletine hcl) ®, lowered MEXITIL (mexiletine hcl) plasma levels have been reported. Monitoring of MEXITIL (mexiletine hcl) plasma levels is recommended during such concurrent use to avoid ineffective therapy.

In a formal study, benzodiazepines were shown not to affect MEXITIL (mexiletine hcl) plasma concentrations. ECG intervals (PR, QRS, and QT) were not affected by concurrent MEXITIL (mexiletine hcl) and digoxin, diuretics, or propranolol.

Concurrent administration of cimetidine and MEXITIL (mexiletine hcl) has been reported to increase, decrease, or leave unchanged MEXITIL (mexiletine hcl) plasma levels; therefore patients should be followed carefully during concurrent therapy.

MEXITIL (mexiletine hcl) does not alter serum digoxin levels but magnesium-aluminum hydroxide, when used to treat gastrointestinal symptoms due to MEXITIL (mexiletine hydrochloride, USP) Capsules, has been reported to lower serum digoxin levels.

Concurrent use of MEXITIL (mexiletine hcl) and theophylline may lead to increased plasma theophylline levels. One controlled study in eight normal subjects showed a 72% mean increase (range 35-136%) in plasma theophylline levels. This increase was observed at the first test point which was the second day after starting MEXITIL (mexiletine hcl) . Theophylline plasma levels returned to pre- MEXITIL (mexiletine hcl) values within 48 hours after discontinuing MEXITIL (mexiletine hcl) . If MEXITIL (mexiletine hcl) and theophylline are to be used concurrently, theophylline blood levels should be monitored, particularly when the MEXITIL (mexiletine hcl) dose is changed. An appropriate adjustment in theophylline dose should be considered.

Additionally, in one controlled study in five normal subjects and seven patients, the clearance of caffeine was decreased 50% following the administration of MEXITIL (mexiletine hcl) .

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
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WARNINGS

Mortality: In the National Heart, Lung and Blood Institute's Cardiac Arrhythmia Suppression Trial (CAST), a long-term, multicentered, randomized, double-blind study in patients with asymptomatic non-life-threatening ventricular arrhythmias who had a myocardial infarction more than six days but less than two years previously, an excessive mortality or non-fatal cardiac arrest rate (7.7%) was seen in patients treated with encainide or flecainide compared with that seen in patients assigned to carefully matched placebo-treated groups (3.0%). The average duration of treatment with encainide or flecainide in this study was ten months.

The applicability of the CAST results to other populations (e.g., those without recent myocardial infarction) is uncertain. Considering the known proarrhythmic properties of MEXITIL (mexiletine hcl) and the lack of evidence of improved survival for any antiarrhythmic drug in patients without life-threatening arrhythmias, the use of MEXITIL (mexiletine hcl) as well as other antiarrhythmic agents should be reserved for patients with life-threatening ventricular arrhythmia.

Acute Liver Injury

In post-marketing experience abnormal liver function tests have been reported, some in the first few weeks of therapy with MEXITIL (mexiletine hydrochloride, USP). Most of these have been observed in the setting of congestive heart failure or ischemia and their relationship to MEXITIL (mexiletine hcl) has not been established.

PRECAUTIONS

General

If a ventricular pacemaker is operative, patients with second or third degree heart block may be treated with MEXITIL (mexiletine hydrochloride, USP) if continuously monitored. A limited number of patients (45 of 475 in controlled clinical trials) with pre-existing first degree AV block were treated with MEXITIL (mexiletine hcl) ; none of these patients developed second or third degree AV block. Caution should be exercised when it is used in such patients or in patients with pre-existing sinus node dysfunction or intraventricular conduction abnormalities.

Like other antiarrhythmics MEXITIL (mexiletine hydrochloride, USP) can cause worsening of arrhythmias. This has been uncommon in patients with less serious arrhythmias (frequent premature beats or non-sustained ventricular tachycardia: see ADVERSE REACTIONS), but is of greater concern in patients with life-threatening arrhythmias such as sustained ventricular tachycardia. In patients with such arrhythmias subjected to programmed electrical stimulation or to exercise provocation, 10-15% of patients had exacerbation of the arrhythmia, a rate not greater than that of other agents.

MEXITIL (mexiletine hcl) should be used with caution in patients with hypotension and severe congestive heart failure because of the potential for aggravating these conditions.

Since MEXITIL (mexiletine hcl) is metabolized in the liver, and hepatic impairment has been reported to prolong the elimination half-life of MEXITIL (mexiletine hcl) , patients with liver disease should be followed carefully while receiving MEXITIL (mexiletine hcl) . The same caution should be observed in patients with hepatic dysfunction secondary to congestive heart failure.

Concurrent drug therapy or dietary regimens which may markedly alter urinary pH should be avoided during MEXITIL (mexiletine hcl) therapy. The minor fluctuations in urinary pH associated with normal diet do not affect the excretion of MEXITIL (mexiletine hcl) .

SGOT Elevation and Liver Injury

In three-month controlled trials, elevations of SGOT greater than three times the upper limit of normal occurred in about 1% of both mexiletine-treated and control patients. Approximately 2% of patients in the mexiletine compassionate use program had elevations of SGOT greater than or equal to three times the upper limit of normal. These elevations frequently occurred in association with identifiable clinical events and therapeutic measures such as congestive heart failure, acute myocardial infarction, blood transfusions and other medications. These elevations were often asymptomatic and transient, usually not associated with elevated bilirubin levels and usually did not require discontinuation of therapy. Marked elevations of SGOT ( > 1000 U/L) were seen before death in four patients with end-stage cardiac disease (severe congestive heart failure, cardiogenic shock).

Rare instances of severe liver injury, including hepatic necrosis, have been reported in association with MEXITIL (mexiletine hcl) treatment. It is recommended that patients in whom an abnormal liver test has occurred, or who have signs or symptoms suggesting liver dysfunction, be carefully evaluated. If persistent or worsening elevation of hepatic enzymes is detected, consideration should be given to discontinuing therapy.

Blood Dyscrasias

Among 10,867 patients treated with mexiletine in the compassionate use program, marked leukopenia (neutrophils less than 1000/mm3) or agranulocytosis were seen in 0.06% and milder depressions of leukocytes were seen in 0.08%, and thrombocytopenia was observed in 0.16%. Many of these patients were seriously ill and receiving concomitant medications with known hematologic adverse effects. Rechallenge with mexiletine in several cases was negative. Marked leukopenia or agranulocytosis did not occur in any patient receiving MEXITIL (mexiletine hcl) alone; five of the six cases of agranulocytosis were associated with procainamide (sustained release preparations in four) and one with vinblastine. If significant hematologic changes are observed, the patient should be carefully evaluated, and, if warranted, MEXITIL (mexiletine hcl) should be discontinued. Blood counts usually return to normal within one month of discontinuation. (See ADVERSE REACTIONS).

Convulsions (seizures) did not occur in MEXITIL (mexiletine hcl) controlled clinical trials. In the compassionate use program, convulsions were reported in about 2 of 1000 patients. Twenty-eight percent of these patients discontinued therapy. Convulsions were reported in patients with and without a prior history of seizures. Mexiletine should be used with caution in patients with known seizure disorder.

Carcinogenesis, Mutagenesis and Impairment of Fertility

Studies of carcinogenesis in rats (24 months) and mice (18 months) did not demonstrate any tumorigenic potential. MEXITIL (mexiletine hcl) was found to be non-mutagenic in the Ames test. MEXITIL (mexiletine hcl) did not impair fertility in the rat.

Pregnancy

Teratogenic Effects

Pregnancy Category C

Reproduction studies performed with MEXITIL (mexiletine hydrochloride, USP) in rats, mice and rabbits at doses up to four times the maximum human oral dose (24 mg/kg in a 50 kg patient) revealed no evidence of teratogenicity or impaired fertility but did show an increase in fetal resorption. There are no adequate and well-controlled studies in pregnant women; this drug should be used in pregnancy only if the potential benefit justifies the potential risk to the fetus.

Nursing Mothers

MEXITIL (mexiletine hcl) appears in human milk in concentrations similar to those observed in plasma. Therefore, if the use of MEXITIL (mexiletine hcl) is deemed essential, an alternative method of infant feeding should be considered.

Pediatric Use

Safety and effectiveness in the pediatric population have not been established.

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

OVERDOSE

Clinical findings associated with MEXITIL (mexiletine hydrochloride, USP) overdosage have included drowsiness, confusion, nausea, hypotension, sinus bradycardia, paresthesia, seizures, bundle branch block, AV heart block, asystole, ventricular tachyarrhythmia, including ventricular fibrillation, cardiovascular collapse and coma. The lowest known dose in a fatality case was 4.4g with postmortem serum mexiletine level of 34-37 mcg/ml (Jequier P. et al. Lancet 1976: 1 (7956): 429). Patients have recovered from ingestion of 4g to 18g of mexiletine (Frank S. E. et al. Am J Emerg Med 1991: 9:43-48).

There is no specific antidote for MEXITIL (mexiletine hcl) . Management of MEXITIL (mexiletine hcl) overdosage includes general supportive measures, close observation and monitoring of vital signs. In addition, the use of pharmacologic interventions (e.g., pressor agents, atropine or anticonvulsants) or transvenous cardiac pacing is suggested, depending on the patient's clinical condition.

CONTRAINDICATIONS

MEXITIL (mexiletine hydrochloride, USP) is contraindicated in the presence of cardiogenic shock or pre-existing second- or third-degree AV block (if no pacemaker is present).

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

CLINICAL PHARMACOLOGY

Mechanism of Action

MEXITIL (mexiletine hydrochloride, USP) is a local anesthetic, antiarrhythmic agent, structurally similar to lidocaine, but orally active. In animal studies, MEXITIL (mexiletine hcl) has been shown to be effective in the suppression of induced ventricular arrhythmias, including those induced by glycoside toxicity and coronary artery ligation. MEXITIL (mexiletine hcl) , like lidocaine, inhibits the inward sodium current, thus reducing the rate of rise of the action potential, Phase 0. MEXITIL (mexiletine hcl) decreased the effective refractory period (ERP) in Purkinje fibers. The decrease in ERP was of lesser magnitude than the decrease in action potential duration (APD), with a resulting increase in the ERP/APD ratio.

Electrophysiology in Man

Mexiletine is a Class 1B antiarrhythmic compound with electrophysiologic properties in man similar to lidocaine, but dissimilar from quinidine, procainamide, and disopyramide.

In patients with normal conduction systems, MEXITIL (mexiletine hcl) has a minimal effect on cardiac impulse generation and propagation. In clinical trials, no development of second-degree or third-degree AV block was observed. MEXITIL (mexiletine hcl) did not prolong ventricular depolarization (QRS duration) or repolarization (QT intervals) as measured by electrocardiography. Theoretically, therefore, MEXITIL (mexiletine hcl) may be useful in the treatment of ventricular arrhythmias associated with a prolonged QT interval.

In patients with pre-existing conduction defects, depression of the sinus rate, prolongation of sinus node recovery time, decreased conduction velocity and increased effective refractory period of the intraventricular conduction system have occasionally been observed.

The antiarrhythmic effect of MEXITIL (mexiletine hcl) has been established in controlled comparative trials against placebo, quinidine, procainamide and disopyramide. MEXITIL (mexiletine hcl) , at doses of 200-400 mg q8h, produced a significant reduction of ventricular premature beats, paired beats, and episodes of non-sustained ventricular tachycardia compared to placebo and was similar in effectiveness to the active agents. Among all patients entered into the studies, about 30% in each treatment group had a 70% or greater reduction in PVC count and about 40% failed to complete the 3 month studies because of adverse effects. Follow-up of patients from the controlled trials has demonstrated continued effectiveness of MEXITIL (mexiletine hcl) in long-term use.

Hemodynamics

Hemodynamic studies in a limited number of patients, with normal or abnormal myocardial function, following oral administration of MEXITIL (mexiletine hcl) , have shown small, usually not statistically significant, decreases in cardiac output and increases in systemic vascular resistance, but no significant negative inotropic effect. Blood pressure and pulse rate remain essentially unchanged. Mild depression of myocardial function, similar to that produced by lidocaine, has occasionally been observed following intravenous MEXITIL (mexiletine hcl) therapy in patients with cardiac disease.

Pharmacokinetics

MEXITIL (mexiletine hcl) is well absorbed (~90%) from the gastrointestinal tract. Unlike lidocaine, its first-pass metabolism is low. Peak blood levels are reached in two to three hours. In normal subjects, the plasma elimination half-life of MEXITIL (mexiletine hcl) is approximately 10-12 hours. It is 50-60% bound to plasma protein, with a volume of distribution of 5-7 liters/kg. MEXITIL (mexiletine hcl) is mainly metabolized in the liver, the primary pathway being CYP2D6 metabolism, although it is also a substrate for CYP1A2. With involvement of CYP2D6, there can be either poor or extensive metabolizer phenotypes. Since approximately 90% of MEXITIL (mexiletine hcl) is metabolized in the liver into inactive metabolites, pathological changes in the liver can restrict hepatic clearance of MEXITIL (mexiletine hcl) and its metabolites. The metabolic degradation proceeds via various pathways including aromatic and aliphatic hydroxylation, dealkylation, deamination and N-oxidation. Several of the resulting metabolites are submitted to further conjugation with glucuronic acid (phase II metabolism); among these are the major metabolites p-hydroxymexiletine, hydroxy-methylmexiletine and N-hydroxy-mexiletine. Approximately 10% is excreted unchanged by the kidney. While urinary pH does not normally have much influence on elimination, marked changes in urinary pH influence the rate of excretion: acidification accelerates excretion, while alkalinization retards it.

Several metabolites of mexiletine have shown minimal antiarrhythmic activity in animal models. The most active is the minor metabolite N-methylmexiletine, which is less than 20% as potent as mexiletine. The urinary excretion of N-methylmexiletine in man is less than 0.5%. Thus the therapeutic activity of MEXITIL (mexiletine hcl) is due to the parent compound.

Hepatic impairment prolongs the elimination half-life of MEXITIL (mexiletine hcl) . In eight patients with moderate to severe liver disease, the mean half-life was approximately 25 hours.

Consistent with the limited renal elimination of MEXITIL (mexiletine hcl) , little change in the half-life has been detected in patients with reduced renal function. In eight patients with creatinine clearance less than 10 ml/min, the mean plasma elimination half-life was 15.7 hours; in seven patients with creatinine clearance between 11-40 ml/min, the mean half-life was 13.4 hours.

The absorption rate of MEXITIL (mexiletine hcl) is reduced in clinical situations such as acute myocardial infarction in which gastric emptying time is increased. Narcotics, atropine and magnesium-aluminum hydroxide have also been reported to slow the absorption of MEXITIL (mexiletine hcl) . Metoclopramide has been reported to accelerate absorption.

Mexiletine plasma levels of at least 0.5 mcg/ml are generally required for therapeutic response. An increase in the frequency of central nervous system adverse effects has been observed when plasma levels exceed 2.0 mcg/ml. Thus the therapeutic range is approximately 0.5 to 2.0 mcg/ml. Plasma levels within the therapeutic range can be attained with either three times daily or twice daily dosing but peak to trough differences are greater with the latter regimen, creating the possibility of adverse effects at peak and arrhythmic escape at trough. Nevertheless, some patients may be transferred successfully to the twice daily regimen. (See DOSAGE AND ADMINISTRATION).

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

PATIENT INFORMATION

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

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

>

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

PATIENT INFORMATION

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

Last reviewed on RxList: 4/8/2009
This monograph has been modified to include the generic and brand name in many instances.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

Disclaimer

Mexitil 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.

MEXILETINE - ORAL

(mex-IL-e-teen)

COMMON BRAND NAME(S): Mexitil

WARNING: Though this medication often gives great benefits to people with irregular heartbeat, it may infrequently cause a serious new irregular heartbeat. Therefore, when starting treatment with this drug, your doctor may recommend that you stay in the hospital for proper monitoring. Talk with your doctor about the benefits and risks of taking this medication for your condition.

USES: This medication is used to treat certain types of serious (possibly fatal) irregular heartbeat (such as persistent ventricular tachycardia). It is used to restore normal heart rhythm and maintain a regular, steady heartbeat. Mexiletine is known as an anti-arrhythmic drug. It works by blocking certain electrical signals in the heart that can cause an irregular heartbeat. Treating an irregular heartbeat can decrease the risk for blood clots, and this effect can reduce your risk of heart attack or stroke.

OTHER USES: This section contains uses of this drug that are not listed in the approved professional labeling for the drug but that may be prescribed by your health care professional. Use this drug for a condition that is listed in this section only if it has been so prescribed by your health care professional.

This drug may also be used to treat pain, numbness, and tingling from a certain nerve problem (peripheral neuropathy) which may occur in people with diabetes.

HOW TO USE: Take this medication by mouth with a full glass of water (8 ounces/240 milliliters and food or an antacid, usually 2 to 3 times daily or exactly as directed by your doctor. Taking this medication with food or an antacid helps to decrease certain side effects (nausea, heartburn). Ask your pharmacist if you have questions about which antacids to use with this medication.

Dosage is based on your age, liver function, medical condition, and response to treatment.

Use this medication regularly to get the most benefit from it. To help you remember, take it at the same times each day.

Tell your doctor if your condition does not improve or if it worsens.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

Disclaimer

Mexitil Consumer (continued)

SIDE EFFECTS: See also Warning section.

Nausea, vomiting, heartburn, dizziness, lightheadedness, vision problems (such as blurred vision), headache, shaking, nervousness, or problems with muscle control (coordination difficulties) may occur. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

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 rare but serious side effects occur: worsening symptoms of heart failure (such as ankle/leg swelling, increased tiredness, increased shortness of breath when lying down), signs of liver problems (such as persistent nausea/vomiting, stomach/abdominal pain, yellowing eyes/skin, dark urine).

Seek immediate medical attention if any of these rare but very serious side effects occur: chest pain, seizure.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: 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 Mexitil (mexiletine hcl) Side Effects Center for a complete guide to possible side effects »

PRECAUTIONS: Before taking mexiletine, tell your doctor or pharmacist if you are allergic to it; 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: other heart problems (such as heart failure, slow heartbeat, previous heart attack), liver problems, seizure disorder.

This drug may make you dizzy or cause blurred vision. Do not drive, use machinery, or do any activity that requires alertness or clear vision until you are sure you can perform such activities safely. Limit alcoholic beverages.

During pregnancy, this medication should be used only when clearly needed. Discuss the risks and benefits with your doctor.

This medication passes into breast milk. However, this drug is unlikely to harm a nursing infant. Consult your doctor before breast-feeding.

Disclaimer

Mevacor Consumer (continued)

DRUG INTERACTIONS: See also How to Use section.

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Some products that may interact with this drug include: "blood thinners" (such as warfarin), gemfibrozil.

Other medications can affect the removal of lovastatin from your body, which may affect how lovastatin works. Examples include azole antifungals (such as itraconazole, ketoconazole, posaconazole), colchicine, cyclosporine, delavirdine, macrolide antibiotics (such as clarithromycin, erythromycin), nefazodone, HIV protease inhibitors (such as ritonavir), hepatitis C virus protease inhibitors (such as boceprevir, telaprevir), telithromycin, among others.

OVERDOSE: If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call the US National Poison Hotline at 1-800-222-1222. Canada residents can call a provincial poison control center.

NOTES: Do not share this medication with others.

Laboratory and/or medical tests (such as blood cholesterol/triglyceride levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

MISSED DOSE: If you miss a dose, take 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 away from light and moisture. Storage temperature ranges differ according to different manufacturers, so consult your pharmacist for more information. Do not store in the bathroom. 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. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

Information last revised March 2012. Copyright(c) 2012 First Databank, Inc.

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

Mexitil Patient Information Including Side Effects

Brand Names: Mexitil

Generic Name: mexiletine (Pronunciation: mex IL e teen)

What is mexiletine (Mexitil)?

Mexiletine affects the way that your heart beats.

Mexiletine is used to treat seriously irregular heartbeats.

Mexiletine may also be used for purposes other than those listed in this medication guide.

Mexiletine 150 mg-TEV

brown/orange, imprinted with N 739, 150

Mexiletine 200 mg-TEV

orange, imprinted with N 740, 200

Mexiletine 250 mg-TEV

blue/orange, imprinted with N 741, 250

What are the possible side effects of mexiletine (Mexitil)?

If you experience any of the following serious side effects, stop taking mexiletine and seek emergency medical attention:

  • an allergic reaction (difficulty breathing; closing of your throat; swelling of your lips, tongue, or face; or hives);
  • a new or a worsening irregular heartbeat pattern;
  • wheezing, coughing, chest pain, or chest discomfort;
  • unusual bruising or bleeding; or
  • fever, sore throat, a sore mouth, mouth ulcers, or an infection.

Other, less serious side effects may be more likely to occur. Continue to take mexiletine and talk to your doctor if you experience

  • dizziness, lightheadedness, or tiredness;
  • poor coordination;
  • dry mouth;
  • upset stomach, heartburn, vomiting, or decreased appetite;
  • diarrhea or constipation;
  • headache or blurred vision;
  • weakness;
  • numbness, tingling, or tremor (shaking);
  • ringing in your ears;
  • a rash; or
  • depression.

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. You may report side effects to FDA at 1-800-FDA-1088.

Read the Mexitil (mexiletine hcl) Side Effects Center for a complete guide to possible side effects »

What is the most important information I should know about mexiletine (Mexitil)?

Do not skip doses, change your dosing schedule, or stop taking mexiletine without talking to your doctor. Changing your schedule could make your condition much worse.

Use caution when driving, operating machinery, or performing other hazardous activities. Mexiletine may cause dizziness, drowsiness, or blurred vision. If you experience dizziness, drowsiness, or blurred vision, avoid these activities.

Side Effects Centers

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

Mexitil Patient Information including How Should I Take

What should I discuss with my healthcare provider before taking mexiletine (Mexitil)?

Before taking mexiletine, tell your doctor if you have

  • any other type of heart disease or heart problem,
  • liver disease, or
  • seizures or epilepsy.

You may not be able to take mexiletine, or you may require a lower dose or special monitoring during treatment if you have any of the conditions listed above.

Mexiletine is in the FDA pregnancy category C. This means that it is not known whether mexiletine will harm an unborn baby. Do not take this medication without first talking to your doctor if you are pregnant.

Mexiletine passes into breast milk. It is not known whether mexiletine will affect a nursing infant. Do not take this medication without first talking to your doctor if you are breast-feeding a baby.

How should I take mexiletine (Mexitil)?

Take mexiletine exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each dose with a full glass of water.

Also, take mexiletine with food or an antacid to lessen stomach upset.

Do not skip doses, change your dosing schedule, or stop taking mexiletine without talking to your doctor. Changing your schedule could make your condition much worse.

Store mexiletine at room temperature away from moisture and heat.

Side Effects Centers

Discontinued Warning IconPlease Note: This Brand Name drug is no longer available in the US.
(Generic versions may still be available.)

Mexitil Patient Information including If I Miss a Dose

What happens if I miss a dose (Mexitil)?

Try not to miss any doses of this medication. Missing doses could be very dangerous.

If you do miss a dose, take it as soon as you remember. However, if it is almost time for your next dose, skip the missed dose and take only your next regularly scheduled dose. Do not take a double dose of this medication. A double dose could be dangerous.

What happens if I overdose (Mexitil)?

Seek emergency medical attention.

Symptoms of a mexiletine overdose include nausea, seizures, numbness or tingling, tiredness, dizziness, a loss of consciousness, and a worsening irregular heartbeat.

What should I avoid while taking mexiletine (Mexitil)?

Use caution when driving, operating machinery, or performing other hazardous activities. Mexiletine may cause dizziness, drowsiness, or blurred vision. If you experience dizziness, drowsiness, or blurred vision, avoid these activities.

Follow any other special instructions your doctor gives you regarding food, beverages, or activities.

What other drugs will affect mexiletine (Mexitil)?

Before taking mexiletine, tell your doctor if you are taking any of the following medicines:

  • phenytoin (Dilantin), mephenytoin (Mesantoin), or ethotoin (Peganone);
  • rifampin (Rimactane, Rifadin);
  • metoclopramide (Reglan);
  • cimetidine (Tagamet, Tagamet HB); or
  • theophylline (Theo-Dur, Theolair, Elixophyllin, Slo-Phyllin, others).

You may require a dosage adjustment or special monitoring if you are taking any of the medicines listed above.

Drugs other than those listed here may also interact with mexiletine. Talk to your doctor and pharmacist before taking any prescription or over-the-counter medicines.

Where can I get more information?

Your pharmacist can provide more information about mexiletine.


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: 4.02. Revision date: 12/15/2010.

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