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Mexitil (Mexiletine Hydrochloride) - Side Effects and Adverse Reactions

 
 



ADVERSE REACTIONS

MEXITIL (mexiletine hydrochloride, USP) commonly produces reversible gastrointestinal and nervous system adverse reactions but is otherwise well tolerated. MEXITIL 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 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
   Palpitations7.510.2
   Chest Pain7.54.1
   Increased Ventricular
      Arrhythmia /PVC's

1.9

-
Digestive
   Nausea/Vomiting/Heartburn39.66.1
Central Nervous System
   Dizziness/
      Lightheadedness

26.4

14.3
   Tremor13.2
   Nervousness11.36.1
   Coordination Difficulties9.4
   Changes in Sleep Habits7.516.3
   Paresthesias/Numbness3.82.0
   Weakness1.94.1
   Fatigue1.92.0
   Tinnitus1.94.1
   Confusion/Clouded Sensorium1.92.0
Other
   Headache7.56.1
   Blurred Vision/Visual
      Disturbances

7.5

2.0
   Dyspnea/Respiratory5.710.2
   Rash3.82.0
   Non-specific Edema3.8

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 Quinidine Procainamide Disopyramide
N = 430N = 262N = 78N = 69
Cardiovascular
   Palpitations4.34.61.35.8
   Chest Pain2.63.41.32.9
   Angina/Angina-
      like Pain

1.7

1.9

2.6

2.9
   Increased Ventricular
      Arrhythmias/PVC's

1.0

2.7

2.6

Digestive
   Nausea/Vomiting/Heartburn39.321.433.314.5
   Diarrhea5.233.22.68.7
   Constipation4.06.411.6
   Changes in Appetite2.61.9
   Abdominal Pain/Cramps/Discomfort1.21.51.4
Central Nervous System
   Dizziness/Lightheadedness18.914.114.12.9
   Tremor13.22.33.81.4
   Coordination Difficulties9.71.11.3
   Changes in Sleep Habits7.12.711.58.7
   Weakness5.05.37.72.9
   Nervousness5.01.96.45.8
   Fatigue3.85.75.11.4
   Speech Difficulties2.60.4
   Confusion/Clouded Sensorium2.63.8
   Paresthesias/Numbness2.42.32.6
   Tinnitus2.41.5
   Depression2.41.11.31.4
Other
   Blurred Vision/Visual Disturbances5.73.15.17.2
   Headache5.76.97.74.3
   Rash4.23.810.31.4
   Dyspnea/ Respiratory3.33.15.12.9
   Dry Mouth2.81.95.114.5
   Arthralgia1.72.35.11.4
   Fever1.23.12.6

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 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 therapy with or without other drugs or diseases that are known to produce pulmonary toxicity. A causal relationship to MEXITIL 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 treatment.



REPORTS OF SUSPECTED MEXITIL SIDE EFFECTS / ADVERSE REACTIONS

Below is a sample of reports where side effects / adverse reactions may be related to Mexitil. The information is not vetted and should not be considered as verified clinical evidence.

Possible Mexitil side effects / adverse reactions in 60 year old male

Reported by a physician from Japan on 2011-07-15

Patient: 60 year old male weighing 89.0 kg (195.8 pounds)

Reactions: Back Pain, Blood Alkaline Phosphatase Increased, Blood Lactate Dehydrogenase Increased, Alanine Aminotransferase Increased, Liver Disorder, Pruritus Generalised, Malaise, Dyspnoea Exertional, Gamma-Glutamyltransferase Increased, Aspartate Aminotransferase Increased, Cold Sweat, Cough

Adverse event resulted in: hospitalization

Suspect drug(s):
Warfarin Sodium
    Dosage: 4 mg (1 mg,4 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-05-11
    End date: 2011-05-31

Mexitil
    Dosage: 50mg x 6t x 3 (50 mg),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-05-11
    End date: 2011-06-03

Amlodipine Besylate
    Dosage: 5 mg (5 mg,1 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-05-11
    End date: 2011-06-03

Diovan
    Dosage: 160 mg (80 mg,2 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-05-11
    End date: 2011-06-03

Bisoprolol Fumarate
    Dosage: 5 mg (2.5 mg,2 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-06-27
    End date: 2011-06-03

Mecobalamine (Becobalamin)
    Dosage: 550ug x 3t x 3 (500 mcg),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2010-03-03
    End date: 2011-06-03

Epinastine Hydrochloride (Aleroff)
    Dosage: (20 mg,1 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2011-04-14
    End date: 2011-06-03

Doxazosin Mesylate
    Dosage: 4 mg (2 mg,2 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-07-15
    End date: 2011-06-03

Lansoprazole
    Dosage: 15 mg (15 mg,1 in 1 d),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-05-11
    End date: 2011-06-03

Pirmenol Hydrochloride/hydrate (Pimenol)
    Dosage: 50mg x 2capsules x 2 (50 mg),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-05-11
    End date: 2011-06-03

Mosapride Citrate/hydrate (Gasmotin)
    Dosage: 5mg x 3t x 3 (5 mg),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-12-02
    End date: 2011-06-03

Magnesium Oxide (Magmitt)
    Dosage: 250mg x 3t x 3 (250 mg),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2009-07-04
    End date: 2011-05-31

Sairei-TO
    Dosage: 8.1mg x 2t x 2 (8.1 mg),oral
    Administration route: Oral
    Indication: Product Used FOR Unknown Indication
    Start date: 2010-08-05
    End date: 2011-05-30



See index of all Mexitil side effect reports >>

Drug label data at the top of this Page last updated: 2006-02-16

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