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Query: UMLS:C0030193 (pain)
 261,466 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

We examined the effect of mexiletine on the threshold for pain perception as determined by the application of mechanical noxious stimuli (tail-pinch) in diabetic mice. Mexiletine produced a pronounced analgesic effect in diabetic mice in a dose-dependent manner. Mexiletine (10(-5)M) significantly inhibited the K(+)-evoked release of substance P from the slices of spinal cord of diabetic mice. These results suggest that the reduction of release of substance P from the nociceptive afferent terminal in the spinal cord is involved in the mechanisms of mexiletine analgesia in diabetic mice.
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PMID:Antinociceptive effect of mexiletine in diabetic mice. 127 69

Neuropathic pain is often a difficult condition to treat. Clinical and laboratory studies using intravenously administered local anesthetics or antiarrhythmic agents support the use of these drugs for the treatment of neuropathic pain. The availability of the oral antiarrhythmic medication, mexiletine, has made it possible to study the effects of an orally administered medication on chronic neuropathic pain. The study used a double-blind placebo-controlled design to examine 11 subjects in whom treatment with conventional pain medications had been unsuccessful. Subjects had a history of peripheral nerve injury or dysfunction, and all complained of symptoms consistent with neuropathic pain. After baseline pain measurements, mexiletine or placebo was given in gradually increasing doses to a maximum daily dose of 750 mg mexiletine. After 1 month at steady state, the subject received the alternative medication. Mexiletine was found to produce a statistically significant reduction in reported pain when compared to baseline or placebo. Pain scores were rated on a scale from 0 (no pain) to 10 (unbearable pain). Median pain scores prior to mexiletine were 7, after placebo treatment 7, and while receiving mexiletine (750 mg/day) 4. Side effects were mild and well-tolerated. Mexiletine may be effective in reducing neuropathic pain for patients in whom alternative pain medications have been unsatisfactory.
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PMID:The use of oral mexiletine for the treatment of pain after peripheral nerve injury. 131 97

The thalamic pain syndrome, a rare sequelae of cerebrovascular event, is a severe and disabling form of central pain which treatment remains a major clinical problem. We present our results of a preliminary open label study using mexiletine, an orally active antiarrhythmic agent, in the management of thalamic pain in 9 patients. Using a dose of 10 mg/kg/day over a 4-week period, mexiletine produced improvement in pain in 8 of the 9 patients. Mexiletine was generally well tolerated with only two patients experiencing transient nausea and dizziness. Our findings suggest that mexiletine may be a safe and effective agent in the management of thalamic pain and possibly other paroxysmal pain syndromes of central origin.
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PMID:Mexiletine for thalamic pain syndrome. 208 39

We measured the plasma concentrations of mexiletine in patients admitted to a hospital coronary care unit after the intramuscular injection (IMI) of 200, 300, 400, and 500 mg mexiletine. Mexiletine was rapidly absorbed and concentrations greater than 0.75 microgram/ml were achieved in some patients within 5 min of the injection. The maximum mean plasma concentration increased with 200, 300, and 400 mg but was lower after 500 mg than after 400 mg. After 400 mg mexiletine, plasma concentrations greater than 0.75 microgram/ml were achieved in at least seven of nine patients from 15 min to 2 h after administration. There were no local reactions to 200, 300, or 400 mg mexiletine, but local pain and tenderness occurred in three of nine patients after 500 mg. It was decided that 400 mg mexiletine would probably be the desired dose for intramuscular administration. In 14 patients given mexiletine 400 mg by IMI followed at 2 and 12 h by 360 mg by mouth the plasma concentration was in the therapeutic range (0.75-2.0 micrograms/ml) from 15 min to 24 h in at least 64% of patients. In 12 healthy volunteers the IMI of 400 mg mexiletine increased total creatinine kinase (CK), aspartate amino-transferase, and lactate dehydrogenase enzymes but CK-MB, LDi, and LDii concentration or LDi/LDii ratio were not outside the normal range. These studies indicate that mexiletine can be safely given to patients by IMI and that therapeutic plasma concentrations are achieved.
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PMID:Plasma concentrations and acceptability of mexiletine given by intramuscular injection in patients admitted to a coronary care unit. 241 87

The effects of intravenously administered subanesthetic concentrations of lidocaine, tocainide, and mexiletine on spontaneously active fibers (SAFs) originating in 7-day-old rat sciatic neuromas were studied. Control injections of normal saline caused no decrease in SAF or discharge rate. Lidocaine and tocainide given in incremental doses of 5, 10, 15, 20 and up to 25 mg/kg caused nearly all observed SAFs to stop firing. Mexiletine given in doses of 3, 5, 7, 10 and up to 15 mg/kg showed similar results at lower doses. All agents decreased the sensitivity of SAF to mechanical stimulation. No conduction blockade occurred at these doses of intravenously administered local anesthetics. The demonstrated reduction in firing rate of SAF may explain the pain relief observed in clinical trials of these orally available agents.
Pain 1989 Sep
PMID:The effect of intravenous lidocaine, tocainide, and mexiletine on spontaneously active fibers originating in rat sciatic neuromas. 251 Jan 16

Sixteen of nineteen patients completed a randomised double-blind crossover trial to assess the effect of oral mexiletine (10 mg/kg bodyweight daily) on the symptoms and signs of chronic painful diabetic neuropathy. The median age of the sixteen patients was 50 years (range 30-64). Assessment with a five-item clinical symptom scale showed significant improvement during the mexiletine phase compared with the placebo phase. Pain was reduced during mexiletine but not during placebo, as assessed by a visual analogue rating scale. Mexiletine treatment had no effect on tendon reflexes, vibration threshold levels, beat-to-beat variation in heart rate during deep breathing, and postural blood pressure response. Mild side-effects were seen in three of the sixteen patients during mexiletine treatment.
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PMID:Mexiletine for treatment of chronic painful diabetic neuropathy. 289 40

To study the effects of acute myocardial infarction on its pharmacokinetics a single oral dose of 400 mg mexiletine HCl was administered to seven patients. The study was performed within 24 h of the onset of pain (Study I) and was repeated 10-14 days later, during the recovery phase (Study II). Mexiletine in plasma and urine was quantified by a GLC method. The peak plasma concentrations of mexiletine were 0.65 +/- 0.05 (SEM) microgram ml and 1.08 +/- 0.11 micrograms/ml (p less than 0.05) in Studies I and II, respectively. The corresponding peak times were 4.68 +/- 2.04 h and 1.46 +/- 0.17 h (N.S.). The lag time averaged 0.48 +/- 0.08 h in Study I and 0.39 +/- 0.05 h in Study II (N.S.). The area under the plasma concentration-time curve remained unchanged. The elimination half-life was 15.03 +/- 0.61 h and 11.75 +/- 0.80 h (p less than 0.01) in Studies I and II, respectively. The recovery of unchanged mexiletine in urine and its renal clearance was also the same in both studies. The plasma protein binding of mexiletine was similar in Studies I and II (61 +/- 2% and 63 +/- 3%; N.S.). Thus, the rate of gastrointestinal absorption of mexiletine was definitely slowed in the acute phase of myocardial infarction, whereas the extent of absorption was not altered. The prolongation of the elimination half-life of mexiletine in the acute phase of myocardial infarction is probably related to an increase in its volume of distribution.
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PMID:Pharmacokinetics of oral mexiletine in patients with acute myocardial infarction. 666 76

The objective of this double-blind placebo controlled multicenter study was to prove the efficacy of mexiletine in painful diabetic neuropathy. Treatment was provided for in three dosages. For pain measurements a visual analogue scale (VAS) and McGill's verbal rating scale were chosen. 95 patients were included. A global assessment of the VAS showed no differences in treatment. The total evaluation (PRIT = Pain Rating Index Total) of the McGill scale just failed the level of significance. More specific exploratory evaluation of subclasses of the McGill scale, representing different qualities of pain, gave remarkable differences between mexiletine and placebo. According to types of complaints an evaluation showed substantial advantages of the mexiletine treatment with both the VAS and the McGill scale. There is strong evidence that particularly patients with stabbing or burning pain, heat sensations or formication will benefit most by mexiletine therapy. Concerning the dosage, a medium regimen of 450 mg per day seems to be appropriate in this indication. With an increase in dosage the efficacy does not rise proportionally. Mexiletine proved a very safe therapy with negligible side effects at the medium dose range, even less than placebo. There were no cardiovascular side effects. Further investigations should pay more attention to the variety of the complaints and include the quality of life.
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PMID:[Mexiletine in treatment of painful diabetic neuropathy]. 819 72

This article reports a series of 31 patients with true phantom pain. Mexiletine was used in an open-label study to evaluate its effectiveness in the treatment of this disorder. Eighteen of these patients had good to excellent results with mexiletine alone. Eleven other patients responded favorably with a combination of mexiletine and clonidine. Two patients did not respond to either drug alone or in combination. Three patients elected to discontinue use of the mexiletine because of persistent nausea, even at low doses.
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PMID:Successful treatment for phantom pain. 829 Mar 90

Severe pain occurs in 5-30% of the spinal cord-injured (SCI) population and is difficult to treat. Subarachnoid lidocaine has been used in selected patients with some success. Mexiletine, an analog of lidocaine that acts at Na+/K+ channels in the peripheral nerve, has been found effective in persons with diabetic dysesthetic neuropathy. The effect of mexiletine in the treatment of spinal cord dysesthetic pain was examined in this study. Fifteen patients were enrolled, and 11 patients completed the prospective, randomized, placebo-controlled, double-blind, crossover design trial. Inclusion/exclusion criteria were carefully defined. A 1-wk washout period was followed by a 4-wk drug trial of either mexiletine (450 mg/day) or placebo. This was repeated for the second medication in the second arm of the study. Patients were followed weekly with McGill and visual analog pain scales. Baseline, midpoint, and endpoint Barthel function scores were recorded. The Wilcoxon's signed-rank test and paired t test were used for statistical analysis. Results showed no significant effect of mexiletine on SCI dysesthetic pain scales or Barthel index. In conclusion, in this trial, mexiletine did not appear to decrease spinal cord injury-related dysesthetic pain.
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PMID:Effect of mexiletine on spinal cord injury dysesthetic pain. 863 Jan 99


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