Prophylactic tolperisone for post‐exercise muscle soreness causes reduced isometric force—adouble‐blind randomized crossover control study

Abstract

The role of tolperisone hydrochloride, a centrally acting muscle relaxant in relieving painful muscle spasm is recently being discussed. The present study hypothesizes that the prophylactic use of tolperisone hydrochloride may effectively relieve post-exercise muscle soreness, based on the spasm theory of exercise pain. Twenty male volunteers, aged 25.2 +/- 0.82 years (mean +/- SEM) participated in 10 sessions in which they received oral treatment with placebo or the centrally acting muscle relaxant tolperisone hydrochloride (150 mg) three times daily for 8 days, in randomized crossover double-blind design. Time course assessments were made for pressure pain threshold, Likert's pain score (0-5), pain areas, range of abduction, isometric force, and electromyography (EMG) root mean square (RMS) during maximum voluntary isometric force on day 1 and 6, immediately after an eccentric exercise of first dorsal interosseous muscle, and 24 and 48 h after the exercise. Treatment with placebo or tolperisone hydrochloride was initiated immediately after the assessments on the first day baseline assessments. On the sixth day baseline investigations were repeated and then the subjects performed six bouts of standardized intense eccentric exercise of first dorsal interosseous muscle for provocation of post-exercise muscle soreness (PEMS). Perceived intensity of warmth, tiredness, soreness and pain during the exercise bouts were recorded on a 10 cm visual analogue pain scale. VAS scores and pressure pain thresholds did not differ between tolperisone and placebo treatment. All VAS scores increased during the exercise bouts 2, 3, 4, 5 and 6 as compared to bout 1. Increased pain scores and pain areas were reported immediately after, 24 and 48 h after exercise. Pressure pain thresholds were reduced at 24 and 48 h after the exercise in the exercised hand. Range of abduction of the index finger was reduced immediately after the exercise and was still reduced at 24 h as compared to the non-exercised hand. The EMG RMS amplitude was also reduced immediately after the exercise, but was increased at 24 and 48 h. Isometric force was reduced immediately after the exercise as compared to days 1, 6, and the 24 and 48 h post-exercise assessments with a greater reduction following the tolperisone hydrochloride treatment and the reduction was more in tolperisone group as compared to the placebo group. The results suggest, that the prophylactic intake of tolperisone hydrochloride provides no relief to pain in course of post-exercise muscle soreness but results in reduction in isometric force.

Basic Aspects of the Pharmacodynamics of Tolperisone, A Widely Applicable Centrally Acting Muscle Relaxant

“…In a double-blind randomized crossover control study Bajaj et al found that prophylactic intake of tolperisone hydrochloride (150 mg three times daily for 8 days) provides no relief to pain in course of post-exercise muscle soreness but results in reduction in isometric force [7]. …”

Determination of tolperisone in human plasma by liquid chromatography/tandem mass spectrometry for clinical application

“…(2-methyl-1-(4-methylphenyl)-3-(1-piperidyl) propan-1-one) is a centrally acting muscle relaxant that is used for relieving spasticity of neurological origin and muscle spasms associated with painful locomotor diseases [1][2][3]. There is little information about the pharmacokinetic behavior of tolperisone in humans, in which rapid oral absorption, very low oral bioavailability, and short elimination half-life have been observed [4,5].…”

A Double-Blind Randomized Placebo Controlled Parallel Group Study Evaluating the Effects of Ibuprofen and Glucosamine Sulfate on Exercise Induced Muscle Soreness

“…Subjects, who gave an informed written consent prior to the experiment, were randomized to ibuprofen 1,200 mg/day, 1,500 mg/day glucosamine sulphate, or placebo, respectively, taken for 22 days. On day 14 PEMS was developed in the left first dorsal interosseous [FDI] muscle by means of an exercise program carried out on an established PEMS pain model (13).…”

“…The subject's hand was positioned on the PEMS hand apparatus as described previously (13,14). On the first visit, the hand was positioned on the exerciser by fully pronating the forearm while the elbow was flexed and shoulder abducted to the right angles.…”

“…Eccentric exercises were carried out by lifting the weights attached to the finger splint as described in previous studies (13,14). Briefly, the subjects were provided with a foot pedal to lift the weights attached to the finger splint so that the finger could be fully abducted without having to lift any weight.…”