Pridinol

The active substance pridinol as pridinol mesilate, a piperidin- polyalcohol derivative with the chemical formula: 1,1-Diphenyl-1-ol-3-piperidin-propan-methanesulfonate.

Its pharmacological effect develops via an atropine-like mechanism that acts on both smooth and the striated muscles. This effect is used for the treatment of skeletal muscle tension of both central and peripheral origin.

Pridinol relieves muscle tensions more readily the early the myotonolytic treatment is started. In the cases of long-standing muscle spasms, where anatomical changes have also occurred in the muscle fibers, ligaments and joint capsules, Pridinol can only have a partial effect.

The kinetics of pridinol mesilate in humans have shown that, with oral administration, the maximum blood concentration is attained after about 1 hour and that there is a uniform distribution in the body. The active substance pridinol is largely excreted within 24 hours. This takes place via the kidneys, partly in unchanged form and partly as the glucoronate and as the sulfate-conjugate.

Acute toxicity was investigated in studies on various animal species. The LD50 was 250 mg/kg in mice after oral administration, 446 mg/kg in rats after subcutaneous administration. In a chronic 6-month toxicity study in rats, no toxic effects were seen at doses of 5 to 20 mg/kg/day.

No teratogenic effects were observed in mice treated with a dose of 25 mg/kg/day pridinol mesilate.