[Human pharmacologic studies on transdermal administration of mepindolol. Pharmacodynamic and orienting...

The pharmacodynamic effects of acute and repeated application of a transdermal patch (BIO TSD) containing 20 mg of the beta-receptor blocking agent mepindolol were assessed in 13 normotensive male volunteers. Orienting measurements of mepindolol serum levels were performed additionally. At rest, the effects on blood pressure and heart rate were very limited. However, during submaximum ergometer exercise, significant systemic beta-blocking effects were observed, especially after 5 days treatment. Repeated administration did not induce tachyphylaxis but resulted in an enhanced efficacy. The mepindolol serum concentrations were markedly lower than those measured after oral application of the drug. No systemic or local adverse reactions nor any relevant changes in laboratory parameters were observed.