Pergolide mesylate is an antiparkinsonian agent which functions as a dopaminergic agonist.Target: Dopamine ReceptorPergolide mesylate (trade name Permax) is an ergoline-based dopamine receptor agonist used in some countries for the treatment of Parkinson's disease. Pergolide mesylate functions as an agonist at the dopamine D2, D1 and serotonin 5-HT1A, 5-HT1B, 5-HT2A, 5-HT2B, and 5-HT2C receptors. It may possess agonist activity at other dopamine receptor subtypes as well, similar to cabergoline [1, 2]. Pergolide mesylate decreases plasma prolactin concentrations [3]. The weak agonist activity of pergolide at D1 receptors somewhat alters its clinical and side effect profile in the treatment of Parkinson's disease. The drug is in decreasing use, as it is reported to be associated with a form of heart disease called cardiac fibrosis. The use of pergolide or cabergoline is associated with a significantly increased risk of newly diagnosed cardiac-valve regurgitation [4].
References:
[1]. Lemberger, L. and R.E. Crabtree, Pharmacologic effects in man of a potent, long-acting dopamine receptor agonist. Science, 1979. 205(4411): p. 1151-3.
[2]. Koller, W.C., et al., The pharmacological evaluation of pergolide mesylate as a potential anti-parkinson agent. Neuropharmacology, 1980. 19(9): p. 831-7.
[3]. Franks, S., et al., Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. British medical journal (Clinical research ed.), 1983. 286(6372): p. 1177.
[4]. Schade, R., et al., Dopamine agonists and the risk of cardiac-valve regurgitation. N Engl J Med, 2007. 356(1): p. 29-38.