The pharmacokinetics of pergolide in Parkinson's disease.
Three decades of research have led to a fuller understanding of the pharmacokinetics of pergolide. Pergolide is rapidly absorbed following oral dosing, reaching peak plasma concentrations within 2-3 h. It is about 90% protein bound yet has negligible drug interactions. Pergolide undergoes extensive first-pass metabolism and is completely eliminated within 4-5 days. The metabolism/elimination profile varies between patients but is consistent within the individual, highlighting the importance of careful titration to an effective dose. Pergolide has a long half-life of about 21 h; this has interesting implications, as it should produce a more physiological or continuous stimulation of dopamine receptors, avoiding or delaying the induction of dyskinesia.
Blin
Olivier
O
FRE-CNRS-University 2109, Institute of Physiological and Clinical Neurosciences, CPCET, Hôpital de la Timone, Marseille, France. oblin@mail.ap-hm.fr
D000818:Animals; D018491:Dopamine Agonists / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D004305:Dose-Response Relationship, Drug; D004347:Drug Interactions / Q000502:physiology; D014644:Genetic Variation / Q000502:physiology; D006801:Humans; D008657:Metabolic Clearance Rate / Q000502:physiology; D010300:Parkinson Disease / Q000188:drug therapy*; D010479:Pergolide / Q000097:blood / Q000493:pharmacokinetics* / Q000627:therapeutic use; D011954:Receptors, Dopamine / Q000187:drug effects / Q000378:metabolism
D018491:Dopamine Agonists; D011954:Receptors, Dopamine; D010479:Pergolide