Anticholinergic drugs used in Parkinson's disease: An overlooked class of drugs from a pharmacokinetic perspective.

摘要: Anticholinergic drugs were the first pharmacological agents used in treatment of Parkinson"s disease. Although levodopa and other centrally acting dopaminergic agonists have largely supplanted their use, they still a place As therapeutic class, there is little pharmacokinetic information available for these drugs, which inclusive benztropine, biperiden, diphenhydramine, ethopropazine, orphenadrine, procyclidine trihexyphenidyl. Pharmacokinetic restricted to studies involving young health volunteers given single doses. In general, this class rapidly absorbed after oral administration humans. Oral bioavailability variable between different ranging from 30% over 70%. Each appears possess large Vd humans animals, distribution tissues rapid. The are all characterized by relatively low clearance relative hepatic blood flow, appear be extensively metabolized, primarily N-dealkylated hydroxylated metabolites. suggests that excretion parent drug metabolite via urine bile. existence plasma concentration vs. effect relationship has not been explored, some evidence suggesting peripheral side effects. Elderly tolerate less well than do younger patients. There notable lack elderly. multiple dose elderly may possible hindrance safe effective use patients with