Transdermal delivery of dopamine receptor agonists.
Conceptually, continuous dopaminergic stimulation is universally accepted to be the preferred therapeutic strategy to prevent or postpone dyskinesia in Parkinson's disease (PD). L-dopa has a short half-life of 2 hours and causes dyskinesia, whereas dopamine receptor agonists usually have a much longer half-life. Of the latter agents, cabergoline has the longest half-life of 68 hours and is ideal for the prevention of dyskinesia; but this is also true for other dopamine receptor agonists such as ropinirole or pramipexole, which have a shorter half-life of about 6-8 hours. Due to the possible development of valvular fibrosis, cabergoline is, however, only approved as a second-line treatment in PD, and patch technology has therefore gained major interest. So far, rotigotine is the only dopamine receptor agonist available as a patch. There is good evidence that once-daily patch usage provides patients with constant dopaminergic stimulation, and that patches are of equal potency to other oral non-ergot derivatives such as ropinirole and pramipexole. The disadvantages of patches are skin irritation and crystallization of the drug if not kept in the refrigerator.
Reichmann
Heinz
H
Department of Neurology, Dresden University of Technology, Dresden, Germany. Heinz.Reichmann@uniklinikum-dresden.de
D000279:Administration, Cutaneous; D000818:Animals; D018491:Dopamine Agonists / Q000008:administration & dosage* / Q000493:pharmacokinetics; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy / Q000378:metabolism; D012869:Skin Absorption / Q000187:drug effects* / Q000502:physiology
D018491:Dopamine Agonists