Transdermal delivery of dopamine receptor agonists.

Abstract

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.

• Authors: Heinz Reichmann
• Journal: Parkinsonism & related disorders (Parkinsonism Relat Disord) Vol. 15 Suppl 4 Pg. S93-6 (Dec 2009) ISSN: 1873-5126 [Electronic] England
• PMID: 20123566 (Publication Type: Journal Article, Review)
• Copyright: Copyright 2009 Elsevier Ltd. All rights reserved.

Chemical References

• Dopamine Agonists

Topics

• Administration, Cutaneous
• Animals
• Dopamine Agonists (administration & dosage, pharmacokinetics)
• Drug Delivery Systems (methods)
• Humans
• Parkinson Disease (drug therapy, metabolism)
• Skin Absorption (drug effects, physiology)