title: The safety of istradefylline for the treatment of Parkinson's disease.
abstract: BACKGROUND
  Antagonism of the A2A receptor improves motor behavior in patients with Parkinson's disease (PD), according to results of clinical studies which confirm findings of previous experimental research. The xanthine derivative, istradefylline , has the longest half-life out of the available A2A receptor antagonists. Istradefylline easily crosses the blood-brain barrier and shows a high affinity to the human A2A receptor.
  
  
  METHODS
  This narrative review aims to discuss the safety and tolerability of istradefylline against the background of the currently available drug portfolio for the treatment of PD patients.
  
  
  CONCLUSIONS
  Istradefylline was safe and well tolerated in clinical trials, which have focused on l-DOPA-treated PD patients. The future of istradefylline as a complementary drug for modulation of the dopaminergic neurotransmission also relies on its potential to act like an l-DOPA plus dopamine agonist sparing future treatment alternative and to reduce the risk of predominant l-DOPA-related onset of motor complications in addition to its direct ameliorating effect on motor symptoms. Dopamine-substituting drugs may dose-dependently produce systemic side effects, particularly onset of hypotension and nausea by peripheral dopamine receptor stimulation. Istradefylline does not interfere with these peripheral receptors and therefore shows a good safety and tolerability profile.
authors: St. Joseph Hospital Berlin-Weißensee, Department of Neurology , Gartenstr. 1, 13088 Berlin , Germany +49 30 92790223 ; +49 30 92790703 ; th.mueller@alexius.de ; thomas.mueller@ruhr-uni-bochum.de.
authors: Thomas
authors: T
authors: Müller
mesh_terms: D058917:Adenosine A2 Receptor Antagonists / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use; D000818:Animals; D000978:Antiparkinson Agents / Q000009:adverse effects / Q000494:pharmacology / Q000627:therapeutic use; D001812:Blood-Brain Barrier / Q000378:metabolism; D004305:Dose-Response Relationship, Drug; D006207:Half-Life; D006801:Humans; D010300:Parkinson Disease / Q000188:drug therapy* / Q000503:physiopathology; D011687:Purines / Q000009:adverse effects* / Q000494:pharmacology / Q000627:therapeutic use
chemical_list: D058917:Adenosine A2 Receptor Antagonists; D000978:Antiparkinson Agents; D011687:Purines; C111599:istradefylline
keywords: Parkinson’s disease; adenosine; dopamine substitution; istradefylline; l-DOPA