Ropinirole, a non-ergoline dopamine agonist, has selective affinity for dop
amine D-2-like receptors and little or no affinity for non-dogaminergic bra
in receptors, Ropinirole is indicated as adjunct therapy to levodopa in pat
ients with advanced Parkinson's disease. It is also indicated, and recent c
linical trials have focused on its use, as monotherapy in patients with ear
ly Parkinson's disease.
In the symptomatic treatment of early Parkinson's disease ropinirole monoth
erapy was significantly more effective than placebo in 2 multicentre, rando
mised, double-blind trials of 3 to 12 months duration as assessed by the Un
ified Parkinson's Disease Rating Scale (UPDRS) motor scores and Clinical Gl
obal Impression/Clinical Global Evaluation Scales. In a similarly designed
3-year comparative study with bromocriptine, ropinirole recipients showed a
significant improvement in UPDRS-activities of daily living (ADL) scores;
however, motor scores were similar between the 2 groups. Ropinirole and lev
odopa treatments were similar in efficacy as measured by UPDRS ADL scores,
although ropinirole recipients showed significantly less improvement on UPD
RS motor scores at the 5-year study end-point in a multicentre, randomised
double-blind trial.
As an adjunct therapy to levodopa in patients with more advanced Parkinson'
s disease, ropinirole was reported to be as effective as bromocriptine and
significantly more effective than placebo, In general in the comparisons wi
th placebo ropinirole allowed a greater than or equal to 20% reduction in t
he concomitant dose of levodopa without compromising efficacy in a signific
ant proportion of patients and, in some trials decreased the amount of awak
e time spent in the 'off' state ('off' state is defined as a gradual return
to parkinsonism despite adequate medication).
Ropinirole was well tolerated either as monotherapy or as an adjunct to lev
odopa treatment. Nausea, dizziness and somnolence were the most commonly re
ported adverse events and were reported at a higher incidence by patients r
eceiving ropinirole than by those receiving placebo. In patients with early
Parkinson's disease, ropinirole generally showed a similar overall tolerab
ility profile to bromocriptine although, over a 3-year period nausea was mo
re commonly reported with ropinirole recipients, In a 5-year study, the inc
idence of dyskinesia was significantly lower with ropinirole than with levo
dopa regardless of levodopa supplementation. Prior to the addition of suppl
ementary levodopa 5% of ropinirole recipients had experienced dyskinesia co
mpared with 36% of those receiving levodopa.
Conclusions: In patients with early Parkinson's disease, ropinirole monothe
rapy was more efficacious than bromocriptine with regard to improvement in
activities of daily living, and need for supplemental levodopa, Ropinirole
recipients had a higher requirement for levodopa supplementation than levod
opa recipients in a 5-year study, but the incidence of dyskinesia was signi
ficantly lower with ropinirole than with levodopa (markedly so in the one t
hird of ropinirole recipients who were able to remain on monotherapy with n
o levodopa supplementation). Thus available data suggest that ropinirole ma
y provide a means of treating early Parkinson's disease while minimising th
e risk of dyskinesia and delaying the need for supplemental levodopa in som
e patients. In addition, ropinirole is also efficacious in the management o
f more advanced Parkinson's disease in patients who are experiencing motor
complications after long term levodopa use.