Why doesn't ropinirole work for me

Retarded ropinirole helps to prolong the on-phase during the day

Dopamine agonists are drugs of first choice for the treatment of early-stage Parkinson's patients under 70 years of age. But they are also used successfully in the middle and late stages - usually together with levodopa.

However, treatment with levodopa (L-Dopa) often leads to dyskinesia. The reason for this could be the short half-life of L-Dopa and the associated pulsatile stimulation of the postsynaptic dopaminergic receptors. This is suspected of modifying the receptors plastically and influencing their response. The postsynaptic dopamine receptors are also only stimulated intermittently when dopamine agonists are administered in several individual doses over the course of the day, as was previously the case. Longer gaps in effectiveness then arise, especially at night.

Continuous dopaminergic stimulation

The non-ergoline dopamine agonist, ropinirole, has been available in the form of a prolonged-release tablet since the beginning of March 2008. The delayed formulation of the "modulated tablet" ReQuip® Modutab was studied in monotherapy in more than 100 ropinirole-naïve patients in the early stages of the disease. The ropinirol dose was flexible. The motor part of the UPDRS (Unified Parkinson Disease Rating Scale) improved from about 20 by 10.4 points with ropinirole retard (CR) vs. 8.9 points with immediately released (IR) ropinirole. The undesirable effects were largely identical; With the sustained release formulation, tiredness and daytime sleepiness were somewhat lower.

In another study, almost 400 Parkinson's patients in advanced stages of the disease were treated either with L-Dopa alone or with L-Dopa and ropinirole retard. Result: In the verum group, the off times of the patients, i.e. the times of extensive akinesia, were shortened by an average of 2.1 hours from the previous nine hours, in the control group by only 0.3 hours. The extended on-time was not bought at the cost of more disabling dyskinesia. Furthermore, 164 mg of L-Dopa could be saved with placebo and 278 mg of L-Dopa per day with ropinirole retard.

 

 

Improving the quality of sleep

The continuous stimulation of the postsynaptic dopamine receptors is also suitable for preventing the akinesia of Parkinson's patients in the early morning hours. These and other sleep disorders affect the quality of life of up to 90% of Parkinson's patients, especially in the later stages of the disease.

Uncomplicated adjustment and changeover

The ropinirole prolonged-release tablet is approved for the treatment of Parkinson's disease in the initial treatment as monotherapy to delay the use of levodopa and in combination with levodopa during the course of the disease if the efficacy of levodopa decreases or becomes irregular and fluctuations in the therapeutic effect occur . When changing to the ropinirole prolonged-release tablets, the dosage can be increased quickly: in weekly steps of 2 mg each up to a daily dose of 8 mg, which is usually sufficient. If necessary, titration can be continued in steps of 4 mg per week up to a daily dose of 24 mg. It is also easy to switch from three times a day un-delayed ropinirole administration to ropinirole retard once a day: It takes place overnight by adding the entire previous daily dose and converting it to the next possible daily dose with the ropinirole prolonged-release tablets. The prolonged-release tablets can either be taken with or without food. The three-layer prolonged-release tablets must be taken whole and must not be chewed, crushed or divided.

 

source

Prof. Dr. Wolfgang Jost, Wiesbaden; Prof. Dr. Claudia Trenkwalder, Kassel; Prof. Dr. Heinz Reichmann, Dresden: "ReQuip® Modutab 1 x daily: effectiveness day and night through continuous dopaminergic therapy ", Frankfurt / Main, March 10, 2008, organized by GlaxoSmithKline GmbH & Co. KG, Munich.

Efficacy and Safety Evaluation in Parkinsons DiseaseMonotherapy Study (168), submitted for publication.

Pahwa, A .; et al .: Efficacy and Safety Evaluation in Parkinsons Disease Adjunct Therapy Study (169), Neurology 2007.

 


Simone Reisdorf, freelance medical journalist