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Movement disorders
Published in Henry J. Woodford, Essential Geriatrics, 2022
DAs have also been tried as supplementary therapy to levodopa in advanced PD. A study randomised 360 patients (mean age 63), with sub-optimally controlled PD plus motor fluctuations, to receive either pramipexole or placebo over a 32-week period.49 There were significant improvements in UPDRS scores with pramipexole compared to placebo for motor symptoms (25% v 12%) and reduction in ‘off' time (31% v 7%). Resting tremor, rigidity and bradykinesia were improved. Adverse effects seen more commonly with pramipexole included dyskinesia (61%), hallucinations (19%) and confusion (11%). Similar results have been found with studies of ropinirole.50 The addition of DAs to levodopa can allow a reduction in levodopa dose of up to 30%. This potential levodopa-sparing effect may reduce the occurrence of future motor fluctuations but perhaps at the cost of other adverse effects, especially in frail older people. DA can be considered as an adjunct to levodopa for people with motor fluctuations.7
Degenerative Diseases of the Nervous System
Published in Philip B. Gorelick, Fernando D. Testai, Graeme J. Hankey, Joanna M. Wardlaw, Hankey's Clinical Neurology, 2020
James A. Mastrianni, Elizabeth A. Harris
Ropinirole: Dose: up to 24 mg/day, divided bid or tid.A once-daily extended-release formulation is available.For patients with early untreated PD, monotherapy increases motor scores by 24% compared with placebo, and controls symptoms in about 30% of patients. After 5 years' monotherapy, patients have fewer dyskinesias than if taking levodopa.For patients with motor fluctuations, ropinirole reduces ‘off’ time by 20%, and enables the levodopa dose to be reduced by about 30%.
Drugs Affecting the Central Nervous System
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited, and the reproduction studies in animals have shown the risk of digital malformations associated with the use of Ropinirole.
A patent update on therapeutic applications of urease inhibitors (2012–2018)
Published in Expert Opinion on Therapeutic Patents, 2019
Abdul Hameed, Mariya Al-Rashida, Maliha Uroos, Syeda Uroos Qazi, Sadia Naz, Marium Ishtiaq, Khalid Mohammed Khan
The development of new drugs involves high cost, extensive experimentation, and many steps of redesigning and optimization to overcome toxicity issues before finally making them available in the markets. However, exploring known drugs against different biological targets can prove to be an efficient and cost-effective way in medicinal chemistry. The major advantages associated with the repurposing of known drugs are that their pharmacological and toxicity profiles and other necessary requirements to market a drug are already well established. Therefore, the biological evaluations of such drug molecules for other targets could quickly lead to advanced clinical trials and can speed up the process of developing new therapeutic agents [48]. Khan et al. [49] explored known dopamine agonist drug ropinirole (25), 4-[2-(dipropylamino)ethyl]1,3-di-hydro-2H-indol-2-one, as a urease inhibitor (Figure 3). The known drug, ropinirole, has been used to treat Parkinson’s disease and restless legs syndrome. Compound 25 has been tested for in vitro urease inhibition activity against Jack bean urease and found to possess excellent inhibitory activity with IC50 value of 11.7 ± 0.46 µM in comparison to reference inhibitors acetohydroxamic acid (IC50 = 41.5 ± 0.11 µM) and thiourea (IC50 = 21.0 ± 0.50 µM). The mechanistic study revealed ropinirole to be a mixed-type inhibitor.
Predicting the dopamine D2 receptor occupancy of ropinirole in rats using positron emission tomography and pharmacokinetic–pharmacodynamic modeling
Published in Xenobiotica, 2019
Chenrong Huang, Ziteng Wang, Linsheng Liu, Xiaoxue Liu, Ji Dong, Qingqing Xu, Bin Zhang, Liyan Miao
Parkinson's disease, also known as Parkinsonism, is primarily characterized by degenerative changes in dopaminergic nerve pathways and clinical manifestations of resting tremor, bradykinesia, rigidity and gait abnormalities. Its prevalence rate among individuals in China aged ≥65 years is 1.7% (Zhang et al., 2005). According to the Chinese Guidelines for Parkinson's Disease Treatment (3rd edition) (Association 2014), ropinirole is a non-ergoline dopamine D2-like receptor agonist that exerts antiparkinsonian effects by directly and continuously stimulating dopamine receptors. Ropinirole has been recommended as a first-line medicine for Parkinson’s disease (Deleu et al., 2002; Matheson & Spencer, 2000) and is widely used in clinical settings.
‘Dopamine agonist Phobia’ in Parkinson’s disease: when does it matter? Implications for non-motor symptoms and personalized medicine
Published in Expert Review of Neurotherapeutics, 2020
Silvia Rota, Iro Boura, Lucia Batzu, Nataliya Titova, Peter Jenner, Cristian Falup-Pecurariu, K Ray Chaudhuri
We conclude that ropinirole is likely to be effective in the treatment of depression and possibly apathy in PD. With the strongest evidence for depression coming from a multicentre phase III clinical trial for the 24-h prolonged release formulation of ropinirole [57], it is suggested that attempts at continuous delivery of this DA might contribute to a positive effect on mood. On the other hand, no randomized controlled trials (RCTs) have demonstrated such an effect on apathy so far. However, the positive responses to ropinirole administration in post-deep brain stimulation (DBS) apathetic patients [59], though not generalizable, are promising.