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Biogenic amines
Published in William L. Nyhan, Georg F. Hoffmann, Aida I. Al-Aqeel, Bruce A. Barshop, Atlas of Inherited Metabolic Diseases, 2020
William L. Nyhan, Georg F. Hoffmann, Aida I. Al-Aqeel, Bruce A. Barshop
First-choice medications appear to be dopamine agonists, such as bromocriptine or pramipexole, or ropinirole, followed by MAO inhibitors such as selegeline or tranylcypromine. An additional trial with the anticholinergic drug trihexyphenidyl can be helpful. Pergolide and cabergoline should not be used because of the high risk of fibrotic complications. Amantadine with 4 mg/kg/d can help against drug induced dyskinesias.
Pharmacological Management of Parkinson’s Disease
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Newman Osafo, Samuel Obeng, David D. Obiri, Oduro K. Yeboah, Leslie B. Essel
The most significant adverse effects seen with pergolide are dyskinesias (30%), hallucinations (10–20%), disturbances of the gastrointestinal system (10%), insomnia (10%), somnolence, mild and transient bradycardia, and rarely hepatic injury (Langtry and Clissold, 1990). Coadministration with domperidone may substantially improve tolerability (Barone et al., 1999).
Prejunctional Dopamine Receptor Stimulants
Published in M.D. Francesco Amenta, Peripheral Dopamine Pathophysiology, 2019
Only one report relates to the cardiovascular effects of pergolide in man. In a study in normotensive patients with prolactinomas, treatment for 2 months resulted in reductions in supine and erect blood pressure, but plasma noradrenaline levels were not reduced. By contrast, treatment of a parallel group of patients with doses of bromocriptine-producing comparable falls in plasma prolactin levels produced a significant reduction. Both compounds depressed the rise in plasma noradrenaline in response to furosemide.114 The potential effects of pergolide in hypertensive patients have not as yet been investigated.
Treatment of psychiatric disturbances in hypokinetic movement disorders
Published in Expert Review of Neurotherapeutics, 2019
Isabella Berardelli, Daniele Belvisi, Massimo Pasquini, Andrea Fabbrini, Federica Petrini, Giovanni Fabbrini
Sleep disorders are frequent in PD patients and include insomnia, REM behavior disorders (RBD), vivid dreams and nightmares, restless leg syndrome, periodic legs movements, nocturia, pain and other symptoms [145]. In the study by Comella et al [146] on 26 PD patients treated with pergolide 1 mg/day given at bedtime, pergolide worsened sleep efficiency and increased sleep fragmentation when compared to placebo. Melatonin 5 mg at bedtime improved sleep quality in 43 PD patients when compared to placebo treated patients [147]. Eszopiclone, a ligand of the benzodiazepine allosteric site of GABAA receptors, reduced significantly the number of awakenings in 30 PD patients when compared to placebo [148]. In 20 PD patients with difficulty in sleep onset and night awakenings, the antidepressant doxepin at the dose of 10 mg at bedtime combined with CBT was better than sham-light intervention as measured through the SCOPA sleep [149]. Pan et al [150] showed that in 70 PD patients Yang-Xue-Qing-Nao granules produced a significant improvement on actigraphically measured sleep activity. Finally rivastigmine 4,6 mg bedtime patch improved RBD in 12 PD patients whose RBD was refractory to melatonin and clonazepam [151] and CBT improved sleep disturbances in 22 PD patients with insomnia [152].
Systematic review of the pharmacoeconomics of Parkinson disease medications
Published in Expert Opinion on Pharmacotherapy, 2019
Alexander S. Wang, Steven A. Gunzler
Bromocriptine, pergolide, and cabergoline are ergot-derivative DAs. They are not commonly used because of potential cardiac valvular side effects and because pergolide was withdrawn from the US market. There were two studies looking at bromocriptine and pergolide compared to CL [30,52]. A government-funded CUA compared bromocriptine adjunct therapy and pergolide adjunct therapy to levodopa monotherapy [52]. The authors found that when started in H&Y stage 2, neither dopamine agonist was cost-effective as adjunct compared to levodopa. When started in H&Y stage 3 or higher, both therapies were dominant over levodopa [52]. An industry-funded CEA found pergolide to be dominant over bromocriptine for treatment of PD in any stage [30]. There was one CEA looking at cabergoline versus CL in early PD, which found that initial treatment with cabergoline (with the possibility of later adding CL) is likely cost-effective compared to CL monotherapy [37].
Dopamine-induced functional activation of Gαq mediated by dopamine D1-like receptor in rat cerebral cortical membranes
Published in Journal of Receptors and Signal Transduction, 2019
Yuji Odagaki, Masakazu Kinoshita, Toshio Ota
As for SKF83566 and R(+)-SCH23390, the data presented herein clearly indicate that stimulatory effects of pergolide on specific [35S]GTPγS bindings to Gαq in rat cerebral cortical membranes are mediated through 5-HT2A receptor, but not dopamine D-l like receptors. The agonistic effects of this compound on 5-HT2A receptor-mediated signaling or function have been reported previously [51,52]. Pergolide is an ergot alkaloid derivative that is used in the treatment of Parkinson’s disease and hyperprolactinemia. Although it remains in use in some countries as an antiparkinson drug, it has been withdrawn from the U.S. market owing to the risk of fibrotic valvular heart disease, the adverse effect usually attributable to its agonistic effect on 5-HT2B receptor expressed in heart valves [53]. However, the possibility that 5-HT2A agonist properties participate in development of pergolide-induced cardiac valve regurgitation cannot be completely ruled out [52]. Another possible clinical implication of 5-HT2A receptor agonist effects is psychotic symptoms often associated with treatment with pergolide in patients with Parkinson’s disease. It has been reported that psychotic episodes seen in patients with Parkinson’s disease are strongly associated with the use of pergolide as compared to other dopamine agonists, that is, levodopa, ropinirole, pramipexole, and cabergoline [54].