Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0027497 (nausea)
 23,468 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Ropinirol (SK&F 101468) is a novel drug characterized preclinically as a potent and selective D2-dopaminergic agonist. In the present study the effects of acute doses of 0.4, 0.8 and 1 mg were profiled in eight healthy male volunteers, using a placebo-controlled cross-over study design with incremental dosing. The drug was found to cause mild nausea and postural faintness at the highest dose in one subject. There were no further relevant clinical events, and the postural responses at 200 and 360 min after dosing remained in general well maintained, with the exception of a slight reduction of standing systolic blood pressure. The drug furthermore was found to reduce serum prolactin levels; the magnitude and duration of this effect were dose-related. The drug tended to reduce the noradrenaline responses to 5 min isometric handgrip testing (30% of maximal strength) at 165 min after dosing, and the noradrenaline responses to 3 min immobile standing at 200 min after dosing. The drug also tended to blunt the venous plasma dopamine responses to 3 min cold pressor test (90 min after dosing) and to standing at 200 min after dosing. These changes are concluded to be compatible with the assumed peripheral D2-dopaminergic actions of the drug.
 ...
PMID:Effects of the novel D2-dopaminergic agonist ropinirol on supine resting and stimulated circulatory and neuroendocrine variables in healthy volunteers. 197 Nov 70

Ropinirole (Requip, GlaxoSmithKline) is a novel nonergoline dopamine D2 agonist indicated for the treatment of early and advanced Parkinson's disease. It is mainly metabolized by the liver and its elimination half-life is approximately 5.8 h. When used as monotherapy in early Parkinson's disease, ropinirole improves signs and symptoms of the disorder. When used as an adjunct to levodopa in advanced Parkinson's disease patients with motor fluctuations, ropinirole reduces off time and allows a reduction of levodopa dose. The initial use of ropinirole in early Parkinson's disease to which levodopa is added when necessary, has been demonstrated to lead to a lower incidence of dyskinesias compared with treatment with levodopa alone. An 18F-dihydroxyphenylalanine positron emission tomography study suggested the possibility that ropinirole could slow the progression of loss of dopamine neurons compared with treatment with levodopa but this remains to be proven. Side effects of ropinirole include nausea, somnolence, edema, orthostatic hypotension, hallucinations and dyskinesia. A once-daily formulation of ropinirole is currently in development that has the potential for greater convenience, improved tolerability and greater efficacy.
 ...
PMID:Ropinirole therapy for Parkinson's disease. 1585 77

The number of dopamine agonists (DA) used in Parkinson's disease (PD) is gradually increasing. They have different affinity to the dopamine receptor subtypes. When choosing one of these drugs one should consider its efficacy in monotherapy in early phase and in combined therapy with levodopa in advanced PD, side effects profile, effectiveness in non-motor symptoms of PD, dosing and route of administration. The efficacy of new DA (pramipexol, ropinirol, cabergoline) is probably higher than bromocriptine and comparable to pergolide with similar profile of the most common side effects (headache, vertigo, nausea, somnolence, oedema). However, fibrosis of the pleura, peritoneum and pericardium as well as valvular heart disease (caused by noninflammatory fibrotic degeneration) are significantly more common after ergoline DA (pergolide, cabergoline). Pramipexol shows antidepressant activity. Ropinirol is metabolised by the liver and can be safely administered in renal insufficiency. Pramipexol is excreted in urine and the risk of interaction with other drugs metabolised in the liver is reduced. Rotigotine is the only DA available as skin patches. Whenever necessary, one DA agent can be changed safely overnight to another one.
 ...
PMID:[Choosing a dopamine agonist in Parkinson's disease]. 1794 54