Ropinirole hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden
R-Sätze Betriebsanweisung:
R22:Gesundheitsschädlich beim Verschlucken.
R50/53:Sehr giftig für Wasserorganismen, kann in Gewässern längerfristig schädliche Wirkungen haben.
R36/38:Reizt die Augen und die Haut.
S-Sätze Betriebsanweisung:
S36:DE: Bei der Arbeit geeignete Schutzkleidung tragen.
S60:Dieses Produkt und sein Behälter sind als gefährlicher Abfall zu entsorgen.
S61:Freisetzung in die Umwelt vermeiden. Besondere Anweisungen einholen/Sicherheitsdatenblatt zu Rate ziehen.
S37/39:Bei der Arbeit geeignete Schutzhandschuhe und Schutzbrille/Gesichtsschutz tragen.
S26:Bei Berührung mit den Augen sofort gründlich mit Wasser abspülen und Arzt konsultieren.
Beschreibung
ReQuip was launched in the UK as a monotherapy or in combination with
low-dose levodopa for the treatment of early-stage idiopathic Parkinson's disease.
An eight step (24% overall yield) synthesis from isochroman provides access to
ropinirole. It is a non-ergot postsynaptic dopamine D
2 agonist with activity in the
extrapyramidal system. It has weak or no significant activity at α
2-adrenergic, 5-HT
2
receptors and is inactive at 5-HT
1, benzodiazepine, GABA, α
1 and β adrenoreceptors.
Thus it has essentially no CNS side effects, fewer dyskinesias and on-off fluctuations.
In animals, it was able to reverse all motor deficits induced by MPTP. Tolerance is
not developed and ropinirole has similar postsynaptic potency to apomorphine but
with significantly less stereotyped behavior.
Chemische Eigenschaften
Off-White Solid
Verwenden
An antiparkinsonian agent. A selective dopamine D2-receptor agonist
Allgemeine Beschreibung
Ropinirole hydrochloride,4-(2-(dipropylamino)ethyl)indolin-2-one hydrochloride(Requip), is a white to pale greenish yellow powder that isvery soluble in water. Ropinirole is rapidly absorbed afteroral administration with maximal plasma concentrationsgenerally reached after about 1.5 hours, and the eliminationhalf-life appears to be approximately 3 hours. Ropinirole isalso rapidly and extensively distributed from the vascularcompartment and shows low plasma protein binding that isindependent of its plasma concentration. This drug iscleared by metabolism in the liver, with only 10% being excretedunchanged. The main metabolite of ropinirole is theN-despropyl metabolite. The glucuronide of this metaboliteand the carboxylic acid metabolite, 4-carboxymethylindolin-2-one, account only for 10% of the administered dose.None of the metabolites is pharmacologically active, and theexcretion of ropinirole-derived products is mainly via theurine. The main CYP450 isozyme involved in the metabolismof ropinirole is CYP1A2. Inhibitors or inducers ofthis enzyme have been shown to alter the clearance ofropinirole.Ropinirole is believed to act as an agonist atpostsynaptic D
2 receptors. Ropinirole is indicated for thetreatment of the signs and symptoms of idiopathic PD andmoderate to severe primary RLS.
Biologische Aktivität
Selective D 2 -like receptor agonist (D 3 > D 2 > D 4 ). Causes biphasic spontaneous locomotor activity and contralateral circling in 6-OHDA-lesioned mice. Displays antiParkinsonian activity.
Ropinirole hydrochloride Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
