ROPINIROLE HYDROCHLORIDE

First approved in 1997

Details

Stereochemistry	ACHIRAL
Molecular Formula	C16H24N2O.ClH
Molecular Weight	296.836
Optical Activity	NONE
Defined Stereocenters	0 / 0
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

Cl.CCCN(CCC)CCC1=C2CC(=O)NC2=CC=C1

InChI

InChIKey=XDXHAEQXIBQUEZ-UHFFFAOYSA-N

InChI=1S/C16H24N2O.ClH/c1-3-9-18(10-4-2)11-8-13-6-5-7-15-14(13)12-16(19)17-15;/h5-7H,3-4,8-12H2,1-2H3,(H,17,19);1H

HIDE SMILES / InChI

Molecular Formula	C16H24N2O
Molecular Weight	260.3746
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Molecular Formula	ClH
Molecular Weight	36.461
Charge	0
Count

Stereochemistry	ACHIRAL
Additional Stereochemistry	No
Defined Stereocenters	0 / 0
E/Z Centers	0
Optical Activity	NONE

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020658s034lbl.pdf
Curator's Comment: description was created based on several sources, including http://reference.medscape.com/drug/requip-xl-ropinirole-343051 | https://www.drugs.com/cdi/ropinirole.html | https://www.drugbank.ca/drugs/DB00268

Ropinirole (INN; trade names Requip, Repreve, Ronirol, Adartrel) is a dopamine agonist of the non-ergoline class of medications, used in the treatment of Parkinson's disease and restless legs syndrome. Although the precise mechanism of action of ropinirole as a treatment for Parkinson's disease is unknown, it is believed to be related to its ability to stimulate dopamine receptors in the striatum. This conclusion is supported by electrophysiologic studies in animals that have demonstrated that ropinirole influences striatal neuronal firing rates via activation of dopamine receptors in the striatum and the substantia nigra, the site of neurons that send projections to the striatum. Ropinirole is a nonergot dopamine agonist with high relative in vitro specificity and full intrinsic activity at the D2 subfamily of dopamine receptors, binding with higher affinity to D3 than to D2 or D4 receptor subtypes. The relevance of D3 receptor binding in Parkinson's disease is unknown. The mechanism of ropinirole-induced postural hypotension is presumed to be due to a D2 -mediated blunting of the noradrenergic response to standing and subsequent decrease in peripheral vascular resistance. Ropinirole can cause nausea, dizziness, hallucinations, orthostatic hypotension, and sudden sleep attacks during the daytime. Unusual side effects specific to D3 agonists such as ropinirole and pramipexole can include hypersexuality, punding, and compulsive gambling, even in patients without a history of these behaviors.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Potency
Dopamine D2 receptor 311 Target ID: CHEMBL217 Sources: https://www.ncbi.nlm.nih.gov/pubmed/17976986	Agonist 2752	83.0 nM [EC50]
Dopamine D3 receptor 97 Target ID: CHEMBL234 Sources: https://www.ncbi.nlm.nih.gov/pubmed/20038106	Partial Agonist 297	19.2 nM [EC50]
Dopamine receptor 60 Target ID: CHEMBL2096905 Sources: https://www.ncbi.nlm.nih.gov/pubmed/4045928	Agonist 2752	100.0 nM [EC50]

Conditions

Condition	Modality	Highest Phase	Product
Parkinson's disease 232 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020658s034lbl.pdf	Primary	Approved 8583	REQUIP Approved Use Parkinson's Disease Ropinirole tablets are indicated for the treatment of the signs and symptoms of idiopathic Parkinson's disease. The effectiveness of ropinirole tablet was demonstrated in randomized, controlled trials in patients with early Parkinson's disease who were not receiving concomitant L-dopa therapy as well as in patients with advanced disease on concomitant L-dopa (see CLINICAL PHARMACOLOGY: Clinical Trials). Restless Legs Syndrome Ropinirole tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS). Key diagnostic criteria for RLS are: an urge to move the legs usually accompanied or caused by uncomfortable and unpleasant leg sensations; symptoms begin or worsen during periods of rest or inactivity such as lying or sitting; symptoms are partially or totally relieved by movement such as walking or stretching at least as long as the activity continues; and symptoms are worse or occur only in the evening or night. Difficulty falling asleep may frequently be associated with moderate-to-severe RLS. Launch Date 1997
Restless legs syndrome 17 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/020658s034lbl.pdf	Primary	Approved 8583	REQUIP Approved Use Parkinson's Disease Ropinirole tablets are indicated for the treatment of the signs and symptoms of idiopathic Parkinson's disease. The effectiveness of ropinirole tablet was demonstrated in randomized, controlled trials in patients with early Parkinson's disease who were not receiving concomitant L-dopa therapy as well as in patients with advanced disease on concomitant L-dopa (see CLINICAL PHARMACOLOGY: Clinical Trials). Restless Legs Syndrome Ropinirole tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS). Key diagnostic criteria for RLS are: an urge to move the legs usually accompanied or caused by uncomfortable and unpleasant leg sensations; symptoms begin or worsen during periods of rest or inactivity such as lying or sitting; symptoms are partially or totally relieved by movement such as walking or stretching at least as long as the activity continues; and symptoms are worse or occur only in the evening or night. Difficulty falling asleep may frequently be associated with moderate-to-severe RLS. Launch Date 1997
Sexual dysfunction 2 Sources: https://clinicaltrials.gov/ct2/show/NCT00334048	Primary	Phase IV 63	REQUIP Approved Use Parkinson's Disease Ropinirole tablets are indicated for the treatment of the signs and symptoms of idiopathic Parkinson's disease. The effectiveness of ropinirole tablet was demonstrated in randomized, controlled trials in patients with early Parkinson's disease who were not receiving concomitant L-dopa therapy as well as in patients with advanced disease on concomitant L-dopa (see CLINICAL PHARMACOLOGY: Clinical Trials). Restless Legs Syndrome Ropinirole tablets are indicated for the treatment of moderate-to-severe primary Restless Legs Syndrome (RLS). Key diagnostic criteria for RLS are: an urge to move the legs usually accompanied or caused by uncomfortable and unpleasant leg sensations; symptoms begin or worsen during periods of rest or inactivity such as lying or sitting; symptoms are partially or totally relieved by movement such as walking or stretching at least as long as the activity continues; and symptoms are worse or occur only in the evening or night. Difficulty falling asleep may frequently be associated with moderate-to-severe RLS. Launch Date 1997

C_max

Value	Dose	Co-administered	Analyte	Population
6.53 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9578193	2 mg 3 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ROPINIROLE HYDROCHLORIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
5.01 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9578193	2 mg 3 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ROPINIROLE HYDROCHLORIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

AUC

Value	Dose	Co-administered	Analyte	Population
29.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9578193	2 mg 3 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ROPINIROLE HYDROCHLORIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
25.9 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/9578193	2 mg 3 times / day steady-state, oral dose: 2 mg route of administration: Oral experiment type: STEADY-STATE co-administered:		ROPINIROLE HYDROCHLORIDE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FED

T_1/2

Value	Dose	Co-administered	Analyte	Population
6 h DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unknown, oral		ROPINIROLE HYDROCHLORIDE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
60% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unknown, oral		ROPINIROLE HYDROCHLORIDE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
50 mg 1 times / day steady, oral Highest studied dose Dose: 50 mg, 1 times / day Route: oral Route: steady Dose: 50 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28442303	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/28442303	Sources: https://pubmed.ncbi.nlm.nih.gov/28442303
435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	Other AEs: Nausea, Dizziness... Other AEs: Nausea Dizziness Claustrophobia Chorea Palpitations Asthenia Nightmares Hyperhidrosis Visual hallucinations Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
0.5 mg 2 times / day steady, oral Recommended Dose: 0.5 mg, 2 times / day Route: oral Route: steady Dose: 0.5 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	Disc. AE: Nausea, Dizziness... AEs leading to discontinuation/dose reduction: Nausea (2%) Dizziness (2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
24 mg 1 times / day steady, oral Recommended Dose: 24 mg, 1 times / day Route: oral Route: steady Dose: 24 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/28442303	unhealthy Health Status: unhealthy Sources: https://pubmed.ncbi.nlm.nih.gov/28442303	Sources: https://pubmed.ncbi.nlm.nih.gov/28442303

AEs

AE	Significance	Dose	Population
Asthenia		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Chorea		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Claustrophobia		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Dizziness		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Hyperhidrosis		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Nausea		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Nightmares		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Palpitations		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Visual hallucinations		435 mg 1 times / day multiple, oral Overdose Dose: 435 mg, 1 times / day Route: oral Route: multiple Dose: 435 mg, 1 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Dizziness	2% Disc. AE	0.5 mg 2 times / day steady, oral Recommended Dose: 0.5 mg, 2 times / day Route: oral Route: steady Dose: 0.5 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf
Nausea	2% Disc. AE	0.5 mg 2 times / day steady, oral Recommended Dose: 0.5 mg, 2 times / day Route: oral Route: steady Dose: 0.5 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2020/020658Orig1s037lbl.pdf

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
	inhibitor 2438	inhibitor 2507

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP2C8 1057 CYP3A 227 CYP1A2 2153 CYP2C19 2057 CYP2A6 879 CYP2E1 1060	CYP3A 220 CYP1A2 1197 P-gp 2052	CYP 74

Drug as perpetrator

Target	Modality	Activity	Metabolite
CYP 150	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020658s038lbl.pdf#page=22 Page: 22.0	no
CYP 150	inducer 1966 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020658s038lbl.pdf#page=22 Page: 22.0	no	Circulating Metabolites 2
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP1A2 2333	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP2A6 911	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP2C19 2141	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP2C8 1117	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP2C9 2497	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP2E1 1146	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no
CYP3A 317	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	no	Circulating Metabolites 2
CYP2D6 2546	inhibitor 4027 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/2008/022008s000_ClinPharmR_P1.pdf#page=53 Page: 53.0	weak

Drug as victim

Target	Modality	Activity	Clinical evidence
CYP1A2 1197	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020658ap_Requip_phrmrP1.pdf#page=58 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020658s038lbl.pdf#page=22 Page: 58, (Label) 22	major	yes (co-administration study) Comment: Ciprofloxacin increased Ropinirole AUC by 84% and Cmax by 60%. Sources: https://www.accessdata.fda.gov/drugsatfda_docs/nda/97/020658ap_Requip_phrmrP1.pdf#page=58 \| https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020658s038lbl.pdf#page=22 Page: 58, (Label) 22
CYP3A 220	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/9224778/	minor
P-gp 2052	substrate 4014 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2021/020658s038lbl.pdf#page=22 Page: 22.0	no

Sourcing

Vendor/Aggregator	ID	URL
ChEBI	CHEBI:8888	https://www.ebi.ac.uk/chebi/searchId.do?chebiId=CHEBI:8888
eMolecules	902428	https://www.emolecules.com/cgi-bin/more?vid=902428
MolPort	MolPort-003-666-598	https://www.molport.com/shop/molecule-link/MolPort-003-666-598
ZINC	ZINC000000002041	http://zinc15.docking.org/substances/ZINC000000002041

PubMed

Title	Date	PubMed
Sleep disorders in patients with Parkinson's disease: epidemiology and management.	2001	11463132
Neostriatal muscarinic receptor subtypes involved in the generation of tremulous jaw movements in rodents implications for cholinergic involvement in parkinsonism.	2001 Apr 27	11392629
Efficacy and tolerability of dopamine agonists in a parkinsonian population.	2001 Feb	11487183
Molecular mechanism in activation of glutathione system by ropinirole, a selective dopamine D2 agonist.	2001 Jan	11358279
Adjunctive dopamine agonists in treatment-resistant bipolar II depression: an open case series.	2001 Jul	11518474
The frissonnant mutant mouse, a model of dopamino-sensitive, inherited motor syndrome.	2001 Jun	11442353
Warfarin and ropinirole interaction.	2001 Oct	11675845
Alterations in striatal neuropeptide mRNA produced by repeated administration of L-DOPA, ropinirole or bromocriptine correlate with dyskinesia induction in MPTP-treated common marmosets.	2002	12453478
Restless legs syndrome in the older adult: diagnosis and management.	2002	12390051
[Use of dopamine agonists in the treatment of Parkinson's disease].	2002	12378886
DA agonists -- non-ergot derivatives: ropinirole: management of Parkinson's disease.	2002	12211149
Choosing the right dopamine agonist for patients with Parkinson's disease.	2002	12201621
Two advances in the management of Parkinson disease.	2002 Aug	12184472
Effect of ropinirole on sleep onset: a randomized, placebo-controlled study in healthy volunteers.	2002 Feb 12	11839850
Long-term studies of dopamine agonists.	2002 Feb 26	11909984
Pergolide in the treatment of patients with early and advanced Parkinson's disease.	2002 Jan-Feb	11852289
GSK's Requip slow the loss of dopamine function in Parkinson's disease.	2002 Jul	12137117
Gateways to clinical trials.	2002 Jul-Aug	12224444
Effect of dopamine receptor agonists on sensory nerve activity: possible therapeutic targets for the treatment of asthma and COPD.	2002 Jun	12055141
[Multiple latency test in a patient with episodes of sleep induced by pergolide].	2002 Jun 16-30	12134281
Sleep attacks in patients taking dopamine agonists: review.	2002 Jun 22	12077032
Do dopamine agonists or levodopa modify Parkinson's disease progression?	2002 Nov	12464117
Ropinirole for antidepressant-induced sexual dysfunction.	2002 Nov	12409684
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. II. Agonist and antagonist properties at subtypes of dopamine D(2)-like receptor and alpha(1)/alpha(2)-adrenoceptor.	2002 Nov	12388667
Differential actions of antiparkinson agents at multiple classes of monoaminergic receptor. I. A multivariate analysis of the binding profiles of 14 drugs at 21 native and cloned human receptor subtypes.	2002 Nov	12388666
Practical importance of neuroprotection in Parkinson's disease.	2002 Oct	12522574
Dosing with ropinirole in a clinical setting.	2002 Oct	12225314
Do dopaminergic agents increase the daytime sleep propensity? Article reviewed: Effect of ropinirole on sleep onset. A randomized, placebo-controlled study in healthy volunteers.	2002 Sep	14592182
Combination of two different dopamine agonists in the management of Parkinson's disease.	2002 Sep	12548370
Gabapentin versus ropinirole in the treatment of idiopathic restless legs syndrome.	2003	14504416
Cabergoline, pramipexole and ropinirole used as monotherapy in early Parkinson's disease: an evidence-based comparison.	2003	12964891
Comparison of the risk of adverse events with pramipexole and ropinirole in patients with Parkinson's disease: a meta-analysis.	2003	12688834
Cost analysis of ropinirole versus levodopa in the treatment of Parkinson's disease.	2003	12515573
Sleep attacks--facts and fiction: a critical review.	2003	12442691
[Sexual delinquency and Parkinson's disease].	2003 Apr	12707708
Current status of Parkinson's disease treatment in Korea.	2003 Aug	12915074
Piribedil-induced sleep attacks in Parkinson's disease.	2003 Feb	12588638
Slowing Parkinson's disease progression: recent dopamine agonist trials.	2003 Feb 11	12580184
Ropinirole as an adjunct to levodopa in the treatment of Parkinson's disease A short commentary.	2003 Jan	12528000
Ropinirole as an adjunct to levodopa in the treatment of Parkinson's disease: a 16-week bromocriptine controlled study.	2003 Jan	12527999
Parkinson's disease: is the initial treatment established?	2003 Jul	12930698
REAL and CALM: what have we learned?	2003 Jul	12815670
The increased utilisation of dopamine agonists and the introduction of COMT inhibitors have not reduced levodopa consumption--a nation-wide perspective in Sweden.	2003 Jun	12781593
[Pseudopheochromocytoma in Parkinson disease and depression].	2003 May	14509040
The initial drug treatment of older patients with Parkinson's disease - consider an agonist, but don't demonise dopa.	2003 May	12720606
Dihydroergocriptine in Parkinson's disease: clinical efficacy and comparison with other dopamine agonists.	2003 May	12713527
Potent activation of dopamine D3/D2 heterodimers by the antiparkinsonian agents, S32504, pramipexole and ropinirole.	2003 Nov	14535946
Dopamine receptor agonists in current clinical use: comparative dopamine receptor binding profiles defined in the human striatum.	2003 Oct	14523624
Current treatment options for restless legs syndrome.	2003 Oct	14521483
Clinical strategies to prevent and delay motor complications.	2003 Sep 23	14504375

Patents

Sample Use Guides

In Vivo Use Guide

Parkinson Disease: 0.25 mg PO q8hr for 1 week initially, then increased weekly by 0.25 mg q8hr; if necessary, after week 4, may be increased weekly by 1.5 mg/day up to 9 mg/day, then increased weekly by 3 mg/day up to 24 mg/day Restless Leg Syndrome: 0.25 mg/day PO 1-3 hr before bedtime; after day 2, may be increased to 0.5 mg/day PO; at end of week 1, increased to 1 mg/day, then increased weekly by 0.5 mg/day up to 4 mg/day

Route of Administration: Oral

In Vitro Use Guide

Human SH-SY5Y neuroblastoma cells were grown to confluence in Dulbecco’s Modified Eagle’s media (DMEM) supplemented with 10% fetal calf serum, 100 mkg/mL penicillin, 100 mkg/mL streptomycin, 0.25 mkg/mL amphotericin B, and 0.01 mkM non-essential amino acids (Gibco Grand Island, NY, USA) and then sub-cultured for differentiation in 48 well Costar culture plates. For differentiation, the cells were grown in same media containing 10 mkM retinoic acid for 3 days; then the media was removed and replaced with media containing 160 nM of the phorbol ester 12-O-tetradecanoyl-phorbol-13-acetate (TPA) for 3 days of differentiation. The cells were then administered a range doses of pramipexole, ropinirole and S32504 (10 nM to 1 mM) in DMEM for three days prior to addition of 1 mM MPP+. Following transfer of MPP+ to the media cells were tested every 24 h for 72 h for the cytotoxicity of MPP+ as measured by the MTT and LDH assays which accurately measure different aspects of apoptosis. In addition, we tested for the neuroprotective effects of a fixed dose of each drug (50 mkM) and a range of doses of S32504 on MPP+ induced apoptosis, and the effects of ropinirole alone (1 mM) as measured by DNA laddering.

Substance Class	Chemical Created by `admin` on `Mon Mar 31 18:11:06 GMT 2025` Edited by `admin` on `Mon Mar 31 18:11:06 GMT 2025`
Record UNII	D7ZD41RZI9
Record Status	`Validated (UNII)`
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Name

Type

Language

ROPINIROLE HYDROCHLORIDE

Official Name

English

REQUIP

Preferred Name

English

ROPINIROLE HYDROCHLORIDE [MI]

Common Name

English

4-[2-(Dipropylamino)ethyl]-2-indolinone monohydrochloride

Systematic Name

English

ROPINIROLE HYDROCHLORIDE [USAN]

Common Name

English

ROPINIROLE (AS HYDROCHLORIDE)

Common Name

English

ROPINIROLE HYDROCHLORIDE [VANDF]

Common Name

English

2H-INDOL-2-ONE, 4-(2-(DIPROPYLAMINO)ETHYL)-1,3-DIHYDRO-, MONOHYDROCHLORIDE

Systematic Name

English

ROPINIROLE HYDROCHLORIDE [MART.]

Common Name

English

SK&F 101468-A

Code

English

ROPINIROLE HCL

Common Name

English

ROPINIROLE HYDROCHLORIDE [ORANGE BOOK]

Common Name

English

ROPINIROLE HYDROCHLORIDE [JAN]

Common Name

English

Ropinirole hydrochloride [WHO-DD]

Common Name

English

ROPINIROLE HYDROCHLORIDE [USP-RS]

Common Name

English

4-(2-(DIPROPYLAMINO)ETHYL)-1,3-DIHYDRO-2H-INDOL-2-ONE MONOHYDROCHLORIDE

Systematic Name

English

ROPINIROLE HYDROCHLORIDE [EP MONOGRAPH]

Common Name

English

ROPINIROLE HYDROCHLORIDE [USP MONOGRAPH]

Common Name

English

SK&F-101468-A

Code

English

SK&F-101468A

Common Name

English

Classification Tree Code System Code

NCI_THESAURUS

C38149