塩酸ロピニロール

関: ropinirole

WordNet

a complex consisting of an organic base in association with hydrogen chloride

Wikipedia preview

出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/11/20 23:24:04」(JST)

wiki en

Ropinirole (INN; trade names Requip, Ronirol, Adartrel) is a dopamine agonist of the non-ergoline class of medications. It is manufactured by GlaxoSmithKline (GSK), Cipla, Dr. Reddy's Laboratories and Sun Pharmaceutical. It is used in the treatment of Parkinson's disease and restless legs syndrome (RLS). Ropinirole is one of three medications approved by the FDA to treat Restless Legs Syndrome (RLS), the other two being pramipexole (Mirapex) and gabapentin enacarbil (Horizant). The discovery of the drug's utility in RLS has been used as a successful example of drug repurposing.^[2]

Ropinirole's patent expired in May 2008, and the drug is now available in generic form.^[3]

Medical uses[edit]

Ropinirole is prescribed for mainly Parkinson's disease, restless leg syndrome, and extrapyramidal symptoms. It can also reduce the side effects caused by selective serotonin reuptake inhibitors, including Parkinsonism syndrome as well as sexual dysfunction and erectile dysfunction caused by either SSRIs^[4] or antipsychotics.

Dosage[edit]

Ropinirole in the Requip form is available in various preparations, ranging from a 0.25 mg tablet to a 5 mg tablet. The primary reason is dose titration. This implies that the person taking Requip has to closely interact and communicate with the primary care physician with regard to how much should actually be taken by the patient.

For restless leg syndrome (RLS), the maximum recommended dose is 4 mg per day, taken 1 to 3 hours before bedtime. A 52-week open label study had a mean dosage of 1.90 mg, once daily 1 to 3 hours before bedtime.^[5]

For Parkinson's disease (PD), the maximum recommended dose is 24 mg per day, taken in three separate doses spread throughout the day. The maximum dose recommendations of ropinirole for subjects with end stage renal disease (ESRD) should be reduced by 25% compared with those recommended for subjects with normal renal function. A 25% dose reduction represents a more straightforward dosage regimen in terms of available tablet strength, compared with a 30% dose reduction.^[6]

Pharmacology[edit]

Ropinirole acts as a D₂, D₃, and D₄ dopamine receptor agonist with highest affinity for D₂. It is weakly active at the 5-HT₂, and α₂ receptors and is said to have virtually no affinity for the 5-HT₁, benzodiazepine, GABA, muscarinic, α₁, and β-adrenoreceptors.^[7]

Ropinirole is metabolized primarily by cytochrome P450 CYP1A2 to form two metabolites; SK&F-104557 and SK&F-89124, both of which are renally excreted,^[6] and at doses higher than clinical, is also metabolized by CYP3A4. At doses greater than 24 mg, CYP2D6 may be inhibited, although this has only been tested in vitro.^[1]

Side effects[edit]

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 prior history of these behaviours.^[8]

Lawsuits[edit]

In November 2012, GlaxoSmithKline was ordered by a Rennes, France appeals court to pay Frenchman Didier Jambart 197,000 euros ($255,824); Jambart had taken ropinirole from 2003 to 2010 and exhibited risky hypersexual behavior and gambled excessively until stopping the Parkinson's treatment.^[9]

References[edit]

^ ^a ^b ^c ^d Tompson, Debra J. et al. (2007). "Steady-State Pharmacokinetic Properties of a 24-Hour Prolonged-Release Formulation of Ropinirole: Results of Two Randomized Studies in Patients with Parkinson’s Disease". Clinical Pharmacokinetics 29 (12): 2654. doi:10.1016/j.clinthera.2007.12.010. PMID 18201581.
^ Lipp, Elizabeth (2008-08-01). "Novel Approaches to Lead Optimization". Genetic Engineering & Biotechnology News. Drug Discovery 28 (14) (Mary Ann Liebert). p. 20. ISSN 1935-472X. Retrieved 2008-09-28 Note: The opinion that ropinirole's use in RLS was a successful example of drug repurposes was reported as being that of Josef Scheiber, a post-doctoral fellow at the Novartis Institutes for BioMedical Research.
^ New pharmaceutical products: Ceftriaxon-Rocephin, Granisetron-Kytril, Ipratropium-Albuterol
^ ClinicalTrials.gov NCT00334048 - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"
^ Garcia-Borreguero D, Grunstein R, Sridhar G, et al. (November 2007). "A 52-week open-label study of the long-term safety of ropinirole in patients with restless leg syndrome". Sleep Med. 8 (7–8): 742–52. doi:10.1016/j.sleep.2006.09.009. PMID 17512789.
^ ^a ^b An open-label, parallel-group, repeat-dose study to investigate the effects of end-stage renal disease and haemodialysis on the pharmacokinetics of ropinirole | Authors: Debra J. Tompson, Deborah Hewens, Nancy Earl, David Oliveira, Jorg Taubel, Suzanne Swan, Luigi Giorgi | 13th International Congress of Parkinson’s Disease and Movement Disorders, Paris, France, June 7–11, 2009
^ Eden, R. J. et al. (1991). "Preclinical Pharmacology of Ropinirole (SK&F 101468-A) a Novel Dopamine D 2 Agonist". Pharmacology Biochemistry & Behavior 38: 147–154. doi:10.1016/0091-3057(91)90603-Y.
^ Bostwick JM, Hecksel KA, Stevens SR, Bower JH, Ahlskog JE (2009). "Frequency of new-onset pathologic compulsive gambling or hypersexuality after drug treatment of idiopathic Parkinson disease". Mayo Clinic Proceedings 84 (4): 310–6. doi:10.4065/84.4.310. PMC 2665974. PMID 19339647.
^ http://www.huffingtonpost.com/2012/11/29/didier-jambart-parkinsons-drug-gay-sex-addict-glaxosmithkline_n_2212348.html

External links[edit]

Requip for RLS
Requip for PD
Requip - Clinical Pharmacology

UpToDate Contents

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1. パーキンソン病に対する神経保護療法 neuroprotective therapy for parkinson disease
2. Treatment of restless legs syndrome/Willis-Ekbom disease and periodic limb movement disorder in adults
3. 多系統萎縮症：予後および治療 multiple system atrophy prognosis and treatment
4. パーキンソン病の薬理学的治療 pharmacologic treatment of parkinson disease
5. 成人における単極性大うつ病：刺激薬および stimulant-like drugsによる抗うつ薬の増強 unipolar major depression in adults augmentation of antidepressants with stimulants and stimulant like drugs

English Journal

Assessment of ropinirole as a reinforcer in rhesus monkeys.

Freeman KB, Heal DJ, McCreary AC, Woolverton WL.SourceDivision of Neurobiology and Behavior Research, Department of Psychiatry and Human Behavior, The University of Mississippi Medical Center, Jackson, MS 39216, USA.
Drug and alcohol dependence.Drug Alcohol Depend.2012 Sep 1;125(1-2):173-7. Epub 2012 Apr 28.
BACKGROUND: Ropinirole, a D(2)/D(3)/5-HT(1A) agonist, is used for the treatment of Parkinson's disease and restless leg syndrome, and is currently being evaluated as a treatment for cocaine dependence. However, there is little information available on ropinirole's reinforcing effects.METHODS: The cu
PMID 22546848

Therapies in Parkinson's disease.

Jankovic J, Poewe W.SourceaDepartment of Neurology, Parkinson's Disease Center and Movement Disorders Clinic, Baylor College of Medicine, Houston, Texas, USA bUniversitätsklinik für Neurologie, Innsbruck Medical University, Innsbruck, Austria.
Current opinion in neurology.Curr Opin Neurol.2012 Aug;25(4):433-47.
PURPOSE OF REVIEW: This review examines currently available therapeutic strategies for Parkinson's disease, emphasizing evidence-based data as well as a patient-centered approach to the treatment of motor and nonmotor symptoms.RECENT FINDINGS: Although clinical trials of disease-modifying approaches
PMID 22691758

Japanese Journal

レビー小体型認知症の行動と心理症状に対するドパミン・アゴニストの有用性について

江原嵩,近藤典子,長岡研太郎
臨床精神医学 38(2), 219-226, 2009-02
NAID 40016478351

パーキンソン病治療薬ロピニロール塩酸塩(レキップ^【○!R】錠)の薬理作用と臨床効果

新井裕幸,南順子
日本薬理学雑誌 : FOLIA PHARMACOLOGICA JAPONICA 130(4), 313-319, 2007-10-01
ロピニロール塩酸塩（以下，ロピニロール）は非麦角系ドパミン受容体アゴニストであり，D2受容体ファミリー（D2，D3，D4）に高い選択性を示す．ロピニロールはマーモセットの1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine（MPTP）誘発運動障害に対して改善作用を示し，その作用は反復投与により減弱しなかった．また，中脳腹側被蓋野を破壊したサルの振戦を速やかに抑制 …
NAID 10020167589

Related Pictures

★リンクテーブル★

リンク元	「ロピニロール」
関連記事	「hydrochloride」

「ロピニロール」

Ropinirole
Systematic (IUPAC) name
	4-[2-(dipropylamino)ethyl]-1,3-dihydro-2H-indol-2-one
Clinical data
Trade names	Requip
AHFS/Drugs.com	monograph
MedlinePlus	a698013
Pregnancy cat.	C
Legal status	℞ Prescription only
Routes	Oral
Pharmacokinetic data
Bioavailability	50%
Metabolism	Hepatic (CYP1A2)
Half-life	5-6 hours
Identifiers
CAS number	91374-21-9
ATC code	N04BC04
PubChem	CID 5095
DrugBank	DB00268
ChemSpider	4916
UNII	030PYR8953
KEGG	D08489
ChEBI	CHEBI:8888
ChEMBL	CHEMBL589
Chemical data
Formula	C16H24N2O
Mol. mass	260.375 g/mol
	SMILES O=C2Nc1cccc(c1C2)CCN(CCC)CCC;
	InChI InChI=1S/C16H24N2O/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) ; Key:UHSKFQJFRQCDBE-UHFFFAOYSA-N ;
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　　[★]

英: ropinirole
化: 塩酸ロピニロール ropinirole hydrochloride
商: レキップCR、レキップ
関: 抗パーキンソン剤

「hydrochloride」

　　[★] 塩酸塩、ハイドロクロライド　

[TompsonD-1] Tompson, Debra J. et al. (2007). "Steady-State Pharmacokinetic Properties of a 24-Hour Prolonged-Release Formulation of Ropinirole: Results of Two Randomized Studies in Patients with Parkinson’s Disease". Clinical Pharmacokinetics 29 (12): 2654. doi:10.1016/j.clinthera.2007.12.010. PMID 18201581.

[Lipp_GEN2008-2] Lipp, Elizabeth (2008-08-01). "Novel Approaches to Lead Optimization". Genetic Engineering & Biotechnology News. Drug Discovery 28 (14) (Mary Ann Liebert). p. 20. ISSN 1935-472X. Retrieved 2008-09-28 Note: The opinion that ropinirole's use in RLS was a successful example of drug repurposes was reported as being that of Josef Scheiber, a post-doctoral fellow at the Novartis Institutes for BioMedical Research.

[3] New pharmaceutical products: Ceftriaxon-Rocephin, Granisetron-Kytril, Ipratropium-Albuterol

[4] ClinicalTrials.gov NCT00334048 - "Treating Sexual Dysfunction From SSRI Medication: a Study Comparing Requip CR to Placebo"

[52wkOpenLabel-5] Garcia-Borreguero D, Grunstein R, Sridhar G, et al. (November 2007). "A 52-week open-label study of the long-term safety of ropinirole in patients with restless leg syndrome". Sleep Med. 8 (7–8): 742–52. doi:10.1016/j.sleep.2006.09.009. PMID 17512789.

[RPL-6] An open-label, parallel-group, repeat-dose study to investigate the effects of end-stage renal disease and haemodialysis on the pharmacokinetics of ropinirole | Authors: Debra J. Tompson, Deborah Hewens, Nancy Earl, David Oliveira, Jorg Taubel, Suzanne Swan, Luigi Giorgi | 13th International Congress of Parkinson’s Disease and Movement Disorders, Paris, France, June 7–11, 2009

[RopPharmacology-7] Eden, R. J. et al. (1991). "Preclinical Pharmacology of Ropinirole (SK&F 101468-A) a Novel Dopamine D 2 Agonist". Pharmacology Biochemistry & Behavior 38: 147–154. doi:10.1016/0091-3057(91)90603-Y.

[8] Bostwick JM, Hecksel KA, Stevens SR, Bower JH, Ahlskog JE (2009). "Frequency of new-onset pathologic compulsive gambling or hypersexuality after drug treatment of idiopathic Parkinson disease". Mayo Clinic Proceedings 84 (4): 310–6. doi:10.4065/84.4.310. PMC 2665974. PMID 19339647.

[9] ttp://www.huffingtonpost.com/2012/11/29/didier-jambart-parkinsons-drug-gay-sex-addict-glaxosmithkline_n_2212348.html

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案内

ropinirole hydrochloride