Ropinirol

Ropinirol
(IUPAC) ime
	4-[2-(dipropilamino)etil]-1,3-dihidro-2H-indol-2-on
Klinički podaci
Robne marke	Requip
AHFS/Drugs.com	Monografija
MedlinePlus	a698013
Identifikatori
CAS broj	91374-21-9
ATC kod	N04BC04
PubChem	5095
DrugBank	APRD00302
ChemSpider	4916
UNII	030PYR8953
KEGG	D08489
ChEBI	CHEBI:8888
ChEMBL	CHEMBL589
Hemijski podaci
Formula	C16H24N2O
Mol. masa	260,375 g/mol
SMILES	eMolekuli & PubHem
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
Farmakokinetički podaci
Bioraspoloživost	50%
Metabolizam	Hepatički (CYP1A2)
Poluvreme eliminacije	5-6 sata
Farmakoinformacioni podaci
Trudnoća	?
Pravni status	℞ Prescription only
Način primene	Oralno

Ropinirol (INN) (Requip, Ropark, Adartrel) je dopaminski agonist. Ovaj lek proizvode kompanije GlaksoSmitKlajn (GSK), Cipla i Sun farmaceutikal. On se koristi u tretmanu Parkinsonove bolesti. Ropinirol je jedan od tri leka koje je FDA odobrila za lečenje sindroma nemirnih nogu. Druga dva su pramipeksol (Mirapeks) i gabapentin enakarbil (Horizant). Otkriće da je ovaj lek primenljiv u lečenju sindroma nemirnih nogu je korišćeno kao primer uspešne promene namene leka.^[7]

Patent na ropinirol je istekao maja 2008, te je ovaj lek dostupan u generičkom obliku.^[8]

Farmakologija

Ropinirol deluje kao agonist D₂, D₃, i D₄ dopaminskih receptora sa visokim afinitetom za D₂. On je u manjoj meri aktivan na 5-HT₂, i α₂ receptorima. On nema afiniteta za 5-HT₁, benzodiazepinski, GABA, muskarinski, α₁, i β-adrenoreceptore.^[9]

Ropinirol metabolizuje prvenstveno citohrom P450 CYP1A2, čime se formiraju dva metabolita; SK&F-104557 i SK&F-89124, oba od kojih se renalno uklanjaju.^[10] Pri dozama većim od kliničkih, on je takođe supstrat za CYP3A4, dok ori dozama većim od 24 mg, CYP2D6 može da bude inhibiran.^[6]

Izvori

↑ Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit
↑ Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.
↑ Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit
↑ Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.
↑ Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit
↑ ^6,0 ^6,1 ^6,2 ^6,3 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 (1. 8. 2008.). „Novel Approaches to Lead Optimization”. Genetic Engineering & Biotechnology News (Mary Ann Liebert) 28 (14): str. 20. ISSN 1935-472X. Pristupljeno 28. 9. 2008
↑ „New pharmaceutical products: Ceftriaxon-Rocephin, Granisetron-Kytril, Ipratropium-Albuterol”. Arhivirano iz originala na datum 2011-11-08. Pristupljeno 2014-04-05.
↑ 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.
↑ Debra J. Tompson, Deborah Hewens, Nancy Earl, David Oliveira, Jorg Taubel, Suzanne Swan, Luigi Giorgi. „An open-label, parallel-group, repeat-dose study to investigate the effects of end-stage renal disease and haemodialysis on the pharmacokinetics of ropinirole”. 13th International Congress of Parkinson’s Disease and Movement Disorders, Paris, France , June 7–11, 2009. Arhivirano iz originala na datum 2012-03-17. Pristupljeno 2014-04-05.

Povezano

Spoljašnje veze

	Portal Medicina
	Portal Hemija

Ropinirol zs sindrom nemirnih nogu Arhivirano 2010-01-07 na Wayback Machine-u
Ropinirol za Parkinsonovu bolest Arhivirano 2008-06-05 na Wayback Machine-u

[1] Li Q, Cheng T, Wang Y, Bryant SH (2010). „PubChem as a public resource for drug discovery.”. Drug Discov Today 15 (23-24): 1052-7. DOI:10.1016/j.drudis.2010.10.003. PMID 20970519. edit

[2] Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). „Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities”. Annual Reports in Computational Chemistry 4: 217-241. DOI:10.1016/S1574-1400(08)00012-1.

[3] Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). „Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining”. J Cheminform 2 (1): 3. DOI:10.1186/1758-2946-2-3. PMID 20331846. edit

[4] Joanne Wixon, Douglas Kell (2000). „Website Review: The Kyoto Encyclopedia of Genes and Genomes — KEGG”. Yeast 17 (1): 48–55. DOI:10.1002/(SICI)1097-0061(200004)17:1<48::AID-YEA2>3.0.CO;2-H.

[5] Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). „ChEMBL: a large-scale bioactivity database for drug discovery”. Nucleic Acids Res 40 (Database issue): D1100-7. DOI:10.1093/nar/gkr777. PMID 21948594. edit

[TompsonD-6] 6,0 ^6,1 ^6,2 ^6,3 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_GEN2008-7] Lipp Elizabeth (1. 8. 2008.). „Novel Approaches to Lead Optimization”. Genetic Engineering & Biotechnology News (Mary Ann Liebert) 28 (14): str. 20. ISSN 1935-472X. Pristupljeno 28. 9. 2008

[8] „New pharmaceutical products: Ceftriaxon-Rocephin, Granisetron-Kytril, Ipratropium-Albuterol”. Arhivirano iz originala na datum 2011-11-08. Pristupljeno 2014-04-05.

[RopPharmacology-9] 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.

[RPL-10] Debra J. Tompson, Deborah Hewens, Nancy Earl, David Oliveira, Jorg Taubel, Suzanne Swan, Luigi Giorgi. „An open-label, parallel-group, repeat-dose study to investigate the effects of end-stage renal disease and haemodialysis on the pharmacokinetics of ropinirole”. 13th International Congress of Parkinson’s Disease and Movement Disorders, Paris, France , June 7–11, 2009. Arhivirano iz originala na datum 2012-03-17. Pristupljeno 2014-04-05.

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