Peringatan Keamanan

The most likely symptoms of overdose would be those related to the pharmacodynamic profile of a dopamine agonist, including nausea, vomiting, hypotension, involuntary movements, hallucinations, confusion, convulsions, and other signs of excessive dopaminergic stimulation.

Rotigotine

DB05271

small molecule approved

Deskripsi

Rotigotine (Neupro) is a non-ergoline dopamine agonist indicated for the treatment of Parkinson's disease (PD) and restless legs syndrome (RLS) in Europe and the United States. It is formulated as a once-daily transdermal patch which provides a slow and constant supply of the drug over the course of 24 hours.

Like other dopamine agonists, rotigotine has been shown to possess antidepressant effects and may be useful in the treatment of depression as well.

Rotigotine was developed by Aderis Pharmaceuticals. In 1998 Aderis licensed worldwide development and commercialization rights to Schwarz Pharma of Germany. It was approved by the European Medicines Agency in 2006 and by the FDA in 2007. However, all Neupro patches in the United States and some of Europe were recalled in 2008 due to delivery mechanism issues. Rotigotine has been authorized as a treatment for RLS since August 2008.

Struktur Molekul 2D

Berat 315.48
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) After removal of the patch, plasma levels decreased with a terminal half-life of 5 to 7 hours. The pharmacokinetic profile showed a biphasic elimination with an initial half-life of 3 hours.
Volume Distribusi The weight normalized apparent volume of distribution, (Vd/F), in humans is approximately 84 L/kg after repeated dose administration.
Klirens (Clearance) -

Absorpsi

Bioavailability varies depending on the application site. Differences in bioavailability were very small between the abdomen and hip (<1%). In contrast, the shoulder and thigh had a very large different in measured bioavailability (46%), with the shoulder showing the higher value. Tmax, 8 mg dose = 15 - 18 hours (it take approximately 3 hours until rotigotine reaches detectable levels in the plasma). The peak concentration cannot be observered. Steady state is reached in 2-3 days.

Metabolisme

Hepatic (CYP-mediated). Rotigotine is extensively and rapidly metabolized by conjugation and N-dealkylation. After intravenous dosing the predominant metabolites in human plasma are sulfate conjugates of rotigotine, glucuronide conjugates of rotigotine, sulfate conjugates of the N-despropyl-rotigotine and conjugates of N-desthienylethyl-rotigotine. Multiple CYP isoenzymes, sulfotransferases and two UDP-glucuronosyltransferases catalyze the metabolism of rotigotine.

Rute Eliminasi

Urine (71%), Fecal (23%). Most of rotigotine that is excreted in the urine is in the form of inactive conjugates. Unchanged drug made up less <1%.

Interaksi Obat

1359 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Rotigotine is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Rotigotine is combined with Levodopa.
Risperidone Rotigotine may increase the hypotensive activities of Risperidone.
Furosemide Rotigotine may decrease the antihypertensive activities of Furosemide.
Valsartan Rotigotine may decrease the antihypertensive activities of Valsartan.
Ramipril Rotigotine may decrease the antihypertensive activities of Ramipril.
Remikiren Rotigotine may decrease the antihypertensive activities of Remikiren.
Torasemide Rotigotine may decrease the antihypertensive activities of Torasemide.
Bethanidine Rotigotine may decrease the antihypertensive activities of Bethanidine.
Guanadrel Rotigotine may decrease the antihypertensive activities of Guanadrel.
Olmesartan Rotigotine may decrease the antihypertensive activities of Olmesartan.
Chlorthalidone Rotigotine may decrease the antihypertensive activities of Chlorthalidone.
Nitroprusside Rotigotine may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Rotigotine may decrease the antihypertensive activities of Minoxidil.
Treprostinil Rotigotine may decrease the antihypertensive activities of Treprostinil.
Bendroflumethiazide Rotigotine may decrease the antihypertensive activities of Bendroflumethiazide.
Prazosin Rotigotine may decrease the antihypertensive activities of Prazosin.
Fosinopril Rotigotine may decrease the antihypertensive activities of Fosinopril.
Trandolapril Rotigotine may decrease the antihypertensive activities of Trandolapril.
Metolazone Rotigotine may decrease the antihypertensive activities of Metolazone.
Benazepril Rotigotine may decrease the antihypertensive activities of Benazepril.
Enalapril Rotigotine may decrease the antihypertensive activities of Enalapril.
Cyclothiazide Rotigotine may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Rotigotine may decrease the antihypertensive activities of Candoxatril.
Guanabenz Rotigotine may decrease the antihypertensive activities of Guanabenz.
Mecamylamine Rotigotine may decrease the antihypertensive activities of Mecamylamine.
Moexipril Rotigotine may decrease the antihypertensive activities of Moexipril.
Phentolamine Rotigotine may decrease the antihypertensive activities of Phentolamine.
Lisinopril Rotigotine may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Rotigotine may decrease the antihypertensive activities of Nitroglycerin.
Hydroflumethiazide Rotigotine may decrease the antihypertensive activities of Hydroflumethiazide.
Cryptenamine Rotigotine may decrease the antihypertensive activities of Cryptenamine.
Perindopril Rotigotine may decrease the antihypertensive activities of Perindopril.
Candesartan cilexetil Rotigotine may decrease the antihypertensive activities of Candesartan cilexetil.
Tolazoline Rotigotine may decrease the antihypertensive activities of Tolazoline.
Eprosartan Rotigotine may decrease the antihypertensive activities of Eprosartan.
Chlorothiazide Rotigotine may decrease the antihypertensive activities of Chlorothiazide.
Quinapril Rotigotine may decrease the antihypertensive activities of Quinapril.
Omapatrilat Rotigotine may decrease the antihypertensive activities of Omapatrilat.
Phenoxybenzamine Rotigotine may decrease the antihypertensive activities of Phenoxybenzamine.
Telmisartan Rotigotine may decrease the antihypertensive activities of Telmisartan.
Methyldopa Rotigotine may decrease the antihypertensive activities of Methyldopa.
Hydrochlorothiazide Rotigotine may decrease the antihypertensive activities of Hydrochlorothiazide.
Trichlormethiazide Rotigotine may decrease the antihypertensive activities of Trichlormethiazide.
Deserpidine Rotigotine may decrease the antihypertensive activities of Deserpidine.
Pentolinium Rotigotine may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Rotigotine may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Rotigotine may decrease the antihypertensive activities of Diazoxide.
Bretylium Rotigotine may decrease the antihypertensive activities of Bretylium.
Terazosin Rotigotine may decrease the antihypertensive activities of Terazosin.
Rescinnamine Rotigotine may decrease the antihypertensive activities of Rescinnamine.
Epoprostenol Rotigotine may decrease the antihypertensive activities of Epoprostenol.
Polythiazide Rotigotine may decrease the antihypertensive activities of Polythiazide.
Cilazapril Rotigotine may decrease the antihypertensive activities of Cilazapril.
Saprisartan Rotigotine may decrease the antihypertensive activities of Saprisartan.
Spirapril Rotigotine may decrease the antihypertensive activities of Spirapril.
Dexpropranolol Rotigotine may decrease the antihypertensive activities of Dexpropranolol.
Tienilic acid Rotigotine may decrease the antihypertensive activities of Tienilic acid.
Diethylnorspermine Rotigotine may decrease the antihypertensive activities of Diethylnorspermine.
Temocapril Rotigotine may decrease the antihypertensive activities of Temocapril.
Indoramin Rotigotine may decrease the antihypertensive activities of Indoramin.
Trimazosin Rotigotine may decrease the antihypertensive activities of Trimazosin.
Moxonidine Rotigotine may decrease the antihypertensive activities of Moxonidine.
Rauwolfia serpentina root Rotigotine may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Rotigotine may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Rotigotine may decrease the antihypertensive activities of Angiotensin 1-7.
Rilmenidine Rotigotine may decrease the antihypertensive activities of Rilmenidine.
Imidapril Rotigotine may decrease the antihypertensive activities of Imidapril.
BQ-123 Rotigotine may decrease the antihypertensive activities of BQ-123.
Cicletanine Rotigotine may decrease the antihypertensive activities of Cicletanine.
Dihydralazine Rotigotine may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Rotigotine may decrease the antihypertensive activities of Zofenopril.
Guanoxan Rotigotine may decrease the antihypertensive activities of Guanoxan.
Delapril Rotigotine may decrease the antihypertensive activities of Delapril.
Vincamine Rotigotine may decrease the antihypertensive activities of Vincamine.
Linsidomine Rotigotine may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Rotigotine may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Rotigotine may decrease the antihypertensive activities of Tolonidine.
Endralazine Rotigotine may decrease the antihypertensive activities of Endralazine.
Cadralazine Rotigotine may decrease the antihypertensive activities of Cadralazine.
Cyclopenthiazide Rotigotine may decrease the antihypertensive activities of Cyclopenthiazide.
Bietaserpine Rotigotine may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Rotigotine may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Rotigotine may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Rotigotine may decrease the antihypertensive activities of Guanoclor.
Muzolimine Rotigotine may decrease the antihypertensive activities of Muzolimine.
Xipamide Rotigotine may decrease the antihypertensive activities of Xipamide.
Candesartan Rotigotine may decrease the antihypertensive activities of Candesartan.
Tocopherylquinone Rotigotine may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Rotigotine may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Rotigotine may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Rotigotine may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Rotigotine may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Rotigotine may decrease the antihypertensive activities of Quinaprilat.
Captopril Rotigotine may decrease the antihypertensive activities of Captopril.
Guanethidine Rotigotine may decrease the antihypertensive activities of Guanethidine.
Amlodipine Rotigotine may decrease the antihypertensive activities of Amlodipine.
Nimodipine Rotigotine may decrease the antihypertensive activities of Nimodipine.
Nisoldipine Rotigotine may decrease the antihypertensive activities of Nisoldipine.
Bosentan Rotigotine may decrease the antihypertensive activities of Bosentan.

Target Protein

D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
D(2) dopamine receptor DRD2
D(1B) dopamine receptor DRD5
D(1A) dopamine receptor DRD1
5-hydroxytryptamine receptor 1A HTR1A
Alpha-2B adrenergic receptor ADRA2B

Referensi & Sumber

Synthesis reference: Hans-Michael Wolff, Luc Quere, Jens Riedner, "NOVEL POLYMORPHIC FORM OF ROTIGOTINE AND PROCESS FOR PRODUCTION." U.S. Patent US20090143460, issued June 04, 2009.
Artikel (PubMed)
  • PMID: 17935234
    Giladi N, Boroojerdi B, Korczyn AD, Burn DJ, Clarke CE, Schapira AH: Rotigotine transdermal patch in early Parkinson's disease: a randomized, double-blind, controlled study versus placebo and ropinirole. Mov Disord. 2007 Dec;22(16):2398-404.
  • PMID: 19947805
    Chen JJ, Swope DM, Dashtipour K, Lyons KE: Transdermal rotigotine: a clinically innovative dopamine-receptor agonist for the management of Parkinson's disease. Pharmacotherapy. 2009 Dec;29(12):1452-67. doi: 10.1592/phco.29.12.1452.
  • PMID: 22320451
    Perez-Lloret S, Rey MV, Ratti PL, Rascol O: Rotigotine transdermal patch for the treatment of Parkinson's Disease. Fundam Clin Pharmacol. 2013 Feb;27(1):81-95. doi: 10.1111/j.1472-8206.2012.01028.x. Epub 2012 Feb 9.
  • PMID: 22808933
    de Biase S, Merlino G, Lorenzut S, Valente M, Gigli GL: ADMET considerations for restless leg syndrome drug treatments. Expert Opin Drug Metab Toxicol. 2012 Oct;8(10):1247-61. doi: 10.1517/17425255.2012.708023. Epub 2012 Jul 18.

Contoh Produk & Brand

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