Rivastigmine

DB00989

small molecule approved investigational

Deskripsi

Rivastigmine is a parasympathomimetic or cholinergic agent for the treatment of mild to moderate dementia of the Alzheimer's type. Rivastigmine is a cholinesterase inhibitor that inhibits both butyrylcholinesterase and acetylcholinesterase.

Struktur Molekul 2D

Berat 250.3367
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 1.5 hours
Volume Distribusi * 1.8 to 2.7 L/kg
Klirens (Clearance) * renal cl=2.1-2.8 L/hr

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Rivastigmine is rapidly metabolized by cholinesterase-mediated hydrolysis.

Rute Eliminasi

Rivastigmine is extensively metabolized primarily via cholinesterase-mediated hydrolysis to the decarbamylated metabolite NAP226-90. Renal excretion of the metabolites is the major route of elimination. Less than 1% of the administered dose is excreted in the feces.

Interaksi Makanan

1 Data
  • 1. Take with food. Administering rivastigmine capsules with food delays absorption but increases the AUC.

Interaksi Obat

393 Data
Ceritinib Rivastigmine may increase the bradycardic activities of Ceritinib.
Ivabradine Rivastigmine may increase the bradycardic activities of Ivabradine.
Ruxolitinib Ruxolitinib may increase the bradycardic activities of Rivastigmine.
Esmolol Esmolol may increase the bradycardic activities of Rivastigmine.
Betaxolol Betaxolol may increase the bradycardic activities of Rivastigmine.
Metoprolol Metoprolol may increase the bradycardic activities of Rivastigmine.
Atenolol Atenolol may increase the bradycardic activities of Rivastigmine.
Timolol Timolol may increase the bradycardic activities of Rivastigmine.
Sotalol Sotalol may increase the bradycardic activities of Rivastigmine.
Propranolol Propranolol may increase the bradycardic activities of Rivastigmine.
Labetalol Labetalol may increase the bradycardic activities of Rivastigmine.
Bisoprolol Bisoprolol may increase the bradycardic activities of Rivastigmine.
Alprenolol Alprenolol may increase the bradycardic activities of Rivastigmine.
Pindolol Pindolol may increase the bradycardic activities of Rivastigmine.
Carvedilol Carvedilol may increase the bradycardic activities of Rivastigmine.
Propafenone Propafenone may increase the bradycardic activities of Rivastigmine.
Acebutolol Acebutolol may increase the bradycardic activities of Rivastigmine.
Nadolol Nadolol may increase the bradycardic activities of Rivastigmine.
Bevantolol Bevantolol may increase the bradycardic activities of Rivastigmine.
Practolol Practolol may increase the bradycardic activities of Rivastigmine.
Penbutolol Penbutolol may increase the bradycardic activities of Rivastigmine.
Oxprenolol Oxprenolol may increase the bradycardic activities of Rivastigmine.
Dexpropranolol Dexpropranolol may increase the bradycardic activities of Rivastigmine.
Celiprolol Celiprolol may increase the bradycardic activities of Rivastigmine.
Nebivolol Nebivolol may increase the bradycardic activities of Rivastigmine.
Bufuralol Bufuralol may increase the bradycardic activities of Rivastigmine.
Bopindolol Bopindolol may increase the bradycardic activities of Rivastigmine.
Bupranolol Bupranolol may increase the bradycardic activities of Rivastigmine.
Indenolol Indenolol may increase the bradycardic activities of Rivastigmine.
Arotinolol Arotinolol may increase the bradycardic activities of Rivastigmine.
Levobetaxolol Levobetaxolol may increase the bradycardic activities of Rivastigmine.
Talinolol Talinolol may increase the bradycardic activities of Rivastigmine.
Anisodamine Anisodamine may increase the bradycardic activities of Rivastigmine.
Bucindolol Bucindolol may increase the bradycardic activities of Rivastigmine.
Esatenolol Esatenolol may increase the bradycardic activities of Rivastigmine.
Cloranolol Cloranolol may increase the bradycardic activities of Rivastigmine.
Mepindolol Mepindolol may increase the bradycardic activities of Rivastigmine.
Epanolol Epanolol may increase the bradycardic activities of Rivastigmine.
Tertatolol Tertatolol may increase the bradycardic activities of Rivastigmine.
Landiolol Landiolol may increase the bradycardic activities of Rivastigmine.
Dipyridamole The therapeutic efficacy of Rivastigmine can be decreased when used in combination with Dipyridamole.
Ephedrine Rivastigmine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Rivastigmine may increase the neuromuscular blocking activities of Bambuterol.
Sar9, Met (O2)11-Substance P Rivastigmine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Mirabegron Rivastigmine may increase the neuromuscular blocking activities of Mirabegron.
Moxisylyte Rivastigmine may increase the neuromuscular blocking activities of Moxisylyte.
Procaine Rivastigmine may increase the neuromuscular blocking activities of Procaine.
Cocaine Rivastigmine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Rivastigmine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Rivastigmine may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Rivastigmine may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Rivastigmine may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Rivastigmine may increase the neuromuscular blocking activities of Aclidinium.
Clevidipine Rivastigmine may increase the neuromuscular blocking activities of Clevidipine.
Propacetamol Rivastigmine may increase the neuromuscular blocking activities of Propacetamol.
Butyrylthiocholine Rivastigmine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Oxybuprocaine Rivastigmine may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Rivastigmine may increase the neuromuscular blocking activities of Benzonatate.
Metoclopramide The risk or severity of adverse effects can be increased when Rivastigmine is combined with Metoclopramide.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Rivastigmine.
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Rivastigmine.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Rivastigmine.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Rivastigmine.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Rivastigmine.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Rivastigmine.
Benzatropine The therapeutic efficacy of Benzatropine can be decreased when used in combination with Rivastigmine.
Ziprasidone The therapeutic efficacy of Ziprasidone can be decreased when used in combination with Rivastigmine.
Disopyramide The therapeutic efficacy of Disopyramide can be decreased when used in combination with Rivastigmine.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Rivastigmine.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Rivastigmine.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Rivastigmine.
Olanzapine The therapeutic efficacy of Olanzapine can be decreased when used in combination with Rivastigmine.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Rivastigmine.
Buclizine The therapeutic efficacy of Buclizine can be decreased when used in combination with Rivastigmine.
Clozapine The therapeutic efficacy of Clozapine can be decreased when used in combination with Rivastigmine.
Doxylamine The therapeutic efficacy of Doxylamine can be decreased when used in combination with Rivastigmine.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Rivastigmine.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Rivastigmine.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Rivastigmine.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Rivastigmine.
Secobarbital The therapeutic efficacy of Secobarbital can be decreased when used in combination with Rivastigmine.
Promazine The therapeutic efficacy of Promazine can be decreased when used in combination with Rivastigmine.
Hyoscyamine The therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Rivastigmine.
Cyproheptadine The therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Rivastigmine.
Methscopolamine bromide The therapeutic efficacy of Methscopolamine bromide can be decreased when used in combination with Rivastigmine.
Metharbital The therapeutic efficacy of Metharbital can be decreased when used in combination with Rivastigmine.
Fluoxetine The therapeutic efficacy of Fluoxetine can be decreased when used in combination with Rivastigmine.
Chlorpromazine The therapeutic efficacy of Chlorpromazine can be decreased when used in combination with Rivastigmine.
Tridihexethyl The therapeutic efficacy of Tridihexethyl can be decreased when used in combination with Rivastigmine.
Triflupromazine The therapeutic efficacy of Triflupromazine can be decreased when used in combination with Rivastigmine.
Dextromethorphan The therapeutic efficacy of Dextromethorphan can be decreased when used in combination with Rivastigmine.
Anisotropine methylbromide The therapeutic efficacy of Anisotropine methylbromide can be decreased when used in combination with Rivastigmine.
Amoxapine The therapeutic efficacy of Amoxapine can be decreased when used in combination with Rivastigmine.
Lamotrigine Lamotrigine may increase the bradycardic activities of Rivastigmine.
Atropine The therapeutic efficacy of Atropine can be decreased when used in combination with Rivastigmine.
Thiopental The therapeutic efficacy of Thiopental can be decreased when used in combination with Rivastigmine.
Nicardipine The therapeutic efficacy of Nicardipine can be decreased when used in combination with Rivastigmine.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Rivastigmine.
Pirenzepine The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Rivastigmine.
Paroxetine The therapeutic efficacy of Paroxetine can be decreased when used in combination with Rivastigmine.

Target Protein

Acetylcholinesterase ACHE
Cholinesterase BCHE

Referensi & Sumber

Synthesis reference: Venkata Naga Brahmeswara Rao Mandava, Venkata Reddy Vajrala, Ganesh Varanasi, Vijay Kumar Adla, Mukund Reddy Jambula, Vijaypal Reddy Kanumathi Reddy, "PREPARATION OF RIVASTIGMINE AND ITS SALTS." U.S. Patent US20080255383, issued October 16, 2008.
Artikel (PubMed)
  • PMID: 12369954
    Camps P, Munoz-Torrero D: Cholinergic drugs in pharmacotherapy of Alzheimer's disease. Mini Rev Med Chem. 2002 Feb;2(1):11-25.
  • PMID: 10066203
    Rosler M, Anand R, Cicin-Sain A, Gauthier S, Agid Y, Dal-Bianco P, Stahelin HB, Hartman R, Gharabawi M: Efficacy and safety of rivastigmine in patients with Alzheimer's disease: international randomised controlled trial. BMJ. 1999 Mar 6;318(7184):633-8.
  • PMID: 15336465
    Finkel SI: Effects of rivastigmine on behavioral and psychological symptoms of dementia in Alzheimer's disease. Clin Ther. 2004 Jul;26(7):980-90.
  • PMID: 11568422
    Rosler M, Retz W, Retz-Junginger P, Dennler HJ: Effects of two-year treatment with the cholinesterase inhibitor rivastigmine on behavioural symptoms in Alzheimer's disease. Behav Neurol. 1998;11(4):211-216.
  • PMID: 15590953
    Emre M, Aarsland D, Albanese A, Byrne EJ, Deuschl G, De Deyn PP, Durif F, Kulisevsky J, van Laar T, Lees A, Poewe W, Robillard A, Rosa MM, Wolters E, Quarg P, Tekin S, Lane R: Rivastigmine for dementia associated with Parkinson's disease. N Engl J Med. 2004 Dec 9;351(24):2509-18.
  • PMID: 19370562
    Birks J, Grimley Evans J, Iakovidou V, Tsolaki M, Holt FE: Rivastigmine for Alzheimer's disease. Cochrane Database Syst Rev. 2009 Apr 15;(2):CD001191. doi: 10.1002/14651858.CD001191.pub2.
  • PMID: 19470293
    Naik RS, Hartmann J, Kiewert C, Duysen EG, Lockridge O, Klein J: Effects of rivastigmine and donepezil on brain acetylcholine levels in acetylcholinesterase-deficient mice. J Pharm Pharm Sci. 2009;12(1):79-85.
  • PMID: 14587496
    Farlow MR: Update on rivastigmine. Neurologist. 2003 Sep;9(5):230-4.

Contoh Produk & Brand

Produk: 452 • International brands: 1
Produk
  • Act Rivastigmine Patch 10
    Patch • 18 mg / 10 sq cm • Transdermal • Canada • Approved
  • Act Rivastigmine Patch 5
    Patch • 9 mg / 5 sq cm • Transdermal • Canada • Approved
  • Apo-rivastigmine
    Capsule • 1.5 mg • Oral • Canada • Generic • Approved
  • Apo-rivastigmine
    Capsule • 3 mg • Oral • Canada • Generic • Approved
  • Apo-rivastigmine
    Capsule • 4.5 mg • Oral • Canada • Generic • Approved
  • Apo-rivastigmine
    Capsule • 6 mg • Oral • Canada • Generic • Approved
  • Auro-rivastigmine
    Capsule • 1.5 mg • Oral • Canada • Generic • Approved
  • Auro-rivastigmine
    Capsule • 3 mg • Oral • Canada • Generic • Approved
Menampilkan 8 dari 452 produk.
International Brands
  • Exelon Patch

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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