Peringatan Keamanan

Overdosage with cholinesterase inhibitors can cause a cholinergic crisis characterized by severe nausea/vomiting, salivation, sweating, bradycardia, hypotension, collapse, and convulsions. Increasing muscle weakness is a possibility and may result in death if respiratory muscles are involved. The estimated median lethal dose of tacrine following a single oral dose in rats is 40 mg/kg, or approximately 12 times the maximum recommended human dose of 160 mg/day.

Tacrine

DB00382

small molecule approved investigational withdrawn

Deskripsi

A centerally active cholinesterase inhibitor that has been used to counter the effects of muscle relaxants, as a respiratory stimulant, and in the treatment of Alzheimer's disease and other central nervous system disorders. Tacrine has been discontinued for the United States market.

Struktur Molekul 2D

Berat 198.2637
Wujud solid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) 2 to 4 hours
Volume Distribusi * 349 ± 193 L
Klirens (Clearance) -

Absorpsi

Tacrine is rapidly absorbed. Absolute bioavailability of tacrine is approximately 17%.

Metabolisme

Hepatic. Cytochrome P450 1A2 is the principal isozyme involved in tacrine metabolism. The major metabolite, 1-hydroxy-tacrine (velnacrine), has central cholinergic activity.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Makanan

1 Data
  • 1. Take on an empty stomach. Take tacrine at least one hour before meals for optimal absorption.

Interaksi Obat

663 Data
Deferasirox The serum concentration of Tacrine can be increased when it is combined with Deferasirox.
Peginterferon alfa-2b The serum concentration of Tacrine can be increased when it is combined with Peginterferon alfa-2b.
Leflunomide The serum concentration of Tacrine can be decreased when it is combined with Leflunomide.
Teriflunomide The serum concentration of Tacrine can be decreased when it is combined with Teriflunomide.
Dipyridamole The therapeutic efficacy of Tacrine can be decreased when used in combination with Dipyridamole.
Ephedrine Tacrine may increase the neuromuscular blocking activities of Ephedrine.
Bambuterol Tacrine may increase the neuromuscular blocking activities of Bambuterol.
Clevidipine Tacrine may increase the neuromuscular blocking activities of Clevidipine.
Sar9, Met (O2)11-Substance P Tacrine may increase the neuromuscular blocking activities of Sar9, Met (O2)11-Substance P.
Moxisylyte Tacrine may increase the neuromuscular blocking activities of Moxisylyte.
Procaine Tacrine may increase the neuromuscular blocking activities of Procaine.
Cocaine Tacrine may increase the neuromuscular blocking activities of Cocaine.
Trimethaphan Tacrine may increase the neuromuscular blocking activities of Trimethaphan.
Doxacurium Tacrine may increase the neuromuscular blocking activities of Doxacurium.
Chloroprocaine Tacrine may increase the neuromuscular blocking activities of Chloroprocaine.
Tubocurarine Tacrine may increase the neuromuscular blocking activities of Tubocurarine.
Aclidinium Tacrine may increase the neuromuscular blocking activities of Aclidinium.
Butyrylthiocholine Tacrine may increase the neuromuscular blocking activities of Butyrylthiocholine.
Mirabegron Tacrine may increase the neuromuscular blocking activities of Mirabegron.
Oxybuprocaine Tacrine may increase the neuromuscular blocking activities of Oxybuprocaine.
Benzonatate Tacrine may increase the neuromuscular blocking activities of Benzonatate.
Succinylcholine The metabolism of Succinylcholine can be decreased when combined with Tacrine.
Abiraterone The serum concentration of Tacrine can be increased when it is combined with Abiraterone.
Cyproterone acetate The metabolism of Tacrine can be increased when combined with Cyproterone acetate.
Tramadol The therapeutic efficacy of Tramadol can be decreased when used in combination with Tacrine.
Trospium The therapeutic efficacy of Trospium can be decreased when used in combination with Tacrine.
Oxyphenonium The therapeutic efficacy of Oxyphenonium can be decreased when used in combination with Tacrine.
Butabarbital The therapeutic efficacy of Butabarbital can be decreased when used in combination with Tacrine.
Butalbital The therapeutic efficacy of Butalbital can be decreased when used in combination with Tacrine.
Benzatropine The therapeutic efficacy of Benzatropine can be decreased when used in combination with Tacrine.
Ziprasidone The therapeutic efficacy of Ziprasidone can be decreased when used in combination with Tacrine.
Talbutal The therapeutic efficacy of Talbutal can be decreased when used in combination with Tacrine.
Pentobarbital The therapeutic efficacy of Pentobarbital can be decreased when used in combination with Tacrine.
Ipratropium The therapeutic efficacy of Ipratropium can be decreased when used in combination with Tacrine.
Methadone The therapeutic efficacy of Methadone can be decreased when used in combination with Tacrine.
Metixene The therapeutic efficacy of Metixene can be decreased when used in combination with Tacrine.
Terfenadine The therapeutic efficacy of Terfenadine can be decreased when used in combination with Tacrine.
Buclizine The therapeutic efficacy of Buclizine can be decreased when used in combination with Tacrine.
Doxylamine The therapeutic efficacy of Doxylamine can be decreased when used in combination with Tacrine.
Trihexyphenidyl The therapeutic efficacy of Trihexyphenidyl can be decreased when used in combination with Tacrine.
Oxyphencyclimine The therapeutic efficacy of Oxyphencyclimine can be decreased when used in combination with Tacrine.
Procyclidine The therapeutic efficacy of Procyclidine can be decreased when used in combination with Tacrine.
Profenamine The therapeutic efficacy of Profenamine can be decreased when used in combination with Tacrine.
Hyoscyamine The therapeutic efficacy of Hyoscyamine can be decreased when used in combination with Tacrine.
Cyproheptadine The therapeutic efficacy of Cyproheptadine can be decreased when used in combination with Tacrine.
Methscopolamine bromide The therapeutic efficacy of Methscopolamine bromide can be decreased when used in combination with Tacrine.
Metharbital The therapeutic efficacy of Metharbital can be decreased when used in combination with Tacrine.
Darifenacin The therapeutic efficacy of Darifenacin can be decreased when used in combination with Tacrine.
Tridihexethyl The therapeutic efficacy of Tridihexethyl can be decreased when used in combination with Tacrine.
Triflupromazine The therapeutic efficacy of Triflupromazine can be decreased when used in combination with Tacrine.
Dextromethorphan The therapeutic efficacy of Dextromethorphan can be decreased when used in combination with Tacrine.
Anisotropine methylbromide The therapeutic efficacy of Anisotropine methylbromide can be decreased when used in combination with Tacrine.
Amoxapine The therapeutic efficacy of Amoxapine can be decreased when used in combination with Tacrine.
Atropine The therapeutic efficacy of Atropine can be decreased when used in combination with Tacrine.
Thiopental The therapeutic efficacy of Thiopental can be decreased when used in combination with Tacrine.
Nicardipine The therapeutic efficacy of Nicardipine can be decreased when used in combination with Tacrine.
Mecamylamine The therapeutic efficacy of Mecamylamine can be decreased when used in combination with Tacrine.
Pirenzepine The therapeutic efficacy of Pirenzepine can be decreased when used in combination with Tacrine.
Homatropine methylbromide The therapeutic efficacy of Homatropine methylbromide can be decreased when used in combination with Tacrine.
Scopolamine The therapeutic efficacy of Scopolamine can be decreased when used in combination with Tacrine.
Isoflurane The therapeutic efficacy of Isoflurane can be decreased when used in combination with Tacrine.
Benzquinamide The therapeutic efficacy of Benzquinamide can be decreased when used in combination with Tacrine.
Clidinium The therapeutic efficacy of Clidinium can be decreased when used in combination with Tacrine.
Propiomazine The therapeutic efficacy of Propiomazine can be decreased when used in combination with Tacrine.
Propantheline The therapeutic efficacy of Propantheline can be decreased when used in combination with Tacrine.
Dicyclomine The therapeutic efficacy of Dicyclomine can be decreased when used in combination with Tacrine.
Biperiden The therapeutic efficacy of Biperiden can be decreased when used in combination with Tacrine.
Brompheniramine The therapeutic efficacy of Brompheniramine can be decreased when used in combination with Tacrine.
Methylphenobarbital The therapeutic efficacy of Methylphenobarbital can be decreased when used in combination with Tacrine.
Amantadine The therapeutic efficacy of Amantadine can be decreased when used in combination with Tacrine.
Methantheline The therapeutic efficacy of Methantheline can be decreased when used in combination with Tacrine.
Hexafluronium The therapeutic efficacy of Hexafluronium can be decreased when used in combination with Tacrine.
Cycrimine The therapeutic efficacy of Cycrimine can be decreased when used in combination with Tacrine.
Desloratadine The therapeutic efficacy of Desloratadine can be decreased when used in combination with Tacrine.
Glycopyrronium The therapeutic efficacy of Glycopyrronium can be decreased when used in combination with Tacrine.
Tolterodine The therapeutic efficacy of Tolterodine can be decreased when used in combination with Tacrine.
Oxybutynin The therapeutic efficacy of Oxybutynin can be decreased when used in combination with Tacrine.
Promethazine The therapeutic efficacy of Promethazine can be decreased when used in combination with Tacrine.
Diphenhydramine The therapeutic efficacy of Diphenhydramine can be decreased when used in combination with Tacrine.
Pentolinium The therapeutic efficacy of Pentolinium can be decreased when used in combination with Tacrine.
Flavoxate The therapeutic efficacy of Flavoxate can be decreased when used in combination with Tacrine.
Escitalopram The therapeutic efficacy of Escitalopram can be decreased when used in combination with Tacrine.
Quetiapine The therapeutic efficacy of Quetiapine can be decreased when used in combination with Tacrine.
Levacetylmethadol The therapeutic efficacy of Levacetylmethadol can be decreased when used in combination with Tacrine.
Diphenidol The therapeutic efficacy of Diphenidol can be decreased when used in combination with Tacrine.
Aripiprazole The therapeutic efficacy of Aripiprazole can be decreased when used in combination with Tacrine.
Chlorprothixene The therapeutic efficacy of Chlorprothixene can be decreased when used in combination with Tacrine.
Fenoterol The therapeutic efficacy of Fenoterol can be decreased when used in combination with Tacrine.
Amobarbital The therapeutic efficacy of Amobarbital can be decreased when used in combination with Tacrine.
Aprobarbital The therapeutic efficacy of Aprobarbital can be decreased when used in combination with Tacrine.
Butobarbital The therapeutic efficacy of Butobarbital can be decreased when used in combination with Tacrine.
Heptabarbital The therapeutic efficacy of Heptabarbital can be decreased when used in combination with Tacrine.
Hexobarbital The therapeutic efficacy of Hexobarbital can be decreased when used in combination with Tacrine.
Methotrimeprazine The therapeutic efficacy of Methotrimeprazine can be decreased when used in combination with Tacrine.
Tiotropium The therapeutic efficacy of Tiotropium can be decreased when used in combination with Tacrine.
Barbital The therapeutic efficacy of Barbital can be decreased when used in combination with Tacrine.
Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione The therapeutic efficacy of Dihydro-2-thioxo-5-((5-(2-(trifluoromethyl)phenyl)-2-furanyl)methyl)-4,6(1H,5H)-pyrimidinedione can be decreased when used in combination with Tacrine.
Solifenacin The therapeutic efficacy of Solifenacin can be decreased when used in combination with Tacrine.
Isopropamide The therapeutic efficacy of Isopropamide can be decreased when used in combination with Tacrine.
Mepenzolate The therapeutic efficacy of Mepenzolate can be decreased when used in combination with Tacrine.

Target Protein

Cholinesterase BCHE
Acetylcholinesterase ACHE
Liver carboxylesterase 1 CES1

Referensi & Sumber

Synthesis reference: S. Shirley Yang, Wayne Boisvert, Nouman A. Muhammad, Jay Weiss, "Controlled release tacrine drug delivery systems and methods for preparing same." U.S. Patent US5576022, issued February, 1993.
Artikel (PubMed)
  • PMID: 9842955
    Qizilbash N, Whitehead A, Higgins J, Wilcock G, Schneider L, Farlow M: Cholinesterase inhibition for Alzheimer disease: a meta-analysis of the tacrine trials. Dementia Trialists' Collaboration. JAMA. 1998 Nov 25;280(20):1777-82.
  • PMID: 20480924
    Hansen RA, Gartlehner G, Kaufer DJ, Lohr KN, Carey T: Drug Class Review: Alzheimer's Drugs: Final Report Internet .

Contoh Produk & Brand

Produk: 4 • International brands: 1
Produk
  • Cognex
    Capsule • 10 mg/1 • Oral • US • Approved
  • Cognex
    Capsule • 20 mg/1 • Oral • US • Approved
  • Cognex
    Capsule • 30 mg/1 • Oral • US • Approved
  • Cognex
    Capsule • 40 mg/1 • Oral • US • Approved
International Brands
  • Talem — LKM

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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