Peringatan Keamanan

The onset of impairment of consciousness is relatively rapid in benzodiazepine poisoning. Onset is more rapid following larger doses and with agents of shorter duration of action. The most common and initial symptom is somnolence. This may progress to coma (Grade I or Grade II) following very large ingestions. Oral, rat LD50 is 825 mg/kg.

Tofisopam

DB08811

small molecule experimental

Deskripsi

Tofisopam (marketed under brand names Emandaxin and Grandaxin) is a 2,3-benzodiazepine drug which is a benzodiazepine derivative. In contrast to classical 1,4-benzodiazepines, the compound does not bind to the benzodiazepine binding site of the gamma-aminobutyric acid receptor and its psychopharmacological profile differs from such compounds. Although Tofisopam is not approved for sale in North America, it is approved for use in various countries worldwide, including parts of Europe. The D-enantiomer (dextofisopam) is currently in phase II trials in the U.S. for the treatment of irritable bowel syndrome.

Struktur Molekul 2D

Berat 382.4528
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 6-8 hours
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Hepatic.

Rute Eliminasi

Data eliminasi belum tersedia.

Interaksi Obat

699 Data
Buprenorphine Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Buprenorphine.
Doxylamine Doxylamine may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Dronabinol The serum concentration of Dronabinol can be increased when it is combined with Tofisopam.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Hydrocodone Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Hydroxyzine Hydroxyzine may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Magnesium sulfate The therapeutic efficacy of Tofisopam can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Tofisopam may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Mirtazapine Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Mirtazapine.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Orphenadrine Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Paraldehyde.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Pramipexole Tofisopam may increase the sedative activities of Pramipexole.
Ropinirole Tofisopam may increase the sedative activities of Ropinirole.
Rotigotine Tofisopam may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Tofisopam.
Sodium oxybate Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Suvorexant.
Tapentadol Tapentadol may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Thalidomide Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Yohimbine The therapeutic efficacy of Tofisopam can be increased when used in combination with Yohimbine.
Eliglustat The metabolism of Eliglustat can be decreased when combined with Tofisopam.
Ibrutinib The metabolism of Ibrutinib can be decreased when combined with Tofisopam.
Cilostazol The metabolism of Cilostazol can be decreased when combined with Tofisopam.
Colchicine The metabolism of Colchicine can be decreased when combined with Tofisopam.
Fentanyl The risk or severity of CNS depression can be increased when Fentanyl is combined with Tofisopam.
Iloperidone The metabolism of Iloperidone can be decreased when combined with Tofisopam.
Retapamulin The metabolism of Retapamulin can be decreased when combined with Tofisopam.
Tofacitinib The metabolism of Tofacitinib can be decreased when combined with Tofisopam.
Vardenafil The metabolism of Vardenafil can be decreased when combined with Tofisopam.
Zopiclone The metabolism of Zopiclone can be decreased when combined with Tofisopam.
Lovastatin The metabolism of Lovastatin can be decreased when combined with Tofisopam.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Tofisopam.
Alfuzosin The metabolism of Alfuzosin can be decreased when combined with Tofisopam.
Alprazolam The metabolism of Alprazolam can be decreased when combined with Tofisopam.
Warfarin The serum concentration of Warfarin can be increased when it is combined with Tofisopam.
Acenocoumarol The serum concentration of Acenocoumarol can be increased when it is combined with Tofisopam.
(R)-warfarin The serum concentration of (R)-warfarin can be increased when it is combined with Tofisopam.
R,S-Warfarin alcohol The serum concentration of R,S-Warfarin alcohol can be increased when it is combined with Tofisopam.
S,R-Warfarin alcohol The serum concentration of S,R-Warfarin alcohol can be increased when it is combined with Tofisopam.
(S)-Warfarin The serum concentration of (S)-Warfarin can be increased when it is combined with Tofisopam.
Dicoumarol The risk or severity of adverse effects can be increased when Tofisopam is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Tofisopam is combined with Phenindione.
Coumarin The risk or severity of adverse effects can be increased when Tofisopam is combined with Coumarin.
Tioclomarol The risk or severity of adverse effects can be increased when Tofisopam is combined with Tioclomarol.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Tofisopam is combined with Ethyl biscoumacetate.
Diphenadione The risk or severity of adverse effects can be increased when Tofisopam is combined with Diphenadione.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Tofisopam is combined with 4-hydroxycoumarin.
Fluindione The risk or severity of adverse effects can be increased when Tofisopam is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Tofisopam is combined with Clorindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Tofisopam is combined with Phenprocoumon.
Midazolam The serum concentration of Midazolam can be increased when it is combined with Tofisopam.
Tacrolimus The serum concentration of Tacrolimus can be increased when it is combined with Tofisopam.
Atorvastatin The metabolism of Atorvastatin can be decreased when combined with Tofisopam.
Ethanol Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Tofisopam may increase the central nervous system depressant (CNS depressant) activities of Azelastine.
Brimonidine Brimonidine may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Zimelidine The risk or severity of adverse effects can be increased when Tofisopam is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Tofisopam is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Tofisopam is combined with Seproxetine.
Fluvoxamine The risk or severity of adverse effects can be increased when Tofisopam is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Tofisopam is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Tofisopam is combined with Duloxetine.
Trazodone The risk or severity of adverse effects can be increased when Tofisopam is combined with Trazodone.
Paroxetine The risk or severity of adverse effects can be increased when Tofisopam is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Tofisopam is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Tofisopam is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Tofisopam is combined with Nefazodone.
Escitalopram The risk or severity of adverse effects can be increased when Tofisopam is combined with Escitalopram.
Milnacipran The risk or severity of adverse effects can be increased when Tofisopam is combined with Milnacipran.
Desvenlafaxine The risk or severity of adverse effects can be increased when Tofisopam is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Tofisopam is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Tofisopam is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Tofisopam is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Tofisopam is combined with Alaproclate.
Cyproheptadine The risk or severity of CNS depression can be increased when Cyproheptadine is combined with Tofisopam.
Propiomazine The risk or severity of CNS depression can be increased when Propiomazine is combined with Tofisopam.
Amitriptyline The risk or severity of CNS depression can be increased when Amitriptyline is combined with Tofisopam.
Imipramine The risk or severity of CNS depression can be increased when Imipramine is combined with Tofisopam.
Doxepin The risk or severity of CNS depression can be increased when Doxepin is combined with Tofisopam.
Olanzapine The risk or severity of CNS depression can be increased when Olanzapine is combined with Tofisopam.
Clozapine The serum concentration of Clozapine can be increased when it is combined with Tofisopam.
Nortriptyline The risk or severity of CNS depression can be increased when Nortriptyline is combined with Tofisopam.
Botulinum toxin type B The risk or severity of CNS depression can be increased when Botulinum toxin type B is combined with Tofisopam.
Botulinum toxin type A The risk or severity of CNS depression can be increased when Botulinum toxin type A is combined with Tofisopam.
Baclofen Baclofen may increase the central nervous system depressant (CNS depressant) activities of Tofisopam.
Ethchlorvynol The risk or severity of CNS depression can be increased when Ethchlorvynol is combined with Tofisopam.
Succinylcholine The risk or severity of CNS depression can be increased when Succinylcholine is combined with Tofisopam.
Enflurane The risk or severity of CNS depression can be increased when Enflurane is combined with Tofisopam.
Butabarbital The risk or severity of CNS depression can be increased when Butabarbital is combined with Tofisopam.
Butalbital The risk or severity of CNS depression can be increased when Butalbital is combined with Tofisopam.
Topiramate The risk or severity of CNS depression can be increased when Topiramate is combined with Tofisopam.
Clemastine The risk or severity of CNS depression can be increased when Clemastine is combined with Tofisopam.
Etomidate The risk or severity of CNS depression can be increased when Etomidate is combined with Tofisopam.
Talbutal The risk or severity of CNS depression can be increased when Talbutal is combined with Tofisopam.
Pentobarbital The risk or severity of CNS depression can be increased when Pentobarbital is combined with Tofisopam.

Target Protein

cAMP and cAMP-inhibited cGMP 3',5'-cyclic phosphodiesterase 10A PDE10A
3',5'-cyclic-AMP phosphodiesterase 4A PDE4A
cGMP-dependent 3',5'-cyclic phosphodiesterase PDE2A
cGMP-inhibited 3',5'-cyclic phosphodiesterase 3A PDE3A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 20967473
    Rundfeldt C, Socala K, Wlaz P: The atypical anxiolytic drug, tofisopam, selectively blocks phosphodiesterase isoenzymes and is active in the mouse model of negative symptoms of psychosis. J Neural Transm (Vienna). 2010 Nov;117(11):1319-25. doi: 10.1007/s00702-010-0507-3. Epub 2010 Oct 22.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Emandaxin
  • Grandaxin

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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