Peringatan Keamanan

Etoperidone presented major cardiovascular effects recorded as abnormal electrocardiogram, changes in blood pressure and even cardiac arrest. From the changes in blood pressure hypotension was the primary effect. These cardiovascular reactions are consistent with its effect to catecholamines.A31351

Etoperidone

DB09194

small molecule withdrawn

Deskripsi

Etoperidone is an atypical antidepressant introduced in Europe in 1977. It is a phenylpiperazine-substituted triazole derivative with a composition that classifies it as an analog of tradozone and presents a similar pharmacological profile.T45 Etoperidone was developed by Angelini Francesco ACRAF.A4909

Struktur Molekul 2D

Berat 377.92
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) After oral administration of etoperidone the terminal half-life was 21.7 hours.[A31350]
Volume Distribusi The high protein binding presented in etoperidone modulates its volume of distribution to a range of 0.23 to 0.69 L/kg.[A245129]
Klirens (Clearance) The apparent clearance of etoperidone was 1.01 ml/min.[A31350]

Absorpsi

The absorption and bioavailability is highly variable between individuals and can be as low as 12%. The lower bioavailability is explained due to its high metabolism.A31351 The mean time to peak plasma concentration is ranged from 1.4-4.8 hours.T49

Metabolisme

Etoperidone is highly metabolized and it forms 21 different metabolites that can be found in plasma, urine and faeces. The metabolism of etoperidone is thought to be related to 5 different reaction pathways that are alkyl oxidation, piperazinyl oxidation, N-dealkylation, phenyl hydroxylation and conjugation.A31350

Rute Eliminasi

The elimination of an oral dose of etoperidone presents a division of 78.8% found in urine and 9.6% found in faeces. On the elimination route, less than 0.01% of the etoperidone dose is represented by the unchanged drug while the rest is formed by 21 different metabolites.A31350

Interaksi Obat

1323 Data
Buprenorphine Etoperidone 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 Etoperidone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Etoperidone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Etoperidone.
Hydrocodone Etoperidone 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 Etoperidone.
Magnesium sulfate The therapeutic efficacy of Etoperidone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Etoperidone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Etoperidone may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Etoperidone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Etoperidone.
Orphenadrine Etoperidone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Etoperidone 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 Etoperidone.
Pramipexole Etoperidone may increase the sedative activities of Pramipexole.
Ropinirole Etoperidone may increase the sedative activities of Ropinirole.
Rotigotine Etoperidone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Etoperidone.
Sodium oxybate Etoperidone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Etoperidone 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 Etoperidone.
Thalidomide Etoperidone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Etoperidone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Etoperidone.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Etoperidone.
Dicoumarol The risk or severity of adverse effects can be increased when Etoperidone is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Etoperidone is combined with Phenindione.
Phenprocoumon The risk or severity of adverse effects can be increased when Etoperidone is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Etoperidone is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Etoperidone is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Etoperidone is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Etoperidone is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Etoperidone is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Etoperidone is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Etoperidone is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Etoperidone is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Etoperidone is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Etoperidone is combined with (S)-Warfarin.
Tedizolid phosphate The risk or severity of serotonin syndrome can be increased when Tedizolid phosphate is combined with Etoperidone.
Mirtazapine Etoperidone may increase the serotonergic activities of Mirtazapine.
Ethanol Etoperidone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Etoperidone 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 Etoperidone.
Fluvoxamine The risk or severity of adverse effects can be increased when Etoperidone is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Etoperidone is combined with Citalopram.
Duloxetine The risk or severity of adverse effects can be increased when Etoperidone is combined with Duloxetine.
Paroxetine The risk or severity of adverse effects can be increased when Etoperidone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Etoperidone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Etoperidone is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Etoperidone is combined with Nefazodone.
Zimelidine The risk or severity of adverse effects can be increased when Etoperidone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Etoperidone is combined with Dapoxetine.
Milnacipran The risk or severity of adverse effects can be increased when Etoperidone is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Etoperidone.
Seproxetine The risk or severity of adverse effects can be increased when Etoperidone is combined with Seproxetine.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Etoperidone is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Etoperidone is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Etoperidone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Etoperidone is combined with Alaproclate.
Methylene blue Etoperidone may increase the serotonergic activities of Methylene blue.
Benzatropine Benzatropine may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Disopyramide Disopyramide may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Clozapine The risk or severity of adverse effects can be increased when Etoperidone is combined with Clozapine.
Chlorpromazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Chlorpromazine.
Lamotrigine The risk or severity of CNS depression can be increased when Lamotrigine is combined with Etoperidone.
Propantheline Propantheline may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Dicyclomine Dicyclomine may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Maprotiline The risk or severity of adverse effects can be increased when Maprotiline is combined with Etoperidone.
Tolterodine Tolterodine may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Promethazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Promethazine.
Doxacurium The risk or severity of CNS depression can be increased when Doxacurium is combined with Etoperidone.
Flavoxate Flavoxate may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Quetiapine The risk or severity of adverse effects can be increased when Etoperidone is combined with Quetiapine.
Tiotropium Tiotropium may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Fesoterodine Fesoterodine may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Aclidinium Aclidinium may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Trimebutine Trimebutine may decrease the excretion rate of Etoperidone which could result in a higher serum level.
Imidafenacin Etoperidone may decrease the excretion rate of Imidafenacin which could result in a higher serum level.
Propiverine Etoperidone may decrease the excretion rate of Propiverine which could result in a higher serum level.
Amitriptyline The risk or severity of adverse effects can be increased when Amitriptyline is combined with Etoperidone.
Imipramine The risk or severity of adverse effects can be increased when Imipramine is combined with Etoperidone.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Etoperidone.
Desipramine The risk or severity of adverse effects can be increased when Desipramine is combined with Etoperidone.
Zopiclone The risk or severity of adverse effects can be increased when Etoperidone is combined with Zopiclone.
Sulpiride The risk or severity of adverse effects can be increased when Etoperidone is combined with Sulpiride.
Remoxipride The risk or severity of adverse effects can be increased when Etoperidone is combined with Remoxipride.
Prochlorperazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Prochlorperazine.
Triflupromazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Triflupromazine.
Fluphenazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Fluphenazine.
Moricizine The risk or severity of adverse effects can be increased when Etoperidone is combined with Moricizine.
Trifluoperazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Trifluoperazine.
Perphenazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Perphenazine.
Mesoridazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Mesoridazine.
Acetophenazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Acetophenazine.
Pimozide The risk or severity of adverse effects can be increased when Etoperidone is combined with Pimozide.
Chlorprothixene The risk or severity of adverse effects can be increased when Etoperidone is combined with Chlorprothixene.
Alimemazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Alimemazine.
Periciazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Periciazine.
Acepromazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Acepromazine.
Aceprometazine The risk or severity of adverse effects can be increased when Etoperidone is combined with Aceprometazine.

Target Protein

5-hydroxytryptamine receptor 2A HTR2A
5-hydroxytryptamine receptor 2C HTR2C
Alpha-1 adrenergic receptors ADRA1A
Alpha-2 adrenergic receptors ADRA2A
D(2) dopamine receptor DRD2
Muscarinic acetylcholine receptor CHRM1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 9537821
    Tatsumi M, Groshan K, Blakely RD, Richelson E: Pharmacological profile of antidepressants and related compounds at human monoamine transporters. Eur J Pharmacol. 1997 Dec 11;340(2-3):249-58.
  • PMID: 7855217
    Cusack B, Nelson A, Richelson E: Binding of antidepressants to human brain receptors: focus on newer generation compounds. Psychopharmacology (Berl). 1994 May;114(4):559-65.
  • PMID: 8386590
    Costa A, Martignoni E, Blandini F, Petraglia F, Genazzani AR, Nappi G: Effects of etoperidone on sympathetic and pituitary-adrenal responses to diverse stressors in humans. Clin Neuropharmacol. 1993 Apr;16(2):127-38.
  • PMID: 11765144
    Caldwell GW, Wu WN, Masucci JA: Evaluation of the absorption, excretion and metabolism of 14C etoperidone in man. Xenobiotica. 2001 Nov;31(11):823-39. doi: 10.1080/00498250110091758 .
  • PMID: 684760
    Lisciani R, Baldini A, Benedetti D, Campana A, Barcellona PS: Acute cardiovascular toxicity of trazodone, etoperidone and imipramine in rats. Toxicology. 1978 Jun;10(2):151-8.
  • PMID: -
    He H, Richardson S: Nefazodone: A Review of Its Neurochemical Mechanisms, Pharmacokinetics, and Therapeutic Use in Major Depressive Disorder CNS Drug Review. 2006 Sept 19;3(1):34-48.
Textbook
  • Ellis G.P. and West G.B. (1986). Progress in Medicinal Chemistry Volume 23 (pp. 159). Elsevier.
  • Morrison-Valfre M. (2016). Foundations of Mental Health Care (pp. 245). Elsevier .
  • Taylor and Francis (2000). Index Nominum 2000: International drug directory. Swiss Pharmaceutical Society.
  • O'Brien R.A. (1986). Receptor Binding in drug research. Marcel Dekker Inc..
  • Barceloux D.G. (2012). Medical toxicology of drug abuse: Synthesized chemicals and psychoactive plants.. Wiley.

Contoh Produk & Brand

Produk: 0 • International brands: 4
International Brands
  • Axiomin — Promeco
  • Depracer — L. Lepori, Lda.
  • Etoran — II Dong
  • Staff — Sigma-Tau

Sekuens Gen/Protein (FASTA)

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