Peringatan Keamanan

Ld50 in rats, 48 mg/kg L1520.
Prolonged Qtc interval. Monitoring with regular ECGs is recommended L1525.

Pipamperone

DB09286

small molecule investigational

Deskripsi

Pipamperone is a typical antipsychotic of the butyrophenone family used in the treatment of schizophrenia. It was developed by Janssen Pharmaceutica in 1961 and started its first round of clinical trials in 1963 L1514, L1518.

In an effort to improve haloperidol's pharmacological effects, Janssen discovered that pipamperone, an agent whose pharmacological profile was distinct from haloperidol and all other known antipsychotic drugs at this time, had significant anti-tryptamine activity. Some studies suggest pipamperone was the first atypical antipsychotic. Interestingly, when risperidone was created, Janssen suggested it was a more potent version of pipamperone. Synthesized in the year 1984, risperidone’s pharmacological properties were similar to pipamperone’s in that both block more serotonin more potently than dopamine L1518.

Struktur Molekul 2D

Berat 375.488
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) 17-26h [L1522]
Volume Distribusi -
Klirens (Clearance) -

Absorpsi

Data absorpsi tidak tersedia.

Metabolisme

Pipamperone is metabolised in the liver L1514.

Rute Eliminasi

Mainly via the kidneys L1514

Interaksi Obat

959 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Pipamperone is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Pipamperone is combined with Levodopa.
Risperidone Pipamperone may increase the hypotensive activities of Risperidone.
Buprenorphine Pipamperone 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 Pipamperone.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Pipamperone.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Pipamperone.
Hydrocodone Pipamperone 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 Pipamperone.
Magnesium sulfate The therapeutic efficacy of Pipamperone can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Pipamperone may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Pipamperone.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Pipamperone.
Orphenadrine Pipamperone may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Pipamperone 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 Pipamperone.
Rotigotine Pipamperone may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Pipamperone.
Sodium oxybate Pipamperone may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Pipamperone 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 Pipamperone.
Thalidomide Pipamperone may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Pipamperone may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amisulpride Pipamperone may increase the antipsychotic activities of Amisulpride.
Methylphenidate The risk or severity of adverse effects can be increased when Pipamperone is combined with Methylphenidate.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Pipamperone.
Metyrosine Pipamperone may increase the sedative activities of Metyrosine.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Pipamperone.
Sulpiride Pipamperone may increase the antipsychotic activities of Sulpiride.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Pipamperone.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Pipamperone.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Pipamperone.
Mequitazine Pipamperone may increase the arrhythmogenic activities of Mequitazine.
Linezolid The risk or severity of serotonin syndrome can be increased when Linezolid is combined with Pipamperone.
Dicoumarol The risk or severity of adverse effects can be increased when Pipamperone is combined with Dicoumarol.
Phenindione The risk or severity of adverse effects can be increased when Pipamperone is combined with Phenindione.
Warfarin The risk or severity of adverse effects can be increased when Pipamperone is combined with Warfarin.
Phenprocoumon The risk or severity of adverse effects can be increased when Pipamperone is combined with Phenprocoumon.
Acenocoumarol The risk or severity of adverse effects can be increased when Pipamperone is combined with Acenocoumarol.
4-hydroxycoumarin The risk or severity of adverse effects can be increased when Pipamperone is combined with 4-hydroxycoumarin.
Coumarin The risk or severity of adverse effects can be increased when Pipamperone is combined with Coumarin.
(R)-warfarin The risk or severity of adverse effects can be increased when Pipamperone is combined with (R)-warfarin.
Ethyl biscoumacetate The risk or severity of adverse effects can be increased when Pipamperone is combined with Ethyl biscoumacetate.
Fluindione The risk or severity of adverse effects can be increased when Pipamperone is combined with Fluindione.
Clorindione The risk or severity of adverse effects can be increased when Pipamperone is combined with Clorindione.
Diphenadione The risk or severity of adverse effects can be increased when Pipamperone is combined with Diphenadione.
Tioclomarol The risk or severity of adverse effects can be increased when Pipamperone is combined with Tioclomarol.
(S)-Warfarin The risk or severity of adverse effects can be increased when Pipamperone is combined with (S)-Warfarin.
Mirtazapine Pipamperone may increase the serotonergic activities of Mirtazapine.
Nicorandil Nicorandil may increase the hypotensive activities of Pipamperone.
Ethanol Pipamperone may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Pipamperone 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 Pipamperone.
Zimelidine The risk or severity of adverse effects can be increased when Pipamperone is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Pipamperone is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Pipamperone is combined with Seproxetine.
Fluvoxamine The risk or severity of adverse effects can be increased when Pipamperone is combined with Fluvoxamine.
Citalopram The risk or severity of adverse effects can be increased when Pipamperone is combined with Citalopram.
Paroxetine The risk or severity of adverse effects can be increased when Pipamperone is combined with Paroxetine.
Sertraline The risk or severity of adverse effects can be increased when Pipamperone is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Pipamperone is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Pipamperone is combined with Nefazodone.
Milnacipran The risk or severity of adverse effects can be increased when Pipamperone is combined with Milnacipran.
Desvenlafaxine The risk or severity of serotonin syndrome can be increased when Desvenlafaxine is combined with Pipamperone.
Levomilnacipran The risk or severity of serotonin syndrome can be increased when Pipamperone is combined with Levomilnacipran.
Indalpine The risk or severity of adverse effects can be increased when Pipamperone is combined with Indalpine.
Ritanserin The risk or severity of adverse effects can be increased when Pipamperone is combined with Ritanserin.
Alaproclate The risk or severity of adverse effects can be increased when Pipamperone is combined with Alaproclate.
Methylene blue Pipamperone may increase the serotonergic activities of Methylene blue.
Tolcapone The therapeutic efficacy of Pipamperone can be decreased when used in combination with Tolcapone.
Entacapone The therapeutic efficacy of Pipamperone can be decreased when used in combination with Entacapone.
Testosterone propionate The therapeutic efficacy of Pipamperone can be decreased when used in combination with Testosterone propionate.
3,5-Dinitrocatechol The therapeutic efficacy of Pipamperone can be decreased when used in combination with 3,5-Dinitrocatechol.
Quercetin The therapeutic efficacy of Pipamperone can be decreased when used in combination with Quercetin.
Opicapone The therapeutic efficacy of Pipamperone can be decreased when used in combination with Opicapone.
Nicardipine The risk or severity of adverse effects can be increased when Nicardipine is combined with Pipamperone.
Zopiclone The risk or severity of adverse effects can be increased when Pipamperone is combined with Zopiclone.
Butalbital Butalbital may increase the hypotensive activities of Pipamperone.
Pentobarbital Pentobarbital may increase the hypotensive activities of Pipamperone.
Secobarbital Secobarbital may increase the hypotensive activities of Pipamperone.
Methohexital Methohexital may increase the hypotensive activities of Pipamperone.
Thiopental Thiopental may increase the hypotensive activities of Pipamperone.
Primidone Primidone may increase the hypotensive activities of Pipamperone.
Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Pipamperone.
Thiamylal Thiamylal may increase the hypotensive activities of Pipamperone.
Phenobarbital Phenobarbital may increase the hypotensive activities of Pipamperone.
Amobarbital Amobarbital may increase the hypotensive activities of Pipamperone.
Hexobarbital Hexobarbital may increase the hypotensive activities of Pipamperone.
Barbital Barbital may increase the hypotensive activities of Pipamperone.
Barbexaclone Barbexaclone may increase the hypotensive activities of Pipamperone.
Bromocriptine The risk or severity of adverse effects can be increased when Bromocriptine is combined with Pipamperone.
Lorpiprazole The risk or severity of adverse effects can be increased when Lorpiprazole is combined with Pipamperone.
Methylenedioxyethamphetamine Pipamperone may decrease the stimulatory activities of Methylenedioxyethamphetamine.
Amphetamine Pipamperone may decrease the stimulatory activities of Amphetamine.
Phendimetrazine Pipamperone may decrease the stimulatory activities of Phendimetrazine.
Aldesleukin The risk or severity of adverse effects can be increased when Aldesleukin is combined with Pipamperone.
Streptokinase The risk or severity of adverse effects can be increased when Streptokinase is combined with Pipamperone.
Methyclothiazide The risk or severity of adverse effects can be increased when Methyclothiazide is combined with Pipamperone.
Triamterene The risk or severity of adverse effects can be increased when Triamterene is combined with Pipamperone.
Spironolactone The risk or severity of adverse effects can be increased when Spironolactone is combined with Pipamperone.

Target Protein

D(2) dopamine receptor DRD2
5-hydroxytryptamine receptor 2A HTR2A
Alpha-1 adrenergic receptors ADRA1A
D(4) dopamine receptor DRD4
D(1A) dopamine receptor DRD1
D(3) dopamine receptor DRD3
5-hydroxytryptamine receptor 2B HTR2B
Alpha-2A adrenergic receptor ADRA2A

Referensi & Sumber

Artikel (PubMed)
  • PMID: 10657547
    Prinssen EP, Koek W, Kleven MS: The effects of antipsychotics with 5-HT(2C) receptor affinity in behavioral assays selective for 5-HT(2C) receptor antagonist properties of compounds. Eur J Pharmacol. 2000 Jan 24;388(1):57-67.
  • PMID: 8632342
    Wainscott DB, Lucaites VL, Kursar JD, Baez M, Nelson DL: Pharmacologic characterization of the human 5-hydroxytryptamine2B receptor: evidence for species differences. J Pharmacol Exp Ther. 1996 Feb;276(2):720-7.
  • PMID: 8935801
    Schotte A, Janssen PF, Gommeren W, Luyten WH, Van Gompel P, Lesage AS, De Loore K, Leysen JE: Risperidone compared with new and reference antipsychotic drugs: in vitro and in vivo receptor binding. Psychopharmacology (Berl). 1996 Mar;124(1-2):57-73.
  • PMID: 21349239
    Wade AG, Crawford GM, Nemeroff CB, Schatzberg AF, Schlaepfer T, McConnachie A, Haazen L, Buntinx E: Citalopram plus low-dose pipamperone versus citalopram plus placebo in patients with major depressive disorder: an 8-week, double-blind, randomized study on magnitude and timing of clinical response. Psychol Med. 2011 Oct;41(10):2089-97. doi: 10.1017/S0033291711000158. Epub 2011 Feb 25.
  • PMID: 17535043
    Gareri P, De Fazio P, Stilo M, Ferreri G, De Sarro G: Conventional and atypical antipsychotics in the elderly : a review. Clin Drug Investig. 2003;23(5):287-322.
  • PMID: 16978659
    Van Craenenbroeck K, Gellynck E, Lintermans B, Leysen JE, Van Tol HH, Haegeman G, Vanhoenacker P: Influence of the antipsychotic drug pipamperone on the expression of the dopamine D4 receptor. Life Sci. 2006 Dec 3;80(1):74-81. doi: 10.1016/j.lfs.2006.08.024. Epub 2006 Aug 25.
  • PMID: 26447610
    Wijma RA, van der Nagel BC, Dierckx B, Dieleman GC, Touw DJ, van Gelder T, Koch BC: Identification and quantification of the antipsychotics risperidone, aripiprazole, pipamperone and their major metabolites in plasma using ultra-high performance liquid chromatography-mass spectrometry. Biomed Chromatogr. 2016 Jun;30(6):794-801. doi: 10.1002/bmc.3610. Epub 2015 Oct 8.
  • PMID: 906888
    Squelart P, Saravia J: Pipamperone (Dipiperon), a useful sedative neuroleptic drug in troublesome chronic psychotic patients. Acta Psychiatr Belg. 1977 Mar-Apr;77(2):284-93.

Contoh Produk & Brand

Produk: 0 • International brands: 2
International Brands
  • Dipiperon
  • Propitan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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