Peringatan Keamanan

Remoxipride was withdrawn from the market after 8 cases of aplastic anemia were reported.A215512 Of those 8 cases, 2 were fatal.A215512

Remoxipride

DB00409

small molecule approved withdrawn

Deskripsi

Remoxipride is an atypical antipsychotic agent that is specific for dopamine D2 receptors.A215422 It gained approval in the UK in 1989 but was withdrawn in 1993 after it was found to be associated with an increased incidence of aplastic anemia.A215422,A215512

Struktur Molekul 2D

Berat 371.269
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The half life of remoxipride in patients with normal creatinine clearance is 5.1 ± 1.6 h, in patients with moderate renal impairment is 6.1 ± 2.6 h, and in patients with severe renal impairment is 9.9 ± 3.8 h.[A215502]
Volume Distribusi The volume of distribution of remoxipride in patients with normal creatinine clearance is 44.3 ± 8.3 L, in patients with moderate renal impairment is 37.4 ± 16.2 L, and in patients with severe renal impairment is 30.2 ± 9.4 L.[A215502]
Klirens (Clearance) The renal clearance of remoxipride in patients with normal creatinine clearance is 23.6 ± 7.0 mL/min, in patients with moderate renal impairment is 9.3 ± 3.8 mL/min, and in patients with severe renal impairment is 3.7 ± 2.9 mL/min.[A215502] The systemic plasma clearance of remoxipride is 120 mL/min.[A215507]

Absorpsi

Remoxipride is approximately 90% bioavailable.A215502 In patients with normal creatinine clearance, remoxipride reaches a Cmax of 5.5 ± 1.1 µmol/L, with a Tmax of 0.8 ± 0.2 h, and an AUC of 39 ± 9 µmol\*h/L.A215502 In patients with moderate renal impairment, remoxipride reaches a Cmax of 7.7 ± 2.7 µmol/L, with a Tmax of 0.9 ± 0.4 h, and an AUC of 63 ± 34 µmol\*h/L.A215502 In patients with severe renal impairment, remoxipride reaches a Cmax of 9.3 ± 2.3 µmol/L, with a Tmax of 1.4 ± 0.9 h, and an AUC of 123 ± 60 µmol\*h/L.A215502

Metabolisme

Remoxipride can be N-dealkylated to FLA 853, oxidized to FLA 850, or N-deethylated to FLA 838.A215417,A215502 FLA 838 can be oxidized to NCL 118 which is further hydroxylated to NCM 009.A215417,A215502 FLA 850 can be N-deethylated to NCL 118 or hydroxylated to NCM 001.A215417,A215502 NCM 001 is further N-deethylated to NCM 009.A215417,A215502 None of these metabolites have measurable activity on dopamine D2 receptors.A215502

Rute Eliminasi

A dose of remoxipride is 89% recovered in the urine and 7% in the feces.A215507 10-40% of a dose of remoxipride is recovered in the urine as the unchanged parent drug.A215507

Interaksi Obat

937 Data
Buprenorphine Remoxipride 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 Remoxipride.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Remoxipride.
Droperidol Droperidol may increase the central nervous system depressant (CNS depressant) activities of Remoxipride.
Hydrocodone Remoxipride 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 Remoxipride.
Magnesium sulfate The therapeutic efficacy of Remoxipride can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Remoxipride may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Remoxipride.
Mirtazapine Remoxipride 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 Remoxipride.
Orphenadrine Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Orphenadrine.
Paraldehyde Remoxipride 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 Remoxipride.
Rotigotine Remoxipride may increase the sedative activities of Rotigotine.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Remoxipride.
Sodium oxybate Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.
Suvorexant Remoxipride 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 Remoxipride.
Thalidomide Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Thalidomide.
Zolpidem Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Zolpidem.
Amisulpride Remoxipride may increase the antipsychotic activities of Amisulpride.
Methylphenidate The risk or severity of adverse effects can be increased when Remoxipride is combined with Methylphenidate.
Dexmethylphenidate The risk or severity of adverse effects can be increased when Remoxipride is combined with Dexmethylphenidate.
Metoclopramide The risk or severity of adverse effects can be increased when Metoclopramide is combined with Remoxipride.
Quinagolide The therapeutic efficacy of Quinagolide can be decreased when used in combination with Remoxipride.
Sulpiride Remoxipride may increase the antipsychotic activities of Sulpiride.
Methadone The risk or severity of adverse effects can be increased when Methadone is combined with Remoxipride.
Lithium citrate Lithium citrate may increase the neurotoxic activities of Remoxipride.
Lithium hydroxide Lithium hydroxide may increase the neurotoxic activities of Remoxipride.
Mequitazine Remoxipride may increase the arrhythmogenic activities of Mequitazine.
Mirabegron The serum concentration of Remoxipride can be increased when it is combined with Mirabegron.
Ethanol Remoxipride may increase the central nervous system depressant (CNS depressant) activities of Ethanol.
Azelastine Remoxipride 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 Remoxipride.
Zimelidine The risk or severity of adverse effects can be increased when Remoxipride is combined with Zimelidine.
Dapoxetine The risk or severity of adverse effects can be increased when Remoxipride is combined with Dapoxetine.
Seproxetine The risk or severity of adverse effects can be increased when Remoxipride is combined with Seproxetine.
Citalopram The risk or severity of adverse effects can be increased when Remoxipride is combined with Citalopram.
Trazodone The risk or severity of adverse effects can be increased when Remoxipride is combined with Trazodone.
Sertraline The risk or severity of adverse effects can be increased when Remoxipride is combined with Sertraline.
Sibutramine The risk or severity of adverse effects can be increased when Remoxipride is combined with Sibutramine.
Nefazodone The risk or severity of adverse effects can be increased when Remoxipride is combined with Nefazodone.
Milnacipran The risk or severity of adverse effects can be increased when Remoxipride is combined with Milnacipran.
Desvenlafaxine The serum concentration of Remoxipride can be increased when it is combined with Desvenlafaxine.
Levomilnacipran The risk or severity of adverse effects can be increased when Levomilnacipran is combined with Remoxipride.
Indalpine The risk or severity of adverse effects can be increased when Remoxipride is combined with Indalpine.
Alaproclate The risk or severity of adverse effects can be increased when Remoxipride is combined with Alaproclate.
Trospium The metabolism of Remoxipride can be decreased when combined with Trospium.
Cyproheptadine The risk or severity of CNS depression can be increased when Remoxipride is combined with Cyproheptadine.
Propiomazine The risk or severity of CNS depression can be increased when Remoxipride is combined with Propiomazine.
Tolterodine The metabolism of Tolterodine can be decreased when combined with Remoxipride.
Oxybutynin The metabolism of Remoxipride can be decreased when combined with Oxybutynin.
Tiotropium The metabolism of Tiotropium can be decreased when combined with Remoxipride.
Solifenacin The metabolism of Solifenacin can be decreased when combined with Remoxipride.
Fesoterodine The metabolism of Fesoterodine can be decreased when combined with Remoxipride.
Umeclidinium The metabolism of Umeclidinium can be decreased when combined with Remoxipride.
Revefenacin The metabolism of Revefenacin can be decreased when combined with Remoxipride.
Doxepin The risk or severity of adverse effects can be increased when Doxepin is combined with Remoxipride.
Zopiclone The risk or severity of adverse effects can be increased when Remoxipride is combined with Zopiclone.
Eletriptan The risk or severity of adverse effects can be increased when Eletriptan is combined with Remoxipride.
Cabergoline The risk or severity of adverse effects can be increased when Cabergoline is combined with Remoxipride.
Zolmitriptan The risk or severity of adverse effects can be increased when Zolmitriptan is combined with Remoxipride.
Dextromethorphan The risk or severity of adverse effects can be increased when Dextromethorphan is combined with Remoxipride.
Mazindol The risk or severity of adverse effects can be increased when Mazindol is combined with Remoxipride.
Linezolid The risk or severity of adverse effects can be increased when Linezolid is combined with Remoxipride.
Sumatriptan The risk or severity of adverse effects can be increased when Sumatriptan is combined with Remoxipride.
Ergotamine The risk or severity of adverse effects can be increased when Ergotamine is combined with Remoxipride.
Fentanyl The risk or severity of adverse effects can be increased when Fentanyl is combined with Remoxipride.
Almotriptan The risk or severity of adverse effects can be increased when Almotriptan is combined with Remoxipride.
Naratriptan The risk or severity of adverse effects can be increased when Naratriptan is combined with Remoxipride.
Rizatriptan The risk or severity of adverse effects can be increased when Rizatriptan is combined with Remoxipride.
Frovatriptan The risk or severity of adverse effects can be increased when Frovatriptan is combined with Remoxipride.
Procarbazine The risk or severity of adverse effects can be increased when Procarbazine is combined with Remoxipride.
Bromocriptine The risk or severity of adverse effects can be increased when Bromocriptine is combined with Remoxipride.
Ergometrine The risk or severity of adverse effects can be increased when Ergometrine is combined with Remoxipride.
Rasagiline The risk or severity of adverse effects can be increased when Rasagiline is combined with Remoxipride.
Etoperidone The risk or severity of adverse effects can be increased when Etoperidone is combined with Remoxipride.
Lorpiprazole The risk or severity of adverse effects can be increased when Lorpiprazole is combined with Remoxipride.
Amphetamine Remoxipride may decrease the stimulatory activities of Amphetamine.
Phentermine Remoxipride may decrease the stimulatory activities of Phentermine.
Pseudoephedrine Remoxipride may decrease the stimulatory activities of Pseudoephedrine.
Benzphetamine Remoxipride may decrease the stimulatory activities of Benzphetamine.
Diethylpropion Remoxipride may decrease the stimulatory activities of Diethylpropion.
Lisdexamfetamine Remoxipride may decrease the stimulatory activities of Lisdexamfetamine.
Mephentermine Remoxipride may decrease the stimulatory activities of Mephentermine.
MMDA Remoxipride may decrease the stimulatory activities of MMDA.
2,5-Dimethoxy-4-ethylamphetamine Remoxipride may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylamphetamine.
Chlorphentermine Remoxipride may decrease the stimulatory activities of Chlorphentermine.
Methylenedioxyethamphetamine Remoxipride may decrease the stimulatory activities of Methylenedioxyethamphetamine.
Dextroamphetamine Remoxipride may decrease the stimulatory activities of Dextroamphetamine.
Metamfetamine Remoxipride may decrease the stimulatory activities of Metamfetamine.
Iofetamine I-123 Remoxipride may decrease the stimulatory activities of Iofetamine I-123.
Ritobegron Remoxipride may decrease the stimulatory activities of Ritobegron.
Mephedrone Remoxipride may decrease the stimulatory activities of Mephedrone.
Methoxyphenamine Remoxipride may decrease the stimulatory activities of Methoxyphenamine.
Gepefrine Remoxipride may decrease the stimulatory activities of Gepefrine.
2,5-Dimethoxy-4-ethylthioamphetamine Remoxipride may decrease the stimulatory activities of 2,5-Dimethoxy-4-ethylthioamphetamine.
Phendimetrazine Remoxipride may decrease the stimulatory activities of Phendimetrazine.

Target Protein

D(2) dopamine receptor DRD2
D(4) dopamine receptor DRD4
D(3) dopamine receptor DRD3
5-hydroxytryptamine receptor 2A HTR2A
Sigma non-opioid intracellular receptor 1 SIGMAR1

Referensi & Sumber

Artikel (PubMed)
  • PMID: 11607043
    Nadal R: Pharmacology of the atypical antipsychotic remoxipride, a dopamine D2 receptor antagonist. CNS Drug Rev. 2001 Fall;7(3):265-82. doi: 10.1111/j.1527-3458.2001.tb00199.x.
  • PMID: 8329289
    Movin-Osswald G, Boelaert J, Hammarlund-Udenaes M, Nilsson LB: The pharmacokinetics of remoxipride and metabolites in patients with various degrees of renal function. Br J Clin Pharmacol. 1993 Jun;35(6):615-22. doi: 10.1111/j.1365-2125.1993.tb04191.x.
  • PMID: 8405075
    Mohell N, Sallemark M, Rosqvist S, Malmberg A, Hogberg T, Jackson DM: Binding characteristics of remoxipride and its metabolites to dopamine D2 and D3 receptors. Eur J Pharmacol. 1993 Jul 6;238(1):121-5. doi: 10.1016/0014-2999(93)90515-j.
  • PMID: 1978486
    von Bahr C, Movin G, Yisak WA, Jostell KG, Widman M: Clinical pharmacokinetics of remoxipride. Acta Psychiatr Scand Suppl. 1990;358:41-4. doi: 10.1111/j.1600-0447.1990.tb05284.x.
  • PMID: 10958256
    King DJ, Wager E: Haematological safety of antipsychotic drugs. J Psychopharmacol. 1998;12(3):283-8. doi: 10.1177/026988119801200309.
  • PMID: 20927748
    Subramanian S, Rummel-Kluge C, Hunger H, Schmid F, Schwarz S, Kissling W, Leucht S, Komossa K: Zotepine versus other atypical antipsychotics for schizophrenia. Cochrane Database Syst Rev. 2010 Oct 6;(10):CD006628. doi: 10.1002/14651858.CD006628.pub3.
  • PMID: 9577836
    Seeman P, Tallerico T: Antipsychotic drugs which elicit little or no parkinsonism bind more loosely than dopamine to brain D2 receptors, yet occupy high levels of these receptors. Mol Psychiatry. 1998 Mar;3(2):123-34.
  • PMID: 2901121
    Farde L, Grind M, Nilsson MI, Ogenstad S, Sedvall G: Remoxipride--a new potential antipsychotic drug. Pharmacological effects and pharmacokinetics following repeated oral administration in male volunteers. Psychopharmacology (Berl). 1988;95(2):157-61. doi: 10.1007/BF00174501.

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