Peringatan Keamanan

The oral LD50 is 423 mg/kg in mice and 791 mg/kg in rats.L31868 The intravenous LD50 is 37 mg/kg in rats.L31873

Flupentixol overdose is characterized by sedation, frequently preceded by extreme agitation, excitement, confusion, somnolence, coma, convulsions, and hyperthermia or hypothermia. Extrapyramidal symptoms or respiratory and circulatory collapse may be observed. ECG changes, QT prolongation, Torsades de Pointes, cardiac arrest and ventricular arrhythmias have been reported from the combined use of drugs known to affect the heart with large doses of flupentixol. In case of overdose, symptomatic treatment should be initiated with airway management. In case of severe hypotension, epinephrine should not be used: instead, intravenous vasopressor drugs, such as levarterenol, can be used. Antiparkinsonian medication should be administered only if extrapyramidal symptoms develop. Gastric lavage should be initiated in the case of flupentixol tablet overdose. Further injections of flupentixol should be discontinued in case of an intramuscularly-administered drug overdose until the patient shows signs of relapse, in which the dosage can subsequently be decreased.L31808

Neuroleptic malignant syndrome is associated with neuroleptic drugs, which should be responded to with immediate discontinuation of the drug and initiation of symptomatic treatment and medical monitoring.L31808

Flupentixol

DB00875

small molecule approved investigational withdrawn

Deskripsi

Flupentixol is an antipsychotic drug of the thioxanthene group. It exists in two geometric isomers, the trans(E) and pharmacologically active cis(Z) forms. Flupentixol decanoate is one of the active ingredients found in injectable drug formulations: it is produced by esterification of cis(Z)?flupentixol with decanoic acid.A229083 Flupentixol is an antagonist of both D1 and D2 dopamine receptors.A229083

Available as oral tablets or long-acting intramuscular injections, flupentixol is marketed under brand names such as Depixol and Fluanxol. It is approved for use in Canada and other countries around the world, but not in the US. It is used for the management of chronic schizophrenia in patients whose main manifestations do not include excitement, agitation or hyperactivity.L31808 It has been marketed to manage symptoms of depression in patients who may or may not exhibit signs of anxiety.L31928 In combination with melitracen, flupentixol is used to manage symptoms of anxiety, depression, and asthenia.L31923

Struktur Molekul 2D

Berat 434.52
Wujud solid

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

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life is about 35 hours following oral administration and three weeks following intramuscular administration.[L31808]
Volume Distribusi The apparent volume of distribution is about 14.1 L/kg. Following administration, the highest levels of flupentixol are found in the lungs, liver, and spleen. Lower concentrations of the drug are found in the blood and brain.[L31808]
Klirens (Clearance) Following oral administration, the mean systemic clearance is about 0.29 L/min.[L31808]

Absorpsi

Following oral administration, flupentixol is readily absorbed from the gastrointestinal tract, with oral bioavailability of about 40%. Tmax ranges from three to eight hours. Steady-state plasma levels are achieved in about seven days and following once-daily oral administration of 5 mg flupentixol, the mean minimum steady-state level was about 1.7 ng/mL (3.9 nmol/L).L31808 From the site of intramuscular injection, esterified flupentixol diffuses slowly from the oil solution and is slowly released into the extracellular fluid and the circulation to be distributed to different tissues. Peak drug concentrations are reached between four and seven days following intramuscular injection. Intramuscularly administered flupentixol is detectable in the blood three weeks after injection and reaches steady-state concentrations after about three months of repeated administration.L31808

Metabolisme

Flupentixol is metabolized in the liver via sulfoxidation, dealkylation, and glucuronidation to form pharmacologically inactive metabolites. Flupentixol decanoate, the active ingredient in the intramuscular formulation, is hydrolyzed to flupentixol.L31808

Rute Eliminasi

Fecal excretion is more predominant than renal excretion. In the feces, flupentixol is recovered in the feces mainly as the unchanged form, as well as its lipophilic metabolites, such as dealkyl-flupentixol. Flupentixol is recovered in the urine as the unchanged form as well as its hydrophilic sulfoxide and glucuronide metabolites.L31808

Interaksi Makanan

2 Data
  • 1. Avoid alcohol. Flupentixol can enhance the sedative effects of alcohol.
  • 2. Take with or without food. Food has negligible effects on drug pharmacokinetics.

Interaksi Obat

1600 Data
Valsartan Flupentixol may decrease the antihypertensive activities of Valsartan.
Remikiren Flupentixol may decrease the antihypertensive activities of Remikiren.
Torasemide Flupentixol may decrease the antihypertensive activities of Torasemide.
Guanadrel Flupentixol may decrease the antihypertensive activities of Guanadrel.
Olmesartan Flupentixol may decrease the antihypertensive activities of Olmesartan.
Nitroprusside Flupentixol may decrease the antihypertensive activities of Nitroprusside.
Minoxidil Flupentixol may decrease the antihypertensive activities of Minoxidil.
Fosinopril Flupentixol may decrease the antihypertensive activities of Fosinopril.
Trandolapril Flupentixol may decrease the antihypertensive activities of Trandolapril.
Benazepril Flupentixol may decrease the antihypertensive activities of Benazepril.
Bosentan Flupentixol may decrease the antihypertensive activities of Bosentan.
Cyclothiazide Flupentixol may decrease the antihypertensive activities of Cyclothiazide.
Candoxatril Flupentixol may decrease the antihypertensive activities of Candoxatril.
Mecamylamine Flupentixol may decrease the antihypertensive activities of Mecamylamine.
Eplerenone Flupentixol may decrease the antihypertensive activities of Eplerenone.
Lisinopril Flupentixol may decrease the antihypertensive activities of Lisinopril.
Nitroglycerin Flupentixol may decrease the antihypertensive activities of Nitroglycerin.
Cryptenamine Flupentixol may decrease the antihypertensive activities of Cryptenamine.
Eprosartan Flupentixol may decrease the antihypertensive activities of Eprosartan.
Quinapril Flupentixol may decrease the antihypertensive activities of Quinapril.
Irbesartan Flupentixol may decrease the antihypertensive activities of Irbesartan.
Deserpidine Flupentixol may decrease the antihypertensive activities of Deserpidine.
Pentolinium Flupentixol may decrease the antihypertensive activities of Pentolinium.
Trimethaphan Flupentixol may decrease the antihypertensive activities of Trimethaphan.
Diazoxide Flupentixol may decrease the antihypertensive activities of Diazoxide.
Epoprostenol Flupentixol may decrease the antihypertensive activities of Epoprostenol.
Hydralazine Flupentixol may decrease the antihypertensive activities of Hydralazine.
Saprisartan Flupentixol may decrease the antihypertensive activities of Saprisartan.
Spirapril Flupentixol may decrease the antihypertensive activities of Spirapril.
Tienilic acid Flupentixol may decrease the antihypertensive activities of Tienilic acid.
Sitaxentan Flupentixol may decrease the antihypertensive activities of Sitaxentan.
Diethylnorspermine Flupentixol may decrease the antihypertensive activities of Diethylnorspermine.
Pinacidil Flupentixol may decrease the antihypertensive activities of Pinacidil.
Temocapril Flupentixol may decrease the antihypertensive activities of Temocapril.
Riociguat Flupentixol may decrease the antihypertensive activities of Riociguat.
Macitentan Flupentixol may decrease the antihypertensive activities of Macitentan.
Aliskiren Flupentixol may decrease the antihypertensive activities of Aliskiren.
Nicorandil Flupentixol may decrease the antihypertensive activities of Nicorandil.
Rauwolfia serpentina root Flupentixol may decrease the antihypertensive activities of Rauwolfia serpentina root.
Enalaprilat Flupentixol may decrease the antihypertensive activities of Enalaprilat.
Angiotensin 1-7 Flupentixol may decrease the antihypertensive activities of Angiotensin 1-7.
Imidapril Flupentixol may decrease the antihypertensive activities of Imidapril.
BQ-123 Flupentixol may decrease the antihypertensive activities of BQ-123.
Dihydralazine Flupentixol may decrease the antihypertensive activities of Dihydralazine.
Zofenopril Flupentixol may decrease the antihypertensive activities of Zofenopril.
Guanoxan Flupentixol may decrease the antihypertensive activities of Guanoxan.
Delapril Flupentixol may decrease the antihypertensive activities of Delapril.
Vincamine Flupentixol may decrease the antihypertensive activities of Vincamine.
Linsidomine Flupentixol may decrease the antihypertensive activities of Linsidomine.
Guanoxabenz Flupentixol may decrease the antihypertensive activities of Guanoxabenz.
Tolonidine Flupentixol may decrease the antihypertensive activities of Tolonidine.
Endralazine Flupentixol may decrease the antihypertensive activities of Endralazine.
Cadralazine Flupentixol may decrease the antihypertensive activities of Cadralazine.
Bietaserpine Flupentixol may decrease the antihypertensive activities of Bietaserpine.
Guanazodine Flupentixol may decrease the antihypertensive activities of Guanazodine.
Methoserpidine Flupentixol may decrease the antihypertensive activities of Methoserpidine.
Guanoclor Flupentixol may decrease the antihypertensive activities of Guanoclor.
Muzolimine Flupentixol may decrease the antihypertensive activities of Muzolimine.
Xipamide Flupentixol may decrease the antihypertensive activities of Xipamide.
Tocopherylquinone Flupentixol may decrease the antihypertensive activities of Tocopherylquinone.
Benazeprilat Flupentixol may decrease the antihypertensive activities of Benazeprilat.
Fosinoprilat Flupentixol may decrease the antihypertensive activities of Fosinoprilat.
Ramiprilat Flupentixol may decrease the antihypertensive activities of Ramiprilat.
Perindoprilat Flupentixol may decrease the antihypertensive activities of Perindoprilat.
Quinaprilat Flupentixol may decrease the antihypertensive activities of Quinaprilat.
Furosemide Flupentixol may decrease the antihypertensive activities of Furosemide.
Enalapril Flupentixol may decrease the antihypertensive activities of Enalapril.
Candesartan cilexetil Flupentixol may decrease the antihypertensive activities of Candesartan cilexetil.
Telmisartan Flupentixol may decrease the antihypertensive activities of Telmisartan.
Captopril Flupentixol may decrease the antihypertensive activities of Captopril.
Cilazapril Flupentixol may decrease the antihypertensive activities of Cilazapril.
Debrisoquine Flupentixol may decrease the antihypertensive activities of Debrisoquine.
Ambrisentan Flupentixol may decrease the antihypertensive activities of Ambrisentan.
Selexipag Flupentixol may decrease the antihypertensive activities of Selexipag.
Candesartan Flupentixol may decrease the antihypertensive activities of Candesartan.
Ramipril Flupentixol may decrease the antihypertensive activities of Ramipril.
Perindopril Flupentixol may decrease the antihypertensive activities of Perindopril.
Levamlodipine Flupentixol may decrease the antihypertensive activities of Levamlodipine.
Buthiazide Flupentixol may decrease the antihypertensive activities of Buthiazide.
Chlorthalidone Flupentixol may decrease the antihypertensive activities of Chlorthalidone.
Bendroflumethiazide Flupentixol may decrease the antihypertensive activities of Bendroflumethiazide.
Metolazone Flupentixol may decrease the antihypertensive activities of Metolazone.
Hydroflumethiazide Flupentixol may decrease the antihypertensive activities of Hydroflumethiazide.
Chlorothiazide Flupentixol may decrease the antihypertensive activities of Chlorothiazide.
Trichlormethiazide Flupentixol may decrease the antihypertensive activities of Trichlormethiazide.
Polythiazide Flupentixol may decrease the antihypertensive activities of Polythiazide.
Cyclopenthiazide Flupentixol may decrease the antihypertensive activities of Cyclopenthiazide.
Azilsartan medoxomil Flupentixol may decrease the antihypertensive activities of Azilsartan medoxomil.
Buprenorphine Flupentixol 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 Flupentixol.
Dronabinol Dronabinol may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
Hydrocodone Flupentixol may increase the central nervous system depressant (CNS depressant) activities of Hydrocodone.
Magnesium sulfate The therapeutic efficacy of Flupentixol can be increased when used in combination with Magnesium sulfate.
Methotrimeprazine Flupentixol may increase the central nervous system depressant (CNS depressant) activities of Methotrimeprazine.
Metyrosine Flupentixol may increase the sedative activities of Metyrosine.
Minocycline Minocycline may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
Nabilone Nabilone may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
Perampanel Perampanel may increase the central nervous system depressant (CNS depressant) activities of Flupentixol.
Rufinamide The risk or severity of adverse effects can be increased when Rufinamide is combined with Flupentixol.
Sodium oxybate Flupentixol may increase the central nervous system depressant (CNS depressant) activities of Sodium oxybate.

Target Protein

D(2) dopamine receptor DRD2
D(1A) dopamine receptor DRD1
5-hydroxytryptamine receptor 2A HTR2A
Alpha-1A adrenergic receptor ADRA1A
D(3) dopamine receptor DRD3
D(4) dopamine receptor DRD4
5-hydroxytryptamine receptor 2C HTR2C
Muscarinic acetylcholine receptor M1 CHRM1

Referensi & Sumber

Synthesis reference: Smith Kline & French Laboratories; British Patent 925,538; May 8, 1963. Craig, P.N. and Zirkle, C.L.; U.S. Patent 3,282,930; November 1, 1966; assigned to Smith Kline & French Laboratories.
Artikel (PubMed)
  • PMID: 24915451
    Mahapatra J, Quraishi SN, David A, Sampson S, Adams CE: Flupenthixol decanoate (depot) for schizophrenia or other similar psychotic disorders. Cochrane Database Syst Rev. 2014 Jun 10;(6):CD001470. doi: 10.1002/14651858.CD001470.pub2.
  • PMID: 6798610
    Hyttel J: Flupentixol and dopamine receptor selectivity. Psychopharmacology (Berl). 1981;75(2):217. doi: 10.1007/BF00432192.
  • PMID: 6674820
    Poldinger W, Sieberns S: Depression-inducing and antidepressive effects of neuroleptics. Experiences with flupenthixol and flupenthixol decanoate. Neuropsychobiology. 1983;10(2-3):131-6. doi: 10.1159/000117999.
  • PMID: 17111172
    Reimold M, Solbach C, Noda S, Schaefer JE, Bartels M, Beneke M, Machulla HJ, Bares R, Glaser T, Wormstall H: Occupancy of dopamine D(1), D (2) and serotonin (2A) receptors in schizophrenic patients treated with flupentixol in comparison with risperidone and haloperidol. Psychopharmacology (Berl). 2007 Feb;190(2):241-9. Epub 2006 Nov 17.
  • PMID: 31337981
    Dong C, Chen Y, Li H, Yang Y, Zhang H, Ke K, Shi XN, Liu X, Li L, Ma J, Kung HF, Chen C, Lin MC: The antipsychotic agent flupentixol is a new PI3K inhibitor and potential anticancer drug for lung cancer. Int J Biol Sci. 2019 Jun 2;15(7):1523-1532. doi: 10.7150/ijbs.32625. eCollection 2019.
  • PMID: 11171942
    Strange PG: Antipsychotic drugs: importance of dopamine receptors for mechanisms of therapeutic actions and side effects. Pharmacol Rev. 2001 Mar;53(1):119-33.
  • PMID: 16198197
    Laruelle M, Frankle WG, Narendran R, Kegeles LS, Abi-Dargham A: Mechanism of action of antipsychotic drugs: from dopamine D(2) receptor antagonism to glutamate NMDA facilitation. Clin Ther. 2005;27 Suppl A:S16-24. doi: 10.1016/j.clinthera.2005.07.017.
  • PMID: 15309042
    Celada P, Puig M, Amargos-Bosch M, Adell A, Artigas F: The therapeutic role of 5-HT1A and 5-HT2A receptors in depression. J Psychiatry Neurosci. 2004 Jul;29(4):252-65.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 10 • International brands: 3
Produk
  • Fluanxol 0.5mg - Tab
    Tablet • 0.5 mg • Oral • Canada • Approved
  • Fluanxol 3mg - Tab
    Tablet • 3 mg • Oral • Canada • Approved
  • Fluanxol Depot 10%- Liq Im 100mg/ml
    Solution • 100 mg / mL • Intramuscular • Canada • Approved
  • Fluanxol Depot 2% -liq Im 20mg/ml
    Solution • 20 mg / mL • Intramuscular • Canada • Approved
  • Fluanxol Depot Inj 100mg/ml
    Liquid • 100 mg / mL • Intramuscular • Canada • Approved
  • Fluanxol Depot Inj 20mg/ml
    Liquid • 20 mg / mL • Intramuscular • Canada • Approved
  • Fluanxol Tab 0.5mg
    Tablet • 0.5 mg • Oral • Canada • Approved
  • Fluanxol Tab 3mg
    Tablet • 3 mg • Oral • Canada • Approved
Menampilkan 8 dari 10 produk.
International Brands
  • Depixol — Lundbeck A/S
  • Fluanxol — Lundbeck A/S
  • Jexit — Johnson

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