Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C23H25F3N2OS |
| Molecular Weight | 434.518 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 1 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OCCN1CCN(CC\C=C2\C3=C(SC4=C2C=C(C=C4)C(F)(F)F)C=CC=C3)CC1
InChI
InChIKey=NJMYODHXAKYRHW-DVZOWYKESA-N
InChI=1S/C23H25F3N2OS/c24-23(25,26)17-7-8-22-20(16-17)18(19-4-1-2-6-21(19)30-22)5-3-9-27-10-12-28(13-11-27)14-15-29/h1-2,4-8,16,29H,3,9-15H2/b18-5-
DescriptionCurator's Comment: Description was created based on several sources, including https://www.medicines.org.uk/emc/PIL.5400.latest.pdf | http://www.lundbeck.com/upload/au/files/pdf/Fluanxol_CMI.pdf
Curator's Comment: Description was created based on several sources, including https://www.medicines.org.uk/emc/PIL.5400.latest.pdf | http://www.lundbeck.com/upload/au/files/pdf/Fluanxol_CMI.pdf
Flupenthixol is a thioxanthene antipsychotic used in the treatment of schizophrenia and other psychoses, with the exception of mania and psychomotor hyperactivity due to an activating effect associated with this drug. It may also be employed as an antidepressant. Flupenthixol has a wide range of pharmacological actions. Flupenthixol blocks dopaminergic receptors, thus interfering with dopaminergic transmission in the brain. Flupenthixol also inhibits serotonin 5-HT, histamine H1,
muscarinic and alpha-1 adrenergic receptors.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL217 Sources: DOI: 10.1016/B978-008055232-3.61770-2 |
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Target ID: CHEMBL2095200 |
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Target ID: CHEMBL2094251 |
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Target ID: CHEMBL231 |
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Target ID: CHEMBL2094109 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | FLUANXOL Approved UseFlupentixol Decanoate Injection and Flupentixol Dihydrochloride Tablets
Indication: Schizophrenia and allied psychoses, especially with symptoms such as hallucinations, delusions and thought disturbances along with apathy, lowered mood and withdrawal. |
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| Primary | FLUANXOL Approved UseFluanxol is used to treat depression in patients who may, or may not, also be showing signs of anxiety. |
PubMed
| Title | Date | PubMed |
|---|---|---|
| Flupenthixol and trifluoperazine: a double-blind investigation in the treatment of schizophrenics. | 1971 Nov |
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| Persistent involuntary movements after treatment with flupenthixol. | 1981 May 30 |
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| Effects of chronic treatment with antidepressants on aggressiveness induced by clonidine in mice. | 1982 |
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| Neuroleptic malignant syndrome. | 1984 Jun 23 |
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| Pharmacology in vivo of the phenylindan derivative, Lu 19-005, a new potent inhibitor of dopamine, noradrenaline and 5-hydroxytryptamine uptake in rat brain. | 1985 Apr |
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| [Pharmacotoxic psychosis and extrapyramidal motor syndrome. A case of acute adverse effect of fluoxetine and flupenthixol]. | 1992 Sep |
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| Characteristics of P388/VMDRC.04, a simple, sensitive model for studying P-glycoprotein antagonists. | 1994 Feb 1 |
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| High agonist-independent activity is a distinguishing feature of the dopamine D1B receptor subtype. | 1994 Nov 11 |
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| Mitochondrial involvement in schizophrenia and other functional psychoses. | 1996 Sep |
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| Tolerability of low dose neuroleptics: a case control study of flupenthixol. | 1997 Nov |
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| Flupenthixol treatment for cocaine abusers with schizophrenia: a pilot study. | 1998 Aug |
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| Effects of flupenthixol and quadazocine on self-administration of speedball combinations of cocaine and heroin by rhesus monkeys. | 1999 Oct |
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| Inhibition of HIV replication by neuroleptic agents and their potential use in HIV infected patients with AIDS related dementia. | 2000 Apr |
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| Nonalcoholic steatohepatitis: a possible side effect of atypical antipsychotics. | 2003 Jul |
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| Permanent activation of the human P-glycoprotein by covalent modification of a residue in the drug-binding site. | 2003 Jun 6 |
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| [Trazodone for the treatment of behavioral and psychological symptoms of dementia (BPSD) in Alzheimer's disease: a retrospective study focused on the aggression and negativism in caregiving situations]. | 2006 Jun |
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| Antitubercular pharmacodynamics of phenothiazines. | 2013 Apr |
Patents
Sample Use Guides
Fluanxol® (flupentixol) 0.5 mg and 1 mg film-coated tablets.
The starting dose is usually 1 mg daily taken as a single dose in the morning. This may be increased to 2 mg per day after one week. The maximum daily dose is 3 mg per day.
Fluanxol® (flupenthixol decanoate) Depot 20 mg/mL, Concentrated Depot 100 mg/mL.
Generally, the starting dose is 20 to 40 mg (1 to 2 mL). A second dose of 20 to 40 mg (1 to 2 mL) is usually given 4-10 days after the first injection, and further doses are given every 2 to 4 weeks for the majority of patients.
Route of Administration:
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SUBSTANCE RECORD
