Details
| Stereochemistry | ACHIRAL |
| Molecular Formula | C20H25N3S.2C4H4O4 |
| Molecular Weight | 571.642 |
| Optical Activity | NONE |
| Defined Stereocenters | 0 / 0 |
| E/Z Centers | 2 |
| Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)\C=C/C(O)=O.OC(=O)\C=C/C(O)=O.CN1CCN(CCCN2C3=C(SC4=C2C=CC=C4)C=CC=C3)CC1
InChI
InChIKey=PQDKNYWKLCFCJU-SPIKMXEPSA-N
InChI=1S/C20H25N3S.2C4H4O4/c1-21-13-15-22(16-14-21)11-6-12-23-17-7-2-4-9-19(17)24-20-10-5-3-8-18(20)23;2*5-3(6)1-2-4(7)8/h2-5,7-10H,6,11-16H2,1H3;2*1-2H,(H,5,6)(H,7,8)/b;2*2-1-
DescriptionCurator's Comment: Description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/12523495 and http://www.genome.jp/dbget-bin/www_bget?D01412
Curator's Comment: Description was created based on several sources, including
http://www.ncbi.nlm.nih.gov/pubmed/12523495 and http://www.genome.jp/dbget-bin/www_bget?D01412
Perazine (Taxilan) is a moderate-potency typical antipsychotic of the phenothiazine class. Perazine is an older antipsychotic drug first introduced in the 1950s. It is suggested to have a low level of side effects (especially for movement disorders). Its use is regional and restricted to countries like Germany, Poland, the Netherlands and the former Yugoslavia. Perazine has being shown to be a potent inhibitor of human CYP1A2. It acts as a dopamine antagonist.
CNS Activity
Originator
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL3356 |
|||
Target ID: CHEMBL217 |
|||
Target ID: Cytochrome P450 2B, Rattus norvegicus |
45.0 µM [Ki] |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | Taxilan Approved UseTaxilan is used in the treatment of schizophrenia |
PubMed
| Title | Date | PubMed |
|---|---|---|
| [Electroconvulsive therapy in treatment of acute life threatening catatonia in toxic epidermal necrolysis (Lyell syndrome)]. | 1992 May |
|
| Relevance of liver enzyme elevations with four different neuroleptics: a retrospective review of 7,263 treatment courses. | 2001 Apr |
|
| Perazine for schizophrenia. | 2002 |
|
| Perazine as a potent inhibitor of human CYP1A2 but not CYP3A4. | 2002 Jul-Aug |
|
| Antipsychotic efficacy of the antidepressant trimipramine: a randomized, double-blind comparison with the phenothiazine perazine. | 2003 Mar-Apr |
|
| Schizophrenia. | 2004 Dec |
|
| Halogenation of drugs enhances membrane binding and permeation. | 2004 May 3 |
|
| Analysis of phenothiazines in human body fluids using disk solid-phase extraction and liquid chromatography. | 2005 Nov-Dec |
|
| Interactions between neuroleptics and CYP2C6 in rat liver--in vitro and ex vivo study. | 2005 Nov-Dec |
|
| Direct effects of neuroleptics on the activity of CYP2A in the liver of rats. | 2005 Nov-Dec |
|
| Automated analysis of quetiapine and other antipsychotic drugs in human blood by high performance-liquid chromatography with column-switching and spectrophotometric detection. | 2006 Jan 18 |
|
| Characterization of human cytochrome p450 enzymes involved in the metabolism of the piperidine-type phenothiazine neuroleptic thioridazine. | 2006 Mar |
|
| Quantitative determination of forty-eight antidepressants and antipsychotics in human serum by HPLC tandem mass spectrometry: a multi-level, single-sample approach. | 2006 Oct 20 |
|
| Perazine and carbamazepine in comparison to olanzapine in schizophrenia. | 2007 |
|
| The activity of cytochrome P450 CYP2B in rat liver during neuroleptic treatment. | 2007 Sep-Oct |
|
| Typical and atypical antipsychotics--the misleading dichotomy. Results from the Working Group 'Drugs in Psychiatry' (AGATE). | 2008 |
|
| The effect of antipsychotic medication on sexual function and serum prolactin levels in community-treated schizophrenic patients: results from the Schizophrenia Trial of Aripiprazole (STAR) study (NCT00237913). | 2008 Dec 22 |
|
| Amisulpride plus valproate vs haloperidol plus valproate in the treatment of acute mania of bipolar I patients: a multicenter, open-label, randomized, comparative trial. | 2008 Jun |
|
| [Antipsychotics in clinical practice. Treatment of the first schizophrenic episode]. | 2008 Nov-Dec |
|
| [Application of liquid chromatography coupled with mass spectrometry (LC/MS) to determine antidepressants in blood samples]. | 2008 Oct-Dec |
|
| Increased D-amino acid oxidase expression in the bilateral hippocampal CA4 of schizophrenic patients: a post-mortem study. | 2009 Dec |
|
| Spectroscopic and electrochemical analysis of psychotropic drugs. | 2009 Jan |
|
| Validation of derivative spectrophotometry method for determination of active ingredients from neuroleptics in pharmaceutical preparations. | 2009 Jul-Aug |
|
| Effects of typical and atypical antipsychotic drugs on gene expression profiles in the liver of schizophrenia subjects. | 2009 Sep 16 |
|
| Perazine at therapeutic drug concentrations inhibits human cytochrome P450 isoenzyme 1A2 (CYP1A2) and caffeine metabolism--an in vitro study. | 2009 Sep-Oct |
|
| The role of CYP2D6 and TaqI A polymorphisms in malignant neuroleptic syndrome: two case reports with three episodes. | 2010 Mar |
|
| [Perazine in the treatment of psychotic disorders--research review]. | 2010 May-Jun |
|
| Main contribution of the cytochrome P450 isoenzyme 1A2 (CYP1A2) to N-demethylation and 5-sulfoxidation of the phenothiazine neuroleptic chlorpromazine in human liver--A comparison with other phenothiazines. | 2010 Oct 15 |
Patents
Sample Use Guides
In Vivo Use Guide
Curator's Comment: In acutely ill and severely disturbed patients 50 mg perazine at time-intervals of 30 minutes can be administered intramuscularly
The customary dose range recommended for this antipsychotic under in-patient conditions is 75-600 mg/day (maximum 1000 mg/day).
Route of Administration:
Oral
| Name | Type | Language | ||
|---|---|---|---|---|
|
Common Name | English | ||
|
Common Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English | ||
|
Common Name | English | ||
|
Systematic Name | English |
| Code System | Code | Type | Description | ||
|---|---|---|---|---|---|
|
100000079420
Created by
admin on Fri Dec 15 16:59:01 GMT 2023 , Edited by admin on Fri Dec 15 16:59:01 GMT 2023
|
PRIMARY | |||
|
5282417
Created by
admin on Fri Dec 15 16:59:01 GMT 2023 , Edited by admin on Fri Dec 15 16:59:01 GMT 2023
|
PRIMARY | |||
|
14516-56-4
Created by
admin on Fri Dec 15 16:59:01 GMT 2023 , Edited by admin on Fri Dec 15 16:59:01 GMT 2023
|
PRIMARY | |||
|
SUB14812MIG
Created by
admin on Fri Dec 15 16:59:01 GMT 2023 , Edited by admin on Fri Dec 15 16:59:01 GMT 2023
|
PRIMARY | |||
|
3VG1507988
Created by
admin on Fri Dec 15 16:59:01 GMT 2023 , Edited by admin on Fri Dec 15 16:59:01 GMT 2023
|
PRIMARY |
ACTIVE MOIETY
PARENT (SALT/SOLVATE)
SUBSTANCE RECORD
