Details
Stereochemistry | RACEMIC |
Molecular Formula | C20H21FN2O.BrH |
Molecular Weight | 405.304 |
Optical Activity | ( + / - ) |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
Br.CN(C)CCCC1(OCC2=C1C=CC(=C2)C#N)C3=CC=C(F)C=C3
InChI
InChIKey=WIHMBLDNRMIGDW-UHFFFAOYSA-N
InChI=1S/C20H21FN2O.BrH/c1-23(2)11-3-10-20(17-5-7-18(21)8-6-17)19-9-4-15(13-22)12-16(19)14-24-20;/h4-9,12H,3,10-11,14H2,1-2H3;1H
Molecular Formula | C20H21FN2O |
Molecular Weight | 324.3919 |
Charge | 0 |
Count |
|
Stereochemistry | RACEMIC |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 1 |
E/Z Centers | 0 |
Optical Activity | ( + / - ) |
Molecular Formula | BrH |
Molecular Weight | 80.912 |
Charge | 0 |
Count |
|
Stereochemistry | ACHIRAL |
Additional Stereochemistry | No |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Optical Activity | NONE |
Citalopram (brand names: Celexa, Cipramil, and others) is an antidepressant drug of the selective serotonin reuptake inhibitor (SSRI) class. It has U.S. Food and Drug Administration approval to treat major depression,[2]which it received in 1998, and is prescribed off-label for other conditions. In Australia, the UK, Germany, Portugal, Poland, and most European countries, it is licensed for depressive episodes and panic disorder with or without agoraphobia. In Spain, it is also used for obsessive-compulsive disorder. Citalopram HBr is a racemic bicyclic phthalane derivative designated (±)-1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5carbonitrile, HBr. The mechanism of action of citalopram HBr as an antidepressant is presumed to be linked to potentiation of serotonergic activity in the central nervous system (CNS) resulting from its inhibition of CNS neuronal reuptake of serotonin (5-HT). In vitro and in vivo studies in animals suggest that citalopram is a highly selective serotonin reuptake inhibitor (SSRI) with minimal effects on norepinephrine (NE) and dopamine (DA) neuronal reuptake. The single-and multiple-dose pharmacokinetics of citalopram are linear and dose-proportional in a dose range of 10-60 mg/day. Biotransformation of citalopram is mainly hepatic, with a mean terminal half-life of about 35 hours.
Originator
Sources: https://lakemedelsverket.se/LMF/Lakemedelsinformation/?nplid=19980626000180Bigler, Allan J., et al. 'Quantitative structure-activity-relationships in a series of selective 5-HT uptake inhibitors.' EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY 12.3 (1977): 289-295.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: CHEMBL228 Sources: https://www.ncbi.nlm.nih.gov/pubmed/19616061 |
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Target ID: CHEMBL228 Sources: https://www.ncbi.nlm.nih.gov/pubmed/23265880 |
0.78 nM [Ki] |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Primary | CELEXA Approved UseCitalopram HBr is indicated for the treatment of depression. The efficacy of citalopram HBr in the treatment of depression was established in 4 to 6 week, controlled trials of outpatients whose diagnosis corresponded most closely to the DSM-III and DSM-III-R category of major depressive disorder (see CLINICAL PHARMACOLOGY ). A major depressive episode (DSM-IV) implies a prominent and relatively persistent (nearly every day for at least 2 weeks) depressed or dysphoric mood that usually interferes with daily functioning, and includes at least five of the following nine symptoms: depressed mood, loss of interest in usual activities, significant change in weight and/or appetite, insomnia or hypersomnia, psychomotor agitation or retardation, increased fatigue, feelings of guilt or worthlessness, slowed thinking or impaired concentration, a suicide attempt or suicidal ideation. The antidepressant action of citalopram HBr in hospitalized depressed patients has not been adequately studied. The efficacy of citalopram HBr in maintaining an antidepressant response for up to 24 weeks following 6 to 8 weeks of acute treatment was demonstrated in two placebo-controlled trials (see CLINICAL PHARMACOLOGY ). Nevertheless, the physician who elects to use citalopram HBr for extended periods should periodically re-evaluate the long-term usefulness of the drug for the individual patient. Launch Date1998 |
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Primary | Celexa Approved UseINDICATIONS AND USAGE. Celexa (citalopram HBr) is indicated for the treatment of depression. Launch Date1998 |
Cmax
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
3.2 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
8.5 ng/mL |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
6.1 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
21.7 ng/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
43.7 ng/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
65.6 ng/mL |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
10.6 ng/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
AUC
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
204.5 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1153.2 ng × h/mL |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
843.7 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
1010.4 ng × h/mL |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2070.3 ng × h/mL |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
2946.5 ng × h/mL |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
533.2 ng × h/mL |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
T1/2
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
77.5 h |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
79.3 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
38.5 h |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
40 h |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
39.5 h |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
36.3 h |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Funbound
Value | Dose | Co-administered | Analyte | Population |
---|---|---|---|---|
26% |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
26% |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
26% |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
DESMETHYLCITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18% |
20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18% |
40 mg single, oral dose: 40 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18% |
60 mg single, oral dose: 60 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
|
18% |
10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered: |
CITALOPRAM plasma | Homo sapiens population: HEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED |
Doses
Dose | Population | Adverse events |
---|---|---|
800 mg single, oral Overdose |
unknown, 14 years n = 1 Health Status: unknown Age Group: 14 years Sex: F Population Size: 1 Sources: |
Other AEs: Dizziness, Drowsiness... Other AEs: Dizziness (mild, 1 patient) Sources: Drowsiness (mild, 1 patient) |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Disc. AE: Asthenia, Nausea... AEs leading to discontinuation/dose reduction: Asthenia (1%) Sources: Nausea (4%) Dry mouth (1%) Vomiting (1%) Dizziness (2%) Insomnia (3%) Somnolence (2%) Agitation (1%) |
760 mg single, oral Overdose |
unknown, 25 years n = 1 Health Status: unknown Age Group: 25 years Sex: F Population Size: 1 Sources: |
Other AEs: Seizures, Tachycardia... Other AEs: Seizures (1 patient) Sources: Tachycardia (1 patient) Neuromuscular disorders NEC (1 patient) Hyperthermia (severe, 1 patient) |
360 mg 1 times / day multiple, oral Highest studied dose Dose: 360 mg, 1 times / day Route: oral Route: multiple Dose: 360 mg, 1 times / day Sources: |
unhealthy, adult |
|
2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
Other AEs: Dizziness, Sweating... Other AEs: Dizziness (grade 5) Sources: Sweating Nausea Vomiting Tremor Somnolence Sinus tachycardia |
AEs
AE | Significance | Dose | Population |
---|---|---|---|
Dizziness | mild, 1 patient | 800 mg single, oral Overdose |
unknown, 14 years n = 1 Health Status: unknown Age Group: 14 years Sex: F Population Size: 1 Sources: |
Drowsiness | mild, 1 patient | 800 mg single, oral Overdose |
unknown, 14 years n = 1 Health Status: unknown Age Group: 14 years Sex: F Population Size: 1 Sources: |
Agitation | 1% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Asthenia | 1% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Dry mouth | 1% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Vomiting | 1% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Dizziness | 2% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Somnolence | 2% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Insomnia | 3% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Nausea | 4% Disc. AE |
80 mg 1 times / day steady, oral (max) Studied dose Dose: 80 mg, 1 times / day Route: oral Route: steady Dose: 80 mg, 1 times / day Sources: |
unhealthy, 18-66 years n = 1063 Health Status: unhealthy Condition: depression Age Group: 18-66 years Sex: M+F Population Size: 1063 Sources: |
Neuromuscular disorders NEC | 1 patient | 760 mg single, oral Overdose |
unknown, 25 years n = 1 Health Status: unknown Age Group: 25 years Sex: F Population Size: 1 Sources: |
Seizures | 1 patient | 760 mg single, oral Overdose |
unknown, 25 years n = 1 Health Status: unknown Age Group: 25 years Sex: F Population Size: 1 Sources: |
Tachycardia | 1 patient | 760 mg single, oral Overdose |
unknown, 25 years n = 1 Health Status: unknown Age Group: 25 years Sex: F Population Size: 1 Sources: |
Hyperthermia | severe, 1 patient | 760 mg single, oral Overdose |
unknown, 25 years n = 1 Health Status: unknown Age Group: 25 years Sex: F Population Size: 1 Sources: |
Nausea | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
|
Sinus tachycardia | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
|
Somnolence | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
|
Sweating | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
|
Tremor | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
|
Vomiting | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
|
Dizziness | grade 5 | 2800 mg single, oral Overdose Dose: 2800 mg Route: oral Route: single Dose: 2800 mg Sources: |
unknown n = 1 Health Status: unknown Population Size: 1 Sources: |
PubMed
Title | Date | PubMed |
---|---|---|
The antidepressants imipramine, clomipramine, and citalopram induce apoptosis in human acute myeloid leukemia HL-60 cells via caspase-3 activation. | 1999 |
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Multicenter, placebo-controlled, fixed-dose study of citalopram in moderate-to-severe depression. | 1999 Dec |
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Bradycardia during citalopram treatment: a case report. | 1999 Feb |
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[Citalopram in forensic samples. Citalopram concentrations in samples from legal autopsies and from living persons in connection with traffic accidents or cases of violence in Denmark 1989-1996]. | 1999 Jul 26 |
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Citalopram and clozapine: potential drug interaction. | 2000 Apr |
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Citalopram and breast-feeding: serum concentration and side effects in the infant. | 2000 Jan 15 |
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Near fatal case of atrio-ventricular block induced by amitriptyline at therapeutic dose. | 2000 Sep |
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Selective serotonin reuptake inhibitors for late-life depression: a comparative review. | 2001 |
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First experiences in combination therapy using olanzapine with SSRIs (citalopram, paroxetine) in delusional depression. | 2001 |
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Citalopram: a comprehensive review. | 2001 Apr |
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Are newer antidepressants really "better tolerated"? | 2001 Apr |
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S33005, a novel ligand at both serotonin and norepinephrine transporters: II. Behavioral profile in comparison with venlafaxine, reboxetine, citalopram, and clomipramine. | 2001 Aug |
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Relationship between central serotonergic neurotransmission and reduction in alcohol intake by citalopram. | 2001 Aug 1 |
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Mood and behavioural disorders following traumatic brain injury: clinical evaluation and pharmacological management. | 2001 Feb |
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Effect of serotonin reuptake inhibitor on syndrome development in obese hyperglycemic mice (Umeå ob/ob). | 2001 Feb |
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Pharmacological characterisation of the decrease in 5-HT synthesis in the mouse brain evoked by the selective serotonin re-uptake inhibitor citalopram. | 2001 Feb |
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Citalopram-induced bruxism. | 2001 Feb |
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Female sexual dysfunction and antidepressant use. | 2001 Feb |
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Evidence for a serotonin transporter deficit in experimental acute liver failure. | 2001 Feb |
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[Depressive disorders in neurologic rehabilitation: therapy with paroxetine]. | 2001 Jan |
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Effects of chronic antidepressant treatments on 5-HT and NA transporters in rat brain: an autoradiographic study. | 2001 Jan |
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Catalepsy induced by the 5-HT(1A) receptor antagonist WAY 100635 in rats pretreated with the selective serotonin reuptake inhibitor citalopram. | 2001 Jan 12 |
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Does interaction between zinc and glutamate system play a significant role in the mechanism of antidepressant action? | 2001 Jan-Feb |
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Citalopram in refractory obsessive-compulsive disorder: an open study. | 2001 Jul |
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Involvement of adenosine in the effect of antidepressants on glutamate and aspartate release in the rat prefrontal cortex. | 2001 Jun |
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Citalopram versus nortriptyline in late-life depression: a 12-week randomized single-blind study. | 2001 Jun |
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Are there differences in the use of selective serotonin reuptake inhibitors and tricyclic antidepressants? A prescription database study. | 2001 Mar |
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Effects of MDMA (ecstasy) on prepulse inhibition and habituation of startle in humans after pretreatment with citalopram, haloperidol, or ketanserin. | 2001 Mar |
|
Quantitative radioluminography of serotonin uptake sites in the porcine brain. | 2001 Mar 15 |
|
A comparison of citalopram and paroxetine in the treatment of panic disorder: a randomized, single-blind study. | 2001 May |
|
Does mirtazapine have a more rapid onset than SSRIs? | 2001 May |
|
Escitalopram (S-enantiomer of citalopram): clinical efficacy and onset of action predicted from a rat model. | 2001 May |
|
Alzheimer's disease and related disorders. | 2001 May |
|
Rapid determination of citalopram in human plasma by high-performance liquid chromatography. | 2001 May 5 |
|
Trichotillomania associated with dementia: a case report. | 2001 May-Jun |
|
Distribution of serotonin, its metabolites and 5-HT transporters in the neostriatum of Lurcher and weaver mutant mice. | 2001 Sep |
|
A retrospective study of citalopram in adolescents with depression. | 2001 Summer |
Sample Use Guides
Initial Treatment Celexa (citalopram HBr) should be administered at an initial dose of 20 mg once daily, with an increase to a maximum dose of 40 mg/day at an interval of no less than one week. Doses above 40 mg/day are not recommended due to the risk of QT prolongation. Additionally, the only study pertinent to dose response for effectiveness did not demonstrate an advantage for the 60 mg/day dose over the 40 mg/day dose. Special Populations 20 mg/day is the maximum recommended dose for patients who are greater than 60 years of age, patients with hepatic impairment, and for CYP2C19 poor metabolizers or those patients taking cimetidine or another CYP2C19 inhibitor.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/27271269
It was investigated the mechanisms of cytotoxic effects of in vitro and in vivo citalopram treatment on liver and the following cytolethal events. For in vitro experiments, freshly isolated rat hepatocytes were exposed to citalopram along with/without various agents. In the in vitro experiments, citalopram (500 µM) exposure demonstrated cell death, a marked elevation in ROS formation, mitochondrial potential collapse, lysosomal membrane leakiness, glutathione (GSH) depletion and lipid peroxidation. In vivo biochemistry panel assays for liver enzymes function (AST, ALT and GGTP) and histological examination confirmed citalopram (20 mg/kg)-induced damage. Citalopram-induced oxidative stress cytotoxicity markers were significantly prevented by antioxidants, ROS scavengers, MPT pore sealing agents, endocytosis inhibitors, ATP generators and CYP inhibitors.
Substance Class |
Chemical
Created
by
admin
on
Edited
Fri Dec 15 15:24:18 GMT 2023
by
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on
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Record UNII |
I1E9D14F36
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Record Status |
Validated (UNII)
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Record Version |
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NCI_THESAURUS |
C265
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NCI_THESAURUS |
C94725
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m3587
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3724
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admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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100000090554
Created by
admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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C28932
Created by
admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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I1E9D14F36
Created by
admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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261-890-6
Created by
admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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I1E9D14F36
Created by
admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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KK-125
Created by
admin on Fri Dec 15 15:24:18 GMT 2023 , Edited by admin on Fri Dec 15 15:24:18 GMT 2023
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Related Record | Type | Details | ||
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PARENT -> SALT/SOLVATE | |||
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (TITRATION)
EP
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BASIS OF STRENGTH->SUBSTANCE |
ASSAY (HPLC)
USP
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Related Record | Type | Details | ||
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
at 254 nm; For the calculation of contents, multiply the peak areas by 0.6
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
EP
|
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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|
IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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IMPURITY -> PARENT |
CHROMATOGRAPHIC PURITY (HPLC/UV)
USP
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Related Record | Type | Details | ||
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ACTIVE MOIETY |