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Details

Stereochemistry ACHIRAL
Molecular Formula 2C21H25N3O2S.C4H4O4
Molecular Weight 883.086
Optical Activity NONE
Defined Stereocenters 0 / 0
E/Z Centers 1
Charge 0

SHOW SMILES / InChI
Structure of QUETIAPINE FUMARATE

SMILES

OC(=O)\C=C\C(O)=O.OCCOCCN1CCN(CC1)C2=NC3=C(SC4=C2C=CC=C4)C=CC=C3.OCCOCCN5CCN(CC5)C6=NC7=C(SC8=C6C=CC=C8)C=CC=C7

InChI

InChIKey=ZTHJULTYCAQOIJ-WXXKFALUSA-N
InChI=1S/2C21H25N3O2S.C4H4O4/c2*25-14-16-26-15-13-23-9-11-24(12-10-23)21-17-5-1-3-7-19(17)27-20-8-4-2-6-18(20)22-21;5-3(6)1-2-4(7)8/h2*1-8,25H,9-16H2;1-2H,(H,5,6)(H,7,8)/b;;2-1+

HIDE SMILES / InChI

Molecular Formula C4H4O4
Molecular Weight 116.0722
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 1
Optical Activity NONE

Molecular Formula C21H25N3O2S
Molecular Weight 383.507
Charge 0
Count
Stereochemistry ACHIRAL
Additional Stereochemistry No
Defined Stereocenters 0 / 0
E/Z Centers 0
Optical Activity NONE

Description
Curator's Comment: description was created based on several sources, including https://www.ncbi.nlm.nih.gov/pubmed/12973385 | https://www.ncbi.nlm.nih.gov/pubmed/10839333

Quetiapine, marketed as SEROQUEL XR, is an atypical antipsychotic approved for the treatment of schizophrenia, bipolar disorder, and along with an antidepressant to treat major depressive disorder. The mechanism of action of SEROQUEL XR in the treatment of schizophrenia, bipolar disorder and major depressive disorder (MDD), is unknown. However, its efficacy in schizophrenia could be mediated through a combination of dopamine type 2 (D2) and serotonin type 2A (5HT2A) antagonism. The active metabolite, N-desalkyl quetiapine (norquetiapine), has similar activity at D2, but greater activity at 5HT2A receptors, than the parent drug (quetiapine). Quetiapine’s efficacy in bipolar depression and MDD may partly be explained by the high affinity and potent inhibitory effects that norquetiapine exhibits for the norepinephrine transporter. Antagonism at receptors other than dopamine and serotonin with similar or greater affinities may explain some of the other effects of quetiapine and norquetiapine: antagonism at histamine H1 receptors may explain the somnolence, antagonism at adrenergic α1b receptors may explain the orthostatic hypotension, and antagonism at muscarinic M1 receptors may explain the anticholinergic effects. Quetiapine and norquetiapine have affinity for multiple neurotransmitter receptors including dopamine D1 and D2, serotonin 5HT1A and 5HT2A, histamine H1, muscarinic M1, and adrenergic α1b and α2 receptors. Quetiapine differs from norquetiapine in having no appreciable affinity for muscarinic M1 receptors whereas norquetiapine has high affinity. Quetiapine and norquetiapine lack appreciable affinity for benzodiazepine receptors.

Approval Year

Targets

Targets

Conditions

Conditions

ConditionModalityTargetsHighest PhaseProduct
Primary
SEROQUEL XR

Approved Use

1.1 Schizophrenia. SEROQUEL XR is indicated for the treatment of schizophrenia. The efficacy of SEROQUEL XR in schizophrenia was established in one 6-week and one maintenance trial in adults with schizophrenia. Efficacy was supported by three 6 week trials in adults with schizophrenia and one 6-week trial in adolescents with schizophrenia (13-17 years) treated with SEROQUEL. 1.2 Bipolar Disorder SEROQUEL XR is indicated for the acute treatment of manic or mixed episodes associated with bipolar I disorder, both as monotherapy and as an adjunct to lithium or divalproex. The efficacy of SEROQUEL XR in manic or mixed episodes of bipolar I disorder was established in one 3-week trial in adults with manic or mixed episodes associated with bipolar I disorder. Efficacy was supported by two 12-week monotherapy trials and one 3-week adjunctive trial in adults with manic episodes associated with bipolar I disorder as well as one 3-week monotherapy trial in children and adolescents (10– 17 years) with manic episodes associated with bipolar I disorder treated with SEROQUEL. 1.3 Adjunctive Treatment of Major Depressive Disorder (MDD) ROQUEL XR is indicated for use as adjunctive therapy to antidepressants for the treatment of MDD. The efficacy of SEROQUEL XR as adjunctive therapy to antidepressants in MDD was established in two 6-week trials in adults with MDD who had an inadequate response to antidepressant treatment.

Launch Date

1.17936003E12
Primary
SEROQUEL XR

Approved Use

1.1 Schizophrenia. SEROQUEL XR is indicated for the treatment of schizophrenia. The efficacy of SEROQUEL XR in schizophrenia was established in one 6-week and one maintenance trial in adults with schizophrenia. Efficacy was supported by three 6 week trials in adults with schizophrenia and one 6-week trial in adolescents with schizophrenia (13-17 years) treated with SEROQUEL. 1.2 Bipolar Disorder SEROQUEL XR is indicated for the acute treatment of manic or mixed episodes associated with bipolar I disorder, both as monotherapy and as an adjunct to lithium or divalproex. The efficacy of SEROQUEL XR in manic or mixed episodes of bipolar I disorder was established in one 3-week trial in adults with manic or mixed episodes associated with bipolar I disorder. Efficacy was supported by two 12-week monotherapy trials and one 3-week adjunctive trial in adults with manic episodes associated with bipolar I disorder as well as one 3-week monotherapy trial in children and adolescents (10– 17 years) with manic episodes associated with bipolar I disorder treated with SEROQUEL. 1.3 Adjunctive Treatment of Major Depressive Disorder (MDD) ROQUEL XR is indicated for use as adjunctive therapy to antidepressants for the treatment of MDD. The efficacy of SEROQUEL XR as adjunctive therapy to antidepressants in MDD was established in two 6-week trials in adults with MDD who had an inadequate response to antidepressant treatment.

Launch Date

1.17936003E12
Palliative
SEROQUEL XR

Approved Use

1.1 Schizophrenia. SEROQUEL XR is indicated for the treatment of schizophrenia. The efficacy of SEROQUEL XR in schizophrenia was established in one 6-week and one maintenance trial in adults with schizophrenia. Efficacy was supported by three 6 week trials in adults with schizophrenia and one 6-week trial in adolescents with schizophrenia (13-17 years) treated with SEROQUEL. 1.2 Bipolar Disorder SEROQUEL XR is indicated for the acute treatment of manic or mixed episodes associated with bipolar I disorder, both as monotherapy and as an adjunct to lithium or divalproex. The efficacy of SEROQUEL XR in manic or mixed episodes of bipolar I disorder was established in one 3-week trial in adults with manic or mixed episodes associated with bipolar I disorder. Efficacy was supported by two 12-week monotherapy trials and one 3-week adjunctive trial in adults with manic episodes associated with bipolar I disorder as well as one 3-week monotherapy trial in children and adolescents (10– 17 years) with manic episodes associated with bipolar I disorder treated with SEROQUEL. 1.3 Adjunctive Treatment of Major Depressive Disorder (MDD) ROQUEL XR is indicated for use as adjunctive therapy to antidepressants for the treatment of MDD. The efficacy of SEROQUEL XR as adjunctive therapy to antidepressants in MDD was established in two 6-week trials in adults with MDD who had an inadequate response to antidepressant treatment.

Launch Date

1.17936003E12
Cmax

Cmax

ValueDoseCo-administeredAnalytePopulation
58.23 ng/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
60.11 ng/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
58.42 ng/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
AUC

AUC

ValueDoseCo-administeredAnalytePopulation
187.44 ng × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
190.39 ng × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
197.55 ng × h/mL
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
T1/2

T1/2

ValueDoseCo-administeredAnalytePopulation
3.86 h
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE / MALE
food status: FASTED
3.98 h
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: MALE
food status: FASTED
3.85 h
25 mg single, oral
dose: 25 mg
route of administration: Oral
experiment type: SINGLE
co-administered:
QUETIAPINE FUMARATE plasma
Homo sapiens
population: HEALTHY
age: ADULT
sex: FEMALE
food status: FASTED
Funbound

Funbound

ValueDoseCo-administeredAnalytePopulation
17%
unknown, unknown
QUETIAPINE FUMARATE plasma
Homo sapiens
population: UNKNOWN
age: UNKNOWN
sex: UNKNOWN
food status: UNKNOWN
Doses

Doses

DosePopulationAdverse events​
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
unhealthy, 18 - 60 years
n = 14
Health Status: unhealthy
Condition: schizophrenia
Age Group: 18 - 60 years
Sex: M+F
Population Size: 14
Sources:
Other AEs: Somnolence, Dizziness...
Other AEs:
Somnolence (13 patients)
Dizziness (10 patients)
Constipation (4 patients)
Tongue paralysis (1 patient)
Dry mouth (1 patient)
Sources:
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Disc. AE: Drowsiness, Tachycardia...
AEs leading to
discontinuation/dose reduction:
Drowsiness (76%)
Tachycardia (56%)
Hypotension (18%)
Coma (10%)
Agitation (6%)
Respiratory depression (5%)
Seizures (2%)
Electrocardiogram QTc interval prolonged (4%)
Death (grade 5, 3 patients)
Sources:
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Other AEs: Agitation, Somnolence...
Other AEs:
Agitation (26 patients)
Somnolence (24 patients)
Headache (18 patients)
Dizziness (11 patient)
Constipation (11 patient)
Insomnia (10 patients)
Tachycardia (7 patients)
Pain (7 patients)
Pharyngitis (7 patients)
Rash (7 patients)
Alanine aminotransferase increased (6 patients)
Dry mouth (6 patients)
Dyspepsia (6 patients)
Nausea (6 patients)
Asthenia (5 patients)
Vomiting (1 patient)
Sources:
24.4 g single, oral
Overdose
Dose: 24.4 g
Route: oral
Route: single
Dose: 24.4 g
Sources:
unknown, 22 - 49 years
n = 9
Health Status: unknown
Age Group: 22 - 49 years
Sex: M+F
Population Size: 9
Sources:
Disc. AE: Somnolence, Tachycardia...
AEs leading to
discontinuation/dose reduction:
Somnolence (9 patients)
Tachycardia (9 patients)
Respiratory depression (9 patients)
Sources:
15 g single, oral
Overdose
Dose: 15 g
Route: oral
Route: single
Dose: 15 g
Co-administed with::
lithium
Sources:
unhealthy, 32 years
n = 1
Health Status: unhealthy
Condition: bipolar disorder
Age Group: 32 years
Sex: M
Population Size: 1
Sources:
Disc. AE: Postural hypotension, Sinus tachycardia...
AEs leading to
discontinuation/dose reduction:
Postural hypotension (1 patient)
Sinus tachycardia (1 patient)
Sources:
400 mg 2 times / day steady, oral (max)
Highest studied dose
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 40 - 72 years
n = 5
Health Status: unhealthy
Condition: schizophrenia
Age Group: 40 - 72 years
Sex: M+F
Population Size: 5
Sources:
Disc. AE: Bladder distension...
AEs leading to
discontinuation/dose reduction:
Bladder distension (1 patient)
Sources:
1.2 g single, oral
Overdose
Dose: 1.2 g
Route: oral
Route: single
Dose: 1.2 g
Co-administed with::
alcohol
smoking cocaine
Sources:
unknown, 45 years
n = 1
Health Status: unknown
Condition: abuse, hypertension, type 2 diabetes mellitus, and schizoaffective disorder
Age Group: 45 years
Sex: M
Population Size: 1
Sources:
Disc. AE: LBBB...
AEs leading to
discontinuation/dose reduction:
LBBB (1 patient)
Sources:
600 mg 1 times / day steady, oral (max)
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 15
Health Status: unhealthy
Condition: cannabis dependence
Age Group: adult
Sex: unknown
Population Size: 15
Sources:
Other AEs: Fatigue, Somnolence...
Other AEs:
Fatigue (80%)
Somnolence (47%)
Sources:
AEs

AEs

AESignificanceDosePopulation
Dry mouth 1 patient
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
unhealthy, 18 - 60 years
n = 14
Health Status: unhealthy
Condition: schizophrenia
Age Group: 18 - 60 years
Sex: M+F
Population Size: 14
Sources:
Tongue paralysis 1 patient
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
unhealthy, 18 - 60 years
n = 14
Health Status: unhealthy
Condition: schizophrenia
Age Group: 18 - 60 years
Sex: M+F
Population Size: 14
Sources:
Dizziness 10 patients
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
unhealthy, 18 - 60 years
n = 14
Health Status: unhealthy
Condition: schizophrenia
Age Group: 18 - 60 years
Sex: M+F
Population Size: 14
Sources:
Somnolence 13 patients
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
unhealthy, 18 - 60 years
n = 14
Health Status: unhealthy
Condition: schizophrenia
Age Group: 18 - 60 years
Sex: M+F
Population Size: 14
Sources:
Constipation 4 patients
800 mg single, oral
Highest studied dose
Dose: 800 mg
Route: oral
Route: single
Dose: 800 mg
Sources:
unhealthy, 18 - 60 years
n = 14
Health Status: unhealthy
Condition: schizophrenia
Age Group: 18 - 60 years
Sex: M+F
Population Size: 14
Sources:
Coma 10%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Hypotension 18%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Seizures 2%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Electrocardiogram QTc interval prolonged 4%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Respiratory depression 5%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Tachycardia 56%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Agitation 6%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Drowsiness 76%
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Death grade 5, 3 patients
Disc. AE
24 g single, oral
Overdose
Dose: 24 g
Route: oral
Route: single
Dose: 24 g
Sources:
unknown, 18 - 84 years
n = 945
Health Status: unknown
Condition: abuse
Age Group: 18 - 84 years
Sex: M+F
Population Size: 945
Sources:
Vomiting 1 patient
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Insomnia 10 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Constipation 11 patient
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Dizziness 11 patient
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Headache 18 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Somnolence 24 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Agitation 26 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Asthenia 5 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Alanine aminotransferase increased 6 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Dry mouth 6 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Dyspepsia 6 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Nausea 6 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Pain 7 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Pharyngitis 7 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Rash 7 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Tachycardia 7 patients
750 mg 1 times / day steady, oral
Highest studied dose
Dose: 750 mg, 1 times / day
Route: oral
Route: steady
Dose: 750 mg, 1 times / day
Sources:
unhealthy, 20 - 61 years
n = 96
Health Status: unhealthy
Condition: schizophrenia
Age Group: 20 - 61 years
Sex: M+F
Population Size: 96
Sources:
Respiratory depression 9 patients
Disc. AE
24.4 g single, oral
Overdose
Dose: 24.4 g
Route: oral
Route: single
Dose: 24.4 g
Sources:
unknown, 22 - 49 years
n = 9
Health Status: unknown
Age Group: 22 - 49 years
Sex: M+F
Population Size: 9
Sources:
Somnolence 9 patients
Disc. AE
24.4 g single, oral
Overdose
Dose: 24.4 g
Route: oral
Route: single
Dose: 24.4 g
Sources:
unknown, 22 - 49 years
n = 9
Health Status: unknown
Age Group: 22 - 49 years
Sex: M+F
Population Size: 9
Sources:
Tachycardia 9 patients
Disc. AE
24.4 g single, oral
Overdose
Dose: 24.4 g
Route: oral
Route: single
Dose: 24.4 g
Sources:
unknown, 22 - 49 years
n = 9
Health Status: unknown
Age Group: 22 - 49 years
Sex: M+F
Population Size: 9
Sources:
Postural hypotension 1 patient
Disc. AE
15 g single, oral
Overdose
Dose: 15 g
Route: oral
Route: single
Dose: 15 g
Co-administed with::
lithium
Sources:
unhealthy, 32 years
n = 1
Health Status: unhealthy
Condition: bipolar disorder
Age Group: 32 years
Sex: M
Population Size: 1
Sources:
Sinus tachycardia 1 patient
Disc. AE
15 g single, oral
Overdose
Dose: 15 g
Route: oral
Route: single
Dose: 15 g
Co-administed with::
lithium
Sources:
unhealthy, 32 years
n = 1
Health Status: unhealthy
Condition: bipolar disorder
Age Group: 32 years
Sex: M
Population Size: 1
Sources:
Bladder distension 1 patient
Disc. AE
400 mg 2 times / day steady, oral (max)
Highest studied dose
Dose: 400 mg, 2 times / day
Route: oral
Route: steady
Dose: 400 mg, 2 times / day
Sources:
unhealthy, 40 - 72 years
n = 5
Health Status: unhealthy
Condition: schizophrenia
Age Group: 40 - 72 years
Sex: M+F
Population Size: 5
Sources:
LBBB 1 patient
Disc. AE
1.2 g single, oral
Overdose
Dose: 1.2 g
Route: oral
Route: single
Dose: 1.2 g
Co-administed with::
alcohol
smoking cocaine
Sources:
unknown, 45 years
n = 1
Health Status: unknown
Condition: abuse, hypertension, type 2 diabetes mellitus, and schizoaffective disorder
Age Group: 45 years
Sex: M
Population Size: 1
Sources:
Somnolence 47%
600 mg 1 times / day steady, oral (max)
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 15
Health Status: unhealthy
Condition: cannabis dependence
Age Group: adult
Sex: unknown
Population Size: 15
Sources:
Fatigue 80%
600 mg 1 times / day steady, oral (max)
MTD
Dose: 600 mg, 1 times / day
Route: oral
Route: steady
Dose: 600 mg, 1 times / day
Sources:
unhealthy, adult
n = 15
Health Status: unhealthy
Condition: cannabis dependence
Age Group: adult
Sex: unknown
Population Size: 15
Sources:
Overview

OverviewOther

Other InhibitorOther SubstrateOther Inducer





Drug as perpetrator​Drug as victim

Drug as victim

TargetModalityActivityMetaboliteClinical evidence
yes [Km 12.3 uM]
yes
yes
yes (co-administration study)
Comment: all metabolites (5) formed from CYP3A4 metabolism; ketoconazole reduces clearance by 84%, increasing maximum plasma concentration by 335%; phenytoin increases clearance by 5-fold
Page: 4.0
Tox targets

Tox targets

TargetModalityActivityMetaboliteClinical evidence
PubMed

PubMed

TitleDatePubMed
Review of atypical antipsychotics and weight gain.
2001
[Receptor occupancy and antipsychotic drug action measured by PET and SPECT].
2001
Atypical antipsychotics: new directions and new challenges in the treatment of schizophrenia.
2001
Asymptomatic QTc prolongation associated with quetiapine fumarate overdose in a patient being treated with risperidone.
2001 Apr
Quetiapine for Tourette's syndrome.
2001 Apr
Granulocytopenia with clozapine and quetiapine.
2001 Apr
Failed challenge with quetiapine after neuroleptic malignant syndrome with conventional antipsychotics.
2001 Aug
The health economic implications of treatment with quetiapine: an audit of long-term treatment for patients with chronic schizophrenia.
2001 Aug
In vivo 5-HT2A receptor blockade by quetiapine: an R91150 single photon emission tomography study.
2001 Aug
Clozapine use in patients with schizophrenia and the risk of diabetes, hyperlipidemia, and hypertension: a claims-based approach.
2001 Dec
Long-term remission of schizophrenia in an adolescent treated with quetiapine.
2001 Fall
The effects of concomitant phenytoin administration on the steady-state pharmacokinetics of quetiapine.
2001 Feb
Bodyweight gain with atypical antipsychotics. A comparative review.
2001 Jan
Consistency of atypical antipsychotic superiority to placebo in recent clinical trials.
2001 Jan 1
Use of atypical antipsychotics in mood disorders.
2001 Jul
Acute neutropenia in a patient treated with quetiapine.
2001 Jul-Aug
Cataracts and quetiapine.
2001 Jun
Neuropsychological change in patients with schizophrenia after treatment with quetiapine or haloperidol.
2001 Mar
Quetiapine-associated hypomania in a woman with schizoaffective disorder.
2001 Mar
Differing tolerability profiles among atypical antipsychotics.
2001 Mar
Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex.
2001 Mar 5
Successful outcome using quetiapine in a case of treatment-resistant schizophrenia with assaultive behavior.
2001 May 30
Short-term inpatient pharmacotherapy of schizophrenia.
2001 May-Jun
[Clinical and pharmacological studies of the second generation antipsychotics].
2001 Nov
Dopamine D(2) receptor occupancy is a common mechanism underlying animal models of antipsychotics and their clinical effects.
2001 Nov
Potent antagonism of 5-HT(3) and 5-HT(6) receptors by olanzapine.
2001 Nov 2
Ziprasidone: profile on safety.
2001 Oct
Quetiapine: efficacy and tolerability in schizophrenia.
2001 Oct
Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor.
2001 Oct
Efficacy of antipsychotic agents at human 5-HT(1A) receptors determined by [3H]WAY100,635 binding affinity ratios: relationship to efficacy for G-protein activation.
2001 Oct 5
A case of depersonalization-derealization syndrome during treatment with quetiapine.
2001 Sep
Priapism from quetiapine overdose: first report and proposal of mechanism.
2001 Sep
Symptom reduction and suicide risk among patients treated with placebo in antipsychotic clinical trials: an analysis of the food and drug administration database.
2001 Sep
Effectiveness of quetiapine in the management of psychotic depression in an adolescent boy with bipolar disorder, mixed, with psychosis.
2001 Summer
Effects of newer antipsychotics on extrapyramidal function.
2002
Ziprasidone: an atypical antipsychotic drug for the treatment of schizophrenia.
2002 Jan
Antipsychotic medication adherence: is there a difference between typical and atypical agents?
2002 Jan
Patents

Sample Use Guides

Schizophrenia- Adults: Day 1: 300 mg/day Dose increases can be made at intervals as short as 1 day and in increments of up to 300 mg/day Schizophrenia-Adolescents: (13 to 17 years): Day 1: 50 mg/day; Day 2: 100 mg/day; Day 3: 200 mg/day; Day 4: 300 mg/day; Day 5: 400 mg/day; Bipolar I Disorder manic or mixed-Acute monotherapy or adjunct to lithium or divalproex-Adults: Day 1: 300 mg/day; Day 2: 600 mg/day; Day 3: between 400 and 800 mg/day. Major Depressive Disorder Adjunctive Therapy with Antidepressants: Adults: Day 1: 50 mg/day; Day 2: 50 mg/day; Day 3: 150 mg/day Bipolar I Disorder, manic ­Acute monotherapy: Children and Adolescents (10 to 17 years) : Day 1: 50 mg/day; Day 2: 100 mg/day; Day 3: 200 mg/day; Day 4: 300 mg/day; Day 5: 400 mg/day.
Route of Administration: Oral
In Vitro Use Guide
Curator's Comment: The antidepressant activity of quetiapine is considered to be mediated by the active metabolite N-desalkylquetiapine, which is mainly formed by CYP3A4. N-desalkylquetiapine is metabolized by both CYP2D6 and CYP3A4 in vitro with preference for the former enzyme. The pharmacologically active metabolite, 7-hydroxy-N-desalkylquetiapine, was exclusively formed by CYP2D6, whereas the two other metabolites were mainly formed by CYP3A4.
Unknown
Substance Class Chemical
Created
by admin
on Fri Dec 16 19:43:04 UTC 2022
Edited
by admin
on Fri Dec 16 19:43:04 UTC 2022
Record UNII
2S3PL1B6UJ
Record Status Validated (UNII)
Record Version
  • Download
Name Type Language
QUETIAPINE FUMARATE
JAN   MART.   ORANGE BOOK   USAN   USP-RS   VANDF   WHO-DD  
USAN  
Official Name English
Quetiapine fumarate [WHO-DD]
Common Name English
UTAPINE
Brand Name English
ZM 204,636
Code English
SEROQUEL
Brand Name English
ETHANOL, 2-(2-(4-DIBENZO(B,F)(1,4)THIAZEPIN-11-YL-1-PIPERAZINYL)ETHOXY)-, (E)-2-BUTENEDIOATE (2:1)
Common Name English
ZD5077
Code English
ICI 204,636
Code English
FK947E
Code English
ZD-5077
Code English
QUETIAPINE (AS FUMARATE)
Common Name English
FK-947E
Code English
QUETIAPINE FUMARATE [ORANGE BOOK]
Common Name English
QUETIAPINE FUMARATE [USP-RS]
Common Name English
ZM-204636
Code English
QUETIAPINE FUMARATE [USAN]
Common Name English
QUETIAPINE FUMARATE [MART.]
Common Name English
QUETIAPINE HEMIFUMARATE
MI  
Common Name English
QUETIAPINE FUMARATE [EP MONOGRAPH]
Common Name English
ICI-204636
Code English
QUETIAPINE FUMARATE [VANDF]
Common Name English
QUETIAPINE HEMIFUMARATE [MI]
Common Name English
QUETIAPINE FUMARATE [JAN]
Common Name English
2-(2-(4-DIBENZO(B,F)(1,4)THIAZEPIN-11-YL-1-PIPERAZINYL)ETHOXY)ETHANOL FUMARATE (2:1)
Common Name English
QUETIAPINE FUMARATE [USP MONOGRAPH]
Common Name English
Classification Tree Code System Code
NCI_THESAURUS C29710
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
NCI_THESAURUS C66885
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
Code System Code Type Description
CAS
111974-72-2
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
CHEBI
8708
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
MERCK INDEX
M9425
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY Merck Index
NCI_THESAURUS
C47700
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
ChEMBL
CHEMBL716
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
PUBCHEM
5281025
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
USAN
HH-80
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
DAILYMED
2S3PL1B6UJ
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
EVMPD
SUB56025
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
RS_ITEM_NUM
1592704
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
DRUG BANK
DBSALT002790
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
EPA CompTox
DTXSID3044201
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
RXCUI
221153
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY RxNorm
FDA UNII
2S3PL1B6UJ
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
EVMPD
SUB15074MIG
Created by admin on Fri Dec 16 19:43:05 UTC 2022 , Edited by admin on Fri Dec 16 19:43:05 UTC 2022
PRIMARY
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