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
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+
| 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 |
| 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 |
DescriptionCurator'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
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.
CNS Activity
Approval Year
Targets
| Primary Target | Pharmacology | Condition | Potency |
|---|---|---|---|
Target ID: CHEMBL224 |
|||
Target ID: CHEMBL217 |
Conditions
| Condition | Modality | Targets | Highest Phase | Product |
|---|---|---|---|---|
| Primary | SEROQUEL XR Approved Use1.1 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 Date2007 |
|||
| Primary | SEROQUEL XR Approved Use1.1 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 Date2007 |
|||
| Palliative | SEROQUEL XR Approved Use1.1 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 Date2007 |
Cmax
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
58.23 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
187.44 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
3.86 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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 EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/25025989 |
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
| Value | Dose | Co-administered | Analyte | Population |
|---|---|---|---|---|
17% |
unknown, unknown |
QUETIAPINE FUMARATE plasma | Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN |
Doses
| Dose | Population | Adverse events |
|---|---|---|
800 mg single, oral Highest studied dose |
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) Sources: Dizziness (10 patients) Constipation (4 patients) Tongue paralysis (1 patient) Dry mouth (1 patient) |
24 g single, oral Overdose |
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%) Sources: Tachycardia (56%) Hypotension (18%) Coma (10%) Agitation (6%) Respiratory depression (5%) Seizures (2%) Electrocardiogram QTc interval prolonged (4%) Death (grade 5, 3 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: |
Other AEs: Agitation, Somnolence... Other AEs: Agitation (26 patients) Sources: 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) |
24.4 g single, oral Overdose |
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) Sources: Tachycardia (9 patients) Respiratory depression (9 patients) |
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) Sources: Sinus tachycardia (1 patient) |
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 Sources: smoking cocaine |
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... |
AEs
| AE | Significance | Dose | Population |
|---|---|---|---|
| Dry mouth | 1 patient | 800 mg single, oral Highest studied dose |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 |
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 Sources: smoking cocaine |
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
| CYP3A4 | CYP2C9 | CYP2D6 | hERG |
|---|---|---|---|
OverviewOther
| Other Inhibitor | Other Substrate | Other Inducer |
|---|---|---|
Drug as perpetrator
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
| yes [IC50 16.9 uM] | ||||
| yes [IC50 66.1 uM] | ||||
| yes [Inhibition 150 uM] | ||||
| yes [Inhibition 30 uM] | ||||
| yes [Inhibition 30 uM] | ||||
| yes [Inhibition 30 uM] | ||||
| yes [Inhibition 30 uM] |
Drug as victim
| Target | Modality | Activity | Metabolite | Clinical 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 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2004/20639se1-017,016_seroquel_lbl.pdf Page: 4.0 |
Tox targets
| Target | Modality | Activity | Metabolite | Clinical evidence |
|---|---|---|---|---|
PubMed
| Title | Date | PubMed |
|---|---|---|
| New antidepressive and antipsychotic drugs in juvenile neuronal ceroid lipofuscinoses--a pilot study. | 2001 |
|
| Hypothesis and hypothesis testing in the clinical trial. | 2001 |
|
| Antipsychotic medications and the elderly: effects on cognition and implications for use. | 2001 |
|
| Asymptomatic QTc prolongation associated with quetiapine fumarate overdose in a patient being treated with risperidone. | 2001 Apr |
|
| Ziprasidone: a novel antipsychotic agent with a unique human receptor binding profile. | 2001 Aug 17 |
|
| Novel antipsychotics and acute dystonic reactions. | 2001 Dec |
|
| Clozapine use in patients with schizophrenia and the risk of diabetes, hyperlipidemia, and hypertension: a claims-based approach. | 2001 Dec |
|
| Dopamine D(2) receptors and their role in atypical antipsychotic action: still necessary and may even be sufficient. | 2001 Dec 1 |
|
| New onset diabetes and atypical antipsychotics. | 2001 Feb |
|
| The effects of concomitant phenytoin administration on the steady-state pharmacokinetics of quetiapine. | 2001 Feb |
|
| Treatment of the agitation of late-life psychosis and Alzheimer's disease. | 2001 Jan |
|
| Enhanced neurotensin neurotransmission is involved in the clinically relevant behavioral effects of antipsychotic drugs: evidence from animal models of sensorimotor gating. | 2001 Jan 15 |
|
| Diabetes mellitus associated with atypical antipsychotic medications: new case report and review of the literature. | 2001 Jul-Aug |
|
| Cataracts and quetiapine. | 2001 Jun |
|
| The 5-HT1A receptor in schizophrenia: a promising target for novel atypical neuroleptics? | 2001 Mar |
|
| Reduction of tardive dyskinesia with quetiapine. | 2001 Mar 1 |
|
| Electrooxidation potential as a tool in the early screening for new safer clozapine-like analogues. | 2001 Mar 1 |
|
| Schizophrenia: elevated mRNA for dopamine D2(Longer) receptors in frontal cortex. | 2001 Mar 5 |
|
| Re: Neuroleptic malignant syndrome associated with quetiapine. | 2001 May |
|
| [Clinical and pharmacological studies of the second generation antipsychotics]. | 2001 Nov |
|
| A comparison of the relative safety, efficacy, and tolerability of quetiapine and risperidone in outpatients with schizophrenia and other psychotic disorders: the quetiapine experience with safety and tolerability (QUEST) study. | 2001 Nov |
|
| Dopamine D(2) receptor occupancy is a common mechanism underlying animal models of antipsychotics and their clinical effects. | 2001 Nov |
|
| [Quetiapine poisoning]. | 2001 Nov 17 |
|
| Ziprasidone: profile on safety. | 2001 Oct |
|
| Inverse agonist actions of typical and atypical antipsychotic drugs at the human 5-hydroxytryptamine(2C) receptor. | 2001 Oct |
|
| 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 |
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| Update and recommendations for the use of antipsychotics in early-onset psychoses. | 2001 Summer |
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| Quetiapine and cataracts. | 2002 Feb |
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| Amisulpride, an unusual "atypical" antipsychotic: a meta-analysis of randomized controlled trials. | 2002 Feb |
|
| Ziprasidone: an atypical antipsychotic drug for the treatment of schizophrenia. | 2002 Jan |
|
| Does cognitive function improve with quetiapine in comparison to haloperidol? | 2002 Jan 15 |
|
| [Drug-induced akathisia]. | 2002 Jan 19 |
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
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on
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| Record UNII |
2S3PL1B6UJ
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NCI_THESAURUS |
C29710
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NCI_THESAURUS |
C66885
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111974-72-2
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8708
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100000091312
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m9425
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C47700
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CHEMBL716
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5281025
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HH-80
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2S3PL1B6UJ
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SUB56025
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1592704
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DBSALT002790
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DTXSID3044201
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221153
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2S3PL1B6UJ
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SUB15074MIG
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ACTIVE MOIETY |
