Overview
| Generic Names: | OPC 31; OPC-14597; aripiprazole |
|---|---|
| Trade Names: | Abilify; Abilitat |
| PharmGKB Accession Id: | PA10026 |
Description
Aripiprazole is an atypical antipsychotic medication used for the treatment of schizophrenia. It has also recently received FDA approval for the treatment of acute manic and mixed episodes associated with bipolar disorder. Aripiprazole appears to mediate its antipsychotic effects primarily by partial agonism at the D2 receptor. In addition to partial agonist activity at the D2 receptor, aripiprazole is also a partial agonist at the 5-HT1A receptor, and like the other atypical antipsychotics, aripiprazole displays an antagonist profile at the 5-HT2A receptor. Aripiprazole has moderate affinity for histamine and alpha adrenergic receptors, and no appreciable affinity for cholinergic muscarinic receptors. (source: Drug Bank)
Indication
For the treatment of schizophrenia (source: Drug Bank)
ATC Therapeutic Category
- N05AX:Other antipsychotics
Pharmacology, Interactions, and Contraindications
Mechanism Of Action
Aripiprazole exhibits high affinity for dopamine D2 and D3, serotonin 5-HT1A and 5- HT2A receptors, moderate affinity for dopamine D4, serotonin 5-HT2C and 5-HT7, alpha1-adrenergic and histamine H1 receptors and moderate affinity for the serotonin reuptake pump. Aripiprazole has no appreciable affinity for cholinergic muscarinic receptors. Aripiprazole functions as a partial agonist at the dopamine D2 and the serotonin 5-HT1A receptors, and as an antagonist at serotonin 5-HT2A receptor. (source: Drug Bank)
Pharmacology
Aripiprazole is a psychotropic agent belonging to the chemical class of benzisoxazole derivatives and is indicated for the treatment of schizophrenia. Aripiprazole is a selective monoaminergic antagonist with high affinity for the serotonin Type 2 (5HT2), dopamine Type 2 (D2), 1 and 2 adrenergic, and H1 histaminergic receptors. Aripiprazole acts as an antagonist at other receptors, but with lower potency. Antagonism at receptors other than dopamine and 5HT2 with similar receptor affinities may explain some of the other therapeutic and side effects of Aripiprazole. Aripiprazole's antagonism of histamine H1 receptors may explain the somnolence observed with this drug. Aripiprazole's antagonism of adrenergic a1 receptors may explain the orthostatic hypotension observed with this drug. (source: Drug Bank)
Food Interactions
Avoid alcohol (possible additive effect to CNS).
Food has no significant effect on absorption.
Take without regard to meals.
(source:
Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic. (source: Drug Bank)
Protein Binding
>99% (source: Drug Bank)
Isomeric SMILES Code:
c1cc(c(c(c1)Cl)Cl)N2CCN(CC2)CCCCOc3ccc4c(c3)NC(=O)CC4 (source: Drug Bank)
Curated Annotations (
)
-
rs1800497
at chr11:112776038
in
ANKK1
Phenotype: Compared with patients who had the A2/A2 (C/C) genotype, the positive and negative syndrome scale (PANSS) positive scores of A1/A1 (T/T) patients were 3.71 lower (p = 0.01) and of A1/A2 patients were 1.36 lower (p = 0.03) after 4-week aripiprazole treatment. These results suggest that A1 carriers are associated with superior therapeutic response on positive symptoms. Study size: 128 schizophrenic patients. Study population: Chinese.- Variant Name:
- TaqIA (C/T)
- Related Drugs:
- aripiprazole
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:18926547
-
rs1800497
at chr11:112776038
in
ANKK1
Phenotype: A meta-analysis, including eight individual studies, was not able to detect an association between clinical response to antipsychotics and the Taq1A variant. Study size: meta-analysis included 8 individual studies, 748 patients total.- Variant Name:
- TaqIA (C/T)
- Related Drugs:
- aripiprazole, Bromperidol, chlorpromazine, clozapine, haloperidol, nemonapride, risperidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:20194480
-
rs6277
at chr11:112788669
in
DRD2
Phenotype: Patients with C/C genotype were associated with poor aripiprazole response for excitement symptoms (measured on the positive and negative syndrome scale, PANSS - excitement subscale) when compared with T/T patients. Study size: 128 schizophrenic patients. Study population: Chinese.- Variant Name:
- C957T
- Related Drugs:
- aripiprazole
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:18926547
-
rs1799732
at chr11:112851462
in
DRD2
Phenotype: After 4-week aripiprazole treatment the −141C Ins/Del polymorphism had no significant effects on the positive and negative syndrome scale performance. Study size:128 schizophrenic patients. Study population: Chinese.- Variant Name:
- DRD2: -141C Ins/Del
- Related Drugs:
- aripiprazole
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:18926547
-
rs1799732
at chr11:112851462
in
DRD2
Phenotype: Results of this meta-analysis showed that the group of Del allele carrier was significantly associated with poorer antipsychotic drug response relative to the Ins/Ins genotype. Study size: meta-analysis included six individual studies, 687 patients total.- Variant Name:
- DRD2: -141C Ins/Del
- Related Drugs:
- aripiprazole, chlorpromazine, clozapine, olanzapine, risperidone
- Related Diseases:
- Schizophrenia
- Evidence:
-
PMID:20194480
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
|---|---|---|---|
|
ANKK1 |
|
Variants |
|
CYP2D6 |
|
Publications |
|
|
DRD2 |
|
Publications, Variants |
|
|
HTR1A |
|
Publications |
|
|
HTR2A |
|
Publications |
|
|
PRKCB |
|
Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| HTR1A |
|
(source: Drug Bank) |
| HTR2A |
|
(source: Drug Bank) |
| DRD2 |
|
(source: Drug Bank) |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| carbamazepine |
|
Carbamazepine decreases the effect of aripiprazole (source: Drug Bank) |
| itraconazole |
|
The imidazole increases the effect of aripiprazole (source: Drug Bank) |
| ketoconazole |
|
The imidazole increases the effect of aripiprazole (source: Drug Bank) |
| quinidine |
|
Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank) |
| quinidine |
|
Quinidine increases the effect and toxicity of aripiprazole (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
|
|
Movement Disorders |
|
Publications |
|
|
Weight gain |
|
Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.