药品详细
Aripiprazole(阿立哌唑)
化学结构式图
中文名
阿立哌唑
英文名
Aripiprazole
分子式
C23H27Cl2N3O2
化学名
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-1,2,3,4-tetrahydroquinolin-2-one
分子量
Average: 448.385
Monoisotopic: 447.148032537
Monoisotopic: 447.148032537
CAS号
129722-12-9
ATC分类
N05A 未知
药物类型
small molecule
阶段
approved
商品名
同义名
基本介绍
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.
生产厂家
- Bristol-Myers Squibb Company
- Otsuka pharmaceutical co ltd
- Otsuka pharmaceutical development and commercialization inc
封装厂家
- Bristol-Myers Squibb Co.
- Bryant Ranch Prepack
- Cardinal Health
- Comprehensive Consultant Services Inc.
- DispenseXpress Inc.
- E.R. Squibb and Sons LLC
- Murfreesboro Pharmaceutical Nursing Supply
- Otsuka America
- PD-Rx Pharmaceuticals Inc.
- Physician Partners Ltd.
- Physicians Total Care Inc.
- Quality Care
- Rebel Distributors Corp.
- Remedy Repack
- Resource Optimization and Innovation LLC
- Southwood Pharmaceuticals
- Stat Rx Usa
参考
| Synthesis Reference | Not Available |
| General Reference | Not Available |
剂型
规格
化合物类型
| Type | small molecule |
| Classes |
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| Substructures |
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适应症
药理
| Indication | For the treatment of schizophrenia and related psychotic disorders. |
| Pharmacodynamics | 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. |
| Mechanism of action | Aripiprazole's antipsychotic activity is likely due to a combination of antagonism at D2 receptors in the mesolimbic pathway and 5HT2A receptors in the frontal cortex. Antagonism at D2 receptors relieves positive symptoms while antagonism at 5HT2A receptors relieves negative symptoms of schizophrenia. |
| Absorption | Not Available |
| Volume of distribution |
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| Protein binding | >99% |
| Metabolism |
Hepatic.
|
| Route of elimination | Less than 1% of unchanged aripiprazole was excreted in the urine and approximately 18% of the oral dose was recovered unchanged in the feces. |
| Half life | 75-146 hours |
| Clearance | Not Available |
| Toxicity | Not Available |
| Affected organisms |
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| Pathways | Not Available |
理化性质
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| State | solid | ||||||||||||||||||||||||||||||||||||||||||
| Experimental Properties |
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| Predicted Properties |
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药物相互作用
| Drug | Interaction |
|---|---|
| Carbamazepine | Carbamazepine, a strong CYP3A4 inducer, may decrease the serum concentration of aripiprazole by increasing its metabolism. |
| Dihydroquinidine barbiturate | Quinidine increases the effect and toxicity of aripiprazole |
| Etravirine | Ariprazole, when administered concomitantly with etravirine (a strong CYP3A4 inducer), may experience a decrease in serum concentration. It is recommended to increase the dose of oral aripiprazole to maintain therapeutic efficacy, and to adjust the dose of aripiprazole appropriately when the dose of etravirine is altered. |
| Itraconazole | Itraconazole may increase the effect of aripiprazole. |
| Ketoconazole | Ketoconazole may increase the effect of aripiprazole. |
| Quinidine | Quinidine increases the effect and toxicity of aripiprazole |
| Quinidine barbiturate | Quinidine increases the effect and toxicity of aripiprazole |
| Tacrine | Tacrine, a central acetylcholinesterase inhibitor, may augment the central neurotoxic effect of antipsychotics such as Aripiprazole. Monitor for extrapyramidal symptoms. |
| Telithromycin | Telithromycin may reduce clearance of Aripiprazole. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Aripiprazole if Telithromycin is initiated, discontinued or dose changed. |
| Terbinafine | Terbinafine may reduce the metabolism and clearance of Aripiprazole. Consider alternate therapy or monitor for therapeutic/adverse effects of Aripiprazole if Terbinafine is initiated, discontinued or dose changed. |
| Tetrabenazine | May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects. |
| Triprolidine | The CNS depressants, Triprolidine and Aripiprazole, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy. |
| Voriconazole | Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of aripiprazole by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of aripiprazole if voriconazole is initiated, discontinued or dose changed. |
食物相互作用
- Avoid alcohol (possible additive effect to CNS).
- Food has no significant effect on absorption.
- Take without regard to meals.
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