Product information

Aripiprazole Basic information

Outline EU approves aripiprazole for treatment of schizophrenia Metabolize Toxicity Drug Interactions Adverse reactions Application

Product Name:	Aripiprazole
Synonyms:	ARIPIPRAZOLE;ARIPIPRAZOLE-D8;ABILIFY;ABILITAT;7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydrocarbostyril;OPC 14597;OPC 31;7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolinone
CAS:	129722-12-9
MF:	C23H27Cl2N3O2
MW:	448.39
EINECS:	200-835-2
Product Categories:	INORGANIC & ORGANIC CHEMICALS;Active Pharmaceutical Ingredients;API;Heterocyclic Compounds;Chemistry;Intermediates & Fine Chemicals;Neurochemicals;Pharmaceuticals;Isotope Labeled Compounds;Heterocycles
Mol File:	129722-12-9.mol

Aripiprazole Chemical Properties

mp	139°C
storage temp.	-20°C Freezer
CAS DataBase Reference	129722-12-9(CAS DataBase Reference)

Safety Information

Hazard Codes	F,Xn
Risk Statements	11-20/21/22-36
Safety Statements	16-36/37
HS Code	29349990
Hazardous Substances Data	129722-12-9(Hazardous Substances Data)

MSDS Information

Provider	Language
Aripiprazole	English

Aripiprazole Usage And Synthesis

Outline	Aripiprazole is a new kind of highly lipid soluble quinoline derivatives, its pharmacological effects characteristic is that it is not only the postsynaptic dopamine D 2 receptor antagonist, but also the presynaptic dopamine D 2 receptor agonist,it can also excite D 1, D 3, D 4 receptors ; it has dual effect of partial activation or receptor antagonistic on 5-HT 1A receptor ; it has a completely antagonistic action on the 5-HT 2A receptor. This feature is different from the first generation, and atypical antipsychotics which belong to the second-generation antipsychotic drugs, and therefore it is called dopamine system stabilizer or third generation antipsychotic. Since it is sold in the market, it is mainly used in clinical schizophrenia, treatment of affective disorders and other psychiatric disorders. According to the literature, aripiprazole has significant effects on schizophrenia positive and negative symptoms and anxiety, depression, cognitive function , while higher safety. It was also reported that the drug can also treat other mental disorders, such as mood disorders manic episodes, senile dementia associated with mental disorders, anxiety disorders, children's behavioral disorders, depression.
EU approves aripiprazole for treatment of schizophrenia	Nowadays,Bristol-Myers Squibb and Otsuka Pharmaceutical Company announced that the European Union has approved Abilify (aripiprazole) in the treatment of schizophrenia listing application.  Schizophrenia affects 1% of the global population, and more in young adults. Schizophrenia affects thinking, emotional control and decision-making ability of the patient. Schizophrenia-positive patients will have symptoms such as hallucinations and delusions, patients with negative symptoms are social withdrawal, lack of emotional changes.  In 2002 the FDA approved Abilify for the treatment of schizophrenia, which has five dosage strengths: 5 mg, 10 mg, 15 mg, 20 mg and 30 mg, since its approval, in the United States ,a 1.8 million Abilify prescriptions have opened. aripiprazole approved by The EU has four sizes: 5 mg, 10 mg, 15mg and 30 mg. Aripiprazole as an kind of antipsychotic drugs, in rare cases it may be associated with life-threatening neuroleptic malignant syndrome induced (NMS), also be associated with tardive dyskinesia (TD) have some relevance. Studies have shown that atypical antipsychotics may lead to hyperglycemia, although the study did not examine aripiprazole, but the relationship between hyperglycemia and aripiprazole remains uncertain, therefore, patients in treatment should be carried out blood glucose monitoring. Patients before receiving aripiprazole treatment should be inform the doctor the physical condition and current drug situation . Aripiprazole should be used with caution in patients with a history of epilepsy aripiprazole. In short-term clinical studies, the most common adverse reactions of aripiprazole compared with placebo groups are: headache (32%: 25%), anxiety (25%: 24%), insomnia (24%: 19%), nausea (14%: 10%), vomiting (12%: 7%), somnolence (11%: 8%), lightheadedness (11%: 7%), restlessness (10%: 7%) and constipation (10% :8%). A double-blind 26-week clinical study showed that there was higher incidence of tremor in aripiprazole group , it is 9%, only 1% while in the placebo group, slight tremor but tolerable , but also often led to discontinuation.
Metabolize	Metabolic pathway of aripiprazole is mainly through three kinds of biotransformation: dehydrogenation, hydroxylation and N- dealkylation. In vitro studies have shown, CYP3A4 and CYP2D6 are the two enzymes of the metabolism of the product , CYP3A4 and CYP2D6 are responsible for dehydrogenation and hydroxylation, and N- dealkylation is caused by CYP3A4 catalysis. Thus, when there is presence affecting two enzymatic activities and number of drugs, the amount of aripiprazole should be adjusted . In the steady state, pharmacokinetics of the product is proportional to dose. Single oral dose of 14C-labeled product showed that 55% of metabolites excreted through the feces, 25% excreted in urine and 18% of the original drug from the feces, 1% of the original drug excreted in the urine.  The above information is edited by the chemicalbook of Tian Ye.
Toxicity	Long-term toxicity: long-term toxicity study at a dose of 60 mg / kg for 26 weeks and 2-year carcinogenicity study at dose of 40 and 60mg / kg showed that this product caused retinal degeneration in rats. It showed no evidence of retinal degeneration in mice and monkey trials. Its mechanism of action has not been further researched, it is not shown that these findings is associated with human risks .  Carcinogenicity: In female mice, the daily 3 ~ 30mg / kg dose (based on surface area, respectively, is 0.5 to 5 times the MRHD; calculated by AUC, respectively, MRHD plasma concentrations of 0.1 to 0.9 times) leads to increasing incidence of pituitary tumors, breast cancer and skin cancer adenoacanthoma ; in female rats, the daily 10mg / kg dose (based on surface area is 3 times the MRHD; calculated by AUC, is MRHD plasma concentrations 0.1 times) causes increasing incidence of breast fibrous tumor ,daily 60mg / kg dose (based on surface area, is 19 times the MRHD; calculated by AUC, is MRHD plasma concentrations 14 times) causes increasing incidence of adrenocortical cancer and adrenal tumors . Mutagenicity: in vitro bacterial reverse mutation assay, in vitro bacterial DNA recovery test, mouse lymphoma cells in vitro gene mutation test, Chinese hamster lung cells in vitro chromosomal aberration test, in vivo micronucleus test in mice and rats Unscheduled DNA synthesis test mutagenicity of this product. As a result, there is a positive response in the mouse micronucleus test in vivo, however, the positive reaction is considered to be independent to the mechanism of human .
Drug Interactions	1.It should be used with caution in combination with drugs acting on the central nervous system and alcohol.  2. aripiprazole has possibility of enhancing the role of certain antihypertensive drugs.  3. CYP3A4 inducer will result in elevated aripiprazole clearance and lower blood concentration, CYP3A4 inhibitor azole) or CYP2D inhibitors can inhibit aripiprazole elimination, increase plasma concentration.
Adverse reactions	The most common adverse reactions during treatment are headache, anxiety and insomnia. Rare adverse reactions are child blood sugar, even hyperglycemia.
Application	Antipsychotics
Chemical Properties	Colourless Flake Crystalline Solid
Usage	A deuterated version of Aripiprazole, a selective dopamine D2-receptor antagonist with dopamine autoreceptor agonist activity. Please note that users have reported separation of this compound and aripiprazole under normal-phase and reverse-phase
Usage	A selective dopamine D2-receptor antagonist with dopamine autoreceptor agonist activity. Antipsychotic.
Usage	cerebral vasodilator, antimotion
Usage	For the treatment of schizophrenia and related psychotic disorders.

 

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