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Aripiprazole

Outline EU approves aripiprazole for treatment of schizophrenia Metabolize Toxicity Drug Interactions Adverse reactions Uses
Aripiprazole
Aripiprazole structure
CAS No.
129722-12-9
Chemical Name:
Aripiprazole
Synonyms
OPC 31;ABILIFY;ABILITAT;OPC 14597;Abilify-d8;OPC 31-d8-;Abilitat-d8;Arpiprazole;Aripirazole;Alipiprazole
CBNumber:
CB8210870
Molecular Formula:
C23H27Cl2N3O2
Formula Weight:
448.39
MOL File:
129722-12-9.mol

Aripiprazole Properties

Melting point:
139°C
storage temp. 
-20°C Freezer
solubility 
DMSO: soluble5mg/mL, clear (warmed)
form 
powder
color 
white to beige
Merck 
14,785
CAS DataBase Reference
129722-12-9(CAS DataBase Reference)
SAFETY
  • Risk and Safety Statements
  • Hazard and Precautionary Statements (GHS)
Hazard Codes  F,Xn
Risk Statements  11-20/21/22-36
Safety Statements  16-36/37
RIDADR  UN 1993C 3 / PGIII
WGK Germany  3
RTECS  VC8275950
HS Code  29349990
Hazardous Substances Data 129722-12-9(Hazardous Substances Data)
Symbol(GHS):
Signal word: Danger
Hazard statements:
Code Hazard statements Hazard class Category Signal word Pictogram P-Codes
H302 Harmful if swallowed Acute toxicity,oral Category 4 Warning P264, P270, P301+P312, P330, P501
H370 Causes damage to organs Specific target organ toxicity, single exposure Category 1 Danger P260, P264, P270, P307+P311, P321,P405, P501
H413 May cause long lasting harmful effects to aquatic life Hazardous to the aquatic environment, long-term hazard Category 4
Precautionary statements:
P261 Avoid breathing dust/fume/gas/mist/vapours/spray.
P264 Wash hands thoroughly after handling.
P264 Wash skin thouroughly after handling.
P270 Do not eat, drink or smoke when using this product.
P280 Wear protective gloves/protective clothing/eye protection/face protection.
P403+P233 Store in a well-ventilated place. Keep container tightly closed.
P501 Dispose of contents/container to..…

Aripiprazole price More Price(11)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich PHR1784 Aripiprazole solution 129722-12-9 500mg $169 2018-11-20 Buy
Sigma-Aldrich 1042634 Aripiprazole United States Pharmacopeia (USP) Reference Standard 129722-12-9 200mg $352.8 2018-11-13 Buy
TCI Chemical A2496 Aripiprazole >98.0%(HPLC)(T) 129722-12-9 1g $56 2018-11-22 Buy
TCI Chemical A2496 Aripiprazole >98.0%(HPLC)(T) 129722-12-9 5g $168 2018-11-22 Buy
Cayman Chemical 19989 Aripiprazole ≥98% 129722-12-9 5mg $20 2018-11-19 Buy

Aripiprazole Chemical Properties,Uses,Production

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.

Uses

Antipsychotics

Description

Aripiprazole was launched for the treatment of psychoses including schizophrenia and offers a novel mechanism of action as a partial D2 receptor agonist. Aripiprazole can be synthesized in three steps beginning by the condensation of 7-hydroxy-1,2,3,4- tetrahydroquinolin-2-one with 1 ,Cdibromobutane followed by reaction with 1-(2,3- dichlorophenyl)piperazine. Aripiprazole is a significant D2 agonist/antagonist, 5-HT2 antagonist and 5-HT agonist combined with minimal affinity for a,-adrenergic, H1 and M1 receptors. It has a low D4:D2 selectivity ratio and a D2:5-HT2 affinity ratio that exceeds 15; resulting in different pharmacological characteristics compared to other atypical antipsychotics agents such as clozapine. In animal models, aripiprazole inhibits apomorphine-induced stereotypy without causing catalepsy and ptosis. Moreover, in contrast to classical antipsychotics that produce disabling movement disorders, aripiprazole does not cause an upregulation of D2 receptors or an increase in immediate early gene expression of e.g. the c-fos mRNA in the striatum. In patients with acute relapse of schizophrenia, treatment with aripiprazole provided significant improvement in both positive and negative syndrome scale (PANSS) total score in both short- and longterm evaluations. These results were comparable to those observed with haloperidol or risperidone; however, the early response rate was greater with aripiprazole. Aripiprazole was well tolerated with mild to moderate adverse events such as nausea, dizziness, somnolence and weight gain. The rates of extrapyramidal symptoms were lower than with haloperidol, prolactin levels increase has been uncommon and no significant Q-Tc interval prolongation was observed compared with placebo. Finally, studies suggested a minimal impact of aripiprazole administration on total cholesterol levels and on fasting blood sugar in contrast to other antipsychotics. Aripiprazole has a bioavailability of 87%, a tmax of 3-5 h and a half-life time of 48-68 h. Aripiprazole has been found to have linear kinetics and is mainly metabolized via the cytochrome systems CYP2D6 and CYP3A4. It has little effect on the blood levels of other medications; interaction with both lithium and divalproex sodium found minimal impact. Aripiprazole has also been studied in other psychiatric disorders, including bipolar disorders and has shown great efficacy.

Chemical Properties

Colourless Flake Crystalline Solid

Originator

Otsuka (Japan)

Uses

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

Uses

A selective dopamine D2-receptor antagonist with dopamine autoreceptor agonist activity. Antipsychotic.

Uses

cerebral vasodilator, antimotion

Uses

For the treatment of schizophrenia and related psychotic disorders.

brand name

Abilify (Otsuka).

General Description

Aripiprazole (Abilify). The newest, longactingaripiprazole (an arylpiperazine quinolinone derivative),appears to be partial agonist of D2 receptors (i.e., itstimulates certain D2 receptors while blocking others dependingon their locations in the brain and the concentrationof drug). Bioavailability of aripiprazole is around 87%, with peak plasma concentration attained at 3 to 5 hours afterdosing. It is metabolized by dehydrogenation, oxidative hydroxylation, and N-dealkylation, largelymediated by hepatic CYPs 3A4 and 2D6.
The diphenylbutylpiperidine class can be considered amodification of the fluorobutyrophenone class. Because oftheir high lipophilicity, the compounds are inherently longacting. Pimozide has been approved for antipsychotic use,and penfluridol has undergone clinical trials in the UnitedStates. Overall, side effects for the two compounds resemblethose produced by the fluorobutyrophenones.

General Description

Aripiprazole, (7-[4-[4-(2,3-dichlorophenyl)-1-piperazinyl]butoxy]-3,4-dihydro-2(1H)-quinolone,is an atypical antipsychotic that is available in tablets(Abilify), orally disintegrating tablets (Abilify Discmelt), anda 1-mg/mL oral solution. Unlike the other atypical antipsychotics,aripiprazole exhibits partial agonist activity at D2, D3,D4, and 5-HT1A receptors, and antagonist action at 5-HT2A receptors.Although aripiprazole exhibits a low incidence ofEPS, the compound occupies about 95% of striatal D2 receptorsat therapeutic doses. Additionally, aripiprazole does nothave a fast rate of dissociation from D2 receptors. Althoughthe mechanism of action of this compound remains to be elucidated,the atypical profile for aripiprazole may be related toits action at other monoamine receptors.The compoundis well absorbed with peak plasma levels occurring 3 to 5hours after oral administration. Food does not affect absorptionof aripiprazole. Aripiprazole is extensively metabolizedin the liver by the action of CYP2D6 and CYP3A4. The primarymetabolite in humans is dehydroaripiprazole. This metabolite represents about 40% of aripiprazoleat steady state.In the presence of CYP3A4 and CYP2D6 inhibitorsor inducers, dosage adjustments of aripiprazole maybe required. The mean elimination half-lives in extensive andpoor metabolizers are 75 hours and 146 hours, respectively.The major adverse effects of aripiprazole are headache, anxiety,and insomnia.Similar to other atypical antipsychotics,aripiprazole shows an increased risk in mortality in elderlypatients with dementia-related psychosis.Aripiprazoledemonstrates a different pharmacological profile from allother atypical antipsychotics.

Hazard

A poison.

Aripiprazole Preparation Products And Raw materials

Raw materials

Preparation Products


Aripiprazole Suppliers

Global( 367)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Capot Chemical Co.,Ltd.
+86 (0)571-855 867 18
+86 (0)571-858 647 95 sales@capotchem.com China 19947 60
Shenzhen Sendi Biotechnology Co.Ltd.
0755-23311925 18102838259
0755-23311925 Abel@chembj.com CHINA 3211 55
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 22084 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20763 55
Mainchem Co., Ltd.
+86-0592-6210733
+86-0592-6210733 sales@mainchem.com CHINA 32607 55
Nanjing ChemLin Chemical Industry Co., Ltd.
025-83697070;product@chemlin.com.cn
product@chemlin.com.cn CHINA 3015 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 1737 55
Chongqing Chemdad Co.,Ltd
+86-19923101450
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Xiamen AmoyChem Co., Ltd
+86 (0)592-605 1114
sales@amoychem.com CHINA 6402 58
Jinan Shengqi pharmaceutical Co,Ltd
86+15552594168
christine@shengqipharm.com CHINA 468 58

View Lastest Price from Aripiprazole manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2019-04-02 Aripiprazole Manufacturer; In stock GMP Factory
129722-12-9
US $1.00 / KG 1KG High quality manufacturer TOP 3 largest production factory in China Chemwill Asia Co.,Ltd.
2018-12-24 Aripiprazole
129722-12-9
US $2.00 / kg 1kg 99% 100kg career henan chemical co

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