Tìm theo
Aripiprazole
Các tên gọi khác (6 ) :
  • Abilify
  • Abilitat
  • Aripiprazol
  • Aripiprazole
  • Aripiprazolum
  • OPC 31
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 129722-12-9
ATC: N05AX12
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C23H27Cl2N3O2
PTK: 448.385
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.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C23H27Cl2N3O2
Phân tử khối
448.385
Monoisotopic mass
447.148032537
InChI
InChI=1S/C23H27Cl2N3O2/c24-19-4-3-5-21(23(19)25)28-13-11-27(12-14-28)10-1-2-15-30-18-8-6-17-7-9-22(29)26-20(17)16-18/h3-6,8,16H,1-2,7,9-15H2,(H,26,29)
InChI Key
InChIKey=CEUORZQYGODEFX-UHFFFAOYSA-N
IUPAC Name
7-{4-[4-(2,3-dichlorophenyl)piperazin-1-yl]butoxy}-1,2,3,4-tetrahydroquinolin-2-one
Traditional IUPAC Name
aripiprazole
SMILES
ClC1=CC=CC(N2CCN(CCCCOC3=CC4=C(CCC(=O)N4)C=C3)CC2)=C1Cl
Độ hòa tan
7.77e-03 g/l
logP
4.5
logS
-4.8
pKa (strongest acidic)
13.51
pKa (Strongest Basic)
7.46
PSA
44.81 Å2
Refractivity
124.34 m3·mol-1
Polarizability
49.23 Å3
Rotatable Bond Count
7
H Bond Acceptor Count
4
H Bond Donor Count
1
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
MDDR-Like Rule
true
Dược Lực Học : 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.
Cơ Chế Tác Dụng : 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. 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.
Dược Động Học :

▧ Volume of Distribution :
* 4.9 L/kg
▧ 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
Chỉ Định : For the treatment of schizophrenia and related psychotic disorders.
Tương Tác Thuốc :
  • 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.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Abilify
  • Công ty :
    Sản phẩm biệt dược : Abilitat
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01238
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=60795
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505745
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C12564
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D01164
ChemSpider
http://www.chemspider.com/Chemical-Structure.54790.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/59148-013-15
PharmGKB
http://www.pharmgkb.org/drug/PA10026
Wikipedia
http://en.wikipedia.org/wiki/Aripiprazole
RxList
http://www.rxlist.com/cgi/generic/abilify.htm
Drugs.com
http://www.drugs.com/cdi/aripiprazole.html
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