Tìm theo
Olanzapine
Các tên gọi khác (6 ) :
  • 2-methyl-4-(4-methyl-1-piperazinyl)-10H-thieno[2,3-b][1,5]benzodiazepine
  • Olanzapin
  • Olanzapina
  • Olanzapine
  • Olanzapinum
  • Zyprexa
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 132539-06-1
ATC: N05AH03
ĐG : Advanced Pharmaceutical Services Inc.
CTHH: C17H20N4S
PTK: 312.432
Olanzapine is an atypical antipsychotic, approved by the FDA in 1996. Olanzapine is manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper ends in 2011.
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H20N4S
Phân tử khối
312.432
Monoisotopic mass
312.14086735
InChI
InChI=1S/C17H20N4S/c1-12-11-13-16(21-9-7-20(2)8-10-21)18-14-5-3-4-6-15(14)19-17(13)22-12/h3-6,11,19H,7-10H2,1-2H3
InChI Key
InChIKey=KVWDHTXUZHCGIO-UHFFFAOYSA-N
IUPAC Name
5-methyl-8-(4-methylpiperazin-1-yl)-4-thia-2,9-diazatricyclo[8.4.0.0^{3,7}]tetradeca-1(14),3(7),5,8,10,12-hexaene
Traditional IUPAC Name
zyprexa
SMILES
CN1CCN(CC1)C1=NC2=CC=CC=C2NC2=C1C=C(C)S2
Độ tan chảy
195 °C
Độ hòa tan
9.42e-02 g/l
logP
2
logS
-3.5
pKa (strongest acidic)
14.17
pKa (Strongest Basic)
7.24
PSA
30.87 Å2
Refractivity
93.87 m3·mol-1
Polarizability
35.37 Å3
Rotatable Bond Count
0
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
Dược Lực Học : Olanzapine, an atypical antipsychotic agent, is used to treat both negative and positive symptoms of schizophrenia, acute mania with bipolar disorder, agitation, and psychotic symptoms in dementia. Future uses may include the treatment of obsessive-compulsive disorder and severe behavioral disorders in autism. Structurally and pharmacologically similar to clozapine, olanzapine binds to alpha(1), dopamine, histamine H1, muscarinic, and serotonin type 2 (5-HT2) receptors.
Cơ Chế Tác Dụng : Olanzapine is an atypical antipsychotic, approved by the FDA in 1996. Olanzapine is manufactured and marketed by the pharmaceutical company Eli Lilly and Company, whose patent for olanzapine proper ends in 2011. Olanzapine'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 :
▧ Absorption :
Well absorbed, with approximately 40% of the dose metabolized before reaching the systemic circulation.
▧ Volume of Distribution :
* 1000 L
▧ Protein binding :
93%
▧ Metabolism :
Hepatic
▧ Route of Elimination :
It is eliminated extensively by first pass metabolism, with approximately 40% of the dose metabolized before reaching the systemic circulation. Following a single oral dose of 14C labeled olanzapine, 7% of the dose of olanzapine was recovered in the urine as unchanged drug, indicating that olanzapine is highly metabolized.
▧ Half Life :
21 to 54 hours
▧ Clearance :
* 12 to 47 L/h
Độc Tính : Symptoms of an overdose include tachycardia, agitation, dysarthria, decreased consciousness and coma. Death has been reported after an acute overdose of 0.45g, but also survival after an acute overdose of 1500g.
Chỉ Định : For the acute and maintenance treatment of schizophrenia and related psychotic disorders, as well as acute treatment of manic or mixed episodes of bipolar 1 disorder. Intramuscular olanzapine is indicated for the rapid control of agitated patients.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Fluvoxamine Fluvoxamine increases the effect and toxicity of olanzapine
  • Galantamine Possible antagonism of action
  • Ritonavir Ritonavir decreases the effect of olanzapine
  • Rivastigmine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Olanzapine, may be reduced due to antagonism. This interaction may be beneficial when the anticholinergic action is a side effect. AChEIs may also augment the central neurotoxic effect of antipsychotics. Monitor for extrapyramidal symptoms and decreased efficacy of both agents.
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Trimethobenzamide Trimethobenzamide and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Additive CNS depressant effects may also occur. Monitor for enhanced anticholinergic and CNS depressant effects.
  • Trospium Trospium and Olanzapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Powder, for solution - Intramuscular
Tablet - Oral
Tablet, orally disintegrating - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : G.L. Pharma
    Sản phẩm biệt dược : Aedon
  • Công ty : Sanitas
    Sản phẩm biệt dược : Amulsin
  • Công ty : LKM
    Sản phẩm biệt dược : Apisco
  • Công ty : LKM
    Sản phẩm biệt dược : Apsico
  • Công ty : Mylan
    Sản phẩm biệt dược : Arkolamyl
  • Công ty : Lavipharm
    Sản phẩm biệt dược : Caprilon
  • Công ty : Cobalt
    Sản phẩm biệt dược : CO Olanzapine
  • Công ty : Square
    Sản phẩm biệt dược : Deprex
  • Công ty : Stein
    Sản phẩm biệt dược : Dominazol
  • Công ty : Daksh
    Sản phẩm biệt dược : Dopin
  • Công ty : EGIS
    Sản phẩm biệt dược : Egolanza
  • Công ty : Elynza
    Sản phẩm biệt dược : Elynza
  • Công ty : Biogen
    Sản phẩm biệt dược : Frenial
  • Công ty : Lupin
    Sản phẩm biệt dược : Jolyon-MD
  • Công ty : Quisisana
    Sản phẩm biệt dược : Kozylex
  • Công ty : Molekule
    Sản phẩm biệt dược : Lanopin
  • Công ty : Biogened
    Sản phẩm biệt dược : Lanzapin
  • Công ty : Renata
    Sản phẩm biệt dược : Lanzep
  • Công ty : Smart Intermed
    Sản phẩm biệt dược : Lapenza
  • Công ty : Medochemie
    Sản phẩm biệt dược : Lapozan
  • Công ty : Portfarma
    Sản phẩm biệt dược : Lazapix
  • Công ty : Lilly
    Sản phẩm biệt dược : Zyprexa
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00334
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07322
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00454
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=35254
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0002-4112-30
PharmGKB
http://www.pharmgkb.org/drug/PA450688
Wikipedia
http://en.wikipedia.org/wiki/Olanzapine
RxList
http://www.rxlist.com/cgi/generic3/symbyax.htm
Drugs.com
http://www.drugs.com/cdi/olanzapine.html
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