Tìm theo
Loxapine
Các tên gọi khác (6 ) :
  • 2-Chloro-11-(4-methyl-1-piperazinyl)dibenz[b,f][1,4]oxazepine
  • Cloxazepine
  • Loxapina
  • Loxapine
  • Loxapinum
  • oxilapine
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 1977-10-2
ATC: N05AH01
ĐG : Actavis Group , http://www.actavis.com
CTHH: C18H18ClN3O
PTK: 327.808
An antipsychotic agent used in schizophrenia. [PubChem]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C18H18ClN3O
Phân tử khối
327.808
Monoisotopic mass
327.11383992
InChI
InChI=1S/C18H18ClN3O/c1-21-8-10-22(11-9-21)18-14-12-13(19)6-7-16(14)23-17-5-3-2-4-15(17)20-18/h2-7,12H,8-11H2,1H3
InChI Key
InChIKey=XJGVXQDUIWGIRW-UHFFFAOYSA-N
IUPAC Name
13-chloro-10-(4-methylpiperazin-1-yl)-2-oxa-9-azatricyclo[9.4.0.0^{3,8}]pentadeca-1(11),3(8),4,6,9,12,14-heptaene
Traditional IUPAC Name
loxapine
SMILES
CN1CCN(CC1)C1=NC2=CC=CC=C2OC2=C1C=C(Cl)C=C2
Độ tan chảy
109-111 °C
Độ hòa tan
1.03e-01 g/l
logP
3.6
logS
-3.5
pKa (Strongest Basic)
7.18
PSA
28.07 Å2
Refractivity
95.11 m3·mol-1
Polarizability
34.99 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
1
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Loxapine, a dibenzoxazepine compound, represents a subclass of tricyclic antipsychotic agents, chemically distinct from the thioxanthenes, butyrophenones, and phenothiazines. Pharmacologically, Loxapine is a tranquilizer for which the exact mode of action has not been established, however, it is believed that by antagonising dopamine and serotonin receptors, there is a marked cortical inhibition which can manifest as tranquilization and suppression of aggression.
Cơ Chế Tác Dụng : An antipsychotic agent used in schizophrenia. [PubChem] Loxapine is a dopamine antagonist, and also a serotonin 5-HT2 blocker. The exact mode of action of Loxapine has not been established, however changes in the level of excitability of subcortical inhibitory areas have been observed in several animal species in association with such manifestations of tranquilization as calming effects and suppression of aggressive behavior.
Dược Động Học :
▧ Absorption :
Systemic bioavailability of the parent drug was only about one third that after an equivalent intramuscular dose (25 mg base) in male volunteers
▧ Metabolism :
Hepatic
▧ Route of Elimination :
Metabolites are excreted in the urine in the form of conjugates and in the feces unconjugated.
▧ Half Life :
Oral-4 hours
Độc Tính : LD50=65 mg/kg (Orally in mice)
Chỉ Định : For the management of the manifestations of psychotic disorders such as schizophrenia
Tương Tác Thuốc :
  • Artemether Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Lumefantrine Additive QTc-prolongation may occur. Concomitant therapy should be avoided.
  • Rivastigmine Possible antagonism of action
  • Rotigotine Pharmacodynamic antagonism may decrease the effects of rotigotine. Consider alternate therapy.
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Loxapine, 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.
  • Tacrolimus Additive QTc-prolongation may occur increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Tetrabenazine May cause dopamine deficiency. Monitor for Tetrabenazine adverse effects.
  • Thiothixene May cause additive QTc-prolonging effects. Increased risk of ventricular arrhythmias. Consider alternate therapy. Thorough risk:benefit assessment is required prior to co-administration.
  • Toremifene Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Consider alternate therapy. A thorough risk:benefit assessment is required prior to co-administration.
  • Trimethobenzamide Trimethobenzamide and Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Trimipramine Additive QTc-prolongation may occur, increasing the risk of serious ventricular arrhythmias. Concomitant therapy should be used with caution.
  • Triprolidine Triprolidine and Loxapine, 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 Loxapine, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Voriconazole Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Vorinostat Additive QTc prolongation may occur. Consider alternate therapy or monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
  • Ziprasidone Additive QTc-prolonging effects may increase the risk of severe arrhythmias. Concomitant therapy is contraindicated.
  • Zuclopenthixol Additive QTc prolongation may occur. Consider alternate therapy or use caution and monitor for QTc prolongation as this can lead to Torsade de Pointes (TdP).
Liều Lượng & Cách Dùng : Liquid - Intramuscular
Solution - Oral
Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Adasuve
  • Công ty :
    Sản phẩm biệt dược : Cloxazepine
  • Công ty : Newai Chem
    Sản phẩm biệt dược : Lopac
  • Công ty : Patron
    Sản phẩm biệt dược : Losagen
  • Công ty : Wyeth
    Sản phẩm biệt dược : Loxapac
  • Công ty : Hisun
    Sản phẩm biệt dược : Loxapine
  • Công ty :
    Sản phẩm biệt dược : Loxitane
  • Công ty : Swiss Pharm
    Sản phẩm biệt dược : Rosup
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00408
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=3964
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46505047
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07104
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D02340
ChemSpider
http://www.chemspider.com/Chemical-Structure.3827.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=22871
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0378-7005-01
PharmGKB
http://www.pharmgkb.org/drug/PA450273
Wikipedia
http://en.wikipedia.org/wiki/Loxapine
RxList
http://www.rxlist.com/cgi/generic2/loxapineoc.htm
Drugs.com
http://www.drugs.com/cdi/loxapine.html
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