Tìm theo
Molindone
Các tên gọi khác (8 ) :
  • (+-)-molindone
  • Moban
  • Molindona
  • Molindone
  • Molindonum
  • SID26755691
  • SID50111112
  • SID90341242
Thuốc chống rối loạn tâm thần
Thuốc Gốc
Small Molecule
CAS: 7416-34-4
ATC: N05AE02
ĐG : Bristol-Myers Squibb Co. , http://www.bms.com
CTHH: C16H24N2O2
PTK: 276.374
An indole derivative effective in schizophrenia and other psychoses and possibly useful in the treatment of the aggressive type of undersocialized conduct disorder. Molindone has much lower affinity for D2 receptors than most antipsychotic agents and has a relatively low affinity for D1 receptors. It has only low to moderate affinity for cholinergic and alpha-adrenergic receptors. Some electrophysiologic data from animals indicate that molindone has certain characteristics that resemble those of clozapine. (From AMA Drug Evaluations Annual, 1994, p283)
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C16H24N2O2
Phân tử khối
276.374
Monoisotopic mass
276.183778022
InChI
InChI=1S/C16H24N2O2/c1-3-13-11(2)17-14-5-4-12(16(19)15(13)14)10-18-6-8-20-9-7-18/h12,17H,3-10H2,1-2H3
InChI Key
InChIKey=KLPWJLBORRMFGK-UHFFFAOYSA-N
IUPAC Name
3-ethyl-2-methyl-5-(morpholin-4-ylmethyl)-4,5,6,7-tetrahydro-1H-indol-4-one
Traditional IUPAC Name
molindone
SMILES
CCC1=C(C)NC2=C1C(=O)C(CN1CCOCC1)CC2
Độ tan chảy
180.5 °C
Độ hòa tan
4.74e-01 g/l
logP
2.04
logS
-2.8
pKa (strongest acidic)
15.34
pKa (Strongest Basic)
6.65
PSA
45.33 Å2
Refractivity
81.06 m3·mol-1
Polarizability
32 Å3
Rotatable Bond Count
3
H Bond Acceptor Count
3
H Bond Donor Count
1
Physiological Charge
0
Number of Rings
3
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Molindone is a dihydroindolone compound which is not structurally related to the phenothiazines, the butyrophenones, or the thioxanthenes. Molindone has a pharmacological profile in laboratory animals which predominantly resembles that of major tranquilizers causing reduction of spontaneous locomotion and aggressiveness, suppression of a conditioned response and antagonism of the bizarre stereotyped behavior and hyperactivity induced by amphetamines. In addition, molindone antagonizes the depression caused by the tranquilizing agent tetrabenazine.
Cơ Chế Tác Dụng : An indole derivative effective in schizophrenia and other psychoses and possibly useful in the treatment of the aggressive type of undersocialized conduct disorder. Molindone has much lower affinity for D2 receptors than most antipsychotic agents and has a relatively low affinity for D1 receptors. It has only low to moderate affinity for cholinergic and alpha-adrenergic receptors. Some electrophysiologic data from animals indicate that molindone has certain characteristics that resemble those of clozapine. (From AMA Drug Evaluations Annual, 1994, p283) The exact mechanism has not been established, however, based on electroencephalogram (EEG) studies, molindone is thought to act by occupying (antagonizing) dopamine (D2) receptor sites in the reticular limbic systems in the brain, thus decreasing dopamine activity. Decreased dopamine activity results in decreased physiological effects normally induced by excessive dopamine stimulation, such as those typically seen in manifestations of psychotic disorders.
Dược Động Học :
▧ Absorption :
Rapidly absorbed from the gastrointestinal tract following oral administration.
▧ Metabolism :
Most likely hepatic. 36 metabolites have been recognized, some of which may be active.
▧ Route of Elimination :
Human metabolic studies show molindone to be rapidly absorbed and metabolized when given orally. There are 36 recognized metabolites with less than 2-3% unmetabolized molindone being excreted in urine and feces.
Chỉ Định : Molindone is used for the management of the manifestations of psychotic disorders.
Tương Tác Thuốc :
  • Donepezil Possible antagonism of action
  • Galantamine Possible antagonism of action
  • Tacrine The therapeutic effects of the central acetylcholinesterase inhibitor (AChEI), Tacrine, and/or the anticholinergic/antipsychotic, Molindone, 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 Molindone, two anticholinergics, may cause additive anticholinergic effects and enhance their adverse/toxic effects. Monitor for enhanced anticholinergic effects.
  • Triprolidine Triprolidine and Molindone, 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 Molindone, two anticholinergics, may cause additive anticholinergic effects and enhanced adverse/toxic effects. Monitor for enhanced anticholinergic effects.
Liều Lượng & Cách Dùng : Tablet - Oral
Dữ Kiện Thương Mại
Giá thị trường
  • Biệt dược thương mại : Moban 5 mg tablet
    Giá bán buôn : USD >1.79
    Đơn vị tính : tablet
  • Biệt dược thương mại : Moban 10 mg tablet
    Giá bán buôn : USD >2.57
    Đơn vị tính : tablet
  • Biệt dược thương mại : Moban 25 mg tablet
    Giá bán buôn : USD >3.02
    Đơn vị tính : tablet
  • Biệt dược thương mại : Moban 50 mg tablet
    Giá bán buôn : USD >5.12
    Đơn vị tính : tablet
Nhà Sản Xuất
  • Công ty :
    Sản phẩm biệt dược : Moban
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB01618
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=23897
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46504744
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07230
ChemSpider
http://www.chemspider.com/Chemical-Structure.22342.html
BindingDB
http://www.bindingdb.org/bind/chemsearch/marvin/MolStructure.jsp?monomerid=50130290
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/63481-072-70
PharmGKB
http://www.pharmgkb.org/drug/PA164746756
Wikipedia
http://en.wikipedia.org/wiki/Molindone
RxList
http://www.rxlist.com/cgi/generic/molindone.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/mob1614.shtml
Drugs.com
http://www.drugs.com/cdi/molindone.html
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