Tìm theo
Mirtazapine
Các tên gọi khác (7 ) :
  • 1,2,3,4,10,14b-Hexahydro-2-methylpyrazino(2,1-a)pyrido(2,3-c)benzazepine
  • 6-Azamianserin
  • Mepirzapine
  • Mirtazapin
  • Mirtazapina
  • Mirtazapine
  • Mirtazapinum
Thuốc điều trị về tâm thần
Thuốc Gốc
Small Molecule
CAS: 61337-67-5
ATC: N06AX11
ĐG : Alphapharm Party Ltd. , http://www.alphapharm.com.au
CTHH: C17H19N3
PTK: 265.3529
Mirtazapine is an antidepressant introduced by Organon International in 1996 used for the treatment of moderate to severe depression. Mirtazapine has a tetracyclic chemical structure and is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). It is the only tetracyclic antidepressant that has been approved by the Food and Drug Administration to treat depression. [Wikipedia]
Nhận Dạng Quốc Tế & Đặc Tính Hóa Học
Công thức hóa học
C17H19N3
Phân tử khối
265.3529
Monoisotopic mass
265.157897623
InChI
InChI=1S/C17H19N3/c1-19-9-10-20-16(12-19)15-7-3-2-5-13(15)11-14-6-4-8-18-17(14)20/h2-8,16H,9-12H2,1H3
InChI Key
InChIKey=RONZAEMNMFQXRA-UHFFFAOYSA-N
IUPAC Name
5-methyl-2,5,19-triazatetracyclo[13.4.0.0^{2,7}.0^{8,13}]nonadeca-1(19),8(13),9,11,15,17-hexaene
Traditional IUPAC Name
5-methyl-2,5,19-triazatetracyclo[13.4.0.0^{2,7}.0^{8,13}]nonadeca-1(19),8(13),9,11,15,17-hexaene
SMILES
CN1CCN2C(C1)C1=CC=CC=C1CC1=C2N=CC=C1
Độ tan chảy
114-116 °C
Độ hòa tan
Slight
logP
2.9
logS
-2.4
pKa (Strongest Basic)
6.67
PSA
19.37 Å2
Refractivity
82.66 m3·mol-1
Polarizability
30.35 Å3
Rotatable Bond Count
0
H Bond Acceptor Count
3
H Bond Donor Count
0
Physiological Charge
0
Number of Rings
4
Bioavailability
1
Rule of Five
true
Ghose Filter
true
Dược Lực Học : Mirtazapine, an antidepressant of the piperazinoazepine class, is a tetracyclic compound with an anxiolytic effect. Mirtazapine has fewer ADRs than tricyclic antidepressants and is better tolerated. Selective blockade of specific serotonin receptors by mirtazapine likey minimizes side effects typical of other antidepressants.
Cơ Chế Tác Dụng : Mirtazapine is an antidepressant introduced by Organon International in 1996 used for the treatment of moderate to severe depression. Mirtazapine has a tetracyclic chemical structure and is classified as a noradrenergic and specific serotonergic antidepressant (NaSSA). It is the only tetracyclic antidepressant that has been approved by the Food and Drug Administration to treat depression. [Wikipedia] Mirtazapine acts as an antagonist at central pre-synaptic alpha(2)-receptors, inhibiting negative feedback to the presynaptic nerve and causing an increase in NE release. Blockade of heteroreceptors, alpha(2)-receptors contained in serotenergic neurons, enhances the release of 5-HT, increasing the interactions between 5-HT and 5-HT1 receptors and contributing to the anxiolytic effects of mirtazapine. Mirtazapine also acts as a weak antagonist at 5-HT1 receptors and as a potent antagonist at 5-HT2 (particularly subtypes 2A and 2C) and 5-HT3 receptors. Blockade of these receptors may explain the lower incidence of adverse effects such as anxiety, insomnia, and nausea. Mirtazapine also exhibits significant antagonism at H1-receptors, resulting in sedation. Mirtazapine has no effects on the reuptake of either NE or 5-HT and has only minimal activity at dopaminergic and muscarinic receptors.
Dược Động Học :
▧ Absorption :
Rapid and complete, but, due to first-pass metabolism, absolute bioavailability is 50%.
▧ Protein binding :
85%
▧ Metabolism :
Mirtazapine is extensively metabolized by demethylation and hydroxylation followed by glucuronide conjugation. Cytochrome P450 2D6 and cytochrome P450 1A2 are involved in formation of the 8-hydroxy metabolite of mirtazapine, and cytochrome P450 3A4 is responsible for the formation of the N-desmethyl and N-oxide metabolites. Several metabolites possess pharmacological activity, but plasma levels are very low.
▧ Route of Elimination :
This drug is known to be substantially excreted by the kidney (75%).
▧ Half Life :
20-40 hours
Độc Tính : Symptoms of overdose include disorientation, drowsiness, impaired memory, and tachycardia. LD50 is 600-720mg/kg (oral, mice) and 320-490mg/kg (oral, rat) [PMID: 10333982]
Chỉ Định : For the treatment of major depressive disorder.
Tương Tác Thuốc :
  • Clonidine Possible hypertensive crisis
  • Desvenlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Donepezil Possible antagonism of action
  • Ethotoin The hydantoins may reduce mirtazapine plasma concentrations and pharmacological effects
  • Fluvoxamine Fluvoxamine may increase the therapeutic and adverse effects of mirtazapine.
  • Fosphenytoin The hydantoins may reduce mirtazapine plasma concentrations and pharmacological effects
  • Galantamine Possible antagonism of action
  • Isocarboxazid Possible severe adverse reaction with this combination
  • Mephenytoin The hydantoins may reduce mirtazapine plasma concentrations and pharmacological effects
  • Phenelzine Possible severe adverse reaction with this combination
  • Phenytoin The hydantoins may reduce mirtazapine plasma concentrations and pharmacological effects
  • Rasagiline Possible severe adverse reaction with this combination
  • Rivastigmine Possible antagonism of action
  • Telithromycin Telithromycin may reduce clearance of Mirtazapine. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Mirtazapine if Telithromycin is initiated, discontinued or dose changed.
  • Terbinafine Terbinafine may reduce the metabolism and clearance of Mirtazapine. Consider alternate therapy or monitor for therapeutic/adverse effects of Mirtazapine if Terbinafine is initiated, discontinued or dose changed.
  • Tramadol Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Tranylcypromine The MAO inhibitor, Tranylcypromine, may increase the central neurotoxic effects of the Mirtazapine. These agents should not be administered within 14 days of each other.
  • Trazodone Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Trimipramine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Triprolidine The CNS depressants, Triprolidine and Mirtazapine, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.
  • Venlafaxine Increased risk of serotonin syndrome. Monitor for symptoms of serotonin syndrome.
  • Voriconazole Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of mirtazapine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of mirtazapine if voriconazole is initiated, discontinued or dose changed.
  • Zolmitriptan Use of two serotonin modulators, such as zolmitriptan and mirtazapine, increases the risk of serotonin syndrome. Consider alternate therapy or monitor for serotonin syndrome during concomitant therapy.
Liều Lượng & Cách Dùng : Tablet - Oral
Tablet, orally disintegrating - Oral
Dữ Kiện Thương Mại
Giá thị trường
Nhà Sản Xuất
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Avanza
  • Công ty : Alphapharm
    Sản phẩm biệt dược : Axit
  • Công ty : ratiopharm
    Sản phẩm biệt dược : Mirtabene
  • Công ty : Pinewood
    Sản phẩm biệt dược : Mirtaz
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Mirtazon
  • Công ty : MSD France
    Sản phẩm biệt dược : Norset
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Promyrtil
  • Sản phẩm biệt dược : Remergil
  • Công ty : Organon
    Sản phẩm biệt dược : Remergon
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Remeron
  • Công ty :
    Sản phẩm biệt dược : Remeron SolTab
  • Công ty : Schering-Plough
    Sản phẩm biệt dược : Rexer
  • Công ty : Organon
    Sản phẩm biệt dược : Zispin
Đóng gói
Tài Liệu Tham Khảo Thêm
drugbank
http://www.drugbank.ca/drugs/DB00370
PubChem Compound
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=4205
PubChem Substance
http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?sid=46506965
KEGG Compound
http://www.genome.jp/dbget-bin/www_bget?cpd:C07570
KEGG Drug
http://www.genome.jp/dbget-bin/www_bget?drug:D00563
ChemSpider
http://www.chemspider.com/Chemical-Structure.4060.html
National Drug Code Directory
http://www.hipaaspace.com/Medical_Billing/Coding/National.Drug.Codes/PDF/0185-0020-30
PharmGKB
http://www.pharmgkb.org/drug/PA450522
Wikipedia
http://en.wikipedia.org/wiki/Mirtazapine
RxList
http://www.rxlist.com/cgi/generic/mirtaz.htm
PDRhealth
http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/rem1371.shtml
Drugs.com
http://www.drugs.com/cdi/mirtazapine.html
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