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Identification
Name Mirtazapine
Accession Number DB00370 (APRD00685)
Type small molecule
Groups approved
Description

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]
Structure Thumb
Download: MOL | SDF | SMILES | InChI
Display: 2D Structure | 3D Structure
Synonyms
  • Mepirzepine
  • Mirtazapina [INN-Spanish]
  • mirtazapine
  • Mirtazapine [Usan:Ban:Inn]
  • Mirtazapinum [INN-Latin]
  • Mirtazepine
Brand names
  • Avanza
  • Axit
  • Mirtabene
  • Mirtaz
  • Mirtazon
  • Norset
  • Promyrtil
  • Remergil
  • Remergon
  • Remeron
  • Remeron Soltab
  • Rexer
  • Zispin
Brand name mixtures Not Available
Categories
  • Histamine H1 Antagonists
  • Adrenergic alpha-Antagonists
  • Antidepressive Agents, Tricyclic
CAS number 61337-67-5
Weight Average: 265.3529
Monoisotopic: 265.157897623
Chemical Formula C17H19N3
InChI Key InChIKey=RONZAEMNMFQXRA-UHFFFAOYSA-N
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
Plain Text
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=C(CC3=CC=CN=C23)C=CC=C1
Plain Text
Mass Spec Not Available
Taxonomy
Kingdom Organic
Classes
  • Phenethylamines
Substructures
  • Aliphatic and Aryl Amines
  • Pyridines and Derivatives
  • Piperazines
  • Benzene and Derivatives
  • Aminopyridines and Derivatives
  • Phenethylamines
  • Heterocyclic compounds
  • Aromatic compounds
Pharmacology
Indication For the treatment of major depressive disorder.
Pharmacodynamics 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.
Mechanism of action 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.
Absorption Rapid and complete, but, due to first-pass metabolism, absolute bioavailability is 50%.
Volume of distribution Not Available
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.

Enzyme Metabolite Reaction Km Vmax
Cytochrome P450 2D6 N-desmethylmirtazapine N-demethylation 196 18.46
Cytochrome P450 2D6 8-hydroxymirtazapine 8-hydroxylation 10 20.43
Cytochrome P450 1A2 mirtazapine-N-oxide N-oxidation 136 4.8
Cytochrome P450 1A2 N-desmethylmirtazapine N-demethylation 121 5.32
Cytochrome P450 1A2 8-hydroxymirtazapine 8-hydroxylation 138 5.32
Cytochrome P450 3A4 mirtazapine-N-oxide N-oxidation 226 63.3
Cytochrome P450 3A4 N-desmethylmirtazapine N-demethylation 378 190.074
Cytochrome P450 3A4 8-hydroxymirtazapine 8-hydroxylation 237 3.31
Route of elimination This drug is known to be substantially excreted by the kidney (75%).
Half life 20-40 hours
Clearance Not Available
Toxicity 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]
Affected organisms
  • Humans and other mammals
Pathways Not Available
Pharmacoeconomics
Manufacturers
  • Actavis totowa llc
  • Aurobindo pharma ltd inc
  • Teva pharmaceuticals usa inc
  • Watson laboratories inc
  • Organon usa inc
  • Actavis elizabeth llc
  • Alphapharm party ltd
  • Apotex inc etobicoke site
  • Aurobindo pharma ltd
  • Caraco pharmaceutical laboratories ltd
  • Ivax pharmaceuticals inc sub teva pharmaceuticals usa
  • Mylan pharmaceuticals inc
  • Roxane laboratories inc
  • Sandoz inc
  • Watson laboratories inc florida
Packagers
Dosage forms
Form Route Strength
Tablet Oral
Tablet, orally disintegrating Oral
Prices
Unit description Cost Unit
Remeron SolTab 30 45 mg Dispersible Tablet Box 114.4 USD box
Remeron SolTab 30 15 mg Dispersible Tablet Box 107.58 USD box
Remeron SolTab 30 30 mg Dispersible Tablet Box 107.27 USD box
Mirtazapine 30 45 mg Dispersible Tablet Box 88.95 USD box
Mirtazapine 30 30 mg Dispersible Tablet Box 83.48 USD box
Mirtazapine 30 15 mg Dispersible Tablet Box 81.02 USD box
Remeron 45 mg tablet 4.61 USD tablet
Remeron 15 mg tablet 4.42 USD tablet
Remeron 45 mg soltab 3.57 USD tablet
Remeron 30 mg soltab 3.55 USD tablet
Remeron 30 mg tablet 3.47 USD tablet
Remeron 15 mg soltab 3.26 USD tablet
Mirtazapine 45 mg tablet 2.91 USD tablet
Mirtazapine 30 mg tablet 2.85 USD tablet
Mirtazapine 15 mg tablet 2.77 USD tablet
Mirtazapine 7.5 mg tablet 2.56 USD tablet
Apo-Mirtazapine 30 mg Tablet 0.73 USD tablet
Mylan-Mirtazapine 30 mg Tablet 0.73 USD tablet
Novo-Mirtazapine 30 mg Tablet 0.73 USD tablet
Phl-Mirtazapine 30 mg Tablet 0.73 USD tablet
Pms-Mirtazapine 30 mg Tablet 0.73 USD tablet
Ratio-Mirtazapine 30 mg Tablet 0.73 USD tablet
Sandoz Mirtazapine 30 mg Tablet 0.73 USD tablet
Pms-Mirtazapine 15 mg Tablet 0.39 USD tablet
Patents
Country Patent Number Approved Expires
United States 5178878 1993-01-12 2010-01-12
Canada 2386547 2010-06-08 2020-10-09
Properties
State solid
Melting point 114-116oC
Experimental Properties
Property Value Source
water solubility Slight PhysProp
logP 2.9 PhysProp
Predicted Properties
Property Value Source
water solubility 1.10e+00 g/l ALOGPS
logP 2.90 ALOGPS
logP 3.21 ChemAxon Molconvert
logS -2.38 ALOGPS
pKa ChemAxon Molconvert
hydrogen acceptor count 3 ChemAxon Molconvert
hydrogen donor count 0 ChemAxon Molconvert
polar surface area 19.37 ChemAxon Molconvert
rotatable bond count 0 ChemAxon Molconvert
refractivity 82.66 ChemAxon Molconvert
polarizability 30.35 ChemAxon Molconvert
References
Synthesis Reference Not Available
General Reference
  1. Gillman PK: A systematic review of the serotonergic effects of mirtazapine in humans: implications for its dual action status. Hum Psychopharmacol. 2006 Mar;21(2):117-25. Pubmed
  2. Burrows GD, Kremer CM: Mirtazapine: clinical advantages in the treatment of depression. J Clin Psychopharmacol. 1997 Apr;17 Suppl 1:34S-39S. Pubmed
  3. Velazquez C, Carlson A, Stokes KA, Leikin JB: Relative safety of mirtazapine overdose. Vet Hum Toxicol. 2001 Dec;43(6):342-4. Pubmed
  4. Gorman JM: Mirtazapine: clinical overview. J Clin Psychiatry. 1999;60 Suppl 17:9-13; discussion 46-8. Pubmed
  5. Baldwin DS, Anderson IM, Nutt DJ, Bandelow B, Bond A, Davidson JR, den Boer JA, Fineberg NA, Knapp M, Scott J, Wittchen HU: Evidence-based guidelines for the pharmacological treatment of anxiety disorders: recommendations from the British Association for Psychopharmacology. J Psychopharmacol. 2005 Nov;19(6):567-96. Pubmed
  6. Pubmed
External Links
Resource Link
KEGG Drug D00563 Link_out
KEGG Compound C07570 Link_out
PubChem Compound 4205 Link_out
PubChem Substance 46506965 Link_out
ChemSpider 4060 Link_out
ChEBI 6950 Link_out
ChEMBL 6950 Link_out
Therapeutic Targets Database DAP000010 Link_out
PharmGKB PA450522 Link_out
Drug Product Database 2256126 Link_out
RxList http://www.rxlist.com/cgi/generic/mirtaz.htm Link_out
Drugs.com http://www.drugs.com/cdi/mirtazapine.html Link_out
PDRhealth http://www.pdrhealth.com/drug_info/rxdrugprofiles/drugs/rem1371.shtml Link_out
Wikipedia http://en.wikipedia.org/wiki/Mirtazapine Link_out
ATC Codes
  • N06AX11
AHFS Codes
  • 28:16.04.92
PDB Entries Not Available
FDA label show (904.1 KB)
MSDS show (57.2 KB)
Interactions
Drug Interactions Not Available
Food Interactions
  • Take without regard to meals. Avoid alcohol.
Targets

1. 5-hydroxytryptamine 2A receptor

Pharmacological action: yes
Actions: antagonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system. This receptor is involved in tracheal smooth muscle contraction, bronchoconstriction, and control of aldosterone production

Organism class: human
UniProt ID: P28223 Link_out
Gene: HTR2A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Westenberg HG: Pharmacology of antidepressants: selectivity or multiplicity? J Clin Psychiatry. 1999;60 Suppl 17:4-8; discussion 46-8. Pubmed
  2. Gorman JM: Mirtazapine: clinical overview. J Clin Psychiatry. 1999;60 Suppl 17:9-13; discussion 46-8. Pubmed
  3. Nutt DJ: Care of depressed patients with anxiety symptoms. J Clin Psychiatry. 1999;60 Suppl 17:23-7; discussion 46-8. Pubmed
  4. Laakmann G, Schule C, Baghai T, Waldvogel E: Effects of mirtazapine on growth hormone, prolactin, and cortisol secretion in healthy male subjects. Psychoneuroendocrinology. 1999 Oct;24(7):769-84. Pubmed
  5. Waldinger MD, Berendsen HH, Schweitzer DH: Treatment of hot flushes with mirtazapine: four case reports. Maturitas. 2000 Oct 31;36(3):165-8. Pubmed
  6. Anttila SA, Leinonen EV: A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64. Pubmed

2. 5-hydroxytryptamine 3 receptor

Pharmacological action: yes
Actions: antagonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor is a ligand-gated ion channel, which when activated causes fast, depolarizing responses in neurons. It is a cation-specific, but otherwise relatively nonselective, ion channel

Organism class: human
UniProt ID: P46098 Link_out
Gene: HTR3A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Westenberg HG: Pharmacology of antidepressants: selectivity or multiplicity? J Clin Psychiatry. 1999;60 Suppl 17:4-8; discussion 46-8. Pubmed
  2. Gorman JM: Mirtazapine: clinical overview. J Clin Psychiatry. 1999;60 Suppl 17:9-13; discussion 46-8. Pubmed
  3. Kast RE, Foley KF: Cancer chemotherapy and cachexia: mirtazapine and olanzapine are 5-HT3 antagonists with good antinausea effects. Eur J Cancer Care (Engl). 2007 Jul;16(4):351-4. Pubmed
  4. de Boer T: The effects of mirtazapine on central noradrenergic and serotonergic neurotransmission. Int Clin Psychopharmacol. 1995 Dec;10 Suppl 4:19-23. Pubmed
  5. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
  6. Anttila SA, Leinonen EV: A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64. Pubmed

3. Alpha-2A adrenergic receptor

Pharmacological action: yes
Actions: antagonist

Alpha-2 adrenergic receptors mediate the catecholamine- induced inhibition of adenylate cyclase through the action of G proteins. The rank order of potency for agonists of this receptor is oxymetazoline > clonidine > epinephrine > norepinephrine > phenylephrine > dopamine > p-synephrine > p-tyramine > serotonin = p-octopamine. For antagonists, the rank order is yohimbine > phentolamine = mianserine > chlorpromazine = spiperone = prazosin > propanolol > alprenolol = pindolol

Organism class: human
UniProt ID: P08913 Link_out
Gene: ADRA2A Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Garcia-Sevilla JA, Ventayol P, Perez V, Rubovszky G, Puigdemont D, Ferrer-Alcon M, Andreoli A, Guimon J, Alvarez E: Regulation of platelet alpha 2A-adrenoceptors, Gi proteins and receptor kinases in major depression: effects of mirtazapine treatment. Neuropsychopharmacology. 2004 Mar;29(3):580-8. Pubmed
  2. Anttila SA, Leinonen EV: A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64. Pubmed
  3. Besson A, Haddjeri N, Blier P, de Montigny C: Effects of the co-administration of mirtazapine and paroxetine on serotonergic neurotransmission in the rat brain. Eur Neuropsychopharmacol. 2000 May;10(3):177-88. Pubmed
  4. Schreiber S, Bleich A, Pick CG: Venlafaxine and mirtazapine: different mechanisms of antidepressant action, common opioid-mediated antinociceptive effects—a possible opioid involvement in severe depression? J Mol Neurosci. 2002 Feb-Apr;18(1-2):143-9. Pubmed
  5. Rogoz Z, Wrobel A, Dlaboga D, Maj J, Dziedzicka-Wasylewska M: Effect of repeated treatment with mirtazapine on the central alpha1-adrenergic receptors. J Physiol Pharmacol. 2002 Mar;53(1):105-16. Pubmed
  6. Rogoz Z, Wrobel A, Dlaboga D, Dziedzicka-Wasylewska M: Effect of repeated treatment with mirtazapine on the central dopaminergic D2/D3 receptors. Pol J Pharmacol. 2002 Jul-Aug;54(4):381-9. Pubmed

4. 5-hydroxytryptamine 2C receptor

Pharmacological action: unknown
Actions: antagonist

This is one of the several different receptors for 5- hydroxytryptamine (serotonin), a biogenic hormone that functions as a neurotransmitter, a hormone, and a mitogen. This receptor mediates its action by association with G proteins that activate a phosphatidylinositol-calcium second messenger system

Organism class: human
UniProt ID: P28335 Link_out
Gene: HTR2C Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Benelli A, Frigeri C, Bertolini A, Genedani S: Influence of mirtazapine on the sexual behavior of male rats. Psychopharmacology (Berl). 2004 Jan;171(3):250-8. Epub 2003 Nov 13. Pubmed
  2. Millan MJ, Gobert A, Rivet JM, Adhumeau-Auclair A, Cussac D, Newman-Tancredi A, Dekeyne A, Nicolas JP, Lejeune F: Mirtazapine enhances frontocortical dopaminergic and corticolimbic adrenergic, but not serotonergic, transmission by blockade of alpha2-adrenergic and serotonin2C receptors: a comparison with citalopram. Eur J Neurosci. 2000 Mar;12(3):1079-95. Pubmed
  3. Meert TF, Melis W, Aerts N, Clincke G: Antagonism of meta-chlorophenylpiperazine-induced inhibition of exploratory activity in an emergence procedure, the open field test, in rats. Behav Pharmacol. 1997 Aug;8(4):353-63. Pubmed
  4. Millan MJ: Serotonin 5-HT2C receptors as a target for the treatment of depressive and anxious states: focus on novel therapeutic strategies. Therapie. 2005 Sep-Oct;60(5):441-60. Pubmed
  5. Dekeyne A, Iob L, Millan MJ: Following long-term training with citalopram, both mirtazapine and mianserin block its discriminative stimulus properties in rats. Psychopharmacology (Berl). 2001 Jan;153(3):389-92. Pubmed
  6. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed

5. Kappa-type opioid receptor

Pharmacological action: unknown
Actions: agonist

Inhibits neurotransmitter release by reducing calcium ion currents and increasing potassium ion conductance. Receptor for dynorphins. May play a role in arousal and regulation of autonomic and neuroendocrine functions

Organism class: human
UniProt ID: P41145 Link_out
Gene: OPRK1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Schreiber S, Rigai T, Katz Y, Pick CG: The antinociceptive effect of mirtazapine in mice is mediated through serotonergic, noradrenergic and opioid mechanisms. Brain Res Bull. 2002 Sep 30;58(6):601-5. Pubmed

6. Histamine H1 receptor

Pharmacological action: no
Actions: antagonist

In peripheral tissues, the H1 subclass of histamine receptors mediates the contraction of smooth muscles, increase in capillary permeability due to contraction of terminal venules, and catecholamine release from adrenal medulla, as well as mediating neurotransmission in the central nervous system

Organism class: human
UniProt ID: P35367 Link_out
Gene: HRH1 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Chen X, Ji ZL, Chen YZ: TTD: Therapeutic Target Database. Nucleic Acids Res. 2002 Jan 1;30(1):412-5. Pubmed
Enzymes

1. Cytochrome P450 3A4

Actions: substrate, inhibitor

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It performs a variety of oxidation reactions (e.g. caffeine 8-oxidation, omeprazole sulphoxidation, midazolam 1'-hydroxylation and midazolam 4- hydroxylation) of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. The enzyme also hydroxylates etoposide

UniProt ID: P08684 Link_out
Gene: CYP3A4
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Anttila SA, Leinonen EV: A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Stormer E, von Moltke LL, Shader RI, Greenblatt DJ: Metabolism of the antidepressant mirtazapine in vitro: contribution of cytochromes P-450 1A2, 2D6, and 3A4. Drug Metab Dispos. 2000 Oct;28(10):1168-75. Pubmed

2. Cytochrome P450 2D6

Actions: substrate, inhibitor, inducer

Responsible for the metabolism of many drugs and environmental chemicals that it oxidizes. It is involved in the metabolism of drugs such as antiarrhythmics, adrenoceptor antagonists, and tricyclic antidepressants

UniProt ID: P10635 Link_out
Gene: CYP2D6 Link_out
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Anttila SA, Leinonen EV: A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Stormer E, von Moltke LL, Shader RI, Greenblatt DJ: Metabolism of the antidepressant mirtazapine in vitro: contribution of cytochromes P-450 1A2, 2D6, and 3A4. Drug Metab Dispos. 2000 Oct;28(10):1168-75. Pubmed

3. Cytochrome P450 1A2

Actions: substrate

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. Most active in catalyzing 2-hydroxylation. Caffeine is metabolized primarily by cytochrome CYP1A2 in the liver through an initial N3-demethylation. Also acts in the metabolism of aflatoxin B1 and acetaminophen

UniProt ID: P05177 Link_out
Gene: CYP1A2
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Anttila SA, Leinonen EV: A review of the pharmacological and clinical profile of mirtazapine. CNS Drug Rev. 2001 Fall;7(3):249-64. Pubmed
  2. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
  3. Stormer E, von Moltke LL, Shader RI, Greenblatt DJ: Metabolism of the antidepressant mirtazapine in vitro: contribution of cytochromes P-450 1A2, 2D6, and 3A4. Drug Metab Dispos. 2000 Oct;28(10):1168-75. Pubmed

4. Cytochrome P450 2C9

Actions: substrate

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. This enzyme contributes to the wide pharmacokinetics variability of the metabolism of drugs such as S- warfarin, diclofenac, phenytoin, tolbutamide and losartan

UniProt ID: P11712 Link_out
Gene: CYP2C9
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed

5. Cytochrome P450 2C8

Actions: substrate

Cytochromes P450 are a group of heme-thiolate monooxygenases. In liver microsomes, this enzyme is involved in an NADPH-dependent electron transport pathway. It oxidizes a variety of structurally unrelated compounds, including steroids, fatty acids, and xenobiotics. In the epoxidation of arachidonic acid it generates only 14,15- and 11,12-cis-epoxyeicosatrienoic acids. It is the principal enzyme responsible for the metabolism the anti- cancer drug paclitaxel (taxol)

UniProt ID: P10632 Link_out
Gene: CYP2C8
Protein Sequence: FASTA
Gene Sequence: FASTA
SNPs: SNPJam Report Link_out

References:
  1. Preissner S, Kroll K, Dunkel M, Senger C, Goldsobel G, Kuzman D, Guenther S, Winnenburg R, Schroeder M, Preissner R: SuperCYP: a comprehensive database on Cytochrome P450 enzymes including a tool for analysis of CYP-drug interactions. Nucleic Acids Res. 2010 Jan;38(Database issue):D237-43. Epub 2009 Nov 24. Pubmed
Comments
Drug created on June 13, 2005 07:24 / Updated on April 19, 2011 15:03

This project is supported by Genome Alberta & Genome Canada, a not-for-profit organization that is leading Canada's national genomics strategy with $600 million in funding from the federal government. This project is also supported in part by GenomeQuest, Inc., an enterprise genomic information company serving the life science community.