CYP2D6

Cytochroma P450 CYP2D6  (Numerus EC: 1.14.14.1) est haemoproteinum et pars gregis Cytochroma P450 ideo in metabolismo medicamentorum inter centesimae vicenas et quinas vicenas interest. 
Huic cytochromati polymorphismus exstat, ideo plures phaenotypi cum variis activitatibus noti sunt.Ingelman-Sundberg M (2005). Genetic polymorphisms of cytochrome P450 2D6 (CYP2D6): clinical consequences, evolutionary aspects and functional diversity. Pharmacogenom J 5: 6-13

 Natura structuraque biochemica 
Cytochroma P450 CYP2D6 est et polypeptidum et haemoproteinum, quod ex 497 acidis aminicis constitutum est. 

 Genetica 
 Phaenotypicae variantia 
Pluribus variantiis geni CYP2D6 (chromosoma 22q13.1) varietates phaenotypicae sequuntur. 
Activitates igitur enzymaticae discriptae suntBertilsson L, Dahl ML, Dalén P, Al-Shurbaji A (2002). Molecular genetics of CYP2D6: clinical relevance with focus on psychotropic drugs. Br J Clin Pharmacol. 53 (2): 111–22.Llerena A, Dorado P, Peñas-Lledó EM (2009). Pharmacogenetics of debrisoquine and its use as a marker for CYP2D6 hydroxylation capacity. Pharmacogenomics. 10 (1): 17–28

 tarda ("poor metabolizer") — functio nulla seu laesa 
 intermedia ("intermediate metabolizer") 
 extensiva ("extensive metabolizer") sive efficiens ("efficient metabolizer") — functionis normalis apte dicens 
 rapida ("ultrarapid metabolizer") — pluria CYP2D6 genorum expressa sunt ex quibus functio aucta nascitur (polymorphismus geneticus)

 Allelonorum variantia 
AllelonorumVerbum de αλλήλων, allelon, alleli n. derivatum quoque variantia CYP2D6 allelo chromosomatis 22 explicabilis est quae plures quam centum allela continet.

 CYP2D6 enzymi activitas for selected alles αλλήλων CYP2D6 activitas CYP2D6*1 normalis CYP2D6*2 normalis CYP2D6*3 nulla CYP2D6*4 nulla CYP2D6*5 nulla CYP2D6*6 nulla CYP2D6*7 nulla CYP2D6*8 nulla CYP2D6*9 laesa CYP2D6*10 laesa CYP2D6*11 nulla CYP2D6*12 nulla CYP2D6*13 nulla CYP2D6*14 nulla CYP2D6*15 nulla CYP2D6*17 laesa CYP2D6*19 nulla CYP2D6*20 nulla CYP2D6*21 nulla CYP2D6*29 laesa CYP2D6*31 nulla CYP2D6*38 nulla CYP2D6*40 nulla CYP2D6*41 laesa CYP2D6*42 nulla CYP2D6*68 nulla CYP2D6*92 nulla CYP2D6*100 nulla CYP2D6*101 nulla CYP2D6 duplicatio aucta

 Pharmaca ad CYP2D6 relata 

 Pharmaca relata ad CYP2D6Cozza KL, Armstrong SC (2001). The Cytochrome P450 System. Drug Interaction Principles for Medical Practice. Washington, DC: American Psychiatric PublishingPreskorn SH (1996). Clinical Pharmacology of Selective Serotonin Reuptake Inhibitors. 1st ed.: Professional Communications, Inc..|-
! Substrati !! InhibitoresInhibitor cum subtratorum effectibus fortioribus !! InductoresInductor cum subtratorum effectibus minoribus
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 Antiarrhythmica (classis I)
 Flecainidum
 Lidocaínum
 Propafenonum
 Encainidum
 Mexiletinum
 Substantiae beta-receptoria inhibendi
 Propranololumsubstratum quoque CYP1A2 (solum gregum chemicorum lateralium)
 Metoprololum
 Carvedilolumsubstratum quoque CYP2C9
 Timololum
 Alprenololum
 Atenololum
 Bisoprololum ( (R)-(+)-bisoprololum > (S)-(-)-bisoprololum) )
 Substantiae antidepressivae
 Antidepressiva tricyclica 
 Imipraminum
 Amitriptylinum
 Doxepinum 
 Antidepressiva tetracyclica
 Mianserinum
 Mirtazapinum
  Inhibitores reabsorptionis Serotonini selectivi (SSRI) 
 Fluoxetinum
 Paroxetinum
 Venlafaxinum
 Opioidi
 Codeinum
 Tramadolum
 Oxicodonum
 Debrisoquinum
 Dextrometorphanum
 Antipsychotica
 Haloperidolum
 Risperidonum
 Perphenazinum
 Thioridazinum
 Zuclopenthixolum
 Remoxipridum
 Aripiprazolum
 Ondansetronum
 Fenforminum
 Tropisetronum
 Amphetamina
 Chlorfenaminum
 Tamoxifenum
 Cinnarizidum 
 Flunarizidum
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 Substantiae beta-receptoria inhibendi
 Metoclopramidum
 Inhibitores reabsorptionis Serotonini selectivi (SSRI):
 Citalopramum
 Fluoxetinum (forte)
 Paroxetinum (forte)
 Moclobemidum
 Terbinaphinum
 Quinidinum
 Amiodaronum
 Alia antidepressiva
 Clomipraminum
 Doxepinum
 Antibiotica
 Ciprofloxacinum
 Antihistaminica
 Chlorphenaminum
 Difenhidraminum
 Antipsychotica
 Pimozidum
 Thioridazinum
 ChlorpromazinumAcute dyskinetic syndrome during chloropromazine treatment of a female patient with CYP2D6 poor metabolism phenotype
 Haloperidolum
 Melperonum   
 Perphenazinum
 Zuclopenthixolum
 Bupropionum (forte)
 Celecoxibum
 Cimetidinum
 Chloranphenicolum
 Cocaina
 Doxorubicinum
 Metoclopramidum
 Metadonum
 Moclobemidum
 Quinidinum
 Ranitidinum
 Ranolazinum
 Ritonavirum
 Halophantrinum
 Imipraminum
 Levomepromazinum
 Vincae alcaloidiTabula subtratorum inhibitorum cytochromatis CYP2D6, fons: Ingelman-Sundberg M: Genetic polymorphisms of cytochrome P450 2D6 (CYP2D6): clinical consequences, evolutionary aspects and functional diversity, The Pharmacogenomics Journal 
 Aimalicinum
 Berberinum
 Coniinum
 Ergotaminum
 Graminum
 Harmalinum
 Laudanosinum
 Sempervirinum
 Vinblastinum
 Vincaminum
 Vincristinum
 Chinidinum (forte)
 Dimenhydrinatum 
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 Piperidinum
 Gluthetimidum''' (forte)
 Carbamazepinum
 Dexametasonum
 Rifampicinum
 Propafenonum

Exempli gratia aegrotus quidam Paroxetinum (inhibitorem reabsorptionis Serotonini selectivum, inhibitorem CYP2D6) simul cum Metoprololo (Substantia beta-receptoria inhibendi, substrato CYP2D6) consumens a causa de Paroxetini inhibitione demonstrare effectus secundarios potest. Istud potissimum φάρμακονpharmacon = Genitivus pluralis: eo φάρμακον vigilantia significat remediorum sive medicamentorum vigilantia vigilantiae est.

 Cancer mammae 
Ad cancri therapiam mammae substratum CYP2D6 tamoxifenum uti potest. Posse aegrotas in depressionem quoque incidere et simul se cum inhibitoribus CYP2D6 antidepressivis, per exemplum paroxetino, tractari notum est. Haec combinatio substrati cum inhibitore ad debilitationem tamoxifeni effectuum ducere potest.Selective serotonin reuptake inhibitors and breast cancer mortality in women receiving tamoxifen: a population based cohort study (Serotoni inhibitores et cancri mammae mortalitas feminarum cum uso tamoxifeni) 

Notae

Nexus externi
 PharmGKB: explanatae PGx genorum informationes ad CYP2D6  

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