CYP2D6

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Cytochroma P450 CYP2D6.

Cytochroma P450 CYP2D6 (-atis, n.) (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.[1]

Natura structuraque biochemica[recensere | fontem recensere]

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

Genetica[recensere | fontem recensere]

Phaenotypicae variantia[recensere | fontem recensere]

Pluribus variantiis geni CYP2D6 (chromosoma 22q13.1) varietates phaenotypicae sequuntur. Activitates igitur enzymaticae discriptae sunt[2][3]

  • 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[recensere | fontem recensere]

Allelonorum[4] 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[recensere | fontem recensere]

Pharmaca relata ad CYP2D6[5][6].
Substrati Inhibitores[7] Inductores[8]
  • Substantiae beta-receptoria inhibendi
    • Metoclopramidum
  • Inhibitores reabsorptionis Serotonini selectivi (SSRI):
  • Moclobemidum
  • Terbinaphinum
  • Quinidinum
  • Amiodaronum
  • Alia antidepressiva
  • Antibiotica
  • Antihistaminica
    • Chlorphenaminum
    • Difenhidraminum
  • Antipsychotica
  • Bupropionum (forte)
  • Celecoxibum
  • Cimetidinum
  • Chloranphenicolum
  • Cocaina
  • Doxorubicinum
  • Metoclopramidum
  • Metadonum
  • Moclobemidum
  • Quinidinum
  • Ranitidinum
  • Ranolazinum
  • Ritonavirum
  • Halophantrinum
  • Imipraminum
  • Levomepromazinum
  • Vincae alcaloidi[17]
    • Aimalicinum
    • Berberinum
    • Coniinum
    • Ergotaminum
    • Graminum
    • Harmalinum
    • Laudanosinum
    • Sempervirinum
    • Vinblastinum
    • Vincaminum
    • Vincristinum
  • Chinidinum (forte)
  • Dimenhydrinatum
  • 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 φάρμακον[18] vigilantiae est.

Cancer mammae[recensere | fontem recensere]

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.[19]

Notae[recensere | fontem recensere]

  1. Ingelman-Sundberg M (2005). Genetic polymorphisms of cytochrome P450 2D6 (CYP2D6): clinical consequences, evolutionary aspects and functional diversity. Pharmacogenom J 5: 6-13
  2. Bertilsson 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.
  3. 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
  4. Verbum de αλλήλων, allelon, alleli n. derivatum
  5. Cozza KL, Armstrong SC (2001). The Cytochrome P450 System. Drug Interaction Principles for Medical Practice. Washington, DC: American Psychiatric Publishing
  6. Preskorn SH (1996). Clinical Pharmacology of Selective Serotonin Reuptake Inhibitors. 1st ed.: Professional Communications, Inc.
  7. Inhibitor cum subtratorum effectibus fortioribus
  8. Inductor cum subtratorum effectibus minoribus
  9. substratum quoque CYP1A2 (solum gregum chemicorum lateralium)
  10. substratum quoque CYP2C9
  11. Yuji Horikiri; Takehiko Suzuki; Masakazu Mizobe (March 1998). "Pharmacokinetics and metabolism of bisoprolol enantiomers in humans". Journal of Pharmaceutical Sciences 87 (3): 289–294 
  12. Lind AB, Reis M, Bengtsson F, Jonzier-Perey M, Powell Golay K, Ahlner J, Baumann P, Dahl ML (2009). "Steady-state concentrations of mirtazapine, N-desmethylmirtazapine, 8-hydroxymirtazapine and their enantiomers in relation to cytochrome P450 2D6 genotype, age and smoking behaviour". Clin Pharmacokinet 48 (1): 63-70 
  13. Acute dyskinetic syndrome during chloropromazine treatment of a female patient with CYP2D6 poor metabolism phenotype
  14. Gahr, M; Gastl, R; Kölle, MA; Schönfeldt-Lecuona, C; Freudenmann, RW (2012). "Successful treatment of schizophrenia with melperone augmentation in a patient with phenotypic CYP2D6 ultrarapid metabolization: a case report". Journal of Medical Case Reports 6 (1): 49  (Anglice)
  15. Köhnke, MD; Lutz, U; Wiatr, G; Schwärzler, F; Weller, B; Schott, K; Buchkremer, G (April 2006). "Cytochrome P450 2D6 dependent metabolization of risperidone is inhibited by melperone". European Journal of Clinical Pharmacology 62 (4): 333–334  (Anglice)
  16. Grözinger, M; Dragicevic, A; Hiemke, C; Shams, M; Müller, MJ; Härtter, S (January 2003). "Melperone is an inhibitor of the CYP2D6 catalyzed O-demethylation of venlafaxine". Pharmacopsychiatry 36 (1): 3–6  (Anglice)
  17. Tabula 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 (Anglice)
  18. pharmacon = Genitivus pluralis: eo φάρμακον vigilantia significat remediorum sive medicamentorum vigilantia
  19. 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) (Anglice)

Nexus externi[recensere | fontem recensere]