Klin Farmakol Farm. 2004;18(2):102-107

Liekové interakcie na úrovni cytochrómov P450. Časť II. Interakcie na úrovni CYP2D6

Jana Baranová, Pavel Anzenbacher, Lucie Kousalová
Ústav farmakologie LF UP a FN Olomouc

Keywords: drug interactions, cytocromes P450, CYP2D6, antipsychotics, antidepresives, beta blockers.

Published: December 31, 2004  Show citation

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Baranová J, Anzenbacher P, Kousalová L. Liekové interakcie na úrovni cytochrómov P450. Časť II. Interakcie na úrovni CYP2D6. Klin Farmakol Farm. 2004;18(2):102-107.

CYP2D6 je forma cytochrómov P450, ktorá sa podieľa na približne 20 % známych premien liečiv, ktoré prebiehajú za účasti cytochrómov P450. Medzi liečivá, ktoré sú považované za typické substráty s veľkým potenciálom k interakciám, patrí väčšina ?-adrenoreceptorových blokátorov, tricyklických antidepresív a selektívnych inhibítorov spätného vychytávania serotonínu (SSRI). Liekové interakcie na úrovni CYP2D6 sú spôsobené predovšetkým inhibíciou CYP2D6. Vzhľadom k závažnosti prípadných nežiaducich účinkov (napr. ťažkej bradykardie v dôsledku súčasného podávania beta blokátorov metoprololu a SSRI paroxetínu) je potreba pri súčasnej medikácii vyberať z ponúkaných liečiv tie možnosti, kde sú liekové interakcie minimálne. Dôležitým faktorom je prítomnosť génového polymorfizmu CYP2D6, kedy u jedincov s fenotypom pomalého metabolizátora je možnosť efektu liekových interakcií výrazne zvýšená.

Kľúčové slová

liekové interakcie, cytochrómy P450, CYP2D6, inhibícia, farmakogenetika, metabolizmus.

DRUG INTERACTIONS BASED ON METABOLISM VIA CYTOCHROMES P450

PART II. INTERACTIONS INVOLVING CYP2D6

CYP2D6 is one of the most typical forms of cytochromes P450 and participates in metabolism of approximately one fifth of drugs with known metabolic pathways. Among drugs which are considered as typical CYP2D6 substrates with great interacting potential belong most of the ?-adrenoreceptor blockers, majority of tricyclic antidepressants and of selective inhibitors of serotonin reuptake (SSRI). Drug interactions on CYP2D6 level are caused mostly by inhibition of CYP2D6. Pharmacogenetic data concerning the presence of many alleles leading to phenotype of slow metabolizers increase the importance of elimination of possible drug interactions at the level of this enzyme. Concerning the relevancy of adverse effects it is necessary to select the drugs which have minimum of drug interactions to avoid cases as e.g severe bradycardia resulting from concomitant medication of metoprolol (beta blocking agent) and paroxetine (SSRI).

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