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Zapytanie: HADUCH
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Tytuł oryginału: Inhibition and possible induction of rat CYP2D after short- and long-term treatment with antidepressants.
Autorzy: Daniel Władysława A., Haduch A., Wójcikowski J.
Źródło: J. Pharm. Pharmacol. 2002: 54 (11) s.1545-1552, il., tab., bibliogr. [45] poz.
Sygnatura GBL: 300,961

Hasła klasyfikacyjne GBL:
  • farmacja

    Typ dokumentu:
  • praca doświadczalna
  • praca opublikowana za granicą
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • szczury
  • in vitro
  • płeć męska

    Streszczenie angielskie: The aim of this study was to investigate the influence of tricyclic (imipramine, amitriptyline, clomipramine, despiramine), selective serotonin reuptake inhibitors (SSRIs: fluoxetine, sertraline) and novel antidepressant drugs (mitrazapine, nefazodone) on the activity of CYP2D, measured as a rate of ethylmorphine )-deethylation. the reaction was studied in control liver microsomes in the presence of the antidepressants, as well as in microsomes of rats treated intraperitoneally for one day or two weeks (twice a day) with pharmacological doses of the drugs (imipramine, amitriptyline, clomipramine, nefazodone 10 mg kg**-1 i.p.; desipramine, fluoxetine, sertaline 5 mg kg**-1 i.p.; mitrazapine 3 mg kg**-1 i.p.), in the absence of the antiderpressants in-vitro. Antidepressants decreased the activity of the rat CYP2D by competitive inhibition of the emzyme, the potency of their inhibitory effect being as follows: clomipramine(Ki = 14 ćm) sertraline ÷ fluoxetine (Ki = 17 and 16 ćm, respectively) imipramine ÷ amitripine (Ki = 26 and 25 ćm, respectively) desipramine (Ki = 44 ćm) nefazodone (Ki = 55 ćm) mirtazapine (Ki = 107 ćm). A oneday treatment with antidepressants caused a significant decrease in the CYP2D activity after imipramine, fluoxetine and sertraline. After prolonged administration of antidepressants, the decreased CYP2D activity produced by imipramine, fluoxetine and sertraline was still maintained. Moreover, amitriptyline and nefazodone significantly decreased, while mirtazapine increased the activity of the enzyme...

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    Tytuł oryginału: The contribution of cytochrome P-450 isoenzymes to the metabolism of phenothiazine neuroleptics.
    Autorzy: Daniel W[ładysława] A., Syrek M., Haduch A.
    Źródło: Eur. Neuropsychopharmacol. 2002: 12 (5) s.371-377, il., tab., bibliogr. s. 376-377
    Sygnatura GBL: 313,361

    Typ dokumentu:
  • praca doświadczalna
  • praca opublikowana za granicą
  • tytuł obcojęzyczny

    Wskaźnik treści:
  • zwierzęta
  • szczury
  • płeć męska
  • in vitro

    Streszczenie angielskie: The aim of the present study was to determine optimum conditions for studying promazine and perazine metabolism in rat liver microsomes and to investigate the influence of specific cytochrome P-450 inhibitors on 5-sulfoxidation and N-denmthylation of these neuroleptics. Based on the developed method, the metabolism of neuroleptics in liver microsomes was studied at linear dependence of product formation on time, and protein and substrate concentrations (incubation time: 10 min; concentration of microsomal proteins; promazine - 0,7 mg ml-1, perazine - 0,5 mg ml-1, substrate concentrations, promazine - 25,40 and 75 nmol ml-1, perazine- 20, 35, 50 mmol ml-1). A Dixon analysis of the metabolism of neuroleptics showed that quinine (a CYP2D1 inhibitor), metyrapone (a CYP2B1/B2 inhibitor) and ŕ-naphthoflavone (a CYP1A2/2 inhibitor) affected, whereas erythromycin (a CYP3A inhibitor) and sulfaphenazole (a CYP2C inhibitor) did not change the neuroleptic biotransformation. N-Demehtylation of promazine was competitively inhibited by quinine (K1=20 ćM) and metyrapone (K1=83 ćM), while of perazine - by quinine (K1=46.5 ćM), metyrapone (K1=46 ćM) and ŕ-napthoflavone (K1=78.8 ćM). 5-Sulfoxidation of promazine was inhibited only by quinine (K1=28.6 ćM), whereas that of perazine - by quinine (K1 = 10 ćM) and metyrapone (K1 = 96 ćM). The results obtained are compared with our previous findings of analogous experiments concerning thioridazine, and with the data on other phenothiazines and species. In summary, it is proposed that N-demethylation of the mentioned phenothiazine neuroleptics...

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