The study was designed to define the contribution of cytochrome p450 2C19 (CYP2C19) and cytochrome p450 3A4 (CYP3A4) to citalopram N-demethylation and to evaluate the relationship between the disposition of citalopram and CYP2C19 genotype. A single oral 40-mg dose of citalopram was administered to eight extensive metabolizers and five poor metabolizers recruited from 77 healthy Chinese voluntee...

Cytochrome P4502C19 (CYP2C19) is an important drug-metabolizing enzyme involved in the biotransformation of, for example, proton pump inhibitors and antidepressants. Several in vivo studies have shown that the CYP2C19 activity is inhibited by oral contraceptives, which can cause important drug interactions. The underlying molecular mechanism has been suggested to be competitive inhibition. Howe...

background: clopidogrel is a standout amongst the most ordinarily recommended medications to avoid ischemic occasions taking after coronary disorder or stant position. however, impaired responses the therapy as well as resistance to the therapy have also been reported. genetic variants play an important role in clopidogrel biotransformation of its active metabolite that may subsequently influen...

Single nucleotide polymorphisms cause amino acid change, and protein structure function are changed. Thus, the patient improves drug resistance does not respond to therapy. Clopidogrel is an antiplatelet used for cardiovascular disease therapy such as heart failure, atherosclerosis, myocardial infarction.CYP2C19 gene a CYP450 enzyme metabolizes clopidogrel. Polymorphism of CYP2C19 causes clopid...

Omeprazole 5-hydroxylation and sulfoxidation activities were determined in liver microsomes of different humans whose levels of individual forms of cytochrome P450 (P450 or CYP) varied. Correlation coefficients between omeprazole 5-hydroxylation activities (when determined at a substrate concentration of 10 microM) and S-mephenytoin 4'-hydroxylation and testosterone 6beta-hydroxylation activiti...

We have identified CYP2C19 and CYP3A4 as the principal cytochrome P450s involved in the metabolism of flunitrazepam to its major metabolites desmethylflunitrazepam and 3-hydroxyflunitrazepam. Human CYP2C19 and CYP3A4 mediated the formation of desmethylflunitrazepam with Km values of 11.1 and 108 microM, respectively, and 3-hydroxyflunitrazepam with Km values of 642 and 34.0 microM, respectively...

Several in vitro criteria were used to assess whether three methylenedioxyphenyl (MDP) compounds, the isoquinoline alkaloids bulbocapnine, canadine, and protopine, are mechanism-based inactivators of CYP2C19. The recently reported fluorometric CYP2C19 progress curve analysis approach was applied first to determine whether these alkaloids demonstrate time-dependent inhibition. In this experiment...

According to recommendations of ESC 2020-year, de-escalation therapy with a P2Y12 receptor inhibitor (transition from prasugrel or ticagrelor clopidogrel) It can be considered as an alternative strategy dual antiplatelet (DAPT) for patients acute coronary syndrome (ACS) who are unsuitable the use strong platelet inhibitor. De-escalation performed based on individual clinical evaluation under su...

In view of conflicting data in the literature regarding the enzyme(s) responsible for metabolism of selegiline, a drug used in the treatment of Parkinson's disease, investigations were carried out in vitro using the human cytochrome P450 enzymes CYP1A1, CYP1A2, CYP2A6, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, CYP2E1, and CYP3A4 recombinantly expressed in yeast to elucidate the enzyme specificit...