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Ayurveda Renaissance – Quo Vadis?
Published in D. Suresh Kumar, Ayurveda in the New Millennium, 2020
Ghodke et al. (2011) studied the gene polymorphism of the CYP2C19 gene involved in metabolism of many drugs (Goldstein and de Morais 1994: Daly 1995) in 132 unrelated healthy subjects. Significant association was observed between CYP2C19 genotype and major classes of prakṛti types. The extensive metabolizer (EM) genotype (∗1/∗1, ∗1/∗2, ∗1/∗3) was found to be predominant in pitta prakṛti (91%). Genotype (∗1/∗3) specific for EM group was present only in pitta prakṛti. The poor metabolizer (P.M.) genotype (∗2/∗2, ∗ 2/∗3, ∗3/∗3) was highest (31%) in kapha prakṛti when compared with vāta (12%) and pitta prakṛti (9%). Genotype (∗2/∗3) which is typical of the P.M. group was significant in kapha prakṛti. The authors observed interesting correlations between CYP2C19 genotypes and prakṛti, with fast and slow metabolism being one of the major distinguishing and differentiating characteristics.
Adrenergic Agonists
Published in Sahab Uddin, Rashid Mamunur, Advances in Neuropharmacology, 2020
Other long-acting β2 receptor selective agonists are salmeterol, formoterol, arformoterol, carmoterol, and indacaterol. Salmeterol is a β2 selective receptor agonist, highly specific and showing long duration of activity which is more than 12 h. It is mainly used for treating COPD. It is metabolized by CYP3A4. The onset of activity is slow. Formoterol β2 receptor selective agonist with quick action while used as an inhalation and a duration of action which is long and lasts for 12 h. The drug is used in treating bronchospasm, asthma, and obstructive pulmonary disease. Arformoterol is a long-acting β2 receptor selective agonist. The drug is used long-term for treating COPD and bronchoconstriction. Metabolism is by the enzymes CYP2C19 and CYP2D6. The adverse events include insomnia, tachycardia, reduction in plasma potassium level and a rise in the level of plasma glucose. Carmoterol, a β2 selective adrenergic agonist is having greater selectivity. The drug shows a fast onset of activity and the duration of activity is very long which lasts more than 24 h. It is a bronchodilator used in treating asthma and COPD. Indacaterol is a β2 adrenergic receptor selective agonist with a rapid onset and long duration in activity. The drug is used in treating COPD and asthma (Brunton et al., 2011; Barisione et al., 2010).
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Published in Caroline Ashley, Aileen Dunleavy, John Cunningham, The Renal Drug Handbook, 2018
Caroline Ashley, Aileen Dunleavy, John Cunningham
Omeprazole is completely metabolised in the liver by the cytochrome P450 system to form inactive metabolites which are excreted mostly in the urine and to a lesser extent in bile. CYP2C19 produces hydroxyomeprazole, the major metabolite, CYP3A4 produces omeprazole sulphone.
Genetic polymorphism of clopidogrel metabolism related gene CYP2C19 gene in Chinese from Foshan area of Guangdong Province
Published in Hematology, 2022
Xiao-wen Yuan, Shi-yun Yuan, Guo-xin Wu, zhi-xin Wu, Zi-yun Guan
CYP2C19 participates in the metabolization of approximately 10% of commonly prescribed medications, such as antidepressants, antipsychotics, clopidogrel, proton pump inhibitors, and antiepileptics [7,8]. The genetic polymorphism of CYP2C19 plays an important role in related drug metabolism and may lead to inter-individual and inter-ethnic variation in patient responsiveness and adverse drug reactions [16]. Currently, at least 34 alleles of CYP2C19 have been identified. Among these alleles, the CYP2C19*2 and CYP2C19*3 alleles are responsible for the reduced activation of metabolized drugs and an increased rate of serious adverse effects that undermine clinical therapeutics [17,18]. Several studies have analysed genetic polymorphisms of the CYP2C19 gene in Chinese populations, but no study has focused on Han populations from Guangdong Province. Therefore, our results provide new data on the CYP2C19 allele frequency that could help to establish a new database for functional research and guide medicine for the Han populations of Guangdong. The CYP2C19 allele and genotype frequencies in all subjects were in Hardy-Weinberg equilibrium (χ2 = 8.00, P > 0.05).
Approaches to de-escalation of antiplatelet treatment in stabilized post-myocardial infarction patients with high ischemic risk
Published in Expert Review of Cardiovascular Therapy, 2022
Placido Maria Mazzone, Dominick J. Angiolillo, Davide Capodanno
POPULAR GENETICS was an open-label, noninferiority and superiority trial investigating the efficacy and safety of CYP2C19 genotype-guided selection of P2Y12 inhibitor versus standard DAPT (with prasugrel or ticagrelor) in 2,488 patients with STEMI undergoing PCI [47]. In patients randomized to the genotype-guided group, CYP2C19 genotyping was performed after PCI at a median of 1 day. Therefore de-escalation, if any, occurred after a very short period of standard DAPT at variance with previous trials. Carriers of a LoF CYP2C19 allele (*2/*3) were prescribed ticagrelor or prasugrel, while noncarriers (*1/*1) were prescribed clopidogrel. This first co-primary endpoint, a composite of all-cause death, stroke, myocardial infarction, definite stent thrombosis, or major bleeding defined according to Platelet Inhibition and Patient Outcomes (PLATO) criteria at 12 months, occurred in 5.1% of patient in the genotype-guided group and in 5.9% of patients in the standard DAPT group, meeting criteria for noninferiority (absolute difference, −0.7%; 95% CI, −2.0 to 0.7; P < 0.001 for noninferiority) but not for superiority. The second co-primary endpoint was a composite of PLATO major or minor bleeding at 12 months, which occurred significantly less in the genotype-guided group (9.8% vs 12.5%; HR, 0.78; 95% CI, 0.61 to 0.98; P = 0.04). There were no significant differences between the two groups in the thrombotic/ischemic components of the two co-primary endpoints, with the exception of significantly less PLATO minor bleeding in the genotype-guided group.
Clinical pharmacology of antiplatelet drugs
Published in Expert Review of Clinical Pharmacology, 2022
Georg Gelbenegger, Bernd Jilma
Proton pump inhibitors (PPI) are known CYP2C19 substrates and show different potency to inhibit CYP2C19 [82]. PPIs are often co-administered with aspirin and P2Y12 inhibitors to prevent gastrointestinal bleeding. Omeprazole, a widely used PPI, is metabolized to hydroxyomeprazole and omeprazole sulfate primarily by CYP2C19 and CYP3A4 [83]. However, it shows a greater affinity for CYP2C19 and therefore has a greater potential for drug-drug interactions mediated by CYP2C19 [84]. Clopidogrel relies heavily on hepatic bioactivation by CYP2C19, and concomitant use with omeprazole has consistently been shown to attenuate the antiplatelet effect of clopidogrel [85–90]. In contrast, pantoprazole does not attenuate clopidogrel responsiveness [91]. A meta-analysis of >150.000 patients indicates that proton pump inhibitor use was associated with an about 30% increase in major cardiovascular events, while gastrointestinal bleeding risk was reduced by about 50% [92].