Search results for "Drug interactions"
showing 10 items of 229 documents
Clinical pharmacology and safety profile of esomeprazole, the first enantiomerically pure proton pump inhibitor
2001
Awareness of important differences in the pharmacological profile of individual optical isomers of chiral drugs led to the development of esomeprazole, the S-isomer of omeprazole, a new pharmacological entity designed to improve the clinical outcome of available proton pump inhibitors in the management of acid-related disorders. The superior acid control achieved by esomeprazole is mainly due to an advantageous metabolism compared with racemate omeprazole, leading to improved bioavailability and to enhanced delivery of the drug to the gastric proton pump.
An overview of statin-induced myopathy and perspectives for the future
2020
Introduction: Statins remain the most commonly prescribed lipid-lowering drug class for the treatment of atherosclerotic cardiovascular disease. Their well-recognized side effects are known as statin-associated muscle symptom (SAMS). Some advances in this field have been made in recent years, but the understanding of the mechanisms has lagged. Investigating the specific role of the anti-HMGCR autoantibody, pharmacokinetic genetic variants, characterization of the known phenotypes of statin toxicity, in relation to clinical markers of disease, is of high importance. Areas covered: We summarized currently available findings (on PubMed) related to SAMS and discussed the therapeutic approaches,…
Recent progress in the pharmacotherapy of cancer pain.
2001
Cancer pain can be relatively well managed with primary therapies, according to the WHO ladder. However, different conditions may limit the response to the analgesic drug used, which are mainly oploids. Specifically, adverse effects may prevail against the analgesic activity in the clinical setting. New pharmacological strategies may enable a more satisfactory response to be obtained, in terms of balance between analgesia and adverse effects. The change of route of administration or the use of alternative opioids is a first-line option. The use of adjuvant drugs may also improve analgesia with different mechanisms. Recent studies have demonstrated the value of these alternative approaches. …
Herbal hepatotoxicity: a hidden epidemic
2011
Complementary and alternative therapies, including herbal products, have become increasingly popular in the general population and among patients and physicians. Regulations and pharmacovigilance regarding herbal drugs are still incomplete and need to be improved. In fact, herbals are commonly marketed on the Internet, and in many countries they are sold as food supplements, which are beyond the control of drug regulatory agencies. In Europe and the U.S., reports of hepatotoxicity from these products, including those advertised for liver diseases, are accumulating. Many herbal drugs are also commonly used in children, and in women during pregnancy and lactation, because they are believed to…
Fast Regulation of Cytochrome P450 Activities by Phosphorylation and Consequences for Drug Metabolism and Toxicity
2002
In contrast to the well-known regulation of cytochrome P450 (CYP) activity by enzyme induction, which represents a process with slow onset and slow offset, more recent studies revealed phosphorylation as a fast (within observation instantaneous) and isoenzyme-selective regulation. The phosphorylated enzyme (investigated isozyme: CYP2B1) was fully inactive. The phosphorylation is mediated by PKA and hence under control of hormones and drugs that alter cellular cAMP levels. The consequences for the metabolic control of toxic species derived from drugs and environmental carcinogens are discussed. This information will help to improve therapy with drugs metabolized by CYPs which are phosphoryla…
Cell Lines: A Tool for In Vitro Drug Metabolism Studies
2008
Primary cultured hepatocytes are a valuable in vitro model for drug metabolism studies. However, their widespread use is greatly hindered by the scarcity of suitable human liver samples. Moreover, the well-known in vitro phenotypic instability of hepatocytes, the irregular availability of fresh human liver for cell harvesting purposes, and the high batch-to-batch functional variability of hepatocyte preparations obtained from different human liver donors, seriously complicate their use in routine testing. To overcome these limitations, different cell line models have been proposed for drug metabolism screening. Human liver-derived cell lines would be ideal models for this purpose given thei…
Pharmacotherapy, drug-drug interactions and potentially inappropriate medication in depressive disorders.
2021
Introduction The aim of this study was to describe the number and type of drugs used to treat depressive disorders in inpatient psychiatry and to analyse the determinants of potential drug-drug interactions (pDDI) and potentially inappropriate medication (PIM). Methods Our study was part of a larger pharmacovigilance project funded by the German Innovation Funds. It included all inpatients with a main diagnosis in the group of depressive episodes (F32, ICD-10) or recurrent depressive disorders (F33) discharged from eight psychiatric hospitals in Germany between 1 October 2017 and 30 September 2018 or between 1 January and 31 December 2019. Results The study included 14,418 inpatient cases.…
Epigenomics and metabolomics reveal the mechanism of the APOA2-saturated fat intake interaction affecting obesity
2018
BACKGROUND: The putative functional variant −265T>C (rs5082) within the APOA2 promoter has shown consistent interactions with saturated fatty acid (SFA) intake to influence the risk of obesity. OBJECTIVE: The aim of this study was to implement an integrative approach to characterize the molecular basis of this interaction. DESIGN: We conducted an epigenome-wide scan on 80 participants carrying either the rs5082 CC or TT genotypes and consuming either a low-SFA (C genotype, promoting an APOA2 expression difference between APOA2 genotypes on a high-SFA diet, and modulating BCAA and tryptophan metabolic pathways. These findings identify potential mechanisms by which this highly reproducible ge…
Identification of P-glycoprotein substrates and inhibitors among psychoactive compounds--implications for pharmacokinetics of selected substrates.
2004
Abstract The pharmacokinetics of antipsychotic drugs has become an integral part in understanding their pharmacodynamic activity and clinical effects. In addition to metabolism aspects, carrier-mediated transport, particularly secretion by ABC transporters, has been discussed as potentially relevant for this group of therapeutics. In this study, the psychoactive compounds perphenazine, flupentixol, domperidone, desmethyl clozapine, haloperidol, fluphenazine, fluvoxamine, olanzapine, levome-promazine, perazine, desmethyl perazine, clozapine, quetiapine and amisulpride were characterized in terms of P-glycoprotein (P-gp) affinity and transport. Experimental methods involved a radioligand disp…
Bio-predictive tablet disintegration: Effect of water diffusivity, fluid flow, food composition and test conditions
2013
Abstract Food intake may delay tablet disintegration. Current in vitro methods have little predictive potential to account for such effects. The effect of a variety of factors on the disintegration of immediate release tablets in the gastrointestinal tract has been identified. They include viscosity of the media, precipitation of food constituents on the surface of the tablet and reduction of water diffusivity in the media as well as changes in the hydrodynamics in the surrounding media of the solid dosage form. In order to improve the predictability of food affecting the disintegration of a dosage form, tablet disintegration in various types of a liquefied meal has been studied under stati…