502 results match your criteria Drug Metabolism and Drug Interactions[Journal]


In vitro inhibitory effects of herbal supplements on tamoxifen and irinotecan metabolism.

Drug Metabol Drug Interact 2014 ;29(4):269-79

Background: As the use of herbal supplements continues to rise throughout the world, the potential for drug-herbal interactions also increases. For chemotherapeutic prodrugs, this interaction could prevent the metabolic conversion of the prodrug to its active metabolite(s), thereby potentially resulting in subtherapeutic systemic exposure of the drug and reduced efficacy of the therapy.

Methods: In this study, in vitro metabolism with human liver microsomes is used to measure the impact of ten commonly used herbal supplements on the biotransformation of the chemotherapeutic prodrugs tamoxifen (TAM) and irinotecan (IR). Read More

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http://dx.doi.org/10.1515/dmdi-2014-0017DOI Listing
July 2015
11 Reads

Effect of silymarin pretreatment on the bioavailability of domperidone in healthy human volunteers.

Drug Metabol Drug Interact 2014 ;29(4):261-7

Background: The aim of this study was to investigate the effect of silymarin pretreatment on domperidone oral bioavailability in humans.

Methods: The rats were pretreated with silymarin for 7 days. The transport of domperidone across the rat intestine (duodenum, jejunum, ileum, and colon) was studied by using in vitro everted and non-everted sac methods. Read More

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http://dx.doi.org/10.1515/dmdi-2014-0013DOI Listing
July 2015
6 Reads

The pharmacogenetics of carboxylesterases: CES1 and CES2 genetic variants and their clinical effect.

Drug Metabol Drug Interact 2014 ;29(3):143-51

Human carboxylesterase 1 (CES1) and carboxylesterase 2 (CES2) are serine esterases responsible for the hydrolysis of ester and amide bonds present in a number of pharmaceutical products. Several common genetic variants of the CES1 and CES2 genes have been shown to influence drug metabolism and clinical outcomes. Polymorphisms of the CES1 gene have been reported to affect the metabolism of dabigatran etexilate, methylphenidate, oseltamivir, imidapril, and clopidogrel, whereas variants of the CES2 gene have been found to affect aspirin and irinotecan. Read More

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https://www.degruyter.com/view/j/dmdi.2014.29.issue-3/dmdi-2
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http://dx.doi.org/10.1515/dmdi-2014-0009DOI Listing
April 2015
11 Reads

Effect of selective cyclooxygenase-2 inhibitor lumiracoxib on phenolsulfonphthalein disposition in rats.

Drug Metabol Drug Interact 2014 ;29(3):203-6

Selective cyclooxygenase-2 inhibitor lumiracoxib was shown to have the strong inhibitory potencies on the renal organic anion transporter (OAT)1 and also on OAT3 from drug transport experiments. The purpose of this study was to examine the effect of lumiracoxib on disposition of phenolsulfonphthalein (PSP) - which is mainly excreted into urine via OATs - from in vivo experiments. After the intravenous injection of PSP and lumiracoxib into rats, pharmacokinetic analysis was performed. Read More

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http://dx.doi.org/10.1515/dmdi-2014-0008DOI Listing
April 2015
9 Reads

Pharmacogenetics in Jewish populations.

Drug Metabol Drug Interact 2014 ;29(4):221-33

Spanning over 2000 years, the Jewish population has a long history of migration, population bottlenecks, expansions, and geographical isolation, which has resulted in a unique genetic architecture among the Jewish people. As such, many Mendelian disease genes and founder mutations for autosomal recessive diseases have been discovered in several Jewish groups, which have prompted recent genomic studies in the Jewish population on common disease susceptibility and other complex traits. Although few studies on the genetic determinants of drug response variability have been reported in the Jewish population, a number of unique pharmacogenetic variants have been discovered that are more common in Jewish populations than in other major racial groups. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0069DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4221483PMC
July 2015
31 Reads

Lurasidone drug-drug interaction studies: a comprehensive review.

Drug Metabol Drug Interact 2014 ;29(3):191-202

Background: To evaluate potential drug-drug interactions with the atypical antipsychotic lurasidone.

Methods: Seven phase I studies were conducted to investigate the effects of repeated dosing of ketoconazole, diltiazem, rifampin, or lithium on the pharmacokinetics (PK) of single oral doses of lurasidone, or the effects of repeated dosing of lurasidone on the PK of digoxin, midazolam, or the oral contraceptive norgestimate/ethinyl estradiol. Two 6-week, phase III studies included evaluation of the potential for interaction between lurasidone and lithium or valproate. Read More

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http://dx.doi.org/10.1515/dmdi-2014-0005DOI Listing
April 2015
25 Reads

Molecular functionality of CYP2C9 polymorphisms and their influence on drug therapy.

Drug Metabol Drug Interact 2014 ;29(4):211-20

CYP2C9 metabolizes approximately 20% of clinically used drugs, including the narrow therapeutic window drugs warfarin and phenytoin. More than 16,000 variants have been reported in the National Center for Biotechnology Information CYP2C9 database, as well as 58 alleles in the official P450 Nomenclature Committee website. Two single nucleotide polymorphisms represented by the CYP2C9*2 and CYP2C9*3 alleles have been studied extensively. Read More

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http://dx.doi.org/10.1515/dmdi-2014-0001DOI Listing
July 2015
3 Reads

Inhibition of OATP-1B1 and OATP-1B3 by tyrosine kinase inhibitors.

Drug Metabol Drug Interact 2014 ;29(4):249-59

Background: The potential of tyrosine kinase inhibitors (TKIs) interacting with other therapeutics through hepatic uptake transporter inhibition has not been fully delineated in drug-drug interactions (DDIs). This study was designed to estimate the half-maximal inhibitory concentration (IC50) values of five small-molecule TKIs (pazopanib, nilotinib, vandetanib, canertinib and erlotinib) interacting with organic anion-transporting polypeptides (OATPs): OATP-1B1 and -1B3.

Methods: The IC50 values of TKIs and rifampicin (positive control) were determined by concentration-dependent inhibition of TKIs on cellular accumulation of radiolabeled probe substrates [3H]estrone sulfate and [3H]cholecystokinin octapeptide. Read More

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http://dx.doi.org/10.1515/dmdi-2014-0014DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407688PMC
July 2015
29 Reads
7 Citations

Importance of ABC transporters in different tissues.

Drug Metabol Drug Interact 2014 ;29(2):65-6

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http://dx.doi.org/10.1515/dmdi-2014-0016DOI Listing
December 2014
3 Reads

Frequency of CYP450 enzyme gene polymorphisms in the Greek population: review of the literature, original findings and clinical significance.

Drug Metabol Drug Interact 2014 ;29(4):235-48

The cytochrome P450 (CYP450) enzyme family is involved in the oxidative metabolism of many therapeutic drugs and various endogenous substrates. These enzymes are highly polymorphic. Prevalence of CYP450 enzyme gene polymorphisms vary among different populations and substantial inter- and intra-ethnic variability in frequency of CYP450 enzyme gene polymorphisms has been reported. Read More

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http://dx.doi.org/10.1515/dmdi-2014-0006DOI Listing
July 2015
72 Reads

Pharmacogenetics of drug metabolizing enzymes in Brazilian populations.

Drug Metabol Drug Interact 2014 ;29(3):153-77

Phase I and II drug metabolizing enzymes (DMEs) play an important role in biotransformation of endogenous and exogenous compounds including drugs currently used in pharmacoterapy. Moreover, the genetic variability of DMEs causes important interindividual differences in drug and metabolite exposure, drug response, and risk of adverse drug reactions. We reviewed pharmacogenetics/pharmacogenomics (PGx) studies that evaluated the influence of polymorphisms in the CYPs genes - mainly CYP1, CYP2 and CYP3 gene families - and in the phase II genes - TPMT, NAT2, GSTs and UGTs - on therapeutic response in Brazilian cohorts. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0067DOI Listing
April 2015
6 Reads

The effect of AST-120 on the single-dose pharmacokinetics of metoprolol extended-release tablets in healthy subjects.

Drug Metabol Drug Interact 2014 ;29(2):115-21

Background: This was a randomized, open-label, three-way crossover study to assess the effects of AST-120 (an orally administered spherical carbon adsorbent acting in the gastrointestinal tract without systemic circulation) on the single-dose pharmacokinetics of metoprolol in an extended-release formulation (metoprolol ER) in healthy volunteers.

Methods: A total of 34 subjects were singly administered metoprolol ER alone (A), and metoprolol ER in combination with AST-120 simultaneously (B) and 1 h later (C).

Results: The total exposure was more significantly reduced in both treatments B and C than that in treatment A; the geometric mean ratios of area under the curve extrapolated to infinity (AUC0-∞) for B/A and C/A were reduced by approximately 30% in both treatments B and C. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0063DOI Listing
December 2014
8 Reads

Role of OATP-1B1 and/or OATP-1B3 in hepatic disposition of tyrosine kinase inhibitors.

Drug Metabol Drug Interact 2014 ;29(3):179-90

Background: The metabolism of tyrosine kinase inhibitors (TKIs) is mainly mediated via hepatic route, but the mechanism responsible for their hepatocellular accumulation is still unknown. This study was designed to understand the contribution of organic anion transporting polypeptides (OATPs) in the hepatic uptake of selected TKIs - pazopanib, canertinib, erlotinib, vandetanib and nilotinib.

Methods: Michaelis-Menten (MM) kinetic parameters for TKIs were determined by concentration-dependent cellular accumulation of selected TKIs using Chinese hamster ovary cells - wild type as well as transfected with humanized OATP-1B1 and OATP-1B3 transporter proteins. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0062DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407685PMC
April 2015
29 Reads
11 Citations

Raloxifene pharmacodynamics is influenced by genetic variants in the RANKL/RANK/OPG system and in the Wnt signaling pathway.

Drug Metabol Drug Interact 2014 ;29(2):111-4

Background: Raloxifene is a selective estrogen receptor (ER) modulator (SERM) used for the treatment of osteoporosis. However, its efficacy and also its safety vary greatly among treated patients, and it might be influenced by the individuals' genetic background. As the receptor activator of the nuclear factor κB (RANK) ligand (RANKL)/RANK/osteoprotegerin (OPG) system is essential for osteoclastogensis and Wnt signaling pathway for osteoblastogenesis, we decided to evaluate the raloxifene treatment in regard to selected polymorphisms in key genes of these two main bone regulatory pathways. Read More

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https://www.degruyter.com/view/j/dmdi.2014.29.issue-2/dmdi-2
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http://dx.doi.org/10.1515/dmdi-2013-0066DOI Listing
December 2014
4 Reads

Venlafaxine pharmacokinetics focused on drug metabolism and potential biomarkers.

Drug Metabol Drug Interact 2014 ;29(3):129-41

Venlafaxine (VEN) is one of the safest and most effective drugs used in the treatment of selective serotonin reuptake inhibitors-resistant depression, and thereby it is nowadays one of the most commonly prescribed antidepressants. Nevertheless, patients treated with antidepressant drugs including VEN have exhibited large inter-individual variability in drug outcomes, possibly due to the influence of genetic and nongenetic factors on the drug pharmacokinetics and/or pharmacodynamics. Among them, an increased interest has emerged over the last few years on the genetic and/or phenotypic profile for drug-metabolizing cytochrome P450 isoenzymes and drug transporters such as potential predictive pharmacokinetic-based biomarkers of the variability found in drug biodisposition and antidepressant response. Read More

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http://search.proquest.com/openview/4145b19093931c8374524ec7
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http://www.degruyter.com/view/j/dmdi.2014.29.issue-3/dmdi-20
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http://dx.doi.org/10.1515/dmdi-2013-0053DOI Listing
April 2015
5 Reads

Liver enzyme abnormalities during antipsychotic treatment: a case report of risperidone-associated hepatotoxicity.

Drug Metabol Drug Interact 2014 ;29(2):123-6

Background: Drug-induced liver enzyme abnormalities may indicate hepatic injury. Antipsychotic drugs also may cause increase in the liver enzymes and serum bilirubin levels. The present report evaluates the case of a patient with risperidone-associated hepatocellular damage. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0064DOI Listing
December 2014
10 Reads

Characterization of ABC transporters in human skin.

Drug Metabol Drug Interact 2014 ;29(2):91-100

Background: Most identified drug transporters belong to the ATP-binding cassette (ABC) and solute carrier (SLC) families. Recent research indicates that these transporters play an important role in the absorption, distribution and excretion of drugs, and are involved in clinically relevant drug-drug interactions for systemic drugs. However, very little is known about the role of drug transporters in human skin, especially in the disposition of topically applied drugs, and their involvement in drug-drug interactions. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0042DOI Listing
December 2014
24 Reads

Potential pharmacokinetic interactions of therapeutic cytokines or cytokine modulators on small-molecule drugs: mechanistic understanding via studies using in vitro systems.

Authors:
Jin Zhou Feng Li

Drug Metabol Drug Interact 2014 ;29(1):17-28

The potential pharmacokinetic interactions between macromolecules and small-molecule drugs have received more and more attention with the increasing development of macromolecule therapeutics. Studies have shown that cytokines can differentially modulate drug-metabolizing enzymes and transporters, which raises concerns on the potential interactions of therapeutic cytokines and cytokine modulators on the disposition of small-molecule drugs. Although many in vitro studies have been conducted to characterize the effects of cytokines on drug-metabolizing enzymes and transporters, these studies were limited to only a handful of cytokines, such as interleukin-1 (IL-1), IL-6, tumor necrosis factor-α, and interferon. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0028DOI Listing
September 2014
4 Reads

Systems medicine, stratified medicine, personalized medicine but not precision medicine.

Authors:
Gérard Siest

Drug Metabol Drug Interact 2014 ;29(1):1-2

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http://dx.doi.org/10.1515/dmdi-2013-0068DOI Listing
September 2014
16 Reads

The pharmacogenetics of drug metabolizing enzymes in the Lebanese population.

Drug Metabol Drug Interact 2014 ;29(2):81-90

Drug metabolizing enzymes (DMEs) play a major role in the metabolism and final elimination of most drugs and xenobiotics from the body. Both phase I and phase II enzymes are highly polymorphic. Most studies on the pharmacogenetics (PGx) of DMEs and its influence on interindividual variability have been conducted in Western countries. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0058DOI Listing
December 2014
9 Reads

Pharmacogenetic potential biomarkers for carbamazepine adverse drug reactions and clinical response.

Drug Metabol Drug Interact 2014 ;29(2):67-79

Carbamazepine (CBZ) is a first-line widely used anticonvulsant. It has a narrow therapeutic index and exhibits considerable interindividual and interethnic variability in clinical efficacy and adverse drug reactions including potentially life-threatening hypersensitivity reactions, such as Stevens-Johnson syndrome and toxic epidermal necrolysis. The most important pharmacogenetic finding is related to the association of CBZ-induced hypersensitivity with human leukocyte antigens (HLA class I and II alleles). Read More

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http://dx.doi.org/10.1515/dmdi-2013-0046DOI Listing
December 2014
8 Reads

Binary and ternary combinations of anti-HIV protease inhibitors: effect on gene expression and functional activity of CYP3A4 and efflux transporters.

Drug Metabol Drug Interact 2014 ;29(2):101-10

Background: The purpose of this study is to identify the effect of binary and ternary combinations of anti-HIV protease inhibitors (PIs) on the expression of metabolizing enzyme (CYP3A4) and efflux transporters [multidrug resistance-associated protein 2 (MRP2), P-glycoprotein (P-gp) and breast cancer resistant protein (BCRP)] in a model intestinal cell line (LS-180).

Methods: LS-180 cells were treated with various combinations of PIs (amprenavir, indinavir, saquinavir and lopinavir), and the mRNA expression levels of metabolizing enzyme and efflux transporters were measured using quantitative reverse transcription polymerase chain reaction. The alteration of gene expression was further correlated to the expression of nuclear hormone receptor PXR. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0056DOI Listing
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4407648PMC
December 2014
20 Reads

New challenges for pharmacogenomics.

Drug Metabol Drug Interact 2013 ;28(4):191-2

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http://dx.doi.org/10.1515/dmdi-2013-0060DOI Listing
August 2014
5 Reads

Drug metabolising enzyme polymorphisms in Middle- and Eastern-European Slavic populations.

Drug Metabol Drug Interact 2014 ;29(1):29-36

Inter-individual differences in genes for drug metabolising enzymes and drug transporters are important for understanding efficacy in drug therapy. These differences are important both for the timely estimation of the dosage that should be prescribed to a patient and for the detection of individuals who are prone to side effects from the drug at normal doses. This review summarises the literature concerning the gene variants within nine major drug metabolising enzymes and drug transporters (i. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0052DOI Listing
September 2014
6 Reads

Ethics and law in research with human biological samples: a new approach.

Authors:
Carlo Petrini

Drug Metabol Drug Interact 2014 ;29(1):61-3

During the last century a large number of documents (regulations, ethical codes, treatises, declarations, conventions) were published on the subject of ethics and clinical trials, many of them focusing on the protection of research participants. More recently various proposals have been put forward to relax some of the constraints imposed on research by these documents and regulations. It is important to distinguish between risks deriving from direct interventions on human subjects and other types of risk. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0055DOI Listing
September 2014
3 Reads

Interaction of vitamin K antagonists and trimethoprim-sulfamethoxazole: ignore at your patient's risk.

Drug Metabol Drug Interact 2014 ;29(1):53-60

The aim of the study was to summarize available literature regarding the interaction between vitamin K antagonists (VKAs) and trimethoprim-sulfamethoxazole (co-trimoxazole, TMP-SMX), and to provide recommendations for managing patient risk from this interaction. Data sources were English-language publications in the medical literature and Internet databases. Relevant publications that directly or indirectly addressed the VKA-TMP-SMX interaction were selected and reviewed. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0049DOI Listing
September 2014
4 Reads

Etomidate with or without flumazenil anesthesia for stem cell transplantation in autistic children.

Drug Metabol Drug Interact 2014 ;29(1):47-51

Background: The aim of this study was to investigate etomidate administration with or without flumazenil in autistic children who underwent intrathecal transplantation of stem cells by lumbar puncture.

Methods: Forty autistic children aged 2-12, who were scheduled for stem cell transplantation via lumbar puncture under anesthesia, were randomized for a double-blind study. The children were randomly assigned to two groups: the flumazenil group (group F, n=20) and the etomidate group (group E, n=20). Read More

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http://dx.doi.org/10.1515/dmdi-2013-0043DOI Listing
September 2014
6 Reads

Pregnane X receptor (PXR)--a contributor to the diabetes epidemic?

Drug Metabol Drug Interact 2014 ;29(1):3-15

Pregnane X receptor (PXR), a ligand-activated nuclear receptor, was originally identified as a regulator of drug and bile acid metabolism. Studies in experimental animals and humans within the last decade have revealed PXR as a regulator of energy metabolism repressing gluconeogenesis and hepatic lipid oxidation. The most recent in vivo studies demonstrate that PXR activation has a detrimental role in the regulation of glucose metabolism. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0036DOI Listing
September 2014
4 Reads

Unexpected interaction between CYP3A4 and BI 11634: is BI 11634 interacting with CYP3A4 similar to nifedipine?

Drug Metabol Drug Interact 2013 ;28(4):239-46

Background: Interactions between cytochrome P450 3A4 (CYP3A4) and its substrates are complex with multiple binding sites within the active site. BI 11634 is a factor Xa inhibitor in drug development and its interaction with CYP3A4 was evaluated.

Methods: Reaction phenotyping studies were conducted to determine human isoform(s) of cytochrome P450 responsible for BI 11634 metabolism using recombinant CYPs and specific chemical inhibitors. Read More

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https://www.degruyter.com/view/j/dmdi.2013.28.issue-4/dmdi-2
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http://dx.doi.org/10.1515/dmdi-2013-0044DOI Listing
August 2014
7 Reads

Caffeic acid inhibits organic anion transporters OAT1 and OAT3 in rat kidney.

Drug Metabol Drug Interact 2013 ;28(4):247-50

Background: Some food components influence drug elimination. Previously, we found that caffeic acid, present in coffee, fruits, and vegetables, strongly inhibited human homologs of organic anion transporters (OATs) OAT1 and OAT3, which are responsible for renal tubular secretion of anionic drugs. In this study, we examined the effect of caffeic acid on drug transport by OAT1 and OAT3 in the rat kidney. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0050DOI Listing
August 2014
4 Reads

Cytochrome P450 genetic polymorphisms of Mexican indigenous populations.

Drug Metabol Drug Interact 2013 ;28(4):193-208

This review focuses on the genetic polymorphisms of the cytochrome P450 (CYP) genes in Mexican indigenous populations, who are a part of the wide ethnic diversity of this country. These native groups have a particular historical trajectory that is different from the Mexican Mestizos. This variability may be reflected in the frequency distribution of polymorphisms in the CYP genes that encode enzymes involved in the metabolism of drugs and other xenobiotics. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0037DOI Listing
August 2014
4 Reads

Present status and perspective of pharmacogenetics in Mexico.

Drug Metabol Drug Interact 2014 ;29(1):37-45

Drug costs account for up to 24% of the country's health expenditure and there are 13,000 registered drugs being prescribed. Diabetes is the main cause of death in the country, with over 85% of diabetic patients currently under drug treatment. The importance of knowing interindividual variability in drug metabolism on Mexican populations is thus evident. Read More

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https://www.degruyter.com/view/j/dmdi.2014.29.issue-1/dmdi-2
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http://dx.doi.org/10.1515/dmdi-2013-0019DOI Listing
September 2014
7 Reads

Evaluation of partial area under the concentration time curve to estimate midazolam apparent oral clearance for cytochrome P450 3A phenotyping.

Drug Metabol Drug Interact 2013 ;28(4):217-23

Background: Midazolam apparent oral clearance (CLORAL) is used to estimate intestinal and hepatic cytochrome P450 (CYP) 3A activity. A limited sampling approach was performed to access a midazolam partial area under the concentration time curve (AUC) to estimate CLORAL.

Methods: Midazolam plasma concentrations from healthy adults were obtained during CYP3A baseline (n=116), inhibition (n=75), and induction or activation (n=66) from seven published studies. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0040DOI Listing
August 2014
11 Reads

A population pharmacokinetic model of remifentanil in pediatric patients using body-weight-dependent allometric exponents.

Drug Metabol Drug Interact 2013 ;28(4):231-7

Background: Allometric exponents in population pharmacokinetic analysis are regularly used but the issue of fixing or estimating an allometric exponent remains controversial. The objective of the current analysis is to evaluate the performance of a body-weight-dependent allometric exponent (BDE) model of remifentanil.

Methods: The study was conducted in 34 patients (neonates to 17 years and 2. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0038DOI Listing
August 2014
3 Reads

Influence of Allium sativum extract on the hypoglycemic activity of glibenclamide: an approach to possible herb-drug interaction.

Drug Metabol Drug Interact 2013 ;28(4):225-30

Background: The use of herbs with allopathic medicines increases the possibility of herb-drug interaction, which may either be beneficial or harmful. Therefore, the present study was undertaken to determine the interaction of glibenclamide, a sulfonylurea, with the aqueous extract of garlic (Allium sativum), an herb used widely as an antidiabetic agent.

Methods: The interaction was evaluated by an acute study, chronic study, oral glucose tolerance test, and body weight estimation in streptozotocin-induced diabetic rats. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0031DOI Listing
August 2014
6 Reads

Recent examples on the clinical relevance of the CYP2D6 polymorphism and endogenous functionality of CYP2D6.

Drug Metabol Drug Interact 2013 ;28(4):209-16

The cytochrome P450 2D6 (CYP2D6) belongs to a group of CYPs considered of utmost importance in the metabolism of xenobiotics. Despite being of only minor abundance in the liver, it is involved in the clearance of >25% of marketed drugs. Accordingly, CYP2D6 can be very efficiently inhibited by a couple of commonly used drugs such as some antidepressants, although induction by any drug has not been observed thus far. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0032DOI Listing
August 2014
7 Reads

Pharmacogenomics: from cell to clinic.

Authors:
Gérard Siest

Drug Metabol Drug Interact 2013 ;28(3):133

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http://dx.doi.org/10.1515/dmdi-2013-0035DOI Listing
March 2014
3 Reads

Biological characterization of the antiproliferative potential of Co(II) and Sn(IV) coordination compounds in human cancer cell lines: a comparative proteomic approach.

Drug Metabol Drug Interact 2013 ;28(3):167-76

Background: The discovery of cisplatin's antitumor activity led to a great interest in the potential application of coordination compounds as chemotherapeutic agents. It is essential to identify new compounds that selectively inhibit tumor proliferation, evading secondary effects and resistance associated with chemotherapeutics.

Methods: The in vitro antiproliferative potential of an organotin(IV) compound was evaluated using colorectal and hepatocellular carcinoma, mammary gland adenocarcinoma cell lines, and human fibroblasts. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0015DOI Listing
March 2014
21 Reads

Evaluation of drug-metabolizing enzyme hydroxylation phenotypes in Hispanic populations: the CEIBA cocktail.

Drug Metabol Drug Interact 2013 ;28(3):135-46

Interindividual differences in response to drug treatments are mainly caused by differences in drug metabolism, in which cytochrome P450 (CYP450) enzymes are involved. Genetic polymorphisms of these enzymes have a key role in this variability. However, environmental factors, endogenous metabolism and disease states also have a great influence on the actual drug metabolism rate (metabolic phenotype). Read More

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http://dx.doi.org/10.1515/dmdi-2013-0020DOI Listing
March 2014
56 Reads

Gastrointestinal bleeding secondary to interaction of Artemisia absinthium with warfarin.

Drug Metabol Drug Interact 2013 ;28(3):187-9

Artemisia absinthium, also known as wormwood, is used widely as an herbal medicine. In this report, we introduce an 82-year-old Turkish woman who was treated with warfarin for atrial fibrillation and was hospitalized for gastrointestinal bleeding as a result of extremely elevated international normalized ratio (INR) after consumption of A. absinthium. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0021DOI Listing
March 2014
88 Reads

Lexical fields of predictive and personalized medicine.

Drug Metabol Drug Interact 2013 ;28(2):125-32

Institut de Biologie Clinique Schaffner, Lens, LABCO, Paris, France.

With human genome mapping, the omics revolution and the empowering sequencing technologies developed at the turn of the century, the new goals in medicine are to switch from population medicine to individualized therapies, not only to cure diseases but also to prevent them. The purpose of this review by the pharmacogenetics and predictive medicine working group of the French clinical biology society (SFBC) is to situate in their correct context the notions of personalized medicine, pharmacogenetics, genetics and genomics, emphasizing their interactions and discussing their significance for researchers and clinicians. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0024DOI Listing
September 2013
7 Reads

Viewing drug action as network perturbation in multiple scale systems.

Authors:
Robert Barouki

Drug Metabol Drug Interact 2013 ;28(2):65-6

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http://dx.doi.org/10.1515/dmdi-2013-0025DOI Listing
September 2013
2 Reads

MDR-1 genotypes and quetiapine pharmacokinetics in healthy volunteers.

Drug Metabol Drug Interact 2013 ;28(3):163-6

Background: P-glycoprotein is an efflux transporter encoded by the multidrug-resistance MDR-1 gene, which influences the absorption and excretion of a variety of drugs. The relation between quetiapine pharmacokinetics and MDR-1 genetic polymorphisms remains controversial. Therefore, the aim of the present study was to analyze the association between quetiapine plasma concentrations and MDR-1 genetic polymorphisms in a bioequivalence trial. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0008DOI Listing
March 2014
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Concept of interactions between consumable substances in Ayurveda with special reference to foods and drugs.

Drug Metabol Drug Interact 2013 ;28(3):147-52

Ayurvedic medicines are available in the market as over-the-counter products. Today people use prescription and nonprescription medicines along with Ayurvedic medicines for quick relief from ailments. In the ancient texts of Ayurveda, the concept of interactions with various examples of food interactions and food-drug interactions are mentioned. Read More

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https://www.degruyter.com/view/j/dmdi.2013.28.issue-3/dmdi-2
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http://dx.doi.org/10.1515/dmdi-2013-0014DOI Listing
March 2014
6 Reads

Utility of a column-switching LC/MS/MS method in cytochrome P450 inhibition assays using human liver microsomes.

Drug Metabol Drug Interact 2013 ;28(3):177-85

Background: Liquid chromatography-tandem mass spectrometry (LC/MS/MS)-based in vitro cytochrome P450 (CYP) inhibition assays in pooled human liver microsomes using therapeutically relevant probe drugs are recommended by the US Food and Drug Administration to assess the potential for drug-drug interactions. As these assays are used routinely in pharmaceutical drug discovery screening of new chemical entities for drug interaction liabilities, there is a need to have higher analytical throughput. Column-switching methods may offer increased chromatographic throughput while maintaining the quality of data generated. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0004DOI Listing
March 2014
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Ospemifene metabolism in humans in vitro and in vivo: metabolite identification, quantitation, and CYP assignment of major hydroxylations.

Drug Metabol Drug Interact 2013 ;28(3):153-61

Background: The metabolism of ospemifene, a novel nonsteroidal selective estrogen receptor modulator, was investigated as part of its development.

Methods: Metabolite identification, tentative quantitation, and CYP assignment of ospemifene were performed in human liver microsomes or homogenate incubations and in plasma samples from volunteer humans. The potential contributions of CYP enzymes were determined by recombinant human CYPs. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0016DOI Listing
March 2014
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An update on the constitutive androstane receptor (CAR).

Drug Metabol Drug Interact 2013 ;28(2):79-93

School of Pharmacy, Faculty of Health Sciences and Biocenter Kuopio, University of Eastern Finland, PO Box 1627, FI-70211 Kuopio, Finland.

The constitutive androstane receptor (CAR; NR1I3) has emerged as one of the main drug- and xenobiotic-sensitive transcriptional regulators. It has a major effect on the expression of several oxidative and conjugative enzymes and transporters, and hence, CAR can contribute to drug/drug interactions. Novel functions for CAR are also emerging: it is able to modulate the metabolic fate of glucose, lipids, and bile acids, and it is also involved in cell-cell communication, regulation of the cell cycle, and chemical carcinogenesis. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0009DOI Listing
September 2013
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Silibinin hemisuccinate binding to proteins in plasma and blood cell/plasma partitioning in mouse, rat, dog and man in vitro.

Drug Metabol Drug Interact 2013 ;28(2):115-22

R&D Division, Rottapharm | Madaus, Via Valosa di Sopra 9, 20900 Monza, Italy.

Background: The determination of plasma protein binding and blood cell/plasma partitioning is important when prescribing silibinin hemisuccinate to patients concomitantly receiving other drugs and to estimate the safety margins of exposure at the no observed adverse events levels determined from toxicity studies conducted in rats and dogs.

Methods: Protein binding of [3'-14C]silibinin hemisuccinate (1, 10, 100, 1000 and 4000 μM) was evaluated in human, dog, rat and mouse plasma by ultrafiltration. Blood cell/plasma partitioning in all these species was also determined. Read More

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http://dx.doi.org/10.1515/dmdi-2013-0013DOI Listing
September 2013
18 Reads