Mechanistic insights of the controlled release capacity of polar functional group in transdermal drug delivery system: the relationship of hydrogen bonding strength and controlled release capacity
This study concluded that drugs with strong hydrogen bond forming ability and high skin permeation were suitable to use amide pressure sensitive adhesives to regulate their release rate from patch. The conclusion was further confirmed by in vivo pharmacokinetic study. (Source: Acta Pharmaceutica Sinica B)
Source: Acta Pharmaceutica Sinica B - November 30, 2019 Category: Cancer & Oncology Source Type: research
SPPARM alpha: the Lazarus effect
Purpose of review
Atherogenic dyslipidaemia, characterized by high plasma triglycerides (a surrogate for triglyceride-rich remnant lipoproteins) and low high-density lipoprotein cholesterol (HDL-C), is prevalent in patients with type 2 diabetes mellitus (T2DM) and contributes to a high modifiable residual cardiovascular risk. Fibrates are effective in managing hypertriglyceridaemia but lack consistent cardiovascular benefit in clinical trials and exhibit pharmacokinetic interaction with statins (gemfibrozil) and renal and hepatic safety issues (fenofibrate). The selective peroxisome proliferator-activated receptor alpha ...
Source: Current Opinion in Lipidology - November 5, 2019 Category: Lipidology Tags: THERAPY AND CLINICAL TRIALS: Edited by Erik S.G. Stroes and Gerald F. Watts Source Type: research
Activation of Peroxisome Proliferator-Activated Receptor- α Increases the Expression of Nuclear Receptor Related 1 Protein (Nurr1) in Dopaminergic Neurons
This study underlines the importance of peroxisome proliferator-activated receptor (PPAR)α in controlling the transcription ofNurr1. Our mRNA analyses followed by different immunoassays clearly indicated that PPAR α agonist gemfibrozil strongly upregulated the expression of Nurr1 in wild-type, but not PPARα−/−, DA neurons. Moreover, identification of conserved PPRE in the promoter ofNurr1 gene followed by chromatin immunoprecipitation analysis, PPRE luciferase assay, and manipulation ofNurr1 gene by viral transduction of different PPAR α plasmids confirmed that PPARα was indeed involved in the expression of Nurr1....
Source: Molecular Neurobiology - October 26, 2019 Category: Neurology Source Type: research
Metal organic framework composite, nano-Fe3O4@Fe-(benzene-1,3,5-tricarboxylic acid), for solid phase extraction of blood lipid regulators from water.
Abstract
The magnetic metal-organic framework Fe3O4@(Fe-(benzene-1,3,5-tricarboxylic acid) (MMOF) was prepared, characterized and studied as a magnetic sorbent for the dispersive solid-phase extraction (DSPE) of several widely used blood lipid regulators (i.e., bezafibrate, clofibric acid, clofibrate, gemfibrozil and fenofibrate) from water samples. Characterization of the synthesized Fe3O4@Fe-BTC magnetic nanomaterial was performed by Fourier transform infrared spectroscopy, powder X-ray diffractometry, thermogravimetric analysis, scanning electron microscopy and transmission electron microscopy. The magn...
Source: Talanta - October 10, 2019 Category: Chemistry Authors: Peña-Méndez EM, Mawale RM, Conde-González JE, Socas-Rodríguez B, Havel J, Ruiz-Pérez C Tags: Talanta Source Type: research
Linking microbial diversity and population dynamics to the removal efficiency of pharmaceutically active compounds (PhACs) in an anaerobic/anoxic/aerobic (A2O) system.
Abstract
The removal efficiencies (REs) of nineteen pharmaceutically active compounds (PhACs) (six antibiotics-clarithromycin, ofloxacin, sulfadiazine, sulfamethazine, sulfamethoxazole and trimethoprim -, four β-blockers -atenolol, metoprolol, propranolol and sotalol-, two antihypertensives/diuretics -furosemide and hydrochlorothiazide-, three lipid regulators -bezafibrate, fenofibrate and gemfibrozil-, and four psychiatric medications -carbamazepine, diazepam, lorazepam and paroxetine) were ascertained in a pilot-scale anaerobic/anoxic/aerobic (A2O) system treating urban wastewater, long term operated du...
Source: Chemosphere - September 20, 2019 Category: Chemistry Authors: Gallardo-Altamirano MJ, Maza-Márquez P, Montemurro N, Rodelas B, Osorio F, Pozo C Tags: Chemosphere Source Type: research
Tendon rupture associated with concomitant simvastatin and gemfibrozil use: Biological and pharmacokinetic implications
Tendon or muscle rupture is a rare complication of statins that could potentially be disabling and result in a significant burden to patients. The co ‐administration of statin and gemfibrozil should warrant prescribers’ awareness of tendon‐related complications of statin use, particularly in high‐risk populations with poor renal function or musculoskeletal comorbidities. AbstractTendon or muscle rupture is a rare complication of statins that could potentially be disabling and result in a significant burden to patients. The co ‐administration of statin and gemfibrozil should warrant prescribers’ awareness of ten...
Source: Clinical Case Reports - August 27, 2019 Category: General Medicine Authors: Edison Jose Cano Cevallos,
Danial Haris Shaikh,
Jose Gonzalez,
William Sanchez,
Madanmohan Patel Tags: CASE REPORT Source Type: research
Occurrence and spatial distribution of statins, fibrates and their metabolites in aquatic environments
This study focuses on the quantification of the levels of statins, fibrates and their metabolites in the aquatic environments using Ultra-High Performance Liquid Chromatography coupled to high resolution quadrupole time-of-flight mass spectrometry (UHPLC-QTOF-MS). The developed UHPLC–QTOF–MS based method was successfully applied to the analysis of statins, fibrates and metabolites in real water samples collected from Daspoort WWWs influent and effluent and Apies River. A series of statin compounds (mevastatin, simvastatin, pravastatin, rosuvastatin, fluvastatin, atorvastatin), fibrates (gemfibrozil, fenofibrate) and th...
Source: Arabian Journal of Chemistry - August 25, 2019 Category: Chemistry Source Type: research
Modelling of emerging contaminant removal during heterogeneous catalytic ozonation using chemical kinetic approaches
This study evaluated the prediction of emerging contaminant (EC) removal during heterogeneous catalytic ozonation by chemical kinetic models. Six ECs with differing ozone reactivity were spiked in a synthetic water and a groundwater, then treated by conventional ozonation and heterogeneous catalytic ozonation with α- or β-MnO2 catalysts. Results show that catalysts did not considerably influence the removal of ECs with high and intermediate ozone reactivity (diclofenac, gemfibrozil, and bezafibrate), but enhanced the removal efficiencies of ECs with low ozone reactivity (2,4-dichlorophenoxyacetic acid, clofibric acid, an...
Source: Journal of Hazardous Materials - July 16, 2019 Category: Environmental Health Source Type: research
Effects of Strong CYP2C8 or CYP3A Inhibition and CYP3A Induction on the Pharmacokinetics of Brigatinib, an Oral Anaplastic Lymphoma Kinase Inhibitor, in Healthy Volunteers
AbstractIn vitro data support involvement of cytochrome P450 (CYP)2C8 and CYP3A4 in the metabolism of the anaplastic lymphoma kinase inhibitor brigatinib. A 3 ‐arm, open‐label, randomized, single‐dose, fixed‐sequence crossover study was conducted to characterize the effects of the strong inhibitors gemfibrozil (of CYP2C8) and itraconazole (of CYP3A) and the strong inducer rifampin (of CYP3A) on the single‐dose pharmacokinetics of brigatinib. Hea lthy subjects (n = 20 per arm) were administered a single dose of brigatinib (90 mg, arms 1 and 2; 180 mg, arm 3) alone in treatment period 1 and coadministered with ...
Source: Clinical Pharmacology in Drug Development - July 8, 2019 Category: Drugs & Pharmacology Authors: Meera Tugnait,
Neeraj Gupta,
Michael J. Hanley,
Daryl Sonnichsen,
David Kerstein,
David J. Dorer,
Karthik Venkatakrishnan,
Narayana Narasimhan Tags: Original Manuscript Source Type: research
Gemfibrozil May Decrease Norclozapine Elimination: A Case Report
No abstract available (Source: Journal of Clinical Psychopharmacology)
Source: Journal of Clinical Psychopharmacology - June 28, 2019 Category: Psychiatry Tags: Letters to the Editors — Case Reports Source Type: research
Physiologically Based Pharmacokinetic Models for Prediction of Complex CYP2C8 and OATP1B1 ( SLCO1B1 ) Drug –Drug–Gene Interactions: A Modeling Network of Gemfibrozil, Repaglinide, Pioglitazone, Rifampicin, Clarithromycin and Itraconazole
ConclusionsWhole-body PBPK models of gemfibrozil, repaglinide, and pioglitazone have been built and qualified for DDI and DGI prediction. PBPK modeling is applicable to investigate complex interactions between multiple drugs and genetic polymorphisms. (Source: Clinical Pharmacokinetics)
Source: Clinical Pharmacokinetics - May 24, 2019 Category: Drugs & Pharmacology Source Type: research
Simultaneous degradation of the pharmaceuticals gemfibrozil, hydrochlorothiazide and naproxen and toxicity changes during UV-C and UV-C/H2O2 processes in different aqueous matrixes
Publication date: Available online 17 May 2019Source: Journal of Environmental Chemical EngineeringAuthor(s): Cleiseano E.S. Paniagua, Ivo Amildon Ricardo, Eduardo O. Marson, Bárbara R. Gonçalves, Alam G. TrovóAbstractThe degradation of pharmaceuticals and toxicity changes in different aqueous matrixes treated by UV-C and UV-C/H2O2 were evaluated. No pH influence (4.0, 6.0 and 7.0) on the degradation of the target compounds was obtained in distilled water for any target compound. Hydrochlorothiazide was the most easily photodegraded followed by naproxen and gemfibrozil. The matrix composition strongly decreased the rate...
Source: Journal of Environmental Chemical Engineering - May 17, 2019 Category: Chemistry Source Type: research
A comprehensive review of the clinical utility of and a combined analysis of the clozapine/norclozapine ratio in therapeutic drug monitoring for adult patients.
This article comprehensively reviews the clinical utility of the serum clozapine/norclozapine (CLO/NCLO) ratio. Areas covered: Fifty-four published studies used this ratio (21 from a PubMed search from onset to 10/21/18 and 33 identified by the authors). To estimate a combined mean of the CLO/NCLO ratio in published studies, a PubMed search on 10/21/18 identified 422 articles leading to 19 included. The systematic review focused on: 1) the combined analysis, 2) CYP1A2 activity, 3) clinical response, 4) cognition, and 5) renal function. Expert opinion: Our combined analysis provided a weighted mean CLO/NCLO ratio of 1.73 in...
Source: Expert Review of Clinical Pharmacology - May 11, 2019 Category: Drugs & Pharmacology Tags: Expert Rev Clin Pharmacol Source Type: research
Parental Gemfibrozil Exposure Impacts Zebrafish F1 Offspring, But Not Subsequent Generations
Publication date: Available online 9 May 2019Source: Aquatic ToxicologyAuthor(s): Shamaila Fraz, Abigail H. Lee, Simon Pollard, Krishna Srinivasan, Abhilasha Vermani, Joanna Y. WilsonAbstractGemfibrozil (GEM) is a fibrate lipid regulator and one of the most commonly occurring fresh water pharmaceuticals. The negative effects of fibrates including GEM on fish reproduction have been frequently reported including effects of F0 GEM exposure on reproduction of the unexposed F1 offspring. We predicted that chronic, direct exposure of zebrafish with low concentrations of GEM would adversely affect parental male reproduction and u...
Source: Aquatic Toxicology - May 10, 2019 Category: Toxicology Source Type: research
