Search results for "drugs."
showing 10 items of 733 documents
Potential transbuccal delivery of l-DOPA methylester prodrug: stability in the environment of the oral cavity and ability to cross the mucosal tissue
2016
Levodopa (l-DOPA) is the most effective pharmacologic agent in Parkinson's disease and remains the "gold standard". Nevertheless, in long-term treatments, dyskinesias and motor complications can emerge. In this work, the combined use of l-DOPA methylester hydrochloride prodrug (LDME) with transbuccal drug delivery was supposed as a good alternative method to optimize the bioavailability of l-DOPA, to maintain constant plasma levels and to decrease the drug unwanted effects. The effects of environmental pH on buccal delivery of LDME were evaluated ex vivo. The increase of pH value from 5.8 to 6.2 implies an improvement of drug permeation. Since the pH increase causes the raising of hydrolyti…
The zebrafish embryo as an in vivo model for screening nanoparticle-formulated lipophilic anti-tuberculosis compounds.
2021
ABSTRACT With the increasing emergence of drug-resistant Mycobacterium tuberculosis strains, new and effective antibiotics against tuberculosis (TB) are urgently needed. However, the high frequency of poorly water-soluble compounds among hits in high-throughput drug screening campaigns is a major obstacle in drug discovery. Moreover, in vivo testing using conventional animal TB models, such as mice, is time consuming and costly, and represents a major bottleneck in lead compound discovery and development. Here, we report the use of the zebrafish embryo TB model for evaluating the in vivo toxicity and efficacy of five poorly water-soluble nitronaphthofuran derivatives, which were recently id…
Gender difference in drug use in hospitalized elderly patients.
2015
Purpose The aims of this study were to evaluate whether or not there are gender differences in drug use at hospital admission and prescription at discharge and to evaluate the effect of hospitalization on medication patterns in the elderly. Method In-patients aged > 65 years included in the REPOSI registry during a recruitment period of 3 years (2008-2010-2012) were analyzed in order to evaluate drug use at hospital admission and prescription at discharge according to gender. Results A total of 3473 patients, 52% women and 48% men, were considered. Polypharmacy (> 5 drugs) is more frequent in men both at hospital admission and discharge. At hospital discharge, the number of prescripti…
Effects of Some Directly-Acting Smooth Muscle Relaxant Drugs on Isolated Human Preparations of the Upper Urinary Tract
1985
It is generally assumed that drugs which induce relaxation of smooth muscles may be of clinical importance in some urological disorders; such drugs are indeed widely used, for example in the therapy of unstable bladders or to facilitate the passage of ureteral stones. Antispasmodic action may be classified in neurotropic and musculo-tropic action; the former acting on the autonomic nervous system and the latter directly on smooth muscle cells. Examples for the first type of action are anticholinergic drugs or alpha-adrenoceptor-antagonists, whereas papaverine is a classic drug with the second type of action.
Selected cytotoxic gold compounds cause significant inhibition of 20S proteasome catalytic activities
2014
Abstract Six structurally diverse cytotoxic gold compounds are reported to cause profound and differential inhibition of the three main catalytic activities of purified 20S proteasome whilst auranofin , an established gold(I) drug in clinical use, is nearly ineffective. In particular, the gold(I) complex [( pbiH ) Au ( PPh 3 )] PF 6 , turns out to be the most potent inhibitor of all three enzyme activities with sub-micromolar IC 50 values. The present results further support the view that proteasome inhibition may play a major – yet not exclusive – role in the cytotoxic actions of gold based anticancer agents.
Perspiration versus saliva--basic aspects concerning their use in roadside drug testing.
1999
Various aspects concerning the practical application and forensic interpretation of data obtained by saliva drug testing and drug monitoring from the skin surface are discussed. Basic information on the composition of saliva and skin secretions and their particular transport mechanisms, as far as known, are given. For drugs of abuse secretion into saliva is suggested to be by passive diffusion and to depend on lipid solubility, pKa, plasma protein binding and on the pH of saliva. Drug molecules from blood are considered to reach the skin surface by various routes such as by sweat and sebum as well as by inter- and/or transcellular diffusion. The role of the stratum corneum as a temporary dr…
Triplet stabilization for enhanced drug photorelease from sunscreen-based photocages
2021
[EN] Recently, sunscreen-based drug photocages have been introduced to provide UV protection to photoactive drugs, thus increasing their photosafety. Here, combined experimental and theoretical studies performed on a photocage based on the commercial UVA filter avobenzone (AB) and on the photosensitizing non-steroidal anti-inflammatory drug ketoprofen (KP) are presented unveiling the photophysical processes responsible for the light-triggered release. Particular attention is paid to solvent stabilization of the drug and UV filter excited states, respectively, which leads to a switching between the triplet excited state energies of the AB and KP units. Most notably, we show that the stabiliz…
Influence of Chemical Enhancers and Iontophoresis on the In Vitro Transdermal Permeation of Propranolol: Evaluation by Dermatopharmacokinetics
2018
[EN] The aims of this study were to assess, in vitro, the possibility of administering propranolol transdermally and to evaluate the usefulness of the dermatopharmacokinetic (DPK) method in assessing the transport of drugs through stratum corneum, using propranolol as a model compound. Four chemical enhancers (decenoic and oleic acid, laurocapram, and R-(+)-limonene) and iontophoresis at two current densities, 0.25 and 0.5 mA/cm(2) were tested. R-(+)-limonene, and iontophoresis at 0.5 mA/cm(2) were proven to be the most efficient in increasing propranolol transdermal flux, both doubled the original propranolol transdermal flux. Iontophoresis was demonstrated to be superior than the chemical…
Calixarene: A Versatile Material for Drug Design and Applications
2016
The therapy of various diseases by the drugs entrapped in calixarene derivatives is gaining attraction of researchers nowadays. Calixarenes are macrocyclic nano-baskets which belong to cavitands class of host-guest chemistry. They are the marvelous hosts with distinct hydrophobic three dimensional cavities to entrap and encapsulate biologically active guest drugs. Calixarene and its derivatives develop inclusion complexes with various types of drugs and vitamins for their sustained/targeted release. Calixarene and its derivatives are used as carriers for anti-cancer, anti-convulsant, anti-hypertensive, anthelmentic, anti-inflammatory, antimicrobial and antipsychotic drugs. They are the impo…
Patterns and trends in scientific research on generic drugs
2016
[Purpose]: The purpose of this study to investigate the evolution and current status of peer-reviewed publications concerning generic drugs during the past few decades. [Methods]: Scientific articles about generic drugs published until 2012 were retrieved through the PubMed/MEDLINE database, and a content analysis was performed. [Findings]: Our study revealed an increasing number of publications on generics since 1984. Statins, antiretroviral therapies, and antiepileptics, followed by immunosuppressants and antithrombotic agents, were the most common therapeutic drug categories. [Implications]: Almost 60% of the generics detailed in studies indexed in MEDLINE were acting on the cardiovascul…