Plasma levels and protein binding of phenytoin during exercise in man: the effect of elevated free fatty acids.

Abstract:

:Five healthy subjects performed submaximal physical exercise approximately 20 h after a single oral dose of phenytoin (5 mg/kg of the sodium salt). The plasma levels of free fatty acids (FFA) increased 2- to 3-fold in the post-exercise period. In spite of this, the degree of plasma binding of phenytoin and its total concentration in plasma were unaffected. Thus FFA at the levels reached (1.5-2.9 mEq/l), did not displace phenytoin from its binding sites on albumin. Furthermore, during the FFA peak the plasma protein binding of warfarin, as measured in vitro, did not decrease as compared to the pre-exercise period. These findings contrast to previous observations in rats and dogs, where FFA caused a considerable displacement of warfarin and phenytoin at relatively low FFA/albumin molar ratios.

journal_name

Pharmacology

journal_title

Pharmacology

authors

Borgå O,Juhlin-Dannfeldt A,Dahlqvist R

doi

10.1159/000136744

subject

Has Abstract

pub_date

1978-01-01 00:00:00

pages

37-43

issue

1

eissn

0031-7012

issn

1423-0313

journal_volume

16

pub_type

杂志文章
  • Effects of nitroglycerin, dipyridamole, nifedipine, verapamil and diltiazem on canine coronary arterial rings contracted with 5-hydroxytryptamine and anoxia.

    abstract::Anoxia has been shown to potentiate the constrictor effects of 5-hydroxytryptamine (5HT) in isolated vascular tissue. In the present study, canine coronary arterial rings were incubated with various treatments and exposed to 5HT (4 X 10(-7) M) and anoxia (95% N2 and 5% CO2). Developed tension was increased by 250 +/- ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138211

    authors: Barrett JA,DePaul Lynch V,Balkon J,Smith RD,Wolf PS

    更新日期:1986-01-01 00:00:00

  • Effect of thiamin deprivation on the in vitro metabolic activation of benzo(a)pyrene.

    abstract::Feeding a thiamin-deficient diet to male and female rats for 3 weeks alters the mixed function oxidases responsible for metabolizing benzo(a)pyrene and enhances the response of these enzymes to induction by phenobarbital or 3-methylcholanthrene. The caloric restriction observed in thiamin deprivation may be partially ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138004

    authors: Wade AE,Bunce OR,Harley W,Baker MT,Holmes D

    更新日期:1984-01-01 00:00:00

  • Effects of adrenoceptor agonists and antagonists on cardiovascular functional parameters in rats.

    abstract::The effects of intravenous administration of adrenoceptor agonists and antagonists on electrocardiographic or blood pressure (BP) functional parameters were assessed in urethane-anesthetized rats. The responses of cardiovascular functional parameters produced by these drugs included: (1) isoproterenol decreased the du...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138922

    authors: Young MS,Lin KW,Lin MT

    更新日期:1992-01-01 00:00:00

  • Effect of stobadine on leukocyte free radical generation in streptozotocin-diabetic rats: comparison with vitamin E.

    abstract::We investigated a possible alteration in the ability of leukocytes to produce reactive oxygen species by stobadine, a pyridoindole antioxidant, in streptozotocin-diabetic rats. The production of free radicals from whole blood was assessed by luminol-enhanced chemiluminescence after stimulation by phorbol myristate ace...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000074236

    authors: Demiryürek AT,Karasu C,Stefek M,Stolc S

    更新日期:2004-01-01 00:00:00

  • Effects of paired analogs of angiotensin II and angiotensin III on rat smooth muscle.

    abstract::The effects of several paired analogs of angiotensin II and angiotensin III, designed as antagonists, have been compared in isolated smooth muscle (rat uterus) and by in vivo rat blood pressure assay. These analogs were (1) the angiotensin II series: (1-sarcosine, 7-X, 8-isoleucine-) angiotensin II, and (2) the angiot...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137342

    authors: Moore GJ,Ko EM

    更新日期:1980-01-01 00:00:00

  • The Alcohol Intolerance Produced by Isoniazid Is Not Due to a Disulfiram-Like Reaction Despite Aldehyde Dehydrogenase Inhibition.

    abstract:BACKGROUND/AIMS:Isoniazid (ISO) has been reported to inhibit the hepatic aldehyde dehydrogenase (ALDH) and to cause a disulfiram (DIS)-like reaction, albeit there are no reports demonstrating increased blood acetaldehyde levels after co-administration of ISO with alcohol. The aim of our study was to clarify whether the...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000448759

    authors: Karamanakos PN,Pappas P,Boumba V,Vougiouklakis T,Marselos M

    更新日期:2016-01-01 00:00:00

  • Stimulation of glucose release of the rat kidney in vivo by epinephrine and isoprenaline.

    abstract::In anesthetized rats the glucose release of the kidneys was estimated from the glucose concentrations in the arterial and renal venous plasma, urinary glucose excretion and the total renal plasma flow. Net renal glucose release was found in control experiments. The glucose release of the kidneys decreased with rising ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136914

    authors: Greven J,van Eys B,Jacobs W

    更新日期:1975-01-01 00:00:00

  • Increased nitric oxide accounts for decreased basal vascular tone and responsiveness in the resistance vessels of high-cholesterol-fed rabbits.

    abstract::The objective of this study was to determine the effects of hypercholesterolemia on basal vascular tone and vascular responses to pharmacologic agents in hindquarter resistance vessels. Blood pressure and hindquarter blood flow were measured in conscious rabbits fed a high cholesterol diet (1%) for 17 weeks (HC) compa...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000056137

    authors: Fitch R,Da Cunha V,Kauser K,Dole W,Parkinson J,Vergona R,Sullivan ME,Wang YX

    更新日期:2001-01-01 00:00:00

  • Self-administration of both ethanol and nicotine in rats.

    abstract::Self-administration of either nicotine (NIC) or ethanol (ETH) has been extensively studied. This study addressed for the first time the self-administration of both substances when offered together. Male and female rats of different ages were offered NIC and ETH using the two- or three-bottle free-choice method. When N...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000067801

    authors: Marshall CE,Dadmarz M,Hofford JM,Gottheil E,Vogel WH

    更新日期:2003-03-01 00:00:00

  • Accumulation of norepinephrine (NE) by rat organs in vivo.

    abstract::In anesthetized rats intravenously infused, norepinephrine (NE) was accumulated by the heart, the spleen and the lung in a dose-related manner. With the lower dose of NE (2.5 mg/kg) the organ/blood ratios were more than unity and were generally greater than with higher doses (5 and 10 mg/kg), indicating that accumulat...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136926

    authors: Sivaramakrishna N,Gulati OD

    更新日期:1975-01-01 00:00:00

  • Carnitine action on neuromuscular disturbances in the fasting rat: potentiation by L-lysine.

    abstract::L-Carnitine (oral route) significantly corrects the muscle hypocontractility and hypoexcitability induced in the rat after 5 consecutive days of fasting. This effect is interpreted on the basis of the dual role of L-carnitine as cofactor in the transport of long-chain fatty acids into the mitochondria and as a detoxif...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139026

    authors: Pierrefiche G,Reynier M,Laborit H

    更新日期:1993-01-01 00:00:00

  • Elimination of organic anions in response to an early stage of renal ischemia-reperfusion in the rat: role of basolateral plasma membrane transporters and cortical renal blood flow.

    abstract:BACKGROUND/AIMS:The knowledge of molecular mechanisms determining drug pharmacokinetics in pathological states is relevant for the development of new therapeutic approaches. This study was undertaken to evaluate the cortical renal blood flow (cRBF) and the renal protein expression of the organic anion transporters (OAT...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000110555

    authors: Di Giusto G,Anzai N,Endou H,Torres AM

    更新日期:2008-01-01 00:00:00

  • Alteration of cyclopiazonic acid-mediated contracture of mouse diaphragm after denervation.

    abstract::As a major Ca(2+) source for muscle contraction, the sarcoplasmic reticulum (SR) of skeletal muscle maintains its Ca(2+) content by uptake of myoplasmic Ca(2+) and by replenishment with extracellular Ca(2+). Since transection of motor nerve alters the functions of SR Ca(2+) pump and sarcolemma ion channels, this study...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000082755

    authors: Hong SJ,Liang HC,Shen CJ

    更新日期:2005-03-01 00:00:00

  • Delta-sleep-inducing peptide potentiates anticonvulsive activity of valproate against metaphit-provoked audiogenic seizure in rats.

    abstract::The effect of delta-sleep-inducing peptide (DSIP) on the anticonvulsive activity of a nonprotective valproate (VPA) dose in a metaphit model of generalized, reflex audiogenic seizures in adult Wistar rats was studied. The animals that received metaphit (10 mg/kg) were exposed to audiogenic stimulation (100 +/- 3 dB, 6...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000093001

    authors: Hrncić D,Stanojlović O,Zivanović D,Susić V

    更新日期:2006-01-01 00:00:00

  • Dexamethasone upregulates Nox1 expression in vascular smooth muscle cells.

    abstract:BACKGROUND/AIM:It has been demonstrated that dexamethasone-induced hypertension can be prevented by the NADPH oxidase inhibitor apocynin. The effect of dexamethasone on NADPH oxidase, however, is unknown. The present study was conducted to investigate the effect of dexamethasone on the gene expression of Nox1, the majo...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000365932

    authors: Siuda D,Tobias S,Rus A,Xia N,Förstermann U,Li H

    更新日期:2014-01-01 00:00:00

  • Study of the vasodilating activity of salbutamol on dog coronary arteries. Unexpected effects of methylene blue.

    abstract::The vascular relaxant effect of salbutamol and its dependence on the endothelium were studied in the isolated dog coronary artery, precontracted with prostaglandin F2 alpha. Salbutamol induced a concentration-dependent relaxation which was partially inhibited by removal of endothelial cells. Atenolol 10(-6) mol/l, a b...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138804

    authors: Bernard F,Jouquey S,Hamon G

    更新日期:1991-01-01 00:00:00

  • Effect of interleukin 6 on the hepatic metabolism of itraconazole and its metabolite hydroxyitraconazole using primary human hepatocytes.

    abstract::A potential cytokine-drug interaction between interleukin 6 (IL-6) and itraconazole (ITZ) was studied using human hepatocytes in primary culture. Cultures from 5 adult males (mean age 42 +/- 15 years) who had not received any medicines known to interact with CYP3A4 were studied. Cultures were exposed to ITZ 500 ng/ml,...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000068401

    authors: Gubbins PO,Melchert RB,McConnell SA,Franks AM,Penzak SR,Gurley BJ

    更新日期:2003-04-01 00:00:00

  • Evaluation of pharmacological profile of meloxicam as an anti-inflammatory agent, with particular reference to its relative selectivity for cyclooxygenase-2 over cyclooxygenase-1.

    abstract::We studied the anti-inflammatory activity of meloxicam on rat carrageenin-induced pleurisy and its toxicity for rat gastric mucosa, relative to its in vitro inhibitory potency against partially purified cyclooxygenase (COX)-1 and COX-2 preparations in order to clarify the pharmacological profile of the compound as an ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139511

    authors: Ogino K,Hatanaka K,Kawamura M,Katori M,Harada Y

    更新日期:1997-07-01 00:00:00

  • Cardioprotective actions of ascorbic acid during isoproterenol-induced acute myocardial infarction in rats.

    abstract:BACKGROUND/AIMS:In the present study, we tested whether or not acute antioxidant treatment with vitamin C is able to protect the heart during myocardial infarction. The effects of vitamin C on the autonomic balancing of the heart and on the histopathological and immunohistochemical changes in response to isoproterenol ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000222245

    authors: Buttros JB,Bergamaschi CT,Ribeiro DA,Fracalossi AC,Campos RR

    更新日期:2009-01-01 00:00:00

  • Effects of Polybrominated Diphenyl Ethers on Rat and Human 11β-Hydroxysteroid Dehydrogenase 1 and 2 Activities.

    abstract::Polybrominated diphenyl ethers (PBDEs) are a class of brominated flame retardants. PBDEs have been widely used in textiles, flexible polyurethane foams, electronic components, electrical components, and plastics. 11β-Hydroxysteroid dehydrogenases, isoform 1 (HSD11B1) and isoform 2 (HSD11B2), have been demonstrated to ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000445213

    authors: Chen X,Dong Y,Cao S,Li X,Wang Z,Chen R,Ge RS

    更新日期:2016-01-01 00:00:00

  • One-year treatment with rosuvastatin reduces intima-media thickness in 45 hypercholesterolemic subjects with asymptomatic carotid artery disease.

    abstract:AIM:An increase in carotid intima-media thickness (CIMT) represents an early phase of the atherosclerotic process. The aim of our study was to evaluate whether a reduction in CIMT could be seen with 1-year treatment with rosuvastatin (10 mg/day). METHODS AND RESULTS:Forty-five patients with hypercholesterolemia and as...

    journal_title:Pharmacology

    pub_type: 杂志文章,随机对照试验

    doi:10.1159/000276476

    authors: Riccioni G,Vitulano N,Mancini B,Zanasi A,D'Orazio N

    更新日期:2010-01-01 00:00:00

  • Effects of delta9-THC on the synaptosomal uptake of 3H-tryptophan and 3H-choline.

    abstract::The in vitro addition of (-)-delta9-tetrahydrocannabinol (delta9-THC) resulted in a dose-responsive inhibition of the high-affinity specific synaptosomal uptake of both 3H-tryptophan and 3H-choline in mouse forebrain crude synaptosomal preparations. The approximate concentrations of delta9-THC required to cause a 50% ...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000136839

    authors: Johnson KM,Dewey WL

    更新日期:1978-01-01 00:00:00

  • Ca2+-induced inhibition of adenylyl cyclase in turkey erythrocyte membranes.

    abstract::We investigated the effects of calcium ions (Ca2+) on the adenylyl cyclase activity in purified turkey erythrocyte membranes. Results showed the following: (i) Ca2+ inhibits cAMP accumulation stimulated by isoproterenol (1 micromol/l), NaF + AlCl3 (10 mmol/l + 20 micromol/l) or forskolin (10 micromol/l) in EGTA-washed...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000028245

    authors: Demirel E,Ugur O,Onaran HO

    更新日期:1998-10-01 00:00:00

  • Quantitative analysis of the electrocorticogram after forebrain ischemia in the rat.

    abstract::The purpose of the study was to test the hypothesis that the postischemic neuronal damage is accompanied by changes of the electrocorticogram (ECoG) of freely moving rats during long-term recovery after forebrain ischemia. Ten minutes forebrain ischemia was induced in male Wistar rats. ECoG was recorded 1 day before a...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000139287

    authors: Peruche B,Klaassens H,Krieglstein J

    更新日期:1995-04-01 00:00:00

  • Effects of L-dopa-induced dopamine accumulation on 45Ca2+ efflux and insulin secretion in isolated rat islets.

    abstract::It has previously been demonstrated in several species that the secretory granules of pancreatic beta-cells have the ability to store substantial amounts of calcium and bioactive amines, such as dopamine and serotonin. Furthermore, evidence for a similar topographical localization for amine and calcium within the peri...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000138053

    authors: Ahrén B,Lundquist I

    更新日期:1985-01-01 00:00:00

  • Effects of peptides and amines on isolated guinea pig tracheae as influenced by inhibitors of the metabolism of arachidonic acid.

    abstract::Stimulants (histamine, acetylcholine and substance P) and relaxants (isoprenaline and bradykinin) of the guinea pig trachea were tested in the absence and presence of mepacrine, eicosatetraynoic acid, BW 755C and indomethacin in order to evaluate the involvement of prostaglandins and congeners in the effects of amines...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000137758

    authors: Mizrahi J,D'Orléans-Juste P,Caranikas S,Regoli D

    更新日期:1982-01-01 00:00:00

  • Attitudes and opinion about adverse drug events of women living in a city of south Italy.

    abstract:BACKGROUND/AIM:Perception of risk of adverse drug events (ADEs) is different between health and nonhealth professionals, but these differences have not been investigated sufficiently in the general population. Women are more affected by ADEs. With the aim to investigate ADE risk perception in a sample of nonhealth prof...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000346737

    authors: Salvo F,Miroddi M,Alibrandi A,Calapai F,Cafeo V,Mancari F,Gangemi S,Caputi AP,Calapai G

    更新日期:2013-01-01 00:00:00

  • Melatonin Induces Osteoblastic Differentiation of Mesenchymal Stem Cells and Promotes Fracture Healing in a Rat Model of Femoral Fracture via Neuropeptide Y/Neuropeptide Y Receptor Y1 Signaling.

    abstract::The function of melatonin (MLT) in promoting fracture healing has been demonstrated in previous studies. However, the molecular mechanism underlying therapeutic effects of MLT is not entirely clear. In this study, mesenchymal stem cells (MSCs) were isolated from rat bone marrow and identified by flow cytometry. We fou...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000492576

    authors: Dong P,Gu X,Zhu G,Li M,Ma B,Zi Y

    更新日期:2018-01-01 00:00:00

  • Superoxide anion stress attenuates the contractile response of the Guinea pig vas deferens to ATP and diadenosine tetraphosphate. Possible effect on calcium dysregulation.

    abstract::Induction of endogenous superoxide anion stress by the use of the superoxide dismutase inhibitor diethylthiocarbamate (DETCA; 10 mmol/l) produced a potent inhibition of the ATP (0.3-10 mmol/l) and diadenosine tetraphosphate (AP(4)A) contractile activity in the isolated vas deferens by 29-92 and 24-90%, respectively. P...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000148260

    authors: Al-Rawi MB,Aleisa AM,Khattab MM

    更新日期:2008-01-01 00:00:00

  • Anti-inflammatory activity of thymol: inhibitory effect on the release of human neutrophil elastase.

    abstract::Elastase, a serine proteinase released by activated human neutrophils, can degrade a wide variety of biomacromolecules including elastin, and is considered a marker of inflammatory diseases. As the logical strategy to protect tissue is to inhibit excessive elastase activity, experimental and clinical researches have c...

    journal_title:Pharmacology

    pub_type: 杂志文章

    doi:10.1159/000093790

    authors: Braga PC,Dal Sasso M,Culici M,Bianchi T,Bordoni L,Marabini L

    更新日期:2006-01-01 00:00:00