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At least 469 records · Page 26Linked to original sources
PubMed2003

Tenofovir disoproxil fumarate (Viread) for the treatment of HIV infection.

Tenofovir disoproxil fumarate (Viread) is the first nucleotide analog reverse transcriptase inhibitor to be approved by the Food and Drug Administration for the treatment of HIV infection. It is a potent agent with a long intracellular half-life that allows for once-daily dosing. It has been well-tolerated in clinical trials to date, without evidence of long term toxicity, including the mitochondrial toxicity that has been associated with some nucleoside analog reverse transcriptase inhibitors. Since its approval in October 2001, tenofovir disoproxil fumarate has quickly become a widely used component of antiretroviral regimens for both treatment-naive and -experienced patients.

Adenine↗
PubMed1998

Preparation and evaluation of erythromycin fumarate--a new derivative of erythromycin.

Erythromycin fumarate, a new water-soluble derivative of erythromycin, was prepared and its physicochemical and biological properties were evaluated. The derivative also has considerable solubility in organic solvents. Its partition coefficient data in different organic solvent-water systems may indicate that it is well-distributed in various tissues in vivo. Antimicrobial potency in vitro of the derivative, 725 micrograms/mg, is much higher than that of the existing derivatives and its antimicrobial spectrum is comparable to that of the parent antibiotic. The LD50 value of the new derivative in mice intraperitoneally is 402.7 mg/kg. Results of this and the previous investigation on pharmacokinetics and protein binding indicate that erythromycin fumarate has high potential for possible clinical application and further investigation may be undertaken.

Animals↗
PubMed2001

Evaluation of efficacy and safety of iron polymaltose complex and folic acid (Mumfer) vs iron formulation (ferrous fumarate) in female patients with anaemia.

Treatment of iron deficiency anaemia with conventional oral preparations is handicapped by unpredictable haematological response in addition to potential for irritating gastrointestinal adverse events. Iron polymaltose complex (IPC), a novel oral iron formulation with better absorbability, predictable haematinic response and less side effects was compared with oral ferrous fumarate in 100 female patients with documented iron deficiency anaemia. Clinical parameters (pallor, weakness) as well as biochemical parameters (Hb, serum iron, total iron binding capacity) show favourable changes with IPC; the physician and patient assessment also favour IPC over ferrous fumarate.

Adult↗
PubMed1992

Succinate-DCPIP and NADH-fumarate oxidoreductases in fresh water snails susceptible and non susceptible to schistosoma infection.

The activities of succinate-DCPIP oxidoreductase (SO) and NADH-fumarate oxidoreductase (FR) were determined in tissue homogenate of Biomphalaria alexandrina and Bulinus truncatus, the snail vectors of Schistosomiasia. A parallel study was done on Lymnea truncatula snails which are not susceptible to Schistosoma infection. The Michaelis constant (Km) and maximum velocities (Vmax) for fumarate reduction and succinate oxidation by the tissue homogenates from the three species were determined. The results obtained showed that both susceptible species are aerobic and lactate is the sole end product of anaerobic glycolysis. Lymnea truncatula snails are facultative anaerobic producing succinate as a major end product in the glycolytic pathway.

Animals↗
PubMed1990

Tissue selectivity of the novel calcium antagonist sesamodil fumarate in isolated smooth muscles and cardiac muscles.

The effects of the novel Ca2+ antagonist sesamodil fumarate (JAN), (+)-3,4-dihydro-2-[5-methoxy-2-[3-[N-methyl-N-[2-[(3,4- methylenedioxy)phenoxy]ethyl]amino]propoxy]phenyl]-4-methyl-3-oxo-2H- 1,4-benzothiazine hydrogen fumarate (SD-3211), on isolated smooth muscles and cardiac muscles were investigated and compared with those of diltiazem, verapamil, nifedipine and nicardipine. Ca2+ antagonistic activity of SD-3211 (pA2 = 8.42) was more potent than that of diltiazem and verapamil, but less potent than that of nifedipine and nicardipine in isolated pig coronary artery. The inhibition of Ca2(+)-induced contraction by SD-3211 was not reversed by drug washout, whereas that by diltiazem was easily reversed by drug washout. SD-3211 produced a concentration-dependent relaxation (EC50 = 5.7 x 10(-8) mol/l) of KCl-contracted pig coronary artery. The order of potency of the various compounds correlated with their respective Ca2+ antagonistic activities. SD-3211 antagonized KCl-induced contraction, but not that induced by A23187, in the rabbit aorta. On the other hand, negative inotropic and chronotropic effects of SD-3211 on the guinea pig right atria approximated those of diltiazem and verapamil. These results suggest that SD-3211 exerts a potent and long-lasting Ca2+ antagonistic effect on isolated arteries, possessing pharmacological properties diverse from those of known Ca2+ antagonists with respect to tissue selectivity, i.e., it is more vasoselective than diltiazem and verapamil, and more cardioselective than nifedipine and nicardipine.

Animals↗
PubMed1985

The high potential iron-sulfur center in Escherichia coli fumarate reductase is a three-iron cluster.

The fumarate reductase complex and soluble enzyme from Escherichia coli have been investigated by low temperature magnetic circular dichroism and electron paramagnetic resonance spectroscopies. The results confirm the presence of one [2Fe-2S] cluster and show that the high potential iron-sulfur center is a 3Fe cluster of the type found in bacterial ferredoxins. Since the 3Fe cluster is present in catalytically competent enzyme and does not appear to be involved in any type of cluster conversion under reducing conditions, we conclude that it is an intrinsic component of the functional enzyme. The significance of the results is discussed in relation to the published amino acid sequence and the iron-sulfur cluster composition of bacterial fumarate reductases.

Amino Acid Sequence↗
PubMed1982

A comparative trial of a controlled-release iron tablet preparation ('Ferrocontin' Continus) and ferrous fumarate tablets.

A single-blind, crossover comparative study was carried out in 40 patients with iron deficiency anaemia to assess the clinical efficacy and tolerance of once daily treatment with a controlled-release preparation of ferrous glycine sulphate ('Ferrocontin' Continus) and ferrous fumarate. Patients were allocated at random to receive 1 tablet (equivalent to 100 mg elemental iron) daily of one or other preparation for 4 weeks and were then crossed over to the alternative preparation for a further 4 weeks. The results showed that the significant increases in haemoglobin, packed cell volume and mean corpuscular volume were similar with both preparations. Seventeen patients reported gastro-intestinal side-effects on one or both preparations and the incidence was slightly less in patients whilst receiving the ferrous glycine sulphate preparation. In 3 patients, side-effects were sufficiently severe whilst taking ferrous fumarate to warrant interruption of treatment in 2 and withdrawal from the study in the other.

Adult↗
PubMed1980

Cardiovascular profile of mixidine fumarate, a compound which attenuates myocardial chronotropic responses.

The effect of mixidine fumarate on myocardial chronotropic responses to various stimulants was examined. Mixidine decreased elevated heart rate in the anesthetized dog to basal levels. It produced a dose-related decrease in heart rate elevated reflexly by aminophylline, by beta adrenergic stimulation induced by isoproterenol, by sympathetic nerve stimulation and by intravenous infusion of glucagon. Mixidine attenuated the increase in contractile force produced by sympathetic nerve stimulation but not that induced by isoproterenol. The compound antagonized the increase in rate of isolated guinea-pig atria induced by both isoproterenol and histamine. In the conscious dog, mixidine caused no decrease in resting heart rate, mean arterial pressure and cardiac output. It reduced atropine-induced sinus tachycardia as well as that induced by treadmill exercise. Experiments in the dog heart-lung preparation indicated that attenuation of an epinephrine-induced sinus tachycardia led to a decrease in myocardial oxygen consumption and an increase in myocardial efficiency. These studies suggest that mixidine fumarate induces an antichronotropic activity by a direct effect on the sinoatrial node and by attenuating sympathetic nervous system input to the heart.

Aminophylline↗
PubMed1993

Escherichia coli fumarate reductase frdC and frdD mutants. Identification of amino acid residues involved in catalytic activity with quinones.

Escherichia coli fumarate reductase (FRD) is a four-subunit enzyme that catalyzes the terminal step in anaerobic respiration to fumarate. The hydrophobic FrdC and FrdD subunits anchor the FrdA and FrdB catalytic subunits to the inner surface of the cytoplasmic membrane and are required for the enzyme to interact with quinones. Thirty-five single-site mutations were constructed in the FrdC and FrdD polypeptides by site-directed mutagenesis. Each mutant enzyme was characterized for its ability to catalyze quinone oxidation and reduction and to support growth of E. coli DW35 (delta frdABCD sdhC::kan) under selective conditions requiring functional enzyme. Replacement of FrdCE29 with Asp, Leu, Lys, or Phe had a deleterious effect both on quinol oxidase and quinone reductase activities. Substitution of FrdCH82 with Arg, Leu, Tyr, or Glu also decreased menaquinol oxidase activity, but had variable effects on the reverse reaction, the reduction of ubiquinone. Data are presented to support the hypothesis that the positive charge at FrdCH82 is required for stabilization of the quinone radical intermediate and the negative charge at FrdCE29 for deprotonation of menaquinol. Other critical amino acids identified in FrdC included Ala-32, Phe-38, Trp-86, Phe-87, and in FrdD residues Phe-57, Gln-59, Ser-60, and His-80. The established roles of such residues in the QA and QB sites of the photosynthetic reaction center would suggest a similar type of structure operative in the FRD complex. In such a model, Glu-29, Ala-32, His-82, Trp-86 of FrdC and His-80 of FrdD are considered participants in a QB-type site, and FrdD Phe-57, Gln-59, and Ser-60 components in an apolar QA-type site.

Amino Acid Sequence↗
PubMed1995

Effectiveness of disseminating culturally appropriate smoking-cessation information: Programa Latino Para Dejar de Fumar.

BACKGROUND: The need for a culturally appropriate smoking-cessation intervention for Latinos is based on data on current patterns of tobacco use, possible targeting by the tobacco industry, and the lack of smoking-cessation interventions that are appropriate to the cultural characteristics of Latino smokers. PURPOSE: Our goal was to evaluate the effectiveness of the Programa Latino Para Dejar de Fumar (PLDF) in disseminating smoking-cessation information in San Francisco's Latino community. METHODS: Annual cross-sectional telephone surveys were conducted from 1986 to 1993 of Latino adults, 18-65 years of age, living in census tracts with at least 10% Latinos. Surveys in 1986 and 1987 formed the base line for comparison of PLDF effects. RESULTS: Awareness of a Hispanic smoking-cessation program (odds ratio [OR] = 1.11; 95% confidence interval [CI] = 1.09-1.14), awareness of PLDF specifically (OR = 1.14; 95% CI = 1.10-1.17), awareness of available printed information to help smokers quit (OR = 1.09; 95% CI = 1.06-1.12), and having a copy of the Guía Para Dejar de Fumar (OR = 1.09; 95% CI = 1.05-1.14) were significantly associated with year of survey. In addition, those same variables were significantly associated with a lower acculturation score (respective ORs = 3.95, and 95% CI = 3.57-4.37; OR = 5.40, and 95% CI = 4.86-6.01; OR = 0.63, and 95% CI = 0.58-0.69; and OR = 4.54, and 95% CI = 3.89-5.30). Women were more likely than men to report awareness of a Hispanic smoking-cessation program (OR = 0.88; 95% CI = 0.81-0.96), awareness of PLDF (OR = 0.84; 95% CI = 0.77-0.92), and awareness of available printed information (OR = 0.78; 95% CI = 0.72-0.85). Cigarette-smoking prevalence decreased from 1986 through 1990, stabilized in 1991, and appeared to increase among all groups in 1993. Prevalence of smoking cessation remained stable overall, but it showed a steady increase among less acculturated respondents. CONCLUSION: We conclude that a culturally appropriate community intervention to promote nonsmoking can be successful at disseminating information about smoking cessation. Latino community norms about smoking are evolving, leading to decreased social acceptability.

Acculturation↗
PubMedDate not supplied

Erythematous bullous lesions on the dorsa of the hands due to contact exposure to ibutilide fumarate for injection.

While waiting to observe the response to ibutilide fumarate by a patient with atrial fibrillation, a nurse preparing the intravenous solution inadvertently spilled the drug on the hands of a medical resident. The resident immediately wiped his hands dry with disposable paper towels. Several hours later he sensed tingling and itching over the area, and the next day two erythematous bullous lesions were present on the dorsal surfaces of both hands. A single application of topical steroid was applied to the affected areas. The lesions were kept clean and dry, and healed completely in approximately 10 days. This is an unusual allergic reaction due to contact with ibutilide fumarate.

Adult↗
PubMed2006

Chemistry of Ru(eta6-1,3,5-cyclooctatriene)(eta2-dimethyl fumarate)2.

The chemistry of a novel zerovalent Ru complex, Ru(eta6-cot)(eta2-dmfm)2 (1) (cot=1,3,5-cyclooctatriene; dmfm=dimethyl fumarate), is reviewed with a focus on its reactivity toward phosphines, amines, and H2O, as well as arenes and p-quinones. A variety of novel zerovalent Ru complexes were synthesized from Ru(eta6-cot)(eta2-dmfm)2 (1), and it was shown that the complexes preferably bear both electron-donating and -accepting ligands simultaneously to exhibit thermodynamic stability. The first isolable zerovalent Ru aqua complexes were successfully prepared, and in these complexes, the generation of a chiral center on the O atom of the coordinated H2O was disclosed. In addition, the characteristic catalytic activity of 1 in organic synthesis was considered by reviewing recently developed novel reactions: (i) dimerization of 2,5-norbornadiene to pentacyclo[6.6.0.0(2,6).0(3,13).0(10,14)]tetradeca-4,11-diene (PCTD), (ii) intramolecular hydroamination of aminoalkynes to cyclic imines, (iii) formal [4+2] cycloaddition of alkynes with dmfm to trans-4-cyclohexene-1,2-dicarboxylates, and (iv) co-dimerization of dihydrofurans with alpha,beta-unsaturated esters to 2-alkylidenetetrahydrofurans. The products obtained here are expected to be used as novel functional organic monomers.

Catalysis↗
PubMed2001

[Granuloma annulare disseminatum: successful therapy with fumaric acid ester].

A 64-year old female patient was treated for a therapy-resistant generalized granuloma annulare with fumaric acid esters (Fumaderm initial). One week following begin of therapy with an initial dose of 30 mg per day, the papules had regressed significantly. A 6-week therapy with a final dose of 90 mg Fumaderm initial per day led to a nearly complete healing of the illness.

Dermatologic Agents↗
PubMed2005

Enhancement of antibacterial superoxide-anion generation in human monocytes by fumaric acid esters.

Fumaric acid esters (FAE) are used for the systemic therapy of psoriasis with high clinical efficacy. Among the potential side effects of FAE therapy, lymphocytopenia is sometimes observed. We have investigated the effect of dimethylfumarate (DMF) and its main metabolite methylhydrogenfumarate (MHF) as well as dexamethasone on superoxide anion generation by human monocytes and neutrophils after stimulation with bacteria (Staphylococcus aureus and Escherichia coli) and the yeast Candida albicans in addition with zymosan particles and with the tripeptide fMLP. Expression of mannose receptors on monocytes and neutrophils was also analyzed. The results showed that dexamethasone significantly inhibited superoxide anion generation from monocytes in response to bacteria and C. albicans, whereas DMF as well as MHF dose dependently increased the production of superoxide anion in monocytes in response to zymosan, fMLP and bacteria. Dexamethasone, DMF or MHF did not modulate superoxide anion generation of neutrophils. Expression of mannose receptors on monocytes was not regulated by DMF or MHF. Our data provide evidence that DMF and MHF do not alter the production of superoxide anions as an important mechanism of innate defense against microorganisms.

Candida albicans↗
PubMed1992

Fumaric acid overproduction in yeast mutants deficient in fumarase.

A nuclear mutant of Saccharomyces cerevisiae deficient in mitochondrial fumarase has been identified through the in vitro biochemical assay of enzyme activity after visual selection due to an increased acidification ability of its colonies. Cells of the fumarase-deficient mutant fermenting glucose accumulated extracellular fumaric acid. This accumulation was observed only in growing cultures and required functional mitochondrial electron transport from succinate dehydrogenase to oxygen.

Anaerobiosis↗
PubMed2001

Inhibition of Escherichia coli by dimethyl fumarate.

The antibacterial activity of dimethyl fumarate (DMF) and six other compounds against Escherichia coli (E. coli, K12) was investigated in culture media and compared. DMF was found to be more efficient than any other compound at the concentration of 200 ppm. The inhibitory activity of DMF against E. coli increased with increasing concentration of DMF. DMF also exhibited more obvious inhibition against E. coli at the initial growth phase than at other phases. The antibacterial ability of DMF showed low stability to heat processing but was less sensitive to pH values. Under conditions of restricted availability of oxygen, E. coli was more sensitive to DMF. The results indicate that DMF may be a potentially effective alternative antimicrobial agent to inhibit E. coli.

Anti-Bacterial Agents↗
PubMed1997

Restructuring the active site of fumarase for the fumarate to malate reaction.

Changes in the active site of fumarase (yeast fumarase II) that occur when fumarate is converted to malate (E.F --> E.M) must be reversed for another cycle of reaction to take place. As shown here, recycling of the enzyme includes two proton transfers and one conformational change. These events, together with the M-off step, are variously rate-determining depending on the medium. In very low salt the release of M is limited by the conformational change. Thus, (V/Km)F decreases with increased viscosity, shown with glycerol. A variety of simple anions, such as Cl- at approximately 50 mM and F itself at low concentration, activate the dissociation of M. This nonspecific anion effect is the basis for the >4-fold apparent cooperative activation by substrate. The M-off step and the conformational change are independent and random-order events. Thus, even when M-off is made rapid the rate of recycling is inhibited by glycerol, which in 100 mM NaCl inhibits Vmax but not V/Km. The enzyme form that results when M is released is M-specific, Em. Thus mesotartarate, competitive toward M, is noncompetitive toward F. The slow conformational change required for recycling of Em is activated by Pi and chaotropic anions such as azide and thiocyanate, giving rise to a nonspecific intermediate, Emf (mesotartarate becomes competitive toward F and Britton's countertransport property disappears with these activators). Evidence is presented for the locations and rates of the two proton transfer steps required to complete the cycle.

Anions↗
PubMed1998

Treatment of psoriasis with fumaric acid esters: results of a prospective multicentre study. German Multicentre Study.

Systemic treatment of psoriasis with fumaric acid esters (FAE) has been found effective by empirical means. In recent years clinical studies have confirmed the antipsoriatic activity of a defined mixture of different FAE. The aim of the present prospective multicentre study was to investigate further the efficacy and safety of FAE therapy in a large number of patients with severe psoriasis vulgaris. From 101 patients included in the study 70 completed the treatment period of 4 months. Discontinuation was due to adverse events in seven, lack of efficacy in two, and other reasons, such as non-attendance for scheduled visits, in 22 patients. Evaluation of overall efficacy showed a decrease in psoriasis area and severity index of 80% after 4 months of FAE therapy. Laboratory investigations revealed a slight overall decrease of lymphocytes during the treatment period which was more than 50% below baseline in 10 patients. During weeks 4 and 8 mean eosinophil counts were above the normal range. At the end of FAE therapy elevated eosinophil counts had returned to normal values. None of the patients showed changes in renal function parameters throughout the study. Adverse events were reported in 69% of the patients mainly consisting of gastrointestinal complaints (56%) and flushing (31%). In five patients gastrointestinal complaints and in two patients flushing led to withdrawal from the study. Taken together the results of this multicentre study showed in a large number of patients that systemic FAE treatment is effective in severe psoriasis vulgaris. Transient eosinophilia seems to be a characteristic feature of FAE therapy, while lymphocytopenia is usually mild. Adverse effects are dose-related and consist mainly of gastrointestinal complaints and flushing.

Adult↗