Search results for "Benzimidazole"

showing 10 items of 161 documents

Effect of histamine and histamine analogues on human isolated myometrial strips.

1992

1. The effect of histamine and histamine H1- and H2-receptor agonists on isolated myometrium strips of premenopausal women has been examined. The effect of acetylcholine was also determined. 2. Histamine, 2-pyridylethylamine, 4-methylhistamine and acetylcholine, but not dimaprit, produced a concentration-related contractile response in human isolated myometrial strips. Histamine also produced a further contraction in human isolated myometrial strips precontracted with KCl (55 mM). 3. The contractile response to histamine was antagonized by the histamine H1-receptor antagonist, clemizole (0.1 microM) but was potentiated by the histamine H2-receptor antagonist, ranitidine (10 microM). Clemizo…

AdultAtropinemedicine.medical_specialtyPyridinesMuscle RelaxationHistamine H1 receptorRanitidineHistamine agonistPotassium ChlorideHistamine Agonistschemistry.chemical_compoundHistamine receptorUterine ContractionHistamine H2 receptorInternal medicinemedicineHumansPharmacologyDose-Response Relationship DrugMethylhistaminesMuscle SmoothMiddle AgedDimapritAcetylcholineClemizoleEndocrinologyMuscle relaxationchemistryMyometriumBenzimidazolesFemaleHistamineHistamineResearch ArticleBritish journal of pharmacology
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Efficacy and safety of glecaprevir/pibrentasvir in renally impaired patients with chronic HCV infection

2019

Background and aims Chronic hepatitis C virus (HCV) infection increases the risk of incident chronic kidney disease (CKD) and progression to end-stage renal disease (ESRD). Previously available direct-acting antiviral regimens are not approved for patients with advanced CKD across all HCV genotypes. Methods EXPEDITION-5 is a phase 3 study to evaluate efficacy and safety of the fixed-dose combination of glecaprevir and pibrentasvir (G/P) for chronic HCV infection (genotype 1 through 6) in adults without cirrhosis or with compensated cirrhosis and with stage 3b, 4 or 5 CKD. Patients received approved duration of G/P according to HCV genotype, cirrhosis status and prior HCV treatment experienc…

AdultCyclopropaneshepatitis C virusmedicine.medical_specialtyAminoisobutyric AcidsPyrrolidinesCirrhosisProlineLactams Macrocyclicmedicine.medical_treatmentAntiviral Agents03 medical and health sciences0302 clinical medicineLeucineQuinoxalinesInternal medicineGenotypeHumansMedicineAdverse effectDialysisSulfonamidesdirect-acting antiviralpangenotypicHepatologychronic kidney disease; cirrhosis; direct-acting antiviral; hepatitis C virus; pangenotypicbusiness.industrycirrhosisGlecaprevirHepatitis C Chronicmedicine.diseasePibrentasvirDrug Combinations030220 oncology & carcinogenesisBronchitisBenzimidazoles030211 gastroenterology & hepatologybusinesschronic kidney diseaseKidney disease
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Identification and expansion of human osteosarcoma-cancer-stem cells by long-term 3-aminobenzamide treatment

2009

A novel cancer stem-like cell line (3AB-OS), expressing a number of pluripotent stem cell markers, was irreversibly selected from human osteosarcoma MG-63 cells by long-term treatment (100 days) with 3-aminobenzamide (3AB). 3AB-OS cells are a heterogeneous and stable cell population composed by three types of fibroblastoid cells, spindle-shaped, polygonal-shaped, and rounded-shaped. With respect to MG-63 cells, 3AB-OS cells are extremely smaller, possess a much greater capacity to form spheres, a stronger self-renewal ability and much higher levels of cell cycle markers which account for G1-S/G2-M phases progression. Differently from MG-63 cells, 3AB-OS cells can be reseeded unlimitedly wit…

AdultHomeobox protein NANOGAdolescentPhysiologyCellular differentiationClinical BiochemistryApoptosisBiologyStem cell markerYoung Adultcancer stemm cells osteosarcoma PARP inhibitorsCancer stem cellCell Line TumorSettore BIO/10 - BiochimicaHumansRhodamine 123Enzyme InhibitorsProgenitor cellChildInduced pluripotent stem cellCell ShapeCell potencyFluorescent DyesOsteosarcomaCell DifferentiationCell BiologyCalcium Channel BlockersDrug Resistance MultipleGene Expression Regulation NeoplasticVerapamilBenzamidesImmunologyNeoplastic Stem CellsCancer researchATP-Binding Cassette TransportersBenzimidazolesStem cellBiomarkersJournal of Cellular Physiology
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Efficacy and safety of lomitapide in homozygous familial hypercholesterolaemia: the pan-European retrospective observational study

2021

Abstract Aims Lomitapide is a lipid-lowering agent indicated as an adjunct therapy for adult homozygous familial hypercholesterolaemia (HoFH). This study evaluated the medium-term effectiveness and safety of lomitapide in a large cohort of HoFH patients in Europe. Methods and results In a multicentre retrospective, observational study including 75 HoFH patients treated with lomitapide in a real-world clinical setting from 9 European countries, low-density lipoprotein cholesterol (LDL-C) changes, adverse events (AEs), and major adverse cardiovascular events (MACE) were assessed. After a median 19 months (interquartile range 11–41 months) of treatment with a mean dosage of 20 mg of lomitapide…

AdultHomozygous Familial HypercholesterolemiaSettore MED/09 - Medicina InternaEpidemiologyAnticholesteremic AgentsHomozygoteMedium-term efficacyCholesterol LDLMedium-term safetyBenzimidazoleLomitapideHomozygous Familial Hypercholesterolemia; atherosclerosis; lomitapide; medium-term efficacy; medium-term safetyHyperlipoproteinemia Type IIHomozygous familial hypercholesterolaemiaRetrospective StudieAtherosclerosiAnticholesteremic AgentHumansBenzimidazolesatherosclerosisCardiology and Cardiovascular MedicineRetrospective StudiesHuman
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Evolution of HCV patient characteristics and DAA regimens in the German Hepatitis C Registry (DHC-R) in 2014 and 2015

2019

 The urgent need in HCV-infected patients with liver disease mandated the rapid implementation of IFN-free DAA combination therapies following their regulatory approval in 2014 and 2015 without full knowledge of the optimal combinations and regimens. Investigating the evolution of the DAA utilization patterns and treatment outcomes could provide learnings for future situations. This was an analysis of a prospective observational database from the German Hepatitis C Registry (DHC-R) covering a period from May 2014 to September 2015. Adult patients had evidence of chronic HCV GT1 or GT4 infection and were treated with an IFN-free combination regimen of simeprevir (SMV) + sofosbuvir (SOF) or o…

AdultLedipasvirSimeprevirmedicine.medical_specialtyDaclatasvirSustained Virologic ResponseSofosbuvirHepacivirusAntiviral Agents03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineHumansMedicineProspective StudiesRegistries030212 general & internal medicineFluorenesDasabuvirbusiness.industryGastroenterologyHepatitis C ChronicHepatitis COmbitasvirDrug CombinationsRegimenTreatment OutcomechemistryParitaprevirBenzimidazolesDrug Therapy Combination030211 gastroenterology & hepatologySofosbuvirbusinessmedicine.drugZeitschrift für Gastroenterologie
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Lomitapide affects HDL composition and function

2016

Abstract Background Lomitapide reduces low-density lipoprotein-cholesterol (LDL-C) but also high-density lipoprotein-cholesterol (HDL-C) levels. The latter may reduce the clinical efficacy of lomitapide. We investigated the effect of lomitapide on HDL-C levels and on cholesterol efflux capacity (CEC) of HDL in patients with homozygous familial hypercholesterolemia (HoFH). Methods and results Four HoFH patients were treated with increasing dosages of lomitapide. Lomitapide decreased LDL-C (range −34 to −89%). Total HDL-C levels decreased (range −16 to −34%) with a shift to buoyant HDL. ABCA1-mediated CEC decreased in all patients (range −39 to −99%). The changes of total, ABCG1- and SR-BI-me…

AdultMale0301 basic medicinemedicine.medical_specialtySettore MED/09 - Medicina InternaHDLHomozygous familial hypercholesterolemiaFamilial hypercholesterolemia030204 cardiovascular system & hematologyHyperlipoproteinemia Type IIYoung Adult03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineHumansMedicineIn patientClinical efficacyHyperlipoproteinemia Type IICholesterolbusiness.industryCholesterol HDLHomozygotenutritional and metabolic diseasesCholesterol LDLCholesterol efflux capacityAtherosclerosismedicine.diseaseCholesterol lowering drugsLomitapideLomitapideCholesterolPhenotypeTreatment Outcome030104 developmental biologyEndocrinologychemistryBenzimidazolesFemalelipids (amino acids peptides and proteins)Composition (visual arts)Cholesterol lowering drugHydroxymethylglutaryl-CoA Reductase InhibitorsLipoproteins HDLCardiology and Cardiovascular MedicinebusinessATP Binding Cassette Transporter 1Atherosclerosis
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Encorafenib plus binimetinib versus vemurafenib or encorafenib in patients with BRAF -mutant melanoma (COLUMBUS): a multicentre, open-label, randomis…

2017

Summary Background Combined BRAF-MEK inhibitor therapy is the standard of care for BRAF V600 -mutant advanced melanoma. We investigated encorafenib, a BRAF inhibitor with unique target-binding properties, alone or in combination with the MEK inhibitor binimetinib, versus vemurafenib in patients with advanced BRAF V600 -mutant melanoma. Methods COLUMBUS was conducted as a two-part, randomised, open-label phase 3 study at 162 hospitals in 28 countries. Eligible patients were aged 18 years or older and had histologically confirmed locally advanced (American Joint Committee on Cancer [AJCC] stage IIIB, IIIC, or IV), unresectable or metastatic cutaneous melanoma, or unknown primary melanoma; a B…

AdultMaleProto-Oncogene Proteins B-raf0301 basic medicineOncologymedicine.medical_specialtySkin NeoplasmsTime FactorsPhases of clinical researchYoung Adult03 medical and health scienceschemistry.chemical_compound0302 clinical medicineInternal medicineAntineoplastic Combined Chemotherapy ProtocolsBiomarkers TumormedicineHumansMolecular Targeted TherapyProgression-free survivalVemurafenibMelanomaProtein Kinase InhibitorsAgedAged 80 and overSulfonamidesPerformance statusbusiness.industryMelanomaMEK inhibitorBinimetinibMiddle Agedmedicine.diseaseProgression-Free Survival030104 developmental biologyVemurafenibOncologyTolerabilitychemistry030220 oncology & carcinogenesisMutationBenzimidazolesFemaleCarbamatesbusinessmedicine.drugThe Lancet Oncology
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The effect duration of candesartan cilexetil once daily, in comparison with enalapril once daily, in patients with mild to moderate hypertension.

2001

To determine the antihypertensive efficacy, effect duration and safety of the angiotensin II type 1 receptor blocker candesartan cilexetil and the angiotensin converting enzyme inhibitor enalapril once daily in patients with mild to moderate hypertension.A multicenter, randomised, double-blind parallel group study was performed in Finland, France, the Netherlands, Spain and Sweden. Three-hundred-and-ninety-five men and women in the age range 20-80 years with primary hypertension were randomised to an 8-week double-blind treatment period with either candesartan cilexetil 8-16 mg or enalapril 10-20 mg once daily, with forced dose titration after 4 weeks. Non-invasive ambulatory blood pressure…

AdultMalemedicine.medical_specialtyAmbulatory blood pressureTime Factorsmedicine.medical_treatmentDiastoleTetrazolesAngiotensin-Converting Enzyme InhibitorsBlood PressureAngiotensin Receptor AntagonistsDouble-Blind MethodEnalaprilHeart RateInternal medicineInternal MedicinemedicineHumansProdrugsEnalaprilAntihypertensive AgentsAgedAged 80 and overChemotherapybiologybusiness.industryBiphenyl CompoundsAngiotensin-converting enzymeGeneral MedicineMiddle AgedAngiotensin IICandesartanEndocrinologyTherapeutic EquivalencyACE inhibitorHypertensionbiology.proteinCardiologyBenzimidazolesFemaleCardiology and Cardiovascular Medicinebusinessmedicine.drugBlood pressure
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Factors related to the impact of antihypertensive treatment in antioxidant activities and oxidative stress by-products in human hypertension

2004

The objective was to study factors related to the changes induced by antihypertensive treatment on oxidative status, antioxidant activities, and reactive oxygen species by-products in whole blood and mononuclear peripheral cells. Eighty-nine hypertensive patients (mean age 46 years, 46 men, average 24-h blood pressure 139/88 mm Hg, body mass index 29) were included. After 3 months of nonrandomized allocation to antihypertensive treatment (20 nonpharmacologic, 36 beta-blockers, 33 angiotensin receptor blocker), oxidized/reduced glutathione ratio and malondialdehyde were significantly reduced, and the activity of superoxide dismutase, catalase, and glutathione peroxidase was significantly inc…

AdultMalemedicine.medical_specialtyAntioxidantmedicine.medical_treatmentAngiotensin-Converting Enzyme Inhibitorsmedicine.disease_causeBenzoatesAntioxidantsSuperoxide dismutasechemistry.chemical_compoundInternal medicineInternal MedicinemedicineHumansTelmisartanAntihypertensive AgentsWhole bloodchemistry.chemical_classificationReactive oxygen speciesbiologybusiness.industryGlutathione peroxidaseGlutathioneMiddle AgedMalondialdehydeOxidative StressHydrochlorothiazideTreatment OutcomeEndocrinologyAtenololchemistryHypertensionbiology.proteinBenzimidazolesDrug Therapy CombinationFemalebusinessOxidative stressDNA DamageAmerican Journal of Hypertension
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Treating homozygous familial hypercholesterolemia in a real-world setting: Experiences with lomitapide

2015

Homozygous familial hypercholesterolaemia (HoFH) is a rare genetic disease characterised by markedly elevated plasma levels of low-density lipoprotein-cholesterol (LDL-C). Lomitapide is a microsomal triglyceride transfer protein (MTP) inhibitor approved as an adjunct to other lipid-lowering therapies (LLTs), with or without lipoprotein apheresis (LA), for the treatment of adult HoFH. Diet with <20% calories from fat is required. Due to a varying genetic and phenotypic profile of patients with HoFH, individual patients may respond to therapy differently; therefore examining individual cases in a 'real-world' setting provides valuable information on the effective day-to-day manag…

AdultMalemedicine.medical_specialtyCalorieSettore MED/09 - Medicina InternaEndocrinology Diabetes and MetabolismCase studyFamilial hypercholesterolemiaHomozygous familial hypercholesterolemiaFamilial hypercholesterolemiaDiseaseCompound heterozygosityHyperlipoproteinemia Type IIchemistry.chemical_compoundInternal medicineCase study; Familial hypercholesterolemia; Homozygous familial hypercholesterolemia; Lomitapide; Treatment; Cardiology and Cardiovascular Medicine; Endocrinology Diabetes and Metabolism; Internal Medicine; Nutrition and DieteticsInternal MedicinemedicineHumansAdverse effectNutrition and Dieteticsbusiness.industryAnticholesteremic AgentsHomozygoteCholesterol LDLMiddle Agedmedicine.diseaseLomitapideLomitapideTreatmentClinical trialEndocrinologychemistryBenzimidazolesFemaleSteatosisCardiology and Cardiovascular Medicinebusiness
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