Search results for "Azoles"

showing 10 items of 899 documents

Simultaneous controlled iontophoretic delivery of pramipexole and rasagiline in vitro and in vivo: Transdermal polypharmacy to treat Parkinson's dise…

2018

[EN] Effective treatment of Parkinson's disease (PD) involves administration of therapeutic agents with complementary mechanisms of action in order to replenish, sustain or substitute endogenous dopamine. The objective of this study was to investigate anodal co-iontophoresis of pramipexole (PRAM; dopamine agonist) and rasagiline (RAS; MAO-B inhibitor) in vitro and in vivo. Passive permeation of PRAM and RAS (20 mM each) across porcine skin after 6 h was 15.7 +/- 1.9 and 16.0 +/- 2.9 mu g/cm(2), respectively. Co-iontophoresis at 0.15, 0.3 and 0.5 mA/cm(2) resulted in statistically significant increases in delivery of PRAM and RAS; at 0.5 mA/cm(2), cumulative permeation of PRAM and RAS was 61…

MaleParkinson's diseaseSwineChemistry PharmaceuticalSkin AbsorptionPharmaceutical SciencePharmacologyAdministration Cutaneous030226 pharmacology & pharmacyDopamine agonistPermeability03 medical and health scienceschemistry.chemical_compound0302 clinical medicinePramipexolePharmacokineticsIn vivomedicineAnimalsHumansBenzothiazolesMAO-B inhibitorRats WistarTransdermalSkinRasagilinePramipexoleIontophoresisDopamine agonistPatient complianceParkinson DiseaseGeneral MedicineIontophoresismedicine.diseaseRatschemistryIndansPolypharmacyElectroosmosisTransdermal030217 neurology & neurosurgeryBiotechnologymedicine.drugEuropean journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V
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Differential uptake of systemic fluorochrome Hoechst 33342 in lung and liver metastasis of B16 melanoma.

1992

The growth and vascularization patterns of B16 melanoma colonies in the liver and lungs were measured and compared by histological techniques and dye diffusion patterns after injection of the fluorochrome Hoechst 33342. In the liver, the fluorescent pattern of dye diffusion revealed that uninodular tumours measuring up to 146 microns in diameter were not functionally vascularized. However, when the nodules fused to give rise to multinodular tumours measuring between 256 and 366 microns in diameter, a reticular dye diffusion pattern revealed functional tumour vascularization. In the lungs, subpleural, parenchymal and peritubular (i.e. surrounding blood vessels and airways) tumours were obser…

MalePathologymedicine.medical_specialtyLung NeoplasmsRatónmedicine.medical_treatmentMelanoma ExperimentalBiologyPathology and Forensic MedicineMetastasisMiceParenchymamedicineAnimalsNeoplasm MetastasisMolecular BiologyChemotherapyLungNeovascularization PathologicRespiratory diseaseLiver NeoplasmsCell BiologyGeneral Medicinemedicine.diseaseRadiation therapyMice Inbred C57BLmedicine.anatomical_structureReticular connective tissueBenzimidazolesVirchows Archiv. A, Pathological anatomy and histopathology
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Dental extraction following zoledronate, induces osteonecrosis in rat´s jaw

2017

Background Bisphosphonate-Related Osteonecrosis of the Jaw (BRONJ) is clinically characterized by the presence of exposed bone in the oral cavity that persists for more than eight weeks. Previous attempts to establish an animal model have not sufficiently considered disease features. Our aim was to establish an inexpensive and replicable animal model that develops BRONJ in a short time. Material and Methods Thirty-two male Wistar rats were randomly divided into two groups: control and experimental. In the experimental group, we administered 0.06mg/kg intraperitoneal dose of zoledronic acid (ZA) 7 and 14 days prior to maxillary second molar extraction. At two, four and six weeks after tooth …

MalePathologymedicine.medical_specialtymedicine.medical_treatmentMaxillary second molarH&E stainZoledronic AcidSequestrumRandom Allocation03 medical and health sciencesPostoperative Complications0302 clinical medicineTrichromemedicineAnimalsRats WistarGeneral DentistryOral Medicine and PathologyBone Density Conservation AgentsDiphosphonatesbusiness.industryResearchImidazoles030206 dentistry030224 pathologymedicine.disease:CIENCIAS MÉDICAS [UNESCO]RatsDisease Models AnimalZoledronic acidOtorhinolaryngologyDental extractionMaxillaTooth ExtractionUNESCO::CIENCIAS MÉDICASBisphosphonate-Associated Osteonecrosis of the JawSurgeryOsteonecrosis of the jawbusinessmedicine.drug
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Rufinamide in children and adults with Lennox-Gastaut syndrome: first Italian multicenter experience

2010

This is the first multicenter Italian experience with rufinamide as an adjunctive drug in children, adolescents and adults with Lennox-Gastaut syndrome. The patients were enrolled in a prospective, add-on, open-label treatment study from 11 Italian centers for children and adolescent epilepsy care. Forty-three patients (26 males, 17 females), aged between 4 and 34 years (mean 15.9 ± 7.3, median 15.0), were treated with rufinamide for a mean period of 12.3 months (range 3-21 months). Twenty patients were diagnosed as cryptogenic and 23 as symptomatic. Rufinamide was added to the baseline therapy at the starting dose of 10mg/kg body weight, evenly divided in two daily doses and then increased…

MalePediatricsLennox-Gastaut syndromeAtypical absence seizuresRufinamideLennox–Gastaut syndrome; Rufinamide; Orphan drug; Pediatrics; Epilepsy; Drop attacksInfantilePediatricsSpasmsEpilepsyRufinamideDrop attacks; Epilepsy; Lennox-Gastaut syndrome; Orphan drug; Pediatrics; Rufinamide; Adolescent; Adult; Anticonvulsants; Child; Child Preschool; Drug Therapy Combination; Female; Humans; Intellectual Disability; Italy; Lennox Gastaut Syndrome; Male; Spasms Infantile; Treatment Outcome; Triazoles; Valproic Acid; Young Adult; Neurology (clinical); NeurologyChildPediatricValproic AcidDrop attacksGeneral MedicineSettore MED/39 - Neuropsichiatria InfantileTreatment OutcomeItalyNeurologyAnesthesiaChild PreschoolCombinationVomitingAnticonvulsantsDrug Therapy CombinationFemalemedicine.symptomSpasms Infantilemedicine.drugAdultmedicine.medical_specialtyAdolescentClinical NeurologyIrritabilityYoung AdultDrug TherapyIntellectual DisabilitymedicineHumanspediatrics epilepsyPreschoolAdverse effectLennox–Gastaut syndrome; rufinamide; orphan drug; pediatrics epilepsy; drop attacks; refractory epilepsy.EpilepsyOrphan drugbusiness.industryLennox Gastaut SyndromeValproic Acidrefractory epilepsyTriazolesmedicine.diseaseNeurology (clinical)businessLennox–Gastaut syndromeLennox–Gastaut syndrome
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Individual analysis of patients with HoFH participating in a phase 3 trial with lomitapide: The Italian cohort

2015

Abstract Background and aims The efficacy and safety of lomitapide as adjunct treatment for adults with homozygous familial hypercholesterolaemia (HoFH) have been confirmed in a phase 3 trial. Given the small number of patients (N = 29), and variations in patient characteristics, examining individual cases provides additional details regarding patient management with lomitapide. Here, we examine the details of the Italian patient cohort in the phase 3 trial. Methods and results The methodology of the multinational, single-arm, open-label, 78-week, dose-escalation, phase 3 trial has been previously reported. The current report details the Italian cohort of six patients (three males, three fe…

MalePediatricsTime FactorsSettore MED/09 - Medicina InternaEndocrinology Diabetes and MetabolismHoFHMedicine (miscellaneous)030204 cardiovascular system & hematologychemistry.chemical_compound0302 clinical medicineEndocrinologyReceptorsNutrition and DieteticMedicine030212 general & internal medicineFamilial hypercholesterolaemia; FH; HoFH; Homozygous familial hypercholesterolaemia; Lomitapide; Therapy; Medicine (miscellaneous); Nutrition and Dietetics; Endocrinology Diabetes and Metabolism; Cardiology and Cardiovascular MedicineFH; Familial hypercholesterolaemia; HoFH; Homozygous familial hypercholesterolaemia; Lomitapide; Therapy; Adolescent; Adult; Anticholesteremic Agents; Benzimidazoles; Biomarkers; Cholesterol LDL; Female; Genetic Predisposition to Disease; Humans; Hyperlipoproteinemia Type II; Italy; Male; Middle Aged; Phenotype; Receptors LDL; Time Factors; Treatment Outcome; Young Adult; Heterozygote; MutationNutrition and DieteticsAnticholesteremic AgentsMiddle AgedPatient managementDiabetes and MetabolismCholesterolPhenotypeTreatment OutcomeTolerabilityItalyCohortPopulation studyFemaleFamilial hypercholesterolaemiaCardiology and Cardiovascular MedicineAdultmedicine.medical_specialtyHeterozygoteAdolescentSocio-culturaleFHLDLHyperlipoproteinemia Type II03 medical and health sciencesIndividual analysisYoung AdultHomozygous familial hypercholesterolaemiaHumansGenetic Predisposition to DiseaseAdverse effectbusiness.industryCholesterol LDLLomitapideLomitapideClinical trialchemistryReceptors LDLMutationBenzimidazolesTherapybusinessBiomarkers
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Comparable Helicobacter pylori eradication rates obtained with 4- and 7-day rabeprazole-based triple therapy: a preliminary study

2003

Abstract Background. Rabeprazole is a new proton pump inhibitor, which has been reported to induce a faster acid suppression than other drugs of the same category. This might be useful to reduce the duration of anti-Helicobacter therapies. Aims. The aim of this study was to assess whether there is the possibility of shortening a rabeprazole-based triple therapy from 7 to 4 days without compromising its efficacy in the eradication of Helicobacter pylori infection. Patients. A total of 128 consecutive dyspeptic patients with H. pylori infection were recruited for this controlled, randomized, open and parallel-group trial comparing the efficacy of two durations of the same rabeprazole-based tr…

MalePeptic Ulcermedicine.medical_specialtymedicine.drug_classUrea breath testRabeprazoleProton-pump inhibitorPilot ProjectsGastroenterology2-PyridinylmethylsulfinylbenzimidazolesDrug Administration ScheduleHelicobacter InfectionsAnti-Infective AgentsClarithromycinMetronidazoleClarithromycinInternal medicinemedicineHumansProspective StudiesDyspepsiaAdverse effectHelicobacter pyloriHepatologybiologymedicine.diagnostic_testbusiness.industryGastroenterologyProton Pump InhibitorsMiddle AgedHelicobacter pyloriAnti-Ulcer Agentsbiology.organism_classificationAnti-Bacterial AgentsMetronidazoleRegimenTreatment OutcomeRabeprazoleBenzimidazolesDrug Therapy CombinationFemalebusinessOmeprazolemedicine.drug
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Downregulation of nNOS and synthesis of PGs associated with endotoxin-induced delay in gastric emptying

2002

A single intraperitoneal injection of endotoxin (40 μg/kg) significantly delayed gastric emptying of a solid nutrient meal. Blockade of nitric oxide synthase (NOS) with 30 mg/kg ip N G-nitro-l-arginine methyl ester or 20 mg/kg ip 7-nitroindazole [neuronal NOS (nNOS) inhibitor] significantly delayed gastric emptying in control animals but failed to modify gastric emptying in endotoxin-treated rats. Administration of 2.5, 5, and 10 mg/kg ip N 6-iminoethyl-l-lysine [inducible NOS (iNOS) inhibitor] had no effect in either experimental group. Indomethacin (5 mg/kg sc), NS-398 (cyclooxygenase-2 inhibitor; 10 mg/kg ip), and dexamethasone (10 mg/kg sc) but not quinacrine (20 mg/kg ip) significantl…

MalePhysiologymedicine.medical_treatmentIndomethacinNitric Oxide Synthase Type IINitric Oxide Synthase Type IprostaglandinsRats Sprague-Dawleychemistry.chemical_compoundPyloric AntrumEnzyme InhibitorsAntrumSulfonamidesArachidonic AcidbiologyReverse Transcriptase Polymerase Chain ReactionStomachdigestive oral and skin physiologyGastroenterologyNitric oxide synthasemedicine.anatomical_structureNG-Nitroarginine Methyl EsterQuinacrinenutrient mealsantrum. pylorusmedicine.medical_specialtyIndazolesIntraperitoneal injectionNitric OxidePhospholipases ANitric oxidenitric oxidePhysiology (medical)Internal medicinemedicineAnimalsCyclooxygenase InhibitorsRNA MessengerNitrobenzenesHepatologyGastric emptyingPylorusdigestive system diseasesRatsEndotoxinsEndocrinologyPyloric AntrumchemistryGastric EmptyingFoodbiology.proteinProstaglandinsNitric Oxide Synthase
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Posaconazole against Candida glabrata Isolates with Various Susceptibilities to Fluconazole

2008

ABSTRACT We investigated the in vitro activities of posaconazole (POS), fluconazole (FLC), amphotericin B (AMB), and caspofungin (CAS) against four clinical isolates of Candida glabrata with various susceptibilities to FLC (FLC MICs ranging from 1.0 to >64 μg/ml). POS MICs ranged from ≤0.03 to 0.5 μg/ml; AMB MICs ranged from 0.25 to 2.0 μg/ml, while CAS MICs ranged from 0.03 to 0.25 μg/ml. When FLC MICs increased, so did POS MICs, although we did not observe any isolate with a POS MIC greater than 0.5 μg/ml. Time-kill experiments showed that POS, FLC, and CAS were fungistatic against all isolates, while AMB at eight times the MIC was fungicidal against three out of four isolates of C. gl…

MalePosaconazoleAntifungal AgentsCandida glabrataMicrobial Sensitivity TestsDrug resistanceBiologyKidneyMicrobiologyMicechemistry.chemical_compoundDrug Resistance Fungalhemic and lymphatic diseasesAmphotericin BmedicineAnimalsHumansExperimental TherapeuticsPharmacology (medical)FluconazolePharmacologyCandida glabrataExperimental modelCandidiasisFungi imperfectiTriazolesbiology.organism_classificationTreatment OutcomeInfectious DiseaseschemistryCaspofunginFluconazolemedicine.drugAntimicrobial Agents and Chemotherapy
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Systolic Blood Pressure Variation and Mean Heart Rate Is Associated With Cognitive Dysfunction in Patients With High Cardiovascular Risk

2015

Abstract— Elevated systolic blood pressure (SBP) correlates to cognitive decline and incident dementia. The effects of heart rate (HR), visit to visit HR variation, and visit to visit SBP variation are less well established. Patients without preexisting cognitive dysfunction (N=24 593) were evaluated according to mean SBP, SBP visit to visit variation (coefficient of variation [standard deviation/mean×100%], CV), mean HR, and visit to visit HR variation (HR-CV) in the Ongoing Telmisartan Alone and in Combination with Ramipril Global Endpoint Trial and the Telmisartan Randomized Assessment Study in ACE Intolerant Subjects with Cardiovascular Disease. Cognitive function was assessed with min…

MalePredictive Value of TestAngiotensin-Converting Enzyme InhibitorsBlood PressureBenzimidazoleBenzoatesRamiprilRetrospective StudieHeart RateRisk FactorsCardiovascular DiseaseTelmisartanCognitive declineMultivariate AnalysiRandomized Controlled Trials as TopicAged 80 and overmedicine.diagnostic_testIncidenceMiddle AgedstrokeAntihypertensive Agentmyocardial infarctionCardiovascular DiseasesHypertensionCardiologyDrug Therapy CombinationFemaleHumanmedicine.drugRamiprilmedicine.medical_specialtyBenzoateFollow-Up StudieCognition DisorderPredictive Value of TestsInternal medicineHeart rateInternal MedicinemedicineHumansDementiaAntihypertensive AgentsAgedRetrospective StudiesMini–Mental State Examinationbusiness.industryRisk FactorAngiotensin-Converting Enzyme InhibitorOdds ratiomedicine.diseaseConfidence intervalBlood pressureMultivariate AnalysisPhysical therapyBenzimidazolesCognition DisordersbusinessFollow-Up StudiesHypertension
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Synthesis and Muscarinic Activity of Isoxazole-substituted 1,2,5,6-Tetrahydropyridines

1994

MalePyridinesGuinea PigsCholinergic AgentsPharmaceutical ScienceMuscarinic acetylcholine receptor M3Muscle SmoothMuscarinic acetylcholine receptor M2Biological activityIsoxazolesMuscarinic acetylcholine receptor M1In Vitro Techniqueschemistry.chemical_compoundchemistryBiochemistryDrug DiscoveryMuscarinic acetylcholine receptorMuscarinic acetylcholine receptor M5Muscarinic acetylcholine receptor M4AnimalsRabbitsIsoxazoleMuscle ContractionArchiv der Pharmazie
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