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showing 10 items of 3616 documents

The striatal and extrastriatal D2/D3 receptor-binding profile of clozapine in patients with schizophrenia.

2005

Positron emission tomography (PET) studies reveal that clozapine at clinically used doses occupies less than 60% of D2/D3 dopamine receptors in human striatum. Here, the occupancy of D2/D3 dopamine receptors by clozapine in patients with schizophrenia was determined to test the hypothesis that clozapine binds preferentially to extrastriatal dopamine receptors. A total of 15 clozapine-treated inpatients with schizophrenia underwent a [18F]fallypride PET scan. Receptor occupancy was calculated as percent reduction in binding potential relative to unblocked values measured in seven normal volunteers. Mean D2/D3 receptor occupancy was statistically significantly higher in cortical (inferior tem…

AdultMalemedicine.medical_specialtyPsychosisPyrrolidinesDopamineStriatumBinding CompetitiveReceptors DopamineDopamine receptor D3Internal medicinemedicineHumansClozapineClozapinePharmacologyTemporal cortexDose-Response Relationship DrugChemistryReceptors Dopamine D2PutamenReceptors Dopamine D3Middle Agedmedicine.diseaseCorpus StriatumTemporal LobePsychiatry and Mental healthEndocrinologyFallyprideDopamine receptorAnesthesiaPositron-Emission TomographyBenzamidesSchizophreniaFemalemedicine.drugAntipsychotic AgentsNeuropsychopharmacology : official publication of the American College of Neuropsychopharmacology
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Antipsychotic effects and tolerability of the sigma ligand EMD 57445 (panamesine) and its metabolites in acute schizophrenia: an open clinical trial.

2000

Antipsychotic efficacy and side effects of the selective sigma ligand EMD 57445 (panamesine) were investigated in 12 patients (6 males, 6 females) who met DSM-III-R criteria for schizophrenia. A 4-week open clinical study revealed only modest effects of EMD 57445 and its metabolites on positive and negative symptoms of schizophrenia. Extrapyramidal and other side effects were moderate, although a significant increase in mild dyskinetic movements was found. Five patients, four of whom were females, completed the trial. Dropouts were mainly due to treatment failure. Antipsychotic effects were significantly greater in female than male patients.

AdultMalemedicine.medical_specialtyPsychosismedicine.medical_treatmentSigma receptorPanamesineDrug Administration ScheduleBasal Ganglia DiseasesPiperidinesInternal medicinemental disordersmedicineHumansReceptors sigmaAntipsychoticOxazolesBiological PsychiatryBiotransformationAgedPsychiatric Status Rating ScalesDose-Response Relationship DrugMiddle Agedmedicine.diseaseClinical trialPsychiatry and Mental healthEndocrinologyTreatment OutcomeTolerabilityDopamine receptorSchizophreniaAcute DiseaseSchizophreniaFemaleSchizophrenic PsychologyPsychologyAntipsychotic AgentsPsychiatry research
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OASIS-HT: design of a pharmacogenomic dose-finding study.

2005

Experimental evidence and observations in humans strongly support an interactive role of mutated α-adducin, sodium (Na+)/potassium (K+)-adenosine triphosphatase (ATPase) activity and endogenous ouabain in Na+homeostasis and the pathogenesis of hypertension. The Ouabain and Adducin for Specific Intervention on Sodium in HyperTension (OASIS-HT) trial is an early Phase II dose-finding study, which will be conducted across 39 European centers. Following a run-in period of 4 weeks without treatment, eligible patients will be randomized to one of five oral doses of rostafuroxin consisting of 0.05, 0.15, 0.5, 1.5, or 5.0 mg/day. Each dose will be compared to a placebo in a double-blind crossover e…

AdultMalemedicine.medical_specialtyRandomizationTime FactorsSystolic hypertensionMolecular ConformationAdministration OralBlood PressurePharmacologyPlaceboOuabainDrug Administration ScheduleDouble-Blind MethodRisk FactorsInternal medicineGeneticsClinical endpointMedicineHumansAndrostanolsOuabainAntihypertensive AgentsPharmacologyCross-Over StudiesDose-Response Relationship Drugbusiness.industryMiddle Agedmedicine.diseaseCrossover studyBlood pressureEndocrinologyTreatment OutcomeHypertensionMolecular MedicineCalmodulin-Binding ProteinsFemalebusinessHomeostasismedicine.drugPharmacogenomics
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Human Corticotropin-Releasing Hormone in Man: Dose-Response of Minute Ventilation and End-Tidal Partial Pressures of Carbon Dioxide and Oxygen*

1987

The respiratory stimulant properties of iv injections of 33, 67, and 100 micrograms synthetic human corticotropin-releasing hormone (hCRH) were studied in 12 normal men in a single blind, placebo-controlled trial. All doses of hCRH induced a respiratory stimulation in every subject, and the stimulation was dose dependent. The onset of respiratory stimulation occurred within 15-30 sec after hCRH infusion was started. Initially, there was an increase in tidal volume (VT), followed by an increase in respiratory rate. The maximum minute ventilation (VE) occurred 60-120 sec after starting the injection. The 33-micrograms hCRH dose induced a 35% increase in VE from 6.3 +/- 0.6 (+/- SD) to 9.7 +/-…

AdultMalemedicine.medical_specialtyRespiratory rateCorticotropin-Releasing HormonePartial PressureEndocrinology Diabetes and MetabolismClinical BiochemistryBlood PressureStimulationPeptide hormoneBiochemistryEndocrinologyDouble-Blind MethodHeart RateInternal medicineHeart rateFlushingmedicineHumansRespiratory systemTidal volumeDose-Response Relationship DrugChemistryRespirationBiochemistry (medical)Carbon DioxideOxygenEndocrinologyAnesthesiaBreathingRespiratory minute volumeThe Journal of Clinical Endocrinology & Metabolism
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Different doses of consensus interferon plus ribavirin in patients with hepatitis C virus genotype 1 relapsed after interferon monotherapy: a randomi…

2006

AIM: To assess the efficacy of different schedules of consensus interferon (CIFN) plus ribavirin in retreating chronic hepatitis C patients who relapsed after recombinant interferon (rIFN) monotherapy. METHODS: Forty-five patients (34 males and 11 females) with chronic hepatitis due to hepatitis C virus (HCV) genotype 1 who relapsed after a previous course of rIFN monotherapy were randomized to receive 9 μg CIFN three times per week for 52 wk (group A, n = 22) or 18 μg CIFN three times per week for 52 wk (group B, n = 23) in combination with ribavirin 800 to 1200 mg daily for 52 wk (according to body weight). Virological response was evaluated at week 24 (EVR), at the end of treatment (ETR)…

AdultMalemedicine.medical_specialtySettore MED/07 - Microbiologia E Microbiologia ClinicavirusesHepacivirusAlpha interferonHepacivirusPharmacologyGastroenterologyAntiviral AgentsDrug Administration Schedulelaw.inventionchemistry.chemical_compoundRandomized controlled triallawInterferonRecurrenceInternal medicineRibavirinmedicineHumansIn patientSettore MED/12 - GastroenterologiabiologyDose-Response Relationship Drugbusiness.industryRibavirinGastroenterologyInterferon-alphaGeneral MedicineHepatitis C ChronicMiddle AgedViral Loadbiology.organism_classificationhumanitiesRecombinant ProteinsTreatment OutcomechemistryInterferon Type IInterferon Ribavirin Hepatitis C virus Hepatitis C RelapserDrug Therapy CombinationFemalebusinessViral loadInterferon type IRapid Communicationmedicine.drugWorld journal of gastroenterology
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Comparison of topical tacrolimus 0.1 % in pectin ointment with clobetasol 0.5% ointment in adults with moderate to severe desquamative gingivitis: A …

2006

BACKGROUND: Desquamative gingivitis (DG) is a clinical condition characterized by red, painful, glazed, and friable gingiva, which might be a manifestation of some autoimmune mucocutaneous diseases. The time from the development of initial signs of DG to diagnosis can vary from months to years. Based on a literature search, no data concerning patients with DG without signs of autoimmune disease were available. OBJECTIVE: The aim of this trial was to compare the efficacy and tolerability of monotherapy with topical tacrolimus 0.1% in pectin ointment versus clobetasol propionate 0.5% ointment in adults affected by DG. METHODS: This randomized, double-blind clinical trial was conducted at the …

AdultMalemedicine.medical_specialtySettore MED/09 - Medicina InternaErythemaAdministration TopicalPopulationSeverity of Illness IndexTacrolimuslaw.inventionOintmentsRandomized controlled trialDouble-Blind Methodlawdesquamative gingivitimedicineClinical endpointHumansPharmacology (medical)educationAgedPharmacologyeducation.field_of_studyDose-Response Relationship Drugbusiness.industryMiddle Agedmedicine.diseaseDermatologyGingivitisdesquamative gingivitisTacrolimusSurgeryDesquamative gingivitisTreatment OutcomeTolerabilityclobetasoltopical tacrolimus; clobetasol; desquamative gingivitis; randomized double-blind clinical trialtacrolimus clobetasol desquamative gingivitisPectinsDrug Therapy CombinationFemaleClobetasol propionatemedicine.symptombusinessImmunosuppressive Agentsmedicine.drugFollow-Up Studiestopical tacrolimurandomized double-blind clinical trial
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Amisulpride doses and plasma levels in different age groups of patients with schizophrenia or schizoaffective disorder.

2008

Abstract Because of a unique pharmacodynamic profile, amisulpride seems appropriate for treatment of elderly patients with schizophrenia. In a large-scale naturalistic therapeutic drug monitoring study, daily amisulpride dose, trough and dose-corrected amisulpride plasma levels, co-medication, clinical effectiveness (CGI) and side effects (UKU) were compared between age groups in 395 patients with schizophrenia or schizoaffective disorder (46% women; mean age 39.1 ± 14.2 years, range 18–83 years) under amisulpride therapy. Mean amisulpride doses (574 ± 269 mg/day), plasma levels (304 ± 274 ng/mL), dose-corrected amisulpride plasma levels (C/D ratios, 0.52 ± 0.41 ng/mL:mg), clinical respons…

AdultMalemedicine.medical_specialtySide effectAdolescentmedicine.drug_classPoison controlAtypical antipsychoticSchizoaffective disorderComorbidityGastroenterologyYoung AdultExtrapyramidal symptomsInternal medicinemedicineHumansPharmacology (medical)AmisulpridePsychiatryAgedPharmacologyAged 80 and overDose-Response Relationship DrugDopamine antagonistAge FactorsMiddle Agedmedicine.diseasePsychiatry and Mental healthPsychotic DisordersSchizophreniaSchizophreniaFemalemedicine.symptomAmisulprideDrug MonitoringSulpiridePsychologymedicine.drugAntipsychotic AgentsJournal of psychopharmacology (Oxford, England)
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Relaxation of the isolated human internal anal sphincter by sildenafil.

2007

Abstract Background Hypertonicity of the internal anal sphincter (IAS) appears to be involved in the pathogenesis of anal fissure. The relaxant effects of sildenafil, a selective phosphodiesterase 5 (PDE5) inhibitor, on isolated human IAS were investigated. Methods The efficacy (maximal effect, Emax) and potency (−log IC50, where IC50 is half-maximal inhibitory concentration) of the PDE5 inhibitors, sildenafil and zaprinast, and of nitric oxide donors, sodium nitroprusside and glyceryl trinitrate, as relaxants of histamine (0·1 mmol/l)-induced tone were examined in IAS strips under isometric contraction. The presence of PDE5 isoenzymes and changes in intracellular calcium and cyclic nucleot…

AdultMalemedicine.medical_specialtySildenafilPhosphodiesterase InhibitorsMuscle RelaxationAnal CanalIn Vitro TechniquesPiperazinesSildenafil CitrateInternal anal sphincterchemistry.chemical_compoundCyclic nucleotideInternal medicinemedicineHumansSulfonesCyclic GMPAgedAged 80 and overAnal fissureDose-Response Relationship Drugbusiness.industryMuscle SmoothMiddle Agedmedicine.diseaseMuscle relaxationEndocrinologychemistryPurinescGMP-specific phosphodiesterase type 5SurgeryFemaleSodium nitroprussideZaprinastbusinessmedicine.drugThe British journal of surgery
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Prostaglandin E2 activates the ciliary beat frequency of cultured human nasal mucosa via the second messenger cyclic adenosine monophosphate.

2001

Prostaglandins influence the ciliary beat frequency (CBF) of ciliated nasal epithelial cells and a stimulatory effect has been described for prostaglandin E2 (PGE2). Until now, it is not known whether PGE2 has direct ciliostimulatory properties or acts through a second messenger. In this study we investigated whether cyclic adenosine monophosphate (cAMP) is implicated in the signal transduction pathway of PGE2-induced activation of CBF. Ciliated cells of the nasal mucosa were cultured for up to 5 days whereafter the culture medium was removed and the cells were incubated with different concentrations of test solutions. The ciliated cells were recorded under a phase-contrast microscope and v…

AdultMalemedicine.medical_specialtyStimulationMucous membrane of noseBiologyIn Vitro TechniquesSecond Messenger SystemsDinoprostonechemistry.chemical_compoundInternal medicinemedicineCyclic AMPHumansCyclic adenosine monophosphateCiliaProstaglandin E2Cells CulturedAgedDose-Response Relationship DrugColforsinEpithelial CellsGeneral MedicineMiddle AgedEpitheliumCell biologyNasal Mucosamedicine.anatomical_structureEndocrinologyOtorhinolaryngologychemistryCell cultureSecond messenger systemFemaleSignal transductionmedicine.drugSignal TransductionEuropean archives of oto-rhino-laryngology : official journal of the European Federation of Oto-Rhino-Laryngological Societies (EUFOS) : affiliated with the German Society for Oto-Rhino-Laryngology - Head and Neck Surgery
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Comparative effects of dilator drugs on human penile dorsal artery and deep dorsal vein

1998

The present study was designed to characterize the response of human penile dorsal artery and deep dorsal vein to dilator drugs used in the diagnosis and treatment of erectile dysfunction with special emphasis on the effects on sympathetic neurotransmission. Ring segments of penile dorsal artery and deep dorsal vein were obtained from 20 multi-organ donors during procurement of organs for transplantation. The rings (3 ;mm long) were suspended in organ bath chambers for isometric recording of tension. We then studied the relaxant responses to prostaglandin E1 (PGE1), vasoactive intestinal peptide (VIP), papaverine (PV), sodium nitroprusside (SNP) and linsidomine chlorhydrate (SIN-1), and ana…

AdultMalemedicine.medical_specialtySympathetic Nervous SystemAdolescentVasodilator AgentsVasoactive intestinal peptideMuscle Smooth Vascularchemistry.chemical_compoundErectile DysfunctionInternal medicinemedicineHumansVeinProstaglandin E1AgedPapaverineDose-Response Relationship Drugbusiness.industryLinsidomineGeneral MedicineMiddle AgedElectric StimulationTransplantationmedicine.anatomical_structureEndocrinologychemistryDilatorRegression AnalysisbusinessPenisArterymedicine.drugClinical Science
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