Search results for "drug evaluation"

showing 10 items of 188 documents

Photochemotherapy Alone or Combined with Interferon Alpha-2a in the Treatment of Cutaneous T-Cell Lymphoma

1990

Eighty-two patients with either mycosis fungoides (MF) or parapsoriasis en plaques were treated with psoralens ultraviolet A light (PUVA). Clinical and histologic parameters were followed for a period from 6 months to 10 years. Complete clinical clearing of lesions was observed in 51 patients (62%) and most of them were in limited-plaque MF group or parapsoriasis en plaque. The mean total dose of PUVA for complete clearing was less for early MF. Thirty-one patients (38%) relapsed and responded to additional PUVA. Patients in early stages of the disease remained clear for up to 68 months after the first course of PUVA. Post-treatment skin biopsies with early MF showed histologic clearing. A …

AdultMalemedicine.medical_specialtySkin NeoplasmsCombination therapyConstitutional symptomsDermatologyInterferon alpha-2BiochemistryMycosis FungoidesInterferonmedicineHumansSezary SyndromePUVA TherapyMolecular BiologyDepression (differential diagnoses)AgedNeoplasm StagingMycosis fungoidesParapsoriasisbusiness.industryCutaneous T-cell lymphomaInterferon-alphaCell BiologyMiddle Agedmedicine.diseaseCombined Modality TherapyDermatologyRecombinant ProteinsLymphoma T-Cell CutaneousDrug EvaluationFemalebusinessProgressive diseasemedicine.drugJournal of Investigative Dermatology
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Systemic Treatment with Interferon-α2B: An Effective Method to Prevent Sterility after Bilateral Mumps Orchitis

1991

In men orchitis represents the most common complication of mumps infection and occurs in 5 to 37% of this population. Bilateral manifestation is observed in 16 to 65% of the patients. The most important danger is the risk of testicular atrophy which results in sterility. Four patients with bilateral mumps orchitis received systemic treatment with interferon-alpha 2B (3 x 10(6) IU per day) for 7 days. All acute symptoms of mumps orchitis disappeared within 2 to 4 days of hospitalization. During 6 to 15 months of followup no incidence of testicular atrophy was observed. In 3 of 4 patients pre-treatment examination revealed subfertility (oligoasthenospermia), while 2 to 4 months after interfer…

AdultMalemedicine.medical_specialtyUrologyPopulationAlpha interferonOrchitisInterferon alpha-2TestismedicineHumansProspective StudiesRadionuclide ImagingAdverse effecteducationMumpsInfertility MaleInterferon alfaAcetaminophenUltrasonographyeducation.field_of_studyPalpationTesticular atrophybusiness.industryInterferon-alphamedicine.diseaseRecombinant ProteinsSurgeryConcomitantDrug EvaluationOrchitisComplicationbusinessmedicine.drugJournal of Urology
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Pharmacokinetics of Droloxifene and Its Metabolites in Breast Cancer Patients

1991

Pharmacokinetics and metabolism of droloxifene, a new antiestrogenic drug, have been investigated by single- and multiple-dose studies in postmenopausal patients with advanced breast cancer. Short terminal elimination half-life, low accumulation, and improved drug tolerability are the most striking features of this safe and effective new antiestrogen. Bioequivalence of film-coated tablet, tablet, and standard solution of droloxifene has been shown. The concentrations of droloxifene and its metabolites have been determined by a highly selective HPLC method.

AdultOncologyDrugCancer Researchmedicine.medical_specialtymedia_common.quotation_subjectAdministration OralBiological AvailabilityAntineoplastic AgentsBreast NeoplasmsBioequivalenceBreast cancerPharmacokineticsInternal medicinemedicineHumansChromatography High Pressure LiquidAgedmedia_commonAged 80 and overbusiness.industryEstrogen AntagonistsCancerMiddle AgedAntiestrogenmedicine.diseaseTamoxifenOncologyTolerabilityDroloxifeneDrug EvaluationFemalebusinessHalf-LifeAmerican Journal of Clinical Oncology
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Screening of pharmacologic adulterant classes in herbal formulations using voltammetry of microparticles.

2013

A solid state electrochemical method for screening different families of adulterant chemicals illegally added to commercial phytotherapuetic formulations is described. The proposed method, based on the voltammetry of microparticles approach, permits a fast and sensitive way to distinguish between anorexics (amfepramone, fenproporex, sibutramine), benzozodiazepinic anxiolytics (clonazepam, flurazepam, alprazolam, midazolam, medazepam, chlordiazepoxide, diazepam), antidepressants (bupropione, fluoxetine, sertraline, paroxetine), diuretics (hydrochlorothiazide, furosemide, chlortalidone, amiloride, spironolactone), and hypoglycemics (glimepiride, chlorpropamide, glibenclamide) based on charact…

AdulterantChromatographyFlurazepamChemistryChemistry PharmaceuticalClinical BiochemistryAmfepramoneDrug Evaluation PreclinicalPharmaceutical ScienceElectrochemical TechniquesPharmacologyFenproporexMicrospheresAnalytical ChemistryMedazepamGlimepirideHydrochlorothiazideDrug DiscoverymedicinePlant PreparationsDrug ContaminationDiazepamSpectroscopymedicine.drugJournal of pharmaceutical and biomedical analysis
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Fingolimod as a Treatment in Neurologic Disorders Beyond Multiple Sclerosis

2020

Abstract Fingolimod is an approved treatment for relapsing–remitting multiple sclerosis (MS), and its properties in different pathways have raised interest in therapy research for other neurodegenerative diseases. Fingolimod is an agonist of sphingosine-1-phosphate (S1P) receptors. Its main pharmacologic effect is immunomodulation by lymphocyte homing, thereby reducing the numbers of T and B cells in circulation. Because of the ubiquitous expression of S1P receptors, other effects have also been described. Here, we review preclinical experiments evaluating the effects of treatment with fingolimod in neurodegenerative diseases other than MS, such as Alzheimer’s disease or epilepsy. Fingolimo…

AgonistSphingosine 1 Phosphate Receptor ModulatorsMultiple Sclerosismedicine.drug_classDrug Evaluation PreclinicalDiseaseReview ArticleRM1-950PharmacologyNeuroprotection03 medical and health sciencesEpilepsyMice0302 clinical medicineNeurotrophic factorsAlzheimer DiseasemedicineAnimalsHumansLymphocytes030304 developmental biologyPharmacology0303 health sciencesEpilepsyMicrogliabusiness.industryFingolimod HydrochlorideMultiple sclerosisAnti-Inflammatory Agents Non-Steroidalmedicine.diseaseFingolimod3. Good healthRatsDisease Models Animalmedicine.anatomical_structureNeuroprotective AgentsTherapeutics. PharmacologyNervous System Diseasesbusiness030217 neurology & neurosurgerymedicine.drugDrugs in R&D
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Synthesis and antioxidant evaluation of novel silybin analogues

2006

In this work, we evaluated the antioxidant properties of the eight novel silybin analogues for their capacity to scavenge free radicals including superoxide anion radicals and 1,1-diphenyl-2-picrylhydrazyl (DPPH) radicals in vitro. Compound 7d demonstrated an excellent antioxidant effect in scavenging superoxide anion free radical with an IC50 value of 26.5 microM, while the IC50 of quercetin (the reference compound) was 38.1 microM. Compounds 7b, 7e, 7h showed certain scavenging activities for both types of free radicals.

AnionsAntioxidantDPPHRadicalmedicine.medical_treatmentDrug Evaluation PreclinicalMedicinal chemistryAntioxidantsInhibitory Concentration 50chemistry.chemical_compoundPicratesSuperoxidesDrug DiscoverymedicineOrganic chemistryIC50PharmacologyDose-Response Relationship DrugSuperoxideBiphenyl CompoundsAnion radicalsFree Radical ScavengersGeneral MedicineIn vitroHydrazinesModels ChemicalchemistrySpectrophotometrySilybinQuercetinQuercetinSilymarinJournal of Enzyme Inhibition and Medicinal Chemistry
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Synthesis of new 2,3-diaryl-1,3-thiazolidin-4-ones as anti-HIV agents

2004

Several 2,3-diaryl-1,3-thiazolidin-4-ones were synthesized and evaluated as anti-HIV agents. The results of the in vitro tests showed that some of them were highly effective inhibitors of HIV-1 replication at 30-50 nM concentrations with minimal cytotoxicity, thereby acting as non-nucleoside HIV-1 reverse transcriptase inhibitors (NNRTIs).

Anti-HIV activity23-diaryl-13-thiazolidin-4-oneAnti-HIV AgentsCell SurvivalT-LymphocytesDrug Evaluation PreclinicalPharmaceutical SciencePharmacologyVirus ReplicationStructure-Activity RelationshipDrug DiscoveryStructure–activity relationshipHumansCytotoxicityCell survivalAnti hiv activityMolecular StructureAnti hivChemistryvirus diseasesSettore CHIM/08 - Chimica FarmaceuticaReverse transcriptaseIn vitroThiazolesViral replicationHIV-2HIV-1NNRTIsReverse Transcriptase Inhibitors
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Effect of selected triterpenoids on chronic dermal inflammation.

1997

The activity of four natural triterpenoids on a 12-O-tetradecanoylphorbol-13-acetate multiple-dose model of skin chronic inflammation was studied. Erythrodiol and ursolic acid were significantly effective. The most important features concerning structure-activity relationship and previous data on the effect of these triterpenoids on other inflammatory conditions are discussed.

Anti-Inflammatory AgentsDrug Evaluation PreclinicalInflammationPharmacologyDermatitis ContactDexamethasonechemistry.chemical_compoundMiceTriterpenoidDermisUrsolic acidTriterpeneEdemamedicineAnimalsOleanolic AcidBetulinic AcidDexamethasonePharmacologychemistry.chemical_classificationintegumentary systembusiness.industryTriterpenesmedicine.anatomical_structurechemistryImmunologyTetradecanoylphorbol AcetateFemalemedicine.symptombusinessPentacyclic Triterpenesmedicine.drugEuropean journal of pharmacology
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DHFR Inhibitors: Reading the Past for Discovering Novel Anticancer Agents.

2019

Dihydrofolate reductase inhibitors are an important class of drugs, as evidenced by their use as antibacterial, antimalarial, antifungal, and anticancer agents. Progress in understanding the biochemical basis of mechanisms responsible for enzyme selectivity and antiproliferative effects has renewed the interest in antifolates for cancer chemotherapy and prompted the medicinal chemistry community to develop novel and selective human DHFR inhibitors, thus leading to a new generation of DHFR inhibitors. This work summarizes the mechanism of action, chemical, and anticancer profile of the DHFR inhibitors discovered in the last six years. New strategies in DHFR drug discovery are also provided, …

AntifungalCancer chemotherapymedicine.drug_classDrug Evaluation Preclinicaldihydrofolate reductase (DHFR) enzymePharmaceutical ScienceAntineoplastic AgentsComputational biologyReview01 natural scienceshybrid compoundsAnalytical Chemistrylcsh:QD241-44103 medical and health sciencesStructure-Activity RelationshipFolic Acidlcsh:Organic chemistryheterocyclic compoundsNeoplasmsDihydrofolate reductaseparasitic diseasesDrug DiscoverymedicineAnimalsHumansPhysical and Theoretical Chemistry030304 developmental biology0303 health sciencesHeterocyclic compoundbiology010405 organic chemistryDrug discoveryOrganic ChemistryDHFR inhibitors as anticancer agentSettore CHIM/08 - Chimica Farmaceutica0104 chemical sciencesDHFR drug discoveryTetrahydrofolate DehydrogenaseMechanism of actionChemistry (miscellaneous)Settore CHIM/03 - Chimica Generale E InorganicaDHFR inhibitors as anticancer agentsbiology.proteinMolecular MedicineFolic Acid Antagonistsmedicine.symptomMolecules (Basel, Switzerland)
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Efficacy of the antioxidant ebselen in experimental uveitis.

1999

Inflammation results in the production of free radicals. In a model of experimental uveitis upon subcutaneous injection of endotoxin to Lewis rats, i.e., endotoxin-induced experimental uveitis (EIU), we have evaluated the status of the antioxidant capacity of ocular tissues. EIU results in a decrease of glutathione (GSH) content and glutathione peroxidase (GPx) activity in whole eye homogenates 24-h after endotoxin administration. Furthermore, an increase in malondialdehyde (MDA) content was observed in these same samples, thus confirming the involvement of oxidative stress in the pathophysiology of the process. In view of the ability of the antioxidant ebselen as GPx enzyme mimic, we teste…

AzolesAntioxidantFree Radicalsmedicine.medical_treatmentDrug Evaluation PreclinicalPharmacologyIsoindolesmedicine.disease_causeBiochemistryAntioxidantsUveitischemistry.chemical_compoundSubcutaneous injectionPhysiology (medical)MalondialdehydeOrganoselenium CompoundsmedicineEscherichia coliAnimalschemistry.chemical_classificationGlutathione PeroxidaseEbselenGlutathione peroxidaseAnti-Inflammatory Agents Non-SteroidalGlutathioneMalondialdehydeGlutathioneeye diseasesRatsEndotoxinsBiochemistrychemistryRats Inbred Lewsense organsPeroxynitriteOxidative stressFree radical biologymedicine
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