Search results for "Narcotic Antagonists"

showing 4 items of 34 documents

Sensitivity of neuronal nicotinic acetylcholine receptors to the opiate antagonists naltrexone and naloxone: receptor blockade and up-regulation

2003

In HEK293 cells stably expressing alpha4beta2 nAChRs, naltrexone, but not naloxone, blocked alpha4beta2 nAChRs via an open-channel blocking mechanism. In primary hippocampal cultures, naltrexone inhibited alpha7 nAChRs up-regulated by nicotine, and in organotypic hippocampal cultures naltrexone caused a time-dependent up-regulation of functional alpha7 nAChRs that was detected after removal of the drug. These results indicate that naltrexone could be used as a smoking cessation aid.

NicotinePatch-Clamp TechniquesTime FactorsNarcotic AntagonistsClinical BiochemistryGene ExpressionPharmaceutical Science(+)-NaloxoneReceptors NicotinicPharmacologyHippocampal formationSensitivity and Specificitycomplex mixturesBiochemistryNaltrexoneCell LineNicotineStructure-Activity Relationshipmental disordersDrug DiscoverymedicineHumansMolecular BiologyAcetylcholine receptorNeuronsNaloxoneChemistryNarcotic antagonistmusculoskeletal neural and ocular physiologyOrganic ChemistryNaltrexoneUp-RegulationNicotinic agonistnervous systemMechanism of actionMolecular MedicineSmoking Cessationsense organsmedicine.symptommedicine.drugBioorganic & Medicinal Chemistry Letters
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Prolonged-release buprenorphine formulations: Perspectives for clinical practice

2020

International audience; Buprenorphine and methadone are the two main opioid agonist treatments approved for opioid use disorder. Buprenorphine is a partial agonist of the mu opioid receptors, which has been merely available through sublingual form until now. In practice, the use of buprenorphine is smoother than that of methadone, and it induces reduced risks of overdose. However, sublingual buprenorphine also exposes to risks (e.g., withdrawal, misuse) and constraints (e.g., daily intake). Three new galenic formulations of prolonged-release buprenorphine (PRB) are being commercialized and should allow some improvements in patients' comfort and safety. This narrative review aims to describe…

medicine.medical_specialtyDoseNarcotic Antagonists[SDV.MHEP.PSM] Life Sciences [q-bio]/Human health and pathology/Psychiatrics and mental healthReceptors Opioid mu030226 pharmacology & pharmacyPartial agonistOpioid dependenceDependance aux opioides03 medical and health sciencesSubcutaneous injection0302 clinical medicineProlonged releasemedicineHumansProlonged-releasePharmacology (medical)OpiacésAction prolongeebusiness.industryOpioid use disorderOpioid-Related Disordersmedicine.disease3. Good healthBuprenorphineAnalgesics OpioidOpiatesOpioid[SDV.MHEP.PSM]Life Sciences [q-bio]/Human health and pathology/Psychiatrics and mental healthEmergency medicinebusinessSubstitutionMethadoneBuprenorphinemedicine.drugMethadone
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The future: critical knowledge about anti-itch therapy.

2005

:  Itch is an extremely frequent and enervating symptom of many diseases. Current anti-itch therapy, which is based almost exclusively on an “immunocentric” viewpoint, is often unsatisfactory. Recent studies show that this symptom is in fact the result of a complex interplay among skin, nervous system, endocrine system, and immune system. This explains the frequent failure of therapeutic strategies focused only on a single factor and suggests the usefulness of a polypharmacologic symptomatic treatment, designed on a case-by-case basis as a result of a multidisciplinary approach. We discuss the perspectives of anti-itch therapy in light of the new pathogenetic and pharmacologic acquisitions.

medicine.medical_specialtybusiness.industryNarcotic AntagonistsPruritusSymptomatic treatmentSingle factorDermatologyGeneral MedicineAntipruriticsMultidisciplinary approachImmunologyNeural PathwaysmedicineHumansDrug Therapy CombinationProtease InhibitorsCapsaicinIntensive care medicinebusinessDermatologic therapy
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Therapies in early development for the treatment of opiate addiction.

2015

Opiate drugs are psychoactive substances used to manage severe pain. However, their chronic use is associated with the development of addiction. Opiate addiction represents a significant public health concern.This review focuses on the most recent advances in the pharmacological treatment of opiate addiction, from those being tested in clinical trials (Phase I and II), to preclinical studies that point to new targets. Readers will gain knowledge of the wide variety of treatments used to treat opiate addiction, including their strengths and weaknesses, and the promising pharmacological targets identified by preclinical research.Among the currently available agonist therapies, new dosage form…

medicine.medical_specialtymedia_common.quotation_subjectNarcotic AntagonistsNaltrexonePharmacological treatmentmedicineAnimalsHumansPharmacology (medical)Molecular Targeted TherapyPsychiatrymedia_commonPharmacologybusiness.industryAddictionGeneral MedicineOpioid-Related DisordersNaltrexoneBuprenorphineClinical trialAnalgesics OpioidDrug DesignOpiate addictionOpiatebusinessmedicine.drugMethadoneBuprenorphineExpert opinion on investigational drugs
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