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1.
Expert Rev Neurother ; 22(8): 639-653, 2022 08.
Artigo em Inglês | MEDLINE | ID: mdl-35913401

RESUMO

INTRODUCTION: Acute behavioral disturbances in psychosis, including agitation, comprise a heterogeneous group of manifestations varying in intensity and duration they last for. They require rapid, non-coercive treatments ranging from verbal de-escalation to the calming effect of pharmacological agents. The treatment goals are reduction of patient suffering and prevention of disease deterioration. Stabilizing rather than sedating is preferred to ensure improved compliance and a stronger therapeutic alliance. Furthermore, animal pharmacology and clinical studies on agitation reveal the robust calming and anxiolytic properties of loxapine. AREAS COVERED: This review covers the pharmacological and clinical history of loxapine along with research developments. It emphasizes the advantages of its multiple formulations ranging from injectable forms and tablets to orally inhaled forms to attain rapid and fine-tuned tranquilization. EXPERT OPINION: Rapid tranquillization is achieved within 2-6 hours using liquid orally-consumed loxapine, and within an hour or less with its IM or orally inhaled forms. Loxapine has been adopted in the management of a wide range of acute disturbances, such as agitation in psychosis. In the context of personalized medicine, key cellular and molecular elements of the schizophrenia phenotype were recently shown to be improved with loxapine.


Assuntos
Antipsicóticos , Transtorno Bipolar , Loxapina , Esquizofrenia , Administração por Inalação , Antipsicóticos/uso terapêutico , Transtorno Bipolar/tratamento farmacológico , Humanos , Loxapina/uso terapêutico , Agitação Psicomotora/tratamento farmacológico , Esquizofrenia/tratamento farmacológico
2.
Expert Opin Pharmacother ; 22(18): 2507-2519, 2021 Dec.
Artigo em Inglês | MEDLINE | ID: mdl-34338130

RESUMO

Antipsychotic (AP) dosing is well established in nonelderly patients with acute exacerbations of schizophrenia, but not in special populations.This review describes the AP dosing procedures that have been used in clinical studies for acute psychotic agitation, a first episode of psychosis (FEP), and elderly patients. AP dosing data was extracted from the databases of drug regulatory authorities, and from clinical studies available in the medical literature. In acute psychotic agitation, intramuscular and oral APs are frequently prescribed in higher doses than those that saturate D2 receptors. Supersaturating doses of APs should be avoided due to an increased risk of adverse effects. In FEP, many studies showed efficacy of low doses of APs. Studies with risperidone and haloperidol suggested a dose reduction of approximately one third. Titration with a lower starting dose is recommended in elderly patients, due to possible decreases in pharmacokinetic clearance, and due to the risk of concomitant diseases and drug interactions. Exposure to some APs has been associated with QTc prolongation and arrhythmias, and a small but significant increase in the risk of stroke and mortality with APs has been seen, particularly in older people with dementia-related psychosis.


Assuntos
Antipsicóticos , Transtornos Psicóticos , Esquizofrenia , Idoso , Antipsicóticos/efeitos adversos , Humanos , Agitação Psicomotora/tratamento farmacológico , Transtornos Psicóticos/tratamento farmacológico , Risperidona/uso terapêutico , Esquizofrenia/tratamento farmacológico
3.
Int J Neuropsychopharmacol ; 21(4): 355-360, 2018 04 01.
Artigo em Inglês | MEDLINE | ID: mdl-29106549

RESUMO

Background: The denomination of typical antipsychotic for loxapine has poor relation to current knowledge of the molecule's relevant modes of action. Materials and Methods: Competition binding experiments were performed on expressed human recombinant receptors in CHO cells and HEK-293 cells for D1 to D5, 5-HT1A, 5-HT2A, 5-HT2C, 5-HT4, 5-HT6, and 5-HT7. In vitro autoradiographies using [11C]-Raclopride [18F]-Altanserin [18F]-MPPF [11C]-SB207145, and [18F]-2FNQ1P were measured in brain tissue of a male primate followed by addition of increasing doses of loxapine succinate. Results: In cell cultures, the measured Kb confirmed high affinity of loxapine for the D2; intermediate affinity for the D1, D4, D5, 5-HT2C receptorsl and a lack of affinity toward D3, 5-HT1A, 5-HT4, 5-HT6, and 5-HT7 receptors. In brain tissue, PET autoradiographies showed a radiopharmaceutical displacement at low concentrations of loxapine on D2 and 5-HT2A receptors. Conclusion: This preclinical study reveals that loxapine receptorial spectrum is close to an "atypical" profile (D2/5HT2A ratio, 1.14). Loxapine is rightly classified as a DS-RAn agent in the Neuroscience Based Nomenclature classification.


Assuntos
Antipsicóticos/farmacocinética , Loxapina/farmacocinética , Receptores Dopaminérgicos/efeitos dos fármacos , Receptores de Serotonina/efeitos dos fármacos , Animais , Antipsicóticos/classificação , Células CHO , Cricetulus , Células HEK293 , Humanos , Loxapina/classificação , Tomografia por Emissão de Pósitrons , Compostos Radiofarmacêuticos
4.
Biophys J ; 84(3): 2058-70, 2003 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-12609907

RESUMO

Cell adhesion requires nanometer scale membrane alignment to allow contact between adhesion receptors. Little quantitative information is presently available on this important biological process. Here we present an interference reflection microscopic study of the initial interaction between monocytic THP-1 cells and adhesive surfaces, with concomitant determination of cell deformability, using micropipette aspiration, and adhesiveness, using a laminar flow assay. We report that 1), during the first few minutes after contact, cells form irregular-shaped interaction zones reaching approximately 100 micro m(2) with a margin extension velocity of 0.01-0.02 micro m/s. This happens before the overall cell deformations usually defined as spreading. 2), These interference reflection microscopic-detected zones represent bona fide adhesion inasmuch as cells are not released by hydrodynamic forces. 3), Alignment is markedly decreased but not abolished by microfilament blockade with cytochalasin or even cell fixation with paraformaldehyde. 4), In contrast, exposing cells to hypotonic medium increased the rate of contact extension. 5), Contacts formed in presence of cytochalasin, after paraformaldehyde fixation or in hypotonic medium, were much more regular-shaped than controls and their extension matched cell deformability. 6), None of the aforementioned treatments altered adhesiveness to the surface. It is concluded that adhesive forces and passive membrane deformations are sufficient to generate initial cell alignment to adhesive surfaces, and this process is accelerated by spontaneous cytoskeletally-driven membrane motion.


Assuntos
Membrana Celular/química , Membrana Celular/fisiologia , Fluidez de Membrana/fisiologia , Fusão de Membrana/fisiologia , Monócitos/citologia , Monócitos/fisiologia , Polilisina/química , Adesão Celular/fisiologia , Polaridade Celular/fisiologia , Tamanho Celular , Células Cultivadas , Materiais Revestidos Biocompatíveis/química , Elasticidade , Humanos , Microscopia de Interferência/métodos , Monócitos/química , Estresse Mecânico
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