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1.
J Pharm Technol ; 37(3): 147-151, 2021 Jun.
Artigo em Inglês | MEDLINE | ID: mdl-34752568

RESUMO

Objective: To review the safety and efficacy of apixaban for the treatment of nonvalvular atrial fibrillation or venous thromboembolism in patients receiving peritoneal dialysis (PD). Data Sources: A PubMed and MEDLINE search was conducted through December 2020 using the following keywords and Medical Subject Headings (MeSH) terms alone or in various combinations: apixaban, peritoneal dialysis, continuous ambulatory peritoneal dialysis, end-stage renal disease, and hemodialysis. Study Selection and Data Extraction: English-language studies evaluating clinical outcomes pertaining to the use of apixaban in end stage renal disease (ESRD), which included patients receiving peritoneal dialysis were eligible for inclusion. Data Synthesis: Four studies were identified that met inclusion for this review, all retrospective in nature. These studies compared the safety and efficacy of apixaban with standard therapy in ESRD included patients on dialysis, with a very limited number of subjects receiving PD. In these studies, apixaban was shown to be potentially safer and more effective than warfarin. Outcomes did not differentiate between patients receiving PD or not. Conclusions: Use of apixaban in patients receiving PD may be safe and effective based on data from limited patients. Pharmacokinetics and pharmacodynamics of apixaban in the PD setting is an important question that clinicians should consider with use of this medication in the ESRD population. More studies focusing on the PD population are needed to better assess the use of apixaban in this understudied population.

2.
Bioorg Med Chem Lett ; 29(18): 2690-2694, 2019 09 15.
Artigo em Inglês | MEDLINE | ID: mdl-31387791

RESUMO

As part of our on-going effort to explore the role of dopamine receptors in drug addiction and identify potential novel therapies for this condition, we have a identified a series of N-(4-(4-phenyl piperazin-1-yl)butyl)-4-(thiophen-3-yl)benzamide D3 ligands. Members of this class are highly selective for D3 versus D2, and we have identified two compounds (13g and 13r) whose rat in vivo IV pharmacokinetic properties that indicate that they are suitable for assessment in in vivo efficacy models of substance use disorders.


Assuntos
Benzamidas/farmacologia , Desenho de Fármacos , Piperazinas/farmacologia , Receptores de Dopamina D3/metabolismo , Animais , Benzamidas/síntese química , Benzamidas/química , Relação Dose-Resposta a Droga , Ligantes , Microssomos Hepáticos/química , Microssomos Hepáticos/metabolismo , Simulação de Acoplamento Molecular , Estrutura Molecular , Piperazinas/síntese química , Piperazinas/química , Ratos , Relação Estrutura-Atividade
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