Oral opioids are the treatment of choice for chronic cancer pain. Morphine is the strong opioid of choice for the treatment of moderate to severe cancer pain according to guidelines from the World Health Organization (WHO). This recommendation by the WHO was derived from availability, familiarity to clinicians, established effectiveness, simplicity of administration, and relative inexpensive co...

BACKGROUND Osteoarthritis is the most common form of joint disease and the leading cause of pain and physical disability in the elderly. Opioids may be a viable treatment option if patients suffer from severe pain or if other analgesics are contraindicated. However, the evidence about their effectiveness and safety is contradictory. OBJECTIVES To determine the effects on pain and function and...

Investigations of the effects of valinomycin on mitochondria" 2 led to the discovery of antibiotic-mediated ion transport.3 Subsequent work revealed that this property is shared by valinomycin, the enniatins, the macrolide actins, and the gramicidins, including an extensive array of natural and synthetic analogues.4-6 Passive ion permeability effects have been reported obtained with these agent...

The proton-translocating F1F0 ATP synthase from Clostridium thermoautotrophicum was solubilized from cholate-washed membranes with Zwittergent 3-14 at 58 degrees C and purified in the presence of octylglucoside by sucrose gradient centrifugation and ion-exchange chromatography on a DEAE-5PW column. The purified enzyme hydrolyzed ATP at a rate of 12.6 micromol min(-1) mg(-1) at 58 degrees C and ...

AMP-dependent kinase (AMPK) and GLUT1-mediated sugar transport in blood-brain barrier endothelial cells are activated during acute cellular metabolic stress. Using murine brain microvasculature endothelium bEnd.3 cells, we show that AMPK phosphorylation and stimulation of 3-O-methylglucose transport by the AMPK agonist AICAR are inhibited in a dose-dependent manner by the AMPK antagonist Compou...

Pain is characterized by its multi-dimensional nature, explaining in part why the pharmacokinetic/pharmacodynamic (PK/PD) relationships are not straightforward for analgesics. The first part of this MiniReview gives an overview of PK, PD and PK/PD models, as well as of population approach used in analgesic studies. The second part updates the state-of-the-art in the PK/PD relationship of opioid...

Agonist-selective actions of opioids on the desensitization of -opioid receptors (MORs) have been well characterized, but few if any studies have examined agonist-dependent recovery from desensitization. The outward potassium current induced by several opioids was studied using whole-cell voltage-clamp recordings in locus ceruleus neurons. A brief application of the irreversible opioid antagoni...

Descrição do método de coleta de evidência Este estudo revisou artigos nas bases de dados do MEDLINE (PubMed) e demais fontes de pesquisa sem limite de tempo. Para tanto, adotou-se a estratégia de busca baseada em perguntas estruturadas na forma (P.I.C.O.) das seguintes iniciais: “Paciente”; “Intervenção”; “Controle”; “Outcome”. Como descritores, utilizaram-se: Pergunta 1: low back pain AND (an...

Background: Chronic pain affects many Americans, yet treatment of pain remains inadequate due in part to clinician beliefs and knowledge regarding the best ways to manage pain and concern for misuse. 1 In April 2011 the FDA announced, in concert with the White House ONDCP, a new risk reduction program, Approved Risk Evaluation and Mitigation Strategies (REMS), for all extended-release and long-...