Current Pharmaceutical Design - Volume 18, Issue 37, 2012

Opioids induce respiratory depression via activation of μ-opioid receptors at specific sites in the central nervous system including the pre-Bötzinger complex, a respiratory rhythm generating area in the pons. Full opioid agonists like morphine and fentanyl affect breathing with onset and offset profiles that are primarily determined by opioid transfer to the receptor site, while the effects of partial opioid agonists such as buprenor Read More

Opioid consumption is associated with a wide range of side effects. Potential interference of opioids with bone and joint activity has emerged in the last few years. Opioids increase the risk of fracture, especially in elderly patients. Moreover, opioids interfere with the endocrine system, and their chronic use is a recognized risk factor for osteoporosis. Pathogenetic mechanisms at the basis of the interference of opioids with bones Read More

The therapeutic action of opioid analgesics is compromised by peripheral adverse effects among which opioid-induced constipation (OIC) is the most disabling, with a prevalence reported to vary between 15 and 90 %. Although OIC is usually treated with laxatives, there is insufficient clinical evidence that laxatives are efficacious in this indication. In contrast, there is ample evidence from double- blind, randomized and placeb Read More

Administration of opioids for analgesia may produce pruritus. It was believed, that this effect is mediated centrally by activation of μ-opioid receptors (MOR). However, recent data suggested that opioids may also mediate pruritus directly in the skin. A number of skin cell types, including keratinocytes, dermal mast cells, fibroblasts or macrophages, were shown to express both MOR as well as other opioid receptors. It was Read More

The exact effect of opioid analgesics on sleep is to be determined. Although literature data are sporadically reported, the aim of this review is to summarize the already known effects of such medications on sleep. A variety of effects, both positive and negative, has been suggested, when opioids are used for pain treatment, but in the absence of pain as well. Although often thought to promote restful sleep, the reality is mu Read More

This review provides an overview of the immunological effects of commonly used analgesic opioid drugs, focusing mainly on two aspects: the mechanisms involved and the potential clinical relevance. The immunomodulatory effects of morphine have been characterized in animal and human studies. Morphine decreases the effectiveness of both natural and acquired immunity, interfering with intracellular pathways inv Read More

Nausea and vomiting are common gastrointestinal symptoms following opioid administration, for either chronic or acute pain management. As a consequence, patients’ dissatisfaction has a negative impact on treatment efficacy. A number of mechanisms have been identified, involving both central and peripheral sites. This article will review the pathophysiology of opioid-induced nausea and vomiting and the various pharmac Read More

Opioids are the gold standard for pain treatment but systemic opioid use is accompanied by central and intestinal side effects. As opioid receptors are expressed on peripheral sensory nerve endings, cutaneous and immune cells, local opioid application is being used for pain reduction in patients with inflammatory lesions such as burns, skin grafts, arthritis, acute or chronic wounds. In addition, peripherally active opioids h Read More

Opioids are among the oldest known and most widely used analgesics. The application of opioids has expanded over the last few decades, especially in the treatment of chronic non-malignant pain. This upsurge in opioid use has been accompanied by the increasingly recognized occurrence of opioid-associated endocrinopathy. This may arise after exposure to enteral, parenteral, or neuraxial opioids. Opioid-associ Read More

Opioids are increasingly used to manage not only acute but also chronic pain and heroine addiction. These patients usually receive many other medications that can interfere with the effects of opioids and vice versa. Patients often need combinations of drugs for their pain management, for treating opioid-related adverse effects or for other indications including depression and anxiety. Several antibiotics can also have interac Read More

Opioid peptides and their G protein-coupled receptors (GPCRs) are important regulators within the cardiovascular system, implicated in modulation of electrophysiological function, heart rate, myocardial inotropy, vascular function, and cellular stress resistance. The opioid system is also involved in cardiovascular development, adaptation to injury and effects of advanced age. The significant roles of opioids are emphasized by the Read More

Inadequate blood flow in the retina (ischemia) is a common cause of visual impairment and blindness. Retinal ischemia plays a pivotal role in a number of ocular degenerative diseases such as diabetic retinopathy, glaucoma, and retinal artery occlusion. The sequence of events by which ischemia leads to retinal degeneration are not completely understood, but likely involve both necrotic and apoptotic processes. A variety Read More

Abuse-deterrent opioid formulations are receiving renewed interest in light of the increasing legitimate medical use of prescription opioids for the adequate treatment of pain. Unfortunately, there is an inevitable associated potential for misuse, diversion, and abuse. The challenges of deterrence are significant: opioid abusers are a heterogeneous population; studies on drug “liking” and opioid “attractiveness” are infor Read More

Opioids constitute the basis for pharmacological treatment of moderate to severe pain in cancer pain and non-cancer pain patients. Their action is mediated by the activation of opioid receptors, which integrates the pain modulation system with other effects in the central nervous system including cognition resulting in complex interactions between pain, opioids and cognition. The literature on this complexity is sparse and Read More

Nampt/Visfatin/PBEF is a primary, rate-limiting enzyme involved in NAD+ biosynthesis, which serves as a pivotal substance for proteins, and is required for cell growth, survival, DNA replication and repair and energy metabolism. Growing researches have elucidated that it is a pleiotropic protein that functions not only as an enzyme, but also as an adipocytokin, a growth factor, and a cytokine. Additionally, accumulated evi Read More

This work presents the development of quantitative structure activity relationship (QSAR) model to predict the antimalarial activity of artemisinin derivatives. The structures of the molecules are represented by chemical descriptors that encode topological, geometric, and electronic structure features. Screening through QSAR model suggested that compounds A24, A24a, A53, A54, A62 and A64 possess significant antimalarial Read More

Lung cancer, of which non-small-cell lung cancer (NSCLC) is the most common form, remains the leading cause of cancerrelated mortality worldwide, with many patients presenting with advanced disease at initial diagnosis. In advanced NSCLC patients whose tumors harbor activating epidermal growth factor receptor (EGFR) mutations, the use of EGFR tyrosine kinase inhibitors (TKIs) as first-line treatment has provided Read More

In the last two decades a tremendous development has been noticed in our understanding of the purinergic system, consisting of heterogeneously expressed purinoceptor subtypes and its classical agonists: e.g., adenosine triphosphate, uridine triphosphate or complex dinucleoside polyphosphates. These agonists exert multiple effects on the vascular system: they regulate the relaxation and constriction of arterial bl Read More