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Available Drugs (available + drug)
Selected AbstractsBlood Pressure Components in Clinical HypertensionJOURNAL OF CLINICAL HYPERTENSION, Issue 9 2006Michel E. Safar MD This review offers a critical evaluation of the remarkable progress in antihypertensive therapy since its inception. Despite the introduction of newer, more sophisticated drugs, treatment results have remained stable. Problems impeding further improvement include limited patient compliance, clinical inertia, incomplete adherence to guidelines, and dependence on brachial artery cuff pressures for diagnosis, risk assessment, and treatment response. Brachial artery systolic and pulse pressures do not reliably represent aortic or carotid artery pressures, which are better risk predictors for the heart and brain. Mean pressure, which is the same throughout the arterial tree, is directly measurable by cuff oscillometry, and might become the best single risk predictor. Available drugs have limited ability to decrease the aortic stiffness that is responsible for the elevated systolic blood pressure of aging. Therefore, to improve risk assessment and therapeutic benefit, we might include mean blood pressure and pulse pressure into blood pressure measurements, pursue efforts to measure central blood pressure, and search for new drugs to reduce arterial stiffness. [source] Adverse effects of conventional non-steroidal anti-inflammatory drugs on the upper gastrointestinal tractFUNDAMENTAL & CLINICAL PHARMACOLOGY, Issue 4 2003Michael J. S. Langman Abstract This article reviews the clinical and epidemiological features of conventional non-steroidal anti-inflammatory drug (NSAID) related peptic ulcer complications, and the associated risk factors. The degree of gastrointestinal toxicity varies widely between the available drugs and with dose of each. The risk of ulcer complications can however be reduced, and perhaps completely removed, by using the lowest dose of the least toxic member of the class. Enteric coating and other delayed release formulations have not been shown to reduce risk. Estimates of the imposed disease burden have varied widely, in part through assuming that risks in selected patient groups will necessarily translate to the general population. Nevertheless, the imposed disease burden is one of the largest associated with current drug treatment. Associated risk factors such as prior ulcer, corticosteroid use and concurrent aspirin as well as general cardiovascular disease will raise the likelihood of an ulcer complication in NSAID takers and non-takers. Therefore, strategies dependent on substituting COX-selective drugs will then be only partially successful. [source] Drugs Used to Treat Osteoporosis: The Critical Need for a Uniform Nomenclature Based on Their Action on Bone Remodeling,JOURNAL OF BONE AND MINERAL RESEARCH, Issue 2 2005B Lawrence Riggs MD Abstract There continues to be uncertainty about the classification of available drugs for treating osteoporosis. We find that grouping them into anti-catabolic and anabolic classes based on the mechanisms of their action on bone remodeling and fracture reduction removes ambiguities and provides a relatively straightforward classification. The recent introduction of teriparatide into clinical practice initiated the era of anabolic therapy for osteoporosis, but it is still unclear how to define an anabolic drug. All drugs that increase bone mass do so by affecting bone remodeling. When their mechanisms of action on bone remodeling and on fracture reduction are considered, we find that anti-osteoporotic drugs fall naturally into either anti-catabolic or anabolic classes. Anti-catabolic drugs increase bone strength and reduce fractures mainly by decreasing the number of bone multicellular units (BMUs). This reduces perforative resorption and preserves skeletal microarchitecture (by preventing further structural damage to trabecular bone and increased porosity in cortical bone induced by high bone remodeling). Reduction in bone remodeling by anti-catabolic drugs may increase bone mass moderately during the interval in which previously initiated BMUs are completing mineralization. Some anti-catabolic drugs may also enhance the formation phase of the remodeling cycle, but their major action is to reduce overall bone turnover (i.e., the number of BMUs in bone). In contrast, anabolic drugs increase bone strength and reduce fractures by substantially increasing bone mass as a result of an overall increase in the number of BMUs combined with a positive BMU balance (the magnitude of the formation phase is greater than that of the resorption phase). Some anabolic drugs also induce renewed modeling, increase periosteal apposition and repair of trabecular microstructure. We hope that this classification will serve as a starting point for continued discussion on the important issue of nomenclature. [source] Pharmacotherapy of allergic rhinitis: a pharmaco-economic approachALLERGY, Issue 1 2009S. Simoens This article reports on a systematic literature review of the costs of allergic rhinitis (AR), the economic value of pharmacotherapy of AR, and the factors affecting costs and economic value of pharmacotherapy. Included studies had carried out a cost-of-illness analysis, cost analysis, cost-effectiveness, cost-utility or cost-benefit analysis. Allergic rhinitis imposes a substantial economic burden on society, with indirect costs of productivity loss being larger than the direct healthcare costs. Cost estimates were biased because of difficulties of diagnosis; exclusion of patients who do not seek healthcare; exclusion of over-the-counter medication; difficulties in estimating productivity loss. There is limited evidence on costs of seasonal/perennial and intermittent/persistent AR. Little is known of the economic value of pharmacotherapy of AR, although levocetirizine appears to be cost-effective as compared with placebo. Economic evaluations suffered limitations from small sample sizes, short trial duration, lack of standardized effectiveness measure, restricted scope of costs. Finally, the economic value of pharmacotherapy of AR is influenced by the perspective of the economic evaluation, relative effectiveness and costs of available drugs, patient compliance with treatment. [source] Local anaesthetics and adjuvants , future developmentsANAESTHESIA, Issue 2010M. D. Wiles Summary The introduction of local anaesthesia some years after the first public demonstration of general anaesthesia not surprisingly created less excitement and interest amongst both the public and the medical profession. However, in its own way, a new revolution was happening. Local anaesthesia produced an increase in the choice of anaesthetic techniques available to practitioners and patients. In common with general anaesthesia, the choice of agents remained very limited for the first six decades, and interest in the practice of local, regional or central neuraxial blockade and the development of new techniques and drugs were hampered by perceived safety issues even as late as the second half of the 20th century. It is only in the last few years that, with an apparent renaissance in the use of local anaesthesia, the pace of development has picked up. As the use and range of techniques has increased, so has interest in solving some of the longstanding problems with the available drugs. [source] Mutation of surface residues to promote crystallization of activated factor XI as a complex with benzamidine: an essential step for the iterative structure-based design of factor XI inhibitorsACTA CRYSTALLOGRAPHICA SECTION D, Issue 10 2005Pramod Pandey Activated factor XI (FXIa) is a key enzyme in the amplification phase of the blood-coagulation cascade. Thus, a selective FXIa inhibitor may have lesser bleeding liabilities and provide a safe alternative for antithrombosis therapy to available drugs on the market. In a previous report, the crystal structures of the catalytic domain of FXIa (rhFXI370,607) in complex with various ecotin mutants have been described [Jin et al. (2005), J. Biol. Chem.280, 4704,4712]. However, ecotin forms a matrix-like interaction with rhFXI370,607 and is impossible to displace with small-molecule inhibitors; ecotin crystals are therefore not suitable for iterative structure-based ligand design. In addition, rhFXI370,607 did not crystallize in the presence of small-molecule ligands. In order to obtain the crystal structure of rhFXI370,607 with a weak small-molecule ligand, namely benzamidine, several rounds of surface-residue mutation were implemented to promote crystal formation of rhFXI370,607. A quadruple mutant of rhFXI370,607 (rhFXI370,607 -S434A,T475A,C482S,K437A) readily crystallized in the presence of benzamidine. The benzamidine in the preformed crystals was easily exchanged with other FXIa small-molecule inhibitors. These crystals have facilitated the structure-based design of small-molecule FXIa inhibitors. [source] Antimalarial drugs , host targets (re)visitedBIOTECHNOLOGY JOURNAL, Issue 3 2006Margarida Cunha-Rodrigues Abstract Every year, forty percent of the world population is at risk of contracting malaria. Hopes for the erradication of this disease during the 20th century were dashed by the ability of Plasmodium falciparum, its most deadly causative agent, to develop resistance to available drugs. Efforts to produce an effective vaccine have so far been unsuccessful, enhancing the need to develop novel antimalarial drugs. In this review, we summarize our knowledge concerning existing antimalarials, mechanisms of drug-resistance development, the use of drug combination strategies and the quest for novel anti-plasmodial compounds. We emphasize the potential role of host genes and molecules as novel targets for newly developed drugs. Recent results from our laboratory have shown Hepatocyte Growth Factor/MET signaling to be essential for the establishment of infection in hepatocytes. We discuss the potential use of this pathway in the prophylaxis of malaria infection. [source] | ||||||||||