Evaluation of the Structure-Activity Relationship of Rifabutin and Analogs: A Drug-Membrane Study.

Evaluation of the Structure-Activity Relationship of Rifabutin and Analogs: A Drug-Membrane Study.

Chemphyschem. 2013 Jul 2;
Pinheiro M, Pereira-Leite C, Arêde M, Nunes C, Caio JM, Moiteiro C, Giner-Casares JJ, Lúcio M, Brezesinski G, Camacho L, Reis S

This work focuses on the influence of rifabutin and two novel analogs, namely, N’-acetyl-rifabutin and N’-butanoyl-rifabutin, on the biophysical properties of lipid membranes. Monolayers and multilamellar vesicles composed of egg L-?-phosphatidylcholine:cholesterol in a molar ratio of 4:1 are chosen to mimic biological membranes. Several accurate biophysical techniques are used to establish a putative relationship between the chemical structure of the antimycobacterial compounds and their activity on the membranes. A combination of in?situ experimental techniques, such as Langmuir isotherms, Brewster angle microscopy, polarization-modulated infrared reflection-absorption spectroscopy, and small-angle X-ray scattering, is used to assess the drug-membrane interaction. A relationship between the effect of a drug on the organization of the membranes and their chemical structure is found and may be useful in the development of new drugs with higher efficacy and fewer toxic effects. HubMed – drug


Immunosuppression: What’s Standard and What’s New?

Semin Respir Crit Care Med. 2013 Jun; 34(3): 405-413
Witt CA, Hachem RR

Lung transplantation is the ultimate treatment option for patients with end-stage lung disease. Chronic rejection, in the form of bronchiolitis obliterans syndrome, and noncytomegalovirus infections are the major causes of morbidity and mortality beyond the first year after transplantation. Most lung transplant recipients are treated lifelong with a three-drug immunosuppression regimen consisting of a calcineurin inhibitor, an antimetabolite, and low-dose corticosteroids. However, induction and maintenance immunosuppression strategies vary widely between centers, and a consensus on the ideal management of this patient population remains elusive. Over the past 20 years, several studies comparing the calcineurin inhibitors cyclosporine and tacrolimus and other studies comparing the antimetabolites azathioprine and mycophenolate mofetil have been performed. Additionally, the role of mammalian target of rapamycin (mTOR) inhibitors in the treatment of lung transplant recipients and the utility of azithromycin to treat and prevent bronchiolitis obliterans syndrome are areas of active investigation. This review discusses induction and traditional maintenance immunosuppressive agents and regimens and the evidence that exists to help guide therapy. Newer research involving the use of mTOR inhibitors in place of calcineurin inhibitors or antimetabolites and azithromycin for the treatment and prevention of bronchiolitis obliterans syndrome is also explored. HubMed – drug


Mold Infections in Lung Transplant Recipients.

Semin Respir Crit Care Med. 2013 Jun; 34(3): 371-379
Bhaskaran A, Hosseini-Moghaddam SM, Rotstein C, Husain S

Fungal infections continue to produce morbidity and mortality in lung transplant recipients despite the widespread use of antifungal prophylaxis. There has been a decline in Candida infections but Aspergillus species predominate. Other mold pathogens including Fusarium, Scedosporium, and Zygomycetes also cause infections in lung transplant recipients. Furthermore, the widespread use of antifungal prophylaxis has prompted a delay in onset of Aspergillus infection in lung transplant recipients. Pulmonary parenchymal disease has become the most common manifestation of invasive aspergillosis. Among the risk factors pre- or posttransplant Aspergillus colonization is the most important risk factor reported in several retrospective studies. Recently posttransplant colonization has been implicated in the development of bronchiolitis obliterans syndrome. Other factors that have been reported include preceding cytomegalovirus infections, hypogammaglobulinemia, and single-lung transplantation. The risk factors for other mold infections such as Scedosporium, Fusarium, and Zygomycetes are not well studied. The best antimold prophylaxis strategy and choice of drug remains to be elucidated. Most lung transplant centers use either voriconazole or inhaled amphotericin preparations. However, data have emerged regarding the increased risk of squamous cell cancer in lung transplant recipients on voriconazole prophylaxis. Advances in the diagnosis and treatment of invasive aspergillosis have resulted in a significant decrease in mortality. HubMed – drug



09 Interview with Robert G Smith, the Creator of FasterEFT – In this video Keith Hulstaert interviews the Creator of FasterEFT, Robert G Smith and asks some frequently questions about FasterEFT. The video was filmed at…