Linagliptin for Type 2 Diabetes Mellitus: A Review of the Pivotal Clinical Trials.

Linagliptin for type 2 diabetes mellitus: a review of the pivotal clinical trials.

Filed under: Drug and Alcohol Rehabilitation

Ther Adv Endocrinol Metab. 2012 Aug; 3(4): 113-24
McGill JB

Patients with type 2 diabetes mellitus (T2DM) frequently require multiple therapies to effectively control hyperglycemia, and many new agents for glucose control have been developed over the past few decades. Linagliptin is a recently approved oral antidiabetic drug that acts by inhibiting the enzyme dipeptidyl peptidase-4 (DPP-4). Unlike other DPP-4 inhibitors, linagliptin is excreted chiefly via the enterohepatic system, and can be used without dose adjustment in patients with renal or hepatic impairment. Linagliptin was approved by the US Food and Drug Administration based on a large development program, including four pivotal trials in patients with T2DM, assessing the efficacy and safety of linagliptin when used as monotherapy or in combination with other oral antidiabetes drugs. Linagliptin was associated with significant improvements in glycosylated hemoglobin, fasting plasma glucose and postprandial glucose, and more patients receiving linagliptin showed meaningful improvements and achieved targets for glycosylated hemoglobin. Linagliptin was well tolerated, with an adverse event profile similar to that of placebo, and low rates of hypoglycemic events. Taken together, the pivotal trials confirm linagliptin is effective and safe in patients with T2DM: the convenience of oral dosing with no requirement for dose adjustment in patients with renal or hepatic impairment make linagliptin a valuable option when considering therapies for patients with T2DM.
HubMed – drug

Recurrent mesalazine-induced myopericarditis in a patient with ulcerative colitis.

Filed under: Drug and Alcohol Rehabilitation

J Cardiovasc Ultrasound. 2012 Sep; 20(3): 154-6
Park EH, Kim BJ, Huh JK, Jeong EH, Lee SH, Bang KB, Seol JS, Sung JW, Kim BS, Kang JH

Inflammatory bowel disease (IBD) is considered as a dysregulated immune mediated disease. Pericarditis in IBD is a very rare disease both as an extra-intestinal manifestation of IBD and an adverse reaction of therapeutic drug for IBD such as mesalazine or sulfasalazine. A 26-year-old IBD male patient who had been taking mesalazine regularly for about 1 month was referred to our hospital because of fever, chest discomfort, and abnormal electrocardiographic findings. The patients was diagnosed as acute myopericarditis, and recovered after cessation of mesalazine using steroid and aspirin. When mesalazine was re-medicated some days after discharge, he suffered from myopericarditis again. Subsequently, myopericarditis was resolved just after cessation of mesalazine again. These findings suggest that the development of myopericarditis is caused by mesalazine.
HubMed – drug

Dendrimer-Fullerenol Soft-Condensed Nanoassembly.

Filed under: Drug and Alcohol Rehabilitation

J Phys Chem C Nanomater Interfaces. 2012 Jul 26; 116(29): 15775-15781
Bhattacharya P, Kim SH, Chen P, Chen R, Spuches AM, Brown JM, Lamm MH, Ke PC

Nanoscale assembly is an area of research that has vast implications for molecular design, sensing, nanofabrication, supramolecular chemistry, catalysis, and environmental remediation. Here we show that poly(amidoamine) (PAMAM) dendrimers of both generations 1 (G1) and 4 (G4) can host 1 fullerenol per 2 dendrimer primary amines as evidenced by isothermal titration calorimetry, dynamic light scattering and spectrofluorometry. Thermodynamically, the interactions were similarly spontaneous between both generations of dendrimers and fullerenols, however, G4 formed stronger complexes with fullerenols resulting from their higher surface charge density and more internal voids, as demonstrated by spectrofluorometry. In addition to hydrogen bonding that existed between the dendrimer primary amines and the fullerenol oxygens, hydrophobic and electrostatic interactions also contributed to complex formation and dynamics. Such hybrid of soft and condensed nanoassembly may have implications for environmental remediation of discharged nanomaterials and entail new applications in drug delivery.
HubMed – drug

Hierarchical unilamellar vesicles of controlled compositional heterogeneity.

Filed under: Drug and Alcohol Rehabilitation

PLoS One. 2012; 7(11): e50156
Hadorn M, Boenzli E, Eggenberger Hotz P, Hanczyc MM

Eukaryotic life contains hierarchical vesicular architectures (i.e. organelles) that are crucial for material production and trafficking, information storage and access, as well as energy production. In order to perform specific tasks, these compartments differ among each other in their membrane composition and their internal cargo and also differ from the cell membrane and the cytosol. Man-made structures that reproduce this nested architecture not only offer a deeper understanding of the functionalities and evolution of organelle-bearing eukaryotic life but also allow the engineering of novel biomimetic technologies. Here, we show the newly developed vesicle-in-water-in-oil emulsion transfer preparation technique to result in giant unilamellar vesicles internally compartmentalized by unilamellar vesicles of different membrane composition and internal cargo, i.e. hierarchical unilamellar vesicles of controlled compositional heterogeneity. The compartmentalized giant unilamellar vesicles were subsequently isolated by a separation step exploiting the heterogeneity of the membrane composition and the encapsulated cargo. Due to the controlled, efficient, and technically straightforward character of the new preparation technique, this study allows the hierarchical fabrication of compartmentalized giant unilamellar vesicles of controlled compositional heterogeneity and will ease the development of eukaryotic cell mimics that resemble their natural templates as well as the fabrication of novel multi-agent drug delivery systems for combination therapies and complex artificial microreactors.
HubMed – drug

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