Menopause is accompanied by accelerated bone loss, and increasing incidence of fractures. Several studies have shown that hormone replacement therapy (HRT) can reduce bone loss, increase bone mineral density, and decrease the risk of fracture. However, the duration of treatment needed and of the protective effect after treatment is stopped, and the influence of age [...]
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Carbamazepine (CBZ) is considered as the primary drug for the treatment of partial and tonic-clonic seizures. It is also the drug of choice for trigeminal neuralgia and frequently used for treating bipolar depression. The originator patent expired long ago (in 1986) and there are now several generic alternatives. However, after the introduction of the generic [...]
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The cytochrome P450 3A enzymes (CYP3A4 and CYP3A5) participate in the biotransformation of approximately half of the drugs that undergo metabolic clearance in human adults. CYP3A4 is highly expressed in the liver and the epithelium of the small intestine and represents on average 30% of total hepatic CYP protein and 33â87% of intestinal CYP. CYP3A5 [...]
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Despite many decades of clinical utilization, the drug interaction potential of tricyclic antidepressants (TCAs), particularity inhibition of drugs eliminated by cytochromes P450 (CYP), is not completely understood. Desipramine is known to cause modest increases in the plasma concentrations of paroxetine and nefazodone whereas imipramine and nortriptyline may precipitate phenytoin toxicity. Amitriptyline increases the metabolic [...]
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The thiazolidinediones rosiglitazone and pioglitazone are peroxisome proliferator-activated receptor-γ agonists, with insulin-sensitizing properties, used in the treatment of Type 2 diabetes. The oral bioavailability of rosiglitazone is nearly 100% and that of pioglitazone >80%. Both drugs are extensively metabolized in the liver. Rosiglitazone is mainly biotransformed by N-demethylation and pyridine ring hydroxylation and pioglitazone by [...]
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Treatment of inflammatory bowel disease (IBD) is currently based on aminosalicylates, corticosteroids, immunosuppressives, biologicals, antibiotics, nutritional support and surgery. These therapies are limited by side-effects and may be inefficient in up to 30% of patients. Steroid-refractory and steroid-dependent patients are at great risk of extensive bowel resections, even though surgery cannot cure IBD. These patients [...]
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Antilymphocyte globulins (ALGs) are polyclonal antibodies used in organ transplantation to prevent or treat acute allograft rejection. ALGs are obtained by immunizing animals (rabbits or horses) with human lymphoid cells (lymphoblasts, lymphocytes or thymocytes). Although ALGs have been in use for several decades, the interindividual variability in patient response remains poorly understood. Monitoring of drug [...]
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The three isoforms of nitric oxide synthase (NOS), neuronal NOS (nNOS, NOS 1), inducible NOS (iNOS, NOS 2) and endothelial (eNOS, NOS 3), convert l-arginine to nitric oxide (NO) and l-citrulline. NO is a vasoactive compound that induces vasodilation of arterial and venous blood vessels. In endothelial cells, l-arginine is transported via the cell membrane [...]
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