Voriconazole is a broad-spectrum triazole antifungal agent with potent activity against a range of medically important fungal pathogens. 1,2 Voriconazole is often recommended as the primary treatment for acute invasive aspergillosis and as salvage therapy for serious fungal infections caused by rare moulds such as those of the Scedosporium and Fusarium species in adults, and for the treatment of Candida infections in nonneutropenic adults. 3,4 Voriconazole can be used to prevent invasive fungal infections in immunocompromised patients. 5,6 In several cases with Aspergillus infections, long-term, even lifelong antifungal therapy may be required to control the disease. 3,4 Voriconazole is available in both intravenous and oral forms. Thus, switching from intravenous to oral medication among patients whose clinical condition allows for intake of oral
This paper introduces a pair of query editors for SuperSQL: SSedit and SSvisual. SSedit is a structured editor specialized for SuperSQL, which is mainly used to create a query statement from scratch. SSvisual is a WYSIWYG editor, which is mainly used to fine tune the layout and visual effects on HTML.
The human mass balance of [C]Z-215, a novel proton pump inhibitor, was characterised in six healthy male volunteers following single oral administration of [C]Z-215 (20 mg, 3.7 MBq) to determine the elimination pathway of Z-215 and the distribution of its metabolites in plasma, urine, and faeces (NCT02618629). [C]Z-215 was rapidly absorbed, with a C of 434 ng/mL at 0.38 h for Z-215 and 732 ng eq./mL at 0.5 h for total radioactivity. Means of 59.61% and 31.36% of the administered radioactive dose were excreted in urine and faeces, respectively, within 168 h post-dose. The majority of the dose was recovered within 24 h in urine and 96 h in faeces. Unchanged Z-215 was excreted in urine at trace levels but was not detected in faeces. The main components in plasma were Z-215 and Z-215 sulphone, accounting for 29.8% and 13.3% of the total circulating radioactivity, respectively. Additionally, Z-215 was metabolised through oxidation, reduction and conjugation. Our in vitro Z-215 metabolism study showed that the major isozyme contributing to the oxidation of Z-215, including the formation of Z-215 sulphone, was CYP3A4. In conclusion, Z-215 is well absorbed in humans and primarily eliminated via metabolism, where CYP3A4 plays an important role.
The acetylcholinesterase inhibitor, acotiamide, improves gastric motility and is clinically used to treat functional dyspepsia. The present study aimed to identify the transporters involved in the distribution of acotiamide in stomach tissue. Acotiamide uptake by the gastric cancer-derived model cell line, Hs746 T, was Na + -and pH-independent. The initial uptake velocity of acotiamide was saturable with increasing concentrations of acotiamide and was inhibited by selective serotonin reuptake inhibitors, which are potent inhibitors of the plasma membrane monoamine transporter (PMAT). The uptake of acotiamide by PMAT gene-transfected HEK293 cells was saturable, with similar K m (197.9 μM) values to those of uptake by Hs 746T cells (106 μM). Moreover, immunoreactivity of PMAT was found in the gastric smooth muscle and vascular endothelial cells. These results suggest that PMAT contributes to the distribution of acotiamide in the stomach, where it exerts its pharmacological effects.
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