氟替卡松加沙美特罗的临床药物动力学。
文章的细节
-
引用
复制到剪贴板 -
Cazzola M,包括R,马泰拉毫克
氟替卡松加沙美特罗的临床药物动力学。
Pharmacokinet。2002; 41 (1): 19-30。doi: 10.2165 / 00003088-200241010-00003。
- PubMed ID
-
11825095 (在PubMed]
- 文摘
-
吸入氟替卡松加沙美特罗是一个长效选择性β(2)肾上腺素能受体激动剂,是商用xinafoate (1-hydroxy-2-naphthoic酸)盐的外消旋混合物的两个光学异构体(R) - (S) -,氟替卡松加沙美特罗。它在肺部通过行动beta2受体。有限的数据已经公布在氟替卡松加沙美特罗的药物动力学。此外,没有数据的程度吸入氟替卡松加沙美特罗经历了初步的新陈代谢。这种信息的缺乏是最有可能由于非常低的等离子体浓度达到治疗剂量的氟替卡松加沙美特罗和吸入后的问题在发展中足够灵敏的分析方法来确定这些浓度。吸入氟替卡松加沙美特罗时,等离子体浓度的药物往往无法检测到,即使在30分钟后的治疗剂量。大剂量吸入给大约比例增加血药浓度。等离子体浓度氟替卡松加沙美特罗0.1到0.2和1到2 microg / L在健康志愿者获得约5到15分钟后的单剂量吸入50和400 microg,分别。beplayapp在患者吸入氟替卡松加沙美特罗50 microg连续10个月每天两次,第二次峰值浓度的0.07到0.2 microg / L吸入后发生45到90分钟,可能是因为肠胃吸收的吞下了药。氟替卡松加沙美特罗xinafoate在溶液中水解酸氟替卡松加沙美特罗和1-hydroxy-2-naphthoic。 These two compounds are then absorbed, distributed, metabolised and excreted independently. The xinafoate moiety has no apparent pharmacological activity, is highly protein bound (>99%), largely to albumin, and has a long elimination half-life of about 12 to 15 days in healthy individuals. For this reason, it accumulates in plasma during repeated administration, with steady-state concentrations reaching about 80 to 90 microg/L in patients treated with salmeterol 50microg twice daily for several months. The cytochrome P450 (CYP) isoform 3A4 is responsible for aliphatic oxidation of salmeterol base, which is extensively metabolised by hydroxylation with the major metabolite being alpha-hydroxysalmeterol, with subsequent elimination predominantly in the faeces. It has been demonstrated that 57.4% of administered radioactivity is recovered in the faeces and 23% in the urine; most is recovered between 24 and 72 hours after administration. Unchanged salmeterol accounts for <5% of the excreted dose in the urine. Since the therapeutic dose of salmeterol is very low, it is unlikely that any clinically relevant interactions will be observed as a consequence of the coadministration of salmeterol and other drugs, such as fluticasone propionate, that are metabolised by CYP3A. All the available data clearly show that at the recommended doses of salmeterol, systemic concentrations are low or even undetectable. This is an important point, because it has been demonstrated that the systemic effects of salmeterol are more likely to occur with higher doses, which lead to approximately proportionally increased blood concentrations.
beplay体育安全吗DrugBank数据引用了这篇文章
- 药物
- 药物靶点
-
药物 目标 类 生物 药理作用 行动 氟替卡松加沙美特罗 β2肾上腺素能受体 蛋白质 人类 是的受体激动剂细节 - 药物酶
-
药物 酶 类 生物 药理作用 行动 氟替卡松加沙美特罗 细胞色素P450 3 a4 蛋白质 人类 未知的底物细节 氟替卡松加沙美特罗 细胞色素P450 3 a5 蛋白质 人类 未知的底物细节 氟替卡松加沙美特罗 细胞色素P450 3 a7 蛋白质 人类 未知的底物细节 - 药物载体
-
药物 航空公司 类 生物 药理作用 行动 氟替卡松加沙美特罗 alpha1-acid糖蛋白(蛋白质组) 蛋白质组 人类 未知的粘结剂细节 氟替卡松加沙美特罗 血清白蛋白 蛋白质 人类 未知的粘结剂细节 - 药物反应
-
反应 细节 - 药物的相互作用Learn More" title="" id="structured-interactions-info" class="drug-info-popup" href="javascript:void(0);">
-
药物 交互 整合药物之间
在您的软件的交互氟替卡松加沙美特罗 Terfenadine 时可以减少氟替卡松加沙美特罗的新陈代谢与Terfenadine相结合。 氟替卡松加沙美特罗 例如 时可以减少氟替卡松加沙美特罗的新陈代谢与例如相结合。 氟替卡松加沙美特罗 依法韦伦 的新陈代谢时可以减少氟替卡松加沙美特罗结合依法韦伦。 氟替卡松加沙美特罗 麦角胺 时可以减少氟替卡松加沙美特罗的新陈代谢与麦角胺相结合。 氟替卡松加沙美特罗 Delavirdine 时可以减少氟替卡松加沙美特罗的新陈代谢与Delavirdine相结合。 氟替卡松加沙美特罗 甲硫咪唑 的新陈代谢时可以减少氟替卡松加沙美特罗结合甲巯基咪唑。 氟替卡松加沙美特罗 Conivaptan 时可以减少氟替卡松加沙美特罗的新陈代谢与Conivaptan相结合。 氟替卡松加沙美特罗 Tipranavir 时可以减少氟替卡松加沙美特罗的新陈代谢与Tipranavir相结合。 氟替卡松加沙美特罗 Telithromycin 时可以减少氟替卡松加沙美特罗的新陈代谢与Telithromycin相结合。 氟替卡松加沙美特罗 酮康唑 时可以减少氟替卡松加沙美特罗的新陈代谢与酮康唑相结合。
