临床药物动力学和药效学的丁螺环酮,一种抗焦虑的药物。
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马哈茂德我,维C
临床药物动力学和药效学的丁螺环酮,一种抗焦虑的药物。
Pharmacokinet。1999年4月,36 (4):277 - 87。doi: 10.2165 / 00003088-199936040-00003。
- PubMed ID
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10320950 (在PubMed]
- 文摘
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丁螺环酮是一种抗焦虑药物在15毫克/天的剂量。药物的作用机制并没有很好的特点,但它可能施加的影响作用于多巴胺能系统在中枢神经系统或通过绑定5 -羟色胺(5 -羟色胺)受体。丁螺环酮的口服剂量20毫克,药物迅速吸收。平均血浆浓度峰值(Cmax)大约是2.5微克/ L,和到达峰值的时间是1小时。丁螺环酮的绝对生物利用度为4%左右。丁螺环酮广泛代谢。丁螺环酮的主要代谢产物之一是1-pyrimidinylpiperazine (1-PP),这可能导致丁螺环酮的药理作用。丁螺环酮的体积分布的5.3 L /公斤,系统性间隙约为1.7 L / h /公斤,消除半衰期约2.5小时和药物动力学线性剂量范围10至40毫克。后multiple-dose管理丁螺环酮10毫克/天9天,没有积累的母体化合物或代谢物(1-PP)。政府与食品增加了Cmax和血浆浓度时间曲线下面积(AUC)丁螺环酮的2倍。 After a single 20 mg dose, the Cmax and AUC increased 2-fold in patients with renal impairment as compared with healthy volunteers. The Cmax and AUC were 15-fold higher for the same dose in patients with hepatic impairment compared with healthy individuals. The half-life of buspirone in patients with hepatic impairment was twice that in healthy individuals. The pharmacokinetics of buspirone were not affected by age or gender. Coadministration of buspirone with verapamil, diltiazem, erythromycin and itraconazole substantially increased the plasma concentration of buspirone, whereas cimetidine and alprazolam had negligible effects. Rifampicin (rifampin) decreased the plasma concentrations of buspirone almost 10-fold.
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