阿普唑仑的临床药物动力学。治疗的影响。
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格林布拉特DJ,赖特CE
阿普唑仑的临床药物动力学。治疗的影响。
Pharmacokinet。1993年6月,24 (6):453 - 71。doi: 10.2165 / 00003088-199324060-00003。
- PubMed ID
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8513649 (在PubMed]
- 文摘
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阿普唑仑是triazolobenzodiazepine规定在西方世界广泛用于治疗焦虑和恐慌紊乱。其苯二氮受体结合特性定性类似其他的苯二氮卓类。药物主要由肝微粒体代谢氧化,收益率阿尔法羟基-和4-hydroxy-alprazolam主要初始代谢物。内在苯二氮受体亲和力都低于阿普唑仑和出现在人血浆浓度小于10%的父母的药物。等离子体4-hydroxy代谢物的浓度超过阿尔法羟基衍生物,但尿复苏4-hydroxy-alprazolam alpha-hydroxy-alprazolam大大超过。这可能是解释4-hydroxy-alprazolam体外的化学不稳定性。在人类单1毫克口服剂量后,阿普唑仑是典型的药代动力学变量:血浆浓度峰值发生12至22毫克/升0.7 - 1.8 h postdose体积分布的0.8到1.3 L /公斤,消除半衰期为9到16 h和间隙0.7到1.5毫升/分钟/公斤。口服阿普唑仑的绝对生物利用度平均100%到80。药物动力学dose-independent multiple-dose治疗期间保持不变。平均而言,意味着阿普唑仑稳态等离子体浓度变化10到12毫克/ L为每个每日剂量的变化1毫克/天。 Most studies show that alprazolam pharmacokinetics are not significantly influenced by gender. Clearance of alprazolam is reduced in many elderly individuals, even those who are apparently healthy. Clearance is significantly reduced in patients with cirrhosis. Renal disease causes reduced plasma protein binding of alprazolam (increased free fraction) and some data suggest reduced free clearance of alprazolam in such patients. Pharmacokinetics of alprazolam are not significantly altered in abstinent alcoholics or patients with panic disorder, and are not influenced by the phase of the menstrual cycle in women. Coadministration of cimetidine, fluoxetine, fluvoxamine or propoxyphene significantly impairs alprazolam clearance. However, alprazolam clearance is not altered by coadministration of propranolol, metronidazole, disulfiram, oral contraceptives or ethanol. Imipramine clearance may be impaired if alprazolam is coadministered. Alprazolam does not alter the pharmacokinetics of digoxin. Although a therapeutic concentration range is not clearly established, some studies indicate that optimal reduction of anxiety associated with panic disorder occurs at steady-state plasma alprazolam concentrations of 20 to 40 micrograms/L. Concentrations higher than this may be needed for suppression of the actual panic attacks. Side effects associated with alprazolam (drowsiness, sedation, etc.) are consistent with its primary benzodiazepine agonist action and increase in frequency with higher steady-state plasma concentrations.(ABSTRACT TRUNCATED AT 400 WORDS)
DrugBank数据引用了这篇文章
- 药物
- 药物载体
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药物 航空公司 类 生物 药理作用 行动 阿普唑仑 alpha1-acid糖蛋白(蛋白质组) 蛋白质组 人类 未知的粘结剂细节 - 药物反应
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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);">
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药物 交互 整合药物之间
在您的软件的交互1,2-Benzodiazepine 氟西汀 1的血清浓度,2-Benzodiazepine结合时可以增加氟西汀。 Bromazepam 氟西汀 的血清浓度Bromazepam结合时可以增加氟西汀。 利眠宁 氟西汀 利眠宁的血清浓度可以增加时结合氟西汀。 Clobazam 氟西汀 的血清浓度Clobazam结合时可以增加氟西汀。 氯硝西泮 氟西汀 氯硝西泮的血清浓度可以增加时结合氟西汀。 Clorazepic酸 氟西汀 的血清浓度Clorazepic酸可以增加时结合氟西汀。 Clotiazepam 氟西汀 的血清浓度Clotiazepam结合时可以增加氟西汀。 艾司唑仑 氟西汀 艾司唑仑的血清浓度可以增加时结合氟西汀。 Flunitrazepam 氟西汀 的血清浓度Flunitrazepam结合时可以增加氟西汀。 安眠药 氟西汀 安眠药的血清浓度可以增加时结合氟西汀。
