Schumacher G E
Am J Hosp Pharm. 1979 Sep;36(9):1222-6.
Pharmacokinetic methods that have been used to improve antihypertensive drug therapy, including antihypertensive dosage regimens, are reviewed. Pharmacokinetic variables have been determined that allow: (1) derivation of the loading dose necessary to achieve rapid control of blood pressure with propranolol hydrochloride, guanethidine, minoxidil and clonidine hydrochloride; (2) reduced frequency of dosing with methyldopa, hydralazine hydrochloride, prazosin hydrochloride, propranolol and clonidine; and (3) alteration of propranolol and hydralazine dosage based on physiologic factors (e.g., renal and hepatic impairment, binding to plasma proteins, altered enzyme activity). More rapid control of hypertension is possible, patient compliance is enhanced and drug toxicity is reduced by applying pharmacokinetic principles to develop individualized antihypertensive dosage regimens.
本文综述了用于改善抗高血压药物治疗的药代动力学方法，包括抗高血压给药方案。已确定的药代动力学变量能够：(1) 推算出使用盐酸普萘洛尔、胍乙啶、米诺地尔和盐酸可乐定实现血压快速控制所需的负荷剂量；(2) 减少甲基多巴、盐酸肼屈嗪、盐酸哌唑嗪、普萘洛尔和可乐定的给药频率；(3) 根据生理因素（如肾和肝功能损害、与血浆蛋白结合、酶活性改变）调整普萘洛尔和肼屈嗪的剂量。通过应用药代动力学原理制定个体化抗高血压给药方案，可以更快地控制高血压，提高患者依从性并降低药物毒性。
