Markham A, Goa K L
Adis International Limited, Auckland, New Zealand.
Drugs. 1997 Aug;54(2):299-311. doi: 10.2165/00003495-199754020-00009.
Valsartan competitively and selectively inhibits the actions of angiotensin II at the AT1 receptor subtype which is responsible for most of the known effects of angiotensin II. In clinical trials in patients with mild to moderate essential hypertension valsartan was as effective as losartan, lisinopril, enalapril, amlodipine and hydrochlorothiazide. Addition of the latter reduced blood pressure in patients who did not respond sufficiently to valsartan monotherapy. Preliminary data also suggest valsartan may be effective in patients with severe essential hypertension. The drug was as effective as lisinopril as treatment for mild to moderate essential hypertension in patients with renal insufficiency and did not worsen renal function. Headache, dizziness and fatigue were the most common adverse events in placebo-controlled studies; the incidence of these adverse events was not significantly different between placebo and valsartan recipients. Compared with ACE inhibitors, valsartan was associated with a significantly lower incidence of dry cough. Thus, valsartan is an effective treatment for mild to moderate essential hypertension and may be particularly useful in patients who experience persistent cough during ACE inhibitor therapy.
缬沙坦竞争性地、选择性地抑制血管紧张素II在AT1受体亚型上的作用，AT1受体亚型介导血管紧张素II的大部分已知效应。在轻度至中度原发性高血压患者的临床试验中，缬沙坦与氯沙坦、赖诺普利、依那普利、氨氯地平和氢氯噻嗪的疗效相当。对于缬沙坦单药治疗反应不足的患者，加用后者可降低血压。初步数据还表明，缬沙坦可能对重度原发性高血压患者有效。在肾功能不全的轻度至中度原发性高血压患者中，该药物作为治疗药物与赖诺普利疗效相当，且不会使肾功能恶化。在安慰剂对照研究中，头痛、头晕和疲劳是最常见的不良事件；安慰剂组和缬沙坦组这些不良事件的发生率无显著差异。与ACE抑制剂相比，缬沙坦引起干咳的发生率显著更低。因此，缬沙坦是治疗轻度至中度原发性高血压的有效药物，对于在ACE抑制剂治疗期间出现持续性咳嗽的患者可能特别有用。
