Hunyor S N, Bauer G E, Ross M, Larkin H
Aust N Z J Med. 1980 Apr;10(2):162-6. doi: 10.1111/j.1445-5994.1980.tb03705.x.
Labetalol administered in a small to moderate dose (first month 400 mg/day, second month average 585 mg/day) was effective in lowering blood pressure (BP) (-21/-18 mmHg, recumbent) in 11 of 13 mild essential hypertensives over an eight-week period, despite a significant (+294 ml) increase in plasma volume. The effect of propranolol (first month 160 mg/day, second month average 234 mg/day) was significantly less on both blood pressure (-9/-9 mmHg) and plasma volume (+98 ml), although the pre-propranolol BP was lower and the final BP achieved on the two medications was comparable (labetalol 147/89 mmHg, propranolol 145/89). Six patients who continued labetalol for periods of up to 14 months had persistent plasma volume expansion. Three of these, taking a higher dose of labetalol, developed resistance to the drug's antihypertensive effect. Addition of a diuretic restored antihypertensive efficacy and led to a fall in plasma volume. No such plasma volume expansion was seen in six patients who were followed on long term propranolol therapy. Some plasma volume expansion with the combined alpha- beta-adrenoceptor blocker labetalol may be appropriate to its vasodilator action. Provided this effect is not excessive, it appears not to lead to resistance to its antihypertensive action. Small to moderate doses of labetalol would, therefore, seem effective without concomitant diuretic. Such sole use of labetalol could help minimise orthostatic symptoms which can be a major side effect of combination therapy.
小剂量至中等剂量的拉贝洛尔(第一个月400毫克/天,第二个月平均585毫克/天)在8周内对13例轻度原发性高血压患者中的11例有效降低卧位血压(-21/-18毫米汞柱),尽管血浆容量显著增加(+294毫升)。普萘洛尔(第一个月160毫克/天,第二个月平均234毫克/天)对血压(-9/-9毫米汞柱)和血浆容量(+98毫升)的作用明显较小,尽管普萘洛尔治疗前血压较低,且两种药物最终达到的血压相当(拉贝洛尔147/89毫米汞柱,普萘洛尔145/89)。6例持续使用拉贝洛尔长达14个月的患者出现持续性血浆容量扩张。其中3例服用较高剂量拉贝洛尔的患者对该药的降压作用产生了耐药性。加用利尿剂可恢复降压疗效并导致血浆容量下降。长期接受普萘洛尔治疗的6例患者未出现这种血浆容量扩张。联合α-β肾上腺素能受体阻滞剂拉贝洛尔引起的一定程度的血浆容量扩张可能与其血管舒张作用有关。只要这种作用不过度,似乎不会导致对其降压作用产生耐药性。因此,小剂量至中等剂量的拉贝洛尔似乎无需联用利尿剂即可有效。单独使用拉贝洛尔有助于将直立性症状减至最低,而直立性症状可能是联合治疗的主要副作用。