Labetalol in the treatment of patients with hypertension and renal function impairment.

Abstract

1 Labetalol has been used to treat patients with renal hypertension or hypertension in the presence of renal functional impairment. In some patients changes in the glomerular filtration rate (GFR) were followed during the treatment. 2 Sixty patients were treated with labetalol for up to 24 months. Forty-nine of the patients were taking a diuretic and 23 were receiving additional antihypertensive therapy. The antihypertensive effect of labetalol has so far been assessed in 51 patients. Forty-six of these 51 patients have responded with a fall in the mean supine BP from 184/115 to 148/93 mmHg and the mean erect BP from 176/112 to 138/89 mmHg. 3 The mean daily maintenance dose of labetalol for the responders was 418 mg (range 100-1200 mg). The majority of patients were controlled by less than 600 mg daily. 4 Side-effects occurred in 38% of patients, the most serious of which was left ventricular failure in four patients with severe cardiac and renal disease. Other side-effects included transient postural hypotension, scalp tingling and problems with micturition. Fluid retention was frequent but was easily controlled with diuretics. 5 In only three of 31 patients was there a fall in the GFR which could possibly be attributable to the treatment. These changes were small and not clinically significant. An improvement or stabilization of the GFR was noted frequently. 6 Labetalol by intravenous infusion proved disappointing and quite unpredictable in its action. A large single oral dose was effective in hypertensive emergencies. 7 Labetalol, preferably in combination with a diuretic, was a safe and effective drug for patients with hypertension and renal functional impairment.

Clinical Pharmacokinetics of Labetalol

“…At present, no information is available concerning the pharmacokinetics of labetalol in children, although there have been several reports of the successful clinical use of the drug in this age group (Bailey, 1979;Jones, 1979;Jureidini, 1980).…”

“…Labetalol has been used successfully as an antihypertensive agent in patients with mild degrees of renal impairment without causing significant deterioration in renal function (Bailey, 1979;Thompson et al (1977). Wood et al (l982b) have studied the pharmacokinetics of intravenously administered labetalol in 4 patients with severe renal failure and creatinine clearance values in the region of 0.1 ml/sec (normal> 1.4 ml/sec).…”

Labetalol, an alpha‐ and beta‐adrenoceptor‐blocking agent: its use in therapeutics. A summary of the symposium.

“…Transient tiredness in three patients, and transient calf muscle pain in two patients were reported in a series of 17 patients by Andersson et al (1976). Urinary retention due to labetalol has been reported (Bailey, 1979;Dargie et al, 1976) and there have been isolated reports of patients suffering from vivid dreams that could have been due to labetalol (Hansson & Hiinel, 1976). Bolli et al (1976), in a series of 17 patients, reported two patients with mild constipation and one patient with angina, which worsened when labetalol was substituted for metoprolol.…”

“…Long term studies of renal function in hypertensive patients who had pre-existing compromised renal function have shown that labetalol treatment per se does not have any deliterious effect on the underlying renal function (Thompson et al, 1979;Bailey, 1979;Williams, 1979). It can be used alone or together with diuretics (Bailey, 1979), the dose of labetalol required to control BP being reduced due to the additive effect of the diuretic.…”

“…In those patients whose BP is difficult to control or when substitution is required for multiple drug treatments, it is now clear that labetalol may be useful (Williams et al, 1979;Bailey, 1979;New Zealand Hypertension Study Group, 1979). Long term studies of renal function in hypertensive patients who had pre-existing compromised renal function have shown that labetalol treatment per se does not have any deliterious effect on the underlying renal function (Thompson et al, 1979;Bailey, 1979;Williams, 1979).…”