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Labetalol bio availability drug plasma levels plasma renin and catecholamines in acute and chronic treatment of resistant hypertension

Labetalol bio availability drug plasma levels plasma renin and catecholamines in acute and chronic treatment of resistant hypertension

Australian and New Zealand Journal of Medicine 8(6): 602-609

The antihypertensive effects of labetalol were studied in 30 patients with severe hypertension. In 7 of these patients acute administration was associated with falls in blood pressure which were maximal at 2 min, for i.v. injection and 1 h for oral administration. The bioavailability of acute oral administration was studied and varied between 11-76%. There were no statistically significant changes in plasma renin and plasma catecholamines following acute administration. In 30 patients labetalol was administered, together with a thiazide diuretic, on a chronic basis over 10 mo. There was a significant relationship (r = 0.517, P < 0.001) between drug dosage and plasma levels and in 4 cases poor response could be attributed to low peak plasma levels of the drug. Improved blood pressure control was associated with a substantial reduction in the number and type of tablets patients were taking and an overall reduction in side effects. The most common side effect was mild postural hypotension. A patient in the trial and another more recently showed hyper-reactivity to the drug and developed profound postural hypotension with the initial dose. Labetalol when combined with a thiazide diuretic is an important therapeutic advance in the treatment of the difficult hypertensive subject.

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Accession: 005787144

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PMID: 285681

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