Chronic carvedilol reduces mortality and renal damage in hypertensive stroke-prone rats

J Pharmacol Exp Ther. 1996 Nov;279(2):948-55.

Abstract

The effects of carvedilol, a novel vasodilating beta-blocker and antioxidant, and propranolol on survival, neurobehavioral deficits, cardiovascular parameters, plasma renin, plasma aldosterone levels and renal pathology were determined in stroke-prone spontaneously hypertensive rats. Stroke-prone spontaneously hypertensive rats were allowed access to 1% NaCl as the drinking solution and a high fat diet supplemented with carvedilol (1200 or 2400 ppm) or propranolol (2400 ppm). The control group consisted of stroke-prone spontaneously hypertensive rats placed on the same diet with no drug supplement. Animals fed propranolol had a blood level of 864 +/- 68 ng/ml, whereas carvedilol-fed animals had blood levels of 24 +/- 4 ng/ml at 1200 ppm and 471 +/- 145 ng/ml at 2400 ppm. Carvedilol and propranolol treatment resulted in significant beta adrenoceptor blockade. Both compounds reduced heart rate, but had no significant effects on systolic arterial blood pressure. Carvedilol- and propranolol-treated animals also exhibited significant, prolonged protection from neurobehavioral deficits and mortality (P < .01). Elevated plasma renin activity and aldosterone levels seen in untreated controls were significantly decreased by propranolol (P < .05), and to a considerably greater extent by the same dose of carvedilol (P < .01). Carvedilol decreased renal histopathological damage and cardiac hypertrophy to a greater extent (P < .01) than propranolol (at equal doses). Both carvedilol (P < .01)- and propranolol (P < .01)-treated animals had considerably reduced renal damage at 18 weeks of treatment. Carvedilol reduced renal damage more than propranolol (P < .05). In addition, the lower (1200 ppm) dose of carvedilol, which decreased neurobehavioral deficits and mortality, had no significant effects on organ mass or renal function, but significantly (P < .01) reduced renal damage. These data indicate that both beta adrenoceptor blockers, especially carvedilol to a considerably greater degree, convey significant protection in a genetic model of severe hypertension that results in renal and cardiovascular organ pathology, neurobehavioral deficits and premature death.

MeSH terms

  • Adrenergic beta-Antagonists / pharmacology*
  • Aldosterone / blood
  • Animals
  • Antihypertensive Agents / pharmacology*
  • Blood Pressure / drug effects
  • Body Weight / drug effects
  • Carbazoles / blood
  • Carbazoles / pharmacology*
  • Carvedilol
  • Heart Rate / drug effects
  • Hypertension / drug therapy*
  • Hypertension / pathology
  • Kidney / drug effects*
  • Kidney / pathology
  • Male
  • Propanolamines / blood
  • Propanolamines / pharmacology*
  • Propranolol / pharmacology
  • Rabbits
  • Rats
  • Rats, Inbred SHR
  • Renin / blood

Substances

  • Adrenergic beta-Antagonists
  • Antihypertensive Agents
  • Carbazoles
  • Propanolamines
  • Carvedilol
  • Aldosterone
  • Propranolol
  • Renin