SD-3211, a novel benzothiazine calcium antagonist, alone and in combination with a beta-adrenoceptor antagonist, produces antihypertensive effects without affecting heart rate and atrioventricular conduction in conscious renal hypertensive dogs

J Cardiovasc Pharmacol. 1991 Jan;17(1):102-7. doi: 10.1097/00005344-199101000-00015.

Abstract

We compared the effects of SD-3211, a novel calcium antagonist, on blood pressure, heart rate, and atrioventricular conduction with those of diltiazem using conscious renal hypertensive dogs (one-kidney, one-clip type). We also examined the combined effects of these calcium antagonists with a beta-adrenoceptor antagonist, propranolol, on these variables. Oral administration of SD-3211 (1.25, 2.5, and 5 mg/kg) resulted in a dose-dependent decrease in blood pressure without affecting heart rate. SD-3211 at all three doses significantly decreased systolic blood pressure. At 2.5 and 5 mg/kg the compound elicited significant decreases in mean blood pressure and diastolic blood pressure. Hypotension obtained with the highest dose of SD-3211 lasted for at least 9 h. No significant alteration in PR interval was observed in electrocardiograms after administration of SD-3211. Diltiazem, given orally at doses of 2.5 and 5 mg/kg but not 1.25 mg/kg, produced significant hypotension with little change in heart rate. The duration of hypotension induced by the highest dose of diltiazem was only 3 h. Diltiazem prolonged PR interval in a dose-dependent manner, causing second-degree atrioventricular block in some dogs. Combined administration of SD-3211 or diltiazem (2.5 mg/kg) with propranolol (30 mg/kg) resulted in enhanced hypotension with no alteration in heart rate. SD-3211 plus propranolol had little effect on the PR interval, whereas diltiazem plus propranolol caused a markedly enhanced prolongation. These results indicate that SD-3211 is an antihypertensive agent with long-lasting action and little effect on heart rate and atrioventricular conduction and, when administered alone or in combination with propranolol, may be useful in the treatment of hypertension.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Oral
  • Adrenergic beta-Antagonists / pharmacology
  • Animals
  • Antihypertensive Agents* / administration & dosage
  • Antihypertensive Agents* / pharmacology
  • Atrioventricular Node / drug effects*
  • Atrioventricular Node / physiology
  • Blood Pressure / drug effects*
  • Calcium Channel Blockers / administration & dosage
  • Calcium Channel Blockers / pharmacology*
  • Diltiazem / administration & dosage
  • Diltiazem / pharmacology
  • Dogs
  • Drug Therapy, Combination
  • Electrocardiography / drug effects
  • Heart Rate / drug effects
  • Hypertension, Renal / drug therapy*
  • Hypertension, Renal / physiopathology
  • Male
  • Propranolol / pharmacology*
  • Thiazoles / administration & dosage
  • Thiazoles / pharmacology*

Substances

  • Adrenergic beta-Antagonists
  • Antihypertensive Agents
  • Calcium Channel Blockers
  • Thiazoles
  • Propranolol
  • sesamodil
  • Diltiazem