Hemodynamic Effects of Dilevalol and N-696, New β-Blocking Agents with Vasodilating Properties, and Doxazosin and Urapidil, New α-Blocking Agents, in Essential Hypertension

Tsukiyama, Hisaichito; Otsuka, Keiko; Takasaki, Izumi; Horii, Masako

doi:10.1097/00005344-198800000-00008

Cited by 10 publications

(8 citation statements)

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“…Then the resistance increases above pretreatment levels, and although there is a significant reduction in cardiac output, blood pressure is usually unchanged during the first hours until total peripheral resistance starts to drop [10]. Our results with dilevalol given acutely agree well with what has been observed in other studies [32][33][34][35].…”

Section: Discussionsupporting

confidence: 89%

Acute and chronic hemodynamic effects of drugs with different actions on adrenergic receptors: A comparison between alpha blockers and different types of beta blockers with and without vasodilating effect

Lund‐Johansen

Omvik

1991

Cardiovasc Drug Ther

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The regulation of vascular resistance, cardiac output, and thus blood pressure can be influenced by antihypertensive drugs acting at central and peripheral adrenergic receptors. The results presented here are from acute or chronic studies in 205 patients with mild or moderately severe essential hypertension: beta blockers (N = 101); alpha blockers (N = 36); a separate alpha- + beta-blocker combination or the combination agent labetalol (N = 37); prizidilol, a beta-blocker/vasodilator (N = 14); and dilevalol, a beta blocker/beta 2-stimulator (N = 17). Beta blockers without strong intrinsic sympathomimetic activity reduce heart rate and cardiac output immediately, but due to a reflex increase in total peripheral resistance index, blood pressure is unchanged or only slightly reduced. During chronic use, total peripheral resistance drops towards pretreatment level and pressure falls. Beta blockers with strong intrinsic sympathomimetic activity do not reduce heart rate or cardiac output at rest when sympathetic tone is low. During exercise, heart rate and cardiac output are reduced, but less than with conventional beta blockers, and resistance is unchanged or slightly reduced. An acute and chronic reduction in blood pressure can be produced by alpha-adrenergic receptor blockers (prazosin, doxazosin, trimazosin), and in these cases the fall occurs via a reduction in total peripheral resistance index without reflex tachycardia. These drugs tend to increase exercise stroke volume and cardiac output during chronic treatment. Free combinations of beta and alpha blockers or the use of the fixed combination drug, labetalol, induce marked reductions in blood pressure at rest and during exercise, mainly through a reduction in total peripheral resistance index. During chronic treatment, exercise stroke volume and cardiac output are well maintained. In acute studies with dilevalol, systolic blood pressure, diastolic blood pressure, and mean arterial pressure were reduced (p less than 0.001) within 1 hour in 17 males with essential hypertension (WHO stage I) who received 200-400 mg oral dilevalol. The reduction in MAP was around 16-17% and was associated with an immediate fall in the total peripheral resistance index of the same magnitude (14%, p less than 0.001) after 1 hour at rest. There were no significant changes in heart rate or cardiac index.(ABSTRACT TRUNCATED AT 400 WORDS)

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Section: Discussionsupporting

confidence: 89%

Acute and chronic hemodynamic effects of drugs with different actions on adrenergic receptors: A comparison between alpha blockers and different types of beta blockers with and without vasodilating effect

Lund‐Johansen

Omvik

1991

Cardiovasc Drug Ther

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“…Tilisolol hydrochloride is a beta-blocking agent with direct vasodilatory properties [3][4][5][6][7][8]. To assess the vasodilatory potency of this agent in coronary vessels, we first compared the coronary effects of tilisolol (2 mg/kg) with those of two beta-blocking agents, propranolol (1 mg/kg) and arotinolol (0.25 mg/kg) [9].…”

Section: Discussionmentioning

confidence: 99%

“…It also has little membrane-stabilizing activity (MSA). Although tilisolol has been reported to have a direct vasodilatory effect both in animals [4,5] and humans [6,7], the mechanism of this effect remains unclear. Recently, tilisolol was shown to produce vasodilation through a mechanism involving potassium (K +) channel opening in isolated rat thoracic aorta preparations and in pithed rats [8].…”

mentioning

confidence: 99%

Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K+-channel opening mechanism in dogs

Liu

Nakae

Takahashi

et al. 1996

Cardiovasc Drug Ther

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Tilisolol is a beta-blocking agent with vasodilatory properties that was recently shown to possess a potassium (K+) channel opening activity. We investigated whether tilisolol has vasodilatory effects on coronary circulation in dogs. Mongrel dogs were chronically instrumented for measurements of circumflex coronary artery diameter (CoD) and coronary blood flow (CBF). We compared the effects of tilisolol on dog coronary arteries with those of two beta-blockers, propranolol and arotinolol. Both propranolol (1 mg/kg, intravenously, i.v.) and arotinolol (0.25 mg/kg, i.v.) decreased CoD and increased coronary vascular resistance (CVR). Tilisolol (2 mg/kg, i.v.) decreased CVR but had no significant effect on CoD. To investigate the mechanism of the coronary action of tilisolol, we examined differences in the response to tilisolol in the absence and presence of glibenclamide, an ATP-sensitive K+ channel blocker. Tilisolol (1,2,4, and 8 mg/kg, i.v.) produced a dose-dependent decrease in CVR without glibenclamide, whereas pretreatment with glibenclamide significantly suppressed this effect. Without glibenclamide, tilisolol had no significant effect on CoD at doses of 1-4 mg/kg (i.v.). However, at the higher dose of 8 mg/kg (i.v.), tilisolol significantly increased CoD (1.00 +/- 0.15%, p < 0.01). After pretreatment with glibenclamide, tilisolol (1-8 mg/kg, i.v.) produced a significant decrease in CoD. Therefore, we concluded that tilisolol exerts its vasodilatory effect on the coronary circulation through an ATP-sensitive K+ channel opening mechanism, and that its vasodilatory action is more prominent in coronary resistance vessels than in large coronary arteries.

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“…The different effects among the 13-blockers are likely due to different effects of these /?-blockers on nutritional blood flow. Thus, with pletysmography it has been demonstrated that dilevalol is a vasodilator (24) but selective /9-blockers as well as non-selective /9-blockers without intrinsic sympathetic activity are vasoconstrictors. These different effects will probably influence insulin action in muscle tissue.…”

Section: Metabolic Effects Of A1-blockersmentioning

confidence: 99%

Antihypertensive Treatment in Insulin Resistant Patients

Lithell

Andersson

1996

Hypertens Res

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Hemodynamic Effects of Dilevalol and N-696, New β-Blocking Agents with Vasodilating Properties, and Doxazosin and Urapidil, New α-Blocking Agents, in Essential Hypertension

Cited by 10 publications

References 0 publications

Acute and chronic hemodynamic effects of drugs with different actions on adrenergic receptors: A comparison between alpha blockers and different types of beta blockers with and without vasodilating effect

Acute and chronic hemodynamic effects of drugs with different actions on adrenergic receptors: A comparison between alpha blockers and different types of beta blockers with and without vasodilating effect

Tilisolol hydrochloride dilates coronary arteries through an ATP-sensitive K+-channel opening mechanism in dogs

Antihypertensive Treatment in Insulin Resistant Patients

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