Vasoconstrictor effect of midodrine, ST 1059, noradrenaline, etilefrine and dihydroergotamine on isolated human veins

Thulesius, Olav; Gjöres, J E; Berlin, E

doi:10.1007/bf00568204

Cited by 42 publications

(13 citation statements)

References 1 publication

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“…MR-proADM is produced in equimolar amounts to ADM, which has peripheral vasorelaxing effects (6,22,23). Midodrine hydrochloride, an ␣-adrenoceptor agonist, is able to facilitate the vasoconstriction (24). That explains why the patients with higher plasma levels of MR-proADM had better responses to midodrine hydrochloride.…”

Section: Possible Implications Of Mr-proadm In Potsmentioning

confidence: 89%

Midregional Pro-Adrenomedullin as a Predictor for Therapeutic Response to Midodrine Hydrochloride in Children With Postural Orthostatic Tachycardia Syndrome

Zhang

Ochs

et al. 2012

Journal of the American College of Cardiology

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Section: Possible Implications Of Mr-proadm In Potsmentioning

confidence: 89%

Midregional Pro-Adrenomedullin as a Predictor for Therapeutic Response to Midodrine Hydrochloride in Children With Postural Orthostatic Tachycardia Syndrome

Zhang

Ochs

et al. 2012

Journal of the American College of Cardiology

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“…The half-life of etilefrine was about 15 min [27] which was longer than the half-life of NE which was less than 2 min [28]. With regard to the c~-adrenergic stimulating effects of etilefrine, it was reported that smooth muscle contraction by etilefrine was about 30 times less potent than norepinephrine in isolated dog femoral arteries [29] and 50 times less potent than norepinephrine in isolated human veins [30]. These results agrees with ours, i.e., effective dose (ED) (20%) of MABP value was about 60 times less potent than norepinephrine in the support dogs (Table 1).…”

Section: Discussionmentioning

confidence: 96%

Pharmacological analysis of positive chronotropic and inotropic responses to etilefrine in isolated dog heart preparations

et al. 1992

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Positive chronotropic and inotropic responses to etilefrine (alpha-[(ethylamino)methyl]-m-hydroxybenzyl alcohol), an orally active cardiovascular agent, were investigated in isolated dog right atrial and left ventricular preparations. Intravenous administration of etilefrine to a support dog increased heart rate and mean systemic blood pressure, and increased sinus rate and atrial contractile force in the isolated right atrium perfused with blood from the support dog. Etilefrine injected intra-arterially to isolated atria and ventricles induced dose-dependent positive chronotropic and inotropic effects. Etilefrine was about 100 times less potent than isoproterenol. The effects of etilefrine in isolated atria were significantly inhibited by treatment with atenolol, but were not significantly inhibited by ICI 118,551. The effects of etilefrine were partially inhibited by imipramine. These results indicate that etilefrine is a highly selective beta-1 adrenoceptor agonist and suggest a moderate catecholamine-releasing activity by tyramine-like action in the blood-perfused dog heart.

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“…Desglymidodrine, the active metabolite of midodrine, constricts peripheral human veins in vitro and in healthy volunteers. 31,32 Thus, in theory, midodrine could reduce splanchnic capacitance. However, selective α1-adrenoreceptor stimulation with systemic infusion of phenylephrine failed to increase venous return and cardiac output in normal subjects, 33–35 and in autonomic failure patients midodrine 10 mg did not decrease calf venous compliance.…”

Section: Discussionmentioning

confidence: 99%

Efficacy of Servo-Controlled Splanchnic Venous Compression in the Treatment of Orthostatic Hypotension

et al. 2016

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Splanchnic venous pooling is a major hemodynamic determinant of orthostatic hypotension (OH), but is not specifically targeted by pressor agents, the mainstay of treatment. We developed an automated inflatable abdominal binder that provides sustained servo-controlled venous compression (40 mmHg) and can be activated only on standing. We tested the efficacy of this device against placebo and compared it to midodrine in nineteen autonomic failure patients randomized to receive either placebo, midodrine (2.5–10 mg) or placebo combined with binder on separate days in a single-blind, crossover study. Systolic blood pressure (SBP) was measured seated and standing before and 1-hour post-medication; the binder was inflated immediately before standing. Only midodrine increased seated SBP (31±5 vs. 9±4 placebo and 7±5 binder, P=0.003); whereas orthostatic tolerance (defined as area under the curve of upright SBP [AUCSBP]) improved similarly with binder and midodrine (AUCSBP, 195±35 and 197±41 vs. 19±38 mmHg*min for placebo, P=0.003). Orthostatic symptom burden decreased with the binder (from 21.9±3.6 to 16.3±3.1, P=0.032) and midodrine (from 25.6±3.4 to 14.2±3.3, P<0.001), but not with placebo (from 19.6±3.5 to 20.1±3.3, P=0.756). We also compared the combination of midodrine and binder, with midodrine alone. The combination produced a greater increase in orthostatic tolerance (AUCSBP, 326±65 vs. 140±53 mmHg*min for midodrine alone, P=0.028, n=21), and decreased orthostatic symptoms (from 21.8±3.2 to 12.9±2.9, P<0.001). In conclusion, servo-controlled abdominal venous compression with an automated inflatable binder is as effective as midodrine, the standard of care, in the management of OH. Combining both therapies produces greater improvement in orthostatic tolerance.

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Vasoconstrictor effect of midodrine, ST 1059, noradrenaline, etilefrine and dihydroergotamine on isolated human veins

Abstract: ST 1059, the pharmacologically active metabolite of midodrine, is a powerful vasoconstrictor compound, acting by stimulation of alpha-receptors. It elicited 80% of noradrenaline-induced contraction of human veins.

Cited by 42 publications

References 1 publication

Midregional Pro-Adrenomedullin as a Predictor for Therapeutic Response to Midodrine Hydrochloride in Children With Postural Orthostatic Tachycardia Syndrome

Midregional Pro-Adrenomedullin as a Predictor for Therapeutic Response to Midodrine Hydrochloride in Children With Postural Orthostatic Tachycardia Syndrome

Pharmacological analysis of positive chronotropic and inotropic responses to etilefrine in isolated dog heart preparations

Efficacy of Servo-Controlled Splanchnic Venous Compression in the Treatment of Orthostatic Hypotension

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