N-Methyldopamine (epinine), one of the few modifications of the dopamine (DA) molecule that retains agonist activity at the DA1 receptor, was administered orally as the diisobutyric ester, ibopamine (100, 200, and 300 mg), to 15 patients with congestive heart failure. An increase in cardiac index and decline in systemic vascular resistance was observed with each dose, and these hemodynamic effects persisted for 3 to 6 hr. Small transient increments in right atrial and pulmonary capillary wedge pressures occurred 0.5 hr after ingestion of 200 and 300 mg of ibopamine, but these pressures returned to baseline or lower levels within 30 min. Heart rate and mean arterial pressure were unchanged. Plasma concentrations of epinine peaked 0.5 hr after administration of drug and then declined to minimal levels at 3 hr. Ten patients enrolled in a trial to evaluate the efficacy of long-term therapy with ibopamine; after 8 weeks of treatment, the initial hemodynamic responses to the drug were attenuated and no significant improvement in oxygen uptake at peak exercise was observed. A decline in plasma norepinephrine concentrations, which could be attributed to activation of alpha 2-adrenoceptors and/or DA2 receptors on sympathetic nerves, was observed after initial administration of ibopamine and persisted after long-term drug ingestion; no long-term hemodynamic benefit could be ascribed to the reduction in sympathetic activity.

Effects of long-term therapy with oral ibopamine on resting hemodynamics and exercise capacity in patients with heart failure: relationship to the generation of N-methyldopamine and to plasma norepinephrine levels.

Ibopamine is an orally active derivative of dopamine which undergoes hydrolysis to the active moiety epinine. In single-dose and short term studies ibopamine demonstrated inotropic and vasodilating properties. It improved cardiac and systemic haemodynamics by increasing cardiac output and reducing afterload, both at rest and during exercise. In non-comparative clinical studies ibopamine produced benefits in functional class and clinical symptoms for up to 1 year in patients with moderate to severe congestive heart failure. Similarly, short term comparative studies with placebo have indicated ibopamine as a useful adjunct in the treatment of patients maintained on conventional therapy with digoxin, diuretics and vasodilators. Preliminary evidence also suggests that ibopamine is as effective as digoxin in the treatment of patients with moderate congestive heart failure. Should the results of long term comparative studies confirm these encouraging findings, ibopamine will be a useful addition to the drugs available or as an alternative to digoxin for the treatment of congestive heart failure.

Ibopamine. A preliminary review of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy.

Considerable effort and resources have been directed at the development and study of positive inotropic drugs over the past 10–15 years. Much has been learned about the physiology and pharmacology of myocardial contraction, the application of agents to augment contractility, and, importantly, the general and specific limitations of positive inotropic therapy. Studies on acute inotropic intervention have now shown that a drug's ability to augment overall cardiac performance is heavily dependent on its effects on vasculature, vascular control, and ventricular-vascular coupling. The clinical research on new agents has served to remind us how difficult it is to formulate the “ideal” positive inotropic or cardiovascular support drug for the critical care setting. The vast effort to develop a chronically and orally administrate drug to replace or even supplement digitalis has generally been disappointing. The dopaminergic agents (e.g., ibopamine, levodopa) act primarily via vasodilation and their effectiveness and role in managing heart failure remain unresolved. The initial excitement about the phosphodiesterase III inhibitors (e.g., amrinone, milrinone, enoximone) has been tempered by the results of large well-designed trials indicating variable effectiveness and a prominent adverse effect profile. During long-term oral administration none of these agents has been shown to improve clinical status or exercise capacity beyond that achieved by digoxin, when administered either separately or in combination with digoxin. The Prospective Randomized Milrinone Survival Evaluation (PROMISE) trial, showing that repeated oral administration of milrinone can increase mortality in heart failure, is having a devastating effect on the further development of this class of drugs. Investigation is proceeding at basic levels to unravel the intricate mechanisms of myocardial contraction and we are beginning to see the results of this research. Agents have been developed to “sensitize” the contractile apparatus to calcium and to act in very precise locations. We are hopeful that some of these agents will have a favorable benefit to adverse effect ratio and earn a position in the clinical therapeutics of heart failure.

Current status of non-digitalis positive inotropic drugs

Ibopamine as a substitute for digitalis in patients with congestive heart failure on chronic digoxin therapy

In 7 patients with congestive heart failure acute oral administration of ibopamine, a new dopamine derivative, induced a significant decrease in serum prolactin and aldosterone without affecting serum growth hormone or cortisol. The Metoclopramide-induced secretion of prolactin and aldosterone was blunted in 6 patients pretreated with 200 mg ibopamine. The data are consistent with a dopaminergic effect of ibopamine due to a peripheral action, probably on D-2 receptors.

Inhibition of prolactin and aldosterone secretion by the dopamine derivative ibopamine

The acute effects of ibopamine, a new, orally active dopaminergic agent, were assessed invasively in 8 patients with congestive heart failure (NYHA Class IV). The cardiac Index increased (P<0.01) and preload and afterload decreased (P<0.05) after a single mean dose of ibopamine 1.4 mg/kg. The peak effect occurred after 1 to 3 h and activity was still demonstrable after 4 to 6 h. There was no change in blood pressure, heart rate or rhythm. No clinical evidence of cardiac toxicity or side effects was noted. Oral ibopamine shows promise in the treatment of congestive heart failure, but more extensive studies after chronic treatment are desirable.

Ibopamine in very severe congestive heart failure: pilot haemodynamic invasive assessment.

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Ibopamine in very severe congestive heart failure: pilot haemodynamic invasive assessment.