Nicardipine, a new intravenous calcium antagonist: a review of its pharmacology, pharmacokinetics, and perioperative applications

The cardiovascular responses to an infusion of KRN2391, a potassium channel opener, was studied in halothane-anesthetized dogs. Intravenous administration of KRN2391 at 1.0 and 5.0 μg·kg·min for 60 min produced dose-dependent decreases in mean arterial pressure (MAP) and systemic vascular resistance (SVR) associated with dose-dependent increases in the cardiac index (CI) and stroke volume index (SVI) but was not accompanied by an increase in heart rate (HR). The maximum decrease in MAP during the infusion of KRN2391 at 1.0 and 5.0 μg·kg·min was -13±7% (P<0.01) and -37±10% (P<0.01), respectively. The maximum reduction in SVR after 1.0 and 5.0 μg·kg·min was -20±11% (P<0.01) and -60±16% (P<0.01), respectively. A KRN2391 infusion of 1.0 and 5.0 μg·kg·min increased Cl a maximum of 11±13% (P<0.05) and 65±33% (P<0.01), respectively. KRN2391 1.0 μg·kg·min showed a tendency to increase SVI but this change was not significant, KRN2391 5.0 μg·kg·min, however, produced a significant increase in SVI. The present results demonstrate that the decrease in MAP and the increases in CI and SVI caused by KRN2391 are due to a reduction in the afterload. Therefore, we conclude that these cardiovascular profiles of KRN2391 may be benificial in perioperative uses including the control of systemic blood pressure and the treatment of hypertension during halothane anesthesia in clinical practice.

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“…Although both organic nitrates and calcium channel antagonists produce antihypertensive actions, their cardiovascular effects are different [1].…”

Section: Introductionmentioning

confidence: 99%

Hemodynamic effects of KRN2391 (potassium channel opener) in halothane-anesthetized dogs

et al. 1995

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“…11 It is not only a potent arterial vasodilator, but also produces a favourable effect on the coronary circulation 12 and is devoid of systemic toxicity. 13 Intravenous nicardipine has proven to be an effective anti-hypertensive treatment in cases of moderate-to-severe hypertension, 14 and is as effective as sodium nitroprusside for the immediate control of blood pressure in patients with severe hypertension. 15 It has also proven to be as effective as nitroprusside for the control of hypertension after coronary artery bypass grafting.…”

Section: Discussionmentioning

confidence: 99%

Nicardipine Hydrochloride Injectable Phase IV Open-Label Clinical Trial: Study on the Anti-Hypertensive Effect and Safety of Nicardipine for Acute Aortic Dissection

et al. 2002

J Int Med Res

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We performed a multicentre, phase IV, open-label clinical trial to examine the clinical usefulness of a continuous infusion of nicardipine hydrochloride to control hypertension in 31 patients with acute aortic dissection. Target blood pressure levels were reached within 15 min in 16 patients; in 15-30 min in 10 patients; in 30-45 min in three patients; and in 45-60 min in two patients. Baseline average systolic, diastolic and mean arterial blood pressures were 147 +/- 23 mmHg, 82 +/- 18 mmHg and 104 +/- 18 mmHg, respectively, with third-day pressures significantly reduced at 119 +/- 12 mmHg, 69 +/- 9 mmHg and 86 +/- 8 mmHg. Blood pressures after discontinuation of the infusion were not significantly different from those measured on the third day of infusion and no definite adverse effects attributable to the treatment were observed. Nicardipine hydrochloride was both effective and safe at controlling blood pressure in patients with acute aortic dissection.

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“…They inhibit calcium entry into vascular smooth muscles, lowering systemic vascular resistance and blood pressure. They increase cardiac output, cerebral and renal flow [1,2,15]. Nicardipine has less negative inotropic effects and produces less tachycardia then the other calcium channel antagonists [13].…”

Section: References Discussionmentioning

confidence: 99%

“…Its properties, water solubility, short half-life, rapidity of therapeutic response and dose dependent reduction of blood pressure, have made it a first line drug for management of hypertensive episodes in adult patients with vital distress [8, 10,15,16]. To our knowledge, no data are available about utilisation of intravenous nicardipine in children.…”

Section: Introductionmentioning

confidence: 99%

Intravenous nicardipine in hypertensive children

et al. 1993

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Fourteen hypertensive patients hospitalized in a paediatric intensive care unit were studied to evaluate safety and hypotensive efficacy of intravenous nicardipine. Systolic and diastolic blood pressure significantly decreased 1 h after the beginning of the treatment (1 microgram/kg per minute). Mean decrease in systolic blood pressure during the first 24 h was between 9.9% and 13.4% of the initial value. Mean lowering of diastolic blood pressure was between 16.7% and 25.6%. Nicardipine did not significantly affect heart rate with dose of 1 microgram/kg per minute. No clinical side-effects were observed. Nicardipine could be a first line drug for the treatment of hypertension in paediatric intensive care units.

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Nicardipine, a new intravenous calcium antagonist: a review of its pharmacology, pharmacokinetics, and perioperative applications

Cited by 50 publications

References 37 publications

Hemodynamic effects of KRN2391 (potassium channel opener) in halothane-anesthetized dogs

Hemodynamic effects of KRN2391 (potassium channel opener) in halothane-anesthetized dogs

Nicardipine Hydrochloride Injectable Phase IV Open-Label Clinical Trial: Study on the Anti-Hypertensive Effect and Safety of Nicardipine for Acute Aortic Dissection

Intravenous nicardipine in hypertensive children

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