CARDENE I.V.: Selective Mechanism of Action

“The mechanism of action of [calcium channel blockers]…produces vasodilation and lowers blood pressure by reducing systemic vascular resistance….”

— Wallin JD et al. Arch Intern Med. 1989¹

CARDENE I.V. is a calcium ion influx inhibitor (slow channel blocker or calcium channel blocker). It prevents calcium ions from entering cardiac and vascular smooth muscle cells. The contractile processes of cardiac muscle and vascular smooth muscle depend upon the movement of extracellular calcium ions into these cells through specific ion channels. The drug, which is more selective to vascular smooth muscle, causes arteries to dilate and blood pressure to decrease.

A Pure Afterload Reducer

• Arteriolar vasodilation provides selective decrease in systemic vascular resistance (SVR)²

• Maintains or increases cardiac output²

• Does not induce bradycardia²

• Is more selective to vascular smooth muscle than cardiac muscle²

Abrupt Increase in SVR Triggers Acute Hypertension^4,5

• CARDENE I.V. produces significant decreases in SVR² .

• Hemodynamic studies demonstrate significant increases in ejection fraction and cardiac output²

• CARDENE I.V. is a potent arteriolar dilator²

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Important Safety Information
Close monitoring of the blood pressure is required during therapy. CARDENE I.V. is contraindicated in patients with known hypersensitivity to the drug and in patients with advanced aortic stenosis. Reduction of diastolic pressure and reduced afterload may worsen rather than improve myocardial oxygen balance. Caution is advised when administering CARDENE I.V. to patients with impaired renal or hepatic function, in combination with a beta-blocker in patients with congestive heart failure, or portal hypertension. Observe caution in patients with significant left ventricular dysfunction due to possible negative inotropic effect. CARDENE I.V. gives no protection against the dangers of abrupt beta-blocker withdrawal; beta-blocker dosage should be gradually reduced. Levels of cyclosporine should be closely monitored during therapy. The most common side effects of CARDENE I.V. are headache (14.6%), hypotension (5.6%), nausea/vomiting (4.9%), and tachycardia (3.5%). Less frequent adverse effects, in each case occurring at 1.4%, include ECG abnormalities, postural hypotension, ventricular extrasystoles, injection-site reaction, dizziness, sweating and polyuria.

Please see full prescribing information.

References: 1. Wallin JD, Fletcher E, Ram CVS, et al. Intravenous nicardipine for the treatment of severe hypertension: a double-blind, placebo-controlled multicenter trial. Arch Intern Med. 1989;149(12):2662-2669. 2. CARDENE I.V. prescribing information, 2008. EKR Therapeutics, Bedminster, NJ. 3. Kerins DM, Robertson RM, Robertson D. Drugs used for the treatment of myocardial ischemia. In: Hardman JG, Limbird LE, Gilman AG, eds. Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill; 2001:843-870. 4. Marik PE, Varon J. Hypertensive crises: challenges and management. Chest. 2007;131(6):1949-1962. 5. Rose JC, Mayer SA. Optimizing blood pressure in neurological emergencies. Neurocrit Care. 2004;1(3):287-299. 6. Kaplan NM. Systemic hypertension: mechanisms and diagnosis. In: Zipes DP, Libby P, Bonow R, Braunwald E, eds. Braunwald's Heart Disease: a Textbook of Cardiovascular Medicine. 7th ed. Philadelphia, PA: Elsevier Saunders; 2005;959-987. 7. Labetalol [package insert]. Bedford, OH: Bedford Laboratories; 2000. 8. Oates JA, Brown NJ. Antihypertensive agents and the drug therapy of hypertension. In: Hardman JG, Limbird LE, Gilman AG, eds. Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 10th ed. New York, NY: McGraw-Hill; 2001:871-900. 9. Nitropress. Drugs.com Web site. http:www.drugs.com/pro/nitropress.html. Accessed July 22, 2009. 10. Hydralazine. Drugs.com Web site. http:www.drugs.com/pro/hydralazine.html?printable =1. Accessed July 22, 2009. 11. Nitroglycerin. Drugs.com Web site. http:www.drugs.com/pro/nitroglycerin.html?printable=1. Accessed July 22, 2009. 12. Esmolol. Drugs.com Web site. http:www.drugs.com/pro/esmolol.html. Accessed July 22, 2009.

© EKR Therapeutics, Inc. All rights reserved. August 2009.