Nicardipine
- Atc Codes:C08CA04
- CAS Codes:54527-84-3#55985-32-5
- PHARMGKB ID:54527-84-3#55985-32-5
Table of contents
- Brand Names
- Chemistry
- Pharmacologic Category
- Mechanism of Action
- Therapeutic Use
- Unlabeled Use
- Pregnancy and Lactation Implications
- Contraindications
- Warnings and Precautions
- Adverse Reactions
- Toxicological Effects
- Caution and personalized dose adjustment in patients with the following genotypes
- Other genes that may be involved
- Substrate of
- Inhibits
- Induces
- Drug Interactions
- Nutrition/Nutraceutical Interactions
- Dosage
- Pharmacokinetics and Pharmacodynamics
- Special Considerations
Brand Names
Europe
Belgium: Rydene; France: Loxen, Nicardipine; Germany: Antagonil; Italy: Bionicard, Lisanirc, Nicardal, Nicardipina, Nicarpin, Nicaven, Perdipina, Vasodin; Luxembourg: Rydene; Netherlands: Cardene; Portugal: Nerdipina; Spain: Dagan, Flusemide, Lecibral, Lincil, Lucenfal, Nerdipidina, Nicardipino, Vasonase; UK: Cardene.
North America
USA: Cardene.
Asia
Japan: Apodipine, Aprovan, Cartran, Cepadipin, Coponent, Dromer, Isedipeal, Nicadirus L, Nicardirate, Nicarpine, Nicodel, Nisutadil, Perdipine, Plealpin, Radistmin, Salipex, Tsurusepin.
Drug combinations
Chemistry
Nicardipine Hydrochloride: C~26~H~29~N~3~O~6~ HCl. Mw: 515.99. (1) 3,5-Pyridinedicarboxylic acid, 1,4-dihydro-2,6-dimethyl-4-(3-nitrophenyl)-, methyl 2-[methyl(phenylmethyl)amino]ethyl ester, monohydrochloride; (2) 2-(Benzylmethylamino)ethyl methyl 1,4-dihydro-2,6-dimethyl-4-(m-nitrophenyl)-3,5-pyridinedicarboxylate monohydrochloride. CAS-54527-84-3; CAS-55985-32-5 (nicardipine)(1979).
Pharmacologic Category
Vasodilating Agents, Miscellaneous. Calcium-Channel Blocking Agents; Dihydropyridines. (ATC-Code: C08CA04).
Mechanism of action
Inhibits calcium ions from entering «slow channels» or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing relaxation of coronary vascular smooth muscle and coronary vasodilation. Increases myocardial oxygen delivery in vasospastic angina.
Therapeutic use
Chronic stable angina. Management of hypertension.
Pregnancy and lactiation implications
Crosses placenta. May exhibit tocolytic effects. Not recommended in nursing women.
Unlabeled use
Congestive heart failure. Control of blood pressure in acute ischemic stroke and spontaneous intracranial hemorrhage. Postoperative hypertension associated with carotid endarterectomy. Perioperative hypertension. Prevention of migraine headaches. Subarachnoid hemorrhage-associated cerebral vasospasm.
Contraindications
Hypersensitivity to nicardipine or any component of the formulation. Advanced aortic stenosis.
Warnings and precautions
Increased angina and/or myocardial infarction occurred with initiation or dosage titration of dihydropyridine calcium channel blockers. Symptomatic hypotension with or without syncope can rarely occur. Peripheral edema common. Reflex tachycardia may occur. Use with caution in heart failure. Use in severe left ventricular dysfunction may experience worsened symptoms of heart failure due to mild negative inotropic effects of nicardipine. Use with caution in hepatic impairment, in hypertrophic cardiomyopathy and outflow tract obstruction (reduction in afterload may worsen symptoms associated with this condition), and in portal hypertension (can cause increase in hepatic pressure gradient). Concurrent fentanyl anesthesia and I.V. nicardipine (with a β-blocker) may result in hypotension. Peripheral infusion sites (for I.V. therapy) should be changed every 12 hours. Abrupt withdrawal may cause rebound angina in coronary artery disease.