Drug information of Nicardipine
Mechanism of effect
By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.
Onset: PO, 0.5-2 hr; IV, 10-20 min
Duration: Immediate release and IV, 8 hr; extended release, 8-12 hr
Peak plasma time: Immediate release, 0.5-2 hr; extended release, 2-4 hr
Protein bound: 95%
Vd: 8.3 L/kg
Metabolized in liver by CYP3A4 (first pass)
Metabolites: Pyridine analogue (inactive)
Half-life: 2-4 hr
Dialyzable: HD, no
Total plasma clearance: IV, 0.3-0.9 L/hr/kg; PO, 1.62-7.86 L/hr/kg
Excretion: Urine (60%), feces (35%)
PO: 20-40 mg (conventional) q8hr or 30-60 mg (extended release) q12hr
IV: 5 mg/hr by slow infusion (50 mL/hr) initially; may be increased by 2.5 mg/hr every 15 minutes; not to exceed 15 mg/hr
IV as substitute for conventional PO
- PO dose: 20 mg q8hr; equivalent IV infusion: 0.5 mg/hr
- PO dose: 30 mg q8hr; equivalent IV infusion: 1.2 mg/hr
- PO dose: 40 mg q8hr; equivalent IV infusion: 2.2 mg/hr
- If transitioning to PO nicardipine, initiate PO dosing 1 hr before discontinuance of IV
Chronic Stable Angina
20-40 mg (conventional) PO q8hr
Start at 20 mg, and allow 3 days between dose increases to achieve steady-state plasma drug concentration; usual dosage range, 60-120 mg/day
Not approved by FDA; limited data available
0.5-3 mcg/kg/min IV
Drug contraindicationsAortic Stenosis
InteractionsDaunorubicin , fentanyl , Doxazosin , Axitinib , Dolasetron , brigatinib , Copanlisib , Dabrafenib , Cabazitaxel , Erythromycin , Everolimus , Itraconazole , Tadalafil , Tamsulosin , Trastuzumab , lofexidine , lurasidone , Venetoclax , Ruxolitinib , conivaptan , bosutinib , bedaquiline , neratinib , vemurafenib , Sonidegib , Avanafil , Cabozantinib , Cobimetinib , Ceritinib , Eliglustat , Acalabrutinib , Palbociclib , Ibrutinib , Pimavanserin , trabectedine , Apalutamide , Osimertinib , Mefloquine , Ribociclib , Idelalisib , Regorafenib , Ponatinib , Nefazodone , Dantrolene , Vilazodone , Ivabradine , pomalidomide , Tofacitinib , Carbamazepine , Ketoconazole , Daclatasvir , Rifabutin , Oxycodone , Lomitapide , Topotecan , Dihydroergotamine , Rifampin , Cimetidine , Fluticasone , Lovastatin , Ixazomib , Tasimelteon , Flibanserin , Estazolam , Edoxaban , Treprostinil , Abemaciclib , riociguat , Cannabidiol , lasmiditan
May cause symptomatic hypotension or tachycardia; titrate slowly to avoid systemic hypotension and possible negative inotropic effects with congestive heart failure (CHF), angina, and left ventricular dysfunction (particularly during treatment initiation, after dose increase, or after withdrawal of beta blocker)
To reduce possibility of venous thrombosis, phlebitis, and vascular impairment, do not use small veins, such as those on dorsum of hand or wrist; avoid intraarterial administration or extravasation
Caution should be exercised when using the drug in congestive heart failure patients, particularly in combination with a beta-blocker; nicardipine gives no protection against dangers of abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of dose of beta-blocker, preferably over 8 to 10 days
Closely monitor response in patients with angina, congestive heart failure, impaired hepatic function, portal hypertension, and renal impairment and pheochromocytoma
Peripheral edema may occur
Exacerbation of angina or MI reported with dosage titration of dihydropyridine calcium-channel blockers
With acute cerebral infarction or hemorrhage, titrate slowly to avoid systemic hypotension
Use with caution in patients with hypertrophic cardiomyopathy and mild-to-moderate aortic stenosis
Use with caution in hepatic or renal impairment; lower doses may be required
Use with caution in hypertension associated with pheochromocytoma and portal hypertension when administering IV
Change infusion site every 12 hr to minimize risk of peripheral venous irritation
Blood pressure starts to fall within min of infusion; calcium channel blockers, may occasionally produce symptomatic hypotension; caution is advised to avoid systemic hypotension when administering drug to patients who have sustained acute cerebral infarction or hemorrhage
Extended-release form not recommended for angina
Points of recommendation
Follow all directions on your prescription label and read all medication guides or instruction sheets. Your doctor may occasionally change your dose. Use the medicine exactly as directed.
Do not crush, chew, break, or open an extended-release capsule. Swallow it whole.
You may have more severe or more frequent episodes of angina when you first start taking nicardipine, or whenever your doses are changed.
Your blood pressure will need to be checked often.
Do not stop using any of your medications suddenly. Stopping suddenly may make your condition worse.
Store at room temperature away from moisture, heat, and light. Keep the bottle tightly closed when not in use.
Take the medicine as soon as you can, but skip the missed dose if it is almost time for your next dose. Do not take two doses at one time.