pharmacopeia
GET
/api/v1/drug/nicardipine
2D structure
5-O-[2-[benzyl(methyl)amino]ethyl] 3-O-methyl 2,6-dimethyl-4-(3-nitrophenyl)-1,4-dihydropyridine-3,5-dicarboxylate
SMILES CC1=C(C(C(=C(N1)C)C(=O)OCCN(C)CC2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OC
InChIKey ZBBHBTPTTSWHBA-UHFFFAOYSA-N

Mechanism of action

Sourced from openFDA

Nicardipine hydrochloride capsules are a calcium entry blocker (slow channel blocker or calcium ion antagonist) that inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle without changing serum calcium concentrations. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels.

Calcium ChannelCytochrome P450 2C19Cytochrome P450 2C8Cytochrome P450 2D6Cytochrome P450 3A4L-Calcium Channel Receptor

Indications

Sourced from openFDA
  • I. Stable Angina Nicardipine hydrochloride capsules are indicated for the management of patients with chronic stable angina (effort-associated angina).ICD-10: I20.9

Contraindications

Sourced from openFDA
  • Nicardipine hydrochloride capsules are contraindicated in patients with hypersensitivity to the drug. Because part of the effect of nicardipine hydrochloride capsules are secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis.contraindicated

Dosage & administration

Sourced from openFDA

Angina The dose should be individually titrated for each patient beginning with 20 mg three times daily. Doses in the range of 20 to 40 mg three times a day have been shown to be effective. At least 3 days should be allowed before increasing the nicardipine hydrochloride capsuels dose to ensure achievement of steady-state plasma drug concentrations. Concomitant Use With Other Antianginal Agents Sublingual NTG may be taken as required to abort acute anginal attacks during nicardipine hydrochloride capsules therapy. Prophylactic Nitrate Therapy: nicardipine hydrochloride capsules may be safely coadministered with short- and long-acting nitrates. Beta-blockers : Nicardipine hydrochloride capsules may be safely coadministered with beta-blockers (see Drug Interactions ). Hypertension The dose of nicardipine hydrochloride capsules should be individually adjusted according to the blood pressure response beginning with 20 mg three times daily. The effective doses in clinical trials have ranged from 20 mg to 40 mg three times daily. The maximum blood pressure lowering effect occurs approximately 1 to 2 hours after dosing. To assess the adequacy of blood pressure response, the blood pressure should be measured at trough (8 hours after dosing). Because of the prominent peak effects of nicardipine, blood pressure should be measured 1 to 2 hours after dosing, particularly during initiation of therapy (see PRECAUTIONS : Blood Pressure , INDICATIONS AND USAGE , CLINICAL PHARMACOLOGY , Effects in Hypertension ).

Warnings & precautions

Sourced from openFDA

Increased Angina About 7% of patients in short-term, placebo-controlled angina trials have developed increased frequency, duration or severity of angina on starting nicardipine hydrochloride capsules or at the time of dosage increases, compared with 4% of patients on placebo. Comparisons with beta-blockers also show a greater frequency of increased angina, 4% vs 1%. The mechanism of this effect has not been established (see ADVERSE REACTIONS ). Use in Patients With Congestive Heart Failure Although preliminary hemodynamic studies in patients with congestive heart failure have shown that nicardipine hydrochloride capsules reduced afterload without impairing myocardial contractility, it has a negative inotropic effect in vitro and in some patients. Caution should be exercised when using the drug in congestive heart failure patients, particularly in combination with a beta-blocker. Beta-Blocker Withdrawal Nicardipine hydrochloride capsules are not a beta-blocker and therefore gives no protection against the dangers of abrupt beta-blocker withdrawal; any such withdrawal should be by gradual reduction of the dose of beta-blocker, preferably over 8 to 10 days.

Adverse reactions

Sourced from openFDA

In multiple-dose U.S. and foreign controlled short-term (up to 3 months) studies 1910 patients received nicardipine hydrochloride capsules alone or in combination with other drugs. In these studies adverse events were reported spontaneously; adverse experiences were generally not serious but occasionally required dosage adjustment and about 10% of patients left the studies prematurely because of them. Peak responses were not observed to be associated with adverse effects during clinical trials, but physicians should be aware that adverse effects associated with decreases in blood pressure (tachycardia, hypotension, etc.) could occur around the time of the peak effect. Most adverse effects were expected consequences of the vasodilator effects of nicardipine hydrochloride capsules. Angina The incidence rates of adverse effects in anginal patients were derived from multicenter, controlled clinical trials. Following are the rates of adverse effects for nicardipine hydrochloride capsules (n=520) and placebo (n=310), respectively, that occurred in 0.4% of patients or more. These represent events considered probably drug-related by the investigator (except for certain cardiovascular events that were recorded in a different category). Where the frequency of adverse effects for nicardipine hydrochloride capsules and placebo is similar, causal relationship is uncertain. The only dose-related effects were pedal edema and increased angina.

Use in specific populations

Sourced from openFDA

Pregnancy Pregnancy Category C Nicardipine was embryocidal when administered orally to pregnant Japanese White rabbits, during organogenesis, at 150 mg/kg/day (a dose associated with marked body weight gain suppression in the treated doe) but not at 50 mg/kg/day (25 times the maximum recommended antianginal or antihypertensive dose in man). No adverse effects on the fetus were observed when New Zealand albino rabbits were treated, during organogenesis, with up to 100 mg nicardipine/kg/day (a dose associated with significant mortality in the treated doe). In pregnant rats administered nicardipine orally at up to 100 mg/kg/day (50 times the maximum recommended human dose) there was no evidence of embryolethality or teratogenicity. However, dystocia, reduced birth weights, reduced neonatal survival, and reduced neonatal weight gain were noted. There are no adequate and well-controlled studies in pregnant women. Nicardipine hydrochloride capsules should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Nursing Mothers Studies in rats have shown significant concentrations of nicardipine in maternal milk following oral administration. For this reason it is recommended that women who wish to breastfeed should not take this drug. Pediatric Use Safety and efficacy in patients under the age of 18 have not been established.

Overdosage

Sourced from openFDA

Overdosage with a 600-mg single dose (15 to 30 times normal clinical dose) has been reported. Marked hypotension (blood pressure unobtainable) and bradycardia (heart rate 20 bpm in normal sinus rhythm) occurred, along with drowsiness, confusion and slurred speech. Supportive treatment with a vasopressor resulted in gradual improvement with normal vital signs approximately 9 hours posttreatment. Based on results obtained in laboratory animals, overdosage may cause systemic hypotension, bradycardia (following initial tachycardia) and progressive atrioventricular conduction block. Reversible hepatic function abnormalities and sporadic focal hepatic necrosis were noted in some animal species receiving very large doses of nicardipine. For treatment of overdose standard measures (for example, evacuation of gastric contents, elevation of extremities, attention to circulating fluid volume, and urine output) including monitoring of cardiac and respiratory functions should be implemented. The patient should be positioned so as to avoid cerebral anoxia. Frequent blood pressure determinations are essential. Vasopressors are clinically indicated for patients exhibiting profound hypotension.

Approval history

Sourced from openFDA
  • Jan 30, 1992NDANDA019734Chiesi
  • Oct 28, 1996ANDAANDA074670Ani Pharms
  • Mar 19, 1998ANDAANDA074928Epic Pharma Llc
  • Jul 24, 2008NDANDA022276Hikma Intl Pharms
  • Nov 17, 2009ANDAANDA090534Am Regent
  • Nov 17, 2009ANDAANDA090664Somerset Theraps Llc
  • Nov 17, 2009ANDAANDA090671Mankind Pharma
  • Apr 8, 2021ANDAANDA211121Eugia Pharma

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
4,258 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Acute Kidney Injury2375.6%
  2. 2Premature Baby2054.8%
  3. 3Off Label Use2014.7%
  4. 4Foetal Exposure During Pregnancy1954.6%
  5. 5Drug Ineffective1914.5%
  6. 6Maternal Exposure During Pregnancy1834.3%
  7. 7Hypotension1704.0%
  8. 8Drug Interaction1673.9%
  9. 9Hypertension1613.8%
  10. 10Pyrexia1222.9%
  11. 11Premature Delivery1082.5%
  12. 12Exposure During Pregnancy1042.4%
  13. 13Renal Failure1022.4%
  14. 14Vomiting1022.4%
  15. 15Anaemia1012.4%

Literature

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Recent PubMed references pinned to Nicardipine as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 67 ClinicalTrials.gov registrations naming Nicardipine as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Structural analogs

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Ranked by 2D fingerprint (Tanimoto) similarity over PubChem structures. Structural proximity only — not a claim of therapeutic equivalence.

Frequently asked questions

How does Nicardipine work?
Nicardipine hydrochloride capsules are a calcium entry blocker (slow channel blocker or calcium ion antagonist) that inhibits the transmembrane influx of calcium ions into cardiac muscle and smooth muscle without changing serum calcium concentrations. The contractile processes of cardiac muscle and vascular smooth muscle are dependent upon the movement of extracellular calcium ions into these cells through specific ion channels.
What is Nicardipine used for?
According to FDA labeling, Nicardipine carries indications including: I. Stable Angina Nicardipine hydrochloride capsules are indicated for the management of patients with chronic stable angina (effort-associated angina).. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Nicardipine?
Nicardipine is classified as Dihydropyridine derivatives, Dihydropyridine Calcium Channel Blocker, Calcium Channel Antagonists, Cytochrome P450 2C19 Inhibitors, Cytochrome P450 2C8 Inhibitors, Cytochrome P450 2D6 Inhibitors, Cytochrome P450 3A4 Inhibitors, L-Calcium Channel Receptor Antagonists, Coronary Arterial Vasodilation, Decreased Blood Pressure.
What are the brand names for Nicardipine?
Nicardipine is marketed under brand names including Cardene.
What are the contraindications for Nicardipine?
Nicardipine labeling lists contraindications including: Nicardipine hydrochloride capsules are contraindicated in patients with hypersensitivity to the drug. Because part of the effect of nicardipine hydrochloride capsules are secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis.. Always consult the full prescribing information and a clinician.
Note. Data for nicardipine is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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