Nicardipine Hydrochloride 2.5 mg/mL Injection, Solution
Other active recalls for Nicardipine Hydrochloride (different manufacturers) — 4 · tap to view
Past resolved recalls for this product (1)
🆔 Identity & classification
Where does this data come from?
🏷️ RxNorm drug class
This medicine belongs to the Dihydropyridine Calcium Channel Blocker class.
Where does this data come from?
🏭 Manufacturer & labeler
Where does this data come from?
🩺 Clinical
- Nicardipine is a calcium channel blocker — a type of blood pressure medication. The oral capsules treat two things: high blood pressure and chronic stable angina, which is chest pa...
- It can, yes — dizziness, headaches, and flushing are among the more common side effects, since the medication works by widening blood vessels. Most people find these effects mild a...
- Will nicardipine make me dizzy or give me headaches?
- That depends on which medications. A few important ones to know about: if you take cyclosporine or tacrolimus (common transplant drugs), nicardipine can raise those drug levels sig...
Patient education
Supplement & herbal interactions
Nicardipine may be associated with lower levels of 2 nutrients — worth a chat with your pharmacist, not a cause for alarm.
Where does this data come from?
Ask a licensed pharmacist directly — free, answered by our team.
🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
💡 Tap an ingredient (hover on desktop) to see what it is and why it’s used.
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0.525 mg / 1 mL
UNII 2968PHW8QP
A weak organic acid derived from citrus fruits or made through fermentation. It works as a buffer to control pH, a preservative to extend shelf life, and a flavoring agent in medications.
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0.04 mg / 1 mL
UNII 7FLD91C86K
Edetate disodium is a chemical compound that binds and removes certain metal ions. In medicines, it acts as a preservative and stabilizer by preventing metals like calcium from interfering with the product's shelf life and consistency.
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0.09 mg / 1 mL
UNII 55X04QC32I
A strong alkaline chemical used to adjust and maintain the pH balance of liquid medicines. It helps keep the medicine stable and ensures it stays effective during storage.
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48 mg / 1 mL
UNII 506T60A25R
Sorbitol is a natural sugar alcohol derived from glucose. It serves as a sweetener, humectant, and bulking agent in medications to improve taste and help maintain moisture in the product.
4 inactive ingredients listed in the exact product block matched to this NDC.
Where does this data come from?
ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
Are inactive ingredients the same for every manufacturer?
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per mL | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | Not in the retail survey — common for institutional, discontinued, or low-volume packs. | |
| Medicaid paysCMS SDUD · 12 mo | $2.52 | $252.40 / 100 ml |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
| Medicare Part B allowsASP · J2404 | $0.070 / J2404 unit | — |
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🧾 Billing & reimbursement
Where does this data come from?
🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Nicardipine Hydrochloride 2.5 mg/mL 00143-9542-10 | Hikma | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mL 00143-9593-10 | West-Ward | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 25 mg/10mL 00143-9689-10 | Hikma | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mL 00517-0735-10 | American | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mL 25021-0333-10 | Sagent | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mL 42571-0394-89 | Micro | 10 vials | — | AP | FDA listed | — |
| Cardene Iv 2.5 mg/10mL 43066-0029-10 | Baxter | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 25 mg/10mL 51662-1482-01 | HF | 10 ml | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 25 mg/10mL 55150-0183-11 | Eugia | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 25 mg/10mL 65219-0818-10 | Fresenius | 1 vial | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mL 67184-0611-02 | Qilu | 10 vials | — | AP | FDA listed | — |
| Nicardipine hydrochloride 2.5 mg/mL 70756-0686-10 | Lifestar | 10 vials | — | AP | FDA listed | — |
| nicardipine hydrochloride 2.5 mg/mL 71288-0204-11 | Meitheal | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 25 mg/10mL 72485-0116-10 | Armas | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mLthis 72572-0470-10 | Civica, | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 2.5 mg/mL 72819-0149-07 | Archis | 10 vials | — | AP | FDA listed | — |
| Nicardipine Hydrochloride 25 mg/10mL 82432-0103-01 | Chengdu | 1 vial | — | AP | FDA listed | — |
Where does this data come from?
⏳ Availability & generic status
This product is an FDA-approved generic. Other versions of the same drug are listed under Therapeutic equivalents, least expensive first.
Where does this data come from?
🗺️ Medicaid utilization & spend
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 72572-0470-10 You're viewing this | 10 VIAL in 1 CARTON (72572-470-10) / 10 mL in 1 VIAL (72572-470-01) | 2020-10-29 | Active |
🧭 About this NDC listing & data coverage
What data is (and isn’t) available for this NDC — tap to expand
| NDC identity (package / product / labeler codes) | ✓ Available |
| Labeler | ✓ Available |
| Product & package description | ✓ Available |
| Marketing category & status | ✓ Available |
| Active ingredient / dosage form / route | ✓ Available |
| FDA label (SPL via DailyMed) | ✓ Available |
| Package photos | ✓ Available |
| Inactive ingredients (structured) | ✓ Available |
| NADAC pharmacy acquisition price (CMS) | — Not published for this NDC CMS publishes NADAC only for NDCs reported in its retail-pharmacy survey. |
| Orange Book / therapeutic-equivalence data | ✓ Available |
| HCPCS J-code billing crosswalk | ✓ Available |
| Medicaid utilization (CMS SDUD) | ✓ Available |
Questions about this listing
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📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1. INDICATIONS AND USAGE niCARdipine hydrochloride injection is a calcium channel blocker indicated for the short-term treatment of hypertension when oral therapy is not feasible. ( 1.1 )
1.1Hypertension niCARdipine Hydrochloride Injection, USP is indicated for the short-term treatment of hypertension when oral therapy is not feasible or not desirable. For prolonged control of blood pressure, transfer patients to oral medication as soon as their clinical condition permits [see Dosage and Administration ( 2.1 )] .
⏱️ Dosage and Administration ▾
2. DOSAGE AND ADMINISTRATION For Intravenous Use. ( 2.1 ) Dilution is required.
( 2.3 ) When substituting for oral nicardipine therapy, use the intravenous infusion rate from the table below ( 2.1 ): Oral Nicardipine Dose Equivalent Intravenous Infusion Rate (0.1 mg/mL) 20 mg q8h 0.5 mg/hr = 5 mL/hr 30 mg q8h 1.2 mg/hr = 12 mL/hr 40 mg q8h 2.2 mg/hr = 22 mL/hr In a patient not receiving oral nicardipine, initiate therapy at 50 mL/hr (5 mg/hr) 0.1 mg/mL solution. Increase the infusion rate by 25 mL/hr every 5 minutes (for rapid titration) to 15 minutes (for gradual titration) up to a maximum of 150 mL/hr until desired blood pressure reduction is achieved.
( 2.1 ) If unacceptable hypotension or tachycardia occurs, discontinue the infusion. When blood pressure and heart rate stabilize, restart the infusion at low doses such as 30 to 50 mL/hr. ( 2.2 )
2.1Recommended Dosing niCARdipine Hydrochloride Injection, USP is intended for intravenous use. Vial must be diluted 0.1 mg/mL before use [see Dosage and Administration ( 2.3 )]. Titrate dose to achieve the desired blood pressure reduction.
Individualize dosage depending on the blood pressure to be obtained and the response of the patient. Dosage as a Substitute for Oral Nicardipine Therapy The intravenous infusion rate required to produce an average plasma concentration equivalent to a given oral dose at steady state is shown in the following table: Table 1: Oral Equivalent Dosage Oral Nicardipine Dose Equivalent Intravenous Infusion Rate (0.1 mg/mL) 20 mg q8h 0.5 mg/hr = 5 mL/hr 30 mg q8h 1.2 mg/hr = 12 mL/hr 40 mg q8h 2.2 mg/hr = 22 mL/hr Dosage for Initiation of Therapy in a Patient Not Receiving Oral Nicardipine Initiate therapy at 50 mL/hr (5 mg/hr).
If desired blood pressure reduction is not achieved at this dose, the infusion rate may be increased by 25 mL/hr (2.5 mg/hr) every 5 minutes (for rapid titration) to 15 minutes (for gradual titration) up to a maximum of 150 mL/hr (15 mg/hr), until desired blood pressure reduction is achieved. Following achievement of the blood pressure goal utilizing rapid titration, decrease the infusion rate to 30 mL/hr (3 mg/hr). Drug Discontinuation and Transition to an Oral Antihypertensive Agent Discontinuation of infusion is followed by a 50% offset of action in about 30 minutes.
If treatment includes transfer to an oral antihypertensive agent other than oral nicardipine, initiate therapy upon discontinuation of nicardipine hydrochloride injection. If oral nicardipine is to be used, administer the first dose 1 hour prior to discontinuation of the infusion. Specific Populations Titrate nicardipine hydrochloride injection slowly in patients with heart failure or impaired hepatic or renal function [see Warnings and Precautions ( 5.2 , 5.3 and 5.4 )]
2.2Monitoring The time course of blood pressure decrease is dependent on the initial rate of infusion and the frequency of dosage adjustment. With constant infusion, blood pressure begins to fall within minutes. It reaches about 50% of its ultimate decrease in about 45 minutes.
Monitor blood pressure and heart rate continually during infusion and avoid too rapid or excessive blood pressure drop during treatment. If there is concern of impending hypotension or tachycardia, the infusion should be discontinued. Then, when blood pressure has stabilized, restart infusion of nicardipine hydrochloride injection at low doses such as 30 to 50 mL/hr (3 to 5 mg/hr) and adjust to maintain desired blood pressure.
2.3Instructions for Administration Administer nicardipine hydrochloride by a central line or through a large peripheral vein. Change the infusion site every 12 hours if administered via peripheral vein [see Warnings and Precautions ( 5.5 )] . Preparation for Administration Vials must be diluted before infusion.
Inspection As with all parenteral drugs, nicardipine hydrochloride injection should be inspected visually for particulate matter and discoloration prior to administration, whenever solution an…
💊 Dosage Forms and Strengths ▾
3. DOSAGE FORMS AND STRENGTHS Injection: 25 mg of nicardipine hydrochloride in 10 mL (2.5 mg/mL) as a clear, yellow solution in a vial for dilution . niCARdipine hydrochloride injection is supplied in a vial containing 25 mg of nicardipine hydrochloride in 10 mL (2.5 mg/mL) for intravenous infusion. ( 3 )
⛔ Contraindications ▾
4. CONTRAINDICATIONS Do not use in patients with advanced aortic stenosis. ( 4.1 ).
4.1Advanced Aortic Stenosis Nicardipine hydrochloride injection is contraindicated in patients with advanced aortic stenosis because part of the effect of nicardipine hydrochloride injection is secondary to reduced afterload. Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.
⚠️ Warnings and Cautions ▾
5. WARNINGS AND PRECAUTIONS Closely monitor response in patients with angina, heart failure, impaired hepatic function, or renal impairment. ( 5.1 , 5.2 , 5.3 , 5.4 ) To reduce the possibility of venous thrombosis, phlebitis, and vascular impairment, do not use small veins, such as those on the dorsum of the hand or wrist.
Exercise extreme care to avoid intra-arterial administration or extravasation. ( 5.5 ) To minimize the risk of peripheral venous irritation, change the site of infusion of nicardipine hydrochloride every 12 hours. ( 5.5 )
5.1Exacerbation of Angina Increases in frequency, duration, or severity of angina have been seen in chronic oral therapy with oral nicardipine. Induction or exacerbation of angina has been seen in less than 1% of coronary artery disease patients treated with nicardipine hydrochloride. The mechanism of this effect has not been established.
5.2Exacerbation of Heart Failure Titrate slowly when using nicardipine hydrochloride injection, particularly in combination with a beta-blocker, in patients with heart failure or significant left ventricular dysfunction because of possible negative inotropic effects.
5.3Increased effect with Impaired Hepatic Function Since nicardipine is metabolized in the liver, consider lower dosages and closely monitor responses in patients with impaired liver function or reduced hepatic blood flow.
5.4Prolonged effect with Impaired Renal Function When nicardipine hydrochloride injection was given to mild to moderate hypertensive patients with moderate renal impairment, a significantly lower systemic clearance and higher area under the curve (AUC) was observed. These results are consistent with those seen after oral administration of nicardipine. Titrate gradually in patients with renal impairment.
5.5Local Irritation To reduce the possibility of venous thrombosis, phlebitis, local irritation, swelling, extravasation, and the occurrence of vascular impairment, administer drug through large peripheral veins or central veins rather than arteries or small peripheral veins, such as those on the dorsum of the hand or wrist. To minimize the risk of peripheral venous irritation, change the site of the drug infusion every 12 hours.
🤒 Adverse Reactions ▾
6. ADVERSE REACTIONS Most common adverse reactions are headache (15%), hypotension (6%), tachycardia (4%) and nausea/vomiting (5%). ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact American Regent, Inc. at 1-800-734-9236, or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. The adverse reaction information from clinical trials does, however, provide a basis for identifying the adverse events that appear to be related to drug use and for approximating rates. Two hundred forty-four patients participated in two multicenter, double-blind, placebo-controlled trials of nicardipine hydrochloride injection.
Adverse experiences were generally not serious and most were expected consequences of vasodilation. Adverse experiences occasionally required dosage adjustment. Therapy was discontinued in approximately 12% of patients, mainly due to hypotension, headache, and tachycardia.
Table 2 shows percentage of patients with adverse reactions where the rate is >3% more common on nicardipine hydrochloride injection than placebo. Table 2: Adverse Reactions Adverse Event Nicardipine Hydrochloride Injection (n=144) Placebo (n=100) Body as a Whole Headache, n (%) 21 (15) 2 (2) Cardiovascular Hypotension, n (%) 8 (6) 1 (1) Tachycardia, n (%) 5 (4) 0 Digestive Nausea/vomiting, n (%) 7 (5) 1 (1) Other adverse events have been reported in clinical trials or in the literature in association with the use of intravenously administered nicardipine: Body as a Whole: fever, neck pain Cardiovascular: angina pectoris, atrioventricular block, ST segment depression, inverted T wave, deep-vein thrombophlebitis Digestive: dyspepsia Hemic and Lymphatic: thrombocytopenia Metabolic and Nutritional: hypophosphatemia, peripheral edema Nervous: confusion, hypertonia Respiratory: respiratory disorder Special Senses: conjunctivitis, ear disorder, tinnitus Urogenital: urinary frequency Sinus node dysfunction and myocardial infarction, which may be due to disease progression, have been seen in patients on chronic therapy with orally administered nicardipine.
6.2Postmarketing Because adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate reliably their frequency or to establish a causal relationship to drug exposure. The following adverse reaction has been identified during post-approval use of nicardipine hydrochloride injection: decreased oxygen saturation (possible pulmonary shunting).
6.2Postmarketing Because adverse reactions are reported voluntarily from a population of uncertain size, it is not always possible to estimate reliably their frequency or to establish a causal relationship to drug exposure. The following adverse reaction has been identified during post-approval use of nicardipine hydrochloride injection: decreased oxygen saturation (possible pulmonary shunting).
🔄 Drug Interactions ▾
7. DRUG INTERACTIONS Cimetidine increases oral nicardipine plasma levels. ( 7.2 ) Oral or intravenous nicardipine may increase cyclosporine and tacrolimus plasma levels. Frequent monitoring of trough blood levels of cyclosporine and tacrolimus is recommended when co-administering nicardipine hydrochloride injection. ( 7.3 , 7.4 )
7.1Beta-Blockers In most patients, nicardipine hydrochloride injection can safely be used concomitantly with beta-blockers. However, titrate slowly when using nicardipine hydrochloride injection in combination with a beta-blocker in heart failure patients [see Warnings and Precautions ( 5.2 )].
7.2Cimetidine Cimetidine has been shown to increase nicardipine plasma concentrations with oral nicardipine administration. Frequently monitor response in patients receiving both drugs. Data with other histamine-2 antagonists are not available.
7.3Cyclosporine Concomitant administration of oral or intravenous nicardipine and cyclosporine results in elevated plasma cyclosporine levels through nicardipine inhibition of hepatic microsomal enzymes, including CYP3A4. Closely monitor plasma concentrations of cyclosporine during nicardipine hydrochloride injection administration, and reduce the dose of cyclosporine accordingly.
7.4Tacrolimus Concomitant administration of intravenous nicardipine and tacrolimus may result in elevated plasma tacrolimus levels through nicardipine inhibition of hepatic microsomal enzymes, including CYP3A4. Closely monitor plasma concentrations of tacrolimus during nicardipine hydrochloride injection administration, and adjust the dose of tacrolimus accordingly.
7.5In Vitro Interaction The plasma protein binding of nicardipine was not altered when therapeutic concentrations of furosemide, propranolol, dipyridamole, warfarin, quinidine, or naproxen were added to human plasma in vitro.
👥 Use in Specific Populations ▾
8. USE IN SPECIFIC POPULATIONS Pregnancy: Based on animal data may cause fetal harm. ( 8.1 ) Nursing mothers: Minimally excreted into human milk. ( 8.3 ) Safety and efficacy in patients under the age of 18 have not been established. ( 8.4 )
8.1Pregnancy Pregnancy Category C There are no adequate and well-controlled studies of nicardipine use in pregnant women. However, limited human data in pregnant women with preeclampsia or pre-term labor are available. In animal studies, no embryotoxicity occurred in rats with oral doses 8 times the maximum recommended human dose (MRHD) based on body surface area (mg/m 2 ), but did occur in rabbits with oral doses at 24 times the maximum recommended human dose (MRHD) based on body surface area (mg/m 2 ).
Nicardipine hydrochloride injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Hypotension, reflex tachycardia, postpartum hemorrhage, tocolysis, headache, nausea, dizziness, and flushing have been reported in pregnant women who were treated with intravenous nicardipine for hypertension during pregnancy. Fetal safety results ranged from transient fetal heart rate decelerations to no adverse events.
Neonatal safety data ranged from hypotension to no adverse events. Adverse events in women treated with intravenous nicardipine during pre-term labor include pulmonary edema, dyspnea, hypoxia, hypotension, tachycardia, headache, and phlebitis at site of injection. Neonatal adverse event includes acidosis (pH<7.25).
In embryofetal toxicity studies, nicardipine was administered intravenously to pregnant rats and rabbits during organogenesis at doses up to 0.14 times the MRHD based on body surface area (mg/m 2 ) (5 mg/kg/day) (rats) and 0.03 times the MRHD based on body surface area (mg/m 2 ) (0.5 mg/kg/day) (rabbits). No embryotoxicity or teratogenicity was seen at these doses. Embryotoxicity, but no teratogenicity was seen at 0.27 times the MRHD based on body surface area (mg/m 2 ) (10 mg/kg/day) in rats and at 0.05 times the MRHD based on body surface area (mg/m 2 ) (1 mg/kg/day) in rabbits.
In other animal studies, pregnant Japanese White rabbits received oral nicardipine during organogenesis, at doses 8 and 24 times the MRHD based on body surface area (mg/m 2 ) (50 and 150 mg/kg/day). Embryotoxicity occurred at the high dose along with signs of maternal toxicity (marked maternal weight gain suppression). New Zealand albino rabbits received oral nicardipine during organogenesis, at doses up to 16 times the MRHD based on body surface area (mg/m 2 ) (100 mg nicardipine/kg/day).
While significant maternal mortality occurred, no adverse effects on the fetus were observed. Pregnant rats received oral nicardipine from day 6 through day 15 of gestation at doses up to 8 times the MRHD based on body surface area (mg/m 2 ) (100 mg/kg/day). There was no evidence of embryotoxicity or teratogenicity; however, dystocia, reduced birth weights, reduced neonatal survival, and reduced neonatal weight gain were noted.
8.3Nursing Mothers Nicardipine is minimally excreted into human milk. Among 18 infants exposed to nicardipine through breast milk in the postpartum period, calculated daily infant dose was less than 0.3 mcg and there were no adverse events observed. Consider the possibility of infant exposure when using nicardipine in nursing mothers.
In a study of 11 women who received oral nicardipine 4 to 14 days postpartum, 4 women received immediate-release nicardipine 40 to 80 mg daily, 6 received sustained-release nicardipine 100 to 150 mg daily, and one received intravenous nicardipine 120 mg daily. The peak milk concentration was 7.3 mcg/L (range 1.9 to 18.8), and the mean milk concentration was 4.4 mcg/L (range 1.3 to 13.8). Infants received an average of 0.073% of the weight-adjusted maternal oral dose and 0.14% of the weight-adjusted maternal intravenous dose.
In another study of seven women who received intravenous nicardipine for an average…
🤰 Pregnancy ▾
8.1Pregnancy Pregnancy Category C There are no adequate and well-controlled studies of nicardipine use in pregnant women. However, limited human data in pregnant women with preeclampsia or pre-term labor are available. In animal studies, no embryotoxicity occurred in rats with oral doses 8 times the maximum recommended human dose (MRHD) based on body surface area (mg/m 2 ), but did occur in rabbits with oral doses at 24 times the maximum recommended human dose (MRHD) based on body surface area (mg/m 2 ).
Nicardipine hydrochloride injection should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Hypotension, reflex tachycardia, postpartum hemorrhage, tocolysis, headache, nausea, dizziness, and flushing have been reported in pregnant women who were treated with intravenous nicardipine for hypertension during pregnancy. Fetal safety results ranged from transient fetal heart rate decelerations to no adverse events.
Neonatal safety data ranged from hypotension to no adverse events. Adverse events in women treated with intravenous nicardipine during pre-term labor include pulmonary edema, dyspnea, hypoxia, hypotension, tachycardia, headache, and phlebitis at site of injection. Neonatal adverse event includes acidosis (pH<7.25).
In embryofetal toxicity studies, nicardipine was administered intravenously to pregnant rats and rabbits during organogenesis at doses up to 0.14 times the MRHD based on body surface area (mg/m 2 ) (5 mg/kg/day) (rats) and 0.03 times the MRHD based on body surface area (mg/m 2 ) (0.5 mg/kg/day) (rabbits). No embryotoxicity or teratogenicity was seen at these doses. Embryotoxicity, but no teratogenicity was seen at 0.27 times the MRHD based on body surface area (mg/m 2 ) (10 mg/kg/day) in rats and at 0.05 times the MRHD based on body surface area (mg/m 2 ) (1 mg/kg/day) in rabbits.
In other animal studies, pregnant Japanese White rabbits received oral nicardipine during organogenesis, at doses 8 and 24 times the MRHD based on body surface area (mg/m 2 ) (50 and 150 mg/kg/day). Embryotoxicity occurred at the high dose along with signs of maternal toxicity (marked maternal weight gain suppression). New Zealand albino rabbits received oral nicardipine during organogenesis, at doses up to 16 times the MRHD based on body surface area (mg/m 2 ) (100 mg nicardipine/kg/day).
While significant maternal mortality occurred, no adverse effects on the fetus were observed. Pregnant rats received oral nicardipine from day 6 through day 15 of gestation at doses up to 8 times the MRHD based on body surface area (mg/m 2 ) (100 mg/kg/day). There was no evidence of embryotoxicity or teratogenicity; however, dystocia, reduced birth weights, reduced neonatal survival, and reduced neonatal weight gain were noted.
🧒 Pediatric Use ▾
8.4Pediatric Use Safety and efficacy in patients under the age of 18 have not been established.
🧓 Geriatric Use ▾
8.5Geriatric Use The steady-state pharmacokinetics of nicardipine are similar in elderly hypertensive patients (> 65 years) and young healthy adults. Clinical studies of nicardipine did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects. Other reported clinical experience has not identified differences in responses between the elderly and younger patients.
In general, use low initial doses in elderly patients, reflecting the greater frequency of decreased hepatic, renal or cardiac function, and of concomitant disease or other drug therapy.
🆘 Overdosage ▾
10. OVERDOSAGE Several overdosages with orally administered nicardipine have been reported. One adult patient allegedly ingested 600 mg of immediate-release oral nicardipine, and another patient ingested 2160 mg of the sustained-release formulation of nicardipine.
Symptoms included marked hypotension, bradycardia, palpitations, flushing, drowsiness, confusion and slurred speech. All symptoms resolved without sequelae. An overdosage occurred in a one-year-old child who ingested half of the powder in a 30 mg nicardipine standard capsule.
The child remained asymptomatic. Based on results obtained in laboratory animals, lethal overdose 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 overdosage, implement standard measures including monitoring of cardiac and respiratory functions. Position the patient so as to avoid cerebral anoxia. Use vasopressors for patients exhibiting profound hypotension.
🧬 Clinical Pharmacology ▾
12. CLINICAL PHARMACOLOGY
12.1Mechanism of Action Nicardipine 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. The effects of nicardipine are more selective to vascular smooth muscle than cardiac muscle.
In animal models, nicardipine produced relaxation of coronary vascular smooth muscle at drug levels which cause little or no negative inotropic effect.
12.2Pharmacodynamics Hemodynamics Nicardipine hydrochloride injection produces significant decreases in systemic vascular resistance. In a study of intra-arterially administered nicardipine hydrochloride injection, the degree of vasodilation and the resultant decrease in blood pressure were more prominent in hypertensive patients than in normotensive volunteers. Administration of nicardipine hydrochloride injection to normotensive volunteers at dosages of 0.25 to 3 mg/hr for eight hours produced changes of < 5 mmHg in systolic blood pressure and < 3 mmHg in diastolic blood pressure.
An increase in heart rate is a normal response to vasodilation and decrease in blood pressure; in some patients these increases in heart rate may be pronounced. In placebo-controlled trials, the mean increases in heart rate were 7 ± 1 bpm in postoperative patients and 8 ± 1 bpm in patients with severe hypertension at the end of the maintenance period. Hemodynamic studies following intravenous dosing in patients with coronary artery disease and normal or moderately abnormal left ventricular function have shown significant increases in ejection fraction and cardiac output with no significant change, or a small decrease, in left ventricular end-diastolic pressure (LVEDP).
There is evidence that nicardipine increases blood flow. Coronary dilatation induced by nicardipine hydrochloride injection improves perfusion and aerobic metabolism in areas with chronic ischemia, resulting in reduced lactate production and augmented oxygen consumption. In patients with coronary artery disease, nicardipine hydrochloride injection, administered after beta-blockade, significantly improved systolic and diastolic left ventricular function.
In congestive heart failure patients with impaired left ventricular function, nicardipine hydrochloride injection increased cardiac output both at rest and during exercise. Decreases in left ventricular end-diastolic pressure were also observed. However, in some patients with severe left ventricular dysfunction, it may have a negative inotropic effect and could lead to worsened failure. “Coronary steal” has not been observed during treatment with nicardipine hydrochloride injection.
(Coronary steal is the detrimental redistribution of coronary blood flow in patients with coronary artery disease from underperfused areas toward better perfused areas.) Nicardipine hydrochloride injection has been shown to improve systolic shortening in both normal and hypokinetic segments of myocardial muscle. Radionuclide angiography has confirmed that wall motion remained improved during increased oxygen demand. (Occasional patients have developed increased angina upon receiving oral nicardipine.
Whether this represents coronary steal in these patients, or is the result of increased heart rate and decreased diastolic pressure, is not clear.) In patients with coronary artery disease, nicardipine hydrochloride injection improves left ventricular diastolic distensibility during the early filling phase, probably due to a faster rate of myocardial relaxation in previously underperfused areas. There is little or no effect on normal myocardium, suggesting the improvement is mainly by indirect mechanisms such as afterload reduction and reduced ischemia.
Nicardipine hydrochloride injection has no negative effect on myocardial relaxation at therapeu…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Nicardipine 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. The effects of nicardipine are more selective to vascular smooth muscle than cardiac muscle.
In animal models, nicardipine produced relaxation of coronary vascular smooth muscle at drug levels which cause little or no negative inotropic effect.
📦 How Supplied / Storage and Handling ▾
16. HOW SUPPLIED/STORAGE AND HANDLING
16.1How Supplied niCARdipine Hydrochloride Injection, USP is available in packages of 10 vials of 10 mL as follows: 25 mg/10 mL (2.5 mg/mL), NDC 72572-470-10
16.2Storage and Handling Store at controlled room temperature 20° to 25°C (68° to 77°F), refer to USP Controlled Room Temperature. Freezing does not adversely affect the product, but avoid exposure to elevated temperatures. Protect from light. Store vials in carton until used. Mfd for: Civica, Inc. Lehi, Utah 84043 Mfd by: American Regent, Inc. New Albany, OH 43054 RQ1092-A Civica logo
📦 Storage and Handling ▾
16.2Storage and Handling Store at controlled room temperature 20° to 25°C (68° to 77°F), refer to USP Controlled Room Temperature. Freezing does not adversely affect the product, but avoid exposure to elevated temperatures. Protect from light. Store vials in carton until used. Mfd for: Civica, Inc. Lehi, Utah 84043 Mfd by: American Regent, Inc. New Albany, OH 43054 RQ1092-A Civica logo
📋 Description ▾
11. DESCRIPTION Nicardipine hydrochloride is a calcium ion influx inhibitor (slow channel blocker or calcium channel blocker). niCARdipine Hydrochloride Injection, USP for intravenous administration contains 2.5 mg of nicardipine hydrochloride. Nicardipine hydrochloride is a dihydropyridine derivative with IUPAC (International Union of Pure and Applied Chemistry) chemical name (±)-2-(benzyl-methyl amino) ethyl methyl 1,4-dihydro-2,6-dimethyl-4-( m -nitrophenyl)-3,5-pyridinedicarboxylate monohydrochloride and has the following structure: Nicardipine hydrochloride is a greenish-yellow, odorless, crystalline powder that melts at about 169°C.
It is freely soluble in chloroform, methanol, and glacial acetic acid, sparingly soluble in anhydrous ethanol, slightly soluble in n-butanol, water,
0.01M potassium dihydrogen phosphate, acetone, and dioxane, very slightly soluble in ethyl acetate, and practically insoluble in benzene, ether, and hexane. It has a molecular weight of 515.99. Nicardipine hydrochloride injection is available as a sterile, non-pyrogenic, clear, yellow solution in 10 mL vials for intravenous infusion after dilution.
Each mL contains nicardipine hydrochloride 2.5 mg in water for injection with sorbitol 48 mg, and edetate disodium 0.04 mg, buffered to pH 3.5 with citric acid monohydrate 0.525 mg and sodium hydroxide 0.09 mg. Additional citric acid and/or sodium hydroxide may have been added to adjust pH. Cardene Structure