CARDIPEN LP

A potent calcium channel blockader with marked vasodilator action.

It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects.

It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.

Used for the management of patients with chronic stable angina and for the treatment of hypertension.

Nicardipine, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina.

Nicardipine is similar to other peripheral vasodilators.

Nicardipine inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum.

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.

L-type calcium channel subunit alpha-1C Inhibitor Voltage-dependent L-type calcium channel subunit beta-2 Inhibitor Voltage-dependent calcium channel subunit alpha-2/delta-1 Inhibitor + 1 more target.

While nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.

HCl is metabolized extensively by the liver.

Hover over products below to view reaction partners Nicardipine De-benzylated nicardipine Dehydronicardipine.

Nicardipine has been shown to be rapidly and extensively metabolized by the liver.

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LD 50 Rat = 184 mg/kg, Oral LD 50 Mouse = 322 mg/kg.

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.

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 to 10 days.

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.

Reduction of diastolic pressure in these patients may worsen rather than improve myocardial oxygen balance.

The dose should be individually titrated for each patient beginning with 20 mg three times daily.

Doses in the range of 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.

Therapy: nicardipine hydrochloride capsules may be safely coadministered with short.

• and long-acting nitrates.

Nicardipine hydrochloride capsules may be safely coadministered with beta-blockers.

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 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 to 2 hours after dosing, particularly during initiation of therapy.

At least 3 days should be allowed before increasing the nicardipine hydrochloride capsules dose to ensure achievement of steady-state plasma drug concentrations.

Agents 1.

Diuretics: nicardipine hydrochloride capsules may be safety coadministered with thiazide diuretics. 2.

Beta-blockers: nicardipine hydrochloride capsules may be safely coadministered with beta-blocker.

Although there is no evidence that nicardipine hydrochloride capsules impair renal function, careful dose titration beginning with 20 mg tid is advised.

Nicardipine hydrochloride capsules should be administered cautiously in patients with severely impaired hepatic function.

A suggested starting dose of 20 mg twice a day is advised with individual titration based on clinical findings maintaining the twice a day schedule.

Caution is advised when titrating nicardipine hydrochloride capsules dosage in patients with congestive heart failure See WARNINGS.

Nicardipine hydrochloride 20 mg capsules are available in light blue opaque/white opaque hard gelatin capsules imprinted “E501” in black ink on cap and body, filled with yellow powder.

These are supplied

NDC: 24658-750-90 Bottles of 90 Capsules Nicardipine hydrochloride 30 mg capsules are available in light blue opaque hard gelatin capsules imprinted “E502” with black ink on cap and body, filled with yellow powder.

NDC 24658-751-90 Bottles of 90 Capsules Store at 20° to 25°C (68° to 77°F) .

Dispense contents in a tight, light-resistant container with a child-resistant closure.

The brands listed are trademarks of their respective owners.

Laboratories, LLC DBA Blu Pharmaceuticals Franklin, KY 42134 USA 1-877-264-0258 Manufactured in USA Rev. 08-2017-00 MF501BLUREV08/17 OE2603.

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.

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.

Safety and efficacy in patients under the age of 18 have not been established.

Pharmacokinetic parameters did not differ between elderly hypertensive patients (≥65 years) and healthy controls after 1 week of nicardipine hydrochloride capsules treatment at 20 mg tid.

Plasma nicardipine hydrochloride capsules concentrations in elderly hypertensive subjects were similar to plasma concentrations in healthy young adult subjects when nicardipine hydrochloride capsules were administered at doses of 10, 20, and 30 mg tid, suggesting that the pharmacokinetics of nicardipine hydrochloride capsules are similar in young and elderly hypertensive patients.

Clinical studies of nicardipine did not include sufficient numbers of subjects aged 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, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

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.

Safety and efficacy in patients under the age of 18 have not been established.

Pharmacokinetic parameters did not differ between elderly hypertensive patients (≥65 years) and healthy controls after 1 week of nicardipine hydrochloride capsules treatment at 20 mg tid.

Plasma nicardipine hydrochloride capsules concentrations in elderly hypertensive subjects were similar to plasma concentrations in healthy young adult subjects when nicardipine hydrochloride capsules were administered at doses of 10, 20, and 30 mg tid, suggesting that the pharmacokinetics of nicardipine hydrochloride capsules are similar in young and elderly hypertensive patients.

Clinical studies of nicardipine did not include sufficient numbers of subjects aged 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, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.