Nicardipine

Tell your doctor if you are pregnant or plan to become pregnant.

The FDA categorizes medications based on safety for use during pregnancy. Five categories - A, B, C, D, and X, are used to classify the possible risks to an unborn baby when a medication is taken during pregnancy.

Nicardipine falls into category C. There are no well-controlled studies in pregnant women. Nicardipine should be used during pregnancy only if the possible benefit outweighs the possible risk to the unborn baby.

Nicardipine is a calcium channel blocker. Nicardipine relaxes (widens) your blood vessels, which makes it easier for the heart to pump and reduces its workload.

Nicardipine is used to treat hypertension (high blood pressure) and angina (chest pain).

Nicardipine may also be used for purposes not listed in this medication guide.

Take the missed dose as soon as you remember. Skip the missed dose if it is almost time for your next scheduled dose. Do not take extra medicine to make up the missed dose.

This medicine may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert. Avoid getting up too fast from a sitting or lying position, or you may feel dizzy. Get up slowly and steady yourself to prevent a fall.

Drinking alcohol can increase certain side effects of nicardipine.

Other drugs may interact with nicardipine, including prescription and over-the-counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.

Hypertension

Oral management of hypertension (alone or in combination with other classes of antihypertensive agents).1 2 3 500

Therapy with extended-release capsules generally is preferred because of less frequent dosing, potentially smoother BP control,500 and concerns raised by experience with short-acting (conventional, immediate-release) nifedipine.35 36 37 38 39 40 41 42 43 44 45 46 47 48 49 50 51 52 53 54 55 56 57 58 59 61 72 73

Calcium-channel blockers are recommended as one of several preferred agents for the initial management of hypertension; other options include ACE inhibitors, angiotensin II receptor antagonists, and thiazide diuretics.501 502 503 504 While there may be individual differences with respect to specific outcomes, these antihypertensive drug classes all produce comparable effects on overall mortality and cardiovascular, cerebrovascular, and renal outcomes.501 502 503 504 Individualize choice of therapy; consider patient characteristics (e.g., age, ethnicity/race, comorbidities, cardiovascular risk) as well as drug-related factors (e.g., ease of administration, availability, adverse effects, cost).500 501 502 503 504 515

Calcium-channel blockers may be preferred in hypertensive patients with certain coexisting conditions (e.g., ischemic heart disease)523 and in geriatric patients, including those with isolated systolic hypertension.502 510

Black hypertensive patients generally respond better to monotherapy with calcium-channel blockers or thiazide diuretics than to other antihypertensive drug classes (e.g., ACE inhibitors, angiotensin II receptor antagonists).500 501 504 However, diminished response to these other drug classes is largely eliminated when administered concomitantly with a calcium-channel blocker or thiazide diuretic.500 504

The optimum BP threshold for initiating antihypertensive drug therapy is controversial.501 504 505 506 507 508 515 523 530 Further study needed to determine optimum BP thresholds/goals; individualize treatment decisions.501 503 507 515 526 530

JNC 7 recommends initiation of drug therapy in all patients with uncomplicated hypertension and BP ≥140/90 mm Hg;500 JNC 8 panel recommends SBP threshold of 150 mm Hg for patients ≥60 years of age.501 Although many experts agree that SBP goal of <150 mm Hg may be appropriate for patients ≥80 years of age,502 504 505 530 application of this goal to those ≥60 years of age is controversial, especially for those at higher cardiovascular risk.501 502 505 506 508 511 515

In the past, initial antihypertensive drug therapy was recommended for patients with diabetes mellitus or chronic kidney disease who had BP ≥130/80 mm Hg;500 503 current hypertension management guidelines generally recommend a BP threshold of 140/90 mm Hg for these individuals (same as for the general population of patients without these conditions), although a goal of <130/80 mm Hg may still be considered.501 502 503 504 520 530 535 536 541

IV, short-term management of hypertension when oral therapy is not feasible or desirable.18

IV management of hypertensive crises (e.g., emergencies) in adults.18 500

IV, rapid reduction of BP in the management of severe hypertension in pediatric patients 1–17 years of age†.99

Angina

Management of chronic stable angina pectoris (alone or in combination with other antianginal agents).1 3 25

Storage

Oral

Light resistant containers at 15–30°C.a b

Parenteral

20–25°C; protect from light.c Avoid exposure to increased temperatures.c

20–25°C; protect from light, freezing, and excessive heat.600 601

Compatibility

For information on systemic interactions resulting from concomitant use, see Interactions.

Parenteral

• Importance of informing clinicians of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.1 2 18

• Importance of women informing clinicians if they are or plan to become pregnant or plan to breast-feed.1 2 18

• Importance of informing patients of other important precautionary information.1 2 18 (See Cautions.)

In the U.S.

• Cardene
• Cardene SR

Available Dosage Forms:

• Capsule, Extended Release
• Capsule

Therapeutic Class: Cardiovascular Agent

Pharmacologic Class: Calcium Channel Blocker

Chemical Class: Dihydropyridine

Nicardipine hydrochloride capsules for oral administration each contain 20 mg or 30 mg of Nicardipine hydrochloride. Nicardipine hydrochloride capsules are a calcium ion influx inhibitor (slow channel blocker or calcium channel blocker).

Nicardipine hydrochloride is a dihydropyridine structure with the 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 it 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, 0.01 M 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.

Each capsule, for oral administration, contains 20 mg or 30 mg of Nicardipine hydrochloride. In addition, each capsule contains the following inactive ingredients: magnesium stearate, pregelatinized starch, titanium dioxide, gelatin and FD&C Blue #1. The colorants used in the capsules are black iron oxide, FD&C Blue #2, FD&C Red #40, D&C Yellow #10 and FD&C Blue #1. In addition, the 30 mg capsules also contain propylene glycol.

I. Stable Angina

Nicardipine hydrochloride capsules are indicated for the management of patients with chronic stable angina (effort-associated angina). Nicardipine hydrochloride capsules may be used alone or in combination with beta-blockers.

II. Hypertension

Nicardipine hydrochloride capsules are indicated for the treatment of hypertension. Nicardipine hydrochloride capsules may be used alone or in combination with other antihypertensive drugs. In administering Nicardipine hydrochloride it is important to be aware of the relatively large peak to trough differences in blood pressure effect (See DOSAGE AND ADMINISTRATION).

IV: Within minutes (constant infusion); Oral: 0.5 to 2 hours

Peak effect: Immediate capsules: 1 to 2 hours; Sustained release capsules (at steady state): Sustained from 2 to 6 hours postdose; IV continuous infusion: 50% of the maximum effect is seen by 45 minutes

Time to Peak

Serum: Oral: Immediate release: 30 to 120 minutes (mean: 1 hour) ; Sustained release: 60 to 240 minutes

At least 3 days should be allowed before increasing the dose to assure steady state levels.

The IV infusion should be discontinued if hypotension or tachycardia occurs. Following stabilization of blood pressure and heart rate, the infusion should be restarted at low doses (such as 3 to 5 mg/hour) and titrated to maintain desired response.

Use in patients with advanced aortic stenosis is contraindicated because of the afterload reduction effect of nicardipine.

Because nicardipine decreases peripheral resistance, close monitoring of blood pressure and heart rate during administration is required. Nicardipine, like other calcium channel blockers, may occasionally produce symptomatic hypotension or tachycardia. Systemic hypotension should be avoided when administering the drug to patients who have sustained an acute cerebral infarction or hemorrhage.

Nicardipine should be titrated slowly, particularly when used in combination with a beta-blocker, in patients with heart failure or significant left ventricular dysfunction due to possible negative inotropic effects.

No dosage adjustment is recommended based on age. Steady-state pharmacokinetics were similar between elderly (greater than 65 years of age) patients and young health subjects in clinical studies. However, caution is advised in dose selection because of a greater incidence of reduced organ function, concomitant disease, or drug therapy in the elderly.

Safety and effectiveness have not been established in pediatric patients (less than 18 years of age).