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nicardipine hydrochloride
Overview
What is Cardene?
CARDENE SR is a sustained release formulation of CARDENE .
CARDENE SR capsules for oral administration each contain 30 mg, 45
mg or 60 mg of nicardipine hydrochloride. Nicardipine hydrochloride
is a calcium ion influx inhibitor (slow channel blocker or calcium entry
blocker).
Nicardipine hydrochloride is a dihydropyridine derivative 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.
CARDENE SR is available in hard gelatin capsules containing 30
mg, 45 mg or 60 mg nicardipine hydrochloride. All strengths contain
a two component capsule fill. A powder component containing 25%
of total nicardipine hydrochloride dose contains pregelatinized starch
and magnesium stearate as inactive ingredients. A spherical granule
component containing 75% of total nicardipine hydrochloride dose also
contains microcrystalline cellulose, starch, lactose and methacrylic acid
copolymer Type C as inactive ingredients.
The colorants used in the 30-mg capsules are titanium dioxide, FD&C
Red No. 40 and red iron oxide, and the colorants used in the 45-mg and
60-mg capsule are titanium dioxide and FD&C Blue No. 2.
What does Cardene look like?
What are the available doses of Cardene?
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What should I talk to my health care provider before I take Cardene?
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How should I use Cardene?
CARDENE SR is indicated for the treatment of hypertension. CARDENE
SR may be used alone or in combination with other anti-hypertensive
drugs.
The dose of CARDENE SR should be individually adjusted according to
the blood pressure response beginning with 30 mg two times daily. The
effective doses in clinical trials have ranged from 30 mg to 60 mg two
times daily. The maximum blood pressure lowering effect at steady-state
is sustained from 2 hours until 6 hours after dosing.
When initiating therapy or upon increasing dose, blood pressure should
be measured 2 to 4 hours after the first dose or dose increase, as well as
at the end of a dosing interval.
The total daily dose of immediate release nicardipine (CARDENE) may
not be a useful guide to judging the effective dose of CARDENE SR.
Patients currently receiving immediate release nicardipine may be titrated
with CARDENE SR starting at their current total daily dose of immediate
release nicardipine and then reexamined to assess the adequacy of blood
pressure control.
Concomitant Use With Other Antihypertensive Agents:
What interacts with Cardene?
CARDENE is contraindicated in patients with hypersensitivity to the drug.
Because part of the effect of CARDENE is secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis. Reduction of diastolic pressure by any means in these patients may worsen rather than improve myocardial oxygen balance.
What are the warnings of Cardene?
Increased Angina in Patients With Angina
In short-term, placebo-controlled angina trials with CARDENE (an
immediate release oral dosage form of nicardipine), about 7% of patients
on CARDENE (compared with 4% of patients on placebo) have developed
increased frequency, duration or severity of angina. Comparisons with
beta-blockers also show a greater frequency of increased angina, 4% vs
1%. The mechanism of this effect has not been established.
Use in Patients With Congestive Heart Failure
Although preliminary hemodynamic studies in patients with congestive
heart failure have shown that CARDENE 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
CARDENE is 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.
What are the precautions of Cardene?
General
Because CARDENE decreases peripheral resistance,
careful monitoring of blood pressure during the initial administration
and titration of CARDENE is suggested. CARDENE, like other calcium
channel blockers, may occasionally produce symptomatic hypotension.
Caution is advised to avoid systemic hypotension when administering
the drug to patients who have sustained an acute cerebral infarction or
hemorrhage.
Since the liver is the
major site of biotransformation and since CARDENE is subject to first-pass
metabolism, CARDENE should be used with caution in patients
having impaired liver function or reduced hepatic blood flow. Patients
with severe liver disease developed elevated blood levels (fourfold
increase in AUC) and prolonged half-life (19 hours) of CARDENE.
When 45-mg CARDENE
SR bid was given to hypertensive patients with moderate renal
impairment, mean AUC and C values were approximately 2-fold to
3-fold higher than in patients with mild renal impairment. Doses in these
patients must be adjusted. Mean AUC and C values were similar in
patients with mildly impaired renal function and normal volunteers (see and ).
Drug Interactions
In controlled clinical studies, adrenergic beta-receptor
blockers have been frequently administered concomitantly with
CARDENE. The combination is well tolerated.
Cimetidine increases CARDENE plasma levels. Patients
receiving the two drugs concomitantly should be carefully monitored.
Some calcium blockers may increase the concentration of
digitalis preparations in the blood. CARDENE usually does not alter
the plasma levels of digoxin; however, serum digoxin levels should be
evaluated after concomitant therapy with CARDENE is initiated.
Severe hypotension has been reported during
fentanyl anesthesia with concomitant use of a beta-blocker and a calcium
channel blocker. Even though such interactions were not seen during
clinical studies with CARDENE, an increased volume of circulating fluids
might be required if such an interaction were to occur.
Concomitant administration of nicardipine and cyclosporine
results in elevated plasma cyclosporine levels. Plasma concentrations
of cyclosporine should therefore be closely monitored, and its dosage
reduced accordingly, in patients treated with nicardipine.
When therapeutic concentrations of furosemide, propranolol, dipyridamole,
warfarin, quinidine or naproxen were added to human plasma (in vitro),
the plasma protein binding of CARDENE was not altered.
Array
Carcinogenesis, Mutagenesis, Impairment of Fertility
Rats treated with nicardipine in the diet (at concentrations calculated to
provide daily dosage levels of 5, 15 or 45 mg/kg/day) for 2 years showed a
dose-dependent increase in thyroid hyperplasia and neoplasia (follicular
adenoma/carcinoma). One- and 3-month studies in the rat have suggested
that these results are linked to a nicardipine-induced reduction in plasma
thyroxine (T4) levels with a consequent increase in plasma levels of
thyroid stimulating hormone (TSH). Chronic elevation of TSH is known
to cause hyperstimulation of the thyroid. In rats on an iodine deficient
diet, nicardipine administration for 1 month was associated with thyroid
hyperplasia that was prevented by T4 supplementation. Mice treated
with nicardipine in the diet (at concentrations calculated to provide daily
dosage levels of up to 100 mg/kg/day) for up to 18 months showed no
evidence of neoplasia of any tissue and no evidence of thyroid changes.
There was no evidence of thyroid pathology in dogs treated with up to 25
mg nicardipine/kg/day for 1 year and no evidence of effects of nicardipine
on thyroid function (plasma T4 and TSH) in man.
There was no evidence of a mutagenic potential of nicardipine in a
battery of genotoxicity tests conducted on microbial indicator organisms,
in micronucleus tests in mice and hamsters, or in a sister chromatid
exchange study in hamsters.
No impairment of fertility was seen in male or female rats administered
nicardipine at oral doses as high as 100 mg/kg/day (50 times the
maximum recommended daily dose in man, assuming a patient weight
of 60 kg).
Array
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 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. CARDENE SR should be used during pregnancy only
if the potential benefit justifies the potential risk to the fetus.
Array
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 effectiveness in pediatric patients have not been
established.
Geriatric use
Pharmacokinetic parameters did not differ significantly between elderly
hypertensive subjects (mean age: 70 years) and younger hypertensive
subjects (mean age: 44 years) after 1 week of treatment with CARDENE
SR (see ).
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, 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.
What are the side effects of Cardene?
In multiple-dose US and foreign controlled studies, 667 patients received
CARDENE SR. In these studies adverse events were elicited by non-directed
and in some cases directed questioning; adverse events were
generally not serious and about 9% of patients withdrew prematurely
from the studies because of them.
Array
Hypertension
The incidence rates of adverse events in hypertensive patients were
derived from placebo-controlled clinical trials. Following are the rates
of adverse events for CARDENE SR (n=322) and placebo (n=140),
respectively, that occurred in 0.6% of patients or more on CARDENE
SR. These represent events considered probably drug related by the
investigator. Where the frequency of adverse events for CARDENE SR
and placebo is similar, causal relationship is uncertain. The only dose-related
effect was pedal edema.
Percentage of Patients With Probably Drug Related Adverse Events in Placebo-Controlled Studies
Incidence (%) of Discontinuations Due to Any Adverse Event in Placebo-Controlled Studies
Uncontrolled experience in over 300 patients with hypertension treated
for up to 27.5 months with CARDENE SR has shown no unexpected
adverse events or increase in incidence of adverse events compared to
the controlled clinical trials.
| Headache | 6.2 | 7.1 |
| Pedal Edema | 5.9 | 1.4 |
| Vasodilatation | 4.7 | 1.4 |
| Palpitation | 2.8 | 1.4 |
| Nausea | 1.9 | 0.7 |
| Dizziness | 1.6 | 0.7 |
| Asthenia | 0.9 | 0.7 |
| Postural Hypotension | 0.9 | 0 |
| Increased UrinaryFrequency | 0.6 | 0 |
| Pain | 0.6 | 0 |
| Rash | 0.6 | 0 |
| Sweating Increased | 0.6 | 0 |
| Vomiting | 0.6 | 0 |
| Headache | 2.5 | 1.4 |
| Palpitation | 2.2 | 0.7 |
| Dizziness | 1.9 | 0.7 |
| Asthenia | 1.9 | 0 |
| Pedal Edema | 1.2 | 0 |
| Nausea | 1.2 | 0 |
| Rash | 0.9 | 0.7 |
| Diarrhea | 0.9 | 0 |
| Tachycardia | 0.9 | 0 |
| Blurred Vision | 0.6 | 0 |
| Chest Pain | 0.6 | 0 |
| Face Edema | 0.6 | 0 |
| Myocardial Infarct | 0.6 | 0 |
| Vasodilatation | 0.6 | 0 |
| Vomiting | 0.6 | 0 |
Array
Rare Events
The following rare adverse events have been reported in clinical trials or the literature:
infection, allergic reaction
hypotension, atypical chest pain, peripheral vascular disorder, ventricular extrasystoles, ventricular tachycardia, angina pectoris
sore throat, abnormal liver chemistries
arthralgia
hot flashes, vertigo, hyperkinesia, impotence, depression, confusion, anxiety
rhinitis, sinusitis
tinnitus, abnormal vision, blurred vision
Array
Angina
Data are available from only 91 patients with chronic stable angina pectoris who received CARDENE SR 30 to 60 mg administered twice daily in open-label clinical trials. Fifty-eight of these patients were treated for at least 30 days. The four most frequently reported adverse events thought by the investigators to be probably related to the use of CARDENE SR were vasodilatation (5.5%), pedal edema (4.4%), asthenia (4.4%), and dizziness (3.3%).
What should I look out for while using Cardene?
CARDENE is contraindicated in patients with hypersensitivity to the
drug.
Because part of the effect of CARDENE is secondary to reduced
afterload, the drug is also contraindicated in patients with advanced
aortic stenosis. Reduction of diastolic pressure by any means in these
patients may worsen rather than improve myocardial oxygen balance.
What might happen if I take too much Cardene?
Three overdosages with CARDENE or CARDENE SR have been
reported. Two occurred in adults, 1 of whom ingested 600 mg of
CARDENE and the other 2160 mg of CARDENE SR. Symptoms included
marked hypotension, bradycardia, palpitations, flushing, drowsiness,
confusion, and slurred speech. All symptoms resolved without sequelae.
The third over-dosage occurred in a 1-year-old child who ingested half
of the powder in a 30-mg CARDENE capsule. The child remained
asymptomatic.
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.
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. Intravenous calcium gluconate may help reverse
the effects of calcium entry blockade.
How should I store and handle Cardene?
ISTODAX (romidepsin) for injection is supplied as a kit containing 2 vials in a single carton. The carton must be stored at 20° to 25°C, excursions permitted between 15° to 30°C. (See USP Controlled Room Temperature.)Procedures for proper handling and disposal of anticancer drugs should be considered. A guideline on this subject has been published ISTODAX (romidepsin) for injection is supplied as a kit containing 2 vials in a single carton. The carton must be stored at 20° to 25°C, excursions permitted between 15° to 30°C. (See USP Controlled Room Temperature.)Procedures for proper handling and disposal of anticancer drugs should be considered. A guideline on this subject has been published NDC:68151-0089-0 in a PACKAGE of 1 CAPSULE, EXTENDED RELEASES
Clinical Information
Chemical Structure
No Image foundClinical Pharmacology
Nicardipine is 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.
The effects of nicardipine are more selective to vascular smooth muscle
than cardiac muscle. In animal models, nicardipine produces relaxation
of coronary vascular smooth muscle at drug levels that cause little or no
negative inotropic effect.
Non-Clinical Toxicology
CARDENE is contraindicated in patients with hypersensitivity to the drug.Because part of the effect of CARDENE is secondary to reduced afterload, the drug is also contraindicated in patients with advanced aortic stenosis. Reduction of diastolic pressure by any means in these patients may worsen rather than improve myocardial oxygen balance.
In controlled clinical studies, adrenergic beta-receptor blockers have been frequently administered concomitantly with CARDENE. The combination is well tolerated.
Cimetidine increases CARDENE plasma levels. Patients receiving the two drugs concomitantly should be carefully monitored.
Some calcium blockers may increase the concentration of digitalis preparations in the blood. CARDENE usually does not alter the plasma levels of digoxin; however, serum digoxin levels should be evaluated after concomitant therapy with CARDENE is initiated.
Severe hypotension has been reported during fentanyl anesthesia with concomitant use of a beta-blocker and a calcium channel blocker. Even though such interactions were not seen during clinical studies with CARDENE, an increased volume of circulating fluids might be required if such an interaction were to occur.
Concomitant administration of nicardipine and cyclosporine results in elevated plasma cyclosporine levels. Plasma concentrations of cyclosporine should therefore be closely monitored, and its dosage reduced accordingly, in patients treated with nicardipine.
When therapeutic concentrations of furosemide, propranolol, dipyridamole, warfarin, quinidine or naproxen were added to human plasma (in vitro), the plasma protein binding of CARDENE was not altered.
Because CARDENE decreases peripheral resistance, careful monitoring of blood pressure during the initial administration and titration of CARDENE is suggested. CARDENE, like other calcium channel blockers, may occasionally produce symptomatic hypotension. Caution is advised to avoid systemic hypotension when administering the drug to patients who have sustained an acute cerebral infarction or hemorrhage.
Since the liver is the major site of biotransformation and since CARDENE is subject to first-pass metabolism, CARDENE should be used with caution in patients having impaired liver function or reduced hepatic blood flow. Patients with severe liver disease developed elevated blood levels (fourfold increase in AUC) and prolonged half-life (19 hours) of CARDENE.
When 45-mg CARDENE SR bid was given to hypertensive patients with moderate renal impairment, mean AUC and C values were approximately 2-fold to 3-fold higher than in patients with mild renal impairment. Doses in these patients must be adjusted. Mean AUC and C values were similar in patients with mildly impaired renal function and normal volunteers (see and ).
In multiple-dose US and foreign controlled studies, 667 patients received CARDENE SR. In these studies adverse events were elicited by non-directed and in some cases directed questioning; adverse events were generally not serious and about 9% of patients withdrew prematurely from the studies because of them.
Reference
This information is obtained from the National Institute of Health's Standard Packaging Label drug database.
"https://dailymed.nlm.nih.gov/dailymed/"
While we update our database periodically, we cannot guarantee it is always updated to the latest version.
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