Nicardipine (Cardene) belongs to the class of dihydropyridine calcium channel blockers.
Nicardipine Uses:
-
Angina:
- It is used in the treatment of chronic stable angina (oral immediate-release product only).
-
Hypertension:
- It is indicated for treating hypertension (oral immediate/ sustained release or intravenous forms).
- Intravenous administration may be used for the short term when oral treatment cannot be given.
Guideline recommendations:
The 2017 Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults recommends if single-agent therapy is to be given in the absence of comorbidities, thiazide-like diuretics or dihydropyridine calcium channel blockers are preferred due to prevention of heart failure and stroke.
ACE inhibitors and ARBs can also be given as monotherapy. Combination therapy is initially preferred in high-risk patients (such as stage 2 hypertension, atherosclerotic cardiovascular disease risk ≥10%).
-
Off Label Use of Nicardipine (Cardene) in Adults:
- Arterial hypertension in acute ischemic stroke.
- Control of blood pressure in patients with spontaneous intracranial hemorrhage.
- Perioperative hypertension.
- Subarachnoid hemorrhage associated cerebral vasospasm.
Nicardipine (Cardene) dosage in adults:
Note: Cardene SR has been discontinued in the US for more than 1 year.
Nicardipine (Cardene) dose for the treatment of Angina:
-
Immediate-release:
- 20 mg per oral thrice daily.
- usual dosage: 20 to 40 mg 3 times daily (allow ≥3 days between dose increases)
Nicardipine (Cardene) dose for the treatment of Hypertension:
-
Immediate-release:
- Initial oral dose of 20 mg thrice daily.
- The usual dosage: 20 to 40 mg 3 times daily (allow ≥3 days between dose increase)
-
Sustained-release:
- The initial dose of 30 mg b.i.d daily
- The usual dosage: 30 to 60 mg per oral b.i.d daily
Nicardipine (Cardene) dose for the treatment of Acute hypertension:
- An initial intravenous dose of 5 mg/hour that can be increased by 2.5 mg/hour every 5 minutes (for fast titration) to every 15 minutes (for slow titration) up to a maximum of 15 mg/hour.
- Adjust infusion rate according to the desired response
- Consider reduction to 3 mg/hour after response in rapid titration.
- The infusion should be stopped if severe hypotension/tachycardia occurs.
Nicardipine (Cardene) dose for the treatment of Arterial hypertension in acute ischemic stroke (off-label use):
- In patients eligible for reperfusion treatment except BP >185/110 mm Hg start intravenous dose 5 mg/hour, titrate by 2.5 mg/hour at 5- to 15-minute intervals (maximum dose: 15 mg/hour).
- If BP still remains >185/110 mm Hg, alteplase should not be given.
-
Management of BP during and after reperfusion treatment to maintain BP ≤180/105 mm Hg:
- If systolic BP >180 to 230 mm Hg or diastolic >105 to 120 mm Hg start with 5 mg/hour titrate by 2.5 mg/hour at 5- to 15-minute intervals
- (maximum dose: 15 mg/hour).
- If hypertension is refractory or diastolic BP >140 mm Hg, consider other intravenous antihypertensives (eg, nitroprusside).
-
Substitution for oral therapy (approximate equivalents):
- 20 mg every 8 hours oral, equivalent to 0.5 mg/hour intravenous infusion
- 30 mg every 8 hours oral, equivalent to 1.2 mg/hour intravenous infusion
- 40 mg every 8 hours oral, equivalent to 2.2 mg/hour intravenous infusion
-
Conversion to oral antihypertensive agent:
- Oral antihypertensive should be started once that intravenous nicardipine is stopped.
Nicardipine (Cardene) Dose in Childrens
Nicardipine dose in children for the treatment of hypertension:
Note: Use should be reserved for acute severe hypertension.
-
Infants, Children, and Adolescents:
-
Continuous intravenous infusion, Bolus dose:
- Initially 30 mcg/kg to a maximum dose: 2 mg/dose, followed by continuous infusion: 0.5 to 1 mcg/kg/minute titrated according to BP.
-
Pregnancy Risk Factor C
- Certain animal reproduction studies have shown negative results.
- It can also be used to treat severe hypertension during pregnancy or preterm labor.
- Nicardipine can cross the placenta, causing changes to the fetal heart rate or neonatal hypotension.
Nicardipine use during breastfeeding:
- Breast milk contains a small amount of Nicardipine.
- Some manufacturers do not recommend breastfeeding.
Nicardipine dose adjustment in renal disease:
- Initial dose of 20 mg thrice daily (immediate release) or 30 mg b.i.d daily (sustained release) with slow titration.
- There are no specific dosage adjustments fr intravenous preparation provided in the manufacturer’s labeling, titration should be slow with careful monitoring.
Nicardipine dose adjustment in liver disease:
- Initial dose of 20 mg per oral b.i.d daily (immediate-release) with slow titration.
- There are no specific dosage adjustments for intravenous preparation provided in the manufacturer’s labeling, titration should be slow with monitoring.
Side Effects of Nicardipine (Cardene):
-
Cardiovascular:
- Flushing
- Pedal Edema
- Exacerbation Of Angina Pectoris
- Hypotension
- Palpitations
- Tachycardia
- Chest Pain
- Extrasystoles
- Hemopericardium
- Hypertension
- Supraventricular Tachycardia
- Edema
-
Central Nervous System:
- Headache
- Dizziness
- Hypoesthesia
- Intracranial Hemorrhage
- Pain
- Somnolence
-
Dermatologic:
- Diaphoresis
- Skin Rash
-
Endocrine & Metabolic:
- Hypokalemia
-
Gastrointestinal:
- Nausea And Vomiting
- Nausea
- Dyspepsia
- Abdominal Pain
- Xerostomia
-
Genitourinary:
- Hematuria
-
Local:
- Injection Site Reaction
- Pain At Injection Site
-
Neuromuscular & Skeletal:
- Weakness
- Myalgia
- Paresthesia
Contraindication to Nicardipine (Cardene):
- Hypersensitivity to nicardipine and any component of the formulation
- Advanced aortic stasis
Warnings and precautions
-
Angina/Myocardial Infarction:
- Angina and MI are becoming more common.
- Patients with obstructive heart disease may experience reflex tachycardia, particularly if they are not taking combination beta-blockers.
-
Hypotension/syncope
- Hypotension may be accompanied by or without syncope, which is rare. It is important to monitor pulse and BP closely.
-
Peripheral edema
- Within 2 to 3 weeks after starting therapy, peripheral edema can be common.
-
Tachycardia
- It is important to monitor your heart rate closely.
-
Aortic stenosis
- Nicardipine can reduce coronary perfusion, which could lead to ischemia. Patients with advanced aortic narrowing should not use Nicardipine.
-
Heart failure:
- Combination beta-blockers may worsen symptoms in patients with severe left ventricular dysfunction or heart failure.
- Patients with heart failure should be advised not to use calcium channel blockers.
-
Hepatic impairment
- Patients with reduced liver function or reduced blood flow should reduce their doses.
-
Hypertrophic cardiomyopathy with outflow tract obstruction (HCM)
- Nicardipine may cause reduced afterload or worsening symptoms.
-
Renal impairment
- Patients with impaired renal function should be cautious when taking TItrate, as the clearance of Nicardipine is decreased.
Nicardipine: Drug Interaction
|
Risk Factor C (Monitor therapy) |
|
|
Alfuzosin |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Alpha1-Blockers |
May enhance the hypotensive effect of Calcium Channel Blockers. |
|
Amphetamines |
May diminish the antihypertensive effect of Antihypertensive Agents. |
|
Antipsychotic Agents (Second Generation [Atypical]) |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). |
|
Aprepitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
ARIPiprazole |
CYP2D6 Inhibitors (Weak) may increase the serum concentration of ARIPiprazole. Management: Monitor for increased aripiprazole pharmacologic effects. Aripiprazole dose adjustments may or may not be required based on concomitant therapy and/or indication. Consult full interaction monograph for specific recommendations. |
|
Atosiban |
Calcium Channel Blockers may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. |
|
Barbiturates |
May increase the metabolism of Calcium Channel Blockers. Management: Monitor for decreased therapeutic effects of calcium channel blockers with concomitant barbiturate therapy. Calcium channel blocker dose adjustments may be necessary. Nimodipine Canadian labeling contraindicates concomitant use with phenobarbital. |
|
Barbiturates |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Benperidol |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Bosentan |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Brigatinib |
May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. |
|
Brimonidine (Topical) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Calcium Channel Blockers (Nondihydropyridine) |
Calcium Channel Blockers (Dihydropyridine) may enhance the hypotensive effect of Calcium Channel Blockers (Nondihydropyridine). Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). |
|
Calcium Salts |
May diminish the therapeutic effect of Calcium Channel Blockers. |
|
Carvedilol |
NiCARdipine may enhance the hypotensive effect of Carvedilol. NiCARdipine may precipitate signs of heart failure in susceptible patients on Carvedilol NiCARdipine may increase the serum concentration of Carvedilol. |
|
Clofazimine |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Clopidogrel |
Calcium Channel Blockers may diminish the therapeutic effect of Clopidogrel. |
|
CycloSPORINE (Systemic) |
Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). |
|
CYP3A4 Inducers (Moderate) |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
CYP3A4 Inhibitors (Moderate) |
May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). |
|
Dapoxetine |
May enhance the orthostatic hypotensive effect of Calcium Channel Blockers. |
|
Deferasirox |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Dexmethylphenidate |
May diminish the therapeutic effect of Antihypertensive Agents. |
|
Diazoxide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
DULoxetine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. |
|
Duvelisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Efavirenz |
May decrease the serum concentration of Calcium Channel Blockers. |
|
Erdafitinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Erdafitinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Erdafitinib |
May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. |
|
Fluconazole |
May increase the serum concentration of Calcium Channel Blockers. |
|
Fosaprepitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Fosnetupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Grapefruit Juice |
May increase the serum concentration of NiCARdipine. |
|
Herbs (Hypertensive Properties) |
May diminish the antihypertensive effect of Antihypertensive Agents. |
|
Herbs (Hypotensive Properties) |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Hypotension-Associated Agents |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. |
|
Ivosidenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Larotrectinib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Levodopa-Containing Products |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. |
|
Lormetazepam |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Magnesium Salts |
Calcium Channel Blockers may enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers. |
|
Melatonin |
May diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine). |
|
Methylphenidate |
May diminish the antihypertensive effect of Antihypertensive Agents. |
|
Molsidomine |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Naftopidil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Netupitant |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Neuromuscular-Blocking Agents (Nondepolarizing) |
Calcium Channel Blockers may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). |
|
Nicergoline |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Nicorandil |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Nitroprusside |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. |
|
Palbociclib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Pentoxifylline |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Perhexiline |
CYP2D6 Inhibitors (Weak) may increase the serum concentration of Perhexiline. |
|
P-glycoprotein/ABCB1 Inhibitors |
May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. P-glycoprotein inhibitors may also enhance the distribution of p-glycoprotein substrates to specific cells/tissues/organs where p-glycoprotein is present in large amounts (e.g., brain, T-lymphocytes, testes, etc.). |
|
Pholcodine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. |
|
Phosphodiesterase 5 Inhibitors |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Prostacyclin Analogues |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
Quinagolide |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. |
|
QuiNIDine |
Calcium Channel Blockers (Dihydropyridine) may decrease the serum concentration of QuiNIDine. Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of QuiNIDine. QuiNIDine may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). |
|
Ranolazine |
May increase the serum concentration of P-glycoprotein/ABCB1 Substrates. |
|
Sarilumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Siltuximab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Simeprevir |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
SUNItinib |
NiCARdipine may increase the serum concentration of SUNItinib. |
|
Tacrolimus (Systemic) |
Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of Tacrolimus (Systemic). |
|
Tocilizumab |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). |
|
Yohimbine |
May diminish the antihypertensive effect of Antihypertensive Agents. |
|
Risk Factor D (Consider therapy modification) |
|
|
Amifostine |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. |
|
Antifungal Agents (Azole Derivatives, Systemic) |
May enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs. Management: Concurrent use of felodipine or nisoldipine with itraconazole is specifically contraindicated. Frequent monitoring is warranted with any such combination; calcium channel blocker dose reductions may be required. Exceptions: Fluconazole; Isavuconazonium Sulfate. |
|
CarBAMazepine |
May increase the metabolism of Calcium Channel Blockers (Dihydropyridine). Management: Consider calcium channel blocker (CCB) dose adjustments or alternative therapy in patients receiving concomitant carbamazepine. Nimodipine Canadian labeling contraindicates concurrent use with carbamazepine. |
|
CYP3A4 Inducers (Strong) |
May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
|
CYP3A4 Inhibitors (Strong) |
May decrease the metabolism of CYP3A4 Substrates (High risk with Inhibitors). |
|
Dabrafenib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). |
|
Enzalutamide |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. |
|
Fosphenytoin |
Calcium Channel Blockers may increase the serum concentration of Fosphenytoin. Management: Monitor for phenytoin toxicity with concomitant use of a calcium channel blocker (CCB) or decreased phenytoin effects with CCB discontinuation. Monitor for decreased CCB therapeutic effects. Nimodipine Canadian labeling contraindicates use with phenytoin. |
|
Lorlatinib |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences. |
|
Macrolide Antibiotics |
May decrease the metabolism of Calcium Channel Blockers. Management: Consider using a noninteracting macrolide. Felodipine Canadian labeling specifically recommends avoiding its use in combination with clarithromycin. Exceptions: Azithromycin (Systemic); Fidaxomicin; Roxithromycin; Spiramycin. |
|
MiFEPRIStone |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. |
|
Mitotane |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. |
|
Obinutuzumab |
May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. |
|
Phenytoin |
Calcium Channel Blockers may increase the serum concentration of Phenytoin. Phenytoin may decrease the serum concentration of Calcium Channel Blockers. Management: Avoid use of nimodipine or nifedipine with phenytoin. Monitor for phenytoin toxicity and/or decreased calcium channel blocker effects with any concurrent use. |
|
Rifamycin Derivatives |
May decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers. Management: The labeling for some US and Canadian calcium channel blockers contraindicate use with rifampin, however recommendations vary. Consult appropriate labeling. |
|
Sincalide |
Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. |
|
St John's Wort |
May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. |
|
Stiripentol |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. |
|
Risk Factor X (Avoid combination) |
|
|
Bromperidol |
Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Bromperidol may diminish the hypotensive effect of Blood Pressure Lowering Agents. |
|
Conivaptan |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Fusidic Acid (Systemic) |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
|
Idelalisib |
May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). |
Monitoring parameters:
Different parameters such as BP and pulse monitoring is recommended.
-
Confirmed hypertension and known CVD or 10-year atherosclerotic cardiovascular disease (ASCVD) risk ≥10%:
- Target blood pressure <130/80 mm Hg is recommended.
-
Confirmed hypertension without markers of increased ASCVD risk:
- Target blood pressure <130/80 mm Hg may be reasonable.
-
Diabetes and hypertension: The American Diabetes Association (ADA) guidelines (ADA 2019):
-
Patients 18-65 years without atherosclerotic disease and 10-year risk <15%:
- Target blood pressure <140/90 mm Hg is recommended
-
Patients 18-65 years and having atherosclerotic disease or 10-year ASCVD risk >15%:
- Target blood pressure <130/80 mm Hg is advised.
-
Patients >65 years of age (healthy):
- Target blood pressure <140/90 mm Hg is recommended
-
Patients >65 years of age (poor health):
- Target blood pressure <150/90 mm Hg is recommended
-
How to administer Nicardipine (Cardene)?
- The total oral daily dose of the immediate-release product differs from the daily sustained-release dose therefore caution should be exercised during conversion.
- It can be taken without regard to meals, although sustained release if given with meal may decrease the fluctuation in plasma levels.
- The tablet should not be chewed or crushed but swallowed as a whole. Do not open or cut capsules.
- Intravenous preparation is given as a slow continuous infusion via central line/large peripheral vein.
- By changing the site of infusion every 12 hours, peripheral venous irritation can be prevented.
Premixed bags:
- Do not combine or run in the same line with other medications.
Mechanism of action of Nicardipine (Cardene):
- It causes calcium ion to be blocked from entering "slow channels" and voltage-sensitive areas in the vascular smooth muscles and myocardium during depolarization.
- This results in relaxation of the coronary vascular smooth muscles and coronary vasodilation. Patients with vasospastic gina have a higher rate of myocardial oxygen delivery.
The onset of action:
- Intravenous infusion is effective within minutes.
- 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 post-dose
- Intravenous continuous infusion: 50% of the maximum effect is seen by 45 minutes
Duration:
- Intravenous ≤8 hours upon discontinuation of continuous infusion, a 50% decrease in effect is seen in half an hour with gradual discontinuing antihypertensive effects for ~50 hours
- Oral: Immediate release: ≤8 hours
- Sustained-release: 8 to 12 hours
Absorption:
- Oral: ~100%, but large first-pass effect
Protein binding:
- >95%
Metabolism:
- Occurs in the liver, extensive first-pass effect (saturable) The major pathway is via cytochrome P450 isoenzyme CYP3A4, 2C8, and 2D6.
Bioavailability:
- Oral: ~35%
Half-life elimination:
- Follows dose-dependent (nonlinear) pharmacokinetics; “apparent” or calculated half-life is dependent upon serum concentrations.
- Oral: Half-life over the first 8 hours is 2 to 4 hours; terminal half-life: 8.6 hours.
- Serum concentrations decrease tri-exponentially after intravenous infusion; alpha half-life: 3 minutes; beta half-life: 45 minutes; terminal half-life: 14 hours
- Note: Terminal half-life can only be seen after long-term infusions).
Time to peak, serum: Oral:
- Immediate release: 30 to 120 minutes (mean: 1 hour)
- Sustained release: 60 to 240 minutes
Excretion:
- Urine (oral: 60% as metabolites; IV: 49% as metabolites; <1% as unchanged drug)
- feces (oral: 35%; IV: 43%)
- Clearance: Decreased in patients with liver impairment; may be decreased in patients with renal impairment
Nicardipine Brand Names (International):
- Cardene IV
- Antagonil
- Barizin
- Binicapin
- Blistra
- Cardene
- Cardene SR
- Cardepine
- Cardepine SR
- Cardibloc SR
- Cardibrain
- Cardilon
- Cardimed
- Cardipene
- Carsive
- Convertal
- Dacarel
- Dafil
- Dipitenz
- Flusemide
- Karden
- Lincil
- Loxen
- Loxen LP
- Nerdipina
- Nicafer
- Nicardal
- Nicardin
- Nidaven
- Nimicor
- Perdipina
- Perdipine
- Perdipine LA
- Ridene
- Rydene
- Tensilo
- Vasonase
- Xian Li
Nicardipine Brand Names in Pakistan:
Nicapress-R 40 mg (Amson Vaccines and Pharmaceuticals)