Nicardipine is 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 cardio-depressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
Nicardipine is a synthetic derivative of nitrophenyl-pyridine and potent calcium channel blocker, Nicardipine (Nifedipine Family) blocks calcium ions from certain cell walls and inhibits contraction of coronary and peripheral arteries, resulting in lowered oxygen requirements for heart muscle and decreased arterial contraction and spasm. It is used clinically as a cerebral and coronary vasodilator.
Nicardipine is a dihydropyridine calcium-channel blocking agent used for the treatment of vascular disorders such as chronic stable angina, hypertension, and Raynaud’s phenomenon.
Mechanism of action of Nicardipine
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.
By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes 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.
Indications of Nicardipine
- Chronic Stable Angina Pectoris
- High Blood Pressure (Hypertension)
- Migraines
- Angina Pectoris Prophylaxis
- Heart Failure
- Blood pressure >185/110 mm Hg arterial hypertension
Contra-Indications of Nicardipine
- Angina
- Severe Narrowing of the Aortic Heart Valve
- Chronic heart failure
- Hemorrhage in the brain
- Acute cerebral infarction
- Abnormally low blood pressure
- Liver problems
- Moderate to severe kidney impairment
- Chronic idiopathic constipation
- Allergies to Calcium Channel Blockers
- Calcium Channel Blocking Agents-Dihydropyridines
Dosage of Nicardipine
Strengths: 30 mg; 45 mg; 60 mg; 20 mg; 2.5 mg/mL; 20 mg/200 mL
Hypertension
Oral, Immediate release
- Initial dose: 20 mg orally 3 times a day
- Maintenance dose: 20 to 40 mg orally 3 times a day
Sustained release
- Initial dose: 30 mg orally twice a day
- Maintenance dose: 30 to 60 mg orally twice a day
IV infusion
As substitute for oral therapy:The following IV infusion rates are required to produce an average plasma level corresponding to a given oral dose at steady state:
- 20 mg orally every 8 hours is equivalent to 0.5 mg/hour via IV infusion
- 30 mg orally every 8 hours is equivalent to 1.2 mg/hour via IV infusion
- 40 mg orally every 8 hours is equivalent to 2.2 mg/hour via IV infusion
For initiation of therapy in patient not receiving oral nicardipine
- Initial dose: 5 mg/hour by IV infusion
- The infusion rate may be increased by 2.5 mg/hour every 5 to 15 minutes (rapid and gradual titration, respectively) up to a maximum of 15 mg/hour, until desired blood pressure reduction is achieved. The infusion rate should be decreased to 3 mg/hour following achievement of the blood pressure goal using rapid titration.
- Maintenance dose: The rate of infusion should be adjusted as needed to maintain the desired response.
Angina Pectoris Prophylaxis
Oral: Immediate release
- Initial dose: 20 mg orally 3 times a day
- Maintenance dose: 20 to 40 mg orally 3 times a day
Sustained release
- Initial dose: 30 mg orally twice a day
- Maintenance dose: 30 to 60 mg orally twice a day
IV infusion
The following IV infusion rates are required to produce an average plasma level corresponding to a given oral dose at steady state
- 20 mg orally every 8 hours is equivalent to 0.5 mg/hr IV infusion
- 30 mg orally every 8 hours is equivalent to 1.2 mg/hr IV infusion
- 40 mg orally every 8 hours is equivalent to 2.2 mg/hr IV infusion
- Initiation of therapy: 5 mg/hour by IV infusion
- May increase by 2.5 mg/hour every 5 to 15 minutes up to a maximum of 15 mg/hour
Congestive Heart Failure
Oral, Immediate release
- Initial dose: 20 mg orally 3 times a day
- Maintenance dose: 20 to 40 mg orally 3 times a day
Sustained release
- Initial dose: 30 mg orally twice a day
- Maintenance dose: 30 to 60 mg orally twice a day
IV infusion
The following IV infusion rates are required to produce an average plasma level corresponding to a given oral dose at steady state
- 20 mg orally every 8 hours is equivalent to 0.5 mg/hr IV infusion
- 30 mg orally every 8 hours is equivalent to 1.2 mg/hr IV infusion
- 40 mg orally every 8 hours is equivalent to 2.2 mg/hr IV infusion
Initiation of therapy: 5 mg/hour by IV infusion
May increase by 2.5 mg/hour every 5 to 15 minutes up to a maximum of 15 mg/hour
Side Effects of Nicardipine
The most common
- a severe headache, rapid heartbeat, stiffness in your neck,
- chest pain, fast or slow heart rate;
- swelling, rapid weight gain;
- Xerostomia (dry mouth)
- A headache
- Fatigue
- Skin reactions
- Hypotension
- Anxiety
- Constipation
- Nausea/vomiting
- Weight gain/loss
- Erectile dysfunction
More common
- Abdominal or stomach pain, discomfort, or tenderness
- chills or fever
- difficulty with moving
- a headache, severe and throbbing
- joint or back pain
- muscle aching or cramping
- muscle pains or stiffness
- chest pressure or squeezing pain in the chest
- discomfort in arms, shoulders, neck or upper back
- excessive sweating
- feeling of heaviness, pain, warmth and/or swelling in a leg or in the pelvis
- sudden tingling or coldness in an arm or leg
- sudden slow or difficult speech
- sudden drowsiness or need to sleep
- fast breathing
- sharp pain when taking a deep breath
- fast or slow heartbeat
- coughing up blood
- rust colored urine
- decreased amount of urine
Rare
- Anxiety
- change in vision
- chest pain or tightness
- confusion
- a cough
- Agitation
- arm, back, or jaw pain
- blurred vision
- chest pain or discomfort
- convulsions
- extra heartbeats
- fainting
- hallucinations
- a headache
- irritability
- lightheadedness
- mood or mental changes
- muscle pain or cramps
- muscle spasm or jerking of all extremities
- nervousness
Drug Interactions of Nicardipine
Nicardipine may interact with the following drug, supplements, & may change the efficacy of the drug
- allopurinol
- alpha blockers (e.g., alfuzosin, doxazosin, tamsulosin)
- alpha agonists (e.g., clonidine, methyldopa)
- angiotensin II receptor blockers (ARBs; e.g., candesartan, losartan)
- antidiabetes medications (e.g., insulin, metformin, glyburide)
- atypical antipsychotics (e.g., clozapine, olanzapine, quetiapine, risperidone)
- azathioprine
- barbiturates (e.g., butalbital, pentobarbital phenobarbital)
- beta-adrenergic blockers (e.g., atenolol, propranolol, sotalol)
- “azole” antifungals (e.g., itraconazole, ketoconazole, voriconazole)
- calcium channel blockers (e.g., amlodipine, diltiazem, nifedipine, verapamil)
- canagliflozin
- ciprofloxacin
- calcium supplements (e.g., calcium carbonate, calcium citrate)
- carbamazepine
- clopidogrel
- cyclosporine
- diuretics (water pills; e.g., furosemide, hydrochlorothiazide, triamterene)
- duloxetine
- “gliptin” diabetes medications (e.g., linagliptin, saxagliptin, sitagliptin)
- guanfacine
- heparin
- levodopa
- medications that increase potassium levels (e.g., potassium supplements, spironolactone, amiloride, and salt substitutes containing potassium)
- metformin
- nonsteroidal anti-inflammatory drugs (NSAIDs; e.g., ibuprofen, indomethacin, naproxen)
- other angiotensin-converting-enzyme inhibitors (ACEIs; e.g., captopril, ramipril)
- pentoxifylline
- macrolide antibiotics (e.g., clarithromycin, erythromycin)
- methylphenidate
- monoamine oxidase inhibitors (MAOIs; e.g., moclobemide, phenelzine, rasagiline, selegiline, tranylcypromine)
- phosphodiesterase-5 inhibitors (e.g., sildenafil, tadalafil, vardenafil)
- pregabalin
- sodium phosphates
- tizanidine
- trimethoprim
- valproic acid
- warfarin
Pregnancy Category of Nicardipine
FDA Pregnancy Category C
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.
Lactation
Studies in rats have shown that nicardipine can pass into breast milk. For this reason, it is recommended that women who wish to breastfeed should not take this drug.
References
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