Isradipine is a second generation calcium channel blocker that is used to treat hypertension. Isradipine is associated with a low rate of serum enzyme elevations during therapy but has not been linked convincingly to instances of clinically apparent liver injury.
Isradipine is a dihydropyridine calcium channel blockers with antihypertensive and vasodilator activities. Isradipine blocks the calcium entry through the calcium ion channels of coronary and peripheral vascular smooth muscle, thereby dilating coronary arteries and peripheral arterioles. This increases oxygen delivery due to an increased blood flow and reduces oxygen requirements due to a decrease in total peripheral resistance.
Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. It is structurally related to felodipine, nifedipine, and nimodipine and is the most potent calcium-channel blocking agent of the DHP class. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells.
Mechanism of action of Isradipine
Indications of Isradipine
- High blood pressure (Hypertension)
- Angina pectoris prophylaxis
- Raynaud’s Syndrome
- Heart failure
- Angina pectoris prophylaxis
- Hypertrophic cardiomyopathy
- Migraine prevention
- Pulmonary edemas
- Pulmonary hypertension
- For the management of mild to moderate essential hypertension. It may be used alone or concurrently with thiazide-type diuretics.
Contra-Indications of Isradipine
- Porphyria
- An acute syndrome of the heart
- Severe narrowing of the aortic heart valve
- Severe heart failure
- Abnormally low blood pressure
- Kidney disease with a reduction in kidney function
- Fluid Retention in the Legs, arms or hands
- Blood Circulation Failure due to Serious Heart Condition
- Chronic idiopathic constipation
- Stomach or intestine blockage
- Narrowing of the intestines
- Decreased motility function of stomach or intestines
- Heart attack
- Allergies to Calcium Channel Blockers
- Calcium Channel Blocking Agents-Dihydropyridines
Dosage of Isradipine
Strengths: 2.5 mg; 5 mg; 10 mg
Hypertension
Initial dose
- Immediate-release capsules: 2.5 mg orally twice a day
- Controlled-release tablets: 5 mg orally once a day
- Maintenance dose: The dose may be adjusted as needed and tolerated in increments of 5 mg at 2 to 4-week intervals.
Side Effects of Isradipine
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 Isradipine
Isradipine may interact with following drugs, 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 Isradipine
FDA Pregnancy Category C
Pregnancy
This medication should not be taken by women who are or may become pregnant, as isradipine may cause harm to the developing baby if it is taken by the mother during pregnancy. If you become pregnant while taking this medication, contact your doctor immediately.
Lactation
This medication should not be taken by women who are breastfeeding. The safety and effectiveness of using this medication have not been established for children.
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