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Isradipine; Mechanism, Uses, Contraindications, Dosage, Side effects

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

Isradipine belongs to the dihydropyridine (DHP) class of calcium channel blockers (CCBs), the most widely used class of CCBs. There are at least five different types of calcium channels in Homo sapiens: L-, N-, P/Q-, R- and T-type. CCBs target L-type calcium channels, the major channel in muscle cells that mediates contraction. Similar to other DHP CCBs, isradipine binds directly to inactive calcium channels stabilizing their inactive conformation. Since arterial smooth muscle depolarizations are longer in duration than cardiac muscle depolarizations, inactive channels are more prevalent in smooth muscle cells. Alternative splicing of the alpha-1 subunit of the channel gives isradipine additional arterial selectivity. At therapeutic sub-toxic concentrations, isradipine has little effect on cardiac myocytes and conduction cells.

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.

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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

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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.

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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.