Nisoldipine; Uses, Dosage, Side Effects, Interactions

Nisoldipine is a dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.

Nisoldipine is a dihydropyridine calcium channel blocking agent. Nisoldipine inhibits the transmembrane influx of extracellular calcium ions into myocardial and vascular smooth muscle cells, causing dilatation of the main coronary and systemic arteries and decreasing myocardial contractility. This agent also inhibits the drug efflux pump P-glycoprotein which is overexpressed in some multi-drug resistant tumors and may improve the efficacy of some antineoplastic agents.

Nisoldipine is a calcium channel blocker of the dihydropyridine class.  Nisoldipine has tropism for cardiac blood vessels. Nisoldipine is a 1,4-dihydropyridine calcium channel blocker. It acts primarily on vascular smooth muscle cells by stabilizing voltage-gated L-type calcium channels in their inactive conformation. By inhibiting the influx of calcium in smooth muscle cells, nisoldipine prevents calcium-dependent smooth muscle contraction and subsequent vasoconstriction.

Mechanism of Action of Nisoldipine

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, Nisoldipine 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 Nisoldipine

• High Blood Pressure (Hypertension)
• Raynaud’s Syndrome
• Angina Pectoris Prophylaxis
• Also for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents.

Contra-Indications of Nisoldipine

• Severe Disease of the Arteries of the Heart
• Chronic heart failure
• Abnormally low blood pressure
• Severely Low Blood Pressure
• Severe liver disease
• Allergies to Calcium Channel Blockers
• Calcium Channel Blocking Agents-Dihydropyridines

Dosage of Nisoldipine

Strengths: 10 mg; 20 mg; 30 mg; 40 mg; 8.5 mg; 17 mg; 25.5 mg; 34 mg

Hypertension

Slow release (old formulation)

• Initial dose: 20 mg orally once a day
• Maintenance dose: 10 to 60 mg orally once a day
• Maximum dose: 60 mg/day

Controlled release (new formulation)

• Initial dose: 17 mg orally once a day
• Maintenance dose: 8.5 to 34 mg orally once a day
• Maximum dose: 34 mg/day

Side Effects of Nisoldipine

The most common 

• severe headache, rapid heartbeat, stiffness in your neck,  
• chest pain, fast or slow heart rate;
• swelling, rapid weight gain;
• Xerostomia (dry mouth)
• 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
• headache, severe and throbbing
• joint or back pain
• muscle aching or cramping
• muscle pains or stiffness
• chest pressure or squeezing pain in 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
• cough
• Agitation
• arm, back, or jaw pain
• blurred vision
• chest pain or discomfort
• convulsions
• extra heartbeats
• fainting
• hallucinations
• headache
• irritability
• lightheadedness
• mood or mental changes
• muscle pain or cramps
• muscle spasm or jerking of all extremities
• nervousness

Drug Interactions of Nisoldipine

Nisoldipine  may interact with following drugs, supplements, & may change the efficacy of drugs

• 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)
• 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

FDA Pregnancy Category C

Pregnancy

This medication should not be taken by women who are or may become pregnant, as nisoldipine 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.

References

People Also Reading

Fimasartan; Uses, Dosage, Side Effects, Interactions, Pregnan Clevidipine; Uses, Dosage, Side effects, Interactions Lercanidipine; Uses, Dosage, Side Effects, Interactions Lavoltidine; Uses, Dosage, Side Effects, Interactions Levamlodipine; Uses, Dosage, Side Effects, Interactions Lacidipine; Uses, Dosage, Side Effects, Interactions Bepridil; Uses, Dosage, Side Effects, Interactions, Pregnancy Antacids; Uses, Dosage, Side Effects, Drug Interactions Nicardipine; Uses, Contraindications, Dosage, Side Effects, Interactions Cinnarizine; Uses, Dosage, Side Effects, Drug Interactions Diltiazem/Cardizem; Uses, Dosage, Side Effects, Interactions Tamsulosin; Uses, Dosage, Side Effects, Interactions