Drug information of Nisoldipine

Mechanism of effect

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.

Pharmacodynamic

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.

Pharmacokinetics

Bioavailability: 4-8%

Peak Plasma Time: 6-12 hr

Duration: 24 hr

Protein Bound: 99%

Vd: 4-5 L/kg

Metabolism

Mainly metabolized in liver by CYP3A4

Metabolites: Hydroxylated isobutyl ester derivative (active, 10% potency of parent drug)

Clearance: 1400-2200 L/hr

Excretion: Urine (60-80%); feces (6-12%)

Dialyzable: HD: No

Drug indications

High Blood Pressure

Dosage

Adult

Hypertension

Hydrogel ER tablets: 17 mg PO qDay initially; may increase slowly by at least 1-week intervals; not to exceed 34 mg PO qDay

Coat-core ER tablets (generic): 20 mg PO qDay initially; may increase slowly by at least 1-week intervals; not to exceed 60 mg/day

Pediatric

Safety and efficacy not established

Side effects

Sinusitis , Headache , nausea , vertigo , palpitations , Peripheral edema

Interactions

Doxazosin , Dolasetron , Efavirenz , Erythromycin , Esomeprazole , Itraconazole , Isoniazid , Pantoprazole , Rabeprazole , Apalutamide , ivosidenib , lofexidine , Calcium carbonate , Rifabutin , Nefazodone , Dantrolene , Aluminium hydroxide , Idelalisib , Rifampin , Cimetidine , Sodium bicarbonate , Lansoprazole , Carbamazepine , Ketoconazole , Aluminium Mg , Treprostinil , tucatinib

Alerts

• Use caution in CHF, aortic stenosis, hypotension (initially or after dose increases), persistent progressive dermatologic reactions, exacerbation of angina (during initiation of treatment, after dose increased, beta blocker withdrawal), liver impairment
• Reflex tachycardia resulting in angina and/or MI in patients with obstructive coronary disease reported
• Peripheral edema may occur within 2-3 weeks of initiating therapy
• Hypotension with or without syncope is possible (particularly with severe aortic stenosis)
• Do not take with high fat meal or grapefruit products
• Start at lower dose with liver/kidney dysfunction, elderly

Points of recommendation

• Tell all of your health care providers that you take nisoldipine. This includes your doctors, nurses, pharmacists, and dentists.
• Avoid driving and doing other tasks or actions that call for you to be alert until you see how nisoldipine affects you.
• To lower the chance of feeling dizzy or passing out, rise slowly if you have been sitting or lying down. Be careful going up and down stairs.
• If you are allergic to tartrazine, talk with your doctor. Some products have tartrazine.
• It is rare, but worse chest pain and heart attack can happen after nisoldipine is first started or after the dose is raised. The risk may be greater in people who have very bad heart blood vessel disease. Talk with the doctor.
• Have your blood pressure checked often. Talk with your doctor.
• Have blood work checked as you have been told by the doctor. Talk with the doctor.
• Avoid grapefruit and grapefruit juice.
• Talk with your doctor before using OTC products that may raise blood pressure. These include cough or cold drugs, diet pills, stimulants, ibuprofen or like products, and some natural products or aids.
• Tell your doctor if you are pregnant or plan on getting pregnant. You will need to talk about the benefits and risks of using nisoldipine while you are pregnant.
• Tell your doctor if you are breast-feeding. You will need to talk about any risks to your baby.

• Take on an empty stomach. Take 1 hour before or 2 hours after meals.
• Swallow whole. Do not chew, break, or crush.
• To gain the most benefit, do not miss doses.
• Keep taking nisoldipine as you have been told by your doctor or other health care provider, even if you feel well.

• Take a missed dose as soon as you think about it.
• If it is close to the time for your next dose, skip the missed dose and go back to your normal time.
• Do not take 2 doses at the same time or extra doses.

Pregnancy level

C

Related drugs

Mibefradil , Nicardipine , Amlodipine , Diltiazem , Nifedipine , Nimodipine , Verapamil , Felodipine , Isradipine , Clevidipine , Lercanidipine

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