Nisoldipine

Oral
Angina pectoris, Hypertension

Immediate-release: Initially, 5 or 10 mg once daily. Modified-release: Initially, 8.5 mg once daily.

Concomitant use w/ CYP3A4 inducers.

Patients w/ severe aortic stenosis, heart failure, hypertrophic cardiomyopathy (HCM) w/ outflow tract obstruction. Hepatic impairment. Elderly. Pregnancy and lactation.

Dizziness, headache, peripheral oedema, chest pain, angina exacerbation, palpitations, vasodilation, pharyngitis, sinusitis, nausea, rash.

PO: C

Monitor BP carefully during the initial admin or if there is subsequent upward dose adjustment.

Symptoms: Hypotension. Management: Symptomatic and supportive treatment. Monitor CV and resp function. Elevation of extremities, use of Ca infusion, pressor agents and fluid may be necessary.

May increase serum levels w/ CYP3A4 inhibitors. Increased levels w/ cimetidine. Increased antihypertensive effect w/ atenolol. Propranolol attenuated heart rate increase following intake of immediate-release nisoldipine. Reduced bioavailability w/ quinidine. Increased quinidine levels w/ immediate-release nisoldipine.
Potentially Fatal: Concomitant use w/ potent CYP3A4 inducers (e.g. phenytoin) may decrease nisoldipine plasma concentration to undetectable levels.

High-fat food increases peak concentration. Avoid grapefruit-containing foods and beverages as it increases peak concentrations and oral bioavailability of nisoldipine. Levels may be reduced w/ St John's wort.

Description: Nisoldipine is a dihydropyridine Ca channel blocker. It inhibits the movement of Ca ions into vascular smooth muscle and cardiac muscle. It reversibly competes w/ other dihydropyridines for binding to the Ca channel.
Duration: >24 hr.
Pharmacokinetics:
Absorption: Well absorbed from the GI tract. High-fat food increases peak concentration. Bioavailability: Approx 4-8%.
Distribution: Plasma protein binding: >99%.
Metabolism: Undergoes rapid and extensive first-pass metabolism in the gut wall and liver.
Excretion: Via urine (approx 60-80%) and faeces (remaining dose as metabolites). Terminal elimination half-life: Approx 7-12 hr.

Store between 20-25°C. Protect from light and moisture.

Calcium Antagonists

Anon. Nisoldipine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com.

Anon. Nisoldipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com.

Buckingham R (ed). Nisoldipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com.

Sular (Physicians Total Care, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/.

Sular Extended Release Tablets. U.S. FDA. https://www.fda.gov/ .