Nisoldipine

Oral
Hypertension

As extended-release tab: Initially, 8.5 mg once daily, preferably taken 1 hour before or 2 hours after a meal. Adjust dose based on clinical response.

Concomitant use with CYP3A4 inducers.

Patient with severe aortic stenosis, heart failure, and hypertrophic cardiomyopathy with left ventricular outflow tract obstruction. Hepatic impairment. Elderly. Pregnancy and lactation.

Significant: Peripheral oedema; increased angina or MI (particularly in patients with coronary artery disease). Rarely, symptomatic hypotension (with or without syncope).
Cardiac disorders: Palpitations, chest pain.
Gastrointestinal disorders: Nausea.
Nervous system disorders: Headache, dizziness.
Respiratory, thoracic and mediastinal disorders: Pharyngitis, sinusitis.
Skin and subcutaneous tissue disorders: Rash.
Vascular disorders: Vasodilation.

PO: C

Monitor blood pressure closely during initial dosing and with dose adjustments; heart rate and LFTs. Assess for signs and symptoms of heart failure development.

Increased nisoldipine plasma concentration with CYP3A4 inhibitors (e.g. cimetidine).
Potentially Fatal: Decreased nisoldipine plasma concentration to undetectable levels with CYP3A4 inducers (e.g. phenytoin).

Increased nisoldipine peak concentrations (but total exposure may be decreased by 25%) with high-fat meals; avoid high-fat diet. Avoid grapefruit-containing foods or beverages (at least 1 hour before and 2 hours after dosing) as it significantly increases the peak concentrations and bioavailability of nisoldipine.

May result in a false-negative aldosterone/renin ratio (ARR).

Description:
Mechanism of Action: Nisoldipine, a dihydropyridine Ca channel blocker, inhibits the transmembrane influx of Ca ions into vascular smooth muscle and cardiac muscle. The inhibition of the Ca channel causes dilation of the arterioles, resulting in increased myocardial oxygen delivery due to coronary vasodilation, decreased myocardial oxygen demand via decreased total peripheral resistance, reduced systemic blood pressure, and afterload reduction.
Duration: >24 hours.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract. High-fat meals increase peak concentration but total exposure may be decreased. Bioavailability: Approx 5%. Time to peak plasma concentration: 9.2 ± 5.1 hours.
Distribution: Plasma protein binding: >99%.
Metabolism: Extensively metabolised in the liver into an active hydroxylated metabolite (approx 10% of the activity of the parent drug). Undergoes rapid and extensive first-pass metabolism in the gut wall and liver.
Excretion: Via urine (approx 60-80%, as inactive metabolites); faeces. Terminal elimination half-life: 13.7 ± 4.3 hours.

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 4499, Nisoldipine. https://pubchem.ncbi.nlm.nih.gov/compound/Nisoldipine. Accessed Nov. 25, 2022.

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

Calcium Antagonists

C08CA07 - nisoldipine ; Belongs to the class of dihydropyridine derivative selective calcium-channel blockers with mainly vascular effects. Used in the treatment of cardiovascular diseases.

Anon. Nisoldipine. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 11/11/2022.

Anon. Nisoldipine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 11/11/2022.

Buckingham R (ed). Nisoldipine. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 11/11/2022.

Nisoldipine. Gold Standard Drug Database in ClinicalKey [online]. Elsevier Inc. https://www.clinicalkey.com. Accessed 11/11/2022.

Sular Extended Release Tablets (Covis Pharma). U.S. FDA. https://www.fda.gov. Accessed 11/11/2022.

Sular Tablet, Film Coated, Extended Release (Covis Pharma US, Inc). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed. Accessed 11/11/2022.