Sular (nisoldipine)
Last reviewed · Source: First Databank (FDB) drug data
Overview
Nisoldipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent (calcium-channel blocker).
Nisoldipine is a 1,4-dihydropyridine-derivative calcium-channel blocking agent that is structurally related to nifedipine. Nisoldipine has pharmacologic actions similar to those of other dihydropyridine calcium-channel blocking agents (e.g., felodipine, nifedipine). The principal physiologic action of nisoldipine is to inhibit the transmembrane influx of extracellular calcium ions across the membranes of myocardial cells and vascular smooth muscle cells.
Nisoldipine is a peripheral arterial vasodilator; the drug acts directly on vascular smooth muscle causing a reduction in peripheral vascular resistance and blood pressure. The effects of nisoldipine are more selective to vascular smooth muscle than cardiac muscle. Nisoldipine currently is commercially available in the US only as extended-release tablets; some dosage forms contain nisoldipine in a hydrogel layer that provides for controlled drug release.
Following oral administration, nisoldipine is relatively well absorbed from the GI tract; peak plasma concentrations are attained in 6-12 (mean 9.2) hours. The low bioavailability (about 5%) of nisoldipine is due, in part, to pre-systemic metabolism in the gut wall, and this metabolism decreases from the proximal to distal parts of the intestine. When nisoldipine is administered with a high-fat meal, peak plasma concentrations increase by up to 245%, but AUC decreases by 25%.
The extended-release hydrogen tablets of nisoldipine containing 8.5, 17, 25.5, and 34 mg of the drug are bioequivalent to the extended-release formulation containing 10, 20, 30, and 40 mg, respectively, of the drug.
Plasma protein binding is greater than 99%; it is not known whether nisoldipine is distributed into human milk. Nisoldipine is extensively metabolized and the drug is excreted principally in the urine (60-80%) as metabolites; the major pathway appears to involve hydroxylation; the drug is thought to be metabolized principally by cytochrome P-450 (CYP) isoenzymes. Nisoldipine is a substrate of CYP3A4 similar to other dihydropyridine-derivative calcium-channel blocking agents.
The manufacturer states a hydroxylated metabolite, present in plasma at concentrations approximately equal to the parent compound, appears to be the only active metabolite, and has about 10% of the activity of the parent compound. The terminal elimination half-life is approximately 13-17 hours.
Nisoldipine peak plasma concentrations and AUC are increased about 2- to 3-fold in geriatric patients compared to young individuals. Nisoldipine plasma concentrations are increased by 4-5 times in patients with hepatic cirrhosis compared to young healthy individuals.
USES: This medication is used to treat high blood pressure. Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. Nisoldipine belongs to a class of drugs known as calcium channel blockers.
It works by relaxing blood vessels so blood can flow more easily.
Generic name: nisoldipine
Pronunciation: (nye-SOL-di-peen)
Reference product & biosimilars
No reference, biosimilar or interchangeable associated with this drug.
Today’s intelligence on Sular
Indications
The following indications are listed for Sular:
- Hypertension
Also known as: Elevated Blood Pressure, Essential Hypertension, Hyperpiesia, Hyperpiesis, Hypertensive Disorder, Systemic Arterial Hypertension.
Dosing
Extended-release nisoldipine hydrogel tablets containing 8.5, 17, 25.5, and 34 mg of nisoldipine are bioequivalent to the extended-release formulations containing 10 (no longer commercially available), 20, 30, and 40 mg, respectively.
Nisoldipine is administered orally as extended-release tablets. Nisoldipine is commercially available as a hydrogel extended-release tablet formulation (Sular(R) and generic equivalents) and as extended-release generic tablet preparations; the tablets should be swallowed intact and should not be chewed, broken, divided, or crushed.
Nisoldipine extended-release tablets should be administered on an empty stomach (1 hour before or 2 hours after a meal); because high-fat food increases the peak concentration of nisoldipine, concomitant administration of the drug with such food should be avoided. In addition, because grapefruit juice increases peak concentrations and oral bioavailability of the drug, patients should be instructed to avoid grapefruit-containing foods and beverages before and after administration of a dose of nisoldipine.
Store nisoldipine extended-release tablets (Sular(R)) at 20-25degreesC (excursions permitted to 15-30degreesC) in a tight, light-resistant container; protect from light and moisture. The manufacturer of generic preparations of nisoldipine extended-release tablets recommends that the drug be stored at 20-25degreesC in a tight, light-resistant container, protected from light and moisture.
No dosing information is available for this tab.
No dosing information is available for this tab.
Drug interactions
Nisoldipine is a substrate of cytochrome P-450 (CYP) isoenzyme 3A4.
There are no contraindication interactions for this drug.
There are no severe interactions for this drug.
There are no moderate interactions for this drug.
Contraindications
*Known hypersensitivity to nisoldipine, any ingredient in the formulation, or other dihydropyridine-derivative calcium-channel blockers.
There are no contraindication contraindications for this drug.
There are no severe contraindications for this drug.
There are no moderate contraindications for this drug.
Adverse reactions
The most common adverse effects of nisoldipine in clinical studies were peripheral edema, headache, dizziness, pharyngitis, vasodilation, sinusitis, palpitation, chest pain, nausea, and rash.
There are no severe adverse reactions for this drug.
There are no less severe adverse reactions for this drug.
Precautions
No enhanced messaging available.
Safety and efficacy of nisoldipine have not been established in pediatric patients younger than 18 years of age.
In animal studies, nisoldipine was not teratogenic, but demonstrated fetotoxicity at maternally toxic doses (reduced maternal body weight gain). Increased fetal resorption (postimplantation loss), decreased fetal and placental weights, and high rates of abortion and mortality, with limb and vertebral abnormalities found in the only surviving fetus, were observed in rats, rabbits, and monkeys, respectively, treated with nisoldipine at doses 5-30 times the maximum recommended human dose (MRHD) on a mg/m2 basis.
There are no adequate and well controlled studies of nisoldipine in pregnant women. Nisoldipine should be used during pregnancy only when the potential benefits justify the possible risks to the fetus.
It is not known whether nisoldipine is distributed into human milk. Because many drugs are excreted in human milk, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.
In geriatric patients older than 65 years of age, the initial dosage should not exceed 8.5 mg daily if using the hydrogel extended-release tablets or 10 mg daily if using generic extended-release tablets, and blood pressure response should be monitored closely with each dosage adjustment.
When nisoldipine is administered to elderly patients, peak plasma concentrations and AUC are 2- to 3-fold higher compared to younger subjects. Clinical studies of nisoldipine did not include sufficient numbers of patients older than 65 years of age to determine whether they respond differently than younger patients. While other clinical experience generally has not revealed age-related differences in response, in general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.
The manufacturer states nisoldipine should be administered cautiously in elderly patients; a lower initial dosage is recommended and blood pressure response should be monitored closely with each dosage adjustment.
ICD codes
No ICD codes are available for this drug.
Formulary status
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Last reviewed · Source: First Databank (FDB) drug data
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