Nisoldipine
Pronouncation: (nye-SOLD-ih-peen)Class: Calcium channel blocking agent
Trade Names:
Sular
- Tablets, extended-release 10 mg
- Tablets, extended-release 20 mg
- Tablets, extended-release 30 mg
- Tablets, extended-release 40 mg
Pharmacology
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Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle and myocardium.
Pharmacokinetics
Absorption
Nisoldipine is well absorbed. Absolute bioavailability is 5% and T max is 6 to 12 h. High fat food significantly affects release of drug from coat-core formulation, resulting in significant increase in peak concentration.
Metabolism
Presystemic metabolism of nisoldipine in gut wall and liver by CYP-450 enzymes.
Elimination
Nisoldipine is eliminated 60% to 80% in urine (traces unchanged), 5 urinary metabolites and only 1 active. The t 1/ 2 is 7 to 12 h.
Special Populations
ElderlyHigher nisoldipine plasma concentrations (C max and AUC) have been found in elderly.
Liver CirrhosisIncreased plasma concentrations. Use lower starting and maintenance doses.
Indications and Usage
Treatment of hypertension, alone or in combination with other antihypertensive agents.
Contraindications
Sensitivity to dihydropyridine calcium channel blockers.
Dosage and Administration
AdultsPO Initiate therapy with 20 mg once daily, then increase by 10 mg/wk, or at longer intervals, to attain adequate BP control. Doses greater than 60 mg once daily are not recommended.
General Advice
- Have patient swallow tablets whole. Do not allow patient to crush, chew, or divide.
- Administer once daily. Do not administer with a high fat meal. Avoid grapefruit products.
Storage/Stability
Store at controlled room temperature (59° to 86°F) protected from light and moisture.
Drug Interactions
Azole antifungal agents (eg, ketoconazole), cimetidine, grapefruit juiceMay increase nisoldipine concentrations and effects.
Hydantoins (eg, phenytoin)May decrease nisoldipine levels and effects.
Laboratory Test Interactions
None well documented.
Adverse Reactions
Cardiovascular
Vasodilation; palpitation; chest pain.
CNS
Headache; dizziness.
Dermatologic
Rash.
EENT
Sinusitis; pharyngitis.
GI
Nausea.
Miscellaneous
Peripheral edema.
Precautions
Pregnancy
Category C .
Lactation
Undetermined.
Children
Safety and efficacy not established.
Elderly
Start with doses no greater than 10 mg in patients older than 65 yr of age.
Hepatic Function
Use drug with caution in patients with severe hepatic function impairment. Start with doses no greater than 10 mg/day.
CHF
Use drug with caution in patients with CHF.
Increased angina, MI
Occasional patients, particularly those with severe obstructive coronary artery disease, may have increased frequency, duration, or severity of angina or acute MI at start of therapy or when dose is increased.
Overdosage
Symptoms
Pronounced hypotension.
Patient Information
- Instruct patient not to chew, crush, or divide extended-release tablets.
- Advise patient not to take with a high-fat meal and to avoid grapefruit products before and after dosing.
- Advise patient to take the medication once daily as directed even if they have no symptoms.
- Teach patient correct technique for monitoring BP and pulse daily.
- Advise patient not to stop or change the dose unless advised by the health care provider.
- Advise patient that drug may cause dizziness and to use caution while driving or performing other tasks requiring mental alertness.
- Instruct patient to report the following symptoms to health care provider: palpitations; increasing chest pain; swelling of ankles, feet or hands; headache; dizziness.
- Stress the need to comply with the other components of the hypertensive regimen, such as dietary changes, weight loss, and exercise.
- Instruct patient never to stop taking the medication suddenly.
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More Nisoldipine resources:
Nisoldipine Extended-Release Tablets
Nisoldipine - Includes detailed dosage instructions.
High Blood Pressure, Angina Pectoris Prophylaxis












