Nisoldipine

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

Higher nisoldipine plasma concentrations (C _max and AUC) have been found in elderly.

Increased 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

PO 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

May increase nisoldipine concentrations and effects.

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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