Nisoldipine

Pronunciation: nye-SOL-di-peen
Class: Calcium channel blocking agent

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Trade Names

Sular
- Tablets, extended-release 8.5 mg
- Tablets, extended-release 17 mg
- Tablets, extended-release 25.5 mg
- Tablets, extended-release 34 mg

Pharmacology

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 9.2 to 5.1 h. High-fat food results in significant increase in peak concentration (up to 245%) and a decrease in AUC by 25%.

Metabolism

Presystemic metabolism of nisoldipine in gut wall and liver by CYP-450 enzymes.

Elimination

87% of the radiolabeled drug is recovered in urine and feces. Nisoldipine is eliminated 60% to 80% in urine (traces unchanged), 5 urinary metabolites and only 1 active. The t _½ is 13.7 to 4.3 h.

Special Populations

Renal Function Impairment

Dosage adjustments are not needed in patients with mild to moderate renal function impairment.

Elderly

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

Liver cirrhosis

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

Adults

PO Initiate therapy with 17 mg once daily, then increase by 8.5 mg/wk, or with longer intervals, to attain adequate BP control (max, 34 mg/day).

Patients older than 65 yr of age, or patients with impaired liver function

Initiate therapy with 8.5 mg once daily.

General Advice

Have patient swallow tablets whole. Do not allow patient to crush, chew, or divide.
Administer once daily 1 h before or 2 h after a meal. Do not administer with a high-fat meal. Avoid grapefruit products.

Storage/Stability

Store at 68° to 77°F. Protect from light and moisture.

Drug Interactions

CYP3A4 inducers (eg, carbamazepine, phenytoin)

Because nisoldipine is a substrate for CYP3A4, in general, avoid coadministration with CYP3A4 inducers. Nisoldipine plasma levels may be reduced, decreasing the efficacy.

CYP3A4 inhibitors (eg, azole antifungal agents [eg, itraconazole, ketoconazole], cimetidine, grapefruit juice, quinidine)

Because nisoldipine is a substrate for CYP3A4, in general, avoid coadministration with CYP3A4 inhibitors. Nisoldipine plasma levels may be elevated, increasing the pharmacologic effect and adverse reactions.

Laboratory Test Interactions

None well documented.

Adverse Reactions

Cardiovascular

Vasodilation (4%); palpitation (3%).

CNS

Headache (22%); dizziness (5%).

Dermatologic

Rash (2%).

EENT

Pharyngitis (5%).

GI

Nausea (2%).

Hypersensitivity

Systemic hypersensitivity including angioedema, chest tightness, hypotension, rash, shortness of breath, and tachycardia (postmarketing).

Respiratory

Sinusitis (3%).

Miscellaneous

Peripheral edema (22%); chest pain (2%).

Precautions

Monitor

Monitor BP during initial administration and titration.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Use with caution, usually starting at the low end of the dosage range because of the greater frequency of decreased hepatic, renal, or cardiac function, and concomitant diseases or other drug therapy.

Hepatic Function

Use drug with caution in patients with severe hepatic function impairment.

Tartrazine Sensitivity

Contains FD&C Yellow No. 5. Use with caution in patients with aspirin sensitivity.

CHF

Use drug with caution in patients with CHF or compromised ventricular function.

Coronary artery disease

Sometimes, 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 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: dizziness; headache; increasing chest pain; palpitations; swelling of ankles, feet, or hands.
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 suddenly stop taking the medication.