General

Pronunciation:
nye-sole-di-peen

Trade Name(s)

• Sular

Ther. Class.

antihypertensives

Pharm. Class.

calcium channel blockers

Indications

Management of hypertension.

Action

Inhibits the transport of calcium into vascular smooth muscle cells, resulting in inhibition of vasoconstriction and dilation of arterioles.

Therapeutic Effect(s):

Systemic vasodilation, resulting in decreased BP.

Pharmacokinetics

Absorption: Well absorbed (87%) following oral administration but rapidly and extensively metabolized in the gut wall, resulting in 5% bioavailability.

Distribution: Unknown.

Metabolism and Excretion: Highly metabolized CYP3A4 enzyme system.

Half-life: 7–12 hr.

TIME/ACTION PROFILE (antihypertensive effects)

Contraindication/Precautions

Contraindicated in:

• Hypersensitivity;
• Cross-sensitivity with calcium channel blockers may occur;
• Concurrent phenytoin use.

Use Cautiously in:

• HF/left ventricular dysfunction;
• Hepatic impairment (dose ↓ may be necessary);
• Coronary artery disease (may precipitate angina);
• OB:  Lactation: Pedi:  Safety not established;
• Geri:  Dose ↓ may be necessary due to age-related ↓ in hepatic, renal or cardiac function.

Adverse Reactions/Side Effects

CNS: headache, dizziness

EENT: pharyngitis, sinusitis

CV: peripheral edema, chest pain, hypotension, palpitations

GI: nausea

Derm: rash

Endo: gynecomastia

* CAPITALS indicate life-threatening.
Underline indicate most frequent.

Interactions

Drug-Drug

• Additive hypotension may occur with other  antihypertensives, acute ingestion of  alcohol, or  nitrates.
• Antihypertensive effects may be ↓ by concurrent use of  NSAIDs.
•  Phenytoin  or other  CYP3A4 inducers  ↓ blood levels and effectiveness (avoid concurrent use).

Drug-Food:

• Grapefruit and grapefruit juice ↑ serum levels and effect.
• Blood levels are ↑ by concurrent ingestion of a high-fat meal and should be avoided.

Route/Dosage

PO (Adults): Extended-release tablets– 20 mg/day as a single dose initially; may be ↑ by 10 mg/day q 7 days, up to 60 mg/day (usual range 20–40 mg/day);  Geomatrix extended-release tablets– 17 mg/day as a single dose initially; may be ↑ by 8.5 mg/day q 7 days, up to 34 mg/day (usual range 8.5–34 mg/day).

Hepatic Impairment 
PO (Adults): Geomatrix extended-release tablets– Initial dose should not exceed 8.5 mg/day.

Availability (generic available)

Extended-release tablets: 20 mg, 30 mg, 40 mg

Geomatrix extended-release tablets: 8.5 mg, 17 mg, 25.5 mg, 34 mg

Assessment

• Monitor BP and pulse prior to therapy, during dose titration, and periodically throughout therapy. Monitor ECG periodically during prolonged therapy.

  • Monitor intake and output ratios and daily weight. Assess for signs of HF (peripheral edema, rales/crackles, dyspnea, weight gain, jugular venous distention).

Lab Test Considerations:

Total serum calcium concentrations are not affected by calcium channel blockers.

Potential Diagnoses

• Decreased cardiac output (Indications) 

Implementation

• PO Avoid administration within 1 hr of high-fat meals or grapefruit products.
  • Do not break, crush, or chew tablets.

Patient/Family Teaching

Advise patient to take medication exactly as directed, even if feeling well. If a dose is missed, take as soon as possible unless almost time for next dose; do not double dose. May need to be discontinued gradually.

• Advise patient to avoid grapefruit or grapefruit juice during therapy.
• Encourage patient to comply with other interventions for hypertension (weight reduction, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, and stress management). Medication controls but does not cure hypertension.
• Instruct patient and family in proper technique for monitoring BP. Advise patient to take BP weekly and to report significant changes to health care professional.
• Caution patient to change positions slowly to minimize orthostatic hypotension.
• May cause dizziness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and to avoid concurrent use of alcohol or OTC medications and herbal products, especially cold preparations, without consulting health care professional.
• Advise patient to notify health care professional if irregular heartbeat, dyspnea, swelling of hands and feet, pronounced dizziness, nausea, constipation, or hypotension occurs or if headache is severe or persistent.

Evaluation/Desired Outcomes

Decrease in BP.