NISOLDIPINE

NISOLDIPINE
(ni-sol'di-peen)
Sular
Classifications: calcium channel blocker; antihypertensive; antianginal;
Therapeutic: antihypertensive
; antianginal
Prototype: Nifedipine
Pregnancy Category: C

Availability

10 mg, 20 mg, 30 mg, 40 mg sustained release tablets

Action

Inhibits calcium ion influx across cell membranes of cardiac muscle and vascular smooth muscle, which results in vasodilation, inotropism, and negative chronotropism.

Therapeutic Effect

Inhibits vasoconstriction in the peripheral vasculature (10 times as potent as nifedipine). Significantly reduces total peripheral resistance, decreases blood pressure, and increases cardiac output. It is also a potent coronary vasodilator.

Uses

Hypertension, angina.

Unlabeled Uses

CHF.

Contraindications

Hypersensitivity to nisoldipine or other calcium blockers; systolic BP <90 mm Hg, advanced aortic stenosis, advanced heart failure, cardiogenic shock, severe hypotension, acute MI, sick sinus syndrome; pregnancy (category C); lactation.

Cautious Use

Liver dysfunction; older adult; paroxysmal atrial fibrillation; GERD; CHF; digital ischemia, ulceration, or gangrene; nonobstructive hypertrophic cardiomyopathy; Duchenne muscular dystrophy.

Route & Dosage

Hypertension, Angina
Adult: PO 10–40 mg/d (max: 60 mg/d), may need to reduce dose in patients with liver disease (cirrhosis, chronic hepatitis)

Administration

Oral
  • Give drug with food to decrease GI distress, but do not give with grapefruit juice or a high-fat meal.
  • Ensure that sustained release form is not chewed or crushed. It must be swallowed whole.
  • Discontinue drug gradually to prevent adverse effects.
  • Consider dosage reductions in older adults; initiate therapy at lower doses and follow with gradual increases.
  • Store at 15°–30° C (59°–86° F).

Adverse Effects (≥1%)

CNS: Dizziness, anxiety, tremor, weakness, fatigue, headache. CV: Hypotension, peripheral edema, palpitations, orthostatic hypotension. GI: Abdominal pain, cramps, constipation, dry mouth, diarrhea, nausea. Skin: Flushing, rash, erythema, urticaria. Urogenital: Urinary frequency. Respiratory: Pulmonary edema (patients with CHF), wheezing, dyspnea. Body as a Whole: Myalgia.

Interactions

Drug: May cause significant increase in digoxin level in patients with CHF. beta blockers may cause hypotension and bradycardia. Phenytoin, carbamazepine, phenobarbital may significantly decrease levels. Azole antifungals may affect metabolism; avoid combination. Food: High-fat food increases availability.

Pharmacokinetics

Absorption: Rapidly from GI tract; 4–8% reaches systemic circulation. Peak Effect: 1–3 h. Duration: 8–12 h for hypertension, 7–8 h for angina. Distribution: 99% protein bound. Metabolism: Extensively in liver. Elimination: 70–75% in urine as metabolites. Half-Life: 2–14 h.

Nursing Implications

Assessment & Drug Effects

  • Monitor blood pressure carefully during period of drug initiation and with dosage increments.
  • Monitor cardiovascular status especially heart rate, frequency of angina attacks, or worsening heart failure.
  • Assess for and report edematous weight gain.
  • Monitor digoxin levels closely with concurrent use and watch for S&S of digoxin toxicity (see Appendix F).

Patient & Family Education

  • Do not discontinue the drug abruptly.
  • Report symptoms of orthostatic hypotension or other bothersome adverse effects to physician.
  • Do not drive or engage in potentially hazardous activities until response to drug is known.

Common adverse effects in italic, life-threatening effects underlined; generic names in bold; classifications in SMALL CAPS; Canadian drug name; Prototype drug

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