fe-LOE-di-peen

Therapeutic Classification: antianginals, antihypertensives

Pharmacologic Classification: calcium channel blockers

• Hypertension.
• Angina pectoris.
• Vasospastic (Prinzmetal’s) angina.

• Inhibits the transport of calcium into myocardial and vascular smooth muscle cells, resulting in inhibition of excitation-contraction coupling and subsequent contraction.

• Systemic vasodilation resulting in decreased BP.
• Coronary vasodilation resulting in decreased frequency and severity of attacks of angina.

Absorption: Well absorbed after oral administration but extensively metabolized, resulting in ↓ bioavailability.

Distribution: Unknown.

Protein Binding: >99%.

Metabolism/Excretion: Mostly metabolized; minimal amounts excreted unchanged by kidneys.

Half-life: 11–16 hr.

(antihypertensive effect)

Contraindicated in:

• Hypersensitivity (cross-sensitivity may occur)
• Sick sinus syndrome
• 2nd- or 3rd-degree AV block (unless an artificial pacemaker is in place)
• Systolic BP <90 mm Hg
• Lactation: Lactation.

Use Cautiously in:

• Severe hepatic impairment (dose ↓ recommended)
• Geri: Dose ↓ recommended; ↑ risk of hypotension
• Severe renal impairment
• History of serious ventricular arrhythmias or HF
• OB: Safety not established in pregnancy
• Pedi: Safety and effectiveness not established in children.

CV: peripheral edema, ARRHYTHMIAS, chest pain, HF, hypotension, palpitations, syncope, tachycardia.

Derm: ↑sweating, dermatitis, erythema multiforme, flushing, photosensitivity, pruritus/urticaria, rash, STEVENS-JOHNSON SYNDROME (SJS).

EENT: blurred vision, disturbed equilibrium, epistaxis, tinnitus.

Endo: gynecomastia, hyperglycemia.

GI: ↑liver enzymes, anorexia, constipation, diarrhea, dry mouth, dyspepsia, gingival hyperplasia, nausea, vomiting.

GU: dysuria, nocturia, polyuria, sexual dysfunction, urinary frequency.

Hemat: anemia, leukopenia, thrombocytopenia.

Metab: weight gain.

MS: joint stiffness, muscle cramps.

Neuro: headache, abnormal dreams, anxiety, confusion, dizziness, drowsiness, dysgeusia, paresthesia, psychiatric disturbances, tremor, weakness.

Resp: cough, dyspnea.

Drug-Drug:

• Additive hypotension may occur when used concurrently with fentanyl, other antihypertensives, nitrates, acute ingestion of alcohol, or quinidine.
• Antihypertensive effects may be ↓ by concurrent use of NSAIDs.
• Ketoconazole, itraconazole, propranolol, and erythromycin may ↑ levels and the risk of toxicity.

Drug-Food:

• Grapefruit juice may ↑ levels and the risk of toxicity.

• PO (Adults): 5 mg/day (2.5 mg/day in geriatric patients); may ↑ every 2 wk (range 5–10 mg/day; not to exceed 10 mg/day).

(Generic available)

• Extended-release tablets: 2.5 mg; 5 mg; 10 mg;

• Monitor BP and pulse before therapy, during dosage titration, and periodically during 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).
• Assess for rash periodically during therapy. May cause SJS. Discontinue therapy if severe or if accompanied with fever, general malaise, fatigue, muscle or joint aches, blisters, oral lesions, conjunctivitis, hepatitis, and/or eosinophilia.
• Angina: Assess location, duration, intensity, and precipitating factors of patient’s anginal pain.
• Hypertension: Check frequency of refills to monitor adherence.

• Total serum calcium concentrations are not affected by calcium channel blockers.
  • Monitor serum potassium periodically. Hypokalemia↑ risk of arrhythmias and should be corrected.
  • Monitor renal and hepatic functions periodically during long-term therapy. May cause ↑ in hepatic enzymes after several days of therapy, which return to normal upon discontinuation of therapy.

• PO: May be administered without regard to meals. May be administered with meals if GI irritation becomes a problem.
• DNC: Swallow tablets whole; do not break, crush, or chew. Empty tablets that appear in stool are not significant.

• Advise patient to take medication 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 doses. May need to be discontinued gradually.
  • Instruct patient on correct technique for monitoring pulse. Instruct patient to contact health care professional if heart rate <50 bpm.
  • Advise patient to avoid grapefruit and grapefruit juice during therapy.
  • Caution patient to change positions slowly to minimize orthostatic hypotension.
  • May cause drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
  • Instruct patient on importance of maintaining good dental hygiene and seeing dentist frequently for teeth cleaning to prevent tenderness, bleeding, and gingival hyperplasia (gum enlargement).
  • 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 rash, irregular heartbeat, dyspnea, swelling of hands and feet, pronounced dizziness, nausea, constipation, or hypotension occurs or if headache is severe or persistent.
  • Caution patient to wear protective clothing and to use sunscreen to prevent photosensitivity reactions.
  • Advise patient to inform health care professional of medication regimen before treatment or surgery.
  • Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected and to avoid breastfeeding.
• Angina: Instruct patient on concurrent nitrate or beta blocker therapy to continue taking both medications as directed and to use SL nitroglycerin as needed for anginal attacks.
  • Advise patient to contact health care professional if chest pain does not improve or worsens after therapy; occurs with diaphoresis or shortness of breath; or if severe, persistent headache occurs.
  • Caution patient to discuss exercise restrictions with health care professional before exertion.
• Hypertension: 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.

• Decrease in BP.
• Decrease in frequency and severity of anginal attacks.
  • Decrease in need for nitrate therapy.
  • Increase in activity tolerance and sense of well-being.

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