felodipine (fe-loe-di-peen) Plendil

 Indications

Management of hypertension, angina pectoris, and vasospastic

(Prinzmetal’s) angina.

Action

Inhibits the transport of calcium into myocardial and

vascular smooth muscle cells, resulting in inhibition of

excitation-contraction coupling and subsequent contraction.

Therapeutic Effects: Systemic vasodilation

resulting in decreased BP. Coronary vasodilation

resulting in decreased frequency and severity of attacks

of angina.

Pharmacokinetics

Absorption: Well absorbed after oral administration,

but extensively metabolized, resulting inpbioavailability.

Distribution: Unknown.

Protein Binding: 99%.

Metabolism and Excretion: Mostly metabolized;

minimal amounts excreted unchanged by kidneys.

Half-life: 11–16 hr.

TIME/ACTION PROFILE (antihypertensive

effect)

ROUTE ONSET PEAK DURATION

PO 1 hr 2–4 hr up to 24 hr

Contraindications/Precautions

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.

Use Cautiously in: Severe hepatic impairment

(doseprecommended); Geri: Doseprecommended;

qrisk of hypotension; Severe renal impairment; History

of serious ventricular arrhythmias or HF; OB, Lactation,

Pedi: Safety not established.

Adverse Reactions/Side Effects

CNS: headache, abnormal dreams, anxiety, confusion,

dizziness, drowsiness, nervousness, psychiatric disturbances,

weakness. EENT: blurred vision, disturbed

equilibrium, epistaxis, tinnitus. Resp: cough, dyspnea.

CV: ARRHYTHMIAS, HF, peripheral edema, chest pain,

hypotension, palpitations, syncope, tachycardia. GI:

anorexia, constipation, diarrhea, dry mouth, dysgeusia,

dyspepsia,qliver enzymes, nausea, vomiting. GU: dysuria,

nocturia, polyuria, sexual dysfunction, urinary frequency. Derm: dermatitis, erythema multiforme,

flushing,qsweating, photosensitivity, pruritus/urticaria,

rash. Endo: gynecomastia, hyperglycemia. Hemat:

anemia, leukopenia, thrombocytopenia.Metab:

weight gain. MS: joint stiffness, muscle cramps.

Neuro: paresthesia, tremor. Misc: STEVENS-JOHNSON

SYNDROME, gingival hyperplasia.

Interactions

Drug-Drug: Additive hypotension may occur when

used concurrently with fentanyl, other antihypertensives,

nitrates, acute ingestion of alcohol,

or quinidine. Antihypertensive effects may bepby

concurrent use of NSAIDs. Ketoconazole, itraconazole,

propranolol, and erythromycinpmetabolism

andqblood levels and the risk of toxicity (dosepmay

be necessary).

Drug-Food: Grapefruit juiceqserum levels and

effect.

Route/Dosage

PO (Adults): 5 mg/day (2.5 mg/day in geriatric patients);

mayqq 2 wk (range 5–10 mg/day; not to exceed

10 mg/day).

Availability (generic available)

Extended-release tablets: 2.5 mg, 5 mg, 10 mg.