Class: Calcium channel blocking agent
- Tablets 2.5 mg
- Tablets 5 mg
- Tablets 10 mg
Inhibits movement of calcium ions across cell membrane in systemic and coronary vascular smooth muscle.
T max is 6 to 12 h. Bioavailability is 64% to 90%. Steady state is reached after 7 to 8 days of consecutive daily dosing.
About 93% is protein bound.
About 90% is converted to inactive metabolites in the liver.
10% of the parent compound and 60% of the metabolites are excreted in the urine. Elimination is biphasic. Half-life is about 30 to 50 h.
Special PopulationsRenal Function Impairment
Pharmacokinetics not significantly influenced.Hepatic Function Impairment
Cl is decreased and AUC may increase about 40% to 60%.Elderly
Cl is decreased and AUC may increase about 40% to 60%.Moderate to severe heart failure
Cl is decreased and AUC may increase about 40% to 60%.
Indications and Usage
Treatment of hypertension; treatment of chronic stable angina; or vasospastic (Prinzmetal or variant) angina; reduction of the risk of hospitalization caused by angina; reduction of the risk of coronary revascularization procedure in patients with recently documented coronary artery disease (CAD).
Dosage and AdministrationHypertension
PO Initial dose is 5 mg daily (max, 10 mg daily). 2.5 mg daily when adding amlodipine to other antihypertensive therapy.Children 6 to 17 years of age
PO 2.5 to 5 mg once daily.CAD
PO 5 to 10 mg once daily.Chronic stable or vasospastic angina
PO 5 to 10 mg once daily.Elderly
PO Start with 5 mg once daily.Hepatic Impairment
PO Initially 2.5 mg every day.Chronic stable or vasospastic angina
PO Start with 5 mg once daily.Elderly
PO Initially 2.5 mg every day.
- Adjust dose as needed; titration should proceed over 7 to 14 days.
- Administer without regard to meals.
Store at 59° to 86°F.
Drug InteractionsAzole antifungals (eg, ketoconazole)
Concurrent use may increase the plasma concentrations of amlodipine.Protease inhibitors (eg, ritonavir)
Pharmacologic effects of amlodipine may be increased.Vasopressin receptor antagonists (conivaptan)
Plasma concentrations of amlodipine may be increased.
Laboratory Test Interactions
None well documented.
Flushing, palpitations (5%).
Headache (7%); fatigue (5%); dizziness (3%); somnolence (2%).
Nausea (3%); abdominal pain (2%).
Hepatic enzyme elevations, jaundice (postmaketing).
Edema (15%); gynecomastia (postmarketing).
Category C .
Safety and efficacy not established in children younger than 6 yr of age.
May require lower initial dose.
Use with caution in patients with severe hepatic impairment.
Use with caution in patients with severe aortic stenosis or CHF.
May occur when starting therapy or at the time of dosage increase.
Abrupt withdrawal may cause increased frequency and duration of chest pain. Gradually taper dose if amlodipine is to be discontinued.
Hypotension, peripheral vasodilation, reflex tachycardia.
- Teach patient how to monitor pulse before taking medication. Tell patient not to take medication if pulse is less than 50 bpm and to contact health care provider.
- Explain to patient how to monitor BP daily.
- Instruct patient not to stop taking this medication suddenly because doing so can cause chest pain and MI.
- Inform patient that frequent follow-up appointments with health care provider are important to adjust medication dosage.
- Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
- Instruct patient to take with or without food.
- Advise breast-feeding woman not to breast-feed.
- Advise patient that drug may cause drowsiness, and to use caution while driving or performing other tasks requiring mental alertness.
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