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AMLODIPINE
AMLODIPINE
AMLODIPINE
(am-lo'di-peen)
Norvasc
Classifications: CARDIOVASCULAR AGENT; CALCIUM CHANNEL BLOCKER;
ANTIHYPERTENSIVE AGENT
Prototype: Nifedipine
Pregnancy Category: C
Availability
2.5 mg, 5 mg, 10 mg tablets
Actions
Amlodipine is a calcium channel blocking agent that selectively blocks calcium ion
reflux across cell membranes of cardiac and vascular smooth muscle without changing
serum calcium concentrations. It predominantly acts on the peripheral circulation,
decreasing peripheral vascular resistance, and increases cardiac output.
Therapeutic Effects
Amlodipine reduces systolic, diastolic, and mean arterial blood pressure.
Uses
Treatment of mild to moderate hypertension and angina.
Contraindications
Hypersensitivity to amlodipine; pregnancy (category C).
Cautious Use
Liver disease; concomitant use with hypotension; CHF; lactation; older adults.
Hypertension
Adult: PO 5–10 mg once daily
Geriatric: Start with 2.5 mg, adjust dose at intervals of not less than 2 wk
Hepatic Impairment
Start with 2.5 mg, adjust dose at intervals of not less than 2 wk
Administration
Oral
Give drug without regard to meals.
Prescribed initial dosages of 2.5 mg daily are common if added to a regimen
including other antihypertensive drugs.
Note: Doses are usually titrated over a period of 14 d or more rapidly if
warranted.
Store at 15°–30° C (59°–86° F).
Interactions
Drug: Adenosine may increase the risk of bradycardia; bosentan may decrease efficacy
of amlodipine; additive hypotensive effects with other ANTIHYPERTENSIVE AGENTS;
AZOLE ANTIFUNGALS (e.g., fluconazole, itraconazole) may inhibit metabolism of
amlodipine; itraconazole may increase edema. Food: Grapefruit juice may increase
amlodipine levels. Herbal: Ephedra, Ma Huang, melatonin may antagonize
antihypertensive effects.
Pharmacokinetics
Absorption: >90% absorbed from GI tract. Onset: Gradual. Peak: 6–9 h. Duration: 24
h. Distribution: >95% protein bound. Metabolism: Extensively metabolized in the liver
to inactive metabolites. Elimination: Inactive metabolites primarily excreted in urine
(<5%–10% excreted unchanged), 20%–25% excreted in feces. Half-Life: <45 y: 28–69 h;
>60 y: 40–120 h.
NURSING IMPLICATIONS
Assessment & Drug Effects
Common adverse effects in italic, life-threatening effects underlined: generic names in bold; classifications
in SMALL CAPS; Canadian drug name; Prototype drug