Pronunciation:

(am LOE di peen)

U.S. Brand Names:

Synonyms:

Generic Available:

Canadian Brand Names:

Use:

Pregnancy Risk Factor:

Pregnancy Implications:

Lactation:

Contraindications:

Warnings/Precautions:

Adverse Reactions:

>10%: Cardiovascular: Peripheral edema (2% to 15% dose related)

1% to 10%:

Cardiovascular: Flushing (1% to 3%), palpitation (1% to 4%)

Central nervous system: Headache (7%; similar to placebo 8%), dizziness (1% to 3%), fatigue (4%), somnolence (1% to 2%)

Dermatologic: Rash (1% to 2%), pruritus (1% to 2%)

Endocrine & metabolic: Male sexual dysfunction (1% to 2%)

Gastrointestinal: Nausea (3%), abdominal pain (1% to 2%), dyspepsia (1% to 2%), gingival hyperplasia

Neuromuscular & skeletal: Muscle cramps (1% to 2%), weakness (1% to 2%)

Respiratory: Dyspnea (1% to 2%), pulmonary edema (15% from PRAISE trial, CHF population)

<1%: Abnormal dreams, abnormal vision, allergic reactions, angioedema, anorexia, anxiety, arrhythmia, arthrosis, back pain, bradycardia, chest pain, conjunctivitis, constipation, depersonalization, depression, diaphoresis increased, diarrhea, diplopia, dysphagia, epistaxis, erythema multiforme, eye pain, female sexual dysfunction, flatulence, hot flushes, hyperglycemia, hypoesthesia, hypotension, insomnia, joint stiffness, leukopenia, malaise, micturition disorder, micturition frequency, myalgia, nervousness, nocturia, pain, pancreatitis, paresthesia, peripheral ischemia, peripheral neuropathy, postural dizziness, postural hypotension, purpura, rash erythematous, rash maculopapular, rigors, syncope, tachycardia, thirst, thrombocytopenia, tinnitus, tremor, vasculitis, vertigo, vomiting, weight gain/loss, xerostomia

<0.1%: Abnormal visual accommodation, agitation, alopecia, amnesia, apathy, appetite increased, ataxia, cardiac failure, cold and clammy skin, cough, dermatitis, dysuria, extrasystoles, gastritis, hypertonia, loose stools, migraine, muscle weakness, parosmia, polyuria, pulse irregularity, rhinitis, skin discoloration, skin dryness, taste perversion, twitching, urticaria, xerophthalmia

Postmarketing and/or case reports: Dysosmia, EPS, erythema multiforme, exfoliative dermatitis, gynecomastia, jaundice, leukocytoclastic vasculitis, nonthrombocytopenic purpura, phototoxicity, Stevens-Johnson syndrome

Overdosage/Toxicology:

Drug Interactions:

Azole antifungals may inhibit calcium channel blocker metabolism; avoid this combination. Try an antifungal like terbinafine (if appropriate) or monitor closely for altered effect of the calcium channel blocker.

Calcium may reduce the calcium channel blocker's effects, particularly hypotension.

CYP1A2 substrates: Amlodipine may increase the levels/effects of CYP1A2 substrates. Example substrates include aminophylline, fluvoxamine, mexiletine, mirtazapine, ropinirole, theophylline, and trifluoperazine.

CYP3A4 inducers: CYP3A4 inducers may decrease the levels/effects of amlodipine. Example inducers include aminoglutethimide, carbamazepine, nafcillin, nevirapine, phenobarbital, phenytoin, and rifamycins.

CYP3A4 inhibitors: May increase the levels/effects of amlodipine. Example inhibitors include azole antifungals, ciprofloxacin, clarithromycin, diclofenac, doxycycline, erythromycin, imatinib, isoniazid, nefazodone, nicardipine, propofol, protease inhibitors, quinidine, and verapamil.

Grapefruit juice: May modestly increase amlodipine levels.

Rifampin increases the metabolism of calcium channel blockers; adjust the dose of calcium channel blocker to maintain efficacy.

Sildenafil, tadalafil, vardenafil: Blood pressure-lowering effects are additive; use caution.

Ethanol/Nutrition/Herb Interactions:

Food: Grapefruit juice may modestly increase amlodipine levels.

Herb/Nutraceutical: St John's wort may decrease amlodipine levels. Avoid dong quai if using for hypertension (has estrogenic activity). Avoid ephedra, yohimbe, ginseng (may worsen hypertension). Avoid garlic (may have increased antihypertensive effects).

Stability:

Mechanism of Action:

Pharmacodynamics/Kinetics:

Onset of action: 30-50 minutes

Peak effect: 6-12 hours

Duration: 24 hours

Absorption: Oral: Well absorbed

Protein binding: 93%

Metabolism: Hepatic (>90%) to inactive metabolite

Bioavailability: 64% to 90%

Half-life elimination: 30-50 hours

Excretion: Urine

Dosage:

Children 6-17 years: Hypertension: 2.5-5 mg once daily

Adults:

Hypertension: Initial dose: 5 mg once daily; maximum dose: 10 mg once daily. In general, titrate in 2.5 mg increments over 7-14 days. Usual dosage range (JNC 7): 2.5-10 mg once daily.

Angina: Usual dose: 5-10 mg

Elderly: Dosing should start at the lower end of dosing range due to possible increased incidence of hepatic, renal, or cardiac impairment. Elderly patients also show decreased clearance of amlodipine.

Hypertension: 2.5 mg once daily

Angina: 5 mg once daily

Dialysis: Hemodialysis and peritoneal dialysis does not enhance elimination. Supplemental dose is not necessary.

Dosage adjustment in hepatic impairment:

Angina: Administer 5 mg once daily.

Hypertension: Administer 2.5 mg once daily.

Administration:

Dietary Considerations:

Patient Education:

Anesthesia and Critical Care Concerns/Other Considerations:

Cardiovascular Considerations:

In the treatment of unstable angina/non-ST-segment elevation MI, a nondihydropyridine calcium antagonist (diltiazem or verapamil) may be considered in patients with continuing or frequently recurring ischemia when beta-blockers are contraindicated (Class I). Oral long acting calcium antagonists may also be considered in addition to beta-blockers and nitrates (Class IIa).

Dental Health: Effects on Dental Treatment:

Dental Health: Vasoconstrictor/Local Anesthetic Precautions:

Mental Health: Effects on Mental Status:

Mental Health: Effects on Psychiatric Treatment:

Dosage Forms:

Extemporaneously Prepared:

Nahata MC, Morosco RS, and Hipple TF, 4th ed, Pediatric Drug Formulations, Cincinnati, OH: Harvey Whitney Books Co, 2000.

International Brand Names: