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AmLODIPine

Medically reviewed by Drugs.com. Last updated on Aug 11, 2020.

Pronunciation

(am LOE di peen)

Index Terms

  • Amlodipine Benzoate
  • Amlodipine Besylate

Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Suspension, Oral, as benzoate:

Katerzia: 1 mg/mL (150 mL) [contains polysorbate 80, sodium benzoate]

Tablet, Oral:

Norvasc: 10 mg

Generic: 10 mg

Tablet, Oral, as besylate:

Norvasc: 2.5 mg, 5 mg

Generic: 2.5 mg, 5 mg

Brand Names: U.S.

  • Katerzia
  • Norvasc

Pharmacologic Category

  • Antianginal Agent
  • Antihypertensive
  • Calcium Channel Blocker
  • Calcium Channel Blocker, Dihydropyridine

Pharmacology

Inhibits calcium ion from entering the “slow channels” or select voltage-sensitive areas of vascular smooth muscle and myocardium during depolarization, producing a relaxation of coronary vascular smooth muscle and coronary vasodilation; increases myocardial oxygen delivery in patients with vasospastic angina. Amlodipine directly acts on vascular smooth muscle to produce peripheral arterial vasodilation reducing peripheral vascular resistance and blood pressure.

Absorption

Well absorbed (Meredith 1992)

Distribution

Mean Vd:

Children >6 years: Similar to adults on a mg per kg basis; Note: Weight-adjusted Vd in younger children (<6 years of age) may be greater than in older children (Flynn 2006)

Adults: 21 L/kg (Scholz 1997)

Metabolism

Hepatic (~90%) to inactive metabolites

Excretion

Urine (10% of total dose as unchanged drug, 60% of total dose as metabolites)

Clearance: May be decreased in patients with hepatic insufficiency or moderate to severe heart failure; weight-adjusted clearance in children >6 years of age is similar to adults; Note: Weight-adjusted clearance in younger children (<6 years of age) may be greater than in older children (Flynn 2006)

Onset of Action

Antihypertensive effect: Significant reductions in blood pressure at 24 to 48 hours after first dose; slight increase in heart rate within 10 hours of administration may reflect some vasodilating activity (Donnelly 1993)

Time to Peak

Plasma: 6 to 12 hours

Duration of Action

Antihypertensive effect: At least 24 hours (Donnelly 1993); has been shown to extend to at least 72 hours when discontinued after 6 to 7 weeks of therapy (Biston 1999)

Half-Life Elimination

Terminal (biphasic): 30 to 50 hours; increased with hepatic dysfunction

Protein Binding

~93%

Special Populations: Hepatic Function Impairment

AUC may increase ~40% to 60%.

Special Populations: Elderly

AUC may increase ~40% to 60%.

Special Populations Note

Moderate to severe heart failure: AUC may increase ~40% to 60%.

Use: Labeled Indications

Angina: Treatment of symptomatic chronic stable angina; treatment of confirmed or suspected vasospastic angina (previously referred to as Prinzmetal or variant angina). May be used alone or in combination with other antianginal agents.

Hypertension: Management of hypertension in adults and children ≥6 years of age.

Off Label Uses

Raynaud phenomenon

Based on the European Society for Vascular Medicine guidelines for the diagnosis and management of Raynaud phenomenon, amlodipine is a reasonable alternative to nifedipine for the management of this condition.

Contraindications

Hypersensitivity to amlodipine or any component of the formulation.

Canadian labeling: Additional contraindications (not in the US labeling): Hypersensitivity to other dihydropyridines; severe hypotension (systolic BP <90 mm Hg); breastfeeding; shock (including cardiogenic shock); obstruction of the outflow tract of the left ventricle (eg, high-grade aortic stenosis); hemodynamically unstable heart failure after acute myocardial infarction; hereditary fructose intolerance (oral solution); hyperglycerolemia or glycerol kinase deficiency (oral solution).

Dosing: Adult

Angina:

Chronic stable angina (alternative agent):

Note: A beta-blocker is the preferred initial therapy; if there are ongoing symptoms on beta-blocker therapy, a long acting dihydropyridine calcium channel blocker (eg, amlodipine) may be added; amlodipine may also be used as an alternative therapy if there are contraindications or unacceptable adverse effects with beta-blockade (ACC/AHA [Fihn 2012]).

Oral: 5 to 10 mg once daily.

Vasospastic angina:

Note: May use alone or in combination with nitrates (ACC/AHA [Fihn 2012]).

Oral: 5 to 10 mg once daily.

Hypertension:

Note: For patients who warrant combination therapy (BP >20/10 mm Hg above goal or suboptimal response to monotherapy), may use with another appropriate agent (eg, angiotensin-converting enzyme [ACE] inhibitor, angiotensin II receptor blocker [ARB], or thiazide diuretic) (ACC/AHA [Whelton 2018]). For combination therapy, some experts recommend amlodipine plus either an ACE inhibitor or ARB (Jamerson 2008; Mann 2020).

Oral: Initial: 2.5 to 5 mg once daily; titrate every 1 to 2 weeks as needed based on patient response; maximum: 10 mg/day (ACC/AHA [Whelton 2018]; Jamerson 2008); antihypertensive effect attenuates with higher doses and adverse effects may become more prominent (Mann 2020).

Raynaud phenomenon (off-label use): Oral: 5 mg once daily; if needed, increase dose gradually based on patient response and tolerability, usually once every 4 weeks, but not more frequently than once every 7 to 10 days; monitor blood pressure closely with each dose increase; maximum dose: 20 mg/day (ESVM [Belch 2017]; Wigley 2020).

Dosing: Geriatric

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

Chronic stable angina (alternative agent); vasospastic angina: Oral: Initial: 5 mg once daily.

Hypertension: Oral: Initial: 2.5 mg once daily.

Dosing: Pediatric

Hypertension:

Children <6 years: Limited data available: Oral: Initial: 0.1 mg/kg/dose once daily; titrate based on clinical response; maximum daily dose: 0.6 mg/kg/day or 5 mg/day (AAP [Flynn 2017]).

Children ≥6 years and Adolescents: Oral: Initial: 2.5 mg once daily; titrate based on clinical response; maximum daily dose: 10 mg/day (AAP [Flynn 2017]).

Raynaud phenomenon, treatment: Very limited data available:

Children ≥6 years and Adolescents: Oral: Usual dosage range: 2.5 to 10 mg once daily; start dose low and increase as tolerated and based on symptom response (Gargh 2010; Kliegman 2020; Wigley 2015). Note: In addition to nonpharmacologic interventions (eg, cold avoidance), dihydropyridine calcium channel blockers are recommended for management; although nifedipine has the most data and is generally used first-line, amlodipine is an acceptable alternative (EULAR [Kowal-Bielecka 2017]; Kliegman 2020).

Extemporaneously Prepared

1 mg/mL Oral Suspension

Note: Commercial oral suspension available (1 mg/mL).

A 1 mg/mL oral suspension may be made with tablets and either a 1:1 mixture of simple syrup and 1% methylcellulose or a 1:1 mixture of Ora-Plus and Ora-Sweet. Crush fifty 5 mg tablets in a mortar and reduce to a fine powder. Add small portions of the chosen vehicle and mix to a uniform paste; mix while adding the vehicle in incremental proportions to almost 250 mL; transfer to a calibrated bottle, rinse mortar with vehicle, and add quantity of vehicle sufficient to make 250 mL. Label "shake well" and "refrigerate". Stable for 56 days at room temperature or 91 days refrigerated.

Nahata MC, Morosco RS, and Hipple TF. Stability of Amlodipine Besylate in Two Liquid Dosage Forms. J Am Pharm Assoc (Wash). 1999;39(3):375-377.10363465

Administration

Oral: Administer without regard to meals.

Storage

Suspension: Store at 2°C to 8°C (36°F to 46°F); avoid freezing and excessive heat. Protect from light.

Tablets: Store at 15°C to 30°C (59°F to 86°F).

Drug Interactions

Abametapir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Alfuzosin: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Alpha1-Blockers: May enhance the hypotensive effect of Calcium Channel Blockers. Monitor therapy

Amifostine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Amifostine. Management: When amifostine is used at chemotherapy doses, blood pressure lowering medications should be withheld for 24 hours prior to amifostine administration. If blood pressure lowering therapy cannot be withheld, amifostine should not be administered. Consider therapy modification

Amphetamines: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Antifungal Agents (Azole Derivatives, Systemic): May enhance the adverse/toxic effect of Calcium Channel Blockers. Specifically, itraconazole may enhance the negative inotropic effects of verapamil or diltiazem. Antifungal Agents (Azole Derivatives, Systemic) may decrease the metabolism of Calcium Channel Blockers. Fluconazole and isavuconazonium likely exert weaker effects than other azoles and are addressed in separate monographs. Management: Concurrent use of felodipine or nisoldipine with itraconazole is specifically contraindicated. Frequent monitoring is warranted with any such combination; calcium channel blocker dose reductions may be required. Exceptions: Fluconazole; Isavuconazonium Sulfate. Consider therapy modification

Antihepaciviral Combination Products: May increase the serum concentration of AmLODIPine. Management: Reduce amlodipine dose by at least 50% and monitor for increased amlodipine effects (eg, hypotension) if an antihepaciviral combination product is initiated. Consider therapy modification

Antipsychotic Agents (Second Generation [Atypical]): Blood Pressure Lowering Agents may enhance the hypotensive effect of Antipsychotic Agents (Second Generation [Atypical]). Monitor therapy

Aprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Atosiban: Calcium Channel Blockers may enhance the adverse/toxic effect of Atosiban. Specifically, there may be an increased risk for pulmonary edema and/or dyspnea. Monitor therapy

Barbiturates: May increase the metabolism of Calcium Channel Blockers. Management: Monitor for decreased therapeutic effects of calcium channel blockers with concomitant barbiturate therapy. Calcium channel blocker dose adjustments may be necessary. Nimodipine Canadian labeling contraindicates concomitant use with phenobarbital. Monitor therapy

Barbiturates: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Benperidol: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Brigatinib: May diminish the antihypertensive effect of Antihypertensive Agents. Brigatinib may enhance the bradycardic effect of Antihypertensive Agents. Monitor therapy

Brimonidine (Topical): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Bromperidol: May diminish the hypotensive effect of Blood Pressure Lowering Agents. Blood Pressure Lowering Agents may enhance the hypotensive effect of Bromperidol. Avoid combination

Calcium Channel Blockers (Nondihydropyridine): Calcium Channel Blockers (Dihydropyridine) may enhance the hypotensive effect of Calcium Channel Blockers (Nondihydropyridine). Calcium Channel Blockers (Nondihydropyridine) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

Calcium Salts: May diminish the therapeutic effect of Calcium Channel Blockers. Monitor therapy

CarBAMazepine: May increase the metabolism of Calcium Channel Blockers (Dihydropyridine). Management: Consider calcium channel blocker (CCB) dose adjustments or alternative therapy in patients receiving concomitant carbamazepine. Nimodipine Canadian labeling contraindicates concurrent use with carbamazepine. Consider therapy modification

Clofazimine: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Clopidogrel: Calcium Channel Blockers may diminish the therapeutic effect of Clopidogrel. Monitor therapy

Conivaptan: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

CycloSPORINE (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of CycloSPORINE (Systemic). CycloSPORINE (Systemic) may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

CYP3A4 Inducers (Moderate): May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

CYP3A4 Inducers (Strong): May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling. Consider therapy modification

CYP3A4 Inhibitors (Moderate): May increase the serum concentration of AmLODIPine. Monitor therapy

CYP3A4 Inhibitors (Strong): May increase the serum concentration of AmLODIPine. Monitor therapy

Dabrafenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects). Consider therapy modification

Dapoxetine: May enhance the orthostatic hypotensive effect of Calcium Channel Blockers. Monitor therapy

Deferasirox: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Dexmethylphenidate: May diminish the therapeutic effect of Antihypertensive Agents. Monitor therapy

Diazoxide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Dofetilide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Dofetilide. Monitor therapy

DULoxetine: Blood Pressure Lowering Agents may enhance the hypotensive effect of DULoxetine. Monitor therapy

Duvelisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Efavirenz: May decrease the serum concentration of Calcium Channel Blockers. Monitor therapy

Enzalutamide: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring. Consider therapy modification

Erdafitinib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Erdafitinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Flibanserin: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Flibanserin. Monitor therapy

Fluconazole: May increase the serum concentration of Calcium Channel Blockers. Monitor therapy

Fosaprepitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosnetupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Fosphenytoin: Calcium Channel Blockers may increase the serum concentration of Fosphenytoin. Calcium Channel Blockers may decrease the serum concentration of Fosphenytoin. Management: Monitor for phenytoin toxicity with concomitant use of a calcium channel blocker (CCB) or decreased phenytoin effects with CCB discontinuation. Monitor for decreased CCB therapeutic effects. Nimodipine Canadian labeling contraindicates use with phenytoin. Consider therapy modification

Fusidic Acid (Systemic): May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Herbs (Hypertensive Properties): May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Herbs (Hypotensive Properties): May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Hypotension-Associated Agents: Blood Pressure Lowering Agents may enhance the hypotensive effect of Hypotension-Associated Agents. Monitor therapy

Idelalisib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Avoid combination

Ivosidenib: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Larotrectinib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Lemborexant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lemborexant. Management: The maximum recommended dosage of lemborexant is 5 mg, no more than once per night, when coadministered with weak CYP3A4 inhibitors. Consider therapy modification

Levodopa-Containing Products: Blood Pressure Lowering Agents may enhance the hypotensive effect of Levodopa-Containing Products. Monitor therapy

Lomitapide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Lomitapide. Management: Patients on lomitapide 5 mg/day may continue that dose. Patients taking lomitapide 10 mg/day or more should decrease the lomitapide dose by half. The lomitapide dose may then be titrated up to a max adult dose of 30 mg/day. Consider therapy modification

Lormetazepam: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Lovastatin: AmLODIPine may increase the serum concentration of Lovastatin. Monitor therapy

Macrolide Antibiotics: May decrease the metabolism of Calcium Channel Blockers. Management: Consider using a noninteracting macrolide. Felodipine Canadian labeling specifically recommends avoiding its use in combination with clarithromycin. Exceptions: Azithromycin (Systemic); Fidaxomicin; Roxithromycin; Spiramycin. Consider therapy modification

Magnesium Salts: Calcium Channel Blockers may enhance the adverse/toxic effect of Magnesium Salts. Magnesium Salts may enhance the hypotensive effect of Calcium Channel Blockers. Monitor therapy

Melatonin: May diminish the antihypertensive effect of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

Methylphenidate: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

MiFEPRIStone: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus. Consider therapy modification

Mitotane: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane. Consider therapy modification

Molsidomine: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Naftopidil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Netupitant: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Neuromuscular-Blocking Agents (Nondepolarizing): Calcium Channel Blockers may enhance the neuromuscular-blocking effect of Neuromuscular-Blocking Agents (Nondepolarizing). Monitor therapy

Nicergoline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Nicorandil: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

NiMODipine: CYP3A4 Inhibitors (Weak) may increase the serum concentration of NiMODipine. Monitor therapy

Nitroprusside: Blood Pressure Lowering Agents may enhance the hypotensive effect of Nitroprusside. Monitor therapy

Obinutuzumab: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Management: Consider temporarily withholding blood pressure lowering medications beginning 12 hours prior to obinutuzumab infusion and continuing until 1 hour after the end of the infusion. Consider therapy modification

Palbociclib: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Pentoxifylline: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Phenytoin: Calcium Channel Blockers may increase the serum concentration of Phenytoin. Phenytoin may decrease the serum concentration of Calcium Channel Blockers. Management: Avoid use of nimodipine or nifedipine with phenytoin. Monitor for phenytoin toxicity and/or decreased calcium channel blocker effects with any concurrent use. Consider therapy modification

Pholcodine: Blood Pressure Lowering Agents may enhance the hypotensive effect of Pholcodine. Monitor therapy

Phosphodiesterase 5 Inhibitors: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Pimozide: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Pimozide. Avoid combination

Prostacyclin Analogues: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

Quinagolide: May enhance the hypotensive effect of Blood Pressure Lowering Agents. Monitor therapy

QuiNIDine: Calcium Channel Blockers (Dihydropyridine) may decrease the serum concentration of QuiNIDine. Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of QuiNIDine. QuiNIDine may increase the serum concentration of Calcium Channel Blockers (Dihydropyridine). Monitor therapy

Rifamycin Derivatives: May decrease the serum concentration of Calcium Channel Blockers. This primarily affects oral forms of calcium channel blockers. Management: The labeling for some US and Canadian calcium channel blockers contraindicate use with rifampin, however recommendations vary. Consult appropriate labeling. Consider therapy modification

Sarilumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Siltuximab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Simeprevir: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Monitor therapy

Simvastatin: AmLODIPine may increase the serum concentration of Simvastatin. Management: Dose of simvastatin should not exceed 20 mg daily if coadministering with levamlodipine or amlodipine. If coadministering with simvastatin and amlodipine, close laboratory and clincal monitoring for signs and symptoms of rhabdomyolysis is warranted. Consider therapy modification

Sincalide: Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction. Consider therapy modification

Stiripentol: May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring. Consider therapy modification

Tacrolimus (Systemic): Calcium Channel Blockers (Dihydropyridine) may increase the serum concentration of Tacrolimus (Systemic). Monitor therapy

Tocilizumab: May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Monitor therapy

Triazolam: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Triazolam. Management: Consider triazolam dose reduction in patients receiving concomitant weak CYP3A4 inhibitors. Consider therapy modification

Ubrogepant: CYP3A4 Inhibitors (Weak) may increase the serum concentration of Ubrogepant. Management: In patients taking weak CYP3A4 inhibitors, the initial and second dose (given at least 2 hours later if needed) of ubrogepant should be limited to 50 mg. Consider therapy modification

Yohimbine: May diminish the antihypertensive effect of Antihypertensive Agents. Monitor therapy

Test Interactions

May lead to false-negative aldosterone/renin ratio (ARR) (Funder 2016).

Adverse Reactions

>10%: Cardiovascular: Peripheral edema (2% to 11% [placebo: 0.6%], dose related; females: 15% [placebo: 5%]; males: 6% [placebo: 1%])

1% to 10%:

Cardiovascular: Flushing (≤3%, dose related, more frequent in females), palpitations (≤5%, dose related, more frequent in females)

Dermatologic: Pruritus (≤2%), skin rash (≤2%)

Gastrointestinal: Abdominal pain (2%), nausea (3%)

Nervous system: Dizziness (doses ≥5 mg/day: 3%), drowsiness (1% to 2%), fatigue (5%), male sexual disorder (≤2%)

Neuromuscular & skeletal: Asthenia (≤2%), muscle cramps (≤2%)

Respiratory: Dyspnea (≤2%)

<1%:

Cardiovascular: Peripheral ischemia, sinus tachycardia, syncope, vasculitis

Dermatologic: Diaphoresis, erythema multiforme

Endocrine & metabolic: Hot flash, hyperglycemia, weight gain, weight loss

Gastrointestinal: Anorexia, constipation, dysphagia, flatulence, gingival hyperplasia, pancreatitis, vomiting, xerostomia

Genitourinary: Difficulty in micturition, nocturia, urinary frequency

Hematologic & oncologic: Leukopenia, purpuric disease, thrombocytopenia (Cvetković 2013)

Hypersensitivity: Angioedema, hypersensitivity reaction

Nervous system: Abnormal dreams, anxiety, depersonalization, depression, female sexual disorder, hypoesthesia, insomnia, malaise, pain, paresthesia, peripheral neuropathy, rigors, vertigo

Neuromuscular & skeletal: Arthralgia, back pain, myalgia, osteoarthritis, tremor

Ophthalmic: Conjunctivitis, diplopia, eye pain

Otic: Tinnitus

Respiratory: Epistaxis

Postmarketing:

Dermatologic: Dermatologic disorder (Schamberg's disease) (Schetz 2015), toxic epidermal necrolysis (Baetz 2011)

Endocrine & metabolic: Gynecomastia (Cornes 2001)

Hepatic: Cholestatic hepatitis (Egbuonu 2019; Zinsser 2004), hepatotoxicity (Demirci 2013; Hammerstrom 2015), increased liver enzymes (Lafuente 2000; Zinsser 2004), jaundice (Lafuente 2000)

Renal: Acute interstitial nephritis (Ejaz 2000)

Warnings/Precautions

Concerns related to adverse effects:

• Angina/MI: Increased angina and/or MI have occurred with initiation or dosage titration of dihydropyridine calcium channel blockers. Reflex tachycardia may occur resulting in angina and/or MI in patients with obstructive coronary disease, especially in the absence of concurrent beta-blockade.

• Hypotension: Symptomatic hypotension can occur; acute hypotension upon initiation is unlikely due to the gradual onset of action. Blood pressure must be lowered at a rate appropriate for the patient's clinical condition.

• Peripheral edema: The most common side effect is peripheral edema; occurs within 2 to 3 weeks of starting therapy.

Disease-related concerns:

• Aortic stenosis: Use amlodipine with extreme caution in patients with severe aortic stenosis; may reduce coronary perfusion resulting in ischemia.

• Heart failure: With the exception of amlodipine, calcium channel blockers should be avoided whenever possible in patients with heart failure with reduced ejection fraction (HFrEF). Amlodipine may be used for the treatment of hypertension or ischemic heart disease in patients with HFrEF, but has no effect on functional status or mortality (ACCF/AHA [Yancy 2013]).

• Hepatic impairment: Use with caution in patients with hepatic impairment; may require lower starting dose; titrate slowly in patients with severe hepatic impairment.

• Hypertrophic cardiomyopathy (HCM) with outflow tract obstruction: Use amlodipine with caution in patients with HCM and outflow tract obstruction since reduction in afterload may worsen symptoms associated with this condition (ACCF/AHA [Gersh 2011]).

Dosage form specific issues:

• Benzyl alcohol and derivatives: Some dosage forms may contain sodium benzoate/benzoic acid; benzoic acid (benzoate) is a metabolite of benzyl alcohol; large amounts of benzyl alcohol (≥99 mg/kg/day) have been associated with a potentially fatal toxicity ("gasping syndrome") in neonates; the "gasping syndrome" consists of metabolic acidosis, respiratory distress, gasping respirations, CNS dysfunction (including convulsions, intracranial hemorrhage), hypotension, and cardiovascular collapse (AAP 1997; CDC 1982); some data suggests that benzoate displaces bilirubin from protein binding sites (Ahlfors 2001); avoid or use dosage forms containing benzyl alcohol derivative with caution in neonates. See manufacturer's labeling.

• Polysorbate 80: Some dosage forms may contain polysorbate 80 (also known as Tweens). Hypersensitivity reactions, usually a delayed reaction, have been reported following exposure to pharmaceutical products containing polysorbate 80 in certain individuals (Isaksson 2002; Lucente 2000; Shelley 1995). Thrombocytopenia, ascites, pulmonary deterioration, and renal and hepatic failure have been reported in premature neonates after receiving parenteral products containing polysorbate 80 (Alade 1986; CDC 1984). See manufacturer's labeling.

Special populations:

• Elderly: Initiate at a lower dose in the elderly.

Other warnings/precautions:

• Titration: Peak antihypertensive effect is delayed; dosage titration should occur after 7 to 14 days on a given dose.

Monitoring Parameters

Heart rate, BP.

Hypertension: The 2017 Guideline for the Prevention, Detection, Evaluation, and Management of High Blood Pressure in Adults (ACC/AHA [Whelton 2017]):

Confirmed hypertension and known cardiovascular disease or 10-year atherosclerotic cardiovascular disease (ASCVD) risk ≥10%: Target BP <130/80 mm Hg is recommended.

Confirmed hypertension without markers of increased ASCVD risk: Target BP <130/80 mm Hg may be reasonable.

Diabetes and hypertension: The American Diabetes Association (ADA) guidelines (ADA 2020):

Patients 18 to 65 years of age, without ASCVD, and 10-year ASCVD risk <15%: Target BP <140/90 mm Hg is recommended.

Patients 18 to 65 years of age and known ASCVD or 10-year ASCVD risk ≥15%: Target BP <130/80 mm Hg may be appropriate if it can be safely attained.

Patients >65 years of age (healthy or complex/intermediate health): Target BP <140/90 mm Hg is recommended.

Patients >65 years of age (very complex/poor health): Target BP <150/90 mm Hg is recommended.

Pregnancy Considerations

Amlodipine crosses the placenta. Cord blood concentrations were ~40% of maternal serum at delivery, and concentrations in the newborn were below the limit of quantification (<0.1 ng/mL) when measured in eight infants within 48 hours of delivery (Morgan 2017; Morgan 2018).

Due to pregnancy-induced pharmacologic changes, amlodipine pharmacokinetics may be altered immediately postpartum (Morgan 2018; Naito 2015b).

Chronic maternal hypertension may increase the risk of birth defects, low birth weight, preterm delivery, stillbirth, and neonatal death. Actual fetal/neonatal risks may be related to duration and severity of maternal hypertension. Untreated hypertension may also increase the risks of adverse maternal outcomes, including gestational diabetes, myocardial infarction, preeclampsia, stroke, and delivery complications (ACOG 203 2019).

Calcium channel blockers may be used to treat hypertension in pregnant women; however, agents other than amlodipine are more commonly used (ACOG 203 2019; ESC [Regitz-Zagrosek 2018]). Females with preexisting hypertension may continue their medication during pregnancy unless contraindications exist (ESC [Regitz-Zagrosek 2018]).

Patient Education

What is this drug used for?

• It is used to treat high blood pressure.

• It is used to treat some types of chest pain (angina).

• It may be given to you for other reasons. Talk with the doctor.

All drugs may cause side effects. However, many people have no side effects or only have minor side effects. Call your doctor or get medical help if any of these side effects or any other side effects bother you or do not go away:

• Fatigue

• Loss of strength and energy

• Flushing

• Nausea

• Abdominal pain

WARNING/CAUTION: Even though it may be rare, some people may have very bad and sometimes deadly side effects when taking a drug. Tell your doctor or get medical help right away if you have any of the following signs or symptoms that may be related to a very bad side effect:

• Liver problems like dark urine, fatigue, lack of appetite, nausea, abdominal pain, light-colored stools, vomiting, or yellow skin.

• Severe dizziness

• Passing out

• Chest pain

• Fast heartbeat

• Abnormal heartbeat

• Stiff muscles

• Tremors

• Abnormal movements

• Swelling of arms or legs

• Signs of an allergic reaction, like rash; hives; itching; red, swollen, blistered, or peeling skin with or without fever; wheezing; tightness in the chest or throat; trouble breathing, swallowing, or talking; unusual hoarseness; or swelling of the mouth, face, lips, tongue, or throat.

Note: This is not a comprehensive list of all side effects. Talk to your doctor if you have questions.

Consumer Information Use and Disclaimer: This information should not be used to decide whether or not to take this medicine or any other medicine. Only the healthcare provider has the knowledge and training to decide which medicines are right for a specific patient. This information does not endorse any medicine as safe, effective, or approved for treating any patient or health condition. This is only a limited summary of general information about the medicine's uses from the patient education leaflet and is not intended to be comprehensive. This limited summary does NOT include all information available about the possible uses, directions, warnings, precautions, interactions, adverse effects, or risks that may apply to this medicine. This information is not intended to provide medical advice, diagnosis or treatment and does not replace information you receive from the healthcare provider. For a more detailed summary of information about the risks and benefits of using this medicine, please speak with your healthcare provider and review the entire patient education leaflet.

Further information

Always consult your healthcare provider to ensure the information displayed on this page applies to your personal circumstances.

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