amlodipine

am-LOE-di-peen

Therapeutic Classification: antianginals, antihypertensives

Pharmacologic Classification: calcium channel blockers

REMS

Hypertension (as monotherapy or in combination with other antihypertensive agents).
Chronic stable angina (as monotherapy or in combination with other antianginal agents).
Vasospastic (Prinzmetal's) angina (as monotherapy or in combination with other antianginal agents).
Recently documented coronary artery disease by angiography and without HF or an ejection fraction <40%.

Inhibits the transport of calcium into myocardial and vascular smooth muscle cells, resulting in inhibition of excitation-contraction coupling and subsequent contraction.

Therapeutic effects:

Reduction in BP.
Decreased frequency and severity of attacks of angina.
Reduction in risk of hospitalization for angina or coronary revascularization in patients with recently documented coronary artery disease.

Absorption: Well absorbed after oral administration (64–90%).

Distribution: Probably crosses the placenta.

Protein Binding: 95–98%.

Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A4 isoenzyme.

Half-Life: 30–50 hr (↑ in geriatric patients and patients with hepatic impairment).

(cardiovascular effects)

ROUTE	ONSET	PEAK	DURATION
PO	unknown	6–9 hr	24 hr

Contraindicated in:

Hypersensitivity;
Systolic BP <90 mm Hg.

Use Cautiously in:

Severe hepatic impairment (dose ↓ recommended);
Aortic stenosis;
History of HF;
OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk; other calcium channel blockers preferred in pregnancy;
Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant;
Pedi: Children 6 yr (safety and effectiveness not established);
Geri: risk of hypotension in older adults (dose recommended).

CV: peripheral edema, angina, bradycardia, hypotension, palpitations

Derm: flushing

GI: gingival hyperplasia, nausea

Neuro: dizziness, fatigue

Drug-drug:

Strong CYP3A4 inhibitors, including ketoconazole, itraconazole, clarithromycin, and ritonavir may ↑ levels.
Additive hypotension may occur when used concurrently with fentanyl, other antihypertensives, nitrates, acute ingestion of alcohol, or quinidine.
Antihypertensive effects may be ↓ by concurrent use of NSAIDs.
May ↑ risk of neurotoxicity with lithium.
↑risk of myopathy with simvastatin (do not exceed 20 mg/day of simvastatin).
May ↑ cyclosporine and tacrolimus levels

PO (Adults ): 5–10 mg once daily
PO Geriatric Patients ): Antihypertensive: Initiate therapy at 2.5 mg/day, ↑ as required/tolerated (up to 10 mg/day); Antianginal: initiate therapy at 5 mg/day, ↑ as required/tolerated (up to 10 mg/day).
PO (Children >6 yr): 2.5–5 mg once daily.

Hepatic Impairment

PO (Adults ): Antihypertensive: Initiate therapy at 2.5 mg/day, ↑ as required/tolerated (up to 10 mg/day); Antianginal: initiate therapy at 5 mg/day, ↑ as required/tolerated (up to 10 mg/day).

(Generic available)

Tablets: 2.5 mg; 5 mg; 10 mg
Oral solution (Norliqva)peppermint flavor: 1 mg/mL
Oral suspension (Katerzia): 1 mg/mL
In combination with: atorvastatin (Caduet), benazepril (Lotrel), olmesartan (Azor), olmesartan/hydrochlorothiazide (Tribenzor), telmisartan, valsartan (Exforge), and valsartan/hydrochlorothiazide (Exforge HCT). See Appendix [not included in this PDA edition].

Monitor BP and pulse before therapy, during dose titration, and periodically during therapy. Monitor ECG periodically during prolonged therapy.
- Monitor intake and output ratios and daily weight. Assess for signs of HF (peripheral edema, rales/crackles, dyspnea, weight gain, jugular venous distention).
Monitor frequency of prescription refills to determine adherence.
Angina: Assess location, duration, intensity, and precipitating factors of patient’s anginal pain.

Lab Test Considerations:

Total serum calcium concentrations are not affected by calcium channel blockers.

Do not confuse amlodipine with amiloride.
PO: May be administered without regard to meals.
- Norliqva is a pale straw colored solution. Katerzia is a white to off-white liquid suspension. Shake before using.

Advise patient to take medication as directed, even if feeling well. Take missed doses as soon as possible within 12 hrs of missed dose. If >12 hrs since missed dose, skip dose and take next dose at scheduled time; do not double doses. May need to be discontinued gradually.
- Caution patient to change positions slowly to minimize orthostatic hypotension.
- May cause drowsiness or dizziness. Advise patient to avoid driving or other activities requiring alertness until response to the medication is known.
- Instruct patient on importance of maintaining good dental hygiene and seeing dentist frequently for teeth cleaning to prevent tenderness, bleeding, and gingival hyperplasia (gum enlargement).
- Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken, to avoid alcohol, and to consult health care professional before taking any new medications, especially cold preparations.
- Advise patient to notify health care professional if irregular heartbeats, dyspnea, swelling of hands and feet, pronounced dizziness, nausea, constipation, or hypotension occurs or if headache is severe or persistent.
- Advise patient to inform health care professional of medication regimen before treatment or surgery.
- Advise females of reproductive potential to notify health care professional if pregnancy is planned or suspected or if breastfeeding.
Angina: Instruct patient on concurrent nitrate or beta-blocker therapy to continue taking both medications as directed and to use SL nitroglycerin as needed for anginal attacks.
- Advise patient to contact health care professional if chest pain does not improve or worsens after therapy, if it occurs with diaphoresis, if shortness of breath occurs, or if severe, persistent headache occurs.
- Caution patient to discuss exercise restrictions with health care professional before exertion.
Hypertension: Encourage patient to comply with other interventions for hypertension (weight reduction, low-sodium diet, smoking cessation, moderation of alcohol consumption, regular exercise, and stress management). Medication controls but does not cure hypertension.
- Instruct patient and family in proper technique for monitoring BP. Advise patient to take BP weekly and to report significant changes to health care professional.

Decrease in BP.
Decrease in frequency and severity of anginal attacks.
- Decrease in need for nitrate therapy.
- Increase in activity tolerance and sense of well-being.
- Reduction in risk of hospitalization for angina or coronary revascularization in patients with recently documented coronary artery disease.

Katerzia, Norliqva, Norvasc

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Pronunciation ⬇

Classifications ⬆ ⬇

Indications ⬆ ⬇

Action ⬆ ⬇

Pharmacokinetics ⬆ ⬇

Time/Action Profile ⬆ ⬇

Contraind./Precautions ⬆ ⬇

Adv. Reactions/Side Effects ⬆ ⬇

Interactions ⬆ ⬇

Route/Dosage ⬆ ⬇

Availability ⬆ ⬇

Assessment ⬆ ⬇

Implementation ⬆ ⬇

Patient/Family Teaching ⬆ ⬇

Evaluation/Desired Outcomes ⬆ ⬇

US Brand Names ⬆ ⬇

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