Amlodipine is a medicine for high blood pressure and for angina (chest pain). It relaxes and widens the blood vessels, making it easier for blood to flow. The most common side effect is swelling of the ankles.
Also known as: Norvasc
No clinically relevant adverse interaction. An ACE inhibitor plus a calcium-channel blocker is a first-line antihypertensive combination; additive hypotension is expected and only requires BP monitoring during titration. Not contraindicated.
An angiotensin-converting enzyme inhibitor (captopril) combined with a calcium-channel blocker (amlodipine) is a first-line combination in the treatment of hypertension, with complementary and synergistic antihypertensive effects. There is no clinically relevant adverse interaction; the only expected effect is additive hypotension, desirable in uncontrolled hypertension, which only requires blood pressure monitoring during titration. In elderly patients or those with orthostatic hypotension, start with low doses and titrate gradually.
No clinically relevant adverse interaction. First-line antihypertensive combination; monitor blood pressure during titration.
Usual and recommended combination. Start at low doses and titrate gradually; monitor blood pressure in the early weeks.
DailyMed/FDA (NIH/NLM) — approved Captopril label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a43a5373-ded9-4912-8c98-edaec8352836 ; approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=58a67272-c4c7-4e2c-85a5-9d39034d12c3
No clinically relevant adverse interaction. An ACE inhibitor plus a calcium-channel blocker is a first-line antihypertensive combination; additive hypotension is expected and only requires BP monitoring during titration. Not contraindicated.
Enalapril (ACE inhibitor) and amlodipine (calcium-channel blocker) are frequently combined in the treatment of hypertension and coronary disease, with complementary effects: the ACE inhibitor blocks the renin-angiotensin system and amlodipine relaxes vascular smooth muscle. There is no relevant adverse interaction; the additive hypotensive effect is the intended therapeutic mechanism and only requires blood pressure monitoring, especially at start and at dose adjustments. In patients with amlodipine-induced peripheral oedema, the ACE inhibitor may even attenuate it.
No clinically relevant adverse interaction. First-line antihypertensive combination; monitor blood pressure during titration.
Usual and recommended combination. Start at low doses and titrate gradually; monitor blood pressure in the early weeks.
DailyMed/FDA (NIH/NLM) — approved Enalapril label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=b31372f7-cda3-4ead-a481-4cde62e843fd ; approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=58a67272-c4c7-4e2c-85a5-9d39034d12c3
Itraconazole raises Amlodipine levels (CYP3A4 inhibition), with a risk of hypotension and oedema.
Amlodipine is metabolised by CYP3A4 and the label states that "co-administration with CYP3A inhibitors (moderate and strong) results in increased systemic exposure to amlodipine and may require dose reduction" (for example, with diltiazem — a moderate inhibitor — exposure increased by 60%). Itraconazole is a potent CYP3A4 inhibitor, so the combination raises amlodipine levels and its dose-dependent effects: hypotension, peripheral oedema, flushing, headache and dizziness, especially in the elderly. Monitor blood pressure and signs of relative overdose; if the combination is needed, consider starting with a lower amlodipine dose or reducing it, monitoring the patient in the first weeks.
Itraconazole + amlodipine: itraconazole inhibits CYP3A4 and raises amlodipine levels. Watch for hypotension, oedema and dizziness; consider a dose reduction.
CYP3A4 inhibition by itraconazole reduces amlodipine metabolism.
Blood pressure, peripheral oedema.
Symptomatic hypotension, significant oedema.
Monitor blood pressure and oedema; consider a reduced amlodipine dose.
DailyMed/FDA (NIH/NLM) — approved Itraconazole label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=a4d555fa-787c-40fb-bb7d-b0d4f7318fd0 ; approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=58a67272-c4c7-4e2c-85a5-9d39034d12c3 — with additional reference: Prontuário Terapêutico do INFARMED, INFARMED (11th ed., 2012)
Voriconazole raises Amlodipine levels (CYP3A4 inhibition), with a risk of hypotension and oedema.
Amlodipine is metabolised by CYP3A4 and the label states that "co-administration with CYP3A inhibitors (moderate and strong) results in increased systemic exposure to amlodipine and may require dose reduction" (with diltiazem, a moderate inhibitor, exposure increased by 60%). Voriconazole is a strong CYP3A4 inhibitor, so the combination raises amlodipine levels and its dose-dependent effects: hypotension, peripheral oedema, flushing, headache and dizziness, especially in the elderly. Monitor blood pressure and signs of relative overdose; if the combination is needed, consider starting with a lower amlodipine dose or reducing it, monitoring the patient in the first weeks.
Amlodipine + voriconazole: voriconazole inhibits CYP3A4 and raises amlodipine levels. Watch hypotension and oedema; consider a dose reduction.
CYP3A4 inhibition by voriconazole reduces amlodipine metabolism.
Blood pressure, peripheral oedema.
Symptomatic hypotension, significant oedema.
Monitor blood pressure and oedema; consider a reduced amlodipine dose.
DailyMed/FDA (NIH/NLM) — approved Voriconazole label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f6a1a792-141b-42e8-8bd1-884e4408eb8a ; approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=58a67272-c4c7-4e2c-85a5-9d39034d12c3 — with additional reference: Prontuário Terapêutico do INFARMED, INFARMED (11th ed., 2012)
Ketoconazole raises Amlodipine levels (CYP3A4 inhibition), with a risk of hypotension and oedema.
Amlodipine is a CYP3A4 substrate, and ketoconazole, by inhibiting this enzyme, can raise its concentrations and potentiate the vasodilator effects (hypotension, peripheral oedema, flushing, headache). In most patients the interaction is managed by monitoring blood pressure and signs of oedema; if symptoms arise, consider reducing the amlodipine dose or using an antihypertensive less dependent on CYP3A4 during the antifungal.
Amlodipine + ketoconazole: CYP3A4 inhibition raising amlodipine levels. Monitor hypotension and oedema.
CYP3A4 inhibition by ketoconazole reduces first-pass amlodipine metabolism.
Blood pressure, peripheral oedema, headache, flushing.
Symptomatic hypotension, significant oedema.
Monitor blood pressure and oedema; consider reducing the amlodipine dose if adverse effects occur.
DailyMed/FDA (NIH/NLM) — approved Ketoconazole label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=f162e616-21b4-49b1-b437-15e21001a6f0 ; approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=58a67272-c4c7-4e2c-85a5-9d39034d12c3 — with additional reference: Prontuário Terapêutico do INFARMED, INFARMED (11th ed., 2012)
Grapefruit juice inhibits CYP3A4, raising amlodipine concentrations and the risk of hypotension and oedema.
Avoid grapefruit juice; may be taken with or without food.
DailyMed/FDA (NIH/NLM) — approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=edf9b22c-e37e-4b4e-8a64-20bb036c7d2d
Amlodipine can be administered with or without food, with no relevant change in absorption.
Take at the same time every day, with or without food.
DailyMed/FDA (NIH/NLM) — approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=edf9b22c-e37e-4b4e-8a64-20bb036c7d2d
Amlodipine is extensively metabolised in the liver; severe hepatic impairment increases the half-life and the risk of adverse effects.
Start with lower doses and titrate slowly in patients with hepatic impairment.
DailyMed/FDA (NIH/NLM) — approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=edf9b22c-e37e-4b4e-8a64-20bb036c7d2d
Amlodipine-induced vasodilation can cause significant hypotension in patients with severe aortic stenosis.
Use with caution and monitor blood pressure.
DailyMed/FDA (NIH/NLM) — approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=edf9b22c-e37e-4b4e-8a64-20bb036c7d2d
Data on amlodipine in pregnancy are limited; calcium channel blockers are used in gestational hypertension when needed.
Use only if the benefit outweighs the risk; nifedipine is preferred in some obstetric situations.
Present in breast milk in small amounts; generally considered compatible.
No specific contraception required.
DailyMed/FDA (NIH/NLM) — approved Amlodipine label: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=edf9b22c-e37e-4b4e-8a64-20bb036c7d2d
Clinical and educational support tool. The information does not replace a medical prescription or the opinion of a qualified healthcare professional.
Antihypertensive and antianginal agent. The maximum antihypertensive effect develops gradually and steady state is reached after 7 to 8 days of daily dosing. In hypertensive patients it is about 93% bound to plasma proteins.
Dihydropyridine calcium channel blocker: inhibits the transmembrane influx of calcium ions into vascular smooth muscle and cardiac muscle, producing peripheral arterial vasodilatation and reduced systemic vascular resistance.
After oral administration, peak plasma concentrations occur between 6 and 12 hours. Absolute bioavailability is 64 to 90% and is not altered by food.
Extensively (about 90%) converted to inactive metabolites via hepatic metabolism; 10% of the parent compound and 60% of the metabolites are excreted in the urine.
Plasma elimination is biphasic, with a terminal half-life of about 30 to 50 hours (approximately 56 hours in patients with severe hepatic impairment).
