Amlodipine
Regulatory sources consulted
- openfda-label-cc27c9a5-dd2e-4a79-af00-28f51408362a
- aemps-cima-ft-65461
- ansm-bdpm-rcp-69930924
- PubMed PMID:36346411 ↗
- PubMed PMID:37551050 ↗
- PubMed PMID:37432701 ↗
- PubMed PMID:40434761 ↗
- Clinical Pharmacist Professional Knowledge
- OpenFDA · C08CA01
- RxNorm rxcui 17767 ↗
Approved indications
- Hypertension, to lower blood pressure. Lowering blood pressure reduces the risk of fatal and nonfatal cardiovascular events, primarily strokes and myocardial infarctions.
- Coronary Artery Disease: Chronic Stable Angina, Vasospastic Angina (Prinzmetal's or Variant Angina), and angiographically documented Coronary Artery Disease in patients without heart failure or an ejection fraction < 40%.
Contraindications
Absolute
- Known sensitivity to amlodipine or other dihydropyridine derivatives.
- Severe hypotension.
- Shock (including cardiogenic shock).
- Obstruction of the left ventricular outflow tract (e.g., high-grade aortic stenosis).
- Hemodynamically unstable heart failure after acute myocardial infarction.
Clinical warnings
- The safety and effectiveness of amlodipine in hypertensive crisis have not been established. — ANSM
Drug interactions
- ModerateSimvastatinC10AA01
Mechanism: Amlodipine increases systemic exposure to simvastatin (77% increase in AUC with 10 mg amlodipine and 80 mg simvastatin).
Recommendation: Limit the dose of simvastatin to 20 mg daily in patients on amlodipine.
OpenFDA label
- ModerateCYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, clarithromycin)
Mechanism: Co-administration with strong or moderate CYP3A4 inhibitors increases systemic exposure to amlodipine.
Recommendation: Monitor for symptoms of hypotension and edema. Amlodipine dose reduction may be required.
OpenFDA labelANSM RCP
- HighCyclosporineL04AD01
Mechanism: Amlodipine may increase the systemic exposure of cyclosporine.
Recommendation: Frequent monitoring of trough blood levels of cyclosporine is recommended and adjust the dose when appropriate.
OpenFDA label
- HighTacrolimusL04AD02
Mechanism: Amlodipine may increase the systemic exposure of tacrolimus.
Recommendation: Frequent monitoring of trough blood levels of tacrolimus is recommended and adjust the dose when appropriate to avoid toxicity.
OpenFDA label
Adverse events
Common (≥1%)
edema · dizziness · flushing · palpitations · fatigue · nausea · abdominal pain · somnolence
Rare but serious
angioedema · myocardial infarction · hypotension · hepatitis · jaundice
Pregnancy and lactation
FDA category: C (Legacy)
The limited available data based on post-marketing reports with amlodipine use in pregnant women are not sufficient to inform a drug-associated risk for major birth defects and miscarriage. There are risks to the mother and fetus associated with poorly controlled hypertension in pregnancy.
Recent literature (PubMed)
Revisión exhaustiva sobre el tratamiento de la hipertensión que posiciona a los bloqueantes de los canales de calcio como amlodipino como terapia farmacológica de primera línea, junto con diuréticos tiazídicos y bloqueadores del sistema renina-angiotensina.
Revisión actualizada que destaca las características únicas de amlodipino, como su larga vida media que permite un control sostenido de la PA incluso con dosis omitidas. Confirma su eficacia y seguridad en diversas poblaciones, incluyendo ancianos y pacientes con diabetes o ERC.
Metaanálisis en red que demuestra la superioridad de las combinaciones en un solo comprimido (SPC) sobre la monoterapia. Las combinaciones de ARA/BCC (como irbesartán/amlodipino o valsartán/amlodipino) mostraron ventajas significativas en la reducción de la presión arterial.
Ensayo clínico de fase 2 que evalúa zilebesiran como terapia añadida a antihipertensivos estándar, incluyendo un brazo con amlodipino. Los resultados muestran una reducción adicional significativa de la PA al añadir zilebesiran a amlodipino, reforzando el rol de amlodipino como terapia de base.