The key difference between amlodipine and lercanidipine is that amlodipine has a lower tolerability in managing hypertension, while lercanidipine has a better tolerability with a lower incidence of side effect profiles in managing hypertension.
Hypertension, also known as high blood pressure, significantly contributes to the global disease burden. It encompasses all age categories and can remain asymptomatic. It is a well-established risk factor for cardiovascular disease and can commonly coexist with other risk factors like smoking, obesity, physical inactivity, and diabetes. Antihypertensive drugs such as amlodipine and lercanidipine belong to the dihydropyridine class and are well-known to prevent cardiovascular morbidity and mortality.
Amlodipine and lercanidipine are calcium channel blockers inhibiting calcium influx into vascular smooth muscle and myocardial cells. This causes dilation of peripheral arterioles and decreases resistance to cardiac muscle function. Both amlodipine and lercanidipine are generally safe and well-tolerated medications. However, they can cause side effects, such as headache, dizziness, flushing, and lightheadedness. In rare cases, they can also cause more severe side effects, such as heart attack, stroke, and liver damage. The best medication for individual patients will depend on their needs and medical history. Therefore, talking to a doctor is needed to decide the best medication.
CONTENT
1. Overview and Key Difference
2. What is Amlodipine
3. What is Lercanidipine
4. Similarities – Amlodipine and Lercanidipine
5. Amlodipine vs. Lercanidipine in Tabular Form
6. Summary – Amlodipine vs. Lercanidipine
What is Amlodipine?
Amlodipine is a type of third-generation calcium channel blocker that is mainly used to treat hypertension and angina. The FDA-approved indications of amlodipine include hypertension, chronic stable angina, vasospastic angina, and angiographically documented coronary artery disease. The Non-FDA-approved off-label indications of amlodipine include diabetic retinopathy, left ventricular hypertrophy, Raynaud pneumonia, and silent myocardial ischemia. It works as a dihydropyridine calcium antagonist, which helps inhibit calcium influx into vascular smooth muscle and myocardial cells. This results in the dilation of peripheral arterioles and reduced resistance against cardiac muscle function. Additionally, amlodipine has been discovered to dilate the main coronary arteries and arterioles upon administration, making it a powerful antioxidant that produces nitric oxide synthase (NO), contributing to the vasodilatory effect. Amlodipine received FDA approval in 1987.
Figure 01: Chemical Structure of Amlodipine
Amlodipine is slowly but completely absorbed in the gastrointestinal tract when administered orally. The drug circulating in the body is bound with plasma proteins and extensively metabolized in the liver. The metabolized and unchanged drug is primarily excreted in the urine. Compared to other medications in the dihydropyridine class, amlodipine has the most extended half-life of 30-50 hours. Studies conducted on animals have shown that amlodipine does not have carcinogenic, mutagenic, or fertility effects in mice models, indicating its safety and absence of toxicity. However, the security of amlodipine in human pregnancy has not been well-studied, and it is considered a pregnancy type C drug.
What is Lercanidipine?
Lercanidipine is another calcium channel blocker that belongs to the dihydropyridine class. It is usually indicated alone or combined with an angiotensin-converting enzyme inhibitor to manage hypertension, angina pectoris, and Raynaud’s syndrome. Lercanidipine decreases the intracellular calcium concentration in myocardial and vascular smooth muscle cells by inhibiting the extracellular calcium influx. The decrease in intracellular calcium levels is associated with inhibition of the contractile process of the myocardial cells and causes dilation of the coronary and other systemic arteries. In addition, reduced calcium levels are also associated with decreased total peripheral resistance, systemic blood pressure, afterload, and increased oxygen supply to the myocardial tissues.
Figure 02: Lercanidipine
Once orally administered, lercanidipine reaches maximum plasma concentration after 2 hours and extensively binds with the plasma protein during the distribution. It is heavily metabolized in the liver by cytochrome P450 (CYP) 3A4 and is eliminated in the urine and feces. Lercanidipine is highly lipophilic and has a slow onset of action, offering comparatively a longer elimination half-life of 8-10 hours. High-fat diets improve the absorption of lercanidipine; therefore, it is recommended to have it after meals.
What are the Similarities Between Amlodipine and Lercanidipine?
- Amlodipine and Lercanidipine are calcium channel blockers for treating hypertension and angina.
- They work by decreasing the intracellular calcium concentration in myocardial and vascular smooth muscle cells.
- They are both generally safe and well-tolerated medications.
- Both these drugs cause similar side effects, such as headache, dizziness, flushing, and lightheadedness.
- They are prescription-type medications.
What is the Difference Between Amlodipine and Lercanidipine?
Amlodipine and Lercanidipine are medications used to treat high blood pressure. They belong to a class of drugs known as calcium channel blockers, and while they share some similarities, they also have differences. Amlodipine has a lower tolerability in managing hypertension, while lercanidipine has a better tolerability with a lower incidence of side effect profiles. Thus, this is the key difference between amlodipine and lercanidipine. Amlodipine has a slower onset of action than lercanidipine, suggesting it takes longer for amlodipine to start working. Moreover, amlodipine causes edema in the ankle and feet and causes a higher risk of drug withdrawal than lercanidipine.
Below is a summary of the difference between amlodipine and lercanidipine in tabular form for side-by-side comparison.
Summary – Amlodipine vs. Lercanidipine
Amlodipine and lercanidipine are calcium channel blockers used to treat hypertension and angina. The key difference between amlodipine and lercanidipine lies in their tolerability for managing hypertension: Amlodipine has a lower tolerability, while lercanidipine has better tolerability with a lower incidence of side effects. Amlodipine has a slower onset of action, indicating it takes longer to start working, whereas lercanidipine may have a more rapid onset. Amlodipine is associated with ankle and foot edema and carries a higher risk of drug withdrawal, while lercanidipine has a lower risk of side effects and withdrawal. Both drugs are effective for treating hypertension and angina, but the choice between them depends on individual needs and medical history.
Reference:
1. Grassi, Guido, et al. “Lercanidipine in the management of hypertension: An update.” Journal of Pharmacology and Pharmacotherapeutics, vol. 8, no. 4, 2017, pp. 155–165.
2. Nayler, Winifred G. “Amlodipine.” Clinical Drug Investigation, vol. 13, no. Supplement 1, 1997, pp. 1–11.
Image Courtesy:
1. “Amlodipine” By DoSiDo – Own work (Public Domain) via Commons Wikimedia
2. “Lercanidipine” By Fvasconcellos – Own work (Public Domain) via Commons Wikimedia