Lercanidipine

Drug Information: Lercanidipine

Lercanidipine is a dihydropyridine calcium channel blocker used to treat hypertension. It works by selectively inhibiting calcium influx into vascular smooth muscle cells, leading to vasodilation and a reduction in blood pressure. Its high lipophilicity allows it to partition into the lipid bilayer of cell membranes, providing a longer duration of action compared to some other calcium channel blockers.

Category

Antihypertensive

Mechanism of Action

Lercanidipine functions as a calcium channel blocker, specifically targeting L-type calcium channels primarily found in vascular smooth muscle. These channels are essential for the influx of calcium ions into the cells, which triggers muscle contraction. Lercanidipine selectively binds to these channels, blocking the entry of calcium. This reduces the intracellular calcium concentration, inhibiting the interaction of actin and myosin, the proteins responsible for muscle contraction. The resulting vasodilation, particularly in the peripheral vasculature, lowers peripheral resistance and subsequently reduces blood pressure. Lercanidipine exhibits a high degree of vascular selectivity, meaning it preferentially affects blood vessels over cardiac muscle, minimizing direct effects on heart rate and contractility. Its slow onset and long duration of action contribute to a gradual and sustained reduction in blood pressure, which is beneficial for minimizing the risk of abrupt hypotension. The drug’s lipophilic nature enhances its binding affinity to the cell membrane, allowing for a prolonged effect after dissociation from the calcium channel.

Clinical Uses

The primary clinical use of Lercanidipine is in the treatment of hypertension (high blood pressure). It is effective as a monotherapy or in combination with other antihypertensive agents, such as ACE inhibitors, angiotensin receptor blockers (ARBs), or diuretics, to achieve optimal blood pressure control. Due to its vasodilatory effects, it can also be used in the management of angina pectoris, particularly in patients with vasospastic angina (Prinzmetal’s angina). Lercanidipine helps to reduce the frequency and severity of anginal attacks by preventing coronary artery spasms. While primarily indicated for hypertension and angina, it is sometimes used off-label in conditions where vasodilation is beneficial, such as Raynaud’s phenomenon, although other calcium channel blockers may be preferred in these cases. It is important to consider individual patient characteristics and potential drug interactions when prescribing lercanidipine.

Dosage

Adults: The typical starting dose of Lercanidipine is 10 mg once daily, preferably in the morning at least 15 minutes before a meal. The dose may be increased to 20 mg once daily if blood pressure control is inadequate after at least 2 weeks. Doses higher than 20 mg daily are not recommended.
Pediatric: Lercanidipine is generally not recommended for use in children due to limited safety and efficacy data.
Route of Administration: Oral. The tablet should be swallowed whole with water, and not chewed or crushed.

Indications

Common indications for Lercanidipine include:

• Hypertension (High Blood Pressure)
• Angina Pectoris (Chest Pain) – particularly vasospastic angina

Contraindications

Lercanidipine is contraindicated in the following conditions:

• Hypersensitivity to lercanidipine or any other dihydropyridine calcium channel blocker
• Severe hepatic impairment
• Severe renal impairment (creatinine clearance < 30 mL/min)
• Unstable angina
• Within one month of a myocardial infarction (heart attack)
• Untreated congestive heart failure
• Concomitant use with strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, erythromycin, ritonavir)
• Pregnancy and lactation

FAQ

1. What is Lercanidipine used for?
   
   Lercanidipine is primarily used to treat high blood pressure (hypertension). It can also be used for angina.
2. How does Lercanidipine work?
   
   It works by blocking calcium channels in the walls of blood vessels, causing them to relax and widen, which lowers blood pressure.
3. What are the common side effects of Lercanidipine?
   
   Common side effects include headache, flushing, peripheral edema (swelling in the ankles and feet), dizziness, and palpitations.
4. Can I take Lercanidipine with other medications?
   
   It’s important to inform your doctor about all medications you are taking, as Lercanidipine can interact with certain drugs, especially strong CYP3A4 inhibitors.
5. What should I avoid while taking Lercanidipine?
   
   Avoid grapefruit juice, as it can increase the levels of Lercanidipine in your blood, potentially leading to increased side effects. Excessive alcohol consumption should also be avoided.
6. What happens if I miss a dose of Lercanidipine?
   
   If you miss a dose, take it as soon as you remember, unless it is almost time for your next dose. In that case, skip the missed dose and continue with your regular dosing schedule. Do not double the dose to catch up.
7. How long does it take for Lercanidipine to start working?
   
   Lercanidipine starts working within a few hours, but it may take several weeks to achieve the full blood pressure-lowering effect.
8. Can I stop taking Lercanidipine suddenly?
   
   Do not stop taking Lercanidipine suddenly without consulting your doctor, as it can cause a rapid increase in blood pressure.