Larcadip10 mg

Larcadip is a third-generation dihydropyridine calcium channel blocker (CCB) indicated for the following condition:

Established / Approved Use

• Mild-to-moderate essential hypertension: Larcadip is indicated as monotherapy or in combination with other antihypertensive agents (e.g., beta-blockers, diuretics, ACE inhibitors) for the management of mild-to-moderate essential hypertension in adults, when blood pressure is not adequately controlled with a single agent or lifestyle measures alone.

Larcadip is not indicated for the treatment of acute anginal attacks, unstable angina, or heart failure, and it is not approved for use in patients under 18 years of age.

Each film-coated tablet typically contains Lercanidipine Hydrochloride equivalent to 10 mg or 20 mg of lercanidipine base, along with pharmaceutically approved excipients. Available strengths and excipients may vary by manufacturer; refer to the specific product package insert for exact composition.

Larcadip is a third-generation, highly lipophilic dihydropyridine calcium channel blocker (CCB) used in the treatment of hypertension. It has high vascular selectivity relative to cardiac tissue, which gives it a gradual onset of action and a lower incidence of reflex tachycardia and acute hypotension compared with some older dihydropyridines.

Although its plasma half-life is relatively short, Larcadip accumulates in the vascular smooth muscle cell membrane, allowing for a prolonged antihypertensive effect that supports once-daily dosing.

Larcadip belongs to the Calcium Channel Blocker class of medications, specifically the dihydropyridine subclass (third-generation). It is classified therapeutically as an antihypertensive agent.

Lercanidipine Hydrochloride inhibits the transmembrane influx of calcium ions into vascular smooth muscle cells by blocking L-type voltage-gated calcium channels. This action reduces calcium-dependent smooth muscle contraction, producing arteriolar vasodilation and a consequent reduction in peripheral vascular resistance and blood pressure.

Because of its high lipophilicity, Lercanidipine Hydrochloride accumulates within the lipid bilayer of the vascular smooth muscle membrane, from which it is slowly released, producing a smooth and prolonged antihypertensive effect despite a short plasma elimination half-life (approximately 8-10 hours). Lercanidipine Hydrochloride demonstrates high vascular selectivity with minimal direct effect on myocardial contractility or cardiac conduction at therapeutic doses.

Lercanidipine Hydrochloride is extensively metabolized in the liver via the cytochrome P450 3A4 (CYP3A4) enzyme system, with negligible unchanged drug excreted in urine or feces. It undergoes significant first-pass metabolism, resulting in low absolute oral bioavailability.

Larcadip tablets should be swallowed whole with water, taken at least 15 minutes before breakfast (or the main meal of the day), at approximately the same time each day. Do not take with grapefruit juice, as this can significantly increase drug levels and the risk of side effects. If a dose is missed, it should not be doubled the next day; the regular dosing schedule should simply be resumed.

Larcadip is metabolized primarily by CYP3A4, so co-administration with drugs that strongly affect this enzyme can significantly alter its plasma levels.

• Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, and other protease inhibitors): markedly increase plasma levels of Larcadip, increasing the risk of hypotension and adverse effects; concomitant use is contraindicated.
• Ciclosporin: plasma levels of both Larcadip and ciclosporin may increase with concomitant use; this combination is contraindicated.
• Grapefruit juice: inhibits intestinal CYP3A4 metabolism and significantly increases Larcadip plasma concentration; should be avoided.
• Strong CYP3A4 inducers (e.g., rifampicin, phenytoin, carbamazepine, St. John's Wort): may reduce plasma levels and antihypertensive efficacy of Larcadip; blood pressure should be monitored closely.
• Other antihypertensives, beta-blockers, and diuretics: may have additive blood-pressure-lowering effects when used with Larcadip, which is often therapeutically desirable but requires monitoring for excessive hypotension.
• Digoxin: Larcadip may modestly increase digoxin peak plasma concentration; monitor for signs of digoxin toxicity when co-administered.
• Simvastatin: co-administration can increase simvastatin exposure; it is advisable to take Larcadip in the morning and simvastatin in the evening, as originally studied.
• Alcohol: may enhance the vasodilatory and hypotensive effect of Larcadip; excessive alcohol intake should be avoided.

Adverse effects associated with Larcadip are generally dose-related and reflect its vasodilatory action.

Common

• Peripheral edema (ankle swelling)
• Headache
• Flushing
• Palpitations / reflex tachycardia
• Dizziness

Less Common

• Nausea, dyspepsia, abdominal pain
• Skin rash
• Fatigue, asthenia
• Polyuria

Rare

• Angina exacerbation
• Syncope
• Gingival hyperplasia (as with other dihydropyridines, with prolonged use)

Patients should seek medical attention if severe or persistent side effects occur.

Pregnancy: The safety of Larcadip in human pregnancy has not been established. Animal studies have shown reproductive toxicity at high doses. As a general precaution, Larcadip should be used during pregnancy only if clearly needed and if the potential benefit to the mother justifies the potential risk to the fetus. A physician should always be consulted before use in pregnancy.

Lactation: It is not known whether Larcadip is excreted in human breast milk. Because many lipophilic drugs pass into breast milk and a risk to the nursing infant cannot be excluded, Larcadip is not recommended during breastfeeding unless a physician determines the benefit outweighs the potential risk.

Larcadip should be used with caution in the following situations:

• Sick sinus syndrome (in the absence of a pacemaker) — caution advised due to vasodilatory effects.
• Mild-to-moderate hepatic or renal impairment — dose titration should be undertaken cautiously; severe impairment is contraindicated (see Contraindications).
• Elderly patients — greater sensitivity to blood-pressure-lowering effects may occur; initiate therapy cautiously.
• Left ventricular outflow obstruction — caution advised.
• Concomitant use with other antihypertensive drugs — increased risk of hypotension; blood pressure should be monitored.
• Grapefruit juice and strong CYP3A4-interacting drugs — should be avoided (see Interactions and Contraindications).

Patients should be advised to rise slowly from a sitting or lying position to reduce the risk of postural hypotension, particularly at the start of treatment.

Overdose with Larcadip may result in excessive peripheral vasodilation leading to marked and prolonged hypotension, reflex tachycardia, and, in severe cases, shock.

There is no specific antidote for Larcadip overdose. If overdose is suspected, seek immediate medical attention or contact emergency services / a poison control center right away. Management is supportive and may include gastric decontamination (if the ingestion is recent), continuous cardiovascular monitoring, intravenous fluids, and vasopressor support for significant hypotension, under close medical supervision. Do not attempt to manage a suspected overdose at home.

Store at room temperature (below 30°C), away from light and moisture. Keep out of reach of children.

Renal Impairment

Use with caution in mild-to-moderate renal impairment. Larcadip is contraindicated in severe renal impairment (creatinine clearance <30 mL/min) and in patients on dialysis.

Hepatic Impairment

Use with caution and careful titration in mild-to-moderate hepatic impairment, as Larcadip is extensively metabolized by the liver. Larcadip is contraindicated in severe hepatic impairment.

Elderly

No dose adjustment is generally required in elderly patients with normal renal and hepatic function, but greater sensitivity to hypotensive effects may occur; caution is advised, particularly at treatment initiation.

Pediatric Patients

Safety and efficacy of Larcadip in patients under 18 years of age have not been established; use in this population is not recommended (see Pediatric Uses).

Larcadip is generally used as a long-term, ongoing therapy for the management of chronic essential hypertension. There is no fixed treatment duration; therapy should continue for as long as the prescribing physician determines it is needed to maintain blood pressure control, with periodic review of efficacy and tolerability. Larcadip should not be stopped abruptly without medical advice.

Calcium Channel Blockers (Dihydropyridine derivatives) — Antihypertensive agents

Lercanidipine Hydrochloride selectively blocks L-type voltage-gated calcium channels in vascular smooth muscle cell membranes, inhibiting calcium influx and thereby preventing calcium-dependent smooth muscle contraction. This produces arteriolar (rather than venous) vasodilation, reducing peripheral vascular resistance and lowering blood pressure, with high vascular selectivity relative to cardiac muscle.

The safety and efficacy of Larcadip in children and adolescents under 18 years of age have not been established. Therefore, Larcadip is not recommended for use in the pediatric population until further data become available. Hypertension in children should be evaluated and managed by a pediatric specialist using agents with established pediatric safety data.