L-Cardin4 mg

L-Cardin is a long-acting dihydropyridine calcium channel blocker indicated for the treatment of hypertension.

• Essential hypertension (established use): L-Cardin is indicated for the management of essential hypertension, used either as monotherapy or in combination with other antihypertensive agents (such as thiazide diuretics or beta-blockers) when blood pressure is not adequately controlled on a single agent.

L-Cardin has not been shown to provide additional benefit for secondary prevention after myocardial infarction and is not indicated for this purpose. The safety and efficacy of L-Cardin in hypertensive emergencies (malignant hypertension) have not been established, and it should not be used for that indication.

Each tablet of Lacidipine typically contains 2 mg or 4 mg of lacidipine as the active ingredient, together with pharmaceutically inert excipients such as lactose, microcrystalline cellulose, magnesium stearate, and film-coating agents. Lacidipine is available only as an oral tablet; injectable, liquid, or reconstitutable forms of Lacidipine do not exist.

L-Cardin is a third-generation dihydropyridine calcium channel blocker used to treat high blood pressure (hypertension). L-Cardin is characterized by high lipophilicity and a slow, gradual onset of action, which allows for smooth, sustained blood pressure control with once-daily dosing and a lower incidence of reflex tachycardia compared with some shorter-acting dihydropyridines. L-Cardin works by relaxing and widening blood vessels, reducing the resistance the heart must pump against and thereby lowering blood pressure.

L-Cardin belongs to the dihydropyridine class of calcium channel blockers (CCBs), a subgroup of antihypertensive agents that act primarily on vascular smooth muscle rather than on cardiac tissue.

Mechanism of Action

Lacidipine selectively blocks voltage-gated L-type calcium channels in vascular smooth muscle cell membranes, inhibiting the influx of extracellular calcium ions. This reduces intracellular calcium availability, leading to relaxation of arteriolar smooth muscle, vasodilation, and a consequent fall in peripheral vascular resistance and blood pressure.

Pharmacokinetics

Lacidipine is highly lipophilic and partitions extensively into the cell membrane, which accounts for its slow onset and long duration of action despite a relatively short plasma half-life (approximately 13–19 hours). Lacidipine undergoes extensive first-pass hepatic metabolism via the CYP3A4 enzyme system, has an oral bioavailability of roughly 10%, and is more than 95% bound to plasma proteins. Lacidipine has no clinically active metabolites, and elimination occurs via hepatic metabolism with excretion of metabolites in urine and feces.

L-Cardin tablets should be taken orally, once daily, preferably in the morning, at approximately the same time each day. L-Cardin may be taken with or without food; however, L-Cardin should not be taken with grapefruit or grapefruit juice, as this can significantly increase L-Cardin blood levels (see Drug Interactions). L-Cardin tablets should be swallowed whole with a glass of water and should not be crushed or chewed unless directed by a physician.

Grapefruit Juice

Grapefruit juice inhibits intestinal CYP3A4 metabolism of L-Cardin, significantly increasing plasma concentrations of L-Cardin and the risk of hypotension and other adverse effects. Patients taking L-Cardin should avoid grapefruit and grapefruit juice.

CYP3A4 Inhibitors

Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, ritonavir, cimetidine) can increase plasma levels of L-Cardin, increasing the risk of hypotension and other adverse effects; concurrent use should be undertaken with caution and, if needed, with dose adjustment of L-Cardin.

CYP3A4 Inducers

Strong CYP3A4 inducers (e.g., rifampicin, carbamazepine, phenytoin, St. John's Wort) can reduce plasma levels of L-Cardin and diminish its antihypertensive effect; blood pressure should be monitored closely if L-Cardin is used together with these agents.

Other Antihypertensive Agents

Concomitant use of L-Cardin with other antihypertensive drugs, diuretics, or agents with hypotensive potential (e.g., alpha-blockers, nitrates) may produce additive blood-pressure-lowering effects; dose titration and monitoring are recommended.

Corticosteroids

Corticosteroids and tetracosactide may reduce the antihypertensive effect of L-Cardin due to fluid retention.

Side effects of L-Cardin are generally dose-related and reflect its vasodilatory action.

Peripheral edema with L-Cardin is a recognized class effect of dihydropyridine calcium channel blockers and is dose-dependent; it is caused by arteriolar dilation rather than fluid overload and typically does not respond to diuretics.

Pregnancy

The safety of L-Cardin in human pregnancy has not been established. L-Cardin should be used during pregnancy only if the potential benefit to the mother clearly justifies the potential risk to the fetus, and only under close medical supervision. Animal studies with L-Cardin have shown effects on uterine contractility; a physician should be consulted before using L-Cardin if pregnancy is confirmed or suspected.

Lactation

It is not known whether L-Cardin is excreted in human breast milk, although related compounds are excreted into the milk of lactating animals. Because of the potential for adverse effects in a nursing infant, a decision should be made whether to discontinue breastfeeding or discontinue L-Cardin, taking into account the importance of L-Cardin to the mother. Consult a physician before using L-Cardin while breastfeeding.

• Heart failure: Although L-Cardin has less negative inotropic effect than non-dihydropyridine calcium channel blockers, L-Cardin should be used with caution in patients with heart failure or reduced cardiac reserve, since dihydropyridines can occasionally precipitate or worsen heart failure symptoms.
• Hepatic impairment: Because L-Cardin is extensively metabolized in the liver, plasma levels of L-Cardin may be significantly increased in patients with hepatic impairment; a reduced dose and close monitoring are advised, and L-Cardin should be used with particular caution in severe hepatic impairment (see Dosage and Administration).
• Sick sinus syndrome/AV conduction abnormalities: Use L-Cardin with caution in patients with sinoatrial or atrioventricular node dysfunction.
• Angina: L-Cardin has not been shown to be effective for secondary prevention after myocardial infarction; occasionally, initiation of L-Cardin may be associated with an increase in frequency, duration, or severity of angina.
• Malignant hypertension: The safety and efficacy of L-Cardin have not been established for this condition.
• Drug interactions: Avoid grapefruit juice and use caution with strong CYP3A4 inhibitors/inducers while taking L-Cardin (see Drug Interactions).
• Driving/operating machinery: L-Cardin may cause dizziness, especially at the start of treatment; patients should be cautious until they know how L-Cardin affects them.

Overdose with L-Cardin may cause pronounced peripheral vasodilation leading to marked and prolonged hypotension, reflex tachycardia, and, in severe cases, bradycardia and disturbances of cardiac conduction.

There is no specific antidote for L-Cardin overdose. Anyone suspected of having taken an overdose of L-Cardin should seek immediate medical attention or contact a poison control center/emergency services. Management of a L-Cardin overdose is supportive and includes monitoring of cardiovascular status (blood pressure, heart rate, ECG), elevation of the legs, and, if needed, intravenous fluids and vasopressor support administered under medical supervision. Do not attempt to manage a L-Cardin overdose at home.

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

Pediatric Patients

The safety and efficacy of L-Cardin have not been established in children and adolescents; use of L-Cardin in this population is not recommended.

Elderly Patients

L-Cardin can be used in elderly patients; no specific dose adjustment is generally required, although it is prudent to start L-Cardin at the lowest effective dose given age-related changes in drug handling.

Renal Impairment

No dose adjustment of L-Cardin is generally necessary since it is not significantly renally cleared; caution is advised in severe renal impairment.

Hepatic Impairment

Dose reduction and close monitoring of L-Cardin are recommended (see Dosage and Administration and Precautions and Warnings).

L-Cardin is intended for long-term, continuous use in the management of chronic hypertension. Blood pressure control and treatment response to L-Cardin should be reassessed periodically by a physician, and L-Cardin should not be stopped abruptly without medical advice.

Calcium Channel Blocker – Dihydropyridine derivative (antihypertensive).

Lacidipine inhibits the transmembrane influx of calcium ions through L-type calcium channels in vascular smooth muscle, with high selectivity for vascular over cardiac tissue. This action of Lacidipine produces arteriolar vasodilation and a reduction in peripheral vascular resistance, lowering blood pressure without a clinically significant negative effect on cardiac contractility or conduction at therapeutic doses.

The safety and efficacy of L-Cardin in children and adolescents below 18 years of age have not been established. L-Cardin is therefore not recommended for use in pediatric patients until further clinical data become available.