Lacidipine

Lacidipine is an antihypertensive agent belonging to the Calcium Channel Blocker class.

Lacidipine is a dihydropyridine calcium channel blocker used for the treatment of hypertension.

Rapidly but poorly absorbed from the gastrointestinal tract. Bioavailability: Approx 10%. Time to peak plasma concentration: 30-150 minutes. Plasma protein binding: >95% to albumin and α-1 glycoprotein. Metabolized in the liver by CYP3A4 isoenzymes; undergoes extensive first-pass metabolism. Mainly via faeces (70% as metabolites); urine (remainder as metabolites). Elimination half-life: 13-19 hours.

Lacidipine shows common side effects like Dizziness and Drowsiness, Headache, Increased heart rate, Nausea and vomiting, Stomach discomfort, Skin rash, Muscle cramps, Cough, etc.

Lacidipine is available in the form of Oral Tablet.

Lacidipine is available in India, UK, Canada, Russia, China, Japan, Korea, Germany, Poland, Vietnam and Africa.

Lacidipine belonging to the Calcium Channel Blockers acts as an antihypertensive agent.

Lacidipine is a dihydropyridine Ca-channel blocker. It inhibits Calcium ions from entering the slow channels or select voltage-sensitive areas of the vascular smooth muscle and myocardium during depolarization, thus producing coronary vascular smooth muscle relaxation resulting in coronary and peripheral vasodilation.

The Data of Onset of action of Lacidipine is not available.

The Data of Duration of Action for Lacidipine in the body is not available.

The Tmax was found within 30-150 minutes following the administration of Lacidipine.

Lacidipine is available in the form of Oral Tablet.

Lacidipine tablet taken orally, usually once a day.

Lacidipine is a calcium channel blocker used in the treatment of high blood pressure. It is used alone or in combination with other antihypertensive medicines. This medicine is used to reduce high blood pressure caused by genetic and environmental factors.

Lacidipine is an antihypertensive agent belonging to Calcium Channel Blockers. It inhibits Calcium ions from entering the slow channels or select voltage-sensitive areas of the vascular smooth muscle and myocardium during depolarization, thus producing coronary vascular smooth muscle relaxation resulting in coronary and peripheral vasodilation.

Lacidipine is approved for use in the following clinical indications

• Hypertension

Lacidipine is used in the treatment of high blood pressure. It is used alone or in combination with other antihypertensive medicines.

• Hypertension

Initially: 2 mg once daily; may increase in increments of 2 mg every 3-4 weeks according to response.

Max: 6 mg once daily.

Lacidipine is available in various strengths as 2mg, 4mg and 6mg.

Lacidipine is available in the form of Oral Tablet.

No information is available.

Lacidipine is contraindicated in patients with Cardiogenic shock, aortic stenosis, unstable angina, recent acute MI.

• Discontinue if cardiogenic shock develops.
• Discontinue if ischemic pain occurs shortly after starting therapy.
• Lacidipine has not been shown to be effective for the secondary prevention of myocardial infarction.
• Lacidipine has not had safety or efficacy established in the treatment of malignant hypertension.
• Lacidipine should be used with caution in patients with hepatic impairment because antihypertensive effect may be increased.

No information is available.

Breastfeeding while using Lacidipine unless the potential benefits for the mother outweigh the adverse effects to the neonate. Animal data reports Lacidipine maybe excreted in breast milk, however presence in human breast milk is unknown. Effects on exposed infants are unknown.

Pregnancy Category

Using Lacidipine during pregnancy unless the potential benefits for the mother outweigh the adverse effects to the foetus or neonate. Animal studies have shown teratogenic effects. Human data is limited and as such a potential risk cannot be ruled out.

No information is available.

• Increased angina and/or MI; QT prolongation, symptomatic hypotension, syncope, Palpitations (transient), tachycardia, Nausea, abdominal discomfort, gingival hyperplasia, Asthenia, transient edema, Increased serum alkaline phosphatase, Headache, dizziness, Polyuria, Rash, pruritus, erythema, Transient flushing (especially of face).

• Other antihypertensive agents

Enhanced hypotensive effect with other antihypertensive agents (e.g., diuretics [e.g., furosemide], β-blockers [e.g., propranolol], ACE inhibitors [e.g., captopril]).

• Cimetidine, and strong CYP3A4 inhibitors

Increased serum concentration with cimetidine, and strong CYP3A4 inhibitors (e.g., itraconazole).

• Patient with renal transplant

May reverse the decrease in renal plasma flow and glomerular filtration rate induced by ciclosporin in patient with renal transplant.

• CYP3A4

Decreased serum concentration with strong CYP3A4 inducers (e.g., rifampicin).

The common side effect of Lacidipine include the following

● Dizziness and Drowsiness, Headache, Increased heart rate, Nausea and vomiting, Stomach discomfort, Skin rash, Muscle cramps, Cough.

• Pregnancy

Pregnancy Category

Using Lacidipine during pregnancy unless the potential benefits for the mother outweigh the adverse effects to the foetus or neonate. Animal studies have shown teratogenic effects. Human data is limited and as such a potential risk cannot be ruled out.

• Nursing Mothers

Breastfeeding while using Lacidipine unless the potential benefits for the mother outweigh the adverse effects to the neonate. Animal data reports Lacidipine maybe excreted in breast milk, however presence in human breast milk is unknown. Effects on exposed infants are unknown.

• Symptoms: Prolonged peripheral vasodilation associated with hypotension and tachycardia, bradycardia, or prolonged atrioventricular conduction.
• Management: Supportive treatment and cardiac function monitoring.

Pharmacodynamic

Lacidipine is a specific and potent calcium antagonist with a predominant selectivity for calcium channels in the vascular smooth muscle. Its main action is to dilate predominantly peripheral and coronary arteries, reducing peripheral vascular resistance and lowering blood pressure. Following the oral administration of 4 mg Lacidipine to volunteer subjects, a minimal prolongation of QTc interval has been observed (mean QTcF increase between 3.44 and 9.60 ms in young and elderly volunteers).

Pharmacokinetics

• Absorption

Since it is a highly lipophilic compound, Lacidipine is rapidly absorbed from the gastrointestinal tract following oral administration with the peak plasma concentrations reached between 30 and 150 minutes of dosing. The peak plasma concentrations display large interindividual variability, with the values ranging from 1.6 to 5.7 μg/L following single-dose oral administration of Lacidipine 4mg in healthy young volunteers. Absolute bioavailability is less than 10% due to extensive first-pass metabolism in the liver.

• Distribution

Lacidipine is highly protein-bound (more than 95%) to predominantly albumin and to a lesser extent, alpha-1-glycoprotein.

• Metabolism and Excretion

Lacidipine undergoes complete CYP3A4-mediated hepatic metabolism, with no parent drug detected in the urine or feces. The 2 main metabolites have no pharmacological activity. The average terminal half-life of Lacidipine ranges from between 13 and 19 hours at steady state. Approximately 70% of the administered dose is eliminated as metabolites in the faeces and the remainder as metabolites in the urine.

• https://www.mims.com/philippines/drug/info/lacidipine?mtype=generic
• https://go.drugbank.com/drugs/DB09236
• https://www.practo.com/medicine-info/lacidipine-2543-api#usage