Perdipin LA

Perdipin LA Uses, Dosage, Side Effects, Food Interaction and all others data.

A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents. [PubChem]

Perdipin LA, a dihydropyridine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal's variant angina. Perdipin LA is similar to other peripheral vasodilators. Perdipin LA inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Perdipin LA
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Perdipin LA
Availability	Prescription only
Generic	Nicardipine
Nicardipine Other Names	Nicardipine, Nicardipino, Nicardipinum
Related Drugs	amlodipine, aspirin, lisinopril, metoprolol, losartan, furosemide, carvedilol, hydrochlorothiazide, spironolactone, atenolol
Type
Formula	C₂₆H₂₉N₃O₆
Weight	Average: 479.525 Monoisotopic: 479.205635675
Protein binding	>95%
Groups	Approved, Investigational
Therapeutic Class
Manufacturer
Available Country	Japan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Perdipin LA is a calcium channel blocker used for the short-term treatment of hypertension and chronic stable angina.

Used for the management of patients with chronic stable angina and for the treatment of hypertension.

Perdipin LA is also used to associated treatment for these conditions: Chronic Stable Angina Pectoris, High Blood Pressure (Hypertension), Migraine, Blood pressure >185/110 mm Hg arterial hypertension

How Perdipin LA works

By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

Toxicity

Oral LD₅₀ Rat = 184 mg/kg, Oral LD₅₀ Mouse = 322 mg/kg

Food Interaction

Avoid grapefruit products.
Take with or without food. The absorption is unaffected by food.

[Moderate] GENERALLY AVOID: The consumption of grapefruit juice may be associated with significantly increased plasma concentrations of some calcium channel blockers (CCBs) when they are administered orally.

The proposed mechanism is inhibition of CYP450 3A4-mediated first-pass metabolism in the gut wall by certain compounds present in grapefruit.

The interaction has been reported with the dihydropyridine CCBs (in roughly decreasing order of magnitude) felodipine, nisoldipine, nifedipine, and nimodipine, often with a high degree of interindividual variability.

Grapefruit juice caused more than twofold increases in felodipine, nifedipine, and nisoldipine AUCs.

MANAGEMENT: The manufacturers of nifedipine and nisoldipine recommend avoiding grapefruit juice.

Patients treated orally with other calcium channel blockers should be advised to avoid consumption of large amounts of grapefruits and grapefruit juice to prevent any undue fluctuations in serum drug levels.

Increased effects on blood pressure may persist for up to 4 days after the consumption of grapefruit juice.

Monitoring for calcium channel blocker adverse effects (e.g., headache, hypotension, syncope, tachycardia, edema) is recommended.

Perdipin LA multivitamins interaction

[Moderate] Calcium-containing products may decrease the effectiveness of calcium channel blockers by saturating calcium channels with calcium.

Calcium chloride has been used to manage acute severe verapamil toxicity.

Management consists of monitoring the effectiveness of calcium channel blocker therapy during coadministration with calcium products.

Perdipin LA Drug Interaction

Moderate: aspirin, aspirinUnknown: Allergy , Allergy , ginkgo, ginkgo, furosemide, furosemide, amlodipine, amlodipine, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Perdipin LA Disease Interaction

Major: aortic stenosis, cardiogenic shock/hypotension, coronary artery disease, liver disease, renal dysfunctionModerate: CHF/AMI

Volume of Distribution

8.3 L/kg

Elimination Route

While nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.