Loxen

Uses

Loxen 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.

Loxen 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 Loxen 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.

Loxen 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.

Loxen 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

Loxen 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.

Half Life

8.6 hours

Clearance

• 0.4 L/hr∙kg [Following infusion]

Elimination Route

Loxen has been shown to be rapidly and extensively metabolized by the liver.

Innovators Monograph

You find simplified version here Loxen