EZETROL - EZETIMIBE

ezetrol image drugs images

Ezetrol – ezetimibe

Cholesterol absorption inhibitor

10MG Tablet

 

Ezetrol alone

+ statin

+ fenofibrate

Indicated for

1.      the reduction of (total-C), (LDL-C), (Apo B), and (TG) and

2.      to increase (HDL-C) in patients with primary (heterozygous familial and non-familial) hypercholesterolemia.

 

Same for Ezetrol alone

 

Indicated for

1.      the reduction of elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia.

 

Recommended Dose and Dosage Adjustment

·        The recommended dose of EZETROL is 10 mg once daily orally, alone, with a statin, or with fenofibrate. EZETROL can be taken with or without food at any time of the day but preferably at the same time each day.

Muscle Effects

 

Myopathy/Rhabdomyolysis

Myalgia

Myopathy and rhabdomyolysis are known adverse effects of statins and fibrates. They may also happen to patients on Ezetrol. If a patient complains about muscle pain,  consideration given to discontinuation of the drugs. Most cases of myopathy/rhabdomyolysis resolved when drugs were discontinued.

In controlled clinical trials, the incidence of myalgia was 5.0% for EZETROL vs 4.6% for placebo. Patients should be instructed to contact their physician if they experience persistent and severe muscle pains with no obvious cause.

 

 

Adverse Drug Reaction Overview

·        The most commonly reported adverse events in clinical studies were upper respiratory tract infection, headache, myalgia and back pain.

Cholestyramine

·        Concomitant cholestyramine administration decreased the mean AUC of total ezetimibe (ezetimibe+ezetimibe-glucuronide) approximately 55%. EZETROL should be administered either 2 hours or longer before or 4 hours or longer after administration of a bile acid sequestrant.

 

 

Mechanism of Action

EZETROL is in a new class of lipid-lowering compounds that selectively inhibit the intestinal absorption of cholesterol and related plant sterols. The molecular target of ezetimibe is the sterol transporter, Niemann-Pick C1-Like 1 (NPC1L1), which is responsible for the intestinal uptake of cholesterol and phytosterols.

Although ezetimibe is rapidly absorbed and is extensively metabolized to an active phenolic glucuronide which reaches the systemic circulation after oral administration, its action is localized at the brush border of the small intestine where it inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This results in a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood.

Ezetimibe inhibited the absorption of [14C]-cholesterol with no effect on the absorption of triglycerides, fatty acids, bile acids, progesterone, ethinyl estradiol, or the fat soluble vitamins A and D.

 

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