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Zetia is a hypolipidemic drug. It is used to treat high blood pressure.

Brand: Ezetimibe

Availability: In Stock
Average Delivery Time: 9 Days
Exp. Date: June 2024
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Zetia 10 mg
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Product description

Drug Name

Zetia (Ezetimibe)

Pharmacological action

Hypolipidemic agent. Selectively inhibits absorption of cholesterol and some plant styrenes in the intestine.

When entering small intestine Zetia (Ezetimibe) is localized in the brush border of small intestine and prevents the absorption of cholesterol (Chs), which leads to a decrease in intestinal Chs flow to liver, due to which the reserves of Chs in liver are reduced and excretion of Chs from blood is increased. Ezetimibe does not increase bile acid excretion (unlike drugs that bind bile acids) and does not inhibit Chs synthesis in the liver (unlike statins).

By reducing absorption of Chs in the intestine Zetia (Ezetimibe) reduces Chs entry into the liver. Statins reduce the synthesis of Chs in the liver. Due to two different mechanisms of action, drugs of these two classes when prescribed together provide an additional reduction of Chs levels.

Clinical studies have shown that elevated levels of total Chs, Chs-LDL, and apolipoprotein-B, the main protein component of LDL, contribute to the development of atherosclerosis. In addition, a decreased level of HDL-C is associated with the development of atherosclerosis. Epidemiological studies have found that cardiovascular morbidity and mortality are directly related to the level of total chs and chs-LDL and inversely related to the level of chs-LDL. Like LDL, cholesterol- and triglyceride-rich lipoproteins, including LDL-C, LDL-C and remnants, can also contribute to atherosclerosis.

In a series of preclinical studies, ezetimibe has been shown to inhibit absorption of 14C-cholesterol and has no effect on absorption of triglycerides, fatty acids, bile acids, progesterone, ethinylestradiol, fat-soluble vitamins A and D.


After oral administration, ezetimibe is rapidly absorbed and intensively conjugates in the small intestine and liver to form pharmacologically active phenolic glucuronide (ezetimibe-glucuronide). Maximal concentration of ezetimibe-glucuronide is reached after 1-2 hours, ezetimibe - after 4-12 hours. Absolute bioavailability of ezetimibe cannot be determined since this compound is virtually water insoluble.

Simultaneous intake of food (both high-fat and low-fat) has no effect on the bioavailability of ezetimibe at an oral dose of 10 mg.

The plasma protein binding of Zetia (Ezetimibe) and ezetimibe-glucuronide is 99.7% and 88-92% respectively.

Zetia (Ezetimibe) is metabolized mainly in the small intestine and liver by conjugation with glucuronide (phase II reaction) with subsequent excretion in the bile. Minimal oxidative metabolism (phase I reaction) is observed in all studied species. Ezetimibe and ezetimibe-glucuronide are the major substances detected in plasma, accounting for approximately 10-20% and 80-90% of total plasma drug content, respectively. Ezetimibe and ezetimibe-glucuronide are slowly eliminated from plasma under conditions of intense intestinal-hepatic recirculation.

The T1/2 of Zetia (Ezetimibe) and ezetimibe-glucuronide is about 22 hours. Within 10 days of the total dose taken, about 78% is excreted in the feces and about 11% in the urine.

Contraindications to use

Moderate (7-9 Child-Pugh scores) and severe (>9 Child-Pugh scores) liver failure; concomitant use with fibrates (efficacy and safety not established); hypersensitivity to ezetimibe.

Use in pregnancy and lactation

No adequate and strictly controlled trials concerning safety of ezetimibe during pregnancy have been carried out, therefore it is not recommended to use it in this category of patients. In case of pregnancy, ezetimibe should be discontinued.

It is unknown whether ezetimibe is excreted with breast milk in humans. If it is necessary to use during lactation, discontinuation of breastfeeding should be considered.

No direct and indirect adverse effects on pregnancy, embryo/fetal development, labor and postnatal development have been observed in experimental animal studies of ezetimibe administration. No teratogenic effects were observed when ezetimibe was administered to pregnant rats in combination with lovastatin, simvastatin, pravastatin and atorvastatin. When administered to pregnant rabbits, fetal skeletal defects were observed with low frequency. It was found that ezetimibe is excreted with breast milk in lactating rats.

Use in liver dysfunction

Contraindicated in moderate (7-9 points by Child-Pugh scale) and severe (> 9 points by Child-Pugh scale) hepatic failure. Preparations containing eucalyptol are not used rectally in liver dysfunction.

Administration in impaired renal function

Preparations containing eucalyptol, do not use rectally if you have impaired kidney function.

Administration in children

Ezetimibe should not be used in children and adolescents under 18 years of age.

Indications for the active substance EZETIMIB

Primary hypercholesterolemia (in combination with statins or as monotherapy in addition to diet to reduce elevated levels of total Chs, Chs-LDL, apolipoprotein B and triglycerides, and to increase HDL-C levels in patients with primary hypercholesterolemia); homozygous familial hypercholesterolemia (in combination with statins is recommended to reduce elevated levels of total Chs, Chs-LDL, LDL-apheresis is also possible); homozygous sitosterolemia (or phytosterolemia) - increased levels of plant sterols in plasma with increased or normal levels of Chs and normal triglycerides.

Dosing regimen

Patients should follow a hypolipidemic diet before and during treatment. The recommended dose as monotherapy and in combination with statins is 10 mg once daily.

In concomitant therapy with fatty acid sequestrants, ezetimibe is used at a dose of 10 mg once daily not later than 2 hours before fatty acid sequestrants administration or not earlier than 4 hours after their administration.