EZECHOL 10

Indications

• Primary hyperlipidemia
• Heterozygous familial hypercholesterolemia
• Homozygous familial hypercholesterolemia
• Mixed dyslipidemia

Dosage

Children: Refer to the BNF for Children for paediatric dosing details.

Adults: Refer to the BNF for detailed dosage information.

Mechanism of action

Ezetimibe selectively inhibits the intestinal absorption of cholesterol and related phytosterols. It does this by targeting the Niemann-Pick C1-like 1 (NPC1L1) transporter, which plays a crucial role in the uptake of cholesterol in the enterocytes of the small intestine. By inhibiting this transporter, ezetimibe decreases the amount of cholesterol that enters the bloodstream, leading to a reduction in plasma cholesterol levels.

Pharmacodynamics

The pharmacodynamic effects of ezetimibe include a reduction in total cholesterol, low-density lipoprotein (LDL) cholesterol, and triglycerides, while potentially increasing high-density lipoprotein (HDL) cholesterol. The drug's lipid-lowering effect is generally seen within a few days of initiation, with maximum effects observed after approximately 2 to 4 weeks of therapy.

Pharmacokinetics

Ezetimibe is well-absorbed from the gastrointestinal tract, with peak plasma concentrations occurring about 1 to 2 hours after oral administration. It undergoes extensive first-pass metabolism in the liver and intestines, forming an active metabolite. The elimination half-life of ezetimibe is approximately 22 hours, and it is primarily excreted via the feces, with a small fraction eliminated in the urine. Food does not significantly affect the absorption of ezetimibe.

Contra-indications

• Hypersensitivity to ezetimibe or any of its excipients
• Active liver disease, including unexplained persistent elevations of hepatic transaminases
• Pregnancy

Adverse effects

• Headache
• Diarrhea
• Muscle pain (myalgia)
• Abdominal pain
• Fatigue
• Elevated liver enzymes
• Rash

Interactions

• May increase the risk of myopathy when used with statins
• Bile acid sequestrants may reduce the absorption of ezetimibe
• Caution when used with cyclosporine, as it may increase ezetimibe levels

Precautions

• Monitor liver function tests before and periodically during therapy
• Use with caution in patients with moderate to severe renal impairment
• Discontinue in case of unexplained muscle pain, tenderness, or weakness

Pregnancy

Ezetimibe is contraindicated in pregnancy due to potential risks to the fetus.

Breast-feeding

It is unknown whether ezetimibe is excreted in human milk; caution is advised when administered to nursing mothers.

Storage

Store at room temperature, away from moisture and heat.

Formulations

• Ezetimibe 10 mg film-coated tablets