Ezetimibe

Ezetimibe is a medicine used to treat high cholesterol. This medicine helps by lowering bad cholesterol (LDL) levels in blood. Cholesterol is a fatty substance that builds up in your blood vessels and causes narrowing, which may lead to a heart attack or stroke.

Ezetimibe is a cholesterol absorption inhibitors. It reduces the cholesterol absorption from the intestine and lowers the levels of total cholesterol and bad cholesterol (LDL) in the blood.

• Primary Hypercholesterolemia: Adjunctive therapy to diet with a statin or alone.
• Cardiovascular Event Prevention: Reduces risk in patients with CHD and history of ACS.
• Homozygous Familial Hypercholesterolemia: Co-administered with a statin.
• Homozygous Sitosterolemia: Adjunctive therapy to diet.

Ezetimibe

Cholesterol Absorption Inhibitor

Ezetimibe localises at the brush border of the small intestine and inhibits absorption of cholesterol via the sterol transporter, Niemann-Pick C1-Like1 (NPC1L1). This results in decreased delivery of cholesterol to the liver, reduction of hepatic cholesterol stores and increased clearance of cholesterol from the blood.

Ezetimibe inhibits cholesterol absorption at the brush border of the small intestine, reducing cholesterol delivery to the liver and increasing cholesterol clearance from the blood.

Adult Dose (Oral):

• Hyperlipidemia, Homozygous Familial Sitosterolemia: 10 mg once daily.
• Mild Hepatic Impairment (Child-Pugh A): No dosage adjustment needed.
• Moderate-Severe Hepatic Impairment (Child-Pugh B or C): Not recommended.

Child Dose (>10 years): 10 mg once daily.

Elderly and Renal Impairment: No dosage adjustment required.

Take this medicine in the dose and duration as advised by your doctor. Swallow it as a whole. Do not chew, crush or break it. Ezetimibe may be taken with or without food, but it is better to take it at a fixed time.

If you miss a dose of Ezetimibe, skip it and continue with your normal schedule. Do not double the dose.

Common Side Effects:

• Joint pain
• Sinus inflammation
• Diarrhea
• Respiratory tract infection
• Fatigue
• Gastro-intestinal disturbances
• Headache
• Myalgia

Rare Side Effects: Anaphylaxis, angioedema, arthralgia, hepatitis, hypersensitivity reactions, rash, cholecystitis, cholelithiasis, myopathy, pancreatitis, rhabdomyolysis.

Precautions:

• Ezetimibe may decrease alertness, affect vision or make you feel sleepy and dizzy; do not drive if these symptoms occur.
• Treats high cholesterol by lowering bad cholesterol (LDL) and raising good cholesterol (HDL); helps prevent heart attack and stroke.
• Take in addition to regular exercise and low-fat diet.
• Notify your doctor if you experience muscle symptoms (pain or weakness), particularly if accompanied with fever.
• Do not stop taking the medication suddenly without talking to your doctor.
• Caution when coadministered with simvastatin exceeding 20 mg due to risk of statin-associated myopathy.

Contraindications:

• Hypersensitivity
• Moderate to severe liver disease or unexplained serum transaminase elevation
• Children <10 years
• Lactation

Drug Interactions:

• Colestyramine: Reduced absorption.
• Ciclosporin: Increased plasma concentrations.
• Oral anticoagulants: May increase INR.
• Fibrates: May increase cholesterol excretion into bile (cholelithiasis).

Food Interactions: It is unsafe to consume alcohol with Ezetimibe.

Use in Pregnancy: Ezetimibe may be unsafe; animal studies have shown harmful effects on the developing baby.

Use in Lactation: Ezetimibe is probably unsafe; limited data suggests drug may pass into breastmilk and harm the baby.

Pediatric Use: Not recommended for children below 10 years; 10-17 years: no dosage adjustment required.

Geriatric Use: No dosage adjustment is required for elderly patients.

Renal Impairment: Safe to use in patients with kidney disease; no dose adjustment recommended.

Hepatic Impairment: Use with caution; mild: no adjustment; moderate-severe: not recommended.

Overdose: 50 mg/day for up to 14 days or 40 mg/day for up to 56 days generally well tolerated; in case of overdose, symptomatic and supportive measures should be employed.

Storage: Store below 30 degree C in a cool and dry place, protected from light and moisture. Keep out of reach of children.

Ezetimibe