API

Ezetimibe (10mg)

Drug classification

Ezetimibe is a lipid-lowering agent; specifically, a cholesterol absorption inhibitor.

Dosage form

Film-coated tablet containing 10 mg of ezetimibe.

API strength per dosage

Dose

Ezentimibe 10 mg is typically taken once daily, with or without food, for adults and children ≥10 years. No dose adjustment is needed for mild-to-moderate renal or hepatic impairment; use is not recommended in severe hepatic impairment. Safety and efficacy in children <10 years are not established. Always follow local prescribing information.

Mechanism of action

Ezetimibe selectively inhibits the Niemann-Pick C1-Like 1 (NPC1L1) transporter on the brush border of the small intestine, reducing intestinal absorption of cholesterol. This decreases delivery of intestinal cholesterol to the liver, lowers hepatic cholesterol stores, and increases clearance of cholesterol from the blood, resulting in reduced total and LDL cholesterol levels.

Indications

High cholesterol

Side effects

Diarrhea Joint pain Sinus inflammation Upper respiratory tract infection Pain in extremity

Pregnancy category

Ezetimibe should be used during pregnancy only if clearly needed; safety in pregnant women is not established. Avoid use unless benefits outweigh risks.

Precautions

Liver function monitoring, caution in hepatic impairment, risk of myopathy with statins, monitor for muscle pain or weakness, assess lipid levels regularly, avoid in active liver disease, use with caution in pregnancy and lactation, monitor for hypersensitivity reactions, consider drug interactions, assess adherence.

Contraindications

Hypersensitivity to ezetimibe or any component of the formulation, active liver disease, unexplained persistent elevations in hepatic transaminases (especially when used with a statin), pregnancy and breastfeeding (when combined with a statin).