Indications
Lipid-altering medicines should be only one part of a wider plan to reduce risk factors in people who are at significantly increased risk of atherosclerotic vascular disease because of hypercholesterolemia. Drug therapy is indicated as an addition to diet when a diet restricted in saturated fat and cholesterol, together with other non-drug measures, has not worked well enough. Primary Hyperlipidemia: Atorvastatin + Ezetimibe tablet is indicated to reduce raised total cholesterol (total-C), low density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), triglycerides (TG) and non-high-density lipoprotein cholesterol (non-HDL-C). It is also indicated to increase high-density lipoprotein cholesterol (HDL-C). This applies to patients with primary (heterozygous familial and non-familial) hyperlipidemia or mixed hyperlipidemia. Homozygous Familial Hypercholesterolemia (HoFH): Atorvastatin + Ezetimibe tablet is indicated to reduce raised total-C and LDL-C in patients with homozygous familial hypercholesterolemia. It is used as an addition to other lipid lowering treatments (e.g., LDL apheresis), or when those treatments are unavailable.
⚠️ Always consult a registered physician before taking any medicine.
Pharmacology
Atorvastatin lowers plasma cholesterol and lipoprotein levels in animal models. It blocks HMG-CoA reductase, so the liver makes less cholesterol, and it increases the number of LDL receptors on the surface of liver cells, so more LDL is taken up and broken down. It also reduces LDL production and the number of LDL particles.
Ezetimibe lowers blood cholesterol by blocking its absorption in the small intestine. Its molecular target is the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), which takes up cholesterol and phytosterols in the intestine. In a 2-week clinical study in 18 patients with hypercholesterolemia, ezetimibe reduced intestinal cholesterol absorption by 54% compared with placebo. It had no clinically meaningful effect on plasma levels of the fat-soluble vitamins A, D and E, and it did not impair adrenocortical steroid hormone production. Ezetimibe does not block cholesterol synthesis in the liver, and it does not increase bile acid excretion. It sits at the brush border of the small intestine and stops cholesterol being absorbed, so less cholesterol from the intestine reaches the liver. The liver's cholesterol stores fall, and cholesterol is cleared from the blood faster. This mechanism is different from that of statins and complements it.
Pregnancy & Breastfeeding
Atorvastatin + Ezetimibe is Pregnancy Category X. This tablet must not be used by women who are pregnant or who may become pregnant. Serum cholesterol and triglycerides rise during a normal pregnancy, and lipid-lowering drugs give no benefit at this time, because the fetus needs cholesterol and cholesterol derivatives to develop normally. Atherosclerosis is a chronic process, so stopping lipid-lowering drugs during pregnancy should have little effect on the long-term results of treatment for primary hypercholesterolemia.
For breastfeeding, it isn't known whether atorvastatin passes into human milk. A small amount of another drug in this class does pass into breast milk.
⚠️ Talk to your doctor before taking any medicine during pregnancy or while breastfeeding.
Dosage Reference
⚠️ Reference ranges from official sources only. Consult your doctor for personalized dosing.
Side Effects & Interactions
Side Effects
No side-effect data recorded yet.