How do cholesterol absorption inhibitors work

The liver does this by increasing the number of LDL receptors on your liver cells. These receptors catch LDL cholesterol as it passes by and removes it from the blood. Ezetimibe comes as a tablet which you take once a day at a dose of 10mg. It might be combined with a statin or you might be prescribed it on it's own if you can't take statins.

Taking ezetimibe with a statin Ezetimibe is allowed alongside a statin when statins aren't bringing your cholesterol levels down to target on their own, including for rare conditions such as homozygous FH and sitosterolaemia. Taking ezetimibe by itself Ezetimibe is licensed to be used by itself if you have primary hypercholesterolaemia, which includes heterozygous FH as well as other conditions, and you can't take statins or they're not working for you. Ezetimibe is not suitable during pregnancy or if you are breastfeeding.

Ezetimibe's side-effect profile resembles that of placebo when given as monotherapy or in combination with statins. In clinical practice, ezetimibe has a role as monotherapy for patients who require modest LDL reductions or cannot tolerate other lipid-lowering agents.

In combination therapy with a statin, ezetimibe is used in patients who cannot tolerate high statin doses or in those who need additional LDL reductions despite maximum statin doses. At the initiation of the trial patients were receiving either atorvastatin or simvastatin. The addition of ezetimibe reduced LDL-C by an additional Similar results were demonstrated in high-risk patients with familial heterozygous hypercholesterolemia HeFH [ 32 ].

The addition of ezetimibe to statins is superior to treatment with statins alone in lowering non-HDL-C, ezetimibe co-administered with simvastatin lowered non-HDL-C by In terms of modifying risk factors other than LDL-C, the co-administration of ezetimibe with statins had a more favorable effect on HDL-C and TG when compared to statins therapy alone [ 33 ].

This effect was superior to that observed by doubling the dose of the statins. Furthermore, the lowering produced was consistent. Ezetimibe co-administration with fibric acid derivatives was examined in a randomized, evaluator-blind, placebo-controlled, parallel-group study of 32 healthy hypereholesterolemics. Ezetimibe co-administration with fenofibrate was found to produce clinically significant reductions in LDL-C First described by Bhattacharyya and Connor in in two sisters of German and German-Swiss ancestry with normal mental development.

The patients presented with tendinous and tuberous xanthoma and elevation of beta-sitosterol, campesterol and stigmasterol plant sterols in the blood [ 36 ]. Affected individuals have increased intestinal absorption of plant sterols mainly sitosterol that are usually absorbed in minute amounts in normal individuals.

Additionally, these patients have diminished clearance of plant sterols, leading to very high levels of plant sterols in the plasma. Patients suffering from sitosterolemia have severely depressed hepatic cholesterol biosynthesis, and decreased levels of HMG-CoA reductase enzyme [ 37 ].

Clinical manifestations include: tendon and tuberous xanthomas, episodes of hemolysis, accelerated atherosclerosis, and premature coronary artery disease. A recently reported trial demonstrated that treatment with ezetimibe reduces plant sterol levels in patients with sitosterolemia. It is generally accepted that atherosclerosis is an inflammatory disorder. It is believed that the atherosclerotic process begins with endothelial cell activation, which is triggered by multiple factors such as oxidized lipoproteins.

Cholesterol lowering agents as a group have demonstrated great efficacy in prevention and cessation of the progression of atherosclerosis. The efficacy of ezetimibe in monotherapy or in combination on CHD morbidity and mortality has not been well established. One of the unique features of cholesterol absorption inhibitors is their ability to modify post-prandial hyperlipidemia.

There is increasing evidence that post-prandial lipoproteins particularly cholesterol-rich chylomicron remnant are atherogenic. High-sensitivity C-reactive protein hs-CRP is an inflammatory mediator whose levels correlate with increased coronary risk. Ezetimibe co-administered with simvastatin resulted in significant incremental decreases in hs-CRP in patients with primary hypercholesterolemia.

Changes in individual lipid parameters did not explain the observed decreases in hs-CRP and were possibly consistent with an additional anti-inflammatory effect compared with simvastatin monotherapy [ 45 ]. Ezetimibe and its class of cholesterol absorption inhibitors are new, and there is a lack of outcomes data to explore whether its cholesterol modifying effects will translate to lower CHD mortality and morbidity. The safety of this medication has not yet been established with long term trials data as most of the studies conducted were short term.

With the advent and increased utilization of combination therapy in the management of dyslipidemia, further trials are needed to explore the efficacy, indications and safety profile of ezetimibe use in combination with Peroxisome proliferator-activated receptors PPARs , niacin and bile acid resins. The increased popularity of special weight loss diets such as the high protein diet, poses questions of whether such diets will alter the efficacy or safety of cholesterol absorption inhibitors.

Finally, the efficacy of statins in reducing CHD related events has lead to the controversial hypothesis regarding whether or not statins poses a pleiotropic non lipoprotein effect. If a pleiotropic effect exists, one might argue that a statin at a higher dose might be more beneficial than combination therapy producing the same effect.

Ezetimibe is the first clinically approved cholesterol absorption inhibitor. It is effective in lowering LDL-C as monotherapy or in combination with statins. It also provides another effective treatment option for HoFH and sitosterolemia patients.

Because of its recent introduction, we still lack both outcomes and long term safety data. Article PubMed Google Scholar. Dallas, Tex. Learn why. Our tremendous staff gives back to our community by coordinating free health screenings, educational programs, and food drives. Learn more. A leading indicator of our success is the feedback we get from our patients. Cholesterol absorption inhibitors are used to manage high cholesterol.

They work by blocking cholesterol in food from entering the bloodstream. These drugs may be used alone or in combination with other medicine. Red yeast rice may increase the risk of side effects from ezetimibe. Though it is rare, it may increase the risk of muscle and tendon pain. Niacin does not interact well with statin drugs.

It may increase the risk of muscle pain or a potentially fatal condition of muscle breakdown called rhabdomyolysis. Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions.

Clin Pharmacokinet. Jacobson TA.