Ezetimibe - Uses, Interactions, Mechanism Of Action
Ezetimibe is mainly employed in management of two genetic disorders: familial hypercholesterolaemia and homozygous sitosterolaemia. It also prevents heart diseases and the propensity for heart diseases through reduction of cholesterol rate within the body.
USES
Primary Hypercholesterolemia: Ezetimibe helps in reducing low density lipoprotein cholesterol or ‘’bad’ cholesterol which is responsible for artery clogging. It is used in cases where the patient's condition is not controlled by statins alone, or where patients are unable to take higher doses of statins because of its side effects.
Familial Hypercholesterolemia: Ezetimibe is beneficial in managing Familial Hypercholesterolemia, a genetic disorder that causes the body to lack the necessary ability to eliminate lipoprotein cholesterol out of the blood stream. hence leading to high concentrations of cholesterol. In these cases, ezetimibe is added to statin or other lipid lowering therapies when needed.
Sitosterolaemia: Ezetimibe is also prescribed for curing sitosterolaemia, which is a disease in which plant sterols are accumulated in body due to genetic disorder in cholesterol metabolism. Ezetimibe has been shown to decrease the absorption of plant sterols in the intestine to treat this condition.
Prevention of Cardiovascular Events: Also, ezetimibe is prescribed to patients with cardiovascular disease history in order to reduce cholesterol levels and further potential events. In addition to statins, ezetimibe can also reduce LDL-C; this treatment improves the prognosis for high-risk individuals.
Mechanism Of Action
Ezetimibe affects cholesterol absorption by the body especially from the small portion of the intestine. It inhibits the function of Niemann-Pick C1-Like 1 protein (NPC1L1) that promotes cholesterol circulation in the blood. Ezetimibe lowers cholesterol in the blood by blocking the action of this protein and thus the amount of cholesterol which can be absorbed from the diet. Ezetimibe can also be prescribed in conjunction with other cholesterol-lowering drugs, called statins to get an even better cholesterol decreasing effect.
Interaction
As with any medication, ezetimibe may interact with other medications or substances. It is important to inform your healthcare provider about all medications you are taking to avoid potential interactions. Some medications that may interact with ezetimibe include cyclosporine, gemfibrozil, and certain statins. Some common interactions Include:
Statins: Ezetimibe is frequently combined with statins to achieve better control over cholesterol levels. Statins work by inhibiting cholesterol synthesis in the liver, while ezetimibe reduces its absorption in the intestine. This combination provides an additive effect in lowering LDL-C levels. However, when used together, there is a slight increase in the risk of liver enzyme elevation or muscle-related side effects like myopathy or rhabdomyolysis, though this risk remains relatively low.
Bile Acid Sequestrants: Drugs like cholestyramine or colesevelam, which bind bile acids in the intestine to lower cholesterol, can interfere with the absorption of ezetimibe. If taken together, ezetimibe should be administered at least two hours before or four hours after bile acid sequestrants to ensure proper absorption.
Fibrates: Fibrates are another class of drugs used to lower triglycerides and also LDL-C to some extent. When combined with ezetimibe, there is a potential increase in the risk of gallstones due to altered bile composition.
Cyclosporine: Ezetimibe may increase the blood levels of cyclosporine, an immunosuppressive drug used in organ transplant patients. Both drugs inhibit cholesterol absorption, and careful monitoring of cyclosporine levels is necessary when using these medications together to avoid toxicity.
Antacids: Antacids may reduce the absorption of ezetimibe, so they should be taken at different times to avoid reducing their efficacy.
Side Effects
Common side effects of ezetimibe may include diarrhoea, stomach pain, fatigue, and muscle pain. These side effects are usually mild and may improve over time as your body adjusts to the medication. However, if you experience severe side effects, such as allergic reactions, muscle weakness, or liver problems, you should seek medical attention immediately.
Ezetimibe - Uses, Interactions, Mechanism Of Action
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