Ezetimibe

BRAND NAMES:

Ezetrol -The main active ingredient is Ezetimibe available as Ezetrol ezetimibe 10mg tablets which helps in medication of high cholesterol levels.

Lypqozet - Lypqozet is a combinational drug containing atorvastatin calcium trihydrate and ezetimibe in the form of tablets, dosage ranging from 10/10 mg/day to 10/80 mg/day. It is mainly administered to patients who require a larger reduction of bad cholesterol LDL-C.

Nexlizet - It is a combinational drug of two active ingredients bempedoic acid and ezetimibe. Available as Nexlizet bempedoic acid and ezetimibe 180mg/10mg tablets. It is used in the case of patients who have high bad cholesterol levels.

Roszet - It is a combined medication of rosuvastatin. It is often used as a nonstatin drug, reducing LDC-C levels by 13% to 20%. It is also used in people with high blood fat levels, either in conjunction with a diet or alone with other cholesterol-lowering medicines. It prevents cholesterol from being absorbed in the gut. Lowering your blood cholesterol and fat levels may help you avoid heart disease, chest pain, strokes, and heart attacks. And ezetimibe, which is marketed under the brand name Roszet. These come in strengths of 5mg/10mg, 10mg/10mg, 20mg/10mg, and 40mg/10mg.

Vytorin- It is a combination of two drugs ezetimibe and simvastatin. It is used in treating high-level cholesterol in adults and children.

Zetia – Ezetimibe is an active ingredient present in Zetia which helps in treating patients suffering from high level cholesterol.

MECHANISM OF ACTION:

Cholesterol is produced in the liver and absorbed through the gastrointestinal tract. Ezetimibe, a synthetic 2-azetidine drug, differs from other cholesterol-lowering medications in that it does not promote bile acid excretion or prevent cholesterol synthesis in the liver. It absorbs cholesterol at the small intestinal barrier via the sterol transporter.  The decrease in cholesterol absorption reduces cholesterol supply to the liver while increasing cholesterol clearance from the bloodstream. The lowering of cholesterol absorption lowers total cholesterol, triglycerides, and LDL cholesterol while increasing HDL cholesterol.

PHARMACOKINETICS:

Absorption - After oral treatment, ezetimibe is absorbed and transformed into a pharmacologically active compound called ezetimibe-glucuronide.It takes 4 to 2 hours to reach the peak plasma concentration. The highest plasma concentrations of ezetimibe glucuronide occur within 1 to 2 hours. Taking meals with ezetimibe does not affect absorption.

Distribution- Ezetimibe and ezetimibe glucuronide complexes are more than 90% protein bound.

Metabolism- It is rapidly metabolized into ezetimibe glucuronide, detected in plasma. Plasma concentration-time profiles show multiple peaks and enterohepatic recycling. The enzyme CYP45 metabolizes ezetimibe, but it has little effect on other drugs because it is quickly conjugated and excreted in the bile as a glucuronide.

Excretion – Ezetimib is primarily excreted in feces and ezetimibe b glucuronide is excreted through urine.

PHARMACODYNAMICS: 

This therapeutic effect was greater when ezetimibe was combined with a statin or fenofibrate than when either therapy was given alone. The recommended therapeutic dose of ezetimibe was successful in lowering LDL levels by 15-20% and boosting HDL-C by 2.5-5%.

DOSAGE AND ADMINISTRATION:

It is an orally administered drug which is available at 10mg. It can be administered with or without food with a cholesterol-lowering drug. The recommended time before taking ezetimibe is 2 to 4 hours after taking bile acid sequestrants.

Ezetimibe is not suggested for patients suffering from moderate to severe renal impairment.

No dose adjustment is required with patients with renal impairment.

CONTRAINDICATIONS: 

Contraindications to ezetimibe include hypersensitivity to any formulation component, concurrent treatment with an HMG-CoA reductase inhibitor in individuals with active hepatic illness, and unexplained persistent increases in blood transaminases. It is also contraindicated during pregnancy and breastfeeding. Ezetimibe has been associated with hypersensitivity responses such as angioedema and anaphylaxis.

DRUG INTERACTIONS:

Have to make sure to discuss this with the physician before starting the treatment with  Ezetamibe.It can be taken at any time of the day.

The below medicines are not recommended with ezetimibe.

•           Cyclosporine

•           Dnazol

•           Gemfibrozil

•           Some medicines are not recommended with Ezetimibe but in some situations, both together should be taken by decreasing the dose 

•           Bezafibrate

•           Cholestyramine

•           Ciprofibrate

•           Cholestyramine

•           Ciprofibrate

•           Colesevelam

•           Colestipol

•           Simeprevir

•           fenofibric acid

FOOD INTERACTIONS:

Taking this medicine with or without food doesn’t affect food absorption.

ADVERSE EFFECTS:

•           Racing Heart

•           Swollen lymph nodes

•           Stomach cramps

•           Trouble swallowing

•           Throat tightness

•           Gaseous stomach pain

•           Indigestion

•           Itching skin rash, hives

•           Tiredness

•           Joint pains

•           Influenza

•           Infection in the nose, throat

OVERDOSE:

Symptoms may include 

•           Stomach pain

•           Nausea

•           Dizziness

•           Vomiting

STORAGE:

Maintain room temperature between 59℉ and 86℉ (15℃ and 30℃). Keep away from high temperatures..