Ezetimibe dosage

Ezetimibe and 10 mg/10 mg, The dosage range is See entries on prior page for each drug (ezetimibe and... 

Dose The recommended usual starting dose is 10 mg ezetimibe/20 mg simvastatin daily. Initiation of therapy with 10 mg ezetimibe/10 mg simvastatin daily may be considered for patients requiring less aggressive LDL-C reductions. Patients who require a larger reduction in LDL-C (more than 55%) may be started at 10 mg ezetimibe/40 mg simvastatin daily. After initiation or titration of ezetimibe/simvastatin, lipid levels may be analyzed after 2 or more weeks and dosage adjusted, if needed. 

Homozygous familial hypercholesterolemia The recommended dosage for patients with homozygous familial hypercholesterolemia is 10 mg ezetimibe/40 mg simvastatin daily or 10 mg ezetimibe/80 mg simvastatin daily in the evening. Use ezetimibe/simvastatin as an adjunct to other lipid-lowering treatments (eg, LDL apheresis) in these patients or if such treatments are unavailable. 

The effect of ezetimibe on cholesterol absorption is constant over the dosage range of 5-20 mg/d. Therefore, a single daily dose of 10 mg is used. Average reduction in LDL cholesterol with ezetimibe alone in patients with primary hypercholesterolemia is about 18%, with minimal increases in HDL cholesterol. It is also effective in patients with phytosterolemia. Ezetimibe is synergistic with reductase inhibitors, producing decrements as great as 25% in LDL cholesterol beyond that achieved with the reductase inhibitor alone. 

There are few spectrophotometric methods published to determine ezetimibe in pharmaceutical dosage forms. The first one was established by Mishra et al. [17] by applying colorimetric assay of phenol group. This method was developed based on the reaction between Folin-Ciocalteu s (FC) phenol reagent and phenol group of ezetimibe, which results in a blue chromogen that was then observed at 760 nm. 

Another spectrophotometric method used the derivative method. Rajput and Raj [19] developed a first-order derivative zero-crossing method to analyze ezetimibe in combination with simvastatin. This method was further applied to determine ezetimibe in combination with lovastatin. The first derivation method also applied to determine ezetimibe in combination with rosuvastatin [20]. Besides the first-derivative method, second- and third-derivative methods were also reported for defermining ezetimibe as a single compound in its dosage form [21]. Flowever, the third-derivative method yielded the lowest limits of defecfion and quantitation relative to other methods used in this research. The maximum wavelength also remained constant regardless of fhe derivative method applied. 

TABLE 3.6 Summary of TLC/HPTLC methods for analysis of ezetimibe in bulk and pharmaceutical dosage forms... 

TABLE 3.8 Summary of MEKC method for analysis of ezetimibe in pharmaceutical dosage form... 

The actions of ezetimibe are complementary to those of statins. Statins, which inhibit cholesterol biosynthesis, increase intestinal cholesterol absorption. Ezetimibe, which inhibits intestinal cholesterol absorption, enhances cholesterol biosynthesis by as much as 3.5 times in experimental animals. Dual therapy with these two classes of drugs prevents the enhanced cholesterol synthesis induced by ezetimibe and the increase in cholesterol absorption induced by statins. This combination provides additive reductions in LDL-C levels irrespective of the statin employed. There is a further reduction of 15 to 20% in LDL-C when ezetimibe is combined with any statin at any dose. Increasing statin dosages from the usual starting dose of 20 mg to 80 mg normally yields only an additional 12% reduction in LDL-C, whereas adding ezetimibe, 10 mg daily, to 20 mg of a statin will reduce LDL-C by an additional 18 to 20%. 

The normal dose of ezetimibe is 10 mg once daily. Dosage reduction for patients with renal impairment, intermittent hemodialysis, or mild hepatic impairment is not necessary. Because of insufficient data, the use of ezetimibe is not recommended in patients with moderate to severe hepatic impairment (15,20,21). 

Therefore it seems that ciclosporin can greatly raise ezetimibe levels, possibly resulting in an increased effect on lipid reduction, and that ciclosporin levels can be raised, possibly significantly in some patients, by ezetimibe. If concurrent use is necessary, until the effects of concurrent treatment are better established, it would seem prudent to monitor both ciclosporin levels and the effects on lipid levels, anticipating the need to reduce the dosage of either drug. The authors of the case report cited sug-... 

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