Miscellaneous Agents

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Chapter: Medicinal Chemistry : Antihyperlipidaemic Agents

Antihyperlipidaemic Agents : i. β-Sitosterol ii. Dextrothyroxine iii. Ezetimibe - Synthesis and Drug Profile


SYNTHESIS AND DRUG PROFILE


Miscellaneous Agents


i. β-Sitosterol


Properties and uses: β-sitosterol lowers plasma concentrations of LDL, and has no effect on VLDL. The sitosterol is believed to lower plasma levels of cholesterol by interfering with its absorption. It is used as an anticholesteremic agent and also used in the treatment of prostatic adenoma.


ii. Dextrothyroxine


Synthesis


Uses: Used as antihyperlipidaemic agent.


iii. Ezetimibe


Metabolism of ezetimibe: It is metabolized rapidly and extensively in the intestinal wall and the liver to its active metabolite, a corresponding phenol glucuronide. This glucuronide is re-excreted in the bile back to its active site. A small amount of Ezetimibe undergoes oxidation to convert the benzylic hydroxyl group to a ketone. Ezetimibe does not appear to exert any significant effect on the activity of CYP450 enzyme.

Uses: Used as an antihyperlipidaemic agent.


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