Vytorin: Difference between revisions
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== Pharmacodynamics == | == Pharmacodynamics == | ||
[[Image:Vhrm-8-415f2.jpg|thumb|left|500x500px|alt=A cartoon centipede reads books and types on a laptop.|<b>Figure 1.</b> Within the cell the NPC1L1 transporter senses high level of extracellular cholesterol. At this point it then is taken in along with the cholesterol via endocytosis. When these extracellular cholesterol levels are low however, the NPC1L1 moves back. As seen above, ezetimibe stops the endocytosis from occurring thus preventing cholesterol storage.]] | |||
===<b>Ezetimibe</b>=== | ===<b>Ezetimibe</b>=== | ||
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Simvastatin interferes in the production of cholesterol and is a member of the statin medication family. As a group statins are known to lower a patient's LDL-C levels within their blood. Both patients with and without congestive heart disease (CHD) have experienced a reduction in their cardiovascular morbidity and mortality rights when prescribed medications in this family. <ref>http://e-lactancia.org/media/papers/StatinasFK-FundClinPhar2004.pdf</ref> Generally, simvastatin acts as a competitive inhibitor of HMG-CoA reductase which catalyzes the formation of mevalonate from HMG-CoA in the blood.<ref>https://www.rpi.edu/dept/bcbp/molbiochem/MBWeb/mb2/part1/cholesterol.htm==Mechanism of Action</ref> This is further explained under mechanism of action. | Simvastatin interferes in the production of cholesterol and is a member of the statin medication family. As a group statins are known to lower a patient's LDL-C levels within their blood. Both patients with and without congestive heart disease (CHD) have experienced a reduction in their cardiovascular morbidity and mortality rights when prescribed medications in this family. <ref>http://e-lactancia.org/media/papers/StatinasFK-FundClinPhar2004.pdf</ref> Generally, simvastatin acts as a competitive inhibitor of HMG-CoA reductase which catalyzes the formation of mevalonate from HMG-CoA in the blood.<ref>https://www.rpi.edu/dept/bcbp/molbiochem/MBWeb/mb2/part1/cholesterol.htm==Mechanism of Action</ref> This is further explained under mechanism of action. | ||
==Mechanism of Action== | ==Mechanism of Action== | ||
[[Image: | [[Image:simvastatin.gif|frame|alt=Puzzle globe|<b>Figure 2. </b>In the liver, cholesterol is synthesized through a process of five steps. The second step is the conversion of HMG-CoA into Mevalonate. Simvastatin inhibits this step by attaching to HMG-CoA reductase, keeping it from binding with HMG-CoA. HMG-CoA is unable to convert into mevalonate when HMG-CoA reductase is not available, therefore the production of cholesterol is inhibited.]] | ||
===<b>Ezetimibe</b>=== | ===<b>Ezetimibe</b>=== | ||
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When administered, the drug is inactive until it is absorbed. Upon absorption ezetimibe is conjugated to active phenolic glucuronide where it is metabolized within the small intestine and liver. <ref>https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021445s019lbl.pdf</ref> Ezetimibe limits the internalization of cholesterol by the small intestine. Cholesterol is absorbed into cells with NPC1L1 through clathrin/AP2-mediated endocytosis. AP2 is a multimeric protein that works on the cell membrane to facilitate endocytosis. Ezetimibe inhibits the absorption of cholesterol by blocking the internalization of NPC1L1. <ref>https://www.ncbi.nlm.nih.gov/pubmed/18522832</ref> | When administered, the drug is inactive until it is absorbed. Upon absorption ezetimibe is conjugated to active phenolic glucuronide where it is metabolized within the small intestine and liver. <ref>https://www.accessdata.fda.gov/drugsatfda_docs/label/2008/021445s019lbl.pdf</ref> Ezetimibe limits the internalization of cholesterol by the small intestine. Cholesterol is absorbed into cells with NPC1L1 through clathrin/AP2-mediated endocytosis. AP2 is a multimeric protein that works on the cell membrane to facilitate endocytosis. Ezetimibe inhibits the absorption of cholesterol by blocking the internalization of NPC1L1. <ref>https://www.ncbi.nlm.nih.gov/pubmed/18522832</ref> | ||
===<b>Simvastatin</b>=== | ===<b>Simvastatin</b>=== | ||
