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Topic: Ezetimibe

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	Zetia (ezetimibe) Drug Information by MedicineNet.com (Site not responding. Last check: 2007-09-11)
		Ezetimibe has a different mechanism of action and lowers blood cholesterol by reducing the absorption of cholesterol from the intestine.
		Ezetimibe was approved by the FDA in October, 2002.
		ezetimibe and simvastatin, Vytorin - Vytorin is a combination of ezetimibe (Zetia) and simvastatin (Zocor) that is used for treating high levels of cholesterol in the blood.
	www.medicinenet.com /ezetimibe/article.htm (584 words)

	Lipids Online Slides: ezetimibe, lipid metabolism, mechanism of action
		It is important to consider that ezetimibe therapy may lead to increased LDL receptor expression in individuals with functional LDL receptors, and that this may comprise a component of the mechanism by which ezetimibe lowers plasma LDL cholesterol and triglyceride concentrations.
		Ezetimibe is the first in the class of cholesterol absorption inhibitors, whose mechanism of action is consistent with the binding to and blockade of the putative sterol transporter on the brush border membrane of intestinal epithelial cells.
		Ezetimibe undergoes glucuronidation in the intestine, and both ezetimibe and its active glucuronidated derivative/metabolite circulate enterohepatically (between the intestine and the liver) resulting in repeated delivery to the intestine (the site of pharmacologic action).
	www.lipidsonline.org /slides/slide01.cfm?q=ezetimibe (911 words)

	Ezetimibe, a New Cholesterol Absorption Inhibitor - March 1, 2003 - American Family Physician
		Ezetimibe is a selective cholesterol inhibitor that has recently been approved by the U.S. Food and Drug Administration for this purpose.
		At the end of 12 weeks, the ezetimibe group had a mean reduction in LDL cholesterol levels of 16.9 percent compared with an increase of 0.4 percent in the placebo group.
		The authors conclude that ezetimibe, which is absorbed in the intestine and excreted primarily in the stool, potently inhibits dietary and biliary cholesterol absorption in the intestine.
	www.aafp.org /afp/20030301/tips/1.html (662 words)

	Institute for rational pharmacotherapy Ezetrol (ezetimibe)
		Ezetimibe’s position in lipid reduction therapy, is as a supplement to statins, for patients who have not achieved sufficient LDL-reductions with statin in monotherapy.
		Ezetimibe is indicated as add-on therapy to statin treatment, for patients with primary hypercholesterolemia, homozygous familial hypercholesterolemia and the rare sitosterolemia.
		Ezetimibe is conjugated to the pharmacological active phenol gluconid.
	www.irf.dk /en/reviews/ezetrol__02.htm (1168 words)

	News: New Study Showed VYTORIN(R) (ezetimibe/simvastatin) Significantly More Effective than Crestor(R) (rosuvastatin) ...
		Ezetimibe localizes and appears to act at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver.
		Ezetimibe and ezetimibe-glucuronide are the major drug-derived compounds detected in plasma, constituting approximately 10 to 20% and 80 to 90% of the total drug in plasma, respectively.
		Ezetimibe In clinical studies, administration of ezetimibe, 50 mg/day to 15 healthy subjects for up to 14 days, or 40 mg/day to 18 patients with primary hypercholesterolemia for up to 56 days, was generally well tolerated.
	www.genengnews.com /news/bnitem.aspx?name=2678140 (9174 words)

	Ezetimibe - Drug Interactions and Warnings
		The long-term safety and the effect on cardiovascular morbidity and mortality of ezetimibe are unknown.
		Ezetimibe inhibits cholesterol absorption and promotes a compensatory increase of cholesterol synthesis, followed by clinically relevant reductions in LDL and total cholesterol concentrations.
		Ezetimibe also reduces plasma concentrations of the noncholesterol sterols sitosterol and campesterol, suggesting an effect on the absorption of these compounds as well.
	www.personalhealthzone.com /drug_interactions/ezetimibe.html (349 words)

	Ezetimibe (Zetia)
		Ezetimibe is a lipid-lowering compound approved as an adjunct to diet for the treatment of hypercholesterolemia.
		Ezetimibe acts at the brush border of the small intestine to reduce cholesterol absorption, leading to lower hepatic cholesterol stores and increased clearance of cholesterol from the blood.
		Ezetimibe was studied in placebo controlled trials as monotherapy and in combination with HMG-CoA reductase inhibitors for the treatment of hypercholesterolemia.
	uuhsc.utah.edu /pharmacy/bulletins/ezetimibe.html (518 words)

	Ezetimibe with Simvastatin Provided Significantly Greater Reductions in LDL Cholesterol Compared to Lipitor and Zocor ... (Site not responding. Last check: 2007-09-11)
		Ezetimibe is primarily metabolized in the small intestine and liver via glucuronide conjugation (a phase II reaction) with subsequent biliary and renal excretion.
		Ezetimibe was the major component in feces and accounted for 69% of the administered dose, while ezetimibe-glucuronide was the major component in urine and accounted for 9% of the administered dose.
		Ezetimibe inhibited the absorption of (14)C cholesterol with no effect on the absorption of triglycerides, fatty acids, bile acids, progesterone, ethyl estradiol, or the fat-soluble vitamins A and D. In 4- to 12-week toxicity studies in mice, ezetimibe did not induce cytochrome P450 drug metabolizing enzymes.
	www.burtonsys.com /ezetimibe_simvastatin.htm (8073 words)

	Clinical use of ezetimibe (Site not responding. Last check: 2007-09-11)
		Ezetimibe is a new cholesterol absorption inhibitor that is safe and effective in total cholesterol and LDL-C reduction.
		The combination of ezetimibe and either atorvastatin or simvastatin has also been found to be beneficial in patients with homozygous familial hypercholesterolemia.
		Thus, ezetimibe is a safe and effective addition to the current LDL-C lowering regimen and is most useful in those patients who cannot achieve sufficient LDL-C reduction with an adequate dose of statin alone, cannot tolerate a statin or are fearful of a statin.
	www.pulsus.com /clin-pha/10_SA/chen_ed.htm (667 words)

	Ezetimibe Information on Healthline
		Ezetimibe is used to reduce the amount of total cholesterol, LDL (bad) cholesterol, and apolipoprotein B (a protein needed to make cholesterol) in the blood.
		Ezetimibe is used with a low cholesterol diet and, in some cases, other cholesterol lowering medications.
		Ezetimibe is in the FDA pregnancy category C. This means that it is not known whether ezetimibe will be harmful to an unborn baby.
	www.healthline.com /multumcontent/ezetimibe (845 words)

	Zetia Side Effects, and Drug Interactions - Ezetimibe - RxList Monographs
		The numbers of patients exposed to co-administration therapy as well as fenofibrate and ezetimibe monotherapy were inadequate to assess gallbladder disease risk.
		The degree of increase in ezetimibe exposure may be greater in patients with severe renal insufficiency.
		In patients treated with cyclosporine, the potential effects of the increased exposure to ezetimibe from concomitant use should be carefully weighed against the benefits of alterations in lipid levels provided by ezetimibe.
	www.rxlist.com /cgi/generic/ezetimibe_ad.htm (833 words)

	HealthLINK: Cardiac: New weapon in war against cholesterol - Yale-New Haven Hospital
		Ezetimibe is the first breakthrough to treat cholesterol since statins were introduced 15 years ago.
		Ezetimibe inhibits cholesterol absorption in the intestine, which makes it complementary to the statin drugs, which work in the liver, so patients who take both can achieve additional reductions in LDL and total cholesterol.
		Ezetimibe is the first of a new class of medications that selectively blocks cholesterol uptake in the small intestine, preventing it from being reabsorbed into the bloodstream.
	www.ynhh.org /healthlink/cardiac/cardiac_6_03.html (1753 words)

	First Approval in Europe of Ezetimibe/Simvastatin for treatment of elevated cholesterol (Site not responding. Last check: 2007-09-11)
		When ezetimibe is used with a statin, liver function tests should be performed at the start of therapy and after that in accordance with the label for that statin.
		Due to the unknown effects of the increased exposure to ezetimibe in patients with moderate or severe hepatic insufficiency, ezetimibe is not recommended in these patients.
		Ezetimibe should not be used in pregnant or nursing women unless the benefit outweighs the potential risks.
	www.news-medical.net /?id=273 (858 words)

	Ezetimibe patient advice including side effects
		Ezetimibe may be taken alone or with a statin drug.
		Ezetimibe is not recommended for people with moderate to severe liver disease, or for children under 10.
		Ezetimibe should be taken during pregnancy only if its benefits outweigh the potential risk to the baby.
	www.drugs.com /pdr/EZETIMIBE.html (943 words)

	Ezetimibe/simvastatin for hypercholesterolemia American Family Physician - Find Articles (Site not responding. Last check: 2007-09-11)
		Ezetimibe/simvastatin (vytorin) is a combination of ezetimibe (Zetia), which inhibits the absorption of cholesterol by the small intestine, and simvastatin (Zocor), a 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, or statin.
		Another two studies, (2,6) with a total of 2,690 participants, showed ezetimibe/simvastatin to be more effective than atorvastatin (lipitor) in lowering LDL cholesterol, resulting in an average reduction of 52 to 53 percent compared with 45 percent in both studies with atorvastatin alone.
		Ezetimibe coadministered with simvastatin in patients with primary hypercholesterolemia.
	www.findarticles.com /p/articles/mi_m3225/is_10_72/ai_n15999073 (719 words)

	Clinical Trial: Higher-Dose Ezetimibe to Treat Homozygous Sitosterolemia
		Ezetimibe is a cholesterol-lowering drug that inhibits intestinal absorption of cholesterol and structurally related plant sterols across the intestinal wall.
		Ezetimibe is the first member of a new class of cholesterol-lowering agents that inhibits the intestinal absorption of cholesterol and structurally-related noncholesterol sterols (plant sterols) across the intestinal wall.
		Ezetimibe has proved to be generally safe and well-tolerated as monotherapy or when coadministered with statins, with an overall clinical adverse experience profile similar to placebo.
	www.clinicaltrials.gov /ct/gui/show/NCT00099996 (1433 words)

	Ezetimibe and Simvastatin (Systemic) - MayoClinic.com
		Ezetimibe and Simvastatin (e-ZET-e-mibe and SIM-va-stat-in) is used to lower cholesterol and triglyceride (fat-like substances) levels in the blood.
		Ezetimibe and simvastatin should not be used during pregnancy or by women who plan to become pregnant.
		Your doctor may need to monitor the amount of ezetimibe and simvastatin that you are taking when you are taking either of these medicines.
	www.mayoclinic.com /health/drug-information/DR500567 (1295 words)

	EZETIMIBE/SIMVASTATIN (MDXexchange)
		Ezetimibe is glucuronidated in the intestinal wall; parent drug and its glucuronide conjugate undergo enterohepatic recirculation.
		Area under the curve (AUC) values for ezetimibe were increased approximately 3 to 4-fold and 5 to 6-fold in patients with moderate (Child-Pugh score, 7 to 9) and severe (Child-Pugh score, 10 to 15) hepatic impairment, respectively.
		Ezetimibe has been proven to be effective in combination with statins in patients unable to achieve or sustain target LDL levels on a statin alone or to reduce the dose of a statin required to achieve target levels.
	www.micromedex.com /products/updates/drugdex_updates/de/ezetimibe.html (4143 words)

	FDA approves ezetimibe for cholesterol reduction (Site not responding. Last check: 2007-09-11)
		The mechanism of ezetimibe is quite different from a currently available class of drugs known as "bile acid sequestrants," which lower cholesterol by physically binding to bile acids in the small intestine.
		Ezetimibe lowers cholesterol through a unique mechanism of action by inhibiting cholesterol absorption in the intestine.
		In clinical trials, ezetimibe was generally well tolerated with an overall side effect profile similar to placebo.
	www.pharmacist.com /articles/h_ts_0137.cfm (186 words)

	Ezetimibe
		You may not be able to take ezetimibe, or you may require a dosage adjustment or special monitoring during treatment.
		Ezetimibe should be taken 2 hours before or 4 hours after a bile acid sequestrant such as cholestyramine (Locholest, Prevalite, Questran), colestipol (Colestid), or colesevelam (Welchol).
		You may not be able to take ezetimibe, or you may require a dosage adjustment or special monitoring during treatment if you are taking any of the medications listed above.
	www.drugs.com /ezetimibe.html (1047 words)

	DG DISPATCH - ACC: New Drug, Ezetimibe, Lowers Cholesterol With Few Side Effects (Site not responding. Last check: 2007-09-11)
		She said that of the 242 patients treated with ezetimibe in this study, more than 50 percent were able to achieve a greater than 15 percent reduction in low density lipoprotein (LDL) and 15 percent of patients lowered LDL by 25 percent.
		"Ezetimibe is taken once-a-day and it can be taken any time of day, with meals or by itself," she said.
		She said trials are underway that may pave the way for ezetimibe to be approved by the Food and Drug Administration.
	www.pslgroup.com /dg/18f326.htm (466 words)

	Ezetimibe - Drugs & Vitamins - Drug Library - DrugDigest (Site not responding. Last check: 2007-09-11)
		EZETIMIBE (Zetia®) blocks the absorption of cholesterol from the stomach.
		Ezetimibe can help lower blood cholesterol for patients who are at risk of getting heart disease or a stroke.
		If you are taking a 'resin' type medication (like cholestyramine, colesevelam, or colestipol) to lower your cholesterol, you should take ezetimibe at least 2 hours before or 4 hours after you take the 'resin' medication.
	www.drugdigest.org /DD/DVH/Uses/0,3915,551491\|Ezetimibe,00.html (639 words)

	IngentaConnect Efficacy and safety of ezetimibe coadministered with simvastatin ...
		Ezetimibe, an intestinal cholesterol absorption inhibitor, has a mechanism of action that differs from that of statins, which inhibit hepatic cholesterol synthesis.
		Ezetimibe plus simvastatin 20 mg also produced significant incremental reductions in non-HDL-C (p < 0.001), very low-density lipoprotein cholesterol (p < 0.05) and apolipoprotein B (p < 0.001) relative to simvastatin 40 mg.
		Co-administration of ezetimibe with simvastatin, a dual inhibition treatment strategy targeting both cholesterol synthesis and absorption, is well tolerated and provides greater LDL-C-lowering efficacy than increasing the dose of simvastatin in T2DM patients taking TZDs.
	www.ingentaconnect.com /content/bsc/dom/2005/00000007/00000001/art00012 (428 words)

	Clinical Trial: Ezetimibe and Simvastatin in Dyslipidemia of Diabetes
		Preliminary data suggest that ezetimibe, combined to a drug that blocks the cholesterol synthesis (statins), could be even more effective in decreasing cholesterol concentration.
		Ezetimibe is the first member of a class of highly selective cholesterol absorption inhibitors that effectively and potently prevents the absorption of cholesterol by inhibiting the passage of biliary and dietary cholesterol across the wall of small intestine, without affecting absorption of other fat-soluble nutrients.
		Phase I/II studies on patients with hypercholesterolemia have explored the safety and efficacy of ezetimibe mono-therapy and co-administration with simvastatin.In these studies, combined therapy was safety and invariably more effective than single therapy in ameliorating the lipid profile.
	www.clinicaltrials.gov /ct/gui/show/NCT00157482 (973 words)

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