Pharmacokinetic and Pharmacodynamic Interactions Between the Cholesterol-lowering Ezetimibe and the Non-nucleoside Reverse Transcriptase Inhibitor Efavirenz During Chronic Treatment in Healthy Volunteers With Reference to Intestinal Expression of CYP3A4, UGT1A1, ABCB1 and ABCC2 - Full Text View. Pharmacokinetics do not appear to be affected by age, gender, race, or weight. It is the first available 2-azetidinone compound, a potent cholesterol absorption inhibitor. Ezetimibe pharmacokinetics influenced by single-dose rifampicin Download PDF. Rosuvastatin Rosuvastatin is an inhibitor of HMG CoA-reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl coenzyme A to mevalonate, a precursor of cholesterol. Concomitant fenofibrate administration significantly increased the mean C max and AUC of total ezetimibe approximately 64% and 48%, respectively. Subjects. The aims of this study were to assess the pharmacokinetics and safety of an ezetimibe/simvastatin combination tablet after oral single-dose administration in healthy Chinese subjects including sex-related differences in pharmacokinetics. Mechanistic studies on metabolic interactions between gemfibrozil and statins. Clin Ther. Listing a study does not mean it has been evaluated by the U.S. Federal Government. Recent clinical research has shown that atorvastatin (ATO) in combination with cholesterol absorption inhibitor ezetimibe (EZE) significantly reduces LDL-C level in patients with hypercholesterolemia, showing a superior lipid-lowering efficacy compared to statin alone. Ezetimibe. This study aimed to compare the pharmacokinetics of fixed-dose combination (FDC) tablet of rosuvastatin 20 mg/ezetimibe 10 mg with that of concurrent administration of individual rosuvastatin 20 mg tablet and ezetimibe 10 mg tablet in healthy subjects. 10 mg daily. 31 Ezetimibe is unlikely to cause drug interactions with common CYP450 substrates. How does Ezetimibe work? The ed50 was fairly low and in a similar range as lamuvidine. Ezetimibe blocks the absorption of dietary and biliary cholesterol and plant sterols resulting in intracellular cholesterol depletion. The apparent decrease in fluvastatin exposure on administration with ezetimibe was likely to be due to the parallel study design and two pharmacokinetic outliers and is considered of no clinical significance. 2005;44 (5):467-94. A randomized, open label, single-dose, two-way crossover study was conducted. The primary metabolic pathway for ezetimibe is by glucuronidation of the 4-hydroxyphenyl group. This was an open-label, single-dose study. Background: Ezetimibe is a cholesterol absorption inhibitor which decreases low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia. Following oral administration, ezetimibe is rapidly . Compare the Pharmacokinetics of NVP-1205 and Coadministration of Rosuvastatin and Ezetimibe (NVP-1205) The safety and scientific validity of this study is the responsibility of the study sponsor and investigators. Ezetimibe is neither an inhibitor nor an inducer and only a minor substrate of common cytochrome P450 (CYP) drug-metabolising isoenzymes (1A2, 2D6, 2C8, 2C9 and 3A4). Ezetimibe is a novel cholesterol-lowering drug that acts at the brush border of the small intestine. The recent . %Excreted unchanged in urine : 11. This is a nice advantage because this is a starting dose and the usual treatment dose. 31 Ezetimibe is unlikely to cause drug interactions with common CYP450 substrates. Ezetimibe is an oral antilipemic agent, approved for use as monotherapy or in combination with HMG-CoA reductase inhibitors ('statins') or fenofibrate for the treatment of hypercholesterolemia. DOSE IN NORMAL RENAL FUNCTION. Ezetimibe is a medication used in the management and treatment of hypercholesterolemia. Ezetimibe does not affect the pharmacokinetics or pharmacodynamics of warfarin. Methods Ezetimibe is the first member of a new class of selective cholesterol absorption inhibitors. Studies in Asian subjects indicated that the pharmacokinetics of ezetimibe were similar to those seen in Caucasian subjects. Pharmacology and Pharmacokinetics. Read More. Ezetimibe Tablets given concomitantly with a statin is contraindicated in patients with active liver disease or unexplained persistent elevations of hepatic transaminase levels [see . Common ezetimibe side effects may include: diarrhea; cold symptoms such as stuffy nose, sneezing, sore throat; pain in an arm or leg; joint pain; or. There was an in vitro study on ezetimibe inhibiting HBV DNA production. In in vivo and in vitro studies, rosuvastatin produces its lipid-modifying effects in two . Ezetimibe Based on a meta-analysis of multiple-dose pharmacokinetic studies, there were no pharmacokinetic differences between Black and Caucasian subjects. [Google Scholar] 21. Hepatic Impairment. A randomized, open label, single-dose, two-way crossover study was conducted. Total ezetimibe pharmacokinetics was best described by a four-compartment model featuring EHC through the inclusion of an additional gallbladder compartment, which was assumed to release drug at . Ezetimibe/simvastatin fixed-combination preparation is bioequivalent to . Ghosal A . Volunteers; Published: 02 February 2013; Ezetimibe pharmacokinetics influenced by single-dose rifampicin. J Pharmacol Exp Ther. Ezetimibe tablets are indicated as adjunctive therapy to diet for the reduction of elevated sitosterol and campesterol levels in patients with homozygous familial sitosterolemia. With no information currently available on the interaction between the two drugs, a pharmacokinetic study was conducted to . Jeu L, Cheng JW. But in an in vitro study you have a constant exposure to the drug, which is . C: The elimination half-life refers to the time it takes for half of the dose to be absorbed through the gut lining. Clin Ther. Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Prueksaritanont T, Zhao JJ, Ma B, et al. muscle pain while taking ezetimibe with a statin. Ezetimibe is the first member of a novel class of lipid-lowering agents that selectively inhibits the absorption of biliary and dietary cholesterol as well as other phytosterol from the intestine without affecting the absorption of fat-soluble vitamins, triglycerides or bile acids. The active metabolite is at least as potent as. Prueksaritanont T, Zhao JJ, Ma B, et al. This study investigated the potential for pharmacodynamic and/or pharmacokinetic interactions between ezetimibe and lovastatin. Ezetimibe is the first of a new class of lipid-lowering drugs, the 2-azetidinones, which selectively inhibits the absorption of intestinal cholesterol. The pharmacokinetics of ezetimibe Abstract Ezetimibe is the first member of a new class of selective cholesterol absorption inhibitors. Homozygous Sitosterolemia (Phytosterolemia): Ezetimibe is indicated as adjunctive therapy to diet for use in patients with homozygous familial sitosterolemia Pharmacology Ezetimibe localises at the brush border of the small intestine and inhibits absorption of cholesterol via the sterol transporter, Niemann-Pick C1-Like1 (NPC1L1). Can J Clin Pharmacol. 2005. Concomitant fenofibrate administration significantly increased the mean C(max) and AUC of total ezetimibe approximately 64% and 48%, respectively. Ezetimibe [SCH 58235; 1-(4-fluorophenyl)-3( R )-[3-(4-fluorophenyl)-3( S )-hydroxypropyl]-4( S )-(4-hydroxyphenyl)-2-azetidinone], a . Call your doctor for medical advice about side effects. Pharmacology and therapeutics of ezetimibe (SCH 58235), a cholesterol-absorption inhibitor. Ezetimibe's mechanism of action complements . Absorption Bioavailability. 5,6,7 It is also indicated to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia in . The pharmacokinetics of ezetimibe are consistent with extensive glucuronidation and enterohepatic recirculation. Abstract Ezetimibe is an inhibitor of cholesterol absorption that is liver glucuronized after its rapid absorption, and is mobilized to the enterocytes, where together with its metabolites it exerts hypolipidemic effects, avoiding the absorption of cholesterol, through the reduction of specific cholesterol-transporter enzymes in the gut. [Google Scholar] 21. B: If a drug is eliminated via zero order kinetics, the half life is always the same. Pharmacology Indication. Low-density lipoprotein cholesterol (LDL-C), high-density lipoprotein cholesterol (HDL-C) and total cholesterol (TC) were investigated for the PD assessments on day 1 (pretreatment) and day 8. However, based on the established safety profile and flat dose-response of ezetimibe, this effect is not considered to be . Pharmacokinetics generally linear over dose range of >60 mg to 220 mg; no time-dependent changes observed following repeated administration at recommended dosage. A secondary outcome was the potential for a pharmacokinetic interaction between ezetimibe and fenofibrate. existing gastrointestinal diseases and/or pathological findings which might interfere with safety, pharmacodynamic effect and/or pharmacokinetics of ezetimibe and sirolimus acute or chronic diseases which could affect drug absorption or metabolism Ezetimibe is administered orally. The pharmacokinetics of ezetimibe. Inpharma Weekly volume 1571, page 19 (2007 . pharmacokinetics of ezetimibe were similar to those seen in Caucasian subjects. Genetic variability may also affect the pharmacokinetics of ezetimibe. 2002; 301:1042-51. , Kosoglou T, Statkevich P, et al. Ezetimibe is metabolized by the P450 system, but has little effect on the pharmacokinetics of other drugs, perhaps because it is rapidly conjugated and excreted in the bile as a glucuronide. Pharmacology and therapeutics of ezetimibe (SCH 58235), a cholesterol-absorption inhibitor. PHARMACOKINETICS. The results of a bioequivalence study in healthy subjects demonstrated that the VYTORIN (ezetimibe/simvastatin) 10 mg/10 mg to 10 mg/80 mg combination tablets are bioequivalent to coadministration of corresponding doses of ezetimibe (ZETIA®) and simvastatin (ZOCOR®) as individual tablets. Mechanism of Action of Ezetimibe It reduces the absorption of cholesterol from the intestine by localising at the brush border of the small intestine, where it inhibits the absorption of cholesterol from the diet. The pharmacokinetics of ezetimibe. 2003;25 (9):2352 . Ezetimibe has a unique mechanism of action compared to other classes of lipid-lowering agents. Ezetimibe Results: Ezetimibe did not significantly affect the pharmacokinetics of fenofibrate. Jeu L, Cheng JW. Ezetimibe was found to have a 50%inhibition conc of 25micromolar, while irbesartan, a commonly used angiotensin inhibitor to reduce blood pressure, was found to inhibit at 11.9 micromolar. A: The half-life is the time required for the plasma concentration of the drug to decrease by 50%. Cases of an autoimmune hepatitis-like syndrome suggest immune mediated injury may be the cause of some clinically apparent liver injury due to ezetimibe. Ezetimibe has a unique mechanism of action compared to other classes of lipid-lowering agents. Ezetimibe is the first of the cholesterol absorption inhibitors, a novel class of lipid modifying drugs, which potently inhibit the absorption of biliary and dietary cholesterol from the small intestine without affecting the absorption of fat-soluble vitamins, triglycerides or bile acids. The drug and its active glucuronide metabolite impair the intestinal reabsorption of both dietary and hepatically excreted biliary cholesterol through inhibition of a membrane transporter yet to be identified. EZETIMIBE Monographs. Journal. Ghosal A . Pharmacology and Pharmacokinetics. Ezetimibe is a cholesterol absorption inhibitor which decreases low-density lipoprotein cholesterol (LDL-C) in patients with hypercholesterolemia. Dr Arthur J. Bergman PhD, Corresponding Author. March 6-10, 2001. Download PDF. [Google Scholar] 20. OBJECTIVE The pharmacokinetic profiles and bioequivalence of a new rosuvastatin/ezetimibe fixed-dose combination (FDC; NVP-1205) vs. rosuvastatin and ezetimibe concomitantly administered as single agents were evaluated. Ezetimibe is a white, crystalline powder that is freely to very soluble in ethanol, methanol, and acetone and practically insoluble in water. Absolute bioavailability cannot be determined because ezetimibe is virtually insoluble in aqueous media suitable for injection. Ezetimibe About Ezetimibe Cholesterol Absorption Inhibitor, 2-Azetidinone derivative, Hypolipidemic agent. : 2 Departmenrt of Clinical . In this study ezetimibe pharmacokinetics were not fully characterized since after oral administration of ezetimibe 0.25 and 1 mg day −1 plasma drug concentrations for ezetimibe and total ezetimibe were expected to be too low relative to the assay LOQ to adequately characterize a pharmacokinetic profile. 27,31 No changes in the pharmacokinetics of statins, warfarin, digoxin, ethinyl estradiol or glipizide were . 2003; 10 (Suppl A):13A-20. Ezetimibe and ezetimibe-glucuronide are highly bound (greater than 90%) to human plasma proteins. This is not a complete list of side effects and others may occur. Dr Arthur J. Bergman PhD. This activity describes the indications, actions, and contraindications for ezetimibe as a valuable agent in the treatment of hypercholesterolemia. The plasma concentrations of rosuvastatin, total ezetimibe and free ezetimibe were measured for 72 h after day 7. Pharmacokinetic drug interaction between atorvastatin and ezetimibe in healthy Korean volunteers Jungsin Park, 1 Choon Ok Kim, 2 Byung Hak Jin, 1, 2 Seoungwon Yang, 3 Min Soo Park, 1, 2, 4 and Taegon Hong 2 1 Department of Pharmaceutical Medicine and Regulatory Sciences, Colleges of Medicine and Pharmacy, Yonsei University, Incheon 21983, Republic of Korea. Total ezetimibe pharmacokinetics was best described by a four-compartment model featuring EHC through the inclusion of an additional gallbladder compartment, which was assumed to release drug at . Can J Clin Pharmacol. [ 26] Limitations of Use The effect of Ezetimibe tablets on cardiovascular morbidity and mortality has not been determined. It inhibits the absorption of dietary and biliary cholesterol decreasing the intestinal absorption by 54%. The primary objectives of this study were to evaluate the pharmacodynamic effects and safety of the co-administration of ezetimibe and the new statin rosuvastatin. The pharmacokinetics of ezetimibe in adolescents (10 to 18 years) have been shown to be similar to that in adults. Treatment with ezetimibe Upon oral administration, ezetimibe is absorbed and conjugated to a pharmacologically active phenolic glucuronide, ezetimibeglucuronide (15,16). Ezetimibe does not have significant effects on plasma levels of HMG-CoA reductase inhibitors commonly known as statins, and coadministration with gemfibrozil and fenofibrate increased the bioavailability of ezetIMibe, but the clinical significance is thought to be minor. Ezetimibe has a melting point of about 163°C and is stable at ambient temperature. The estimated terminal half-life of ezetimibe and ezetimibe-glucuronide is approximately 22 hours. Background: Ezetimibe is a lipid-lowering drug indicated for the treatment of hypercholesterolemia as co-administration with HMG-CoA reductase inhibitors (statins) or as monotherapy. ZETIA is available as a tablet for oral administration containing 10 mg of ezetimibe and the Both compounds have similar MW, but irbesartan is given at up to 300mg per day, while exetimibe is dosed at 10mg. zetia. SUMMARY. [Google Scholar] 20. Bempedoic Acid Pharmacokinetics. Rosuvastatin and Ezetimibe - Clinical Pharmacology Mechanism of Action. Both ezetimibe and ezetimibe-glucuronide are slowly eliminated from the plasma with a half-life of about 22 hours. Results: This study investigated the potential for pharmacodynamic and/or pharmacokinetic interactions between ezetimibe and lovastatin. Mechanistic studies on metabolic interactions between gemfibrozil and statins. The aim of this study was to compare the pharmacokinetic (PK) profiles of an FDC tablet of rosuvastatin/ezetimibe and co-administration of rosuvastatin and ezetimibe as separate tablets in healthy Korean volunteers. After a single dose, mean ezetimibe peak plasma concentrations (C max) of 3.4 to 5.5 ng/ mL were obtained within 4 to 12 hours (T max ). 27,31 No changes in the pharmacokinetics of statins, warfarin, digoxin, ethinyl estradiol or glipizide were . Clinical Pharmacokinetics - Springer Journals. Poster presented at: American Society of Clinical Pharmacology and Therapeutics. They place more emphasis on a target LDL and getting patients to goal. It is among a novel class of selective cholesterol-absorption inhibitors. The rosuvastatin/ezetimibe (10/10 mg) FDC was bioequivalent to single agents concomitantly administered and well tolerated, with no serious adverse events reported. Ezetimibe did not significantly affect the pharmacokinetics of fenofibrate. 2002; 301:1042-51. Zetia (Ezetimibe) is used to treat Hypercholesterolemia or high LDL levels. Effects of Ezetimibe on Cyclosporine Pharmacokinetics in Healthy Subjects. The drug and its active glucuronide metabolite impair the intestinal reabsorption of both dietary and hepatically excreted biliary cholesterol through inhibition of a membrane transporter yet to be identified. Ezetimibe | C24H21F2NO3 | CID 150311 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety . Hepatic Impairment : After a single 10-mg dose of ezetimibe, the mean AUC for total ezetimibe was increased approximately 1.7-fold in patients with mild hepatic impairment (Child-Pugh score 5 to 6), compared to healthy . Based on a meta-analysis of multiple-dose pharmacokinetic studies, there were no pharmacokinetic differences between Black and Caucasian subjects. Ezetimibe possesses unique pharmacokinetic properties that minimise its potential for significant drug-drug interaction with other coadministered medications. 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. Treatment experience with ezetimibe in the pediatric population is limited to 4 patients (9 to 17 years) in the sitosterolemia study and 5 patients (11 to 17 years) in the HoFH study. Both ezetimibe and ezetimibe glucuronide are substrates for the efflux pumps, ABCB1 and ATP-binding cassette, subfamily C, member 2 (ABCC2). Studies in Asian subjects indicated that the pharmacokinetics of ezetimibe were similar to those seen in Caucasian subjects. Approximately 93% of dose is absorbed systemically following oral administration. Ezetimibe is primarily metabolized by UDP glucuronosyltransferase 1 family, polypeptide A1 (UGT1A1) [181] . Ezetimibe is the first lipid-lowering drug that inhibits intestinal uptake of dietary and biliary cholesterol without affecting the absorption of fat-soluble nutrients. Ezetimibe. PHARMACOKINETICS. Compared with separate tablets, fixed-dose combination (FDC) tablets of rosuvastatin/ezetimibe could increase patient compliance. Consistent with the elimination half-life of ezetimibe, an approximate 2-fold accumulation is observed upon repeated once-daily administration. The pharmacokinetics of ezetimibe were not affected by coadministration with fluvastatin. CLINICAL USE. Molecular weight :409.4. Merck Research Laboratories, Rahway, New Jersey, and West Point, Pennsylvania. Ezetimibe is the first lipid-lowering drug that inhibits intestinal uptake of dietary and biliary cholesterol without affecting the absorption of fat-soluble nutrients. Clinical pharmacokinetics. Ezetimibe is dosed at 10 mg once daily. Absorption Ezetimibe Clin Pharmacokinet. J Pharmacol Exp Ther. Pharmacokinetics. Following systemic absorption, ezetimibe is extensively conjugated to a pharmacologically active phenolic glucuronide (ezetimibe-glucuronide). The recent . Ezetimibe is indicated to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with primary hyperlipidemia, alone or in combination with an HMG-CoA reductase inhibitor (statin). Ezetimibe does not, however, affect triglyceride absorption. Common Questions and Answers about Ezetimibe pharmacokinetics. Hepatic Insufficiency After a single 10-mg dose of ezetimibe, the mean area under the curve (AUC) for total ezetimibe was increased approximately 1.7-fold in patients with mild hepatic insufficiency (Child-Pugh score 5 to 6), compared to healthy subjects. So it looked very interesting. Hypercholesterolaemia either in combination with a statin or as monotherapy. %Protein binding :99.7. To evaluate the pharmacokinetic interactions among rosuvastatin, ezetimibe, and telmisartan, a randomized, open-label, 3-period, 6-sequence crossover study was conducted in healthy subjects. PHARMACOKINETICS Ezetimibe, which is water insoluble, is absorbed and extensively conjugated to an active phenolic glucuronide (ezetimibeglucuronide) after oral intake. Effects of ezetimibe on the pharmacodynamics and pharmacokinetics of lovastatin The co-administration of ezetimibe and lovastatin was well tolerated and resulted in a significantly greater percentage reduction in serum LDL-C concentrations than with lovastatin alone, with an average incremental reduction of 16-18%. Subjects randomly received test formulation (FDC tablet of . Pharmacokinetics Within 4-12 hours of the oral administration of a 10-mg dose to fasting adults, the attained mean ezetimibe peak plasma concentration ( C max) was 3.4-5.5 ng/ml. With the most recent cholesterol guideline updates, I do expect ezetimibe to be utilized a little more than it used to be. Following oral administration, ezetimibe is rapidly absorbed and extensively metabolised (>80%) to the pharmacologically active ezetimibe-glucuronide. 2003;25 (9):2352 . Ezetimibe Pharmacokinetics Absorption Bioavailability. It demonstrated less and variable oral bioavailability. Studies in Asian subjects indicated that the pharmacokinetics of ezetimibe were similar to those seen in Caucasian subjects. Anti-hyperlipidemia therapy seeks t. Abstract. This study aimed to compare the pharmacokinetics of fixed-dose combination (FDC) tablet of rosuvastatin 20 mg/ezetimibe 10 mg with that of concurrent administration of individual rosuvastatin 20 mg tablet and ezetimibe 10 mg tablet in healthy subjects. It inhibits the absorption of dietary and biliary cholesterol decreasing the intestinal absorption by 54%. Orlando, FL, U.S.A. TLDR. Ezetimibe pharmacokinetics. existing gastrointestinal diseases and/or pathological findings which might interfere with safety, pharmacodynamic effect and/or pharmacokinetics of ezetimibe and sirolimus acute or chronic diseases which could affect drug absorption or metabolism Ezetimibe Tablet is not recommended in patients with moderate to severe hepatic impairment [see Warnings and Precautions (5.4) and Clinical Pharmacology (12.3)]. Following oral administration, ezetimibe is absorbed and extensively conjugated to a phenolic glucuronide (active metabolite). 2003; 10 (Suppl A):13A-20. Recent studies have further identified the molecular target as the Niemann-Pick C1-like transporter. Ezetimibe does not, however, affect triglyceride absorption. How does Zetia Work? 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