Peringatan Keamanan

Oral LD50 and intraperitoneal LD50 in rat were >2000 mg/kg.L11410 Estimated oral LD50 values in mouse and dog are >5000 mg/kg and >3000 mg/kg, respectively.L11410 One case of accidental overdose occurred in clinical studies in one female patient with homozygous sitosterolemia receiving 120 mg/day for 28 days with no reported clinical or laboratory adverse events.L11347 In case of overdose, symptomatic treatment is recommended.L11347

Ezetimibe

DB00973

small molecule approved

Deskripsi

Ezetimibe is a lipid-lowering compound that inhibits intestinal cholesterol and phytosterol absorption. The discovery and research of this drug began in the early 1990s, after the intravenous administration of radiolabelled ezetimibe in rats revealed that it was being localized within enterocytes of the intestinal villi - this prompted studies investigating the effect of ezetimibe on intestinal cholesterol absorption.A15202 Ezetimibe is used as an adjunctive therapy to a healthy diet to lower cholesterol levels in primary hyperlipidemia, mixed hyperlipidemia, homozygous familial hypercholesterolemia (HoFH), and homozygous sitosterolemia (phytosterolemia).L11347

Unlike other classes of cholesterol-reducing compounds including statins and bile acid sequestrants, ezetimibe has a distinct mechanism of action involving the sterol transporter Niemann-Pick C1-Like 1 (NPC1L1), and is unique in that it does not affect the absorption of fat-soluble nutrients such as fat-soluble vitamins, triglycerides, or bile acids.A33313 In genetically NPC1L1-deficient mice, a 70% reduction in intestinal cholesterol absorption was seen, and these mice were insensitive to ezetimibe treatment - it was determined based on these findings that NPC1L1 plays an essential role in promoting intestinal cholesterol uptake via an ezetimibe-sensitive pathway.A15202 By interfering with the intestinal uptake of cholesterol and phytosterols, ezetimibe reduces the delivery of intestinal cholesterol to the liver.L11347

Struktur Molekul 2D

Berat 409.4252
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Both ezetimibe and ezetimibe-glucuronide display an approximate half-life of 22 hours.[L11347]
Volume Distribusi The relative volume of distribution of ezetimibe is 107.5L.[F133]
Klirens (Clearance) There are no pharmacokinetic data available on the clearance of ezetimibe.

Absorpsi

Administration of a single 10-mg dose of ezetimibe in fasted adults resulted in peak plasma concentrations (Cmax) of 3.4-5.5 ng/mL within 4-12 hours (Tmax).L11347 The Cmax of the major pharmacologically-active metabolite, ezetimibe-glucuronide, was 45-71 ng/mL and its Tmax was 1-2 hours.L11347 Food consumption has minimal effect on ezetimibe absorption, but the Cmax is increased by 38% when administered alongside a high-fat meal.L11347 The true bioavailability of ezetimibe cannot be determined, as it is insoluble in aqueous media suitable for intravenous injection.L11347

Metabolisme

In humans, ezetimibe is rapidly and extensively metabolized via a phase II glucuronide conjugation reaction in the small intestine and liver to form its main phenolic metabolite, ezetimibe glucuronide. The main human liver and/or intestinal uridine 5?-diphosphate (UDP)-glucuronosyltransferase (UGT) enzymes responsible for the glucuronidation of ezetimibe were shown to be UGT1A1, 1A3, and 2B15 in vitro.A15202 Minimal phase I reaction involving oxidation of ezetimibe also occurs to form SCH 57871, and human jejunum microsomes also produced trace levels of a benzylic glucuronide (SCH 488128).A15202 Ezetimibe glucuronide accounts for 80-90% of the total circulating compound in plasma, and retains some pharmacological activity in inhibiting intestinal cholesterol uptake.L11347 In humans, ezetimibe and ezetimibe-glucuronide constitutes approximately 93% of the total drug in plasma.L11347 Plasma concentration-time profiles exhibit multiple peaks, suggestive of enterohepatic recyclingL11347, and about 20% of the drug distributed is reabsorbed due to enterohepatic recirculation.F133

Rute Eliminasi

Approximately 78% and 11% of orally administered radiolabelled ezetimibe are recovered in the feces and urine, respectively.L11347 Unchanged parent drug is the major component in feces and accounts for approximately 69% of an administered dose, while ezetimibe-glucuronide is the major component in urine and accounts for approximately 9% of an administered dose.L11347 High recovery of unchanged parent drug in feces suggests low absorption and/or hydrolysis of ezetimibe-glucuronide secreted in the bile.A15202

Interaksi Makanan

1 Data
  • 1. Take with or without food. Co-administration with food does not affect absorption.

Interaksi Obat

274 Data
Troglitazone Troglitazone may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Reserpine Reserpine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Progesterone Progesterone may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Chlorpromazine Chlorpromazine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Celecoxib Celecoxib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Cimetidine Cimetidine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Bosentan Bosentan may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Tamoxifen Tamoxifen may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Glyburide Glyburide may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Ursodeoxycholic acid Ursodeoxycholic acid may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Cholic Acid Cholic Acid may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Fusidic acid Fusidic acid may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Simeprevir Simeprevir may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Lenvatinib Lenvatinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Letermovir The excretion of Ezetimibe can be decreased when combined with Letermovir.
Valinomycin Valinomycin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Erythromycin Erythromycin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Tipranavir Tipranavir may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Nifedipine Ezetimibe may decrease the excretion rate of Nifedipine which could result in a higher serum level.
Quinidine Quinidine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Olmesartan Olmesartan may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Pralsetinib Pralsetinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Cyclosporine The serum concentration of Cyclosporine can be increased when it is combined with Ezetimibe.
Colestipol Colestipol can cause a decrease in the absorption of Ezetimibe resulting in a reduced serum concentration and potentially a decrease in efficacy.
Sevelamer Sevelamer can cause a decrease in the absorption of Ezetimibe resulting in a reduced serum concentration and potentially a decrease in efficacy.
Colesevelam Colesevelam can cause a decrease in the absorption of Ezetimibe resulting in a reduced serum concentration and potentially a decrease in efficacy.
Cholestyramine Cholestyramine can cause a decrease in the absorption of Ezetimibe resulting in a reduced serum concentration and potentially a decrease in efficacy.
Rifampin The metabolism of Ezetimibe can be increased when combined with Rifampin.
Nelfinavir The metabolism of Ezetimibe can be increased when combined with Nelfinavir.
Desogestrel The metabolism of Ezetimibe can be increased when combined with Desogestrel.
Zidovudine The metabolism of Ezetimibe can be increased when combined with Zidovudine.
Ritonavir The metabolism of Ezetimibe can be increased when combined with Ritonavir.
Lamotrigine The metabolism of Ezetimibe can be increased when combined with Lamotrigine.
Efavirenz The metabolism of Ezetimibe can be increased when combined with Efavirenz.
Primidone The metabolism of Ezetimibe can be increased when combined with Primidone.
Ethinylestradiol Ethinylestradiol may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Phenobarbital The metabolism of Ezetimibe can be increased when combined with Phenobarbital.
Testosterone propionate The metabolism of Ezetimibe can be increased when combined with Testosterone propionate.
Phenytoin The metabolism of Ezetimibe can be increased when combined with Phenytoin.
Carbamazepine The metabolism of Ezetimibe can be increased when combined with Carbamazepine.
Bezafibrate The risk or severity of adverse effects can be increased when Bezafibrate is combined with Ezetimibe.
Gemfibrozil The risk or severity of adverse effects can be increased when Gemfibrozil is combined with Ezetimibe.
Clofibrate The serum concentration of Ezetimibe can be increased when it is combined with Clofibrate.
Fenofibrate The serum concentration of Ezetimibe can be increased when it is combined with Fenofibrate.
Etofibrate The serum concentration of Ezetimibe can be increased when it is combined with Etofibrate.
Ciprofibrate The serum concentration of Ezetimibe can be increased when it is combined with Ciprofibrate.
Simfibrate The serum concentration of Ezetimibe can be increased when it is combined with Simfibrate.
Ronifibrate The serum concentration of Ezetimibe can be increased when it is combined with Ronifibrate.
Aluminium clofibrate The serum concentration of Ezetimibe can be increased when it is combined with Aluminium clofibrate.
Clofibride The serum concentration of Ezetimibe can be increased when it is combined with Clofibride.
Fenofibric acid The serum concentration of Ezetimibe can be increased when it is combined with Fenofibric acid.
Pravastatin Pravastatin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Diethylstilbestrol Diethylstilbestrol may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Beclomethasone dipropionate Beclomethasone dipropionate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Estradiol Estradiol may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Sulfasalazine Sulfasalazine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Teriflunomide Teriflunomide may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Dabrafenib Dabrafenib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Brigatinib Brigatinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Novobiocin Novobiocin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Hesperetin Hesperetin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Rabeprazole Rabeprazole may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Topiroxostat Topiroxostat may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Daidzin Daidzin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Naringenin Naringenin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Vandetanib Vandetanib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Safinamide Safinamide may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Vismodegib Vismodegib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Cannabidiol Cannabidiol may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Gilteritinib Gilteritinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Estradiol acetate Estradiol acetate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Estradiol benzoate Estradiol benzoate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Estradiol cypionate Estradiol cypionate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Estradiol dienanthate Estradiol dienanthate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Estradiol valerate Estradiol valerate may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Nabiximols Nabiximols may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Fedratinib Fedratinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Istradefylline Istradefylline may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Caffeine Caffeine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Vemurafenib Vemurafenib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Isavuconazole Isavuconazole may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Pantoprazole Pantoprazole may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Gefitinib Gefitinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Lansoprazole Lansoprazole may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Imatinib Imatinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Buprenorphine Buprenorphine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Telmisartan Telmisartan may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Saquinavir Saquinavir may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Dasatinib Dasatinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Sunitinib Sunitinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Genistein Genistein may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Quercetin Quercetin may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Taurocholic acid Taurocholic acid may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Elacridar Elacridar may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Dovitinib Dovitinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Rilpivirine Rilpivirine may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Ponatinib Ponatinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Afatinib Afatinib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Cobicistat Cobicistat may decrease the excretion rate of Ezetimibe which could result in a higher serum level.
Palbociclib Palbociclib may decrease the excretion rate of Ezetimibe which could result in a higher serum level.

Target Protein

NPC1-like intracellular cholesterol transporter 1 NPC1L1
Sterol O-acyltransferase 1 SOAT1
Aminopeptidase N ANPEP

Referensi & Sumber

Synthesis reference: Venkataraman Sundaram, Srinivasam Rajan, Vaddadi Ramayya, Sunkara Vardhan, Bulusu Subrahmanyam, Cheemalapati Sasikala, "Polymorphs of ezetimibe and process for preparation thereof." U.S. Patent US20050171080, issued August 04, 2005.
Artikel (PubMed)
  • PMID: 15928087
    Garcia-Calvo M, Lisnock J, Bull HG, Hawes BE, Burnett DA, Braun MP, Crona JH, Davis HR Jr, Dean DC, Detmers PA, Graziano MP, Hughes M, Macintyre DE, Ogawa A, O'neill KA, Iyer SP, Shevell DE, Smith MM, Tang YS, Makarewicz AM, Ujjainwalla F, Altmann SW, Chapman KT, Thornberry NA: The target of ezetimibe is Niemann-Pick C1-Like 1 (NPC1L1). Proc Natl Acad Sci U S A. 2005 Jun 7;102(23):8132-7. Epub 2005 May 31.
  • PMID: 22910633
    Phan BA, Dayspring TD, Toth PP: Ezetimibe therapy: mechanism of action and clinical update. Vasc Health Risk Manag. 2012;8:415-27. doi: 10.2147/VHRM.S33664. Epub 2012 Jul 3.
  • PMID: 15871634
    Kosoglou T, Statkevich P, Johnson-Levonas AO, Paolini JF, Bergman AJ, Alton KB: Ezetimibe: a review of its metabolism, pharmacokinetics and drug interactions. Clin Pharmacokinet. 2005;44(5):467-94.
  • PMID: 14620392
    Nutescu EA, Shapiro NL: Ezetimibe: a selective cholesterol absorption inhibitor. Pharmacotherapy. 2003 Nov;23(11):1463-74.

Contoh Produk & Brand

Produk: 209 • International brands: 3
Produk
  • Ach-ezetimibe
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Act Ezetimibe
    Tablet • 10 mg • Oral • Canada • Approved
  • Ag-ezetimibe
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Apo-ezetimibe
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Auro-ezetimibe
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Bio-ezetimibe
    Tablet • 10 mg • Oral • Canada • Generic • Approved
  • Ezetimibe
    Tablet • 10 mg/1 • Oral • US • Generic • Approved
  • Ezetimibe
    Tablet • 10 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 209 produk.
International Brands
  • Ezedoc
  • Ezetib
  • Zient

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
© 2025 Digital Pharmacy Research - Universitas Esa Unggul