Adverse Drug Reaction Classification System

Pharmaceutical Information
Drug Name Ezetimibe
Drug ID BADD_D00864
Description 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]
Indications and Usage 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).[L11347,L11401,L11404] It is also indicated to reduce elevated total-C, LDL-C, Apo B, and non-HDL-C in patients with mixed hyperlipidemia in combination with fenofibrate, and to reduce elevated total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH), in combination with atorvastatin or simvastatin.[L11347] Ezetimibe may also be used to reduce elevated sitosterol and campesterol in patients with homozygous sitosterolemia (phytosterolemia).[L11347]
Marketing Status approved
ATC Code C10AX09
DrugBank ID DB00973
KEGG ID D01966
MeSH ID D000069438
PubChem ID 150311
TTD Drug ID D09LWS
NDC Product Code 68462-226; 71335-1127; 76333-170; 78206-178; 0591-3713; 70966-0027; 59651-052; 68788-8297; 71335-2123; 82009-024; 16714-813; 71205-277; 15894-0011; 59651-056; 66039-839; 66039-869; 68554-0085; 70518-2262; 70518-3334; 70771-1109; 71335-0684; 72189-118; 14501-0008; 55111-079; 51660-200; 60505-2945; 60687-373; 67877-490; 69238-1154; 0904-7103; 71205-145; 58032-2004; 69218-0800; 0781-5690; 59651-698; 65015-812; 75895-0281; 31722-628; 50268-298; 63629-7413; 71335-0933; 16729-433; 50228-379; 60429-982; 68382-773; 0615-8300; 64176-0042; 65096-0113; 66039-896; 69218-0400
UNII EOR26LQQ24
Synonyms Ezetimibe | (1-(4-fluorophenyl)-(3R)-(3-(4-fluorophenyl)-(3S)-hydroxypropyl)-(4S)-(4-hydroxyphenyl)-2-azetidinone) | Ezetimib | Ezetrol | SCH 58235 | 58235, SCH | SCH-58235 | SCH58235 | Zetia
Chemical Information
Molecular Formula C24H21F2NO3
CAS Registry Number 163222-33-1
SMILES C1=CC(=CC=C1C2C(C(=O)N2C3=CC=C(C=C3)F)CCC(C4=CC=C(C=C4)F)O)O
Chemical Structure
ADRs Induced by Drug
*The priority for ADR severity classification is based on FAERS assessment, followed by the most severe level in CTCAE rating. If neither is available, it will be displayed as 'Not available'.
**The 'Not Available' level is hidden by default and can be restored by clicking on the legend twice..
ADR Term ADReCS ID ADR Frequency (FAERS) ADR Severity Grade (FAERS) ADR Severity Grade (CTCAE)
Abdominal discomfort07.01.06.0010.001877%Not Available
Abdominal distension07.01.04.0010.000521%
Abdominal pain07.01.05.0020.002065%
Abdominal pain upper07.01.05.0030.001469%
Abnormal sensation in eye06.01.01.0010.000138%Not Available
Accommodation disorder06.02.04.0010.000126%Not Available
Acute myocardial infarction24.04.04.001; 02.02.02.0010.000094%Not Available
Affective disorder19.04.04.0010.000063%Not Available
Alanine aminotransferase increased13.03.04.005--
Alopecia23.02.02.001--
Altered state of consciousness19.07.01.003; 17.02.04.0010.000063%Not Available
Amnesia17.03.02.001; 19.20.01.0010.000640%
Anaemia01.03.02.001--
Anaphylactic reaction24.06.03.006; 10.01.07.001--
Anaphylactic shock24.06.02.004; 10.01.07.002--Not Available
Anger19.04.02.0010.000138%Not Available
Angina pectoris02.02.02.002; 24.04.04.0020.000358%
Angina unstable24.04.04.004; 02.02.02.0040.000973%Not Available
Angioedema23.04.01.001; 22.04.02.008; 10.01.05.0090.000389%Not Available
Anuria20.01.03.0020.000063%Not Available
Aphasia17.02.03.001; 19.21.01.0010.000201%
Arrhythmia02.03.02.0010.000094%Not Available
Arteriosclerosis24.04.02.001--Not Available
Arthralgia15.01.02.0010.003836%
Arthritis15.01.01.0010.000320%
Arthropathy15.01.01.0030.000213%Not Available
Aspartate aminotransferase increased13.03.04.011--
Asthenia08.01.01.0010.001061%Not Available
Asthma22.03.01.002; 10.01.03.010--Not Available
Atrial fibrillation02.03.03.002--
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