Formulary
Ezetimibe: Indications, Dosing, Side Effects and Interactions
Ezetimibe inhibits the intestinal absorption of cholesterol.
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Ezetimibe: Indications, Dosing, Side Effects and Interactions
Ezetimibe inhibits the intestinal absorption of cholesterol.
Drug action
Ezetimibe inhibits the intestinal absorption of cholesterol. If used alone, it has a modest effect on lowering LDL-cholesterol, with little effect on other lipoproteins.
Indications and dose
**Adjunct to dietary measures and statin treatment in primary hypercholesterolaemia,Adjunct to dietary measures and statin in homozygous familial hypercholesterolaemia,Primary hypercholesterolaemia (if statin inappropriate or not tolerated),Adjunct to dietary measures in homozygous sitosterolaemia**
- **Adult** (By Mouth): 10 mg once daily.
**Prevention of cardiovascular events [in patients with coronary heart disease and a history of acute coronary syndrome, in combination with a statin]**
- **Adult** (By Mouth): 10 mg once daily.
**Adjunct to dietary measures and statin treatment in primary hypercholesterolaemia, Adjunct to dietary measures and statin in homozygous familial hypercholesterolaemia, Primary hypercholesterolaemia (if statin inappropriate or not tolerated), Adjunct to dietary measures in homozygous sitosterolaemia for ezetimibe**
- **Child 10-17 years** (By mouth): 10 mg once daily.
Side effects
Common or very common Asthenia; diarrhoea; gastrointestinal discomfort; gastrointestinal disorders; headache; muscle complaints Uncommon Appetite decreased; arthralgia; chest pain; cough; dry mouth; hot flush; hypertension; muscle weakness; nausea; pain; paraesthesia; peripheral oedema; skin reactions Frequency not known Constipation; depression; dizziness; dyspnoea; hepatitis; myopathy; pancreatitis; thrombocytopenia
Interactions
**Severe interactions:**
- No clinically significant pharmacokinetic interactions have been observed between ezetimibe and medicinal products known to be metabolised by cytochromes P450 1A2, 2D6, 2C8, 2C9, and 3A4, or...
- Statins No clinically significant pharmacokinetic interactions were seen when ezetimibe was co-administered with atorvastatin, simvastatin, pravastatin, lovastatin, fluvastatin or rosuvastatin.
- In a different study, a renal transplant patient with severe renal impairment who was receiving ciclosporin and multiple other medicinal products, demonstrated a 12-fold greater exposure to total...
- Anticoagulants Concomitant administration of ezetimibe (10 mg once daily) had no significant effect on bioavailability of warfarin and prothrombin time in a study of twelve healthy adult males.
**Other interactions (20):**
- In preclinical studies, it has been shown that ezetimibe does not induce cytochrome P450 drug metabolising enzymes.
- In clinical interaction studies, ezetimibe had no effect on the pharmacokinetics of dapsone, dextromethorphan, digoxin, oral contraceptives (ethinyl estradiol and levonorgestrel), glipizide,...
- Cimetidine, co-administered with ezetimibe, had no effect on the bioavailability of ezetimibe.
- Antacids Concomitant antacid administration decreased the rate of absorption of ezetimibe but had no effect on the bioavailability of ezetimibe.
- Colestyramine Concomitant colestyramine administration decreased the mean area under the curve (AUC) of total ezetimibe (ezetimibe + ezetimibe glucuronide) approximately 55%.
- The incremental low-density lipoprotein cholesterol (LDL-C) reduction due to adding Ezetimibe to colestyramine may be lessened by this interaction (see section 4.2).
Pregnancy
Manufacturer advises use only if potential benefit outweighs risk-no information available.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies.
Hepatic impairment
Manufacturer advises avoid in moderate to severe impairment.
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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