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Dyslipidemia
Published in Jahangir Moini, Matthew Adams, Anthony LoGalbo, Complications of Diabetes Mellitus, 2022
Jahangir Moini, Matthew Adams, Anthony LoGalbo
PCSK9 monoclonal antibodies are formulated for subcutaneous injection, once to twice per month. They stop proprotein convertase subtilisin/kexin type 9 from attaching to LDL receptors, improving their function. The LDL is lowered by 40%–70%. Trials with alirocumab and evolocumab revealed less cardiovascular events when previous atherosclerotic cardiovascular disease was present. The cholesterol absorption inhibitors, including ezetimibe, inhibit absorption of cholesterol and phytosterol in the intestines. The LDL is usually lowered by ezetimibe by 15%–20%, with small increases in HDL and a slight decrease in total triglycerides. Ezetimibe can be used alone if the patient cannot tolerate statins, or it can be added to statins if the patient is on maximum statin dosage, with LDL remaining chronically elevated. Adverse effects of cholesterol absorption inhibitors are rare.
Cardiovascular Drugs
Published in Radhwan Nidal Al-Zidan, Drugs in Pregnancy, 2020
Risk Summary: It should be used with caution because the pregnancy experience in humans is limited and the reproduction studies in animals have shown low risk. However, if treatment for hypercholesterolemia is needed to be given during pregnancy, Ezetimibe is considered a safer alternative to the Statins.
Personalized Nutrition in Hypercholesterolemia
Published in Nilanjana Maulik, Personalized Nutrition as Medical Therapy for High-Risk Diseases, 2020
Aktarul Islam Siddique, Nalini Namasivayam
Medicines can help lower cholesterol levels but it can’t guarantee to cure it, so it is recommended to continue taking medicine to keep cholesterol levels in the recommended stage. Five major types of cholesterol-lowering medicines commercially available include: Statins: reported to lower LDL cholesterol levels.Bile acid sequestrants which also help lower LDL cholesterol.Nicotinic acid documented to lower LDL cholesterol and triglycerides and raise HDL cholesterol levels.Fibrates lower triglycerides, and also can raise HDL cholesterol levels.Ezetimibe lowers LDL cholesterol levels.
Efficacy and safety of add on therapies in patients with hypercholesterolemia undergoing statin therapy
Published in Expert Opinion on Pharmacotherapy, 2020
Brian Tomlinson, Paul Chan, Yuzhen Zhang, Christopher Wai Kei Lam
The early clinical trials with ezetimibe were generally not very supportive. The addition of ezetimibe to statin did not show benefits in the surrogate endpoint studies of carotid intima-media thickness (CIMT) in the Ezetimibe and Simvastatin in Hypercholesterolemia Enhances Atherosclerosis Regression trial (ENHANCE) [41], or benefits in aortic valve disease in the Simvastatin and Ezetimibe in Aortic Stenosis (SEAS) trial [42], but in retrospect such benefits may not have been expected in those trials. Aggressive reduction in LDL-C with ezetimibe combined with statin or more intensive statin alone resulted in similar regression of CIMT in the Stop Atherosclerosis in Native Diabetics Study (SANDS) trial [43] and the addition of ezetimibe to statin appeared to contribute to reduction of CIMT in the VYtorin on Carotid intima-media thickness and overall arterial rigidity (VYCTOR) study [44].
An overview of rosuvastatin/ezetimibe association for the treatment of hypercholesterolemia and mixed dyslipidemia
Published in Expert Opinion on Pharmacotherapy, 2020
Larysa Strilchuk, Giuliano Tocci, Federica Fogacci, Arrigo F. G. Cicero
Ezetimibe blocks a cholesterol transporter called Niemann-Pick C1-Like 1 (NPC1L1) protein, consequently decreasing the intestinal absorption of both dietary and endogenous cholesterol by 54–67%. It undergoes extensive glucuronidation by uridine 5ʹ-diphosphate-glucuronosyltransferase (UGT) enzymes to ezetimibe glucuronide which is more active than the parent compound [21,41–44]. It does not affect the absorption of bile acids, fatty acids, fat-soluble vitamins and triglycerides (TG) [42,45–48]. Ezetimibe can be administered as a monotherapy or in combination with statins, at any time of the day [49]. In monotherapy, it was shown to decrease LDL-C by about 15–20% [7,44], mainly depending on the individual ability to absorb cholesterol from the bowel. Ezetimibe has also anti-inflammatory properties [50], demonstrated by the additional 9–10% reduction in hs-CRP by ezetimibe/statin combination compared with statin monotherapy [50–53]. This additional reduction only weakly correlated with LDL-C decrease, so it seems to be an independent effect, which needs future studies [50,53]. Furthermore, ezetimibe seems to improve insulin resistance [54]. Similar to rosuvastatin, ezetimibe is not metabolized by CYP and has no known significant drug-drug interactions. Consequently, the combination of rosuvastatin and ezetimibe causes very few drug-drug interactions, which contributes to the low-total incidence of adverse effects observed during ezetimibe administration [55]. There is no known significant pharmacokinetic interaction between ezetimibe and rosuvastatin [55].
Current pharmacotherapy for the treatment of dyslipidemia associated with HIV infection
Published in Expert Opinion on Pharmacotherapy, 2019
Anna Gebhardt, Carl J. Fichtenbaum
Ezetimibe lowers serum cholesterol levels by inhibiting the absorption of dietary cholesterol in the small intestine. The IMPROVE-IT was a large-randomized trial in persons with prior ASCVD of ezetimibe added to a simvastatin resulting in significantly lowered on-treatment LDL-C from 70 to 54 mg/dl, with a concomitant statistically significant reduction in MACE endpoints at 7 years (32.7% vs 34.7%, P = 0.016) compared to the simvastatin alone [96]. Several smaller studies in PWH show improvement in lipid values with the use of ezetimibe [92–95]. In a placebo-controlled, crossover study of 48 PWH who received ezetimibe 10 mg daily, LDL-C decreased by 5.3% (11 mg/dL) compared to an increase of 5.5% in the placebo arm [97]. In another placebo-controlled trial ezetimibe significantly lowered LDL-C by 14.1% and TC by 18.6% after 12 weeks within 44 PWH who were on stable statin therapy with either pravastatin or atorvastatin [98]. In a small trial comparing ezetimibe plus fenofibrate to pravastatin, the combination resulted in significant declines in TC, LDL-C, non-HDL-C, TG and increases in HDL-C [99]. In a study comparing the lipid-lowering effects of ezetimibe 10 mg daily plus rosuvastatin 10 mg daily versus an increased dose of rosuvastatin (from 10 mg to 20 mg daily) there were declines in TC (−1.1 mmol/L vs. −0.5 mmol/L, P = 0.03), LDL-C (−0.68 mmol/L vs. 0.48 mmol/L, P = 0.37) and TG (−0.62 mmol/L vs. −0.17 mmol/L, P = 0.03) in the combination group [100]. Currently, there have been no adverse drug interactions and few side effects using ezetimibe alone or in combination with statins.