• 제목/요약/키워드: Ezetimibe

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Development and assessment of nano drug delivery systems for combined delivery of rosuvastatin and ezetimibe

  • Mohamed Ali Metwally;El-Yamani Ibrahim El-Zawahry;Maher Amer Ali;Diaa Farrag Ibrahim;Shereen Ahmed Sabry;Omnia Mohamed Sarhan
    • The Korean Journal of Physiology and Pharmacology
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    • 제28권3호
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    • pp.275-284
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    • 2024
  • Worldwide, cardiovascular disease is the main cause of death, which accordingly increased by hyperlipidemia. Hyperlipidemia therapy can include lifestyle changes and medications to control cholesterol levels. Statins are the medications of the first choice for dealing with lipid abnormalities. Rosuvastatin founds to control high lipid levels by hindering liver production of cholesterol and to achieve the targeted levels of low-density lipoprotein cholesterol, another lipid lowering agents named ezetimibe may be used as an added therapy. Both rosuvastatin and ezetimibe have low bioavailability which will stand as barrier to decrease cholesterol levels, because of such depictions, formulations of this combined therapy in nanotechnology will be of a great assistance. Our study demonstrated preparations of nanoparticles of this combined therapy, showing their physical characterizations, and examined their behavior in laboratory conditions and vivo habitation. The mean particle size was uniform, polydispersity index and zeta potential of formulations were found to be in the ranges of (0.181-0.72) and (-13.4 to -6.24), respectively. Acceptable limits of entrapment efficiency were affirmed with appearance of spherical and uniform nanoparticles. In vitro testing showed a sustained release of drug exceeded 90% over 24 h. In vivo study revealed an enhanced dissolution and bioavailability from loaded nanoparticles, which was evidenced by calculated pharmacokinetic parameters using triton for hyperlipidemia induction. Stability studies were performed and assured that the formulations are kept the same up to one month. Therefore, nano formulations is a suitable transporter for combined therapy of rosuvastatin and ezetimibe with improvement in their dissolution and bioavailability.

Atorvastatin/ezetimibe 복합제 복용 후 발생한 시야결손 부작용 사례보고 (Visual Field Defect after Taking Atorvastatin/Ezetimibe, a Case Study)

  • 김지윤;이경규;김준영;이정민;김나영;이모세;지은희
    • 한국임상약학회지
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    • 제29권2호
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    • pp.133-137
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    • 2019
  • Atorvastatin is one of the most widely prescribed medications for dyslipidemia treatment. In Korea, post combined therapy with ezetimibe, a 73-year-old woman was reported by a community pharmacy to have experienced visual field defect, which recovered after drug discontinuation. She had never experienced this symptom before, and several studies have reported an association between use of statins and visual disorders such as blurred vision, diplopia, and cataract. Blockage of cholesterol accumulation, oxidative stress, or myopathy is expected to be a cause of this symptom. Naranjo scale, Korean causality assessment algorithm (Ver.2), and World Health Organization-Uppsala Monitoring Center (WHO-UMC) criteria were the three tools used to determine causality between the visual disorder and atorvastatin. The results represent 'probable', 'certain', and 'probable/likely' causality, respectively. Our results, in combination with a review of literature, indicate that ocular adverse effects are highly likely related to atorvastatin.

이상지질혈증 경구용 약제와 심혈관질환 예방효과 (Oral Drugs for Treatment of Dyslipidemia and Cardiovascular Disease Prevention)

  • 이윤아;노준승;송상욱;정수영;권지영;강성구
    • 비만대사연구학술지
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    • 제1권1호
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    • pp.14-25
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    • 2022
  • In 1971, Dr. Akira Endo succeeded in isolating a cholesterol synthesis inhibitor, compactin. Later, compactin was renamed mevastatin, meaning that it stops the synthesis of mevalonate, which is considered the first statin. However, mevastatin is not commercially released, whereas lovastatin, developed by Alfred Albert of Merk in 1979, was the first commercially developed statin. After the 4S study, the first largescale clinical trial with statins conducted in Scandinavia showed a dramatic secondary preventive effect against cardiovascular disease, and the effectiveness of statins in patients with dyslipidemia was repeatedly demonstrated. Subsequently, many oral drugs that affect blood lipid concentration; statins and ezetimibe aimed at reducing low-density lipoprotein (LDL)) cholesterol; fibrates and omega 3 formulations aimed at reducing triglycerides were widely developed and used in Korea. In this article, we review the results of clinical studies on representative cardiovascular diseases for four types of oral drugs for dyslipidemia, which are currently the most commonly used in Korea.

Natural products in the research of cholesterol gallstones

  • Castro-Torres, Ibrahim Guillermo;De la O-Arciniega, Minarda;Gallegos-Estudillo, Janeth;Martinez-Vazquez, Mariano;Naranjo-Rodriguez, Elia Brosla;Dominguez-Ortiz, Miguel Angel;Cruz-Sanchez, Jesus Samuel
    • 셀메드
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    • 제3권3호
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    • pp.21.1-21.5
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    • 2013
  • Cholesterol gallstones are a digestive disease of high prevalence that has many risk factors; for this reason, research has focused mainly on how to prevent it rather than how to treat it. Many molecules of the hepatic, bile and intestinal systems are involved in the pathophysiology of this disease, making it very difficult to find a therapeutic target. The pharmacological treatment is limited, so when gallstones generate symptoms, medical treatment indicates gallbladder removal. Ursodeoxycholic acid is used to dissolve cholesterol stones, and ezetimibe and statins are other drugs with possible applications in the treatment of this disease. Given the small number of drugs that have been developed for treating this disease, the research of natural products becomes of paramount importance. Resources such as black radish, glucosinolates, fenugreek, capsaicin, curcumin, garlic, and onion, have all shown significant effects in the prevention and treatment of cholesterol gallstones. In this review, we made a synthesis of the scientific reports that deal with these natural products and that can serve as antecedents for finding a way to treat the most common disease of the gallbladder.

이상지질혈증의 국내 및 국외 치료 가이드라인 비교 (Current Guidelines on the Management of Dyslipidemia)

  • 최윤정;이송;김주영;이경은
    • 한국임상약학회지
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    • 제27권4호
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    • pp.276-283
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    • 2017
  • Objective: Dyslipidemia is recognized as a prominent risk factor for cardiovascular and cerebrovascular diseases but it is manageable through therapeutic and lifestyle intervention. Interpreting the latest guidelines is essential for an application of recommendation from guidelines into clinical practice. Therefore, this study aimed to compare the most recent guidelines on dyslipidemia treatment recommendations in Korea and USA. Methods: This study analyzed and compared 2015 Korean guidelines for the management of dyslipidemia, 2013 American College of Cardiology/American Heart Association (ACC/AHA) guideline and 2016 supportive guidelines from ACC. Results: A comparison was made focused on the following: target patients based on cardiovascular risk assessment, target goal, and treatment strategies including statin and non-statin therapies. Four target patient groups by risk were suggested in 2015 Korean guideline and cardiovascular risk factors were also considered for initiation of lipid lowering therapy. Titrated statin regimen was recommended by Korean guideline to reach LDL cholesterol and non-HDL cholesterol target level. In 2013 ACC/AHA guideline, four statin benefit group was introduced considering ASCVD risk and high intensity statin or intermediate intensity statin use were recommended without dose titration. 2016 update was to support non-statin therapy based on updated evidence and new consideration of ezetimibe, PCSK9-inhibitor and bile acid sequestrant was brought up. Conclusion: Guidelines are continuously updating as new and important clinical data are constantly released along with the advent of newly approved drugs for lipid disorder. This article provides resources that facilitates uptake of these recommendations into clinical practice.

Statin Intolerance: an Overview of the Current Status and Possible Treatment Options

  • Suh, Sunghwan;Jung, Chang Hee;Hong, Soon-Jun;Kim, Jung-Sun;Choi, Sung Hee
    • 지질동맥경화학회지
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    • 제7권2호
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    • pp.77-87
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    • 2018
  • Lowering serum low-density lipoprotein cholesterol (LDL-C) is the mainstay for reduction of risk of cardiovascular disease (CVD), the second most common cause of death in Korea. The 2015 Korean guidelines for management of dyslipidemia strongly recommend the use of statins in patients at risk of CVD. Statin therapy, which is the gold standard for CVD, reduces LDL-C level by 40% to 60% and is generally well tolerated. However, many patients are intolerant to statins and discontinue therapy or become nonadherent to therapy because of actual/perceived side effects. The most common of these side effects is the statin-associated muscle symptom (SAMS). Discontinuation and repetitive re-challenge with statins can help identify SAMS. If serum creatinine kinase level is more than 10 times the upper limit of normal, statin therapy must be stopped immediately, and the physician should identify possible causes including rhabdomyolysis and treat appropriately. In other patients, it might help to switch to a less potent statin or to use statins at intermittent non-daily dosing. To achieve target LDL-C level, non-statin lipid-lowering therapies such as dietary modifications, ezetimibe, and bile acid sequestrants may be added. Several new drugs have recently been approved for lowering LDL-C level. Alirocumab and evolocumab are monoclonal antibodies that inhibit proprotein convertase subtilisin/kexin type 9, and both drugs cause large reductions in LDL-C, similar to statins. Lomitapide and mipomersen are orphan drugs used as adjuncts to other lipid-lowering therapies in patients with homozygous familial hypercholesterolemia.

국내 성인환자에서 이상지질혈증 약물치료와 골다공증 상관성 (The Association between Medication Use for Dyslipidemia and Osteoporosis)

  • 이한솔;김종윤;유기연
    • 한국임상약학회지
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    • 제31권4호
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    • pp.278-284
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    • 2021
  • Background: Osteoporosis is a disease that affects the quality of life and imposes a high socioeconomic burden. Studies have reported that statins, a HMG CoA reductase inhibitor, have a positive or negative effect on osteoporosis. The purpose of this study was to analyze the correlation between statins and osteoporosis risk. Methods: We used the total patient sample data of the Health Insurance Review and Assessment Service (HIRA-NPS-2018). We analyzed the prevalence of osteoporosis in adult patients of Korea who were diagnosed with dyslipidemia and were prescribed statins at the same time. The odds ratio (OR) according to the intensity and type of statin was used to confirming the prevalence. Results: Among the 1,138,899 patients included in the study, 143,895 patients used statins and 27,524 patients (19.13%) were diagnosed with osteoporosis in the statin group. The OR value of statin group was 0.96 (95% CI 0.94-0.98), confirming that the prevalence of osteoporosis decreased, and a significant decrease was seen in all statin intensity. Some of the moderate-intensity statins rather increased the prevalence of osteoporosis, but atorvastatin and rosuvastatin obtained positive results at both medium- and high-intensity doses, and lovastatin, a low-intensity statin, showed the greatest reduction in the prevalence of osteoporosis. Conclusion: We found that the prevalence of osteoporosis was reduced in the statin group, and there was a constant correlation regardless of gender or age. However, a large, prospective, double-blind and randomized study is needed for a long period of time to demonstrate the effectiveness of statins.

Therapeutic Duplication as a Medication Error Risk in Fixed-Dose Combination Drugs for Dyslipidemia: A Nationwide Study

  • Wonbin Choi;Hyunji Koo;Kyeong Hye Jeong;Eunyoung Kim;Seung-Hun You;Min-Taek Lee;Sun-Young Jung
    • 한국임상약학회지
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    • 제33권3호
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    • pp.168-177
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    • 2023
  • Background & Objectives: Fixed-dose combinations (FDCs) offer advantages in adherence and cost-effectiveness compared to free combinations (FCs), but they can also complicate the prescribing process, potentially leading to therapeutic duplication (TD). This study aimed to identify the prescribing patterns of FDCs for dyslipidemia and investigate their associated risk of TD. Methods: This was a retrospective cohort study involving drugs that included statins, using Health Insurance Review & Assessment Service-National Patient Sample (HIRA-NPS) data from 2018. The unit of analysis was a prescription claim. The primary outcome was TD. The risk ratio of TD was calculated and adjusted for patient, prescriber, and the number of cardiovascular drugs prescribed using a multivariable Poisson model. Results: Our study included 252,797 FDC prescriptions and 515,666 FC prescriptions. Of the FDC group, 46.52% were male patients and 56.21% were aged 41 to 65. Ezetimibe was included in 71.61% of the FDC group, but only 0.25% of the FC group. TD occurred in 0.18% of the FDC group, and the adjusted risk ratio of TD in FDC prescriptions compared to FC was 6. 44 (95% CI 5. 30-7. 82). Conclusions: Prescribing FDCs for dyslipidemia was associated with a higher risk of TD compared to free combinations. Despite the relatively low absolute prevalence of TD, the findings underline the necessity for strategies to mitigate this risk when prescribing FDCs for dyslipidemia. Our study suggests the potential utility of Clinical Decision Support Systems and standardizing nomenclature in reducing medication errors, providing valuable insights for clinical practice and future research.