A Comparison of Effectiveness of Crystalline and Amorphous Atorvastatin

2020 ◽  
Vol 103 (9) ◽  
pp. 914-919

Background: Atorvastatin is a widely used statin, of which there are two available polymorphs: crystalline (original) and amorphous (generic). Pharmacological studies showed the similarity between both forms. However, the lipid-lowering effectiveness of the amorphous form was still uncertain. Objective: To compare the effectiveness of crystalline and amorphous form of atorvastatin. Materials and Methods: The authors conducted an observational cross-sectional analytic study by retrospectively collecting data from January 1, 2016 to December 31, 2017 of the patients at Queen Sirikit Heart Center of the Northeast where the original regimen of crystalline atorvastatin had been replaced by the amorphous atorvastatin at the same dose. Patients must have been prescribed each form of atorvastatin for at least six weeks. The lipid profiles taken at the closest to the switching point (before and after) were used. The primary outcome was changes in low-density lipoprotein (LDL) levels. The secondary outcomes were changes in total cholesterol (TC), triglyceride (TG), and high-density lipoprotein (HDL) levels, as well as a comparison of LDL levels in patients whose tablets were split. Results: Eight hundred twenty-five patients were included in the present study. The mean age was 63.7±9.9 years. Five hundred sixty-eight patients (68.8%) were male, and 736 (89.2%) were treated as secondary prevention. The mean LDL levels during crystalline and amorphous atorvastatin use were 92.4±39.0 and 91.8±41.0 mg/dL, respectively (mean difference –0.6; 95% confidence interval [CI], –2.2 to 1.0; p=0.460). The mean TC, TG, and HDL levels during crystalline and amorphous form use were 153.1±43.3 and 152.0±48.6 mg/dL (p=0.400), 153.4±129.0 and 155.0±148.3 (p=0.740), 43.6±11.9, and 44.4±12.0 (p=0.004), respectively. Among the patients who had tablet splitting, the mean LDL levels during crystalline and amorphous atorvastatin use were 89.2±28.3 and 91.0±30.8 mg/dL, respectively (p=0.279). Side effects were recorded in nine patients, one of which was rhabdomyolysis. Conclusion: The effectiveness of amorphous atorvastatin at lowering lipids was comparable to that of atorvastatin in its crystalline form, and patients were generally able to tolerate amorphous atorvastatin. Keywords: Atorvastatin, Crystalline, Amorphous, Lipid-lowering, Low-density lipoprotein

2015 ◽  
Vol 3 (1) ◽  
Author(s):  
Aji M. Sanhia ◽  
Damajanty H. C. Pangemanan ◽  
Joice N. A. Engka

Abstract: Low Density Lipoprotein (LDL) is a type of lipoprotein that transports cholesterol most widely in the body. Smoking is one of the factors that can cause elevated levels of LDL cholesterol, which nicotine is one element in cigarettes cathecolamine that stimulates secretion, increases lipolysis, and also increases free fatty acids. Excessive levels of LDL cholesterol in the blood will increase the risk of cholesterol buildup in the arteries, followed by atherosclerosis. This study aimed to describe the levels of LDL cholesterol in seashores community smoker. This was a descriptive analysis with a cross sectional design. Samples in this study were 40 people. The results showed that the mean LDL cholesterol level of 40 samples was 132.93 mg / dl which 24 sample (60%) was at the above the borderline threshold. There was no subject with high LDL level. Conclusion: There was an increase in LDL level in smokers who lived in seashores.Keywords: low density lipoprotein (LDL), smokers.Abstrak: Low Density Lipoprotein (LDL) merupakan jenis lipoprotein yang paling banyak mengangkut kolesterol di dalam tubuh. Merokok merupakan salah satu faktor yang dapat menyebabkan terjadinya peningkatan kadar kolesterol LDL, dimana nikotin yang merupakan salah satu unsur pada rokok merangsang sekresi katakolamin, meningkatkan lipolisis, dan meningkatkan asam lemak bebas. Kadar kolesterol LDL yang berlebihan dalam darah akan meningkatkan resiko penumpukan kolesterol pada dinding pembuluh darah arteri yang diikuti dengan terjadinya aterosklerosis. Penelitian ini bertujuan untuk mengetahui gambaran kadar kolesterol LDL pada masyarakat di pesisir pantai. Penelitian yang digunakan bersifat deskriptif analisis dengan rancangan Cross Sectional Study. Sampel dalam penelitian ini berjumlah 40 orang yang sesuai kriteria inklusi dan bersedia menjadi responden. Hasil penelitian memperlihatkan tingkat kolesterol LDL rata-rata pada 40 sampel ialah 132,93 mg/dl, dengan 24 sampel (60%) berada di atas ambang batas dan sisanya memiliki kadar LDL di bawah ambang batas. Simpulan: Terdapat peningkatan kadar LDL pada perokok yang tinggal di pesisir pantai.Kata kunci: low density lipoprotein (LDL), perokok.


Medicina ◽  
2007 ◽  
Vol 43 (11) ◽  
pp. 879
Author(s):  
Antanas Griškevičius ◽  
Judita Audzijonienė ◽  
Žaneta Petrulionienė ◽  
Aleksandras Laucevičius

The case of rear complicated homozygous hypercholesterolemia treated by a direct adsorption of lipoprotein apheresis procedure is presented in this article. In total, 30 sessions of direct adsorption of lipoprotein apheresis were performed on a 14–16-year-old patient from June 2004 to December 2006. Blood flow rate was 30–70 mL/min. Central and ulnar veins were punctured. Lipid levels were measured before and after lipid apheresis during each session throughout the study period. The mean decrease in total cholesterol level was 26.4–71.2% compared to baseline, low-density lipoprotein cholesterol – 31.9–72.2%, lipoprotein (a) – 56.6–90.9%, apolipoprotein B – 26.4–60.0%. Clinical procedures were completely uneventful. The last 26 sessions were performed in a day unit.


2020 ◽  
Vol 17 ◽  
Author(s):  
Abdullah Shehab ◽  
Asim Ahmed Elnour ◽  
Akshaya Srikanth Bhagavathula ◽  
Joseph Pulavelil Kurian ◽  
Gazi Hassan ◽  
...  

Aims: We aim to investigate the efficacy and safety of pitavastatin 4 mg in a population of people living in the United Arab Emirates (UAE). Background: Pitavastatin is a member of the HMG-CoA reductase inhibitors family which was approved for use in adult subjects with primary hyperlipidemia or mixed dyslipidemia. To date, no published studies have assessed the efficacy and safety of pitavastatin in the United Arab Emirates. Objective: The main objective of the current study was to investigate the efficacy and safety of pitavastatin in subjects with dyslipidemia for primary prevention of cardiovascular diseases based on total cardiovascular risk. Methods: This was a multicentre (four private hospitals) prospective cohort study to analyze data on the use of pitavastatin for dyslipidemia in adult outpatients in Abu Dhabi and Dubai emirates, United Arab Emirates. We have followed-up the clinical profiles of subjects in four hospitals for six-weeks during the period from June 2015 to June 2017. Efficacy was based on the evaluation of the mean (± standard deviation) change in low-density lipoprotein cholesterol between baseline and week six after the initiation of pitavastatin therapy. Safety was reported as the incidence of adverse events occurred with the use of pitavastatin and the development of new-onset diabetes. Results: A total of 400 subjects who were receiving pitavastatin 4 mg were included. The mean age of subjects was 50.7 ±10.8 years, of these 79.0% were males. At the baseline, the mean level of total cholesterol was 185.4 ±41.5 mg/dL, low density lipoprotein was 154.9 ±48.55 mg/dL, high-density lipoprotein cholesterol was 40.5 ±11.23 mg/dL and fasting blood glucose was 115.0 (±16.63) mg/dl. At the end of six weeks, low density lipoprotein levels significantly decreased to 112.09 ±41.90 mg/dl (standard mean difference [SMD] (-42.8%), 95% CI: -42.88 [-49.17 to -36.58] mg/dl, P <0.001), while high density lipoprotein levels improved (SMD, 95% CI: 1.77% [0.25 to 3.28] mg/dl, P <0.022). There were 55 subjects (13.7%) reported various adverse events such as myalgia (7.5%), sleep disorders (2.5%), and myopathy (2.2%). Furthermore, 4 (1.0%) have had developed new-onset diabetes post six-weeks of initiation of pitavastatin therapy. Conclusion: Pitavastatin 4 mg had howed robust efficacy in reducing LDL-C levels and improving HDL-C levels in subjects with dyslipidemias. The use of pitavastatin was associated with a low discontinuation rate, fewer adverse events, and very limited cases of new-onset diabetes.


2021 ◽  
Vol 10 (14) ◽  
pp. 3098
Author(s):  
Shota Okutsu ◽  
Yoshifumi Kato ◽  
Shunsuke Funakoshi ◽  
Toshiki Maeda ◽  
Chikara Yoshimura ◽  
...  

The aim of this study was to investigate the effects of long-term weight gain from the age of 20 on incidence of hyper-low-density-lipoprotein (LDL) cholesterolemia in the general population of Japanese people. Methods: We conducted a population-based retrospective cohort study using annual health checkup data for residents of Iki City, Nagasaki Prefecture, Japan. A total of 3179 adult (≥30 years old) men and women without hyper-LDL cholesterolemia at baseline, who underwent two or more health checkups were included in the analysis. Information on weight gain (≥10 kg) after 20 years of age was obtained using questionnaire. The outcome of this study was development of hyper-LDL cholesterolemia defined as LDL-cholesterol level ≥3.62 mmol/L and/or initiation of lipid-lowering medications. Results: During a mean follow-up period of 4.53 years, 665 of the 3179 participants developed hyper-LDL cholesterolemia (46.5/1000 person-years). The incidence of hyper-LDL cholesterolemia was higher in participants with a weight gain of ≥10 kg (55.3/1000 person-years) than among those with a weight gain of <10 kg (41.8/1000 person-years). This association remained statistically significant even after adjustment for age, sex, smoking, daily drinking, exercise, obesity, hypertension, and diabetes (multivariable hazard ratio 1.31, 95% confidence interval 1.08–1.58, p = 0.006). Conclusion: A weight gain of ≥10 after 20 years of age affected the development of hyper-LDL cholesterol regardless of age, sex, and obesity in a general population of Japanese.


BMJ Open ◽  
2021 ◽  
Vol 11 (2) ◽  
pp. e041613
Author(s):  
Toshihide Izumida ◽  
Yosikazu Nakamura ◽  
Yukihiro Sato ◽  
Shizukiyo Ishikawa

ObjectivesSmall dense low-density lipoprotein cholesterol (sdLDL-C) might be a better cardiovascular disease (CVD) indicator than low-density lipoprotein cholesterol (LDL-C); however, details regarding its epidemiology remain elusive. The present study aimed at evaluating the association between the demographic factors, such as age, gender and menopausal status, and sdLDL-C levels and sdLDL-C/LDL-C ratio in the Japanese population.DesignThis was a cross-sectional study.Setting13 rural districts in Japan, 2010–2017.ParticipantsThis study included 5208 participants (2397 men and 2811 women), who underwent the health mass screening that was conducted in accordance with the medical care system for the elderly and obtained informed consent for this study.ResultsIn total, 517 premenopausal women (mean age ±SD, 45.1±4.2 years), 2294 postmenopausal women (66.5±8.8 years) and 2397 men (64.1±11.2 years) were analysed. In men, the sdLDL-C levels and sdLDL-C/LDL-C ratio increased during younger adulthood, peaked (36.4 mg/dL, 0.35) at 50–54 years, and then decreased. In women, relatively regular increasing trends of sdLDL-C level and sdLDL-C/LDL-C ratio until approximately 65 years (32.7 mg/dL, 0.28), followed by a downward or pleated trend. Given the beta value of age, body mass index, fasting glucose and smoking and drinking status by multiple linear regression analysis, standardised sdLDL-C levels and sdLDL-C/LDL-C ratio in 50-year-old men, premenopausal women and postmenopausal women were 26.6, 22.7 and 27.4 mg/dL and 0.24, 0.15 and 0.23, respectively. The differences between premenopausal and postmenopausal women were significant (p<0.001).ConclusionsSdLDL-C and sdLDL-C/LDL-C ratios showed different distributions by age, gender and menopausal status. A subgroup-specific approach would be necessary to implement sdLDL-C for CVD prevention strategies, fully considering age-related trends, gender differences and menopausal status.


2021 ◽  
Vol 8 (26) ◽  
pp. 2283-2287
Author(s):  
Swetha Rajshekar Lakshetty ◽  
Nandini Devru

BACKGROUND Hypothyroidism is the second most common endocrinopathy next to diabetes mellitus (DM). Hypothyroidism is associated with increased cardiovascular mortality and morbidity. Cardiovascular complications are some of the most profound, reproducible and reversible clinical findings associated with thyroid disease1 . Hence this study was undertaken to assess the cardiac dysfunction among patients with hypothyroidism by electrocardiogram (ECG) and echocardiogram (ECHO) so as to provide a proper treatment guideline even among milder cases. METHODS This was a cross sectional study carried among 50 new patients of hypothyroidism who presented to Navodaya Hospital, Raichur during 2015 to 2017. They were clinically evaluated and underwent relevant investigations, including thyroid profile estimation, cardiac evaluation using ECG and 2D ECHO. RESULTS Most cases fell in the age group of 31 - 40 years. There was an overall female preponderance (76 %) over all age groups with mean age of 42.02 years. Goiter was found in 8 % of patients, bradycardia and hypertension was seen in 30 % and 22 % respectively. Central nervous system (CNS) examination revealed delayed ankle jerk in 40 % followed by hoarseness of voice in 38 % of patients. Lipid analysis showed increase of total cholesterol (TC), low density lipoprotein (LDL), very low-density lipoprotein (VLDL), triglycerides (TGL) and decrease of highdensity lipoprotein (HDL). Normal ECG was found in 26 % of patients. Bradycardia was most common finding seen in 30 % (15) of patients. 24 % (12) of patients exhibited low voltage complexes. While, 46 % cases showed normal ECHO findings. 24 % of cases presented with pericardial effusion. 18 % cases presented with diastolic dysfunction among which majority were mild. None of the cases had severe diastolic dysfunction. Only a meagre 10 % cases showed intraventricular septum (IVS) thickness. CONCLUSIONS Pericardial effusion was seen among 24 % of patients while diastolic dysfunction was seen in 18 % patients. Thus, any unexplained pericardial effusion should be screened for hypothyroidism. KEYWORDS Hypothyroidism, Cardiac Dysfunction, 2D ECHO, ECG, Thyroid Stimulating Hormone (TSH)


2017 ◽  
Vol 9 (3) ◽  
pp. 315-320 ◽  
Author(s):  
Chidozie N. OKOYE ◽  
Samuel O. EKERE ◽  
Onyinyechukwu A. AGINA ◽  
Ikechukwu J. UDEANI ◽  
Chukwunonso K. EZEASOR

The present study evaluated the effect of whole egg consumption on the liver, testes, cauda epididymal sperm reserve and lipid profile of male rats. These evaluations were carried out on adult twenty (20) male albino rats, which were randomly selected into four groups of 5 rats each, designated groups A, B, C and D. Group A was the control group and received only equivalent volume of distilled water, while groups B, C and D received 0.25mg/kg, 0.5mg/kg; and 1.0mg/kg body weight of the quail egg respectively. Standard procedures were carried out in the tissue processing, cauda epididymal sperm reserve and in lipid profile determinations. On days 35 and 49, the mean serum total cholesterol value of group D was significantly lower than that of the control group. On day 35, the mean serum low density lipoprotein and high density lipoprotein (LDL and HDL cholesterol) values of all the treatment groups were significantly lower and higher than that of the control group, respectively. However, on days 49 and 63, the mean serum very low density lipoprotein (VLDL cholesterol) and triglyceride values of all the treatment groups were significantly higher than that of the control group. A significant increase in cadual epididymal sperm count (CESR) was recorded on day 63 at the mid and high doses. No obvious pathological lesions were observed in the histomorphology of the testes and liver when compared to the control. Therefore, whole quail egg consumption caused an increase in serum triglyceride and very low density lipoprotein concentration, and also improved fertility. In other words, prolonged consumption of quail egg should be done with caution as it may predispose one to cardiovascular disease.


2021 ◽  
Vol 23 (12) ◽  
Author(s):  
Angela Pirillo ◽  
Alberico L. Catapano ◽  
Giuseppe D. Norata

Abstract Purpose of Review Familial hypercholesterolemia (FH) is a monogenic disorder characterized by high plasma levels of low-density lipoprotein cholesterol (LDL-C) since birth and a high risk of premature cardiovascular disease. The genetic defect is carried in only one allele in heterozygous FH (HeFH) or in both in the most severe homozygous FH (HoFH). Current guidelines recommend to reduce substantially LDL-C levels in these high-risk patients, with the need to use association therapy combining agents with different mechanisms of action. As most cases of FH are attributable to mutations in the gene encoding the low-density lipoprotein receptor (LDLR), statins, even in combination with ezetimibe, are less effective in reducing LDL-C plasma levels in FH patients, who require a more intensive approach with additional lipid-lowering agents. Additional targets playing key roles in regulating LDL-C levels are represented by PCSK9 and ANGPTL3. Recent Findings Two monoclonal antibodies (mAbs) targeting PCSK9, evolocumab and alirocumab, significantly reduce LDL-C levels in HeFH patients. In patients with HoFH, the efficacy of mAbs to PCSK9 is strictly related to the presence of a residual LDLR activity; thus, patients carrying null mutations do not respond to the therapy with these mAbs, whereas some effects can be appreciated in HoFH bearing defective mutations. Conversely, evinacumab, the mAb targeting ANGPTL3, is highly effective in reducing LDL-C levels even in HoFH patients carrying null LDLR mutations, thanks to its LDLR-independent mechanism of action. Summary Monoclonal antibodies inhibiting PCSK9 have shown a robust effect in FH patients presenting a residual LDLR activity, while ANGPTL3 inhibitors appear to be promising even in patients carrying null LDLR mutations.


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