Since their introduction in the 1980s, 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase inhibitors (statins) have emerged as the one of the best-selling medication classes to date, with numerous trials demonstrating powerful efficacy in preventing cardiovascular outcomes. As our understanding of low-density lipoprotein cholesterol (LDL-C) and atherosclerosis continues to grow, the concept of 'lower is better' has corresponded with a more is better' approach to statin-based therapy. This review provides a detailed understanding of the clinical efficacy and safety of statins with a particular emphasis on the third generation drug, rosuvastatin.
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"Lipid-lowering medicines and in particular , HMG-CoA reductase inhibitors (statins), are commonly used to reduce the risk of negative cardiovascular outcomes    . Clinical studies have proven the efficacy and safety of statins in the treatment of these diseases    . However, problems associated with adverse drug reactions (ADRs) have emerged as the use of these medicines becomes more widespread. "
[Show abstract][Hide abstract]ABSTRACT: In Estonia, HMG-CoA reductase inhibitors are widely used to modify lipid levels but there are no current data on additional medicines prescribed alongside the statins. The aim of this study was to identify the frequency of potential clinically relevant interactions at a national level among an outpatient population treated with statins between January and June 2008, based on the prescription database of the Estonian Health Insurance Fund. This retrospective prevalence study included 203,646 outpatients aged 50 years or older, of whom 29,367 received statin therapy. The study analysed individuals who had used at least one prescription medicine for a minimum of 7 days concomitantly with statins. Potential drug interactions were analysed using Epocrates online, Stockley’s Drug Interactions, and the drug interaction database developed in Estonia. Statins metabolised by the CYP3A4 isoenzyme were prescribed to 64% of all statin users. Medicines known to have potentially clinically significant interactions with statins were prescribed to 4.6% of patients.
The drugs prescribed concomitantly most often with simvastatin were warfarin (5.7%) and amiodarone (3.9%), whereas digoxin (1.2%) and ethinylestradiol (2%) were prescribed with atorvastatin.
Potential interactions were not detected in the treatment regimens of rosuvastatin, pravastatin, and fluvastatin users.
"The most recent drugs developed for this purpose are statins or 3-hydroxy-3-methyglutaryl coenzyme A reductase inhibitors which used for prevention and treatment of CHD; they lower cholesterol levels by 20% -30%, and even more at higher doses, and this has been clinically proven to produce an equivalent decrease in the risk of myocardial infarction and death . Statins have become one of the best-selling medication classes to date since their introduction into the marketplace in 1986, and include the following drugs commercially available in the US: atorvastatin, lovastatin, pravastatin, fluvastatin, simvastatin and rosuvastatin . Statins are highly effective in reducing cardiovascular mortality and are widely prescribed with best selling. "
[Show abstract][Hide abstract]ABSTRACT: Statins, which are inhibitors of 3-hydroxy-3-methylglutaryl-CoA (HMG-CoA) reductase, are consi-dered as one of the most important drugs and the drug of choice for reducing an abnormal choles-terol level. Statins are normally used to decrease the risk of coronary heart disease (CHD), but they tend to be associated with liver adverse effects. The objective of this prospective study was to investigate the effect of atorvastatin therapy on the liver function in patients with CHD. Study comprised of 66 newly diagnosed CHD patients who were selected from UNRWA clinics in the Gaza Strip. The patients were clinically examined and treated with atorvastatin (10 -40 mg/day). A questionnaire was used to collect the data concerning patient's characteristics. Total cholesterol (TC), triglycerides (TG), high density lipoprotein cholesterol (HDL-C), low-density lipoprotein cholesterol (LDL-C), liver enzymes tests such as alanine aminotransferase (ALT) and aspartate aminotransferase (AST) and total and direct blood bilirubin were measured before starting treatment and after 3 and 6 months of treatment. The results showed a significant increase in the mean values of ALT, AST, total bilirubin and direct bilirubin levels after 3 months then decreased after the next 3 months, but they were higher than the baseline with insignificant association.
"Several clinical trials have shown a positive correlation between greater levels of LDL-C lowering and greater reductions in coronary heart disease risk.83,84 Statins, currently the most powerful class of lipid-lowering drugs, can help decrease LDL-C levels by 20%–55%, depending on the statin molecule and dosage.85 In addition, combination of statins with ezetimibe, bile-acid sequestrants, or niacin produces an additional 10%–20% decrease in LDL-C.86 "
[Show abstract][Hide abstract]ABSTRACT: Proprotein convertase subtilisin/kexin type 9 (PCSK9) directly binds to the epidermal growth factor-like repeat A domain of low-density lipoprotein receptor and induces its degradation, thereby controlling circulating low-density lipoprotein cholesterol (LDL-C) concentration. Heterozygous loss-of-function mutations in PCSK9 can decrease the incidence of coronary heart disease by up to 88%, owing to lifelong reduction of LDL-C. Moreover, two subjects with PCSK9 loss-of-function mutations on both alleles, resulting in a total absence of functional PCSK9, were found to have extremely low circulating LDL-C levels without other apparent abnormalities. Accordingly, PCSK9 could represent a safe and effective pharmacological target to increase clearance of LDL-C and to reduce the risk of coronary heart disease. Recent clinical trials using anti-PCSK9 monoclonal antibodies that block the PCSK9:low-density lipoprotein receptor interaction were shown to considerably reduce LDL-C levels by up to 65% when given alone and by up to 72% in patients already receiving statin therapy. In this review, we will discuss how major scientific breakthroughs in PCSK9 cell biology have led to the development of new and forthcoming LDL-C-lowering pharmacological agents.
Full-text · Article · Oct 2013 · Drug Design, Development and Therapy