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Published on: November 17, 2018
Safety of HMG-CoA reductase inhibitors: focus on atorvastatin
F Bernini1, A Poli, R Paoletti
1Department of Pharmacological Sciences, University of Milano, Italy.
Insights
Statins are safe and effective for lowering LDL-cholesterol and reducing cardiovascular risk. Adverse events are rare and mild, with low withdrawal rates, ensuring good tolerability in patients.
Area of Science:
- Cardiovascular Medicine
- Pharmacology
Background:
- Statins are a class of drugs widely used to lower LDL-cholesterol.
- They are prescribed to patients with or at risk for coronary heart disease to reduce cardiovascular events and mortality.
- Understanding the safety profile of statins is crucial for long-term patient management.
Purpose of the Study:
- To review the safety and tolerability of statins.
- To highlight common and rare adverse events associated with statin therapy.
- To discuss drug interactions and specific considerations for atorvastatin.
Main Methods:
- Review of existing literature on statin efficacy and safety.
- Analysis of reported adverse events, including gastrointestinal symptoms, elevated transaminases, and myopathy.
- Examination of factors influencing statin safety, such as drug interactions and patient populations.
Main Results:
- Statins effectively reduce LDL-cholesterol and cardiovascular risk.
- Most patients tolerate statins well, with low withdrawal rates (<3%) due to adverse events.
- Common side effects are mild gastrointestinal issues; serious adverse events like myopathy and rhabdomyolysis are very rare.
- Elevated transaminases are infrequent, asymptomatic, reversible, and rarely necessitate drug discontinuation.
- Statins do not negatively impact endocrine function, glycemic control in diabetics, or cancer risk.
Conclusions:
- Statins possess a favorable safety profile with significant cardiovascular benefits.
- Careful consideration of drug interactions is necessary, especially with concomitant medications.
- Atorvastatin demonstrates good long-term tolerability and a safety profile comparable to other statins.
Abstract:
Statins effectively lower LDL-cholesterol and some members of this class have been shown to reduce the risk of major cardiovascular events and total mortality in patients with or at risk for coronary heart disease. Statins are in general well tolerated. Withdrawal rates related to adverse events are low (< or =3%). The most common adverse events are mild gastrointestinal symptoms. Elevated serum transaminase levels occur infrequently (< or = 1.5%). These are generally asymptomatic, reversible and rarely require drug withdrawal. Statins do not cause adverse endocrine effects, do not alter glycemic control in diabetic patients, and do not increase cancer risk. Dose-related myopathy and/or rhabdomyolysis also occurs very rarely, although the risk is increased by concomitant administration of cyclosporine, niacin, fibrates, or by CYP3A4 isoenzyme inhibitors (e.g. erythromycin, systemic azole antifungal agents etc.) with statins metabolized by this isoenzyme. The pharmacokinetics of the individual statin should be considered in patients receiving polypharmacological treatments, to minimize the risk of unfavorable drug interactions. Atorvastatin is well tolerated in long-term treatment of dyslipidemia and is characterized by a safety profile similar to the other available statins.
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