HMG-CoA reductase inhibitors (statins)
ATC code: C10AA07 (Rosuvastatin)
Competitive HMG-CoA reductase inhibitor, like atorvastatin. Key differences: more potent lowering per milligram – reduces LDL by 45-55% at the maximum dose. Hydrophilic, with minimal CYP3A4 metabolism – resulting in fewer drug interactions with macrolides, azoles, and grapefruit.
First line
Prescribed according to cardiovascular risk stratification, same as atorvastatin. Rosuvastatin's advantage is greater reduction at lower doses: 5-10 mg of rosuvastatin is equivalent to 20-40 mg of atorvastatin. Convenient when potent lipid lowering is needed at a minimal dose.
First line
High-intensity statin (rosuvastatin 20-40 mg daily) for secondary prevention in established ASCVD. 2019 target: reduction over 50% from baseline and below 1.4 mmol/L. The JUPITER trial showed a 44% reduction in cardiovascular events in patients with elevated CRP. Interchangeable with atorvastatin in the high-intensity regimen.
First line
Familial hypercholesterolemia requires high-intensity statins. Rosuvastatin 20-40 mg provides the greatest reduction among oral statins. If insufficient, ezetimibe is added, followed by PCSK9 inhibitors.
The drug is promoted for these uses outside international guidelines. Each entry below is analyzed against AEMPS, FDA, EMA, Cochrane and major RCTs.
Not recommended
Rosuvastatin is a high-potency statin. It is prescribed for hyperlipidemia and for primary/secondary CV prevention in high-risk patients ( 2019, 2018; the JUPITER 2008 trial showed benefit at below 130 mg/dL with elevated hsCRP). In biohacker and longevity communities, rosuvastatin is actively promoted as a life-extension drug and a suppressor of chronic inflammation of aging. In people with normal lipid profile and low CV risk, clinical studies do not justify prophylactic use: the Ridker 2012 meta-analysis showed that JUPITER's benefit is limited to patients with specific risk markers. The drug causes myalgia, elevated transaminases, risk of rhabdomyolysis, elevated glucose, and new-onset diabetes risk. If rosuvastatin was prescribed at normal lipid levels, consider seeking a second opinion.
7 pairs found. Sorted from critical to minor.
Mechanism
Cyclosporine blocks the OATP1B1 transporter, the uptake route of rosuvastatin into hepatocytes. Rosuvastatin levels rise 7-fold. This is unique among statins: other cyclosporine–statin pairs go through CYP3A4, but rosuvastatin barely uses CYP3A4 – OATP1B1 drives the risk.
Symptoms
Pain and weakness in large muscle groups (thighs, shoulders, calves), dark urine, elevated creatine kinase. Severe cases progress to rhabdomyolysis with acute kidney injury. Symptoms appear within 1–2 weeks of co-prescription.
Management
The combination is not prescribed. For transplant patients needing a statin, use pravastatin up to 20 mg/day. Check creatine kinase at 4–6 weeks.
Mechanism
Additive myopathy and rhabdomyolysis risk. Rosuvastatin suppresses muscle ubiquinone synthesis; colchicine disrupts microtubule function in myocytes. Severe muscle toxicity has been reported, especially in older patients and chronic kidney disease.
Symptoms
Pain and weakness in large muscle groups (thighs, shoulders, calves), dark urine, elevated creatine kinase. Severe cases progress to rhabdomyolysis with acute kidney injury. Symptoms appear within 1–4 weeks of co-administration.
Management
Avoid prolonged combination. For acute gout, a short colchicine course (3–5 days) at 0.3 mg every other day is acceptable with muscle symptom and creatine kinase monitoring. Alternative: intra-articular or short systemic glucocorticoid.
Mechanism
Rosuvastatin barely uses CYP3A4 but is a substrate of OATP1B1 and BCRP transporters, both inhibited by ritonavir. Rosuvastatin plasma levels rise 2- to 4-fold.
Symptoms
Pain and weakness in large muscle groups (thighs, shoulders, calves), dark urine, elevated creatine kinase. Severe cases progress to rhabdomyolysis with acute kidney injury. Symptoms appear within 1–4 weeks of co-administration.
Management
On ritonavir-boosted antiretroviral therapy, cap rosuvastatin at 10 mg/day. Check creatine kinase at 4–6 weeks and on muscle symptoms.
Mechanism
Rosuvastatin is minimally metabolised by CYP3A4, so amiodarone's CYP3A4 inhibition has limited effect. A slight AUC rise is possible via OATP1B1 transport. Additive myopathy risk is modest.
Symptoms
Muscle pain, weakness, dark urine. Rhabdomyolysis with rosuvastatin and amiodarone is rare.
Management
No dose adjustment needed. Cap rosuvastatin at 20 mg/day with amiodarone. Check CK if muscle pain develops. Alternative: pravastatin (minimal interaction).
Mechanism
Dual statin therapy – doubling the same pharmacological class with additive myopathy risk and no therapeutic benefit.
Symptoms
Pain and weakness in large muscle groups (thighs, shoulders, calves), dark urine, elevated creatine kinase. Symptoms usually appear 2–6 weeks after starting the combination.
Management
The combination is not prescribed. Use one statin titrated to target. If LDL is not at goal on the maximum statin dose, add ezetimibe or a PCSK9 inhibitor, not a second statin.
Mechanism
Rosuvastatin is minimally metabolised by CYP2C9 and excreted mainly unchanged via the liver and kidneys. Azithromycin does not affect these routes.
Symptoms
The combination usually causes no specific symptoms. Each drug's individual side effects remain.
Management
No dose adjustment needed. The combination is standard when a macrolide is needed on rosuvastatin.
Mechanism
Rosuvastatin is excreted mainly unchanged and minimally metabolised by CYP. Clarithromycin (a strong CYP3A4 inhibitor) does not significantly change rosuvastatin AUC.
Symptoms
The combination usually causes no specific symptoms. Each drug's individual side effects remain.
Management
No dose adjustment needed. Rosuvastatin is the preferred statin when a short clarithromycin or erythromycin course is needed. Atorvastatin and simvastatin should not be combined with clarithromycin — rhabdomyolysis risk.
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In July 2021 the FDA removed the automatic contraindication during pregnancy from labels of all statins (Drug Safety Communication, 2021-07-20). The FDA pregnancy categories (A/B/C/D/X) were retired in 2015 under the PLLR — historically rosuvastatin was classified as X. The decision is now individualized: in patients without atherosclerotic CVD, statins are usually discontinued before conception and throughout pregnancy; in those with documented atherosclerosis and high event risk, continuation is possible after shared decision-making with a cardiologist. An unplanned pregnancy is a trigger for discussion, not for default discontinuation.
Systemic safety data during lactation are limited. The manufacturer and most international sources recommend avoidance. In patients with a statin indication, options include a temporary switch to formula feeding or deferring therapy until breastfeeding is complete.
Reference information, not a clinical decision. Discuss feeding pauses or changes with your physician or an IBCLC.
Rosuvastatin is evaluated for the following indications with varying evidence strength: Established ASCVD, secondary prevention (evidence tier A), Dyslipidemia, primary CV prevention (evidence tier A), Familial hypercholesterolemia (evidence tier A). See the full indication matrix with dosing and citations above on this page.
Common side effects of Rosuvastatin (≥ 1 in 100): Myalgia without CK elevation, Headache, Dyspepsia, nausea, Arthralgia, Transient transaminase elevation. See the Safety section for uncommon and serious reactions.
FDA category X. In July 2021 the FDA removed the automatic contraindication during pregnancy from labels of all statins (Drug Safety Communication, 2021-07-20). The FDA pregnancy categories (A/B/C/D/X) were retired in 2015 under the PLLR — historically rosuvastatin was classified as X. The decision is now individualized: in patients without atherosclerotic CVD, statins are usually discontinued before conception and throughout pregnancy; in those with documented atherosclerosis and high event risk, continuation is possible after shared decision-making with a cardiologist. An unplanned pregnancy is a trigger for discussion, not for default discontinuation.
Systemic safety data during lactation are limited. The manufacturer and most international sources recommend avoidance. In patients with a statin indication, options include a temporary switch to formula feeding or deferring therapy until breastfeeding is complete.
Rosuvastatin is contraindicated in: Active liver disease or unexplained persistent transaminase elevation; Severe renal impairment (CrCl below 30 mL/min) for the 40 mg dose; Hypersensitivity to rosuvastatin or any component. Full list in the Safety section.