Rosuvastatin dose

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Rosuvastatin Dose: Pharmacokinetics, Efficacy, and Safety

Pharmacokinetics of Rosuvastatin

Rosuvastatin, a potent lipid-lowering agent, is administered once daily in doses ranging from 5 to 80 mg, with 40 mg being the maximum approved daily dose . The drug achieves its maximum plasma concentration approximately 5 hours after administration under fasting conditions . The mean absolute oral availability of rosuvastatin is about 20%, with a total clearance rate of 28.3 L/h and an elimination half-life of around 20 hours . Notably, there is significant variability in the pharmacokinetics of rosuvastatin among different races, with Caucasian subjects exhibiting a 1.7-fold higher clearance rate compared to Chinese subjects . Additionally, rosuvastatin shows a large coefficient of variation in systemic exposure (48%) and minor accumulation with repeated dosing .

Efficacy of Rosuvastatin in Lowering LDL-C

Rosuvastatin is highly effective in reducing low-density lipoprotein cholesterol (LDL-C). In dose-ranging studies, rosuvastatin demonstrated significant, dose-dependent reductions in LDL-C, with decreases ranging from 34% at 1 mg to 65% at 80 mg . The VOYAGER meta-analysis further confirmed that rosuvastatin doses of 5, 10, 20, and 40 mg reduced LDL-C by 39%, 44%, 50%, and 55%, respectively . These reductions were more substantial compared to equivalent doses of atorvastatin and simvastatin, with rosuvastatin showing 3 to 3.5 times higher potency than atorvastatin and 7 to 8 times higher potency than simvastatin .

Comparative Efficacy with Other Statins

In comparative studies, rosuvastatin consistently outperformed other statins in lowering LDL-C and achieving lipid goals. For instance, rosuvastatin 10 mg reduced LDL-C by 44.6%, significantly more than atorvastatin 20 mg, which reduced LDL-C by 42.7% . Similarly, the STELLAR trial demonstrated that rosuvastatin 10 to 80 mg reduced LDL-C by 8.2% more than atorvastatin, 26% more than pravastatin, and 12% to 18% more than simvastatin . These findings highlight rosuvastatin's superior efficacy in lipid management.

Safety and Tolerability

Rosuvastatin is generally well tolerated across various doses. In controlled trials, the adverse event profile of rosuvastatin 10 to 40 mg was similar to that of atorvastatin, simvastatin, and pravastatin . Myopathy occurred in less than 0.03% of patients, and no cases of rhabdomyolysis were reported at doses up to 40 mg . Additionally, clinically significant elevations in liver enzymes were rare, occurring in only 0.2% of patients . Even in patients with a history of statin intolerance, a once-a-week dosing regimen of rosuvastatin was well tolerated and led to significant lipid improvements .

Conclusion

Rosuvastatin is a highly effective and well-tolerated statin for lowering LDL-C and other atherogenic lipoproteins. Its pharmacokinetic profile, superior efficacy compared to other statins, and favorable safety profile make it a valuable option in the management of hypercholesterolemia and dyslipidemia.

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Most relevant research papers on this topic

Pharmacokinetics of Rosuvastatin: A Systematic Review of Randomised Controlled Trials in Healthy Adults

Rosuvastatin's pharmacokinetics vary significantly between races, with potential clinical relevance in drug interactions with darunavir/ritonavir and erythromycin.

Systematic ReviewRigorous Journal

2021·

16citations

·R. Kanukula et al.

Doses of rosuvastatin, atorvastatin and simvastatin that induce equal reductions in LDL-C and non-HDL-C: Results from the VOYAGER meta-analysis

Rosuvastatin doses are equivalent to 3–3.5 times higher atorvastatin and 7–8 times higher simvastatin doses for achieving equal reductions in LDL-C and non-HDL-C levels.

Meta-Analysis

2016·

52citations

·B. Karlson et al.

Effect of rosuvastatin on low-density lipoprotein cholesterol in patients with hypercholesterolemia.

Rosuvastatin rapidly reduces LDL cholesterol and is well-tolerated in hypercholesterolemic patients, with 90% of reduction occurring within 2 weeks of treatment.

RCTHighly Cited

2001·

203citations

·A. Olsson et al.

A double-blind, randomized, incomplete crossover trial to assess the dose proportionality of rosuvastatin in healthy volunteers.

Rosuvastatin systemic exposure is dose proportional in healthy men at doses of 10 to 80 mg, with well-tolerated results in this study.

RCT

2003·

59citations

·Paul D. Martin et al.

Randomized dose-response study of rosuvastatin in Japanese patients with hypercholesterolemia.

Rosuvastatin effectively reduces LDL-C and improves other lipid fractions in Japanese hypercholesterolemic patients, with well-tolerated doses.

RCT

2003·

53citations

·Y. Saito et al.

Once-a-week rosuvastatin (2.5 to 20 mg) in patients with a previous statin intolerance.

Rosuvastatin once a week is well tolerated and leads to significant lipoprotein changes in patients with a history of statin intolerance.

Non-RCTHighly Cited

2009·

70citations

·Janelle F. Ruisinger et al.

Comparison of the efficacy and safety of rosuvastatin 10 mg and atorvastatin 20 mg in high-risk patients with hypercholesterolemia – Prospective study to evaluate the Use of Low doses of the Statins Atorvastatin and Rosuvastatin (PULSAR)

Rosuvastatin 10 mg is more effective and cost-effective than atorvastatin 20 mg in achieving low-density lipoprotein cholesterol goals in high-risk patients with hypercholesterolemia.

RCTLarge Human TrialVery Rigorous JournalHighly Cited

2006·

84citations

·M. Clearfield et al.

A dose-titration and comparative study of rosuvastatin and atorvastatin in patients with homozygous familial hypercholesterolaemia.

Rosuvastatin may have therapeutic value in managing homozygous familial hypercholesterolaemia, with rosuvastatin 80 mg and atorvastatin 80 mg showing similar efficacy and well-tolerated results.

RCTHighly Cited

2008·

91citations

·A. Marais et al.

Comparison of the efficacy and safety of rosuvastatin versus atorvastatin, simvastatin, and pravastatin across doses (STELLAR* Trial).

Rosuvastatin effectively reduces LDL cholesterol more effectively than atorvastatin, simvastatin, and pravastatin, with similar drug tolerability across doses.

RCTLarge Human TrialHighly Cited

2003·

1269citations

·Peter H. Jones et al.

Benefit-risk assessment of Rosuvastatin 10 to 40 milligrams.

Rosuvastatin 10 to 40 mg has a very favorable benefit-risk profile, reducing LDL cholesterol and improving various lipid measures while maintaining similar adverse event profiles to other statins.

Non-RCTLarge Human TrialHighly Cited

2003·

199citations

·H. Brewer

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