Formulary
Rosuvastatin: Indications, Dosing, Side Effects and Interactions
Statins competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in cholesterol synthesis, especially in the liver.
MedNext Academy | 7 min read
Rosuvastatin: Indications, Dosing, Side Effects and Interactions
Statins competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in cholesterol synthesis, especially in the liver.
Drug action
Statins competitively inhibit 3-hydroxy-3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in cholesterol synthesis, especially in the liver.
Indications and dose
**Primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia (type IIb), or homozygous familial hypercholesterolaemia in patients who have not responded adequately to diet and other appropriate measures**
- **Adult** (By Mouth): 70 years and over Initially 5 mg once daily, then increased if necessary up to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
**Primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia (type IIb), or homozygous familial hypercholesterolaemia in patients who have not responded adequately to diet and other appropriate measures and who have risk factors**
- **Adult** (By Mouth): for myopathy or rhabdomyolysis Initially 5 mg once daily, then increased if necessary up to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
**Severe primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia (type IIb), or homozygous familial hypercholesterolaemia in patients with high cardiovascular risk who have not responded adequately to diet and other appropriate measures (specialist use only)**
- **Adult** (By Mouth): 70 years and over Initially 5 mg once daily, then increased if necessary up to 40 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
**Severe primary hypercholesterolaemia (type IIa including heterozygous familial hypercholesterolaemia), mixed dyslipidaemia (type IIb), or homozygous familial hypercholesterolaemia in patients with high cardiovascular risk who have not responded adequately to diet and other appropriate measures, and who have risk factors**
- **Adult** (By Mouth): for myopathy or rhabdomyolysis (specialist use only) Initially 5 mg once daily, then increased if necessary up to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
**Prevention of cardiovascular events in patients at high risk of a first cardiovascular event**
- **Adult** (By Mouth): 70 years and over Initially 5 mg once daily, then increased if tolerated to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
**Prevention of cardiovascular events in patients at high risk of a first cardiovascular event and with risk factors**
- **Adult** (By Mouth): for myopathy or rhabdomyolysis Initially 5 mg once daily, then increased if tolerated to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
**Heterozygous familial hypercholesterolaemia (specialist use only) for rosuvastatin**
- **Child 6-9 years** (By mouth): Initially 5 mg once daily, then increased if necessary up to 10 mg once daily, dose to be increased gradually at intervals of at least 4 weeks.
- **Child 10-17 years** (By mouth): Initially 5 mg once daily, then increased if necessary up to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks, use lower max. dose in children with risk factors for myopathy or rhabdomyolysis (including personal or family history of muscular disorders or toxicity).
**Homozygous familial hypercholesterolaemia (specialist use only) for rosuvastatin**
- **Child 6-17 years** (By mouth): Initially 5-10 mg once daily, then increased if necessary up to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks, use lower max. dose in children with risk factors for myopathy or rhabdomyolysis (including personal or family history of muscular disorders or toxicity).
- **Child 6-17 years (patients of Asian origin)** (By mouth): Initially 5 mg once daily, then increased if necessary up to 20 mg once daily, dose to be increased gradually at intervals of at least 4 weeks, use lower max. dose in children with risk factors for myopathy or rhabdomyolysis (including personal or family history of muscular disorders or toxicity).
Cautions
Risk factors for muscle toxicity, including myopathy or rhabdomyolysis Cautions, further information Muscle effects Muscle toxicity can occur with all statins, however the likelihood increases with higher doses and in certain patients. Statins should be used with caution in patients at increased risk of muscle toxicity. This includes the elderly, those with a personal or family history of muscular disorders, history of muscular toxicity or unexplained persistent muscle pain, history of liver disease, a high alcohol intake, known genetic polymorphisms-consult product literature, renal impairment, hypothyroidism, or those who undertake strenuous exercise. M See also Monitoring requirements . Hypothyroidism Hypothyroidism should be managed adequately before starting treatment with a statin.
Side effects
Common or very common Arthralgia; asthenia; constipation; diarrhoea; dizziness; flatulence; gastrointestinal discomfort; headache; muscle complaints; nausea; sleep disorders; thrombocytopenia Uncommon Alopecia; hepatic disorders; memory loss; pancreatitis; paraesthesia; sexual dysfunction; skin reactions; vomiting Rare or very rare Lupus-like syndrome; myopathy; peripheral neuropathy; tendon disorders Frequency not known Depression; diabetes mellitus (in those at risk); interstitial lung disease; neuromuscular dysfunction Side-effects, further information Muscle effects Although myalgia has been reported commonly in patients receiving statins, muscle toxicity truly attributable to statin use is rare. The risk of myopathy, myositis, and rhabdomyolysis associated with statin use is also rare. If muscle pain, weakness, or cramps occur during treatment, creatine kinase concentrations should be measured; if the concentration is more than 5 times the ULN (in the absence of strenuous exercise), treatment should be discontinued. If muscular symptoms are severe and cause daily discomfort, treatment discontinuation should be considered, even if creatine kinase concentrations are less than 5 times the ULN. If symptoms resolve and creatine kinase concentrations return to normal, the statin can be reintroduced, or introduction of an alternative statin can be considered, at the lowest dose and the patient monitored closely. Diabetes Statins should not be discontinued if there is an increase in the blood-glucose concentration as the benefits continue to outweigh the risks. Interstitial lung disease If patients develop symptoms such as dyspnoea, cough, and weight loss, they should seek medical attention. Side-effects For rosuvastatin Rare or very rare Gynaecomastia; haematuria; polyneuropathy Frequency not known Cough; dyspnoea; oedema; proteinuria; severe cutaneous adverse reactions (SCARs)
Interactions
**Severe interactions:**
- Statins No clinically significant pharmacokinetic interactions were seen when ezetimibe was co-administered with atorvastatin, simvastatin, pravastatin, lovastatin, fluvastatin or rosuvastatin.
- In drug-drug-interaction studies in human, a weak interaction was observed with rosuvastatin (AUC increase between 1.25 and 2.00 fold) but no significant interaction was found with diclofenac.
- Based on drug interaction studies conducted with Biktarvy or the components of Biktarvy, no clinically significant drug interactions are expected with: amlodipine, atorvastatin, buprenorphine,...
- Potential for Cibinqo to affect pharmacokinetics of other medicinal products No clinically significant effects of Cibinqo were observed in drug interaction studies with oral contraceptives (e.g.
- Effect of fidaxomicin on other transporters Fidaxomicin does not have a clinically significant effect on the exposure of rosuvastatin, a substrate for the transporters OATP2B1 and BCRP.
- Co-administration of 200 mg fidaxomicin twice daily with a single dose of 10 mg rosuvastatin to healthy subjects did not have a clinically significant effect on the AUCinf of rosuvastatin.
- Monitor use of BCRP substrates where small concentration changes may lead to serious toxicity (e.g., rosuvastatin) when used concomitantly with voclosporin.
**Other interactions (67):**
- Relugolix is an inhibitor of breast cancer resistant protein (BCRP) in vitro , therefore, an interaction study was conducted with rosuvastatin, a BCRP and organic anion transporting polypeptide 1B1...
- After co-administration with daily 40-mg doses of relugolix, the AUC and C max of rosuvastatin were decreased by 13% and 23%, respectively.
- The effects are not considered clinically meaningful and therefore no dose-adjustments of rosuvastatin upon concomitant use are recommended.
- Breast cancer resistance protein (BCRP) substrate drugs Macitentan 10 mg once daily did not affect the pharmacokinetics of a BCRP substrate drug (riociguat 1 mg; rosuvastatin 10 mg).
- Therefore, co-administration of maribavir with sensitive BCRP substrates such as rosuvastatin, is expected to increase their exposure and lead to undesirable effects.
- Expected: HMG-CoA reductase inhibitors (BCRP inhibition) No dose adjustment is required.
Pregnancy
Statins should be avoided in pregnancy (discontinue 3 months before attempting to conceive) as congenital anomalies have been reported and the decreased synthesis of cholesterol possibly affects fetal development.
Breast feeding
Manufacturer advises avoid-no information available.
Hepatic impairment
In general, manufacturers advise caution (risk of increased exposure); avoid in active disease or unexplained persistent elevations in serum transaminases.
Renal impairment
Avoid if creatinine clearance less than 30 mL/minute. M Dose adjustments See Prescribing in renal impairment . Initially 5 mg once daily (avoid 40 mg daily) if creatinine clearance 30-60 mL/minute. M
Medicinal forms
Suspension,Tablet,Capsule
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
Inside MedNext for this topic
- 411 MedNext-authored chapters
- 80,000+ MCQ bank
- 15 study modes
- Growing visual cheat sheets
Study modes
- Notes
- MCQ
- Audio
- Video
- Visual
- 3D Anatomy
- Trace
- Flashcards
- Mnemonics
- Image Bank
- Clinical
- Microscopy
- Audio QBank
- Cadaver
- Book Match
Continue reading
Subject HubPharmacology Hub
All pharmacology resources in one place.
Drug SchedulesIndian Drug Schedules
Schedule H, H1, X and G classifications.
FormularyBrowse all drugs
Search 1,850+ drug profiles.
Study Rosuvastatin in the MedNext app
Challenge yourself with targeted pharmacology MCQs on this drug class. Every explanation links back to the chapter that teaches the concept.
Start drug challengeExplore the full formulary