Drugs List

Therapeutic Indications

Uses

Homozygous familial hypercholesterolaemia: Adjunct to diet
Mixed dyslipidaemia (type IIb) - adjunct to diet
Primary hypercholesterolaemia (hyperlipidaemia type IIa): Adjunct to diet

Treatment of severe hypercholesterolaemia in patients at high cardiovascular risk (in particular those with familial hypercholesterolaemia) who do not reach full treatment on 20mg.

Administration

For those with swallowing difficulties, rosuvastatin capsules may be given with soft food. The capsule should be opened carefully and the granules sprinkled on one teaspoon of soft food. Do not chew the granules.
For those with a nasogastric tube in place, rosuvastatin capsules may be administered via syringe. The capsule should be opened carefully and the granules emptied into the syringe barrel, then add water. The syringe should be shaken vigorously for 15 seconds and then administered immediately through the nasogastric tube into the stomach. See product literature for further details.

Contraindications

Asian ancestry
Children under 18 years
Creatine kinase levels over 5 times upper limit of normal
Family history of hereditary muscular disorders
High alcohol intake
Predisposition to renal failure secondary to rhabdomyolysis
Within 7 days of discontinuing systemic fusidic acid
Active liver disease
Breastfeeding
Elevated serum transaminases - if persistent and unexplained
Hepatic impairment - Child-Pugh score greater than or equal to 9
Hereditary muscular disorder
History of muscular toxicity secondary to fibrates
History of muscular toxicity secondary to HMG-CoA reductase inhibitors
Hypothyroidism
Myopathy
Pregnancy
Renal impairment - creatinine clearance below 60ml/minute
Serum transaminases above 3 times upper limit of normal

Precautions and Warnings

Females of childbearing potential
Impaired glucose tolerance
Patients over 70 years
Predisposition to myopathy or rhabdomyolysis
SLCO1B1 (OATP1B1) genetic polymorphism
Galactosaemia
Glucose-galactose malabsorption syndrome
Hepatic impairment - Child-Pugh score between 8 and 9
History of hepatic impairment
Lactose intolerance

Advise patient dizziness may affect ability to drive or operate machinery
Correct hypothyroidism before treatment
Exclude secondary causes of hypercholesterolaemia before treatment
Treatment to be initiated and supervised by a specialist
Some formulations contain lactose
Measure creatine kinase levels prior to treatment if risk of rhabdomyolysis
Perform liver function tests before commencing therapy
Monitor creatine kinase levels in patients at risk of rhabdomyolysis
Monitor creatine kinase levels in patients reporting myalgia
Monitor patients with existing or tendency towards diabetes mellitus
Monitor renal function
Repeat liver function tests within 3 months and at 12 months
Advise patient to monitor for and report any skin changes
Advise patient to report any symptoms of interstitial lung disease
Advise patients to report muscle pain/tenderness/weakness
Advise patients to report signs of hepatic damage (malaise, jaundice etc.)
Discontinue if myopathy is suspected
Advise patient to seek advice at first indications of pregnancy
Discontinue and do not restart if severe cutaneous adverse reactions occur
Discontinue if ALT level exceed 3 times the upper limit of normal & persist
Discontinue if AST level exceed 3 times the upper limit of normal & persist
Discontinue if creatine kinase levels >5 times upper limit of normal
Discontinue if evidence of interstitial lung disease
Discontinue if muscular symptoms are severe
Avoid antacids within 2 hours of dose
Dietary restrictions should be maintained
Female: Contraception required during and for 3 months after treatment

Renal function should be assessed throughout treatment.
Statin therapy has been associated with the development of myalgia, myopathy and rhabdomyolysis, particularly in patients receiving higher than 20mg doses.
Do not measure creatine kinase levels following strenuous exercise or in the presence of other factors affecting creatine kinase levels. If creatine kinase is greater than 5 times the upper limit of normal (ULN) levels prior to treatment, re-measure 5 to 7 days later. If symptoms of myopathy resolve and levels of creatinine kinase reduce, treatment can be reinitiated at the lowest dose and with close monitoring.
Some evidence suggests that statins, as a class, raise blood glucose levels. In some patients, at a high risk of future diabetes, rosuvastatin may produce a level of hyperglycaemia where formal diabetes care is appropriate. This risk, however is outweighed by the reduction in vascular risk with statins and therefore should not be a reason for stopping statin treatment. Patients at risk (raised fasting glucose, raised body mass index at baseline, history of hypertension and raised triglycerides) should be monitored both clinically and biochemically according to national guidelines.

Pregnancy and Lactation

Pregnancy

Rosuvastatin is contraindicated during pregnancy.
Use of rosuvastatin during pregnancy is contraindicated by the manufacturer. At the time of writing there is limited published information regarding the use of rosuvastatin during pregnancy. However, as cholesterol is essential for the development of the foetus, the potential risk from inhibition of HMG-CoA reductase outweighs the advantage of treatment during pregnancy.

Lactation

Rosuvastatin is contraindicated during breastfeeding.
Use of rosuvastatin when breastfeeding is contraindicated by the manufacturer. Animal data reports levels of rosuvastatin in the breast milk, however the presence in human breast milk and its effects on exposed infants are unknown.

Side Effects

Abdominal pain
Acute renal failure
Angioedema
Arthralgia
Asthenia
Constipation
Cough
Creatine kinase increased
Depression
Diarrhoea
Dizziness
Drug rash with eosinophilia and systemic symptoms (DRESS)
Dyspnoea
Gynaecomastia
Haematuria
Headache
Hepatitis
Hypersensitivity reactions
Immune mediated necrotizing myopathy
Increase of liver transaminases
Insomnia
Interstitial lung disease
Jaundice
Lupus erythematosus-like syndrome
Memory loss
Muscle rupture
Myalgia
Myopathy
Myositis
Nausea
Nightmares
Oedema
Pancreatitis
Peripheral neuropathy
Polyneuropathy
Precipitation of diabetes
Proteinuria
Pruritus
Rash
Rhabdomyolysis
Sexual dysfunction
Sleep disturbances
Stevens-Johnson syndrome
Tendon disorder
Tendon rupture
Thrombocytopenia
Urticaria

Presentation

Oral formulations of rosuvastatin containing 30mg and 40mg.

Drugs List

Therapeutic Indications

Uses

Homozygous familial hypercholesterolaemia: Adjunct to diet
Mixed dyslipidaemia (type IIb) - adjunct to diet
Primary hypercholesterolaemia (hyperlipidaemia type IIa): Adjunct to diet

Treatment of severe hypercholesterolaemia in patients at high cardiovascular risk (in particular those with familial hypercholesterolaemia) who do not reach full treatment on 20mg.

Dosage

Adults

Patients with Hepatic Impairment

Additional Dosage Information

Administration

For those with swallowing difficulties, rosuvastatin capsules may be given with soft food. The capsule should be opened carefully and the granules sprinkled on one teaspoon of soft food. Do not chew the granules.
For those with a nasogastric tube in place, rosuvastatin capsules may be administered via syringe. The capsule should be opened carefully and the granules emptied into the syringe barrel, then add water. The syringe should be shaken vigorously for 15 seconds and then administered immediately through the nasogastric tube into the stomach. See product literature for further details.

Contraindications

Asian ancestry
Children under 18 years
Creatine kinase levels over 5 times upper limit of normal
Family history of hereditary muscular disorders
High alcohol intake
Predisposition to renal failure secondary to rhabdomyolysis
Within 7 days of discontinuing systemic fusidic acid
Active liver disease
Breastfeeding
Elevated serum transaminases - if persistent and unexplained
Hepatic impairment - Child-Pugh score greater than or equal to 9
Hereditary muscular disorder
History of muscular toxicity secondary to fibrates
History of muscular toxicity secondary to HMG-CoA reductase inhibitors
Hypothyroidism
Myopathy
Pregnancy
Renal impairment - creatinine clearance below 60ml/minute
Serum transaminases above 3 times upper limit of normal

Precautions and Warnings

Females of childbearing potential
Impaired glucose tolerance
Patients over 70 years
Predisposition to myopathy or rhabdomyolysis
SLCO1B1 (OATP1B1) genetic polymorphism
Galactosaemia
Glucose-galactose malabsorption syndrome
Hepatic impairment - Child-Pugh score between 8 and 9
History of hepatic impairment
Lactose intolerance

Advise patient dizziness may affect ability to drive or operate machinery
Correct hypothyroidism before treatment
Exclude secondary causes of hypercholesterolaemia before treatment
Treatment to be initiated and supervised by a specialist
Some formulations contain lactose
Measure creatine kinase levels prior to treatment if risk of rhabdomyolysis
Perform liver function tests before commencing therapy
Monitor creatine kinase levels in patients at risk of rhabdomyolysis
Monitor creatine kinase levels in patients reporting myalgia
Monitor patients with existing or tendency towards diabetes mellitus
Monitor renal function
Repeat liver function tests within 3 months and at 12 months
Advise patient to monitor for and report any skin changes
Advise patient to report any symptoms of interstitial lung disease
Advise patients to report muscle pain/tenderness/weakness
Advise patients to report signs of hepatic damage (malaise, jaundice etc.)
Discontinue if myopathy is suspected
Advise patient to seek advice at first indications of pregnancy
Discontinue and do not restart if severe cutaneous adverse reactions occur
Discontinue if ALT level exceed 3 times the upper limit of normal & persist
Discontinue if AST level exceed 3 times the upper limit of normal & persist
Discontinue if creatine kinase levels >5 times upper limit of normal
Discontinue if evidence of interstitial lung disease
Discontinue if muscular symptoms are severe
Avoid antacids within 2 hours of dose
Dietary restrictions should be maintained
Female: Contraception required during and for 3 months after treatment

Renal function should be assessed throughout treatment.
Statin therapy has been associated with the development of myalgia, myopathy and rhabdomyolysis, particularly in patients receiving higher than 20mg doses.
Do not measure creatine kinase levels following strenuous exercise or in the presence of other factors affecting creatine kinase levels. If creatine kinase is greater than 5 times the upper limit of normal (ULN) levels prior to treatment, re-measure 5 to 7 days later. If symptoms of myopathy resolve and levels of creatinine kinase reduce, treatment can be reinitiated at the lowest dose and with close monitoring.
Some evidence suggests that statins, as a class, raise blood glucose levels. In some patients, at a high risk of future diabetes, rosuvastatin may produce a level of hyperglycaemia where formal diabetes care is appropriate. This risk, however is outweighed by the reduction in vascular risk with statins and therefore should not be a reason for stopping statin treatment. Patients at risk (raised fasting glucose, raised body mass index at baseline, history of hypertension and raised triglycerides) should be monitored both clinically and biochemically according to national guidelines.

Pregnancy and Lactation

Pregnancy

Rosuvastatin is contraindicated during pregnancy.
Use of rosuvastatin during pregnancy is contraindicated by the manufacturer. At the time of writing there is limited published information regarding the use of rosuvastatin during pregnancy. However, as cholesterol is essential for the development of the foetus, the potential risk from inhibition of HMG-CoA reductase outweighs the advantage of treatment during pregnancy.

Lactation

Rosuvastatin is contraindicated during breastfeeding.
Use of rosuvastatin when breastfeeding is contraindicated by the manufacturer. Animal data reports levels of rosuvastatin in the breast milk, however the presence in human breast milk and its effects on exposed infants are unknown.

Side Effects

Abdominal pain
Acute renal failure
Angioedema
Arthralgia
Asthenia
Constipation
Cough
Creatine kinase increased
Depression
Diarrhoea
Dizziness
Drug rash with eosinophilia and systemic symptoms (DRESS)
Dyspnoea
Gynaecomastia
Haematuria
Headache
Hepatitis
Hypersensitivity reactions
Immune mediated necrotizing myopathy
Increase of liver transaminases
Insomnia
Interstitial lung disease
Jaundice
Lupus erythematosus-like syndrome
Memory loss
Muscle rupture
Myalgia
Myopathy
Myositis
Nausea
Nightmares
Oedema
Pancreatitis
Peripheral neuropathy
Polyneuropathy
Precipitation of diabetes
Proteinuria
Pruritus
Rash
Rhabdomyolysis
Sexual dysfunction
Sleep disturbances
Stevens-Johnson syndrome
Tendon disorder
Tendon rupture
Thrombocytopenia
Urticaria

Overdosage

It is strongly recommended that the UK National Poisons Information Service be consulted on cases of suspected or actual overdose where there is doubt over the degree of risk or about appropriate management.
The following number will direct the caller to the relevant local centre (0844) 892 0111
Information may be obtained if you have access to ToxBase the primary clinical toxicology database of the National Poisons Information Service. This is available via password on the internet ( www.toxbase.org ) or if this is unavailable at the backup site ( www.toxbasebackup.org ).

Further Information

Last Full Review Date: April 2022

Reference Sources

Summary of Product Characteristics: Crestor 40mg film-coated tablets. AstraZeneca UK Limited. Revised August 2021.

Summary of Product Characteristics: Rosuvastatin 30mg film-coated tablets. Zentiva UK Ltd. Revised January 2022.
Summary of Product Characteristics: Rosuvastatin 40mg hard capsules. Sun Pharmaceutical Industries Europe B.V. Revised May 2021.
Summary of Product Characteristics: Rosuvastatin 40mg Film-coated Tablets. Teva UK Ltd. Revised July 2021.
NICE Evidence Services Available at: www.nice.org.uk Last accessed: 23 March 2022