Drug reference
In doses of 1.5 to 3 g daily, it lowers both cholesterol and triglyceride concentrations by inhibiting synthesis; it also increases HDL-cholesterol. Statins competitively inhibit 3-hydroxy- 3-methylglutaryl coenzyme A (HMG CoA) reductase, an enzyme involved in cholesterol synthesis, especially in the liver.
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Adjunct to statin in dyslipidaemia or used alone if statin not tolerated ▶BY MOUTH ▶Adult: (consult product literature)
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Active peptic ulcer disease. arterial bleeding
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Acute myocardial infarction. diabetes mellitus. gout. history of peptic ulceration. unstable angina Elderly. high alcohol intake. history of liver disease. hypothyroidism. known genetic polymorphisms—consult product literature. patients at increased risk of muscle toxicity, including myopathy or rhabdomyolysis (e.g. those with a personal or family history of muscular disorders, previous history of muscular toxicity and a high alcohol intake) CAUTIONS, FURTHER INFORMATION ▶Muscle effects Muscle toxicity can occur with all statins, however the likelihood increases with higher doses and in certain patients (see below). Statins should be used with caution in patients at increased risk of muscle toxicity, including those with a personal or family history of muscular disorders, previous history of muscular toxicity, a high alcohol intake, renal impairment or hypothyroidism. In patients at increased risk of muscle effects, a statin should not usually be started if the baseline creatine kinase concentration is more than 5 times the upper limit of normal (some patients may present with an extremely elevated baseline creatine kinase concentration, for example because of a physical occupation or rigorous exercise—specialist advice should be sought regarding consideration of statin therapy in these patients). ▶Hypothyroidism Hypothyroidism should be managed adequately before starting treatment with a statin.
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Patient decision aid Taking a statin to reduce the risk of coronary heart disease and stroke. National Institute for Health and Care Excellence. November 2014. www.nice.org.uk/about/what-we-do/our-programmes/nice- guidance/nice-guidelines/shared-decision-making
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→Appendix 1: nicotinic acid
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Angioedema. arrhythmias. asthenia. burping. cough aggravated. diarrhoea. dizziness. dyspnoea. flushing. gastrointestinal disorders. gout. hepatic disorders. hyperhidrosis. hypotension. insomnia. macular oedema. migraine. myalgia. myopathy. nausea. nervousness. oedema. palpitations. paraesthesia. respiratory disorders. skin reactions. syncope. tongue oedema. vision blurred. vomiting Cardiovascular system SIDE-EFFECTS, FURTHER INFORMATION Prostaglandin- mediated flushing is common, typically within an hour of dosing and lasting for 15–30 minutes (particularly with the initial doses). Taking after a meal or taking asprin before dosing minimises flushing. ▶Common or very common Asthenia. constipation. diarrhoea. dizziness. flatulence. gastrointestinal discomfort. headache. myalgia. nausea. sleep disorders. thrombocytopenia ▶Uncommon Alopecia. hepatic disorders. memory loss. pancreatitis. paraesthesia. sexual dysfunction. skin reactions. vomiting ▶Rare or very rare Myopathy. peripheral neuropathy. tendinopathy ▶Frequency not known Depression. diabetes mellitus (in those at risk). interstitial lung disease SIDE-EFFECTS, FURTHER INFORMATION Muscle effects The risk of myopathy, myositis, and rhabdomyolysis associated with statin use is rare. Although myalgia has been reported commonly in patients receiving statins, muscle toxicity truly attributable to statin use is rare. When a statin is suspected to be the cause of myopathy, and creatine kinase concentration is markedly elevated or if muscular symptoms are severe, treatment should be discontinued. If symptoms resolve and creatine kinase concentrations return to normal, the statin should be reintroduced at a lower dose and the patient monitored closely. 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.
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No information available—manufacturer advises avoid unless potential benefit outweighs risk. 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.
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Present in milk—avoid.
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Avoid in severe impairment. Discontinue if severe abnormalities in liver function tests. Monitoring Manufacturer advises monitor liver function in mild to moderate hepatic impairment. In general, manufacturers advise caution (risk of increased exposure); avoid in active disease or unexplained persistent elevations in serum transaminases.
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Manufacturer advises use with caution—no information available.
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Adequate contraception is required during treatment and for 1 month afterwards.
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▶Before starting treatment with statins, at least one full lipid profile (non-fasting) should be measured, including total cholesterol, HDL-cholesterol, non-HDL-cholesterol (calculated as total cholesterol minus HDL-cholesterol), and triglyceride concentrations, thyroid-stimulating hormone, and renal function should also be assessed. ▶Liver function There is little information available on a rational approach to liver-function monitoring; however, NICE suggests that liver enzymes should be measured before treatment, and repeated within 3 months and at 12 months of starting treatment, unless indicated at other times by signs or symptoms suggestive of hepatotoxicity (NICE clinical guideline 181 (July 2014). Lipid Modification—Cardiovascular risk assessment and the modification of blood lipids for the primary and secondary prevention of cardiovascular disease). Those with serum transaminases that are raised, but less than 3 times the upper limit of the reference range, should not be routinely excluded from statin therapy. Those with serum transaminases of more than 3 times the upper limit of the reference range should discontinue statin therapy. ▶Creatine kinase Before initiation of statin treatment, creatine kinase concentration should be measured in patients who have had persistent, generalised, unexplained muscle pain (whether associated or not with previous lipid-regulating drugs); if the concentration is more than 5 times the upper limit of normal, a repeat measurement should be taken after 7 days. If the repeat concentration remains above 5 times the upper limit, statin treatment should not be started; if concentrations are still raised but less than 5 times the upper limit, the statin should be started at a lower dose. ▶Diabetes Patients at high risk of diabetes mellitus should have fasting blood-glucose concentration or HbA1C checked before starting statin treatment, and then repeated after 3 months.
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There can be variation in the licensing of different medicines containing the same drug. Forms available from special-order manufacturers include: tablet, modified- release tablet, capsule Capsule ▶Solgar Niacin (Solgar Vitamin and Herb) Nicotinic acid 500 mg Solgar Niacin 500mg capsules | 100 capsule s LIPID MODIFYING DRUGS › STATINS Statins f
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Advise patients to report promptly unexplained muscle pain, tenderness, or weakness. eiiii F 214
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(consult product literature)
First-line fragment. Read the complete Indications and Dose section above.
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