Simvastatin is one of the first "statins" (HMG-CoA reductase inhibitors) approved for treating high cholesterol and reducing the risk of stroke, death from heart disease, and risk of heart attacks. Its most common side effects are headache, nausea, vomiting, diarrhea, abdominal pain, and muscle pain. Like other statins it can cause muscle break down. This drug available in 10 mg and 20 mg tablet. It is used along with exercise, diet, and weight loss to decrease elevated lipid levels.It is also used to decrease the risk of heart problems in those at high risk.
Simvastatin is one of the top ten prescribed drugs in the U.S. Simvastatin is generic drug and available in several brands such as Zocor.
Drug Fact
Class : Statin
Category : Prescription Drug / Prescription only
Uses : treating high cholesterol and reducing the risk of stroke, death from heart disease, and risk of heart attacks
Consumed by : Adult and child with age 10 years or above
Pregnancy category : X
Category X: Studies in animals or human beings have demonstrated fetal abnormalities or there is evidence of fetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.
Dosage form : tablet, suspension
Administration
May be taken with or without food. Take in the evening. Avoid excessive consumption (>1 L/day) of grapefruit juice.
Contraindications
Active liver disease or unexplained persistent elevations of serum transaminases, myopathy secondary to other lipid-lowering agents. Concurrent use with potent CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, posaconazole, voriconazole, clarithromycin, erythromycin, telithromycin, nefazodone, HIV protease inhibitors, cobicistat containing products, fusidic acid), ciclosporin, danazol and gemfibrozil. Pregnancy and lactation.
Special Precautions
Patients with diabetes mellitus, predisposing factors for myopathy/rhabdomyolysis (e.g. uncontrolled hypothyroidism, personal or family history of muscular disorders, history of muscular toxicity with a statin or fibrate, alcohol abuse). Renal and hepatic impairment. Children and elderly. Patients with SLCO1B1 gene polymorphism. Coadministration of niacin (≥1 g) in patients of Chinese descent. A dose of 80 mg should be restricted to patients who have been taking simvastatin 80 mg for 12 months or more. Temporarily discontinue simvastatin prior to elective major surgery.
Adverse Reactions
Significant: Increased serum transaminase.
Blood and lymphatic system disorders: Anaemia.
Gastrointestinal disorders: Constipation, abdominal pain, flatulence, dyspepsia, diarrhoea, nausea, acid regurgitation, vomiting, pancreatitis.
Hepatobiliary disorders: Hepatitis, jaundice.
Immune system disorders: Hypersensitivity reactions.
Metabolism and nutrition disorders: Hyperglycaemia.
Musculoskeletal and connective tissue disorders: Myalgia, arthralgia. muscle cramps.
Nervous system disorders: Headache, paraesthesia, dizziness, peripheral neuropathy.
Psychiatric disorders: Insomnia, depression.
Respiratory, thoracic and mediastinal disorders: Upper respiratory infection, bronchitis, interstitial lung disease.
Reproductive system and breast disorders: Erectile dysfunction.
Skin and subcutaneous tissue disorders: Rash, pruritus, alopecia.
Potentially Fatal: Myopathy, rhabdomyolysis with or without acute renal failure, hepatic failure.
Patient Counseling Information
This drug may cause dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor lipid profile, LFT and creatine kinase. Monitor for signs and symptoms of myopathy and rhabdomyolysis.
Drug Interactions
May increase risk of myopathy and rhabdomyolysis with concurrent use with amiodarone, amlodipine, verapamil, diltiazem, lomitapide, daptomycin, and colchicine. May increase serum concentrations of elbasvir and grazoprevir. May increase prothrombin time with coumarin anticoagulants.
Potentially Fatal: Increased risk of myopathy including rhabdomyolysis with potent CYP3A4 inhibitors (e.g. itraconazole, ketoconazole, posaconazole, voriconazole, clarithromycin, erythromycin, telithromycin, nefazodone, HIV protease inhibitors, nelfinavir, boceprevir, telaprevir, cobicistat containing products), gemfibrozil, ciclosporin, danazol and fusidic acid.
Food Interaction
Increased plasma concentrations resulting to increased risk of myopathy and rhabdomyolysis with grapefruit juice. May enhance hepatic side hepatic effects with alcohol.
Action
Description: Simvastatin, a competitive inhibitor of 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase, the enzyme that catalyses the conversion of HMG-CoA to produce mevalonate, an early and rate-limiting step in cholesterol biosynthesis, resulting to reduced total cholesterol, LDL-cholesterol and triglycerides, and increases HDL-cholesterol levels.
Onset: >3 days.
Pharmacokinetics:
Absorption: Well absorbed from the gastrointestinal tract (85%). Bioavailability: <5%. Time to peak plasma concentration: 1.3-2.4 hours.
Distribution: Plasma protein binding: Approx 95%.
Metabolism: Metabolised in the liver by CYP3A4 to active β-hydroxyacid (active metabolite). Undergoes extensive first-pass metabolism.
Excretion: Mainly via faeces (60% as metabolites); urine (13%, inactive form). Elimination half-life: 1.9 hour (active metabolite).
Chemical Structure
Storage
Tablet: Store below 30°C. Suspension: Store between 20-25°C. Protect from heat.
ATC Classification
C10AA01 - simvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
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