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Specification
Requires Prescription (YES/NO)
Yes
Generics
Atorvastatin , Ezitimibe
Used For
Cholesterol Control
How it works
Atorvastatin is a selective, competitive inhibitor of HMG-CoA reductase, the rate limiting enzyme responsible for the conversion of 3-hydroxy-3-methyl-glutarylcoenzyme A to mevalonate, a precursor of sterols, including cholesterol. Triglycerides and cholesterol in the liver are incorporated into very low-density lipoproteins (VLDL) and released into the plasma for delivery to peripheral tissues. Low-density lipoprotein (LDL) is formed from VLDL and is catabolized primarily through the receptor with high affinity to LDL (LDL receptor). Atorvastatin reduces total-C, LDL-C and Apo B in both normal volunteers and in patients with homozygous and heterozygous familial hypercholesterolaemia (FH), non-familial forms of hypercholesterolaemia and mixed dyslipidaemia. Atorvastatin also reduces very low density lipoprotein cholesterol (VLDL-C) and triglycerides and produces variable increases in HDL-C and apolipoprotein A-1. Ezetimibe Ezetimibe localizes at the brush border of the small intestine and inhibits the absorption of cholesterol, leading to a decrease in the delivery of intestinal cholesterol to the liver. This causes a reduction of hepatic cholesterol stores and an increase in clearance of cholesterol from the blood.
Usage And Safety
Dosage
Atorvastatin , Ezitimibe
Side Effects
Common: Diarrhoea and myalgia. Uncommon: influenza, depression, insomnia, sleep disorder, dysgeusia, paraesthesia, dizziness, headache, dyspnoea, sinus bradycardia, hot flush, abdominal discomfort, abdominal pain, abdominal pain lower, abdominal pain upper, frequent bowel movements, stomach discomfort, upset stomach, abdominal distension, constipation, dyspepsia, flatulence, gastritis, nausea, acne, urticaria, arthralgia, back pain, muscle fatigue, muscular weakness, pain in extremity, muscle spasms, musculoskeletal stiffness, asthenia, oedema, fatigue, malaise, ALT and/or AST increased, alkaline phosphatase increased, gamma-glutamyltransferase increased, hepatic enzyme increased, liver function test abnormal, weight increased and blood CK increased.
Drug Interactions
Erythromycin/Clarithromycin , Protease Inhibitors , Itraconazole , Cimetidine , Grapefruit Juice , Colestipol , Cholestyramine , Colchicine , Inhibitors of Breast Cancer Resistance Protein (BCRP) , Ciclosporin , Boceprevir, Anticoagulants , Digoxin , Oral contraceptives.
Indication
It is used to treat : Prevention of Cardiovascular Disease , Primary Hypercholesterolaemia , Homozygous Familial Hypercholesterolaemia (HoFH) .
When not to Use
Atorvastatin + Ezetimibe combination is contraindicated: • In patients with hypersensitivity to ezetimibe, atorvastatin or any component of this medication. • In patients with moderate or severe liver dysfunction. • In patients with active liver disease or unexplained persistent elevations of serum transaminases. • During pregnancy and lactation. • In patients with myopathy secondary to other lipid lowering agents. • In combination with fenofibrate, in patients with gall bladder disease. • To adminster concomitantly use with fusidic acid .
Precautions
Precaution
Atorvastatin may affect the skeletal muscle and cause myalgia, myositis and myopathy that may progress to rhabdomyolysis, a potentially life-threatening condition characterised by markedly elevated creatine phosphokinase (CPK) levels (>10 times ULN), myoglobinaemia and myoglobinuria, which may lead to renal failure. Patients must be asked to promptly report muscle pain, cramps or weakness especially if accompanied by malaise or fever. Atorvastatin + Ezetimibe must be discontinued if clinically significant elevation of CPK levels occur or if rhabdomyolysis is diagnosed or suspected .
Warnings
Warning 1
Exceptional cases of interstitial lung disease have been reported with some statins, especially with long term therapy. If it is suspected that a patient has developed interstitial lung disease, statin therapy should be discontinued.
Warning 2
Some evidence suggests that statins as a class raise blood glucose and in some patients, at high risk of future diabetes, may produce a level of hyperglycaemia where formal diabetes care is appropriate. Patients at risk (fasting glucose 5.6 to 6.9 mmol/L, BMI>30kg/m2 , raised triglycerides, hypertension) should be monitored both clinically and biochemically according to national guidelines.
Warning 3
This formulation contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose malabsorption should not take this medicine.
Additional Information
Pregnancy category
Always consult your physician before using any medicine.
Storage (YES/NO)
Store this medicine at room temperature, away from direct light and heat.
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