Category : ANTIHYPERLIPIDEMIC

Name : ATORVASTATINE     Type & Dosage : F.C.Tab. ; 10 mg Package : 30

Pharmacologic Category Antihyperlipidemic ; HMG – Co A reductase inhibitor. Mechanism Of Action Atorvastatin as a HMG – Co A reductase inhibitor competitively inhibits the enzyme that catalyzes the conversion of HMG – Co A to mevalonate , the rate – limiting step in cholesterol biosynthesis . Atorvastatin lowers plasma cholesterol and lipoprotein concentrations by inhibiting HMG – Co A reductase and cholesterol synthesis in the liver and by increasing the number of hepatic LDL receptors on the cell surface to enhance uptake and catabolism of LDL . Atorvastatin also reduces LDL production and the number of LDL particles . Atorvastatin reduces total – C , LDL – C , and apo B in patients with homozygous and heterozygous familial hypercholesterolemia , nonfamilial forms of hypercholesterolemia , and mixed dyslipidemia . Atorvastatin also reduces VLDL – C and triglyceride and produces variable increases in HDL – C and apolipoprotein A – 1 . Indications Hyperlipidemia ( treatment ) – Atorvastatin is indicated as an adjunct to diet to reduce total – C , LDL – C , apolipoprotein B and triglyceride concentrations in patients with primary hypercholesterolemia ( heterozygous familial and nonfamilial ) and mixed dyslipidemia ( types IIa and IIb hyperlipoproteinemia ) . It is indicated as an adjunct to diet in the treatment of heterozygous familial hypercholesterolemia in boys and postmenarchal girls from 10 to 17 years of age if after an adequate trial of diet therapy the following findings are present : - LDL – C remains greater than or equal to 190 mg / dl or - LDL – C remains greater than or equal to 160 mg / dl and : there is a positive family history of premature cardiovascular disease or two or more other CVD risk factors are present in the pediatric patient. Atorvastatin is also indicated to reduce total – C and LDL – C in patients with homozygous familial hypercholesterolemia as an adjunct to other lipid – lowering treatments . Atorvastatin is indicated for the treatment of patients with primary dysbetalipoproteinemia ( type III hyperlipoproteinemia ) who do not respond adequately to diet . Atorvastatin is indicated as an adjunct to diet for the treatment of patients with elevated serum triglyceride levels ( type IV hyperlipoproteinemia ). Side Adverse Effects a– Those indicating need for medical attention: Allergic reaction ; Liver function abnormalities ( persistent elevation of liver function tests ) ; Muscle disorders , such as leg cramps , uncomplicated myalgia , myopathy and / or rhabdomyolysis and myositis ; Anaphylaxis ; Angioneurotic edema ; Bullous rashes ; Erythema multiforme ; Stevens – Johnson syndrome ; Toxic epidermal necrolysis. b- < Those indicating need for medical attention only if they continue or bothersome: Headache ; Abdominal pain ; Asthenia ; Back pain ; Constipation ; Diarrhea ; Dyspepsia ; Flatulence ; Flu syndrome ; Urinary tract infection ; Sinusitis ; Pharyngitis ; Bronchitis ; rhinitis. Contraindications Hypersensitivity to atorvastatin or any component of the formulation ; Acute liver disease ; Unexplained persistent elevation of serum transaminases ; Pregnancy ; Breast – feeding . Warnings Precautions Secondary causes of hyperlipidemia should be ruled out prior to therapy . Temporarily discontinue in any patient experiencing an acute or serious condition predisposing to renal failure secondary to rhabdomyolysis such as severe electrolyte , endocrine , or metabolic disorders , hypotension , severe acute infection , myopathy , uncontrolled seizures , major surgery and trauma . Use with caution in patients who consume large amounts of ethanol or have a history of liver disease. Pregnancy FDA Pregnancy Category X . Atorvastatin is contraindicated during pregnancy. Breast Feeding While it is not known whether atorvastatin is distributed into breast milk , atorvastatin is contraindicated in women who are breast – feeding because inhibition of cholesterol synthesis may cause serious adverse effects in the nursing infant. Drug Interactions Plasma concentration may be decreased when atorvastatin was administered concurrently with an aluminum and magnesium hydroxide – containing antacids . Azole antifungals , cyclosporine , erythromycin , clofibrate , fenofibrate and niacin increase the risk of myopathy and rhabdomyolysis . Caution should be exercise if atorvastatin is administered concomitantly with cimetidine , ketoconazole and spironolactone that may decrease the levels or activity of endogenous steroid hormones . Plasma concentrations of digoxin may be increased ; patients taking digoxin and atorvastatin should be followed closely for evidence of digoxin toxicity . Grapefruit juice in large doses should not be taken before or after administration of atorvastatin because it may inhibit metabolism of atorvastatin . Ciprof'loxacin , clarithromycin , diclofenac , doxycycline , isoniazid and verapamil may increase the levels / effects of atorvastatin. Monitoring Parameters Lipid levels after 2 – 4 weeks ; Liver function tests prior to and at 12 weeks following both the initiation of therapy and any elevation in dose , and periodically ( eg , semiannually ) thereafter ; Creatine phosphokinase levels. Dietary Considerations The patients should be placed on a standard cholesterol – lowering diet before receiving atorvastatin and should continue on this diet during treatment with atorvastatin . Atorvastatin may be taken with or without food . Administration And Dosage Usual adult dose: Heterozygous familial and nonfamilial hypercholesterolemia and mixed dyslipidemia – Oral , initially 10 mg once a day . The dosage range is 10 to 80 mg once a day , to be administered at any time of the day , with or without food . Homozygous familial hypercholesterolemia – Oral , 10 to 80 mg a day. Usual adult prescribing limits: 80 mg a day. Usual pediatric dose: Heterozygous familial hypercholesterolemia – Oral , 10 mg per day in boys and postmenarchal girls 10 to 17 years of age . Atorvastatin has not been studied in prepubertal patients or patients younger than 10 years of age. Usual pediatric prescribing limits: Doses greater than 20 mg per day have not been studied in this patient population How Supplied Tablet: 10 mg , 20 mg , 40 mg Storage Store at controlled room temperature between 20 and 25°C ( 68 and 77°F ). References USP DI, 2005 Up To Date, Vol. 13.3 (2005) Martindale, The Complete Drug Reference, 34 rd edition 2005