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Full Prescribing Info
Atorvastatin calcium.
Each film-coated tablet contains atorvastatin 10 mg or 20 mg (as atorvastatin calcium).
Pharmacology: Pharmacodynamics: Atorvastatin as well as some of its metabolites are pharmacologically active in humans. The liver is the primary site of action and the principal site of cholesterol synthesis and LDL clearance. Drug dosage rather than systemic drug concentration correlates better with LDL-C reduction. Individualization of drug dosage should be based on therapeutic response.
Pharmacokinetics: Atorvastatin is rapidly absorbed from the gastrointestinal tract. It has low absolute bioavailability of about 12% due to presystemic clearance in the gastrointestinal mucosa and/or first-pass metabolism in the liver, its primary site of action. Atorvastatin is metabolised by the cytochrome P450 isoenzyme CYP3A4 to a number of active metabolites. It is 98% bound to plasma proteins. The mean plasma elimination half-life of atorvastatin is about 14 hours although the half-life of inhibitory activity for HMG-CoA reductase is about 20 to 30 hours due to the contribution of the active metabolites. Atorvastatin is excreted as metabolites, primarily in the bile.
Atorvastatin is used to reduce LDL-cholesterol, apolipoprotein B, and triglycerides, and to increase HDL-cholesterol in the treatment of hyperlipidaemias, including hypercholesterolaemias and combined (mixed) hyperlipidaemia (type IIa or IIb hyperlipoproteinaemias), hypertriglyceridaemia (type IV), and dysbetalipoproteinaemia (type III).
Atorvastatin can also be effective as adjunctive therapy in patients with homozygous familial hypercholesterolaemia who have some LDL-receptor function.
Dosage/Direction for Use
Administration: Atorvastatin is administered orally once daily, at any time of the day, without regard to meals.
The patient should be placed on a standard cholesterol-lowering diet before initiation of atorvastatin therapy and should remain on this diet during treatment with the drug.
The drug should be initiated with a lowest effective dose, thereafter dosage of atorvastatin may be adjusted, if necessary, according to individual requirements and response by increased at intervals of no less than 4 weeks. Patients should be fully advised about adverse reactions, especially myogenic reactions.
Dosage: The usual initial oral dosage of atorvastatin in adults for the management of primary hypercholesterolemia (heterozygous familial or nonfamilial) and mixed dyslipidemia is 10 or 20 mg once daily. Patients requiring reductions in LDL-cholesterol of more than 45% to achieve their goal may be started on an atorvastatin dosage of 40 mg daily. The usual maintenance dosage of atorvastatin in adults is 10 - 80 mg once daily.
The recommended initial dosage of atorvastatin for treatment of heterozygous familial hypercholesterolemia in boys and postmenarchal girls 10 years of age or older is 10 mg once daily. The maximum recommended dosage is 20 mg daily.
The usual oral dosage of atorvastatin for the management of homozygous familial hypercholesterolemia is 10 - 80 mg once daily. The drug may be used as an adjunct to other lipid-lowering therapies (e.g., plasma LDL-apheresis) or when such therapies are not available.
The dosage of atorvastatin should be adjusted at intervals of no less than 4 weeks until the desired effect on lipoprotein concentrations is observed. Reduction of atorvastatin dosage should be considered in patients whose serum cholesterol concentrations fall below the desired target range.
Renal impairment: Because atorvastatin does not undergo substantial renal excretion, dosage modification in patients with renal impairment is not necessary.
There is no specific treatment for atorvastatin overdosage. In the event of an overdose, the patient should be treated symptomatically, and supportive measures instituted as required. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance atorvastatin clearance.
Patients who are hypersensitive to any component of this drug.
Patients with active liver disease or unexplained, persistent increases in serum aminotransferase concentrations.
Safety and efficacy of atorvastatin have not been evaluated in prepubertal children or in children younger than 10 years of age.
Atorvastatin is contraindicated in pregnant women.
Atorvastatin is contraindicated in nursing women.
Special Precautions
It is considered in patients with risk factors resulting in muscle injury during statin therapy. Statin drugs may cause myogenic adverse reactions including myasthenia, myositis especially in patients at risk factors such as patients over 65 years old, patients with uncontrolled hypothyroidism, patients with renal disease. Therapy with the drug under close monitoring is required.
Before instituting therapy with atorvastatin, an attempt should be made to control hypercholesterolemia with appropriate diet, exercise, and weight reduction in obese patients, and to treat other underlying medical problems.
There have been rare postmarketing reports of cognitive impairment (e.g., memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use. These cognitive issues have been reported for all statins. The reports are generally nonserious, and reversible upon statin discontinuation, with variable times to symptom onset (1 day to years) and symptom resolution (median of 3 weeks).
Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors.
Liver dysfunction: Persistent elevations in serum transaminases. It is recommended that liver function tests be performed prior to and at 12 weeks following both the initiation of therapy and any elevation of dose, and periodically (eg, semiannually) thereafter.
Atorvastatin should be used with caution in patients who consume substantial quantities of alcohol and/or have a history of liver disease.
It is recommended that liver function tests should be performed before the initiation of Lipistad and thereafter when clinically indicated.
Skeletal muscle: Uncomplicated myalgia has been reported in atorvastatin-treated patients. Patients should be advised to report promptly unexplained muscle pain, tenderness or weakness, particularly if accompanied by malaise or fever. Atorvastatin therapy should be discontinued if markedly elevated creatine phosphokinase levels occur or myopathy is diagnosed or suspected.
Atorvastatin therapy should be temporarily withheld or discontinued in any patient with an acute, serious condition suggestive of a myopathy or having a risk factor predisposing to the development of renal failure secondary to rhabdomyolysis (eg, severe acute infection, hypotension, major surgery, trauma, severe metabolic, endocrine and electrolyte disorders, and uncontrolled seizures).
Use in Children: Safety and efficacy of atorvastatin have not been evaluated in prepubertal children or in children younger than 10 years of age.
Use In Pregnancy & Lactation
Pregnancy: Atorvastatin may cause fetal harm when administered to pregnant women. Atorvastatin is contraindicated in pregnant women. Atorvastatin should be administered to women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards. If the patient becomes pregnant while taking the drug, therapy should be discontinued and the patient apprised of the potential hazard to the fetus.
Lactation: It is not known whether atorvastatin is distributed into milk in humans. Because of the potential for serious adverse reactions from atorvastatin in nursing infants, the drug is contraindicated in nursing women.
Adverse Reactions
Atorvastatin is generally well-tolerated. Adverse reactions have usually been mild and transient.
10 mg: The most frequent adverse events thought to be related to atorvastatin were constipation, flatulence, dyspepsia, abdominal pain.
Toxic epidermal necrolysis apparently caused by atorvastatin has been reported.
20 mg: The most frequent adverse events thought to be related to atorvastatin were insomnia, headache, nausea, diarrhea, constipation, flatulence, dyspepsia, abdominal pain, myalgia, asthenia.
Drug Interactions
The risk of myopathy during treatment with drugs of this class is increased with concurrent administration of cyclosporine, fibric acid derivatives, niacin (nicotinic acid), erythromycin, azole antifungals.
Co-administration of strong CYP3A4 inhibitors (e.g. ciclosporin, telithromycin, clarithromycin, delavirdine, stiripentol, ketoconazole, voriconazole, itraconazole, posaconazole and HIV protease inhibitors including ritonavir, lopinavir, atazanavir, indinavir, darunavir, etc) should be avoided if possible. In cases where co-administration of these medicinal products with atorvastatin cannot be avoided, lower starting and maximum doses of atorvastatin should be considered and appropriate clinical monitoring of the patient is recommended. In patients taking telaprevir, concomitant use of atorvastatin should be avoided. The dose of atorvastatin should not exceed 40 mg daily when taking with boceprevir and close clinical monitoring is recommended.
Colestipol: Plasma concentrations of atorvastatin decreased approximately 25% when colestipol and atorvastatin were coadministered. However, LDL-C reduction was greater when atorvastatin and colestipol were coadministered than when either drug was given alone.
Digoxin: When multiple doses of atorvastatin and digoxin were coadministered, steady state plasma digoxin concentrations increased by approximately 20%. Patients taking digoxin should be monitored appropriately.
Erythromycin: In healthy individuals, plasma concentrations of atorvastatin increased approximately 40% with coadministration of atorvastatin and erythromycin, a known inhibitor of cytochrome P450 3A4.
Oral contraceptives: Coadministration of atorvastatin and an oral contraceptive increased AUC values for norethindrone and ethinylestradiol by approximately 30% and 20%. These increases should be considered when selecting an oral contraceptive for a woman taking atorvastatin.
10 mg: Antacids: plasma concentrations of atorvastatin decreased. However, LDL-C reduction was not altered.
20 mg: Coadministration of atorvastatin and inhibitors of cytochrome P450 3A4 may increase the risk of myopathy and rhabdomyolysis by increasing atorvastatin concentration in plasma during therapy.
Warfarin: Atorvastatin had no clinically significant effect on prothrombin time when administered to patients receiving chronic warfarin treatment.
Grapefruit juice: Concomitant oral administration of grapefruit juice and atorvastatin should be discouraged since this combination may increase the risk of adverse effects.
Do not store above 30°C.
10 mg: Store in a well-closed container, in a dry place.
20 mg: Store in a dry and cool place.
ATC Classification
C10AA05 - atorvastatin ; Belongs to the class of HMG CoA reductase inhibitors. Used in the treatment of hyperlipidemia.
FC tab 10 mg (white, oval-shaped, biconvex, engraved with "10" on one side and plain on the other side) x 30's. 20 mg (white, oval-shaped, biconvex, engraved with "AT 20" on one side and plain on the other side) x 30's.
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