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These highlights do not include all the information needed to use ATORVASTATIN CALCIUM
TABLETS safely and effectively. See full prescribing information for ATORVASTATIN CALCIUM TABLETS. ATORVASTATIN CALCIUM tablets, for oral use Initial U.S. Approval: 1996 · NuCare Pharmaceuticals,Inc.
Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Drug therapy is recommended as an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other nonpharmacologic measures alone has been inadequate. In patients with CHD or multiple risk factors for CHD, atorvastatin calcium tablets can be started simultaneously with diet.
Atorvastatin calcium tablets, USP are white to off-white color, film-coated oval shaped, and are available in four strengths (see Table 1).
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Tablet Strength
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Identifying Features
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| 10 mg of atorvastatin
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Plain on one side and debossed with '11' on other side
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| 20 mg of atorvastatin
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Plain on one side and debossed with '114' on other side
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| 40 mg of atorvastatin
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Plain on one side and debossed with '115' on other side
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| 80 mg of atorvastatin
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Plain on one side and debossed with '116' on other side
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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.
Advise the patient to read the FDA-approved patient labeling (Patient Information).
Patients taking atorvastatin calcium tablets should be advised that cholesterol is a chronic condition and they should adhere to their medication along with their National Cholesterol Education Program (NCEP)-recommended diet, a regular exercise program as appropriate, and periodic testing of a fasting lipid panel to determine goal attainment.
Patients should be advised about substances they should not take concomitantly with atorvastatin [see Warnings and Precautions ( 5.1)] . Patients should also be advised to inform other healthcare professionals prescribing a new medication that they are taking atorvastatin calcium tablets.
Atorvastatin is a synthetic lipid-lowering agent. Atorvastatin is an inhibitor of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. This enzyme catalyzes the conversion of HMG-CoA to mevalonate, an early and rate-limiting step in cholesterol biosynthesis.
Atorvastatin calcium, USP is [R-(R*, R*)]-2-(4-fluorophenyl)-ß,δ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, calcium salt (2:1) trihydrate. The molecular formula of atorvastatin calcium is (C 33H 34FN 2O 5) 2Ca•3H 2O and its molecular weight is 1209.42. Its structural formula is:
[image: MM1]Atorvastatin calcium USP is a white to off-white crystalline powder that is insoluble in aqueous solutions of pH 4 and below. Atorvastatin calcium is very slightly soluble in distilled water, pH 7.4 phosphate buffer, and acetonitrile; slightly soluble in ethanol; and freely soluble in methanol.
Atorvastatin calcium tablets, USP for oral administration contain 10 mg, 20 mg, 40 mg, or 80 mg atorvastatin and the following inactive ingredients: calcium carbonate, croscarmellose sodium, hydroxypropyl cellulose, lactose monohydrate, magnesium stearate, microcrystalline cellulose, Opadry White YS-1-7040 (hypromellose, polyethylene glycol, talc, titanium dioxide) and polysorbate 80.
Atorvastatin Calcium Tablets, USP meets the requirements of USP dissolution Test 5.
[image: img_0a9d64bf-c454-9bcf-e063-6394a90ac790]
Atorvastatin calcium tablets, USP are available containing atorvastatin calcium, USP equivalent to 10 mg, 20 mg, 40 mg or 80 mg of atorvastatin.
The 10 mg tablets are white to off-white, film-coated, oval shaped tablet plain on one side and debossed with '11' on other side. They are available as follows:
Bottles of 90 tablets with child-resistant closure, NDC 68071-3546-9
Storage
Store at 20° to 25°C (68° to 77°F) [see USP Controlled Room Temperature].
What it looks like
Photos of the product and/or packaging supplied by the manufacturer.
Package codes (NDC)
- 68071-3546-9
Full prescribing information (for healthcare professionals)
12 CLINICAL PHARMACOLOGY
13 NONCLINICAL TOXICOLOGY
13.1 Carcinogenesis, Mutagenesis, Impairment of Fertility
In a 2-year carcinogenicity study in rats at dose levels of 10, 30, and 100 mg/kg/day, two rare tumors were found in muscle in high-dose females: in one, there was a rhabdomyosarcoma and, in another, there was a fibrosarcoma. This dose represents a plasma AUC (0 to 24) value of approximately 16 times the mean human plasma drug exposure after an 80 mg oral dose.
A 2-year carcinogenicity study in mice given 100, 200, or 400 mg/kg/day resulted in a significant increase in liver adenomas in high-dose males and liver carcinomas in high-dose females. These findings occurred at plasma AUC (0 to 24) values of approximately 6 times the mean human plasma drug exposure after an 80 mg oral dose.
In vitro, atorvastatin was not mutagenic or clastogenic in the following tests with and without metabolic activation: the Ames test with Salmonella typhimuriumand Escherichia coli, the HGPRT forward mutation assay in Chinese hamster lung cells, and the chromosomal aberration assay in Chinese hamster lung cells. Atorvastatin was negative in the in vivomouse micronucleus test.
In female rats, atorvastatin at doses up to 225 mg/kg (56 times the human exposure) did not cause adverse effects on fertility. Studies in male rats performed at doses up to 175 mg/kg (15 times the human exposure) produced no changes in fertility. There was aplasia and aspermia in the epididymis of 2 of 10 rats treated with 100 mg/kg/day of atorvastatin for 3 months (16 times the human AUC at the 80 mg dose); testis weights were significantly lower at 30 and 100 mg/kg and epididymal weight was lower at 100 mg/kg. Male rats given 100 mg/kg/day for 11 weeks prior to mating had decreased sperm motility, spermatid head concentration, and increased abnormal sperm. Atorvastatin caused no adverse effects on semen parameters, or reproductive organ histopathology in dogs given doses of 10, 40, or 120 mg/kg for two years.