Pharmacokinetics
Absorption
Bioavailability
Rapidly absorbed following oral administration; undergoes extensive first-pass metabolism in the liver.
Peak plasma concentrations are attained at 1–2 hours.
Absolute bioavailability is 14%.
Evening administration is associated with a decrease in the extent of absorption; however, antilipemic activity remains unchanged.
Onset
A therapeutic response usually is apparent within 2 weeks; maximal response occurs within 4 weeks.
Food
Food decreases rate and extent of absorption but does not alter antilipemic effects.
Distribution
Extent
Distributed mainly to the liver.
Distributes into milk in animals; may distribute into human milk.
Plasma Protein Binding
About 98% (principally albumin).
Elimination
Metabolism
Extensively metabolized in the liver, mainly by CYP3A4, to active metabolites.
Elimination Route
Excreted principally in feces; <2% of a dose excreted in urine.
Half-life
14 hours.
Special Populations
Increased plasma concentrations in patients with hepatic impairment (Child-Pugh class A and B).
Stability
Storage
Oral
Tablets
Atorvastatin: 20–25°C.
Atorvastatin/amlodipine fixed combination: 25° C (may be exposed to 15–30° C).
Actions
- Inhibits HMG-CoA reductase, causing subsequent reduction in hepatic cholesterol synthesis. Reduces serum concentrations of total cholesterol, LDL-cholesterol, VLDL-cholesterol, apo B, and triglycerides.
- Statins may slow progression of and/or induce regression of atherosclerosis in coronary and/or carotid arteries; modulate BP in hypercholesterolemic patients with hypertension; and possess anti-inflammatory activity.
Advice to Patients
- Importance of informing patients about risks, especially rhabdomyolysis, associated with statins alone or combined with other drugs. Importance of patients promptly reporting muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever; brown urine; and flu-like symptoms.
- Importance of adhering to nondrug therapies and measures, including dietary management, weight control, physical activity, and management of potentially contributory disease (e.g., diabetes mellitus).
- Importance of women informing their clinician if they are or plan to become pregnant or plan to breast-feed. Necessity for clinicians to advise women and adolescent girls to avoid pregnancy (i.e., using effective and appropriate contraceptive methods) during therapy and to advise pregnant women of risk to fetus.
- Importance of informing clinician of existing or contemplated concomitant therapy, including prescription and OTC drugs, as well as any concomitant illnesses.
- Importance of informing patients of other important precautionary information. (See Cautions.)
Preparations
Atorvastatin Calcium
| Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|
| Oral | Tablets | 10 mg (of atorvastatin) |
Lipitor® | Pfizer |
| | 20 mg (of atorvastatin) |
Lipitor® | Pfizer |
| | 40 mg (of atorvastatin) |
Lipitor® | Pfizer |
| | 80 mg (of atorvastatin) |
Lipitor® | Pfizer |
Atorvastatin Calcium and Amlodipine Besylate
| Routes | Dosage Forms | Strengths | Brand Names | Manufacturer |
|---|
| Oral | Tablets | 10 mg (of atorvastatin) with Amlodipine 2.5 mg |
Caduet® | Pfizer |
| | 10 mg (of atorvastatin) with Amlodipine 5 mg |
Caduet® | Pfizer |
| | 10 mg (of atorvastatin) with Amlodipine 10 mg |
Caduet® | Pfizer |
| | 20 mg (of atorvastatin) with Amlodipine 2.5 mg |
Caduet® | Pfizer |
| | 20 mg (of atorvastatin) with Amlodipine 5 mg |
Caduet® | Pfizer |
| | 20 mg (of atorvastatin) with Amlodipine 10 mg |
Caduet® | Pfizer |
| | 40 mg (of atorvastatin) with Amlodipine 2.5 mg |
Caduet® | Pfizer |
| | 40 mg (of atorvastatin) with Amlodipine 5 mg |
Caduet® | Pfizer |
| | 40 mg (of atorvastatin) with Amlodipine 10 mg |
Caduet® | Pfizer |
| | 80 mg (of atorvastatin) with Amlodipine 5 mg |
Caduet® | Pfizer |
| | 80 mg (of atorvastatin) with Amlodipine 10 mg |
Caduet® | Pfizer |
Comparative Pricing
This pricing information is subject to change at the sole discretion of DS Pharmacy. For the most current and up-to-date pricing information, please visit drugstore.com.
| Caduet 10-10MG Tablets | PFIZER U.S. | 30/$109.19 or 90/$310.76 |
| Caduet 10-20MG Tablets | PFIZER U.S. | 30/$155.98 or 90/$449.98 |
| Caduet 10-40MG Tablets | PFIZER U.S. | 30/$146.97 or 90/$436.74 |
| Caduet 10-80MG Tablets | PFIZER U.S. | 30/$165.99 or 90/$439.97 |
| Caduet 2.5-10MG Tablets | PFIZER U.S. | 30/$115.99 or 90/$335.97 |
| Caduet 2.5-20MG Tablets | PFIZER U.S. | 30/$157.66 or 90/$451.58 |
| Caduet 2.5-40MG Tablets | PFIZER U.S. | 30/$157.66 or 90/$451.58 |
| Caduet 5-10MG Tablets | PFIZER U.S. | 30/$114.99 or 90/$314.96 |
| Caduet 5-20MG Tablets | PFIZER U.S. | 30/$153.29 or 90/$441 |
| Caduet 5-40MG Tablets | PFIZER U.S. | 30/$149.99 or 90/$445.98 |
| Caduet 5-80MG Tablets | PFIZER U.S. | 30/$155.98 or 90/$445.98 |
| Lipitor 10MG Tablets | PFIZER U.S. | 30/$85.99 or 90/$237.99 |
| Lipitor 20MG Tablets | PFIZER U.S. | 30/$119.99 or 90/$335.97 |
| Lipitor 40MG Tablets | PFIZER U.S. | 30/$119.99 or 90/$335.97 |
| Lipitor 80MG Tablets | PFIZER U.S. | 30/$119.99 or 90/$335.97 |
AHFS Drug Information. © Copyright, 1959-2008, Selected Revisions April 2008. American Society of Health-System Pharmacists, Inc., 7272 Wisconsin Avenue, Bethesda, Maryland 20814.
† Use is not currently included in the labeling approved by the US Food and Drug Administration.
Remember, keep this and all other medicines out of the reach of children,
never share your medicines with others, and use this medication only for the indication prescribed.
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