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Indications
for use:
1. as an adjunct to diet
to reduce elevated total cholesterol and triglyceride levels and to increase
HDL (high density lipoproteins) in patients with primary hypercholesterolemia
and mixed dyslipidemia.
2. as an adjunct to diet
for the treatment of elevated serum triglyceride levels.
Pharmacodynamics:The
liver is the primary site of action and the principal site of cholesterol
synthesis and LDL (low density lipoproteins) clearance.
Pharmacokinetics:Absorption:
peak concentration occurs in within 1 to 2 hours. Distribution:
98% is bound to plasma proteins.
Metabolism: extensively
metabolized to various beta-oxidation products. Excretion: elimination
primarily in bile following hepatic/extrahepatic metabolism.
Adverse Reactions:Digestive
System: constipation, diarrhea, dyspepsia, flatulence.
Metabolic
and Nutritional Disorders: peripheral edema, hyperglycemia, creatine
phosphokinase increase, weight gain, hypoglycemia.
Contraindications:1.
Active liver disease or unexplained elevations of 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 thereafter.
2. The risk of myopathy
during treatment with drugs of this class is increased with concurrent
administration of cyclosporine, fibric acid derivatives, niacin (nicotinic
acid), and erythromycin.
3. Grapefruit juice should
be avoided due to its oxidative metabolism of orally administered medications
by cytochrome P450 3A4 isoenzymes in the intestinal wall, leading to a
reduction in the amount of metabolism of affected drugs, and an increase
in the amount of drug in the bloodstream.
Herb-Drug Interactions:
Some herbs such as Alfalfa, Black Cohosh, Fenugreek, Garlic and Red Yeast
may affect lipid- lowering drugs by increasing the effect of the drug.
St. John’s Wort, oat bran and pectin may decrease the absorption
of lipid-lowering medications such as Lipitor.
Sources
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Bartlett JG, Gallant JE.
2000-2001 Medical Management of HIV Infection. Johns Hopkins University
School of Medicine: Baltimore, MD; 2000.
-
Package Insert. Parke-Davis
Lipitor (Atorvastatin Calcium) tablets. Revised March 2000.
-
Pronsky ZM. Powers and Moore’s
Food Medication Interactions. 11th Edition. Food-Medication Interactions:
Birchrunville, PA; 2000.
-
Herr SM. Herb-Drug Interaction
Handbook. Church Street Books: Nassau, NY;2000.
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