Atorvastatin Tablet Description
Atorvastatin tablet is a drug in statin family. It is used to prevent different heart diseases such as stroke, heart attack and other conditions that is caused by high blood cholesterol.
It comes in different strengths which includes 5 mg, 10 mg, 20 mg, 40 mg and 80 mg.
Pharmacology of Atorvastatin Tablet
Atorvastatin tablet is a selective, competitive inhibitor of HMG-COA reductase, the rate-limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A to mevalonate, a precursor of sterols, including cholesterol.
Pharmacologic inhibition of HMG-COA reductase blocks the synthesis of endogenous cholesterol in the liver, causing a compensatory increase in the activity of hepatic LDL receptors leading to enhanced clearance of LDL-cholesterol from the blood.
These two mechanisms lead to reduction in circulating LDL-C and total cholesterol. Atorvastatin is rapidly absorbed after oral administration; maximum plasma concentrations occur with 1 to 2 hours.
Extent of absorption increases in proportion to atorvastatin dose.
The absolute bioavailability of atorvastatin (parent drug) is approx. 14% and the systemic availability of HMG-CoA reductase inhibitory activity is approximately 30%.
The low systemic availability is attributed to presystemic clearance in Gl mucosa and/or hepatic first-pass metabolism.
Although food decreases the rate and extent of drug absorption by approx. 25% and 9%, respectively, as assessed by Cmax and AUC, LDL-C reduction is similar whether atorvastatin is given with or without food.
Plasma atorvastatin concentrations are lower (approx. 30% for Cmax and AUC) following evening drug administration compared with morning.
However, LDL-C reduction is the same regardless of the time of day of drug administration.
Uses of Atorvastatin Tablet
Hypercholesterolaemia – Atorvastatin tablet is used as an adjunct to diet for reduction of elevated total cholesterol, low density lipoprotein cholesterol, apolipoprotein B, and triglycerides in adults with primary hypercholesterolaemia, including familial hypercholesterolaemia or combined (mixed) hyperlipidaemia when response to diet and other nonpharmacological measures is inadequate;
To reduce total cholesterol and low density lipoprotein cholesterol in adults with homozygous familial hypercholesterolaemia as an adjunct to other lipid-lowering treatments; it also raises high density lipoprotein cholesterol and lowers the LDL/HDL and total cholesterol/HDL ratios.
Prevention of CVD in patients estimated to have a high risk for a first cardiovascular event, as an adjunct to correction of other risk factors.
Atorvastatin Tablets Dosage
Atorvastatin tablet is taken by mouth, initially 10 mg once daily. The dose may be increased up to a maximum of 80 mg once daily depending on goal of therapy and patient response
Atorvastatin tablet is to be given as a single dose at any time of the day, with or without food.
Adjustment of dosage should be made at intervals of 4 weeks or more. The patient should be placed on a standard cholesterol-lowering diet before and during treatment.
Acute coronary syndrome (ACS):
Lipid-lowering: 10-40 mg by mouth once daily.
Angina pectoris (Chronic stable angina):
Lipid-lowering: 10-20 mg by mouth once daily.
While on atorvastatin tablet, avoid taking grapefruit juice. Report promptly any unexplained muscle pain, tenderness, or weakness.
Contraindications of Atorvastatin Tablet
Atorvastatin tablet is not to be used in the following conditions noted below:
- Hypersensitivity to any component of this medication.
- Active liver disease or unexplained persistent elevations of serum transaminases exceeding 3 times the upper limit of normal.
Pregnancy and Lactation
Atorvastatin is contraindicated during pregnancy as it is associated with congenital anomalies and defects in fetal development.
Decreased synthesis of cholesterol possibly affects fetal development.
It is also best avoided during lactation due to concern with disruption of lipid metabolism in breastfeeding infants.
Nevertheless, taking the medication does not require any limitation of breastfeeding.
With any statins, patients should promptly report muscle pain, tenderness, or weakness.
Discontinue drug if myopathy is suspected, if creatinine phosphokinase (CPK) levels rise markedly, or if the patient has risk factors for rhabdomyolysis.
Perform liver function tests before the initiation of treatment, at 12 weeks after initiation of therapy or elevation of dose and periodically (e.g., six monthly) thereafter.
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