Description

Pitavastatin Calcium is a potent medication that belongs to the class of drugs known as statins or HMG-CoA reductase inhibitors. It is a synthetic lipid-lowering agent used to lower high cholesterol and triglyceride levels. Pitavastatin is considered a newer-generation statin and is effective at relatively low doses. The “calcium” in its name refers to the salt form used for stability and bioavailability.

Indications

Pitavastatin Calcium is used for a variety of conditions related to high cholesterol and the prevention of cardiovascular disease. Its primary indications include:

• Primary Hypercholesterolemia: It is used to lower high levels of total cholesterol and LDL (“bad”) cholesterol.

• Mixed Dyslipidemia: It is also effective at lowering high levels of triglycerides and is used when a patient has a combination of high cholesterol and high triglycerides.

• Cardiovascular Risk Reduction: It is prescribed to reduce the risk of heart attack, stroke, and the need for revascularization procedures in patients with or without existing heart disease, but who have multiple risk factors.

Mechanism of Action

Pitavastatin’s therapeutic effect is primarily a result of its ability to inhibit a key enzyme in the cholesterol synthesis pathway.

1. Enzyme Inhibition: Pitavastatin works in the liver by competitively inhibiting the enzyme HMG-CoA reductase. This enzyme is the rate-limiting step in the mevalonate pathway, which is the body’s primary way of synthesizing cholesterol.

2. Reduced Cholesterol Production: By blocking this enzyme, pitavastatin significantly reduces the amount of cholesterol the liver produces.

3. Increased LDL Receptor Activity: The liver, in response to the reduced internal cholesterol production, increases the number of LDL receptors on the surface of its cells. These receptors are responsible for binding to and removing LDL cholesterol from the bloodstream.

4. Decreased LDL and Triglycerides: The increased number of LDL receptors leads to a significant reduction in the amount of circulating LDL (“bad”) cholesterol. Pitavastatin also causes a modest increase in HDL (“good”) cholesterol and a decrease in triglycerides.

5. Unique Properties:

• Pitavastatin is metabolized differently from some other statins (like atorvastatin or simvastatin), as it is not significantly metabolized by the CYP450 enzyme system. This reduces the potential for drug-drug interactions with other medications that rely on this system.
• It is effective at very low doses and has a long duration of action, allowing for once-daily dosing.

By reducing the amount of circulating LDL cholesterol, pitavastatin helps to prevent the formation of atherosclerotic plaque, which is the primary cause of heart attacks and strokes.