ANZITOR 10 mg

Description

Indications:

Anzitor is prescribed as a supplement to diet for lowering elevated levels of total cholesterol, LDL cholesterol, apolipoprotein B (Apo-B), and triglycerides in patients where diet and other non-pharmacological interventions are insufficient.

• Familial Hypercholesterolemia: To reduce total cholesterol and LDL cholesterol in individuals with heterozygous or homozygous familial hypercholesterolemia.
• Mixed Dyslipidemia (Fredrickson Type Ia and Ib): To reduce high cholesterol and triglycerides.
• Hypertriglyceridemia (Fredrickson Type IV): For patients with elevated triglyceride levels.
• Dysbetalipoproteinemia (Fredrickson Type III): To manage this condition effectively.
• Coronary Artery Disease: To decrease the risk of cardiac ischemic events in patients with asymptomatic or mild to moderate coronary artery disease and elevated LDL-cholesterol.
• Hypercholesterolemia in Diabetes or Renal Transplantation: To reduce total and LDL-cholesterol levels in patients with hypercholesterolemia that is either exacerbated or associated with diabetes mellitus or renal transplantation.

Pharmacology:

Atorvastatin is a potent, selective inhibitor of HMG-CoA reductase, the enzyme responsible for converting HMG-CoA to mevalonate, a precursor of cholesterol. By inhibiting this enzyme, Atorvastatin effectively reduces the synthesis of cholesterol in the liver, leading to lower levels of LDL cholesterol in the bloodstream. Additionally, it increases the number of LDL receptors on liver cells, which enhances the uptake and breakdown of LDL cholesterol.

• Absorption: Atorvastatin is quickly absorbed after oral administration. Peak plasma levels occur within 1 to 2 hours after a dose. The extent of absorption increases proportionally with the dose. The absolute bioavailability of the drug is about 14%, while the systemic availability of its HMG-CoA reductase inhibitory effect is approximately 30%.

• Distribution: The drug has a large distribution volume, approximately 381 liters, and is 98% bound to plasma proteins. It is not highly concentrated in red blood cells, and there is evidence suggesting that Atorvastatin may be secreted into human milk based on animal studies.

• Metabolism: Atorvastatin undergoes extensive metabolism in the liver, producing active metabolites that contribute significantly to the drug’s cholesterol-lowering effects. About 70% of the circulating inhibitory activity against HMG-CoA reductase is attributed to these metabolites. The cytochrome P450 3A4 enzyme plays a key role in metabolizing Atorvastatin, which is why the drug’s plasma levels can be increased when taken with inhibitors like erythromycin.

• Excretion: Atorvastatin and its metabolites are predominantly excreted in the bile following liver metabolism. The half-life of the parent drug is about 14 hours, but the duration of inhibitory activity lasts 20-30 hours due to the active metabolites. Only a small fraction (less than 2%) is excreted in the urine.

Dosage & Administration:

• Primary Hypercholesterolemia and Combined Hyperlipidemia:

  • Adults: Starting dose is 10 mg once daily; may be adjusted every 4 weeks up to a maximum of 80 mg daily.
  • Children (10-18 years): Initial dose is 10 mg once daily; may be increased at intervals of at least 4 weeks to a maximum of 20 mg daily.

• Familial Hypercholesterolemia:

  • Adults: Start with 10 mg daily, increasing at 4-week intervals up to 40 mg daily. If needed, the dose can be increased to a maximum of 80 mg daily or 40 mg with anion-exchange resins for heterozygous cases.
  • Children (10-18 years): Start with 10 mg daily, with a possible increase to 80 mg daily after 4 weeks.

• Cardiovascular Risk Reduction:

  • Adults: Initial dose of 10 mg daily, adjusted according to lipid profile and clinical response.

Patients should follow a cholesterol-lowering diet before starting treatment and continue with it during therapy. It’s recommended to adjust the dose based on lipid profile assessments 2-4 weeks after starting treatment.

Interactions:

• Increased Risk of Myopathy: Concurrent use of Atorvastatin with drugs such as cyclosporine, fibric acid derivatives, niacin, erythromycin, and azole antifungals may increase the risk of muscle-related issues.
• Antacids: Decreases plasma levels of Atorvastatin by about 35%, but does not affect its cholesterol-lowering effect.
• Colestipol: Reduces Atorvastatin plasma concentration by 25%, but enhances LDL-C reduction when used together.
• Erythromycin and Cytochrome P450 3A4 Inhibitors: May increase plasma Atorvastatin levels.
• Warfarin: Does not significantly affect prothrombin time.

Contraindications:

Atorvastatin is contraindicated in patients who have a known hypersensitivity to any of its components or have active liver disease or unexplained persistent elevations in serum transaminases. It should also be avoided in patients with a history of serious reactions to other statins.

Side Effects:

Anzitor is generally well tolerated, but some side effects may occur, including:

• Common: Constipation, flatulence, dyspepsia, abdominal discomfort.
• Less frequent: Headache, muscle pain (myalgia), back pain, skin rash, fatigue, and joint pain (arthralgia).

Pregnancy and Lactation:

• Pregnancy: Atorvastatin is contraindicated during pregnancy. It has not been proven safe for use during pregnancy, and animal studies suggest reproductive toxicity. Atorvastatin may also reduce fetal mevalonate, which is essential for cholesterol biosynthesis. Women should discontinue Atorvastatin before conception and during pregnancy.
• Lactation: It is not known if Atorvastatin passes into human milk, but due to potential risks to the infant, breastfeeding should be avoided during treatment.

Precautions & Warnings:

• Liver Function: Liver function tests should be done before starting and periodically during treatment. Discontinue therapy if there is evidence of liver dysfunction or significantly elevated creatine phosphokinase (CPK) levels.
• Alcohol Use: Use with caution in patients who consume large quantities of alcohol or have a history of liver disease.
• Kidney Disease: No dose adjustment is required for patients with renal impairment, but caution should be used.
• Geriatric Population: Elderly individuals may experience higher plasma concentrations, and a stronger response to the drug.

Overdose:

In case of overdose, treatment is symptomatic. Due to its extensive protein binding, Atorvastatin is not expected to be significantly cleared by hemodialysis. Liver function tests and serum CPK levels should be monitored.

Storage Conditions:

Store in a cool, dry place away from direct light and heat. Keep out of reach of children.

Frequently Asked Questions:

1. What is Anzitor 10 mg Tablet? Anzitor 10 mg Tablet is a statin used to lower cholesterol and reduce the risk of heart disease, strokes, and other cardiovascular events.

2. How should I take Anzitor 10 mg Tablet? Take one tablet daily, with or without food. It’s best to take it at the same time each day.

3. What are the common side effects of Anzitor? Common side effects include muscle pain, fatigue, and stomach discomfort. If these symptoms persist, consult your doctor.

4. Can Anzitor be used in children? Yes, Anzitor can be used in children over 10 years old with proper medical supervision.

5. Is Anzitor safe for long-term use? Anzitor is generally considered safe for long-term use, but it should only be taken as prescribed by your healthcare provider.