Indications

Anzitor is an adjunct to diet for reducing elevated levels of total cholesterol, LDL cholesterol, apolipoprotein B (Apo-B), and triglycerides. It is used in conditions where diet and other non-pharmacological measures are insufficient. These conditions include:

• Familial hypercholesterolemia (heterozygous and homozygous)
• Mixed dyslipidemia (Fredrickson Type Ia and Ib)
• Hypertriglyceridaemia (Fredrickson Type IV)
• Dysbetalipoproteinaemia (Fredrickson Type III)
• Patients with coronary artery disease and high LDL-cholesterol to reduce cardiac ischemic events.
• Hypercholesterolemia associated with diabetes mellitus or renal transplantation.

Pharmacology

Atorvastatin, the active ingredient in Anzitor, is a selective inhibitor of HMG-CoA reductase, a key enzyme in cholesterol synthesis in the liver. By inhibiting this enzyme, atorvastatin lowers cholesterol and lipoprotein levels in the plasma. It also increases the number of LDL receptors on liver cell surfaces, which enhances the uptake and breakdown of LDL.

Atorvastatin is rapidly absorbed after oral administration, reaching maximum plasma concentrations within 1-2 hours. Its bioavailability is low (around 14%), but its inhibitory activity for HMG-CoA reductase is higher (around 30%). It is extensively metabolized in the liver by the cytochrome P450 3A4 enzyme to active metabolites. The half-life of its inhibitory activity is 20-30 hours, and it is primarily eliminated in the bile.

Dosage & Administration

• Standard Dosing: The recommended starting dose is 10 or 20 mg once daily. For patients needing a large reduction in LDL-C (over 45%), a starting dose of 40 mg once daily may be used. The total daily dose can range from 10 to 80 mg. Doses can be adjusted at intervals of at least four weeks.
• Children (10-18 years) with hypercholesterolemia: The starting dose is 10 mg once daily, with a usual maximum of 20 mg once daily.
• Adults with familial hypercholesterolaemia: Start with 10 mg daily, increasing to 40 mg once daily, and if needed, further to a maximum of 80 mg once daily.
• Anzitor can be taken as a single dose at any time of day, with or without food.

Interaction

• Myopathy Risk: The risk of muscle disease (myopathy) increases when Anzitor is taken with cyclosporine, fibric acid derivatives, niacin, erythromycin, or azole antifungals.
• Antacids: Antacid suspensions can decrease atorvastatin levels, but this does not affect its LDL-C-lowering effect.
• Colestipol: Taking Anzitor with colestipol can decrease atorvastatin levels, but the reduction in LDL-C is greater than with either drug alone.
• Digoxin: Anzitor can increase digoxin plasma concentrations, so patients should be monitored.
• Erythromycin & Oral Contraceptives: Concomitant use with erythromycin or oral contraceptives can increase the plasma concentrations of atorvastatin and the hormones in the contraceptive, respectively.
• Warfarin: Anzitor does not have a clinically significant effect on prothrombin time in patients taking warfarin.

Contraindications

Anzitor is contraindicated in patients with hypersensitivity to any of its components, active liver disease, or unexplained persistent elevations of liver enzymes. It is also contraindicated in patients with a history of serious adverse reactions to other HMG-CoA reductase inhibitors.

Side Effects

Anzitor is generally well-tolerated. The most frequent side effects are constipation, flatulence, indigestion, and abdominal pain. Other reported side effects include infection, headache, back pain, rash, asthenia, and joint or muscle pain.

Pregnancy & Lactation

Anzitor is contraindicated during pregnancy and breastfeeding. It can cause harm to a fetus by reducing the levels of mevalonate, a precursor to cholesterol. Women who are pregnant, trying to become pregnant, or suspect they are pregnant should not take this medication. It is not known if atorvastatin is excreted in human milk, but due to the potential for serious adverse effects, breastfeeding is not recommended.

Precautions & Warnings

• Liver Effects: Liver function tests should be performed before and during treatment. Anzitor should be used with caution in patients with a history of liver disease or those who consume a significant amount of alcohol.
• Myopathy: The therapy should be stopped if there is a suspicion of myopathy or if CPK levels are significantly elevated.

Use in Special Populations

• Geriatric: Plasma concentrations are higher in elderly patients, but this may lead to a greater LDL-lowering effect.
• Renal Insufficiency: No dose adjustment is necessary for patients with kidney dysfunction. Hemodialysis is not expected to clear the drug.
• Hepatic Insufficiency: Plasma concentrations are significantly increased in patients with chronic alcoholic liver disease.

Overdose Effects

In case of an overdose, there is no specific treatment. The patient should be treated symptomatically, with supportive measures. Liver function tests and serum CK levels should be monitored. Hemodialysis is not effective at clearing atorvastatin.

Therapeutic Class

Anzitor is classified as a statin, and also as an anti-anginal and anti-ischemic drug.

Storage Conditions

Keep in a dry place away from light and heat. Keep out of the reach of children.