Xerova 20 mg

Description

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

• Reduction of total cholesterol and LDL cholesterol in patients with heterozygous and homozygous familial hypercholesterolemia.
• Management of mixed dyslipidemia (Fredrickson Type Ia and Ib).
• Treatment of hypertriglyceridemia (Fredrickson Type IV).
• Addressing dysbetalipoproteinemia (Fredrickson Type III).
• Reduction of cardiac ischemic events in patients with asymptomatic or mild to moderate symptomatic coronary artery disease with elevated LDL-cholesterol levels.
• Managing hypercholesterolemia associated with diabetes mellitus or renal transplantation.

Pharmacology: Atorvastatin is a selective HMG-CoA reductase inhibitor that reduces cholesterol production in the liver, thereby lowering plasma cholesterol and lipoprotein levels. It works by increasing hepatic LDL receptor activity, enhancing LDL uptake and catabolism.

• Absorption: Rapid, with peak plasma concentrations in 1-2 hours. The bioavailability of atorvastatin is about 14%, and the systemic availability of its HMG-CoA reductase inhibitory activity is around 30%.
• Distribution: Atorvastatin has a large volume of distribution (381 liters) and binds 98% to plasma proteins.
• Metabolism: Extensive metabolism via cytochrome P450 3A4, producing active metabolites that contribute significantly to its therapeutic effect.
• Excretion: Primarily eliminated in bile, with a half-life of 14 hours for Atorvastatin and 20-30 hours for its inhibitory activity.

Dosage & Administration:

• Primary hypercholesterolemia and combined hyperlipidemia:
  • Adults: Start at 10 mg daily, adjusting up to 80 mg as necessary.
  • Children (10-18 years): Start at 10 mg, with a maximum dose of 20 mg.
• Familial hypercholesterolemia:
  • Adults: Start at 10 mg daily, with increases up to 80 mg as needed.
  • Children (10-18 years): Start at 10 mg, with a maximum of 80 mg.
• Cardiovascular prevention: Start at 10 mg daily, adjusted according to response.
• Adjustments are made based on lipid levels after 2-4 weeks.

Interactions:

• Concurrent use with drugs like cyclosporine, fibric acid derivatives, niacin, erythromycin, and azole antifungals may increase the risk of myopathy.
• Erythromycin increases Atorvastatin concentrations by approximately 40%, and Colestipol decreases them by about 25%.
• Warfarin and oral contraceptives may show interactions in terms of plasma concentrations.

Contraindications:

• Hypersensitivity to Atorvastatin or its components.
• Active liver disease or unexplained persistent transaminase elevations.
• History of severe adverse reactions to other HMG-CoA reductase inhibitors.

Side Effects: Common side effects include constipation, flatulence, dyspepsia, and abdominal pain. Other effects may include headache, infection, rash, back pain, and muscle-related symptoms (myalgia, arthralgia).

Pregnancy & Lactation:

• Pregnancy: Atorvastatin is contraindicated during pregnancy due to risks to the fetus.
• Lactation: Contraindicated in breastfeeding due to potential harm to infants.

Precautions & Warnings:

• Liver function tests should be conducted before treatment and periodically during therapy.
• Caution is advised for patients with heavy alcohol use or a history of liver disease.
• Discontinue use if significantly elevated CPK levels or suspected myopathy occur.

Special Populations:

• Geriatric: Higher plasma concentrations in the elderly, with an enhanced LDL-lowering effect.
• Pediatric: Limited data; maximum dose is 20 mg for children aged 10-17.
• Renal Insufficiency: No dose adjustment needed.
• Hepatic Insufficiency: Increased plasma concentrations observed in patients with liver disease.

Overdose Effects: No specific antidote for overdose. Symptomatic treatment and monitoring of liver function and serum CK levels are recommended. Hemodialysis is unlikely to significantly reduce atorvastatin levels due to its protein binding.

Therapeutic Class: Other Anti-anginal & Anti-ischaemic drugs, Statins

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