Xerova 10 mg

Description

Indications Xerova is prescribed as an adjunct to dietary modifications to lower elevated levels of total cholesterol, LDL cholesterol, apolipoprotein B (Apo-B), and triglycerides in the following conditions when diet and other non-pharmacological interventions are insufficient:

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

Take medication as per the advice of a registered physician.

Pharmacology Atorvastatin, the active ingredient in Xerova, is a selective inhibitor of HMG-CoA reductase, an enzyme responsible for converting HMG-CoA into mevalonate, a precursor in cholesterol biosynthesis. By inhibiting this enzyme, Atorvastatin reduces plasma cholesterol and lipoprotein levels while enhancing hepatic LDL receptor activity to increase LDL uptake and breakdown.

• Absorption: Rapid absorption occurs after oral administration, with peak plasma concentrations reached within 1 to 2 hours. The extent of absorption is proportional to the dose. The absolute bioavailability of Atorvastatin is approximately 14%, and systemic availability of its HMG-CoA reductase inhibitory activity is around 30%.
• Distribution: The mean volume of distribution is approximately 381 liters, with about 98% of the drug bound to plasma proteins. Limited penetration into red blood cells has been observed. Studies suggest Atorvastatin may be secreted into human milk.
• Metabolism: Primarily metabolized into ortho- and parahydroxylated derivatives and beta-oxidation products. These metabolites contribute significantly to the inhibition of HMG-CoA reductase. Metabolism primarily involves cytochrome P450 3A4, with potential interactions when coadministered with CYP3A4 inhibitors like erythromycin.
• Excretion: Atorvastatin and its metabolites are primarily excreted in bile. The elimination half-life of Atorvastatin is approximately 14 hours, while its inhibitory activity persists for 20 to 30 hours due to active metabolites. Less than 2% of the oral dose is excreted in urine.

Dosage & Administration

• Primary Hypercholesterolemia & Combined Hyperlipidemia:
  • Adults: 10 mg once daily; can be increased at intervals of at least 4 weeks up to a maximum of 80 mg per day.
  • Children (10-18 years): Initial dose of 10 mg once daily, with a maximum recommended dose of 20 mg daily.
• Familial Hypercholesterolemia:
  • Adults: Initial dose of 10 mg daily, adjustable at intervals of 4 weeks up to 40 mg daily. In cases requiring further reduction, the dose may be increased to a maximum of 80 mg daily or 40 mg combined with an anion-exchange resin.
  • Children (10-18 years): 10 mg once daily, with gradual increases if necessary, up to a maximum of 80 mg daily.
• Prevention of Cardiovascular Events:
  • Adults: Initial dose of 10 mg daily, adjusted based on response.

Patients should adhere to a cholesterol-lowering diet before and during treatment. Lipid levels should be monitored every 2 to 4 weeks for dosage adjustments.

Drug Interactions The risk of muscle-related side effects increases when Atorvastatin is used with:

• Cyclosporine, fibric acid derivatives, niacin, erythromycin, and azole antifungals.
• Antacids: Co-administration may reduce Atorvastatin plasma concentration by 35%, but LDL reduction remains unaffected.
• Colestipol: Plasma concentration of Atorvastatin decreases by approximately 25%, though combined use leads to greater LDL reduction.
• Digoxin: Co-administration may increase digoxin plasma concentration by about 20%.
• Erythromycin: Increases Atorvastatin plasma levels by approximately 40%.
• Oral Contraceptives: Increases AUC values of norethindrone and ethinyl estradiol by 30% and 20%, respectively.
• Warfarin: No significant impact on prothrombin time was observed.

Contraindications

• Hypersensitivity to any component of the medication.
• Active liver disease or unexplained persistent elevation of serum transaminases.
• History of severe adverse reactions to HMG-CoA reductase inhibitors.

Side Effects Xerova is generally well-tolerated. Common side effects include:

• Gastrointestinal issues: Constipation, flatulence, dyspepsia, abdominal pain.
• Other effects: Infection, headache, back pain, rash, asthenia, arthralgia, myalgia.

Pregnancy & Lactation

• Pregnancy: Atorvastatin is contraindicated in pregnancy. It may harm fetal development by reducing mevalonate, a crucial precursor for cholesterol biosynthesis. Women who are pregnant or planning to conceive should not use this medication.
• Lactation: The excretion of Atorvastatin in human milk is unknown, but animal studies suggest it may be present. Due to the potential for serious adverse effects, breastfeeding mothers should not take Atorvastatin.

Precautions & Warnings

• Liver Function: Liver function tests should be conducted before and during therapy. Caution is advised in patients with a history of liver disease or significant alcohol consumption. Treatment should be discontinued if significantly elevated CPK levels or myopathy symptoms develop.

Use in Special Populations

• Elderly: Plasma concentrations may be higher, with an increased LDL-lowering effect.
• Pediatrics: Limited pharmacokinetic data available; recommended only for children over 10 years.
• Renal Insufficiency: No significant effect on drug clearance; no dosage adjustment necessary.
• Hemodialysis: Atorvastatin is extensively bound to plasma proteins and is unlikely to be significantly removed by dialysis.
• Hepatic Insufficiency: Plasma concentrations are significantly increased in individuals with chronic liver disease.

Overdose Management There is no specific treatment for an Atorvastatin overdose. Supportive care should be provided as needed. Liver function tests and serum CK levels should be monitored. Due to extensive protein binding, hemodialysis is unlikely to significantly enhance drug clearance.

Therapeutic Class Statins, Anti-anginal & Anti-ischemic drugs.

Storage Conditions Store in a dry place, protected from light and heat. Keep out of reach of children.