LIPOSTAT

COMPOSITION:

Lipostat 10: 

Each film coated tablet contains:Atorvastatin calcium equivalent to Atorvastatin 10mg

Lipostat 20:  

Each film coated tablet contains: Atorvastatin calcium equivalent to Atorvastatin 20mg 

CLINICAL PHARMACOLOGY:

Mechanism of Action:  

Atorvastatin calcium is a selective, competitive inhibitor of HMG-CoA reductase, the key enzyme in cholesterol synthesis. It lowers plasma cholesterol and lipoprotein levels by inhibiting cholesterol production in the liver and increasing hepatic LDL receptors, which enhance the uptake and breakdown of LDL. Additionally, it reduces LDL production and the number of LDL particles.

Pharmacokinetic:

Absorption: Rapidly absorbed after oral administration, with a bioavailability of approximately 14%. It reaches peak plasma concentrations (Tmax) within 1–2 hours. 

Distribution:It has a high plasma protein binding (~98%) and an elimination half-life of about 14 hours, though its pharmacodynamic effect lasts longer due to active metabolites.

Metabolism:Atorvastatin is extensively metabolized by the liver via CYP3A4 into active metabolites, contributing to its cholesterol-lowering effects.

 Excretion: occurs primarily via bile, with less than 2% excreted in urine, highlighting its hepatic clearance. These properties support once-daily dosing, usually at bedtime.

INDICATIONS AND USAGE: 

Atorvastatin is indicated for the prevention of cardiovascular events in patients with hyperlipidemia, including lowering LDL cholesterol levels. It is also used to reduce the risk of stroke, myocardial infarction, and other heart-related complications. Atorvastatin may be prescribed for patients with dyslipidemia or those at high risk for cardiovascular disease.

DOSAGE AND ADMINISTRATION:

Recommended dosage in adult patients with starting dosage is 10 mg to 20 mg once daily. The dosage range is 10 mg to 80 mg once daily. Patients who require a reduction in LDL-C greater than 45% may be started at 40 mg once daily.

The recommended dosage of atorvastatin for pediatric patients aged 10 and older is 10 mg once daily for heterozygous familial hypercholesterolemia (HeFH) and 10–20 mg once daily for homozygous familial hypercholesterolemia (HoFH), with a range up to 80 mg daily.

WARNINGS AND PRECAUTIONS: 

Myopathy and Rhabdomyolysis: Atorvastatin may cause myopathy and rhabdomyolysis, particularly in high-risk patients; discontinue if CK levels are elevated or muscle issues occur.

Immune-Mediated Necrotizing Myopathy (IMNM): Rare cases of autoimmune myopathy may occur with atorvastatin; discontinue if IMNM is suspected.

Hepatic Dysfunction: Atorvastatin may cause liver enzyme elevations and hepatic failure; discontinue if serious liver injury or jaundice occurs.

ADVERSE REACTIONS:

Most common adverse reactions (incidence ≥ 5%) are nasopharyngitis, arthralgia, diarrhea, pain in extremity, and urinary tract infection

DRUG INTERACTIONS:

Concomitant use of atorvastatin with grapefruit juice, rifampin, oral contraceptives, or digoxin may increase the risk of myopathy, alter plasma levels, and require monitoring

USE IN SPECIFIC POPULATIONS:

Pregnancy: May cause fetal harm.

Nursing Mothers: not recommended during treatment with Atorvastatin Calcium tablets

Pediatric Use: The safety and effectiveness of have not been established in pediatric patients.

Geriatric Use: Advanced age (≥65 years) is a risk factor for -associated myopathy and rhabdomyolysis.

Renal Impairment: Risk factor for myopathy and rhabdomyolysis.

Hepatic Impairment: Contraindicated in patients with acute liver failure or decompensated cirrhosis

CONTRAINDICATIONS: 

Acute liver failure or decompensated cirrhosis 

Hypersensitivity to atorvastatin or any excipient in Atorvastatin Calcium tablets

OVERDOSAGE: 

No specific antidotes for Atorvastatin Calcium tablets are known. Due to extensive drug binding to plasma proteins, hemodialysis is not expected to significantly enhance Atorvastatin Calcium tablets clearance.

STORAGE: 

Store at 20° to 25°C protected from light and moisture.

PRESENTATION: 

Lipostat 10 & 20: Box containing 10 strips of 10 tablets