Liposit

Uses

Therapy with lipid-altering agents should be only one component of multiple risk factor intervention in individuals at significantly increased risk for atherosclerotic vascular disease due to hypercholesterolemia. Drug therapy is used for an adjunct to diet when the response to a diet restricted in saturated fat and cholesterol and other non-pharmacologic measures alone has been inadequate.

Liposit is also used to associated treatment for these conditions: Atherosclerosis, Heterozygous Familial Hypercholesterolemia, Mixed Dyslipidemias, Primary Hypercholesterolemia, Revascularization procedures

How Liposit works

Liposit selectively and competitively inhibits the hepatic enzyme hydroxymethylglutaryl-coenzyme A (HMG-CoA) reductase. HMG-CoA reductase is responsible for converting HMG-CoA to mevalonate, the rate-limiting step in cholesterol biosynthesis. Inhibition results in a decrease in hepatic cholesterol levels which stimulates the synthesis of LDL receptors and increases hepatic uptake of LDL cholesterol. The end result is decreased levels of plasma total and LDL cholesterol.

Dosage

Liposit dosage

Oral-Hyperlipidaemias:

• Adult: Initially, 20-40 mg once daily in the evening, may increase at intervals of 4 wk to max 80 mg/day.
• Child: Heterozygous familial hypercholesterolaemia: 9-16 yr 20 mg once daily. If necessary, may increase dose at 6-wkly intervals to 40 mg bid or 80 mg once daily as modified-release.

May be taken with or without food

Side Effects

Headache, nausea, abdominal pain, dyspepsia, diarrhoea, bronchitis, sinusitis, insomnia, fatigue, myopathy, myalgia and UTI. Increased blood creatinine phosphokinase and transaminase.

Toxicity

Generally well-tolerated. May cause gastrointestinal upset (diarrhea, nausea, constipation, gas, abdominal pain), myotoxicity (mypothy, myositis, rhabdomyolysis), and hepatotoxicity.

Precaution

History of liver disease and hereditary muscular disorders; high alcohol intake; patients who undergone major surgery and under immunosuppressive agents. Manage hypothyroidism prior to treatment. Severe renal impairment.

Interaction

Bleeding and increased prothrombin time with coumarin anticoagulants. May increase the risk of myopathy rhabdomyolysis with HIV protease inhibitors, colchicine, bezafibrate, ciprofibrate or niacin (nicotinic acid), ciclosporin and fluconazole. Reduced bioavailability with concomitant rifampicin.

Food Interaction

• Take with or without food. Should be taken consistently in regards to meals.

Liposit Alcohol interaction

[Moderate]

Concomitant use of statin medication with substantial quantities of alcohol may increase the risk of hepatic injury.

Transient increases in serum transaminases have been reported with statin use and while these increases generally resolve or improve with continued therapy or a brief interruption in therapy, there have been rare postmarketing reports of fatal and non-fatal hepatic failure in patients taking statins.

Patients who consume substantial quantities of alcohol and/or have a history of liver disease may be at increased risk for hepatic injury.

Active liver disease or unexplained transaminase elevations are contraindications to statin use.

Patients should be counseled to avoid substantial quantities of alcohol in combination with statin medications and clinicians should be aware of the increased risk for hepatotoxicity in these patients.

Liposit Drug Interaction

Moderate: ezetimibe, ezetimibeUnknown: aspirin, aspirin, ubiquinone, ubiquinone, duloxetine, duloxetine, omega-3 polyunsaturated fatty acids, omega-3 polyunsaturated fatty acids, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, pyridoxine, pyridoxine, ascorbic acid, ascorbic acid, cholecalciferol, cholecalciferol

Liposit Disease Interaction

Major: liver disease, rhabdomyolysisModerate: cognitive impairment, diabetes, renal disease

Volume of Distribution

• 0.35 L/kg

Elimination Route

Rapidly and almost completely absorbed (> 90%), but undergoes extensive first pass metabolism. Bioavailability is 24% (range 9-50%) when a 10 mg dose is given. The mean relative bioavailability of the extended-release tablet is 29% (range: 9% to 66%) compared to an immediate-release capsule administered under fasting conditions. When given orally, fluvastatin reaches peak concentrations (Tmax) in less than one hour. Taking the extended release tablet with a high-fat meal will delay absorption (Tmax = 6 hours) and increase bioavailability by approximately 50%. However, the maximum concentration of fluvastatin sodium extended-release tablets seen after a high fat meal is less than the peak concentration following a single dose or twice daily dose of the 40 mg fluvastatin capsule.

Half Life

3 hours

Clearance

• 0.8 L/h/kg
• 107 ± 38.1 L/h [Hypercholesterolemia patients receiving a single dose of 20 mg]
• 87.8 ± 45 L/h [Hypercholesterolemia patients receiving 20 mg twice daily]
• 108 ± 44.7 L/h [Hypercholesterolemia patients receiving 40 mg single]
• 64.2 ± 21.1 L/h [Hypercholesterolemia patients receiving 40 mg twice daily]

Elimination Route

When orally administered, fluvastatin is primarily excreted in the faces ( ~90%) as metabolites, with less than 2% present as unchanged drug. Approximately 5% was recovered in the urine.

Pregnancy & Breastfeeding use

Category X: Studies in animals or human beings have demonstrated foetal abnormalities or there is evidence of foetal risk based on human experience or both, and the risk of the use of the drug in pregnant women clearly outweighs any possible benefit. The drug is contraindicated in women who are or may become pregnant.

Contraindication

Acute liver disease or unexplained persistent elevation of serum aminotransferases. Pregnancy and lactation. Avoid admin of two 40 mg conventional cap at one time.

Special Warning

Mild to moderate renal impairment: No dosage adjustment needed.

Acute Overdose

Management: Symptomatic and supportive treatment.

Storage Condition

Store between 15-30° C.

Innovators Monograph

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