FloLipid (simvastatin)

FloLipid Oral Suspension is a lipid-lowering agent derived synthetically from Aspergillus terreus. Simvastatin, an inactive lactone, is hydrolyzed to the corresponding β-hydroxyacid form after ingestion.

This inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase, which converts HMG-CoA to mevalonate, an early step in cholesterol biosynthesis.

FloLipid is indicated to:

• Reduce total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and triglycerides (TG) while increasing high-density lipoprotein cholesterol (HDL-C) in patients with primary hyperlipidemia (Fredrickson type IIa, heterozygous familial and nonfamilial) or mixed dyslipidemia (Fredrickson type IIb).
• Reduce elevated TG in patients with hypertriglyceridemia (Fredrickson type IV hyperlipidemia).
• Reduce elevated TG and VLDL-C in patients with primary dysbetalipoproteinemia (Fredrickson type III hyperlipidemia).
• Reduce total-C and LDL-C in patients with homozygous familial hypercholesterolemia (HoFH) as an adjunct to other lipid-lowering treatments or if such treatments are unavailable.

Adolescent Patients With Heterozygous Familial Hypercholesterolemia (HeFH)

FloLipid is indicated as an adjunct to diet to reduce total-C, LDL-C, and Apo B levels in adolescent boys and girls aged 10 to 17 years with HeFH, if after an adequate trial of diet therapy the following findings are present:

1. LDL cholesterol remains ≥190 mg/dL; or
2. LDL cholesterol remains ≥160 mg/dL and there is a positive family history of premature cardiovascular disease (CVD) or two or more other CVD risk factors are present in the adolescent patient.

Limitations Of Use

FloLipid has not been studied in conditions where the major abnormality is elevation of chylomicrons (i.e., hyperlipidemia Fredrickson types I and V).

What are the side effects of FloLipid?

Because clinical studies are conducted under widely varying conditions, adverse reaction rates observed in the clinical studies of a drug cannot be directly compared to rates in the clinical studies of another drug and may not reflect the rates observed in practice.

In the pre-marketing controlled clinical studies and their open extensions (2,423 patients with median duration of follow-up of approximately 18 months), 1.4% of patients were discontinued due to adverse reactions.

The most common adverse reactions that led to treatment discontinuation were gastrointestinal disorders (0.5%), myalgia (0.1%), and arthralgia (0.1%).

The most commonly reported adverse reactions (incidence ≥5%) in simvastatin controlled clinical trials were upper respiratory infections (9.0%), headache (7.4%), abdominal pain (7.3%), constipation (6.6%), and nausea (5.4%).

QUESTION

What is the dosage for FloLipid?

• The usual dosage range is 5 to 40 mg/day.
• FloLipid should be taken in the evening on an empty stomach.
• Shake bottle well for at least 20 seconds before using.
• In patients with CHD or at high risk of CHD, FloLipid can be started simultaneously with diet.
• The recommended usual starting dose is 10 or 20 mg once a day.
• For patients at high risk for a CHD event, the recommended starting dose is 40 mg/day.
• It is recommended to use FloLipid 40 mg/5 mL for dosages ≥40 mg.
• Lipid determinations should be performed after 4 weeks of therapy and periodically thereafter.
• Patients should be advised to measure FloLipid with an accurate measuring device. A household teaspoon is not an accurate measuring device and could lead to overdosage.
• A pharmacist can recommend an appropriate measuring device and provide instructions.

What drugs interact with FloLipid?

Strong CYP3A4 Inhibitors, Cyclosporine, Or Danazol

• Simvastatin is metabolized by CYP3A4 but has no CYP3A4 inhibitory activity; therefore it is not expected to affect the plasma concentrations of other drugs metabolized by CYP3A4.
• Elevated plasma levels of HMG-CoA reductase inhibitory activity increase the risk of myopathy and rhabdomyolysis, particularly with higher doses of simvastatin.
• Concomitant use of drugs labeled as having a strong inhibitory effect on CYP3A4 is contraindicated.
• If treatment with certain drugs is unavoidable, therapy with simvastatin must be suspended during the course of treatment.
• The risk of myopathy is increased by concomitant administration of cyclosporine or danazol. Therefore, concomitant use of these drugs is contraindicated.

Lipid-Lowering Drugs That Can Cause Myopathy When Given Alone

• Gemfibrozil: Contraindicated with simvastatin.
• Other fibrates: Caution should be used when prescribing with simvastatin.

Amiodarone, Dronedarone, Ranolazine, or Calcium Channel Blockers

• The risk of myopathy, including rhabdomyolysis, is increased by concomitant administration of certain drugs.

Niacin

• Cases of myopathy/rhabdomyolysis have been observed with simvastatin coadministered with lipid-modifying doses of niacin-containing products.
• Caution should be used when treating Chinese patients with simvastatin doses exceeding 20 mg/day coadministered with lipid-modifying doses of niacin-containing products.
• Because the risk for myopathy is dose-related, Chinese patients should not receive simvastatin 80 mg coadministered with lipid-modifying doses of niacin-containing products.

Digoxin

• In one study, concomitant administration of digoxin with simvastatin resulted in a slight elevation in digoxin concentrations in plasma.

Coumarin Anticoagulants

• In two clinical studies, simvastatin 20-40 mg/day increased the prothrombin time of coumarin anticoagulants.
• Prothrombin time should be determined before starting simvastatin and frequently enough during early therapy.
• If the dose of simvastatin is changed or discontinued, the same procedure should be repeated.
• Simvastatin therapy has not been associated with bleeding or changes in prothrombin time in patients not taking anticoagulants.

Colchicine

• Cases of myopathy, including rhabdomyolysis, have been reported with simvastatin coadministered with colchicine, and caution should be exercised when prescribing simvastatin with colchicine.

Is FloLipid safe to take when pregnant or breastfeeding?

Summary

FloLipid Oral Suspension is a lipid-lowering agent derived synthetically from Aspergillus terreus. FloLipid is used to reduce elevated total cholesterol (total-C), low-density lipoprotein cholesterol (LDL-C), apolipoprotein B (Apo B), and triglycerides (TG), and to increase high-density lipoprotein cholesterol (HDL-C).