Lescol XL fluvastatin sodium 80 mg Tablet, Extended Release, 30-count
🆔 Identity & classification
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🏷️ RxNorm drug class
This medicine belongs to the HMG-CoA Reductase Inhibitor class.
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🏭 Manufacturer & labeler
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🩺 Clinical
Fluvastatin is used to decrease the amount of cholesterol (a fat-like substance that can build up in blood vessels leading to heart attack or strokes or other medical conditions) reduce the risk of needing procedures to restore blood flow to the heart in patients with congenital heart disease (CHD; a structural problem with the heart) Fluvastatin is in a class of medications called HMG-CoA reductase inhibitors (statins). It works by slowing how much cholesterol your body makes.This lowers the amount of cholesterol that can build up on the walls of the arteries and block blood flow to the...
Read the full MedlinePlus article ↗- Fluvastatin works by blocking the main enzyme your liver uses to make cholesterol. That causes your liver to pull more LDL — the 'bad' cholesterol — out of your bloodstream. Over t...
- What exactly is fluvastatin supposed to do for me?
- For the capsule form, you can take it with or without food — just don't open the capsule. For the extended-release tablet (including Lescol XL), you can take it with or without foo...
- Does it matter what time of day I take it, or whether I take it with food?
Patient education
Supplement & herbal interactions
Fluvastatin may be associated with lower levels of 1 nutrient — worth a chat with your pharmacist, not a cause for alarm.
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Ask a licensed pharmacist directly — free, answered by our team.
💊 What it looks like
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🧪 Inactive Ingredients / Excipients
Inactive ingredients, also called excipients, are components of the drug product other than the active ingredient. They may include fillers, dyes, coatings, preservatives, flavors, or other formulation ingredients.
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UNII EX438O2MRT
Ferric oxide yellow is a naturally occurring iron compound used as a colorant in medications. It gives tablets, capsules, and other forms a yellow or golden hue for identification and appearance.
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UNII RFW2ET671P
Hydroxypropyl cellulose is a plant-derived thickening agent made from cellulose. It acts as a binder to hold tablet ingredients together and as a film-former to coat tablets or control how fast the medicine releases.
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Hypromellose 2208 is a plant-derived thickening agent used as a binder and film-coating material in tablets and capsules. It helps hold ingredients together and creates a protective coating that controls how quickly the medicine dissolves.
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UNII 70097M6I30
Magnesium stearate is a salt made from magnesium and stearic acid, a fatty substance. It's used in tablets and capsules as a lubricant and glidant to help ingredients flow smoothly during manufacturing and prevent sticking.
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Microcrystalline cellulose is a purified form of cellulose, a natural fiber from plant sources. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and give the medicine its shape and size.
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Polyethylene glycol 8000 is a synthetic polymer made from ethylene oxide. It acts as a binder and filler in tablets and capsules, helping hold ingredients together and add bulk to the medicine.
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UNII HM5Z15LEBN
Potassium bicarbonate is a salt that acts as a buffer and pH regulator in medicines. It helps maintain a stable acid-alkaline balance so the drug stays effective and doesn't irritate the stomach or mouth.
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UNII FZ989GH94E
Povidone is a synthetic polymer made from a plastic-like material. It acts as a binder to hold tablet ingredients together and as a disintegrant to help the tablet break apart in your stomach so the medicine can be absorbed.
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UNII 15FIX9V2JP
Titanium dioxide is a bright white mineral powder commonly used as a colorant and opacifying agent. It makes pills and tablets white or lighter in color and helps make coatings non-transparent.
9 inactive ingredients listed in the exact product block matched to this NDC.
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ingredient classCode="IACT" elements from the exact product block matched by this NDC. Label-section narrative from DailyMed / the openFDA label index is shown separately when available.Inactive ingredient FAQ
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💲 Pricing
A drug doesn't have one price. Each row is a different public payment system, and none is what you'd pay at the counter — that depends on your insurance. The ⓘ on each row explains what it measures.
| Price system | Per ea | Per package |
|---|---|---|
| Retail pharmacies payNADAC · weekly | $13.064 | $391.93 / 30 tablets |
| Medicaid paysCMS SDUD · 12 mo | No recent Medicaid claims on file for this NDC — rare and low-volume NDCs are suppressed in the public data. | |
| Medicare drug plans payPart D · quarterly | No Part D plan price is available for this NDC in our data. | |
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🔁 Therapeutic equivalents
| Product | Labeler | Pack | NADAC/unit | TE | Status | Price vs. this |
|---|---|---|---|---|---|---|
| Fluvastatin Sodium 80 mg 00093-7446-01 | Teva | 100 tablets | $2.879 | AB | Availability likely | save 78% |
| Fluvastatin Sodium 80 mg 00527-2580-32 | Lannett | 30 tablets | $2.879 | AB | Availability likely | save 78% |
| Fluvastatin Sodium Er 80 mg 00781-8017-01 | Sandoz | 100 tablets | $2.879 | AB | Availability likely | save 78% |
| Lescol XL 80 mgthis 66758-0211-31 | Sandoz | 30 tablets | $13.064 | AB | Availability likely | — |
Where does this data come from?
⏳ Availability & generic status
FDA-approved generic versions are listed, and recent pricing/market data suggests they may be available — see Therapeutic equivalents.
Where does this data come from?
📊 Medicare Part D spend CMS · PART D · 2026 (Q1)
📦 Packaging — all sizes for this product
| Package NDC | Description | Marketing start | Status |
|---|---|---|---|
| 66758-0211-31 You're viewing this | 30 TABLET, EXTENDED RELEASE in 1 BOTTLE (66758-211-31) | 2024-08-02 | Active |
📄 Full prescribing information FDA SPL
🎯 Indications and Usage ▾
1 INDICATIONS AND USAGE LESCOL XL is indicated: • To reduce the risk of undergoing coronary revascularization procedures and slow the progression of coronary atherosclerosis in adults with clinically evident coronary heart disease. • As an adjunct to diet to reduce low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia. • As an adjunct to diet to reduce LDL-C in adults and pediatric patients 10 years of age and older with heterozygous familial hypercholesterolemia (HeFH) who require 80 mg of fluvastatin daily.
LESCOL XL is indicated ( 1 ): • To reduce the risk of undergoing coronary revascularization procedures and slow the progression of coronary atherosclerosis in adults with clinically evident coronary heart disease. • As an adjunct to diet to reduce low-density lipoprotein cholesterol (LDL-C) in adults with primary hyperlipidemia. • As an adjunct to diet to reduce LDL-C in adults and pediatric patients 10 years of age and older with heterozygous familial hypercholesterolemia (HeFH) who require 80 mg
⏱️ Dosage and Administration ▾
2 DOSAGE AND ADMINISTRATION • LESCOL XL can be taken with or without food and may be taken at any time of the day. ( 2.1 ) • Do not break, crush or chew LESCOL XL tablets prior to administration. ( 2.1 ) • Adults : The recommended starting dose is 80 mg (administered as one 80 mg LESCOL XL once daily).
( 2.2 ) Children : The recommended dose is 80 mg once daily in pediatric patients 10 years of age and older who require 80 mg of fluvastatin. LESCOL XL is not recommended for dosage initiation in pediatric patients because the recommended starting dosage cannot be achieved with the available strength of 80 mg. ( 2.3 )
2.1Important Dosage Information • Take LESCOL XL tablets orally once daily as a single dose, with or without food. • Do not break, crush, or chew LESCOL XL tablets. • LESCOL XL is only available as an 80 mg tablet. LESCOL XL cannot be titrated [see Dosage and Administration (2.2, 2.3)] . • For patients that require a high-intensity statin or are unable to achieve their LDL-C goal receiving LESCOL XL 80 mg daily, prescribe alternative LDL-C-lowering treatment. • Assess LDL-C when clinically appropriate, as early as 4 weeks after initiating LESCOL XL.
2.2Recommended Dosage in Adult Patients The recommended dosage for LESCOL XL is 80 mg once daily.
2.3Recommended Dosage in Pediatric Patients Aged 10 Years of Age and Older with HeFH LESCOL XL is not recommended for dosage initiation in pediatric patients because the recommended starting dosage cannot be achieved with the available strength of 80 mg. Recommend use of another fluvastatin product to initiate dosing in pediatric patients. The recommended dosage of LESCOL XL is 80 mg once daily in pediatric patients 10 years of age and older who require 80 mg of fluvastatin.
💊 Dosage Forms and Strengths ▾
3 DOSAGE FORMS AND STRENGTHS Extended-release tablets: 80 mg of fluvastatin: yellow, round, slightly biconvex film-coated tablets with beveled edges debossed with “LESCOL XL” on one side and “80” on the other. Extended-release tablets: 80 mg of fluvastatin ( 3 )
⛔ Contraindications ▾
4 CONTRAINDICATIONS LESCOL XL is contraindicated in patients with: • Acute liver failure or decompensated cirrhosis [see Warnings and Precautions (5.3)] . • Hypersensitivity to fluvastatin or any of the excipients in LESCOL XL. Hypersensitivity reactions, including anaphylaxis, angioedema, and Stevens-Johnson syndrome have been reported [see Adverse Reactions (6.2)] . • Acute liver failure or decompensated cirrhosis ( 4 ) • Hypersensitivity to fluvastatin or any excipient in LESCOL XL ( 4 )
⚠️ Warnings and Cautions ▾
5 WARNINGS AND PRECAUTIONS • Myopathy and Rhabdomyolysis : Risk factors include age 65 years or greater, uncontrolled hypothyroidism, renal impairment, and concomitant use with certain other drugs. Discontinue LESCOL XL if markedly elevated creatine kinase (CK) levels occur, or myopathy is diagnosed or suspected. Temporarily discontinue LESCOL XL in patients experiencing an acute or serious condition at high risk of developing renal failure secondary to rhabdomyolysis.
Inform patients of the risk of myopathy and rhabdomyolysis when starting or increasing LESCOL XL dosage. Instruct patients to promptly report unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever. ( 5.1 ) • Immune-Mediated Necrotizing Myopathy (IMNM) : Rare reports of IMNM, an autoimmune myopathy, have been reported with statin use.
Discontinue LESCOL XL if IMNM is suspected.( 5.2 ) • Hepatic Dysfunction : Increases in serum transaminases have occurred, some persistent. Rare reports of fatal and non-fatal hepatic failure have occurred. Consider testing liver enzyme before initiating therapy and as clinically indicated thereafter.
If serious hepatic injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs, promptly discontinue LESCOL XL ( 5.3 )
5.1Myopathy and Rhabdomyolysis LESCOL XL may cause myopathy (muscle pain, tenderness, or weakness associated with elevated creatine kinase [CK]) and rhabdomyolysis. Acute kidney injury secondary to myoglobinuria and rare fatalities have occurred as a result of rhabdomyolysis with statins, including LESCOL XL. Myopathy, defined as muscle aching or muscle weakness in conjunction with increases in CK, values to greater than 10 times the upper limit of normal (ULN) was < 0.1% in fluvastatin clinical trials [see Adverse Reactions (6.1)] .
Risk Factors for Myopathy Risk factors for myopathy include age 65 years or greater, uncontrolled hypothyroidism, renal impairment, and concomitant use with certain other drugs (including other lipid-lowering therapies) [see Drug Interactions (7.1)] . Steps to Prevent or Reduce the Risk of Myopathy and Rhabdomyolysis Avoid concomitant use of LESCOL XL with gemfibrozil, cyclosporin, and fluconazole. When used concomitantly with LESCOL XL, lipid modifying doses (≥ 1 g/day) of niacin, fibrates, and colchicine may also increase the risk of myopathy and rhabdomyolysis [see Drug Interactions (7.1)] .
Discontinue LESCOL XL if markedly elevated CK levels occur or if myopathy is either diagnosed or suspected. Muscle symptoms and CK increases may resolve if LESCOL XL is discontinued. Temporarily discontinue LESCOL XL in patients experiencing an acute or serious condition at high risk of developing renal failure secondary to rhabdomyolysis, e.g., sepsis, shock, severe hypovolemia, major surgery, trauma, severe metabolic, endocrine, or electrolyte disorders, or uncontrolled epilepsy.
Inform patients of the risk of myopathy and rhabdomyolysis when starting LESCOL XL. Instruct patients to promptly report any unexplained muscle pain, tenderness, or weakness, particularly if accompanied by malaise or fever.
5.2Immune-Mediated Necrotizing Myopathy There have been rare reports of immune-mediated necrotizing myopathy (IMNM), an autoimmune myopathy, associated with statin use, including reports of recurrence when the same or a different statin was administered. IMNM is characterized by proximal muscle weakness and elevated serum CK, which persist despite discontinuation of statin treatment; positive anti-HMG CoA reductase antibody, muscle biopsy showing necrotizing myopathy, and improvement with immunosuppressive agents. Additional neuromuscular and serologic testing may be necessary.
Treatment with immunosuppressive agents may be required. Discontinue LESCOL XL if IMNM is suspected.
5.3Hepatic Dysfunction Increases in serum transaminases have been reported with use of LESCOL XL [see Adverse Reactions (6.1)] . In most cases, these changes appeared s…
🤒 Adverse Reactions ▾
6 ADVERSE REACTIONS The following serious adverse reactions are discussed in greater detail in other sections of the label: • Myopathy and Rhabdomyolysis [see Warnings and Precautions (5.1)] • Immune-Mediated Necrotizing Myopathy [see Warnings and Precautions (5.2)] • Hepatic Dysfunction [see Warnings and Precautions (5.3)] • Increases in HbA1c and Fasting Serum Glucose Levels [see Warnings and Precautions (5.4)] Most frequent adverse reactions occurring in ≥ 2.5% of subjects treated with LESCOL XL and more than placebo are: influenza-like symptoms, sinusitis, dyspepsia, urinary tract infection, bronchitis, and nausea.
( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Sandoz Inc. at 1-800-525-8747 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
6.1Clinical Trials Experience Because clinical trials are conducted under widely varying conditions, adverse reaction rates observed in the clinical trials of a drug cannot be directly compared to rates in the clinical trials of another drug and may not reflect the rates observed in practice. In the fluvastatin capsule, clinical trials there were 2326 patients treated with fluvastatin (age range, 18 to 75 years, 44% women, 94% White, 4% Black or African American, 2% other ethnicities) with a median treatment duration of 24 weeks.
The most common adverse reactions that led to treatment discontinuation and occurred at an incidence greater than placebo were: transaminase increased (0.8%), upper abdominal pain (0.3%), dyspepsia (0.3%), fatigue (0.2%), and diarrhea (0.2%). In the LESCOL XL clinical trials there were 912 patients treated with LESCOL XL (age range, 21 to 87 years, 52% women, 91% White, 4% Black of African American, 5% other ethnicities) with a median treatment duration of 24 weeks. The most common adverse reactions that led to treatment discontinuation were abdominal pain (0.7%), diarrhea (0.5%), nausea (0.4%), dyspepsia (0.4%) and chest pain (0.3%).
Adverse reactions occurring in the fluvastatin capsules and LESCOL XL controlled trials with a frequency ≥ 2% included the following: Table 1. Adverse Reactions Reported in ≥ 2% in Patients Treated with Fluvastatin Capsules/LESCOL XL and at an Incidence Greater Than Placebo in Placebo-Controlled Trials Pooled Dosages Adverse reaction Placebo a N = 960 (%) Fluvastatin capsules a N = 2326 (%) LESCOL XL b N = 912 (%) Influenza-like symptoms 5.7 5.1
7.1Headache 7.8 8.9
4.7Myalgia 4.5 5.0
3.8Abdominal pain 3.8 4.9
3.7Dyspepsia 3.2 7.9
3.5Sinusitis 1.9 2.6
3.5Diarrhea 4.2 4.9
3.3 Arthropathy NA NA
3.2Urinary tract infection 1.1 1.6
2.7Nausea 2.0 3.2
2.5Bronchitis 1.0 1.8
2.6Fatigue 2.3 2.7
1.6Flatulence 2.5 2.6
1.4Arthritis 2.0 2.1
1.3Allergy 2.2 2.3
1.0Insomnia 1.4 2.7 0.8 a Controlled trials with fluvastatin capsules (20 mg and 40 mg daily and 40 mg twice daily) compared to placebo. b Controlled trials with LESCOL XL 80 mg Tablets as compared to fluvastatin capsules. In the LESCOL Intervention Prevention Study (LIPS), the effect of LESCOL (fluvastatin capsules) 40 mg, administered twice daily on the risk of recurrent cardiac events was assessed in 1677 patients with coronary heart disease who had undergone a percutaneous coronary intervention. This was a multicenter, randomized, double-blind, placebo-controlled trial, patients were treated with dietary/lifestyle counseling and either fluvastatin capsules 40 mg (n = 844) or placebo (n = 833) given twice daily for a median of 3.9 years [see Clinical Studies (14.3)].Table 2.
Adverse Reactions Reported in ≥ 2% in Patients Treated with Fluvastatin Capsules/LESCOL XL and at an Incidence Greater Than Placebo in the LIPS Trial Table 2. Adverse Reactions Reported in ≥ 2% in Patients Treated with Fluvastatin Capsules/LESCOL XL and at an Incidence Greater Than Placebo in the LIPS Trial Adverse reaction Placebo N = 818 (%) Fluvastatin Capsules 40 mg twice daily N = 822 (%) Abdominal pain upper 4.5
6.3Hypertension 4.2
5.8Fatigue 3.8
4.7Dyspepsia 4.0
4.5Edema peripheral 2.…
🔄 Drug Interactions ▾
7 DRUG INTERACTIONS • Gemfibrozil : Avoid use with LESCOL XL. ( 7.1 ) • Cyclosporine and Fluconazole : Avoid use with LESCOL XL. ( 7.1 ) • Fibrates, Lipid-modifying doses (≥ 1 g/day) of Niacin, and Colchicine : Consider if the benefit of concomitant use with LESCOL XL outweighs the increased risk of myopathy and rhabdomyolysis.
If concomitant use is decided, monitor patients for signs and symptoms of myopathy, particularly during initiation of therapy and during upward dose titration. ( 7.1 ) • Warfarin : Obtain an International Normalized Ratio (INR) before starting and frequently enough after initiation or discontinuation to ensure that no significant alteration in INR occurs. Once the INR is stable, monitor INR at regular intervals.
( 7.2 ) • Glyburide : Monitor blood glucose levels when LESCOL XL is initiated. ( 7.2 ) • Phenytoin : Monitor plasma phenytoin levels when LESCOL XL treatment is initiated. ( 7.2 )
7.1Drug Interactions that Increase the Risk of Myopathy and Rhabdomyolysis with LESCOL XL Table 3 includes a list of drugs that increase the risk of myopathy and rhabdomyolysis when used concomitantly with fluvastatin and instructions for preventing or managing them [see Warnings and Precautions (5.1), Clinical Pharmacology (12.3)] . Table 3. Drug Interactions That Increase the Risk of Myopathy and Rhabdomyolysis with LESCOL XL Gemfibrozil Clinical impact There is an increased risk of myopathy/rhabdomyolysis when LESCOL XL is administered with gemfibrozil Intervention Avoid concomitant use of gemfibrozil with LESCOL XL.
Cyclosporine Clinical impact Cyclosporine coadministration increases fluvastatin exposure. The risk of myopathy and rhabdomyolysis may be increased with concomitant use of cyclosporine with LESCOL XL. Intervention Avoid concomitant use of cyclosporine with LESCOL XL.
Fluconazole Clinical impact Fluconazole coadministration increases fluvastatin exposure. The risk of myopathy and rhabdomyolysis may be increased with concomitant use of fluconazole with LESCOL XL. Intervention Avoid concomitant use of fluconazole with LESCOL XL Niacin Clinical impact Risk of myopathy and rhabdomyolysis may be enhanced with concomitant use with lipid-modifying doses (≥ 1 g/day) of niacin with LESCOL XL.
Intervention Consider if the benefit of using lipid-modifying doses (≥ 1 g/day) of niacin concomitantly with LESCOL XL outweighs the increased risk of myopathy and rhabdomyolysis. If concomitant use is decided, monitor patients for signs and symptoms of myopathy, particularly during initiation of therapy and during upward dose titration. Fibrates Clinical impact Fibrates may cause myopathy when given alone.
The risk of myopathy and rhabdomyolysis may be increased with concomitant use of fibrates with LESCOL XL. Intervention Consider if the benefit of using fibrates concomitantly with LESCOL XL outweighs the increased risk of myopathy and rhabdomyolysis. If concomitant use is decided, monitor patients for signs and symptoms of myopathy, particularly during initiation of therapy and during upward dose titration.
Colchicine Clinical impact Cases of myopathy and rhabdomyolysis have been reported with concomitant use of colchicine with fluvastatin. Intervention Consider if the benefit of using colchicine concomitantly with LESCOL XL outweighs the increased risk of myopathy and rhabdomyolysis. If concomitant use is decided, monitor patients for signs and symptoms of myopathy, particularly during initiation of therapy and during upward dose titration.
7.2LESCOL XL Effects on Other Drugs Table 4 presents LESCOL XL’s effect on other drugs and instructions for preventing or managing them. Table 4. LESCOL XL Effects on Other Drugs Warfarin Clinical impact There are postmarketing reports of clinically evident bleeding and/or increased INR in patients taking concomitant statins and warfarin.
Intervention In patients taking warfarin, obtain an INR before starting LESCOL XL and frequently enough after initiation or discontinuation to en…
👥 Use in Specific Populations ▾
8 USE IN SPECIFIC POPULATIONS • Pregnancy: May cause fetal harm ( 8.1 ) • Lactation: Breastfeeding not recommended during treatment with LESCOL XL ( 8.2 )
8.1Pregnancy Risk Summary Discontinue LESCOL XL when pregnancy is recognized. Alternatively, consider the ongoing therapeutic needs of the individual patient. LESCOL XL decreases synthesis of cholesterol and possibly other biologically active substances derived from cholesterol; therefore, LESCOL XL may cause fetal harm when administered to pregnant patients based on the mechanism of action [see Clinical Pharmacology (12.1)] .
In addition, treatment of hyperlipidemia is not generally necessary during pregnancy. Atherosclerosis is a chronic process and the discontinuation of lipid-lowering drugs during pregnancy should have little impact on the outcome of long-term therapy of primary hyperlipidemia for most patients. Available data from case series and prospective and retrospective observational cohort studies over decades of use with statins in pregnant women have not identified a drug-associated risk of major congenital malformations.
Published data from prospective and retrospective observational cohort studies with LESCOL XL use in pregnant women are insufficient to determine if there is a drug-associated risk of miscarriage (see Data) . In animal reproduction studies, no adverse developmental effects were observed in pregnant rats or rabbits orally administered fluvastatin during the period of organogenesis at doses that resulted in 2 and 5 times, respectively, the human exposure at the maximum recommended human dosage of 40 mg/day, based on body surface area (mg/m 2 ) (see Data) .
The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2% to 4% and 15% to 20%, respectively. Data Human Data A Medicaid cohort linkage study of 1152 statin-exposed pregnant women compared to 886,996 controls did not find a significant teratogenic effect from maternal use of statins in the first trimester of pregnancy, after adjusting for potential confounders, including maternal age, diabetes mellitus, hypertension, obesity, and alcohol and tobacco use using propensity score-based methods.
The relative risk of congenital malformations between the group with statin use and the group with no statin use in the first trimester was 1.07 (95% CI: 0.85 to 1.37) after controlling for confounders, particularly preexisting diabetes mellitus. There were also no statistically significant increases in any of the organ-specific malformations assessed after accounting for confounders. In the majority of pregnancies, statin treatment was initiated prior to pregnancy and was discontinued at some point in the first trimester when pregnancy was identified.
Study limitations include reliance on physician coding to define the presence of a malformation, lack of control for certain confounders such as body mass index, use of prescription dispensing as verification for the use of a statin, and lack of information on non-live births. Animal Data Fluvastatin sodium given to rats during organogenesis at doses of 12 mg/kg/day and in rabbits at doses of 10 mg/kg/day produced delays in skeletal development. These doses resulted in 2 times (rat at 12 mg/kg) or 5 times (rabbit at 10 mg/kg) the 40 mg human exposure based on mg/m 2 surface area.
Malaligned thoracic vertebrae were seen in rats at 36 mg/kg, a dose that produced significant maternal toxicity. A study in which female rats were given fluvastatin during the third trimester at 12 and 24 mg/kg/day resulted in maternal mortality at or near term and postpartum. In addition, fetal and neonatal lethality were apparent.
No effects on the dam or fetus occurred at 2 mg/kg/day. A second study at levels of 2, 6, 12 and 24 mg/kg/day confirmed the findings in the first study with neo…
🆘 Overdosage ▾
10 OVERDOSAGE No specific antidotes for LESCOL XL are known. In the event of an overdose of LESCOL XL, consider contacting the Poison Help line (1-800-222-1222) or a medical toxicologist for additional overdosage management recommendations.
🧬 Clinical Pharmacology ▾
12 CLINICAL PHARMACOLOGY
12.1Mechanism of Action Fluvastatin is a competitive inhibitor of HMG-CoA reductase, the rate limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, a precursor of cholesterol.
12.2Pharmacodynamics Inhibition of HMG-CoA reductase by fluvastatin accelerates the expression of LDL-receptors, followed by the uptake of LDL-C from blood to the liver, leading to a decrease in plasma LDL-C and total cholesterol. Sustained inhibition of cholesterol synthesis in the liver also decreases levels of very-low-density lipoproteins. The maximum LDL-C reduction of LESCOL XL is usually achieved by 4 weeks and is maintained after that.
12.3Pharmacokinetics Absorption Fluvastatin administered as LESCOL XL 80 mg tablets reaches peak concentration in approximately 3 hours under fasting conditions, after a low-fat meal, or 2.5 hours after a low-fat meal. The mean relative bioavailability of the XL tablet is approximately 29% (range, 9% to 66%) compared to that of the fluvastatin immediate-release capsule administered under fasting conditions. Administration of a high-fat meal delayed the absorption (T max 6h) and increased the bioavailability of the XL tablet by approximately 50%.
However, the maximum concentration of LESCOL XL 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. Distribution Fluvastatin is 98% bound to plasma proteins. The mean volume of distribution (VD ss ) is estimated at
0.35L/kg. At therapeutic concentrations, the protein binding of fluvastatin is not affected by warfarin, salicylic acid and glyburide. Elimination Metabolism Fluvastatin is metabolized in the liver, primarily via hydroxylation of the indole ring at the 5- and 6-positions.
N-dealkylation and beta-oxidation of the side-chain also occurs. The hydroxy metabolites have some pharmacologic activity, but do not circulate in the blood. Fluvastatin has two enantiomers.
Both enantiomers of fluvastatin are metabolized in a similar manner. In vitro data indicate that fluvastatin metabolism involves multiple Cytochrome P450 (CYP) isozymes. CYP2C9 isoenzyme is primarily involved in the metabolism of fluvastatin (approximately 75%), while CYP2C8 and CYP3A4 isoenzymes are involved to a much less extent, i.e., approximately 5% and approximately 20%, respectively.
Excretion Following oral administration, fluvastatin is primarily (about 90%) excreted in the feces as metabolites, with less than 2% present as unchanged drug. Approximately 5% of a radiolabeled oral dose were recovered in urine. The elimination half-life (t 1/2 ) of fluvastatin is approximately 3 hours.
Specific Populations Geriatric Patients Plasma levels of fluvastatin are not significantly different in patients age > 65 years compared to patients age 21 to 49 years. Gender In a study evaluating the effect of age and gender on fluvastatin pharmacokinetics, there were no significant differences in fluvastatin exposures between males and females, except between younger females and younger males (both ages 21-49 years), where there was an approximate 30% increase in area under the curve (AUC) in females. Adjusting for body weight decreases the magnitude of the differences seen.
For LESCOL XL, the AUC increases 67% and 77% for women compared to men under fasted and high- fat meal fed conditions, respectively. Pediatric Patients Pharmacokinetic data in the pediatric population are not available. Patients with Renal Impairment In patients with moderate to severe renal impairment (CLCr 10-40 mL/min), AUC and Cmax increased approximately 1.2-fold after administration of a single dose of 40 mg fluvastatin compared to healthy volunteers.
In patients with end-stage renal disease on hemodialysis, the AUC increased by approximately 1.5-fold. LESCOL XL was not evaluated in patients with renal impairment [see Use in Specific Populations (8.6)] . However, systemic exposures after…
🧬 Mechanism of Action ▾
12.1Mechanism of Action Fluvastatin is a competitive inhibitor of HMG-CoA reductase, the rate limiting enzyme that converts 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) to mevalonate, a precursor of cholesterol.
📦 How Supplied / Storage and Handling ▾
16 HOW SUPPLIED/STORAGE AND HANDLING How Supplied LESCOL XL extended-release tablets supplied as: Strength How supplied NDC Tablet description 80 mg of fluvastatin bottles of 30 66758-211-31 Yellow, round, slightly biconvex film-coated tablet with beveled edges debossed with “LESCOL XL” on one side and “80” on the other Store and Dispense Store at 20ºC to 25ºC (68ºF to 77ºF); excursions permitted between 15ºC to 30ºC (59ºF to 86ºF) [see USP Controlled Room Temperature]. Dispense in a tight container. Protect from light.
📋 Description ▾
11 DESCRIPTION Fluvastatin sodium inhibits 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase. Fluvastatin sodium is [ R *, S *-( E )]-(±)-7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1 H -indol-2-yl]-3,5-dihydroxy-6-heptenoic acid, monosodium salt. The empirical formula of fluvastatin sodium is C 24 H 25 FNO 4 •Na, its molecular weight is 433.46 g/mol and its structural formula is: Fluvastatin sodium is a white to pale yellow, hygroscopic powder soluble in water, ethanol and methanol.
LESCOL XL is supplied as extended-release tablets containing 84.24 mg of fluvastatin sodium, equivalent to 80 mg of fluvastatin, for oral use. LESCOL XL tablets contain the following inactive ingredients: hydroxypropyl cellulose, hydroxypropyl methyl cellulose, magnesium stearate, microcrystalline cellulose, polyethylene glycol 8000, potassium bicarbonate, povidone, titanium dioxide, and yellow iron oxide. Fluvastatin sodium structural formula
💬 Information for Patients ▾
17 PATIENT COUNSELING INFORMATION Advise the patient to read the FDA-approved patient labeling (Patient Information). Myopathy and Rhabdomyolysis Advise patients that LESCOL XL may cause myopathy and rhabdomyolysis. Instruct patients to promptly report any unexplained muscle pain, tenderness, or weakness particularly if accompanied by malaise or fever [see Warnings and Precautions (5.1), Drug Interactions (7.1)] .
Hepatic Dysfunction Inform patients that LESCOL XL may cause liver enzyme elevations and possibly liver failure. Advise patients to promptly report fatigue, anorexia, right upper abdominal discomfort, dark urine, or jaundice [see Warnings and Precautions (5.3)] . Increases in HbA1c and Fasting Serum Glucose Levels Inform patients that increases in HbA1c and fasting serum glucose levels may occur with LESCOL XL.
Encourage patients to optimize lifestyle measures, including regular exercise, maintaining a healthy body weight, and making healthy food choices [see Warnings and Precautions (5.4)] . Pregnancy Advise pregnant patients and patients who can become pregnant of the potential risk to a fetus. Advise patients to inform their healthcare provider of a known or suspected pregnancy to discuss if LESCOL XL should be discontinued [see Use in Specific Populations (8.1)] .
Lactation Advise patients that breastfeeding is not recommended during treatment with LESCOL XL [see Use in Specific Populations (8.2)] . Manufactured by Pfizer Ireland Pharmaceuticals Newbridge, Ireland for Sandoz Inc., Princeton, NJ 08540