Lescol Xl
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Questions & Answers
Side Effects & Adverse Reactions
Liver Enzymes
Biochemical abnormalities of liver function have been associated with HMG-CoA reductase inhibitors and other lipid-lowering agents. Approximately 1.1% of patients treated with Lescol® (fluvastatin sodium) capsules in worldwide trials developed dose-related, persistent elevations of transaminase levels to more than 3 times the upper limit of normal. Fourteen of these patients (0.6%) were discontinued from therapy. In all clinical trials, a total of 33/2969 patients (1.1%) had persistent transaminase elevations with an average fluvastatin exposure of approximately 71.2 weeks; 19 of these patients (0.6%) were discontinued. The majority of patients with these abnormal biochemical findings were asymptomatic.
In a pooled analysis of all placebo-controlled studies in which Lescol capsules were used, persistent transaminase elevations (>3 times the upper limit of normal [ULN] on two consecutive weekly measurements) occurred in 0.2%, 1.5%, and 2.7% of patients treated with 20, 40, and 80 mg (titrated to 40 mg twice daily) Lescol capsules, respectively. Ninety-one percent of the cases of persistent liver function test abnormalities (20 of 22 patients) occurred within 12 weeks of therapy and in all patients with persistent liver function test abnormalities there was an abnormal liver function test present at baseline or by Week 8.
In the pooled analysis of the 24-week controlled trials, persistent transaminase elevation occurred in 1.9%, 1.8% and 4.9% of patients treated with Lescol® XL (fluvastatin sodium) 80 mg, Lescol 40 mg and Lescol 40 mg twice daily, respectively. In 13 of 16 patients treated with Lescol XL the abnormality occurred within 12 weeks of initiation of treatment with Lescol XL 80 mg.
It is recommended that liver function tests be performed before the initiation of therapy and at 12 weeks following initiation of treatment or elevation in dose. Patients who develop transaminase elevations or signs and symptoms of liver disease should be monitored to confirm the finding and should be followed thereafter with frequent liver function tests until the levels return to normal. Should an increase in AST or ALT of three times the upper limit of normal or greater persist (found on two consecutive occasions) withdrawal of fluvastatin sodium therapy is recommended.
Active liver disease or unexplained transaminase elevations are contraindications to the use of Lescol and Lescol XL (see CONTRAINDICATIONS). Caution should be exercised when fluvastatin sodium is administered to patients with a history of liver disease or heavy alcohol ingestion (see CLINICAL PHARMACOLOGY: Pharmacokinetics/Metabolism). Such patients should be closely monitored.
Skeletal MuscleRhabdomyolysis with renal dysfunction secondary to myoglobinuria has been reported with fluvastatin and with other drugs in this class. Myopathy, defined as muscle aching or muscle weakness in conjunction with increases in creatine phosphokinase (CPK) values to greater than 10 times the upper limit of normal, has been reported.
Myopathy should be considered in any patients with diffuse myalgias, muscle tenderness or weakness, and/or marked elevation of CPK. Patients should be advised to report promptly unexplained muscle pain, tenderness or weakness, particularly if accompanied by malaise or fever. Fluvastatin sodium therapy should be discontinued if markedly elevated CPK levels occur or myopathy is diagnosed or suspected. Fluvastatin sodium therapy should also be temporarily withheld in any patient experiencing an acute or serious condition predisposing to the development of renal failure secondary to rhabdomyolysis, e.g., sepsis; hypotension; major surgery; trauma; severe metabolic, endocrine, or electrolyte disorders; or uncontrolled epilepsy.
The risk of myopathy and/or rhabdomyolysis during treatment with HMG-CoA reductase inhibitors has been reported to be increased if therapy with either cyclosporine, gemfibrozil, erythromycin, or niacin is administered concurrently. Isolated cases of myopathy have been reported during post-marketing experience with concomitant administration of fluvastatin and colchicine. No information is available on the pharmacokinetic interaction between fluvastatin and colchicine. However, myotoxicity, including muscle pain and weakness and rhabdomyloysis, have been reported anecdotally with concomitant administration of colchicine.
Myopathy was not observed in a clinical trial in 74 patients involving patients who were treated with fluvastatin sodium together with niacin.
Uncomplicated myalgia has been observed infrequently in patients treated with Lescol at rates indistinguishable from placebo.
The use of fibrates alone may occasionally be associated with myopathy. The combined use of HMG-CoA reductase inhibitors and fibrates should generally be avoided.
Legal Issues
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FDA Safety Alerts
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Manufacturer Warnings
There is currently no manufacturer warning information available for this drug.
FDA Labeling Changes
There are currently no FDA labeling changes available for this drug.
Uses
Therapy with lipid-altering agents should be used in addition to a diet restricted in saturated fat and cholesterol (see National Cholesterol Education Program [NCEP] Treatment Guidelines, below).
Hypercholesterolemia (heterozygous familial and nonfamilial) and Mixed DyslipidemiaLescol® (fluvastatin sodium) and Lescol® XL (fluvastatin sodium) are indicated to reduce elevated total cholesterol (Total-C), LDL-C, TG and Apo B levels, and to increase HDL-C in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Type IIa and IIb) whose response to dietary restriction of saturated fat and cholesterol and other nonpharmacological measures has not been adequate.
Heterozygous Familial Hypercholesterolemia in Pediatric PatientsLescol and Lescol XL are indicated as an adjunct to diet to reduce Total-C, LDL-C, and Apo B levels in adolescent boys and girls who are at least one year post-menarche, 10-16 years of age, with heterozygous familial hypercholesterolemia whose response to dietary restriction has not been adequate and the following findings are present:
- LDL-C remains > 190 mg/dL or
- LDL-C remains > 160 mg/dL and:
- there is a positive family history of premature cardiovascular disease or
- two or more other cardiovascular disease risk factors are present.
- there is a positive family history of premature cardiovascular disease or
Therapy with lipid-altering agents should be considered only after secondary causes for hyperlipidemia such as poorly controlled diabetes mellitus, hypothyroidism, nephrotic syndrome, dysproteinemias, obstructive liver disease, other medication, or alcoholism, have been excluded. Prior to initiation of fluvastatin sodium, a lipid profile should be performed to measure Total-C, HDL-C and TG. For patients with TG <400 mg/dL (<4.5 mmol/L), LDL-C can be estimated using the following equation:
LDL-C = Total-C - HDL-C - 1/5 TG
For TG levels >400 mg/dL (>4.5 mmol/L), this equation is less accurate and LDL-C concentrations should be determined by ultracentrifugation. In many hypertriglyceridemic patients LDL-C may be low or normal despite elevated Total-C. In such cases, Lescol is not indicated.
Lipid determinations should be performed at intervals of no less than 4 weeks and dosage adjusted according to the patient’s response to therapy.
The National Cholesterol Education Program (NCEP) Treatment Guidelines are summarized below:
| Risk Category | LDL Goal (mg/dL) |
LDL Level at Which to Initiate Therapeutic Lifestyle Changes (mg/dL) |
LDL Level at Which to Consider Drug Therapy (mg/dL) |
| CHD† or CHD risk equivalents (10-year risk >20%) |
<100 | >100 | >130 (100-129: drug optional)†† |
| 2+ Risk factors (10-year risk <20%) |
<130 | >130 | 10-year risk 10%-20%: >130 10-year risk <10%: >160 |
| 0-1 Risk factor††† | <160 | >160 | >190 (160-189: LDL-lowering drug optional) |
† CHD, coronary heart disease
†† Some authorities recommend use of LDL-lowering drugs in this category if an LDL-C level of <100mg/dL cannot be achieved by therapeutic lifestyle changes. Others prefer use of drugs that primarily modify triglycerides and HDL-C, e.g., nicotinic acid or fibrate. Clinical judgement also may call for deferring drug therapy in this subcategory.
††† Almost all people with 0-1 risk factor have 10-year risk <10%; thus, 10-year risk assessment in people with 0-1 risk factor is not necessary.
After the LDL-C goal has been achieved, if the TG is still >200 mg/dL, non-HDL-C (Total-C minus HDL-C) becomes a secondary target of therapy. Non-HDL-C goals are set 30 mg/dL higher than LDL-C goals for each risk category.
At the time of hospitalization for an acute coronary event, consideration can be given to initiating drug therapy at discharge if the LDL-C level is >130 mg/dL (NCEP-ATP II).
Since the goal of treatment is to lower LDL-C, the NCEP recommends that the LDL-C levels be used to initiate and assess treatment response. Only if LDL-C levels are not available, should the Total-C be used to monitor therapy.
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Lipid Elevations | |
| Type | Lipoproteins Elevated |
Major | Minor |
| I (rare) | Chylomicrons | TG | ↑→C |
| IIa | LDL | C | – |
| IIb | LDL, VLDL | C | TG |
| III (rare) | IDL | C/TG | – |
| IV | VLDL | TG | ↑→C |
| V (rare) | Chylomicrons, VLDL | TG | ↑→C |
C = cholesterol, TG = triglycerides, LDL = low density lipoprotein, VLDL = very low density lipoprotein,
IDL = intermediate density lipoprotein
Neither Lescol nor Lescol XL have been studied in conditions where the major abnormality is elevation of chylomicrons, VLDL, or IDL (i.e., hyperlipoproteinemia Types I, III, IV, or V).
The NCEP classification of cholesterol levels in pediatric patients with a familial history of hypercholesterolemia or premature cardiovascular disease is summarized below:
| Category | Total-C (mg/dL) | LDL-C (mg/dL) |
| Acceptable Borderline High |
<170 170-199 >200 |
<110 110-129 >130 |
Children treated with fluvastatin in adolescence should be re-evaluated in adulthood and appropriate changes made to their cholesterol-lowering regimen to achieve adult treatment goals.
Secondary Prevention of Coronary EventsIn patients with coronary heart disease, Lescol and Lescol XL are indicated to reduce the risk of undergoing coronary revascularization procedures.
AtherosclerosisLescol and Lescol XL are also indicated to slow the progression of coronary atherosclerosis in patients with coronary heart disease as part of a treatment strategy to lower total and LDL cholesterol to target levels.
History
There is currently no drug history available for this drug.
Other Information
Lescol® (fluvastatin sodium), is a water-soluble cholesterol lowering agent which acts through the inhibition of 3-hydroxy-3-methylglutaryl-coenzyme A (HMG-CoA) reductase.
Fluvastatin sodium is [R*,S*-(E)]-(±)-7-[3-(4-fluorophenyl)-1-(1-methylethyl)-1H-indol-2-yl]-3,5-dihydroxy-6-heptenoic acid, monosodium salt. The empirical formula of fluvastatin sodium is C24H25FNO4•Na, its molecular weight is 433.46 and its structural formula is:
This molecular entity is the first entirely synthetic HMG-CoA reductase inhibitor, and is in part structurally distinct from the fungal derivatives of this therapeutic class.
Fluvastatin sodium is a white to pale yellow, hygroscopic powder soluble in water, ethanol and methanol. Lescol is supplied as capsules containing fluvastatin sodium, equivalent to 20 mg or 40 mg of fluvastatin, for oral administration. Lescol® XL (fluvastatin sodium) is supplied as extended-release tablets containing fluvastatin sodium, equivalent to 80 mg of fluvastatin, for oral administration.
Active Ingredient: fluvastatin sodium
Inactive Ingredients in capsules: gelatin, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn), red iron oxide, sodium lauryl sulfate, talc, titanium dioxide, yellow iron oxide, and other ingredients.
Capsules may also include: benzyl alcohol, black iron oxide, butylparaben, carboxymethylcellulose sodium, edetate calcium disodium, methylparaben, propylparaben, silicon dioxide and sodium propionate.
Inactive Ingredients in extended-release tablets: microcrystalline cellulose, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, potassium bicarbonate, povidone, magnesium stearate, yellow iron oxide, titanium dioxide and polyethylene glycol 8000.
Sources
Lescol Xl Manufacturers
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Physicians Total Care, Inc.
![Lescol Xl (Fluvastatin Sodium) Tablet, Extended Release [Physicians Total Care, Inc.]](/wp-content/themes/bootstrap/assets/img/loading2.gif)
Lescol Xl | Physicians Total Care, Inc.
The patient should be placed on a standard cholesterol-lowering diet before receiving Lescol® (fluvastatin sodium) or Lescol® XL (fluvastatin sodium) and should continue on this diet during treatment with Lescol or Lescol XL. (See NCEP Treatment Guidelines for details on dietary therapy.)
For patients requiring LDL-C reduction to a goal of ≥25%, the recommended starting dose is 40 mg as one capsule in the evening, 80 mg as one Lescol XL tablet administered as a single dose at any time of the day or 80 mg in divided doses of the 40 mg capsule given twice daily. For patients requiring LDL-C reduction to a goal of <25% a starting dose of 20 mg may be used. The recommended dosing range is 20-80 mg/day. Lescol or Lescol XL may be taken without regard to meals, since there are no apparent differences in the lipid-lowering effects of fluvastatin sodium administered with the evening meal or 4 hours after the evening meal. Do not break, crush or chew Lescol XL tablets or open Lescol capsules prior to administration.
Since the maximal reductions in LDL-C of a given dose are seen within 4 weeks, periodic lipid determinations should be performed and dosage adjustment made according to the patient’s response to therapy and established treatment guidelines. The therapeutic effect of Lescol or Lescol XL is maintained with prolonged administration.
Heterozygous Familial Hypercholesterolemia in Pediatric PatientsThe recommended starting dose is one 20 mg Lescol capsule. Dose adjustments, up to a maximum daily dose administered either as Lescol capsules 40 mg twice daily or one Lescol XL 80 mg tablet once daily, should be made at 6 week intervals. Doses should be individualized according to the goal of therapy (see NCEP Pediatric Panel Guidelines and INDICATIONS AND USAGE.)1.
Concomitant TherapyLipid-lowering effects on total cholesterol and LDL cholesterol are additive when immediate release Lescol is combined with a bile-acid binding resin or niacin. When administering a bile-acid resin (e.g., cholestyramine) and fluvastatin sodium, Lescol should be administered at bedtime, at least 2 hours following the resin to avoid a significant interaction due to drug binding to resin. (See also ADVERSE REACTIONS: Concomitant Therapy.)
Dosage in Patients with Renal InsufficiencySince fluvastatin sodium is cleared hepatically with less than 6% of the administered dose excreted into the urine, dose adjustments for mild to moderate renal impairment are not necessary. Fluvastatin has not been studied at doses greater than 40 mg in patients with severe renal impairment; therefore caution should be exercised when treating such patients at higher doses.
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Carilion Materials Management
Lescol Xl | Carilion Materials Management
2.1 General Dosing InformationDose range: 20 mg to 80 mg/ day.
LESCOL/LESCOL XL can be administered orally as a single dose, with or without food.
Do not break, crush or chew LESCOL XL tablets or open LESCOL capsules prior to administration.
Do not take two LESCOL 40 mg capsules at one time.
Since the maximal effect of a given dose is seen within 4 weeks, periodic lipid determinations should be performed at this time and dosage adjusted according to the patient’s response to therapy and established treatment guidelines.
For patients requiring LDL-C reduction to a goal of ≥25%, the recommended starting dose is 40 mg as one capsule in the evening, 80 mg as one LESCOL XL tablet administered as a single dose at any time of the day or 80 mg in divided doses of the 40 mg capsule given twice daily. For patients requiring LDL-C reduction to a goal of <25% a starting dose of 20 mg may be used.
2.2 Adult Patients with Hypercholesterolemia (Heterozygous Familial and Nonfamilial) and Mixed DyslipidemiaAdult patients can be started on either LESCOL or LESCOL XL. The recommended starting dose for LESCOL is one 40 mg capsule in the evening, or one LESCOL 40 mg capsule twice daily. Do not take two LESCOL 40 mg capsules at one time.
The recommended starting dose for LESCOL XL is one 80 mg tablet administered as a single dose at any time of the day.
2.3 Pediatric Patients (10-16 years of age) with Heterozygous Familial HypercholesterolemiaThe recommended starting dose is one 20 mg LESCOL capsule. Dose adjustments, up to a maximum daily dose administered either as LESCOL capsules 40 mg twice daily or one LESCOL XL 80 mg tablet once daily should be made at 6 week intervals. Doses should be individualized according to the goal of therapy [ ] . see NCEP Pediatric Panel Guidelines and CLINICAL STUDIES(14)1
National Cholesterol Education Program (NCEP): Highlights of the Report of the Expert Panel on Blood Cholesterol Levels in Children and Adolescents. 89(3):495-501. 1992. 1Pediatrics.
2.4 Use with CyclosporineDo not exceed a dose of 20 mg b.i.d. LESCOL in patients taking cyclosporine . [see Drug Interactions 7.1]
2.5 Use with FluconazoleDo not exceed a dose of 20 mg b.i.d. LESCOL in patients taking fluconazole . [see Drug Interactions 7.2]
![Lescol Xl (Fluvastatin Sodium) Tablet, Extended Release [Carilion Materials Management]](http://dailymed.nlm.nih.gov/dailymed/image.cfm?setid=cd12fae6-f277-4679-a7a8-b98719fe6fa9&name=68151-4471.jpg)
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