Drugs Details

Drugs Info of Lescol, Lescol XL
Drugs Details
  • Drugs Type  : Multum
  • Date : 5th Feb 2015 02:20 am
  • Brand Name : Lescol, Lescol XL
  • Generic Name : fluvastatin (Pronunciation: FLOO va sta tin)
Descriptions

LESCOL 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:

 

Lescol® (fluvastatin sodium) Structural Formula Illustration

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 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: calcium carbonate, gelatin, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn), red iron oxide, sodium bicarbonate, 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, sodium lauryl sulfate, 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.

What are the possible side effects of fluvastatin (Lescol, Lescol XL)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking fluvastatin and call your doctor at once if you have any of these serious side effects:

  • unexplained muscle pain, tenderness, or weakness;
  • confusion, memory problems;
  • fever, unusual tiredness, and dark colored urine;
  • pain or burning when you urinate;
  • swelling, weight gain, urinating less than usual or not at all;
  • increased thirst, increased urination,...

Read All Potential Side Effects and See Pictures of Lescol »

What are the precautions when taking fluvastatin sodium (Lescol)?

Before taking fluvastatin, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, alcohol use.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Limit alcoholic beverages. Daily use of alcohol may increase your risk for liver problems, especially when combined with fluvastatin. Ask your doctor or pharmacist for more information.

Older adults may be...

Read All Potential Precautions of Lescol »

This monograph has been modified to include the generic and brand name in many instances.

Indications

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 indicated as 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.

Hypercholesterolemia (Heterozygous Familial and Nonfamilial) and Mixed Dyslipidemia

LESCOL and LESCOL XL are indicated

  • as an adjunct to diet to reduce elevated total cholesterol (Total-C), low-density lipoprotein cholesterol (LDL-C), triglyceride (TG) and apolipoprotein B (Apo B) levels, and to increase high-density lipoprotein cholesterol (HDL-C) in patients with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson Type IIa and IIb).
  • as an adjunct to diet to reduce Total-C, LDL-C, and Apo B levels in adolescent boys and adolescent girls who are at least one year post-menarche, 10-16 years of age, with heterozygous familial hypercholesterolemia 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

The NCEP classification of cholesterol levels in pediatric patients with a familial history of hypercholesterolemia or premature CVD is summarized below.

 

Category Total-C (mg/dL) LDL-C (mg/dL)
Acceptable < 170 < 110
Borderline 170-199 110-129
High ≥ 200 ≥ 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 Cardiovascular Disease

In patients with clinically evident CHD, LESCOL and LESCOL XL are indicated to:

  • reduce the risk of undergoing coronary revascularization procedures
  • slow the progression of coronary atherosclerosis

Limitations of Use

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).

Dosage Administration

General Dosing Information

Dose 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.

Adult Patients with Hypercholesterolemia (Heterozygous Familial and Nonfamilial) and Mixed Dyslipidemia

Adult 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.

Pediatric Patients (10-16 years of age) with Heterozygous Familial Hypercholesterolemia

The 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]1.

Use with Cyclosporine

Do not exceed a dose of 20 mg b.i.d. LESCOL in patients taking cyclosporine [see DRUG INTERACTIONS].

Use with Fluconazole

Do not exceed a dose of 20 mg b.i.d. LESCOL in patients taking fluconazole [see DRUG INTERACTIONS].

How Supplied

Dosage Forms And Strengths

  • LESCOL 20 mg capsules are brown and light brown imprinted twice with “ ” and “20” on one half and “LESCOL” and the LESCOL® (fluvastatin sodium) logo twice on the other half of the capsule.
  • LESCOL 40 mg capsules are brown and gold imprinted twice with “ ” and “40” on one half and “LESCOL” and the LESCOL® (fluvastatin sodium) logo twice on the other half of the capsule.
  • LESCOL XL 80 mg tablets are yellow, round, slightly biconvex film-coated tablet with beveled edges debossed with “LESCOL XL” on one side and “80” on the other.

Storage And Handling

LESCOL ® (fluvastatin sodium) Capsules

20 mg

Brown and light brown imprinted twice with “Logo” and “20” on one half and “LESCOL” and the LESCOL® (fluvastatin sodium) logo twice on the other half of the capsule.

Bottles of 30 capsules………………………...NDC 0078-0176-15
Bottles of 100 capsules………………………...NDC 0078-0176-05

40 mg

Brown and gold imprinted twice with “Logo ” and “40” on one half and “LESCOL” and the LESCOL® (fluvastatin sodium) logo twice on the other half of the capsule.

Bottles of 30 capsules………………………...NDC 0078-0234-15
Bottles of 100 capsules………………………...NDC 0078-0234-05

LESCOL® XL (fluvastatin sodium) Extended-Release Tablets

80 mg

Yellow, round, slightly biconvex film-coated tablet with beveled edges debossed with “LESCOL XL” on one side and “80” on the other.

Bottles of 30 tablets………………………...NDC 0078-0354-15
Bottle of 100 tablets………………………...NDC 0078-0354-05

Store and Dispense

Store at 25°C (77°F); excursions permitted to 15 -30°C (59 -86°F) [see USP Controlled Room Temperature]. Dispense in a tight container. Protect from light.

REFERENCES

1National Cholesterol Education Program (NCEP): Highlights of the Report of the Expert Panel on Blood Cholesterol Levels in Children and Adolescents. Pediatrics. 89(3):495-501. 1992.

Distributed by: Novartis Pharmaceuticals Corporation., East Hanover, New Jersey 07936. Revised February 2012

This monograph has been modified to include the generic and brand name in many instances.

Side Effects

The following serious adverse reactions are discussed in greater detail in other sections of the label:

  • Rhabdomyolysis with myoglobinuria and acute renal failure and myopathy (including myositis) [see WARNINGS AND PRECAUTIONS].
  • Liver Enzyme Abnormalities [see WARNINGS AND PRECAUTIONS].

Clinical Studies Experience in Adult Patients

Because clinical studies on LESCOL/LESCOL XL are conducted in varying study populations and study designs, the frequency of adverse reactions observed in the clinical studies of LESCOL/LESCOL XL cannot be directly compared with that in the clinical studies of other statins and may not reflect the frequency of adverse reactions observed in clinical practice.

In the LESCOL placebo-controlled clinical trials database of 2326 patients treated with LESCOL1 (age range 18-75 years, 44% women, 94% Caucasians, 4% Blacks, 2% other ethnicities) with a median treatment duration of 24 weeks, 3.4% of patients on LESCOL and 2.3% patients on placebo discontinued due to adverse reactions regardless of causality. 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 database of controlled clinical trials of 912 patients treated with LESCOL XL (age range 21-87 years, 52% women, 91% Caucasians, 4% Blacks, 5% other ethnicities) with a median treatment duration of 24 weeks, 3.9% of patients on LESCOL XL discontinued due to adverse reactions regardless of causality. 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%).

Clinically relevant adverse experiences occurring in the LESCOL and LESCOL XL controlled studies with a frequency > 2%, regardless of causality, included the following:

Table 1 : Clinical adverse events reported in > 2% in patients treated with LESCOL/LESCOL XL and at an incidence greater than placebo in placebo-controlled trials regardless of causality (% of patients) Pooled Dosages

    LESCOL1
N=2326
(%)
Placebo1
N=960
(%)
LESCOL XL2
N=912
(%)
Musculoskeletal Myalgia 5.0 4.5 3.8
Arthritis 2.1 2.0 1.3
Arthropathy NA NA 3.2
Respiratory Sinusitis 2.6 1.9 3.5
Bronchitis 1.8 1.0 2.6
Gastrointestinal Dyspepsia 7.9 3.2 3.5
Diarrhea 4.9 4.2 3.3
Abdominal pain 4.9 3.8 3.7
Nausea 3.2 2.0 2.5
Flatulence 2.6 2.5 1.4
Tooth disorder 2.1 1.7 1.4
Psychiatric Insomnia 2.7 1.4 0.8
Genitourinary Urinary tract infection 1.6 1.1 2.7
Miscellaneous Headache 8.9 7.8 4.7
Influenza-like symptoms 5.1 5.7 7.1
Accidental Trauma 5.1 4.8 4.2
Fatigue 2.7 2.3 1.6
Allergy 2.3 2.2 1.0
1Controlled trials with LESCOL Capsules (20 and 40 mg daily and 40 mg twice daily) compared to placebo
2Controlled trials with LESCOL XL 80 mg Tablets as compared to LESCOL Capsules
LESCOL Intervention Prevention Study

In the LESCOL Intervention Prevention Study (LIPS), the effect of LESCOL 40 mg, administered twice daily on the risk of recurrent cardiac events was assessed in 1677 patients with CHD who had undergone a percutaneous coronary intervention (PCI) procedure. This was a multicenter, randomized, double-blind, placebo-controlled study, patients were treated with dietary/lifestyle counseling and either LESCOL 40 mg (n=844) or placebo (n=833) given twice daily for a median of 3.9 years [see Clinical Studies].

Table 2 : Clinical adverse events reported in ≥ 2% in patients treated with LESCOL/LESCOL XL and at an incidence greater than placebo in the LIPS Trial regardless of causality (% of patients)

    LESCOL 40 mg b.i.d
N=822
(%)
Placebo
N=818
(%)
Cardiac disorders Atrial fibrillation 2.4 2.0
Gastrointestinal disorders Abdominal pain upper 6.3 4.5
Constipation 3.3 2.1
Dyspepsia 4.5 4.0
Gastric disorder 2.7 2.1
Nausea 2.7 2.3
General disorders Fatigue 4.7 3.8
Edema peripheral 4.4 2.9
Infections and infestations Bronchitis 2.3 2.0
Nasopharyngitis 2.8 2.1
Musculoskeletal and connective tissue disorders Arthralgia 2.1 1.8
Myalgia 2.2 1.6
Pain in extremity 4.1 2.7
Nervous system disorders Dizziness 3.9 3.5
Syncope 2.4 2.2
Respiratory disorders Dyspnea exertional 2.8 2.4
Vascular disorders Hypertension 5.8 4.2
Intermittent claudication 2.3 2.1

Clinical Studies Experience in Pediatric Patients

In patients aged < 18 years, efficacy and safety have not been studied for treatment periods longer than two years.

In two open-label, uncontrolled studies, 66 boys and 48 girls with heterozygous familial hypercholesterolemia ( 9-16 years of age, 80% Caucasian, 19% Other [ mixed ethnicity], 1% Asians) were treated with fluvastatin sodium administered as LESCOL capsules 20 mg -40 mg twice daily, or LESCOL XL 80 mg extended-release tablet [see Clinical Studies and Use In Specific Populations].

Postmarketing Experience

Because adverse reactions from spontaneous reports are reported voluntarily from a population of uncertain size, it is generally not possible to reliably estimate their frequency or establish a causal relationship to drug exposure. The following effects have been reported with drugs in this class. Not all the effects listed below have necessarily been associated with fluvastatin sodium therapy.

Musculoskeletal: muscle cramps, myalgia, myopathy, rhabdomyolysis, arthralgias, muscle spasms, muscle weakness, myositis.

Neurological: dysfunction of certain cranial nerves (including alteration of taste, impairment of extra-ocular movement, facial paresis), tremor, dizziness, vertigo, paresthesia, hypoesthesia, dysesthesia, peripheral neuropathy, peripheral nerve palsy.

There have been rare postmarketing reports of cognitive impairment (e.g., memory loss, forgetfulness, amnesia, memory impairment, confusion) associated with statin use. These cognitive issues have been reported for all statins. The reports are generally nonserious, and reversible upon statin discontinuation, with variable times to symptom onset (1 day to years) and symptom resolution (median of 3 weeks).

Psychiatric: anxiety, insomnia, depression, psychic disturbances

Hypersensitivity Reactions: An apparent hypersensitivity syndrome has been reported rarely which has included one or more of the following features: anaphylaxis, angioedema, lupus erythematosus-like syndrome, polymyalgia rheumatica, vasculitis, purpura, thrombocytopenia, leukopenia, hemolytic anemia, positive ANA, ESR (erythrocyte sedimentation rate) increase, eosinophilia, arthritis, arthralgia, urticaria, asthenia, photosensitivity reaction, fever, chills, flushing, malaise, dyspnea, toxic epidermal necrolysis, erythema multiforme, including Stevens-Johnson syndrome.

Gastrointestinal: pancreatitis, hepatitis, including chronic active hepatitis, cholestatic jaundice, fatty change in liver, cirrhosis, fulminant hepatic necrosis, hepatoma, anorexia, vomiting, fatal and non-fatal hepatic failure.

Skin: rash, dermatitis, including bullous dermatitis, eczema, alopecia, pruritus, a variety of skin changes (e.g. nodules, discoloration, dryness of skin/mucous membranes, changes to hair/nails).

Reproductive: gynecomastia, loss of libido, erectile dysfunction.

Eye: progression of cataracts (lens opacities), ophthalmoplegia.

Laboratory abnormalities: elevated transaminases, alkaline phosphatase, gamma-glutamyl transpeptidase and bilirubin; thyroid function abnormalities.

Read the Lescol (fluvastatin sodium) Side Effects Center for a complete guide to possible side effects

Learn More »

Interactions

Cyclosporine

Cyclosporine coadministration increases fluvastatin exposure. Therefore, in patients taking cyclosporine, therapy should be limited to LESCOL 20 mg twice daily [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

Fluconazole

Administration of fluvastatin 40 mg single dose to healthy volunteers pre-treated with fluconazole for 4 days results in an increase of fluvastatin exposure. Therefore, in patients taking fluconazole, therapy should be limited to LESCOL 20 mg twice daily [see CLINICAL PHARMACOLOGY].

Gemfibrozil

Due to an increased risk of myopathy/rhabdomyolysis when HMG-CoA reductase inhibitors are coadministered with gemfibrozil, concomitant administration of LESCOL/LESCOL XL with gemfibrozil should be avoided.

Other Fibrates

Because it is known that the risk of myopathy during treatment with HMG-CoA reductase inhibitors is increased with concurrent administration of other fibrates, LESCOL/LESCOL XL should be administered with caution when used concomitantly with other fibrates [see WARNINGS AND PRECAUTIONS and CLINICAL PHARMACOLOGY].

Niacin

The risk of skeletal muscle effects may be enhanced when LESCOL is used in combination with lipid-modifying doses ( ≥ 1 g/day) of niacin; a reduction in LESCOL dosage should be considered in this setting [see WARNINGS AND PRECAUTIONS].

Glyburide

Concomitant administration of fluvastatin and glyburide increased glyburide exposures. Patients on concomitant therapy of glyburide and fluvastatin should continue to be monitored appropriately [see CLINICAL PHARMACOLOGY].

Phenytoin

Concomitant administration of fluvastatin and phenytoin increased phenytoin exposures. Patients should continue to be monitored appropriately when fluvastatin therapy is initiated or when fluvastatin dose is changed [see CLINICAL PHARMACOLOGY].

Warfarin

Bleeding and/or increased prothrombin times have been reported in patients taking coumarin anticoagulants concomitantly with other HMG-CoA reductase inhibitors. Therefore, patients receiving warfarin-type anticoagulants should have their prothrombin times closely monitored when fluvastatin sodium is initiated or the dosage of fluvastatin sodium is changed.

Colchicine

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

Read the Lescol Drug Interactions Center for a complete guide to possible interactions

Learn More »

This monograph has been modified to include the generic and brand name in many instances.

Warnings

Included as part of the PRECAUTIONS section.

Precautions

Skeletal Muscle

Rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with LESCOL/LESCOL XL and other drugs in this class.

LESCOL/LESCOL XL should be prescribed with caution in patients with predisposing factors for myopathy. These factors include advanced age ( > 65 years), renal impairment, and inadequately treated hypothyroidism.

The risk of myopathy and/or rhabdomyolysis with statins is increased with concurrent therapy with cyclosporine, erythromycin, fibrates or niacin. Myopathy was not observed in a clinical trial in 74 patients involving patients who were treated with LESCOL/LESCOL XL together with niacin. Isolated cases of myopathy have been reported during post-marketing experience with concomitant administration of LESCOL/LESCOL XL and colchicine. No information is available on the pharmacokinetic interaction between LESCOL/LESCOL XL and colchicine.

Uncomplicated myalgia has also been reported in LESCOL-treated patients [see ADVERSE REACTIONS]. In clinical trials, uncomplicated myalgia has been observed infrequently in patients treated with LESCOL at rates indistinguishable from placebo. Myopathy, defined as muscle aching or muscle weakness in conjunction with increases in CPK values to greater than 10 times the upper limit of normal, was < 0.1% in fluvastatin clinical trials. Myopathy should be considered in any patient 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.

LESCOL/LESCOL XL therapy should be discontinued if markedly elevated CPK levels occur or myopathy is diagnosed or suspected. LESCOL/LESCOL XL 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.

Liver Enzymes

Increases in serum transaminases (aspartate aminotransferase [AST]/serum glutamic-oxaloacetic transaminase, or alanine aminotransferase [ALT]/serum glutamic-pyruvic transaminase) have been reported with HMG-CoA reductase inhibitors, including LESCOL/LESCOL XL. In most cases, the elevations were transient and resolved or improved on continued therapy or after a brief interruption in therapy.

Approximately 1.1% of patients treated with LESCOL capsules in worldwide trials developed dose-related, persistent elevations of serum 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 LESCOL 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 daily doses of 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 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 enzyme tests be performed prior to the initiation of LESCOL/LESCOL XL, and if signs or symptoms of liver injury occur.

There have been rare postmarketing reports of fatal and non-fatal hepatic failure in patients taking statins, including fluvastatin. If serious liver injury with clinical symptoms and/or hyperbilirubinemia or jaundice occurs during treatment with LESCOL/LESCOL XL, promptly interrupt therapy. If an alternate etiology is not found do not restart LESCOL/LESCOL XL.

In very rare cases, possibly drug-related hepatitis was observed that resolved upon discontinuation of treatment.1 Active liver disease or unexplained serum transaminase elevations are contraindications to the use of LESCOL and LESCOL XL [see CONTRAINDICATIONS. Caution should be exercised when LESCOL is administered to patients with a history of liver disease or heavy alcohol ingestion [see CLINICAL PHARMACOLOGY]. Such patients should be closely monitored.

Endocrine Effects

Increases in HbA1c and fasting serum glucose levels have been reported with HMG-CoA reductase inhibitors, including LESCOL/LESCOL XL.

Statins interfere with cholesterol synthesis and lower circulating cholesterol levels and, as such, might theoretically blunt adrenal or gonadal steroid hormone production.

LESCOL/LESCOL XL exhibited no effect upon non-stimulated cortisol levels and demonstrated no effect upon thyroid metabolism as assessed by measurement of thyroid stimulating hormone (TSH). Small declines in total serum testosterone have been noted in treated groups, but no commensurate elevation in LH occurred, suggesting that the observation was not due to a direct effect upon testosterone production. No effect upon FSH in males was noted. Due to the limited number of premenopausal females studied to date, no conclusions regarding the effect of LESCOL/LESCOL XL upon female sex hormones may be made.

Two clinical studies in patients receiving fluvastatin at doses up to 80 mg daily for periods of 24 to 28 weeks demonstrated no effect of treatment upon the adrenal response to ACTH stimulation. A clinical study evaluated the effect of LESCOL at doses up to 80 mg daily for 28 weeks upon the gonadal response to HCG stimulation. Although the mean total testosterone response was significantly reduced (p < 0.05) relative to baseline in the 80 mg group, it was not significant in comparison to the changes noted in groups receiving either 40 mg of LESCOL or placebo.

Patients treated with LESCOL/LESCOL XL who develop clinical evidence of endocrine dysfunction should be evaluated appropriately. Caution should be exercised if a statin or other agent used to lower cholesterol levels is administered to patients receiving other drugs (e.g. ketoconazole, spironolactone, cimetidine) that may decrease the levels of endogenous steroid hormones.

CNS Toxicity

CNS effects, as evidenced by decreased activity, ataxia, loss of righting reflex, and ptosis were seen in the following animal studies: the 18-month mouse carcinogenicity study at 50 mg/kg/day, the 6-month dog study at 36 mg/kg/day, the 6-month hamster study at 40 mg/kg/day, and in acute, high-dose studies in rats and hamsters (50 mg/kg), rabbits (300 mg/kg) and mice (1500 mg/kg). CNS toxicity in the acute high-dose studies was characterized (in mice) by conspicuous vacuolation in the ventral white columns of the spinal cord at a dose of 5000 mg/kg and (in rats) by edema with separation of myelinated fibers of the ventral spinal tracts and sciatic nerve at a dose of 1500 mg/kg. CNS toxicity, characterized by periaxonal vacuolation, was observed in the medulla of dogs that died after treatment for 5 weeks with 48 mg/kg/day; this finding was not observed in the remaining dogs when the dose level was lowered to 36 mg/kg/day. CNS vascular lesions, characterized by perivascular hemorrhages, edema, and mononuclear cell infiltration of perivascular spaces, have been observed in dogs treated with other members of this drug class. No CNS lesions have been observed after chronic treatment for up to 2 years with fluvastatin in the mouse (at doses up to 350 mg/kg/day), rat (up to 24 mg/kg/day), or dog (up to 16 mg/kg/day).

Prominent bilateral posterior Y suture lines in the ocular lens were seen in dogs after treatment with 1, 8, and 16 mg/kg/day for 2 years.

Patient Counseling Information

Information For Patients

Patients taking LESCOL/LESCOL XL should be advised that high cholesterol is a chronic condition and they should adhere to their medication along with their National Cholesterol Education Program (NCEP)-recommended diet, a regular exercise program, and periodic testing of a fasting lipid panel to determine goal attainment.

Patients should be advised about substances they should not take concomitantly with LESCOL/LESCOL XL [see WARNINGS AND PRECAUTIONS]. Patients should also be advised to inform other healthcare professionals prescribing a new medication that they are taking LESCOL/LESCOL XL.

Muscle Pain

Patients starting therapy with LESCOL/LESCOL XL should be advised of the risk of myopathy and told to report promptly any unexplained muscle pain, tenderness or weakness, particularly if accompanied by malaise or fever.

Liver Enzymes

It is recommended that liver enzyme tests be performed before the initiation of LESCOL/LESCOL XL and if signs or symptoms of liver injury occur. All patients treated with LESCOL/LESCOL XL should be advised to report promptly any symptoms that may indicate liver injury, including fatigue, anorexia, right upper abdominal discomfort, dark urine or jaundice.

Pregnancy

Women of childbearing age should be advised to use an effective method of birth control to prevent pregnancy while using LESCOL/LESCOL XL. Discuss future pregnancy plans with your patients, and discuss when to stop taking LESCOL/LESCOL XL if they are trying to conceive. Patients should be advised that if they become pregnant they should stop taking LESCOL/LESCOL XL and call their healthcare professional.

Breastfeeding

Women who are breastfeeding should not use LESCOL/LESCOL XL. Patients who have a lipid disorder and are breastfeeding should be advised to discuss the options with their healthcare professional.

Nonclinical Toxicology

Carcinogenesis, Mutagenesis, Impairment of Fertility

A 2-year study was performed in rats at dose levels of 6, 9, and 18-24 (escalated after 1 year) mg/kg/day. These treatment levels represented plasma drug levels of approximately 9, 13, and 26-35 times the mean human plasma drug concentration after a 40 mg oral dose. A low incidence of forestomach squamous papillomas and 1 carcinoma of the forestomach at the 24 mg/kg/day dose level was considered to reflect the prolonged hyperplasia induced by direct contact exposure to fluvastatin sodium rather than to a systemic effect of the drug. In addition, an increased incidence of thyroid follicular cell adenomas and carcinomas was recorded for males treated with 18-24 mg/kg/day. The increased incidence of thyroid follicular cell neoplasm in male rats with fluvastatin sodium appears to be consistent with findings from other HMG-CoA reductase inhibitors. In contrast to other HMG-CoA reductase inhibitors, no hepatic adenomas or carcinomas were observed.

The carcinogenicity study conducted in mice at dose levels of 0.3, 15 and 30 mg/kg/day revealed, as in rats, a statistically significant increase in forestomach squamous cell papillomas in males and females at 30 mg/kg/day and in females at 15 mg/kg/day. These treatment levels represented plasma drug levels of approximately 0.05, 2, and 7 times the mean human plasma drug concentration after a 40 mg oral dose.

No evidence of mutagenicity was observed in vitro, with or without rat-liver metabolic activation, in the following studies: microbial mutagen tests using mutant strains of Salmonella typhimurium or Escherichia coli; malignant transformation assay in BALB/3T3 cells; unscheduled DNA synthesis in rat primary hepatocytes; chromosomal aberrations in V79 Chinese Hamster cells; HGPRT V79 Chinese Hamster cells. In addition, there was no evidence of mutagenicity in vivo in either a rat or mouse micronucleus test.

In a study in rats at dose levels for females of 0.6, 2 and 6 mg/kg/day and at dose levels for males of 2, 10 and 20 mg/kg/day, fluvastatin sodium had no adverse effects on the fertility or reproductive performance.

Seminal vesicles and testes were small in hamsters treated for 3 months at 20 mg/kg/day (approximately three times the 40 mg human daily dose based on surface area, mg/m²). There was tubular degeneration and aspermatogenesis in testes as well as vesiculitis of seminal vesicles. Vesiculitis of seminal vesicles and edema of the testes were also seen in rats treated for 2 years at 18 mg/kg/day (approximately 4 times the human Cmax achieved with a 40 mg daily dose).

Fluvastatin sodium produced delays in skeletal development in rats at doses of 12 mg/kg/day and in rabbits at doses of 10 mg/kg/day. Malaligned thoracic vertebrae were seen in rats at 36 mg/kg, a dose that produced maternal toxicity. 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/m2 surface area. A study in which female rats were dosed 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 neonatal mortality beginning at 6 mg/kg. A modified Segment III study was performed at dose levels of 12 or 24 mg/kg/day with or without the presence of concurrent supplementation with mevalonic acid, a product of HMG-CoA reductase which is essential for cholesterol biosynthesis. The concurrent administration of mevalonic acid completely prevented the maternal and neonatal mortality but did not prevent low body weights in pups at 24 mg/kg on days 0 and 7 postpartum.

Use In Specific Populations

Pregnancy

Pregnancy Category X

LESCOL/LESCOL XL is contraindicated in women who are or may become pregnant [see CONTRAINDICATIONS].

Lipid lowering drugs are contraindicated during pregnancy, because cholesterol and cholesterol derivatives are needed for normal fetal development. Serum cholesterol and triglycerides increase during normal pregnancy. Atherosclerosis is a chronic process, and discontinuation of lipid-lowering drugs during pregnancy should have little impact on long-term outcomes of primary hypercholesterolemia therapy

There are no adequate and well-controlled studies of use with LESCOL/LESCOL XL during pregnancy. Rare reports of congenital anomalies have been received following intrauterine exposure to other statins. In a review2 of about 100 prospectively followed pregnancies in women exposed to other statins, the incidences of congenital anomalies, spontaneous abortions, and fetal deaths/stillbirths did not exceed the rate expected in the general population. The number of cases is adequate only to exclude a 3-to 4-fold increase in congenital anomalies over background incidence. In 89% of prospectively followed pregnancies, drug treatment was initiated prior to pregnancy and was discontinued at some point in the first trimester when pregnancy was identified.

Teratology studies with fluvastatin in rats and rabbits showed maternal toxicity at high dose levels, but there was no evidence of embryotoxic or teratogenic potential [see Non-Clinical Toxicology].

LESCOL or LESCOL XL should be administered to women of child-bearing potential only when such patients are highly unlikely to conceive and have been informed of the potential hazards. If a woman becomes pregnant while taking LESCOL or LESCOL XL, the drug should be discontinued and the patient advised again as to the potential hazards to the fetus.

Nursing Mothers

Based on animal data, fluvastatin is present in breast milk in a 2:1 ratio (milk:plasma). Because of the potential for serious adverse reactions in nursing infants, nursing women should not take LESCOL or LESCOL XL [see CONTRAINDICATIONS].

Pediatric Use

The safety and efficacy of LESCOL and LESCOL XL in children and adolescent patients 9-16 years of age with heterozygous familial hypercholesterolemia have been evaluated in open-label, uncontrolled clinical trials for a duration of two years. The most common adverse events observed were influenza and infections. In these limited uncontrolled studies, there was no detectable effect on growth or sexual maturation in the adolescent boys or on menstrual cycle length in girls [see Clinical Studies, ADVERSE REACTIONS and DOSAGE AND ADMINISTRATION]. Adolescent females should be counseled on appropriate contraceptive methods while on LESCOL therapy [see CONTRAINDICATIONS].

Geriatric Use

Fluvastatin exposures were not significantly different between the nonelderly and elderly populations (age ≥ 65 years) [see CLINICAL PHARMACOLOGY]. Since advanced age ( > 65 years) is a predisposing factor for myopathy, LESCOL/LESCOL XL should be prescribed with caution in the elderly.

Hepatic Impairment

LESCOL and LESCOL XL are contraindicated in patients with active liver disease or unexplained, persistent elevations in serum transaminases [see CLINICAL PHARMACOLOGY].

Renal Impairment

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 [see CLINICAL PHARMACOLOGY].

REFERENCES

1. National Cholesterol Education Program (NCEP): Highlights of the Report of the Expert Panel on Blood Cholesterol Levels in Children and Adolescents. Pediatrics. 89(3):495-501.1992.

2. Manson, J.M., Freyssinges, C., Ducrocq, M.B., Stephenson, W.P., Postmarketing Surveillance of Lovastatin and Simvastatin Exposure During Pregnancy, Reproductive Toxicology, 10(6): 439-446, 1996.

This monograph has been modified to include the generic and brand name in many instances.

OverDose

To date, there has been limited experience with overdosage of fluvastatin. If an overdose occurs, it should be treated symptomatically with laboratory monitoring and supportive measures should be instituted as required. The dialyzability of fluvastatin sodium and of its metabolites in humans is not known at present [see WARNINGS AND PRECAUTIONS].

In the pediatric population, there have been reports of overdosage with fluvastatin sodium in children including a 2 year-old and the other 3 years of age, either of whom may have possibly ingested fluvastatin sodium. The maximum amount of fluvastatin sodium that could have been ingested was 80 mg (4 x 20 mg capsules). Vomiting was induced by ipecac in both children and no capsules were noted in their emesis. Neither child experienced any adverse symptoms and both recovered from the incident without problems.

In the postmarketing experience there have been reports of accidental ingestion of LESCOL tablets in infants up to 3 years of age. In one case, increased serum CPK values were noted. There have been reports of intentional overdose in adolescents with the development of hepatic enzyme elevations, convulsions and gastroenteritis/vomiting/diarrhea. One case of intentional overdose as suicide attempt in a 15 year-old female reported ingestion of 2,800 mg LESCOL XL with hepatic enzyme elevation.

ContrainDications

Hypersensitivity to any Component of this Medication

LESCOL and LESCOL XL are contraindicated in patients with hypersensitivity to any component of this medication.

Active Liver Disease

LESCOL and LESCOL XL are contraindicated in patients with active liver disease or unexplained, persistent elevations in serum transaminases [see WARNINGS AND PRECAUTIONS].

Pregnancy

LESCOL and LESCOL XL are contraindicated in women who are pregnant or may become pregnant. Serum cholesterol and triglycerides increase during normal pregnancy, and cholesterol or cholesterol derivatives are essential for fetal development. LESCOL and LESCOL XL may cause fetal harm when administered to pregnant women. 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 hypercholesterolemia.

LESCOL and LESCOL XL should be administered to women of childbearing age only when such patients are highly unlikely to conceive and have been informed of the potential hazards. If the patient becomes pregnant while taking this drug, LESCOL and LESCOL XL should be discontinued and the patient should be apprised of the potential hazard to the fetus [see Use In Specific Populations].

Nursing Mothers

Fluvastatin is secreted into the breast milk of animals and because HMG-CoA reductase inhibitors have the potential to cause serious adverse reactions in nursing infants, women who require treatment with LESCOL or LESCOL XL should be advised not to breastfeed their infants [see Use In Specific Populations].

This monograph has been modified to include the generic and brand name in many instances.

Clinical Pharamacology

Mechanism of Action

LESCOL 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 sterols, including cholesterol. The inhibition of cholesterol biosynthesis reduces the cholesterol in hepatic cells, which stimulates the synthesis of LDL receptors and thereby increases the uptake of LDL particles. The end result of these biochemical processes is a reduction of the plasma cholesterol concentration.

Pharmacokinetics

Absorption

Following oral administration of the capsule, fluvastatin reaches peak concentrations in less than 1 hour. The absolute bioavailability is 24% (range 9%-50%) after administration of a 10 mg dose.

At steady state, administration of fluvastatin with the evening meal results in a 50% decrease in Cmax, a 11% decrease in AUC, and a more than two-fold increase in tmax as compared to administration 4 hours after the evening meal. No significant differences in the lipid-lowering effects were observed between the two administrations. After single or multiple doses above 20 mg, fluvastatin exhibits saturable first-pass metabolism resulting in more than dose proportional plasma fluvastatin concentrations.

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%-66%) compared to that of the LESCOL immediate-release capsule administered under fasting conditions. Administration of a high-fat meal delayed the absorption (Tmax: 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 LESCOL capsule.

Distribution

Fluvastatin is 98% bound to plasma proteins. The mean volume of distribution (VDss) is estimated at 0.35 L/kg. At therapeutic concentrations, the protein binding of fluvastatin is not affected by warfarin, salicylic acid and glyburide.

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 (t½) of fluvastatin is approximately 3 hours.

Specific Populations

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. However, systemic exposures after administration of LESCOL XL are lower than after the 40 mg immediate release capsule.

Hepatic Impairment

In patients with hepatic impairment due to liver cirrhosis, fluvastatin AUC and Cmax increased approximately 2.5-fold compared to healthy subjects after administration of a single 40 mg dose. The enantiomer ratios of the two isomers of fluvastatin in hepatic impairment patients were comparable to those observed in healthy subjects.

Geriatric

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 was 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 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

Pharmacokinetic data in the pediatric population are not available.

Drug-Drug Interactions

Data from drug-drug interactions studies involving coadministration of gemfibrozil, niacin, itraconazole, erythromycin, tolbutamide or clopidogrel indicate that the PK disposition of fluvastatin is not significantly altered when fluvastatin is coadministered with any of these drugs.

The below listed drug interaction information is derived from studies using LESCOL. Similar studies have not been conducted using the LESCOL XL tablet.

Table 3 : Effect of Co-administered Drugs on Fluvastatin Systemic Exposure

Co-administered drug and dosing regimen Fluvastatin    
  Dose (mg)* Change in AUC ** Change in Cmax **
Cyclosporine – stable dose (b.i.d,)† 20 mg QD for 14 weeks ↑90% ↑30%
Fluconazole 400 mg QD day 1, 200 mg b.i.d. day 2-4† 40 mg QD ↑ 84% ↑ 44%
Cholestyramine 8 g QD 20 mg QD administered 4 hrs after a meal plus cholestyramine ↓ 51% ↓ 83%
Rifampicin 600 mg QD for 6 days 20 mg QD ↓53% ↓42%
Cimetidine 400 mg b.i.d. for 5 days, QD on Day 6 20 mg QD ↑30% ↑ 40%
Ranitidine 150 mg b.i.d. for 5 days, QD on Day 6 20 mg QD ↑10% ↑50%
Omeprazole 40 mg QD for 6 days 20 mg QD ↑20% ↑ 37%
Phenytoin 300 mg QD 40 mg b.i.d. for 5 days ↑ 40 % ↑27%
Propranolol 40 mg b.i.d. for 3.5 days 40 mg QD ↓ 5% No change
Digoxin 0.1 – 0.5 mg QD for 3 weeks 40 mg QD No change ↑ 11%
Diclofenac 25 mg QD 40 mg QD for 8 days ↑50 % ↑80%
Glyburide 5 – 20 mg QD for 22 days 40 mg b.i.d for 14 days ↓ 51% ↑ 44%
*Single dose unless otherwise noted
**Mean ratio (with/without coadministered drug and no change = 1-fold) or % change (with/without coadministered drug and no change = 0%); symbols of ↑ and ↓ indicate the exposure increase and decrease, respectively.
† Considered clinically significant [see DOSAGE AND ADMINISTRATION and DRUG INTERACTIONS]

Data from drug-drug interaction studies involving fluvastatin and coadministration of either gemfibrozil, tolbutamide or lorsartan indicate that the PK disposition of either gemfibrozil, tolbutamide or lorsartan is not significantly altered when coadministered with fluvastatin.

Table 4 : Effect of Fluvastatin Co-Administration on Systemic Exposure of Other Drugs

Fluvastatin dosage regimen Co-administered drug    
  Name and Dose (mg)* Change in AUC* Change in Cmax*
40 mg QD for 5 days Phenytoin 300 mg QDf ↑ 20% ↑5%
40 mg b.i.d. for 21 days Glyburide 5 - 20 mg QD for 22 days f ↑70% ↑ 50%
40 mg QD for 8 days Diclofenac 25 mg QD ↑ 25% ↑60%
40 mg QD for 8 days Warfarin 30 mg QD S-warfarin: ↑7%
R-warfarin: no change
S-warfarin: ↑ 10%
R-warfarin: ↑ 6%
*Single dose unless otherwise noted
**Mean ratio (with/without coadministered drug and no change = 1-fold) or % change (with/without coadministered drug and no change = 0%); symbols of ↑ and ↓ indicate the exposure increase and decrease, respectively.
† Considered clinically significant [see DOSAGE AND ADMINISTRATION and DRUG INTERACTIONS]

Clinical Studies

Hypercholesterolemia (Heterozygous Familial and Nonfamilial) and Mixed Dyslipidemia

In 12 placebo-controlled studies in patients with primary hypercholesterolemia and mixed dyslipidemia, LESCOL was administered to 1621 patients in daily dose regimens of 20 mg, 40 mg, and 80 mg (40 mg twice daily) for at least 6 weeks duration (Table 5). After 24 weeks of treatment, treatment with LESCOL resulted in significantly reduced plasma LDL-C, TC, TG, and Apo B compared to placebo and was associated with variable increases in HDL-C across the dose range.

LESCOL XL has been studied in five controlled studies of patients with primary hypercholesterolemia and mixed dyslipidemia. LESCOL XL was administered to over 900 patients in trials from 4 to 26 weeks in duration. In the three largest of these studies, LESCOL XL given as a single daily dose of 80 mg significantly reduced Total-C, LDL-C, TG and Apo B and resulted in increases in HDL-C (Table 5).

In patients with primary mixed dyslipidemia as defined by baseline plasma TG levels ≥ 200 mg/dL and < 400 mg/dL, treatment with LESCOL/LESCOL XL produced significant decreases in Total-C, LDL-C, TG and Apo B and variable increases in HDL-C (Table 5).

Table 5 : Median Percent Change in Lipid Parameters from Baseline to Week 24 Endpoint All Placebo-Controlled Studies (LESCOL) and Active Controlled Trials (LESCOL XL)

Dose Total Chol TG LDL Apo B HDL
N % Δ N N % Δ N % Δ N
All Patients
  LESCOL 20 mg1 747 -17 747 -12 747 -22 114 -19 747 3
  LESCOL 40 mg 1 748 -19 748 -14 748 -25 125 -18 748 4
  LESCOL 40 mg twice daily1 257 -27 257 -18 257 -36 232 -28 257 6
  LESCOL XL 80 mg2 750 -25 750 -19 748 -35 745 -27 750 7
Baseline TG ≥ 200 mg/dL
  LESCOL 20 mg1 148 -16 148 -17 148 -22 23 -19 148 6
  LESCOL 40 mg1 179 -18 179 -20 179 -24 47 -18 179 7
  LESCOL 40 mg twice daily1 76 -27 76 -23 76 -35 69 -28 76 9
  LESCOL XL 80 mg2 239 -25 239 -25 237 -33 235 -27 239 11
1Data for LESCOL from 12 placebo-controlled trials
2Data for LESCOL XL 80 mg tablet from three 24-week controlled trials

Heterozygous Familial Hypercholesterolemia in Pediatric Patients

LESCOL was studied in two open-label, uncontrolled, dose-titration studies. The first study enrolled 29 pre-pubertal boys, 9-12 years of age, who had an LDL-C level > 90th percentile for age and one parent with primary hypercholesterolemia and either a family history of premature ischemic heart disease or tendon xanthomas. The mean baseline LDL-C was 226 mg/dL (range: 137-354 mg/dL). All patients were started on LESCOL capsules 20 mg daily with dose adjustments every 6 weeks to 40 mg daily then 80 mg daily (40 mg b.i.d.) to achieve an LDL-C goal between 96.7 – 123.7 mg/dL. Endpoint analyses were performed at Year 2. LESCOL decreased plasma levels of Total-C and LDL-C by 21% and 27%, respectively. The mean achieved LDL-C was 161 mg/dL (range: 74-336 mg/dL).

The second study enrolled 85 male and female patients, 10 to 16 years of age, who had an LDL-C > 190 mg/dL or LDL-C > 160 mg/dL and one or more risk factors for coronary heart disease, or LDL-C > 160 mg/dL and a proven LDL-receptor defect. The mean baseline LDL-C was 225 mg/dL (range: 148-343 mg/dL). All patients were started on LESCOL capsules 20 mg daily with dose adjustments every 6 weeks to 40 mg daily then 80 mg daily (LESCOL 80 mg XL tablet) to achieve an LDL-C goal of < 130 mg/dL. Endpoint analyses were performed at Week 114. LESCOL decreased plasma levels of Total-C and LDL-C by 22% and 28%, respectively. The mean achieved LDL-C was 159 mg/dL (range: 90-295 mg/dL).

The majority of patients in both studies (83% in the first study and 89% in the second study) were titrated to the maximum daily dose of 80 mg. At study endpoint, 26% to 30% of patients in both studies achieved a targeted LDL-C goal of < 130 mg/dL. The long-term efficacy of LESCOL or LESCOL XL therapy in childhood to reduce morbidity and mortality in adulthood has not been established.

Secondary Prevention of Cardiovascular Disease

In the LESCOL Intervention Prevention Study (LIPS), the effect of LESCOL 40 mg administered twice daily on the risk of recurrent cardiac events (time to first occurrence of cardiac death, nonfatal myocardial infarction, or revascularization) was assessed in 1677 patients with CHD who had undergone a percutaneous coronary intervention (PCI) procedure (mean time from PCI to randomization=3 days). In this multicenter, randomized, double-blind, placebo-controlled study, patients were treated with dietary/lifestyle counseling and either LESCOL 40 mg (n=844) or placebo (n=833) given twice daily for a median of 3.9 years. The study population was 84% male, 98% Caucasian, with 37% > 65 years of age. Mean baseline lipid concentrations were: total cholesterol 201 mg/dL, LDL-C 132 mg/dL, triglycerides 70 mg/dL and HDL-C 39 mg/dL.

LESCOL significantly reduced the risk of recurrent cardiac events (Figure 1) by 22% (p=0.013, 181 patients in the LESCOL group vs. 222 patients in the placebo group). Revascularization procedures comprised the majority of the initial recurrent cardiac events (143 revascularization procedures in the LESCOL group and 171 in the placebo group). Consistent trends in risk reduction were observed in patients > 65 years of age.

Figure 1 : Primary Endpoint – Recurrent Cardiac Events (Cardiac Death, Nonfatal MI or Revascularization Procedure) (ITT Population)

View Enlarged Table

Outcome data for the LESCOL Intervention Prevention Study are shown in Figure 2. After exclusion of revascularization procedures (CABG and repeat PCI) occurring within the first 6 months of the initial procedure involving the originally instrumental site, treatment with LESCOL was associated with a 32% (p=0.002) reduction in risk of late revascularization procedures (CABG or PCI occurring at the original site > 6 months after the initial procedure, or at another site).

Figure 2 : LESCOL® Intervention Prevention Study -Primary and Secondary Endpoints

View Enlarged Table

In the Lipoprotein and Coronary Atherosclerosis Study (LCAS), the effect of LESCOL therapy on coronary atherosclerosis was assessed by quantitative coronary angiography (QCA) in patients with CAD and mild to moderate hypercholesterolemia (baseline LDL-C range 115-190 mg/dL). In this randomized double-blind, placebo-controlled trial, 429 patients were treated with conventional measures (Step 1 AHA Diet) and either LESCOL 40 mg/day or placebo. In order to provide treatment to patients receiving placebo with LDL-C levels ≥ 160 mg/dL at baseline, adjunctive therapy with cholestyramine was added after Week 12 to all patients in the study with baseline LDL-C values of ≥ 160 mg/dL which were present in 25% of the study population. Quantitative coronary angiograms were evaluated at baseline and 2.5 years in 340 (79%) angiographic evaluable patients.

Compared to placebo, LESCOL significantly slowed the progression of coronary atherosclerosis as measured by within-patient per-lesion change in minimum lumen diameter (MLD), the primary endpoint (Figure 3 below), percent diameter stenosis (Figure 4), and the formation of new lesions (13% of all fluvastatin patients versus 22% of all placebo patients). A significant difference in favor of LESCOL was found between all fluvastatin and all placebo patients in the distribution among the three categories of definite progression, definite regression, and mixed or no change. Beneficial angiographic results (change in MLD) were independent of patients' gender and consistent across a range of baseline LDL-C levels.

Figure 3 : Change in Minimum Lumen Diameter (mm)

Change in Minimum Lumen Diameter - Illustration

Figure 4 : Change in % Diameter Stenosis

Change in % Diameter Stenosis - Illustration

This monograph has been modified to include the generic and brand name in many instances.

Patient Information

LESCOL®
(fluvastatin sodium) Capsules 20 mg, 40 mg

LESCOL ® XL
(fluvastatin sodium) Extended-Release Tablets 80 mg

You must read and follow all instructions before using LESCOL or LESCOL XL.

Read the Patient Information every time you or a family member gets LESCOL or LESCOL XL. There may be new information. This Patient Information does not take the place of talking with your doctor about your medical condition or treatment. If you have any questions about LESCOL or LESCOL XL, ask your doctor or pharmacist.

What are LESCOL and LESCOL XL?

LESCOL and LESCOL XL are prescription medicines called “statins” that lower cholesterol in your blood. They lower the “bad” cholesterol and triglycerides in your blood. They can raise your “good” cholesterol as well.

LESCOL and LESCOL XL are for people whose cholesterol does not come down enough with exercise and a low-fat diet alone.

LESCOL and LESCOL XL may be used in patients with heart disease (coronary artery disease) to:

  • lower the chances of heart problems which would require procedures to help restore blood flow to the heart.
  • slow the buildup of too much cholesterol in the arteries of the heart.

Treatment with LESCOL or LESCOL XL has not been shown to prevent heart attacks or stroke.

LESCOL and LESCOL XL have the same active ingredient, fluvastatin. However, LESCOL is a capsule that is taken one or two times a day and LESCOL XL is an extended-release tablet that is only taken one time a day.

Who should not take LESCOL or LESCOL XL?

Do not take LESCOL or LESCOL XL if you:

  • are pregnant or think you may be pregnant, or are planning to become pregnant. LESCOL and LESCOL XL may harm your unborn baby. If you get pregnant, stop taking LESCOL or LESCOL XL and call your doctor right away.
  • are breast-feeding. LESCOL and LESCOL XL can pass into your breast milk and may harm your baby
  • have liver problems
  • are allergic to LESCOL or LESCOL XL or any of its ingredients. The active ingredient in LESCOL and LESCOL XL is fluvastatin. See the end of this leaflet for a complete list of ingredients in LESCOL and LESCOL XL.

LESCOL and LESCOL XL have not been studied in children under 9 years of age.

Before taking LESCOL or LESCOL XL, tell your doctor if you:

  • have muscle aches or weakness
  • drink more than 2 glasses of alcohol daily
  • have diabetes
  • have a thyroid problem
  • have kidney problems

Some medicines should not be taken with LESCOL or LESCOL XL. Tell your doctor about all the medicines you take, including prescription and non-prescription medicines, vitamins and herbal supplements. LESCOL and LESCOL XL and certain other medicines can interact causing serious side effects. Especially tell your doctor if you take medicines for:

  • your immune system
  • cholesterol
  • infections
  • heart failure
  • seizures
  • diabetes
  • heartburn or stomach ulcers

Know all the medicines you take. Keep a list of all the medicines you take with you to show your doctor and pharmacist.

How should I take LESCOL or LESCOL XL?

  • Your doctor will prescribe the medicine that is right for you. Take LESCOL or LESCOL XL exactly as prescribed. Do not change your dose or stop LESCOL or LESCOL XL without talking to your doctor. Your doctor may do blood tests to check your cholesterol levels during treatment with LESCOL and LESCOL XL. Your dose of LESCOL or LESCOL XL may be changed based on these blood test results.
  • LESCOL XL tablets may be taken at any time of the day. Take LESCOL capsules at the same time every evening. When LESCOL capsules are taken twice daily, the capsules may be taken once in the morning and once in the evening. LESCOL and LESCOL XL can be taken with or without food.
  • LESCOL XL tablets must be swallowed whole with a liquid. Do not break, crush or chew LESCOL XL tablets or open LESCOL capsules. Tell your doctor if you cannot swallow tablets whole. You may need LESCOL capsules or a different medicine instead of LESCOL XL tablets.
  • Your doctor should start you on a low-fat and low-cholesterol diet before giving you LESCOL or LESCOL XL. Stay on this low-fat and low-cholesterol diet while taking LESCOL or LESCOL XL.
  • If you miss a dose of LESCOL or LESCOL XL, take it as soon as you remember. Do not take LESCOL or LESCOL XL if it has been more than 12 hours since your last dose. Wait and take the next dose at your regular time. Do not take 2 doses of LESCOL or LESCOL XL at the same time.
  • If you take too much LESCOL or LESCOL XL or overdose, call your doctor or Poison Control Center right away. Or, go to the nearest emergency room.

What should I avoid while taking LESCOL or LESCOL XL?

  • Talk to your doctor before you start any new medicines. This includes prescription and nonprescription medicines, vitamins and herbal supplements. LESCOL and LESCOL XL and certain other medicines can interact causing serious side effects.
  • Do not get pregnant. If you get pregnant, stop taking LESCOL or LESCOL XL right away and call your doctor.

What are the possible side effects of LESCOL and LESCOL XL?

When taking LESCOL and LESCOL XL, some patients may develop serious side effects, including:

muscle problems . These serious muscle problems can sometimes lead to kidney problems, including kidney failure. You have a higher chance for muscle problems if you are taking certain other medicines with LESCOL or LESCOL XL. Call your doctor right away if you have:

  • muscle problems like weakness, tenderness, or pain that happen without a good reason, especially if you also have a fever or feel more tired than usual

liver problems . Your doctor should do blood tests to check your liver before you start taking LESCOL or LESCOL XL, and if you have symptoms of liver problems while you take LESCOL or LESCOL XL. Call your doctor right away if you have the following symptoms of liver problems:

  • feel tired or weak
  • loss of appetite
  • upper belly pain
  • dark amber colored urine
  • yellowing of your skin or the whites of your eyes

The most common side effects of LESCOL or LESCOL XL are headache, upset stomach and stomach pain, diarrhea, flu-like symptoms, muscle pain, sinus infection, tiredness, or trouble sleeping. These side effects are usually mild and may go away. The following additional side effects have been reported with LESCOL/LESCOL XL: memory loss, and confusion.

Talk to your doctor or pharmacist if you have side effects that bother you or that will not go away.

These are not all the side effects of LESCOL and LESCOL XL. Ask your doctor or pharmacist for a complete list.

How should I store LESCOL and LESCOL XL?

  • Store LESCOL and LESCOL XL at room temperature, 59° to 86° F (15° to 30° C). Protect from light.
  • Do not keep medicine that is out of date or that you no longer need.
  • Keep LESCOL and LESCOL XL out of the reach of children. Be sure that if you throw medicines away, it is out of the reach of children.

General information about LESCOL and LESCOL XL

Medicines are sometimes prescribed for conditions that are not mentioned in patient information leaflets. Do not use LESCOL or LESCOL XL for a condition for which it was not prescribed. Do not give LESCOL or LESCOL XL to other people, even if they have the same problem you have; it may harm them.

For more information, you can also visit the Novartis Internet site at www.LESCOLXL.com or call the Novartis help line at 1-888-669-6682.

What are the ingredients in LESCOL and LESCOL XL?

Active Ingredient: fluvastatin sodium

Inactive Ingredients:

LESCOL Capsules: calcium carbonate, gelatin, magnesium stearate, microcrystalline cellulose, pregelatinized starch (corn), red iron oxide, sodium bicarbonate, talc, titanium dioxide, yellow iron oxide, and other ingredients. The capsules may also contain benzyl alcohol, black iron oxide, butylparaben, carboxymethylcellulose sodium, edetate calcium disodium, methylparaben, propylparaben, silicon dioxide, sodium lauryl sulfate, and sodium propionate.

LESCOL XL Tablets: microcrystalline cellulose, hydroxypropyl cellulose, hydroxypropyl methylcellulose, potassium bicarbonate, povidone, magnesium stearate, yellow iron oxide, titanium dioxide and polyethylene glycol 8000.

This monograph has been modified to include the generic and brand name in many instances.

Consumer Overview Uses

IMPORTANT: HOW TO USE THIS INFORMATION: This is a summary and does NOT have all possible information about this product. This information does not assure that this product is safe, effective, or appropriate for you. This information is not individual medical advice and does not substitute for the advice of your health care professional. Always ask your health care professional for complete information about this product and your specific health needs.

 

FLUVASTATIN - ORAL

 

(FLEW-vuh-stat-in)

 

COMMON BRAND NAME(S): Lescol

 

USES: Fluvastatin is used along with a proper diet to help lower "bad" cholesterol and fats (such as LDL, triglycerides) and raise "good" cholesterol (HDL) in the blood. It belongs to a group of drugs known as "statins." It works by reducing the amount of cholesterol made by the liver. Lowering "bad" cholesterol and triglycerides and raising "good" cholesterol decreases the risk of heart disease and helps prevent strokes and heart attacks.

In addition to eating a proper diet (such as a low-cholesterol/low-fat diet), other lifestyle changes that may help this medication work better include exercising, losing weight if overweight, and stopping smoking. Consult your doctor for more details.

 

HOW TO USE: Read the Patient Information Leaflet if available from your pharmacist before you start taking fluvastatin and each time you get a refill. If you have any questions, ask your doctor or pharmacist.

Take this medication by mouth with or without food as directed by your doctor, usually once daily in the evening. Some patients may be directed to take this medication twice daily. Do not open the capsules.

Dosage is based on your medical condition, response to treatment, age, and other medications you may be taking. Be sure to tell your doctor and pharmacist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

If you also take certain other drugs to lower your cholesterol (bile acid-binding resins such as cholestyramine or colestipol), take fluvastatin at least 1 hour before or at least 4 hours after taking these medications. These products can react with fluvastatin, preventing its full absorption.

Take this medication regularly in order to get the most benefit from it. Remember to take it at the same time(s) each day. It is important to continue taking this medication even if you feel well. Most people with high cholesterol or triglycerides do not feel sick.

It is very important to continue to follow your doctor's advice about diet and exercise. It may take up to 4 weeks before you get the full benefit of this drug.

Consumer Overview Side Effect

SIDE EFFECTS: Stomach upset may occur. If this effect persists or worsens, tell your doctor or pharmacist promptly.

Remember that your doctor has prescribed this medication because he or she has judged that the benefit to you is greater than the risk of side effects. Many people using this medication do not have serious side effects.

A very small number of people taking fluvastatin may have mild memory problems or confusion. If these rare effects occur, talk to your doctor.

This drug may infrequently cause muscle problems (which can rarely lead to very serious conditions called rhabdomyolysis and autoimmune myopathy). Tell your doctor right away if you develop any of these symptoms during treatment and if these symptoms persist after your doctor stops this drug: muscle pain/tenderness/weakness (especially with fever or unusual tiredness), change in the amount of urine.

This medication may rarely cause liver problems. If you notice any of the following rare but serious side effects, tell your doctor immediately: yellowing eyes/skin, dark urine, severe stomach/abdominal pain, persistent nausea/vomiting.

A very serious allergic reaction to this drug is rare. However, seek immediate medical attention if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.

This is not a complete list of possible side effects. If you notice other effects not listed above, contact your doctor or pharmacist.

In the US -

Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

In Canada - Call your doctor for medical advice about side effects. You may report side effects to Health Canada at 1-866-234-2345.

 

Read the Lescol (fluvastatin sodium) Side Effects Center for a complete guide to possible side effects

Learn More »

PRECAUTIONS: Before taking fluvastatin, tell your doctor or pharmacist if you are allergic to it; or if you have any other allergies. This product may contain inactive ingredients, which can cause allergic reactions or other problems. Talk to your pharmacist for more details.

Before using this medication, tell your doctor or pharmacist your medical history, especially of: liver disease, kidney disease, alcohol use.

Before having surgery, tell your doctor or dentist about all the products you use (including prescription drugs, nonprescription drugs, and herbal products).

Limit alcoholic beverages. Daily use of alcohol may increase your risk for liver problems, especially when combined with fluvastatin. Ask your doctor or pharmacist for more information.

Older adults may be more sensitive to the side effects of this drug, especially muscle problems.

This medication must not be used during pregnancy. Fluvastatin may harm an unborn baby. Therefore, it is important to prevent pregnancy while taking this medication. Consult your doctor for more details and to discuss the use of reliable forms of birth control (such as condoms, birth control pills) while taking this medication. If you become pregnant or think you may be pregnant, tell your doctor immediately.

This medication passes into breast milk and may have undesirable effects on a nursing infant. Breast-feeding while using this drug is not recommended. Consult your doctor before breast-feeding.

Consumer Overview Missed Dose

DRUG INTERACTIONS: See also How to Use section.

Drug interactions may change how your medications work or increase your risk for serious side effects. This document does not contain all possible drug interactions. Keep a list of all the products you use (including prescription/nonprescription drugs and herbal products) and share it with your doctor and pharmacist. Do not start, stop, or change the dosage of any medicines without your doctor's approval.

Some products that may interact with this drug include: colchicine, cyclosporine, phenytoin.

Do not take any red yeast rice products while you are taking fluvastatin because some red yeast rice products may also contain a statin called lovastatin. Taking fluvastatin and red yeast rice products together can increase your risk of serious muscle and liver problems.

 

OVERDOSE: If overdose is suspected, contact a poison control center or emergency room immediately. US residents can call their local poison control center at 1-800-222-1222. Canada residents can call a provincial poison control center.

 

NOTES: Do not share this medication with others.

Laboratory and/or medical tests (such as blood cholesterol/triglyceride levels) should be performed periodically to monitor your progress or check for side effects. Consult your doctor for more details.

 

MISSED DOSE: If you miss a dose, take it as soon as you remember. If it is near the time of the next dose, skip the missed dose and resume your usual dosing schedule. Do not double the dose to catch up.

 

STORAGE: Store at room temperature at 77 degrees F (25 degrees C) away from light and moisture. Brief storage between 59 and 86 degrees F (15 to 30 degrees C) is permitted. Do not store in the bathroom. Keep all medicines away from children and pets.

Do not flush medications down the toilet or pour them into a drain unless instructed to do so. Properly discard this product when it is expired or no longer needed. Consult your pharmacist or local waste disposal company for more details about how to safely discard your product.

 

Information last revised February 2014. Copyright(c) 2014 First Databank, Inc.

Patient Detailed Side Effect

Brand Names: Lescol, Lescol XL

Generic Name: fluvastatin (Pronunciation: FLOO va sta tin)

  • What is fluvastatin (Lescol)?
  • What are the possible side effects of fluvastatin (Lescol)?
  • What is the most important information I should know about fluvastatin (Lescol)?
  • What should I discuss with my healthcare provider before taking fluvastatin (Lescol)?
  • How should I take fluvastatin (Lescol)?
  • What happens if I miss a dose (Lescol)?
  • What happens if I overdose (Lescol)?
  • What should I avoid while taking fluvastatin (Lescol)?
  • What other drugs will affect fluvastatin (Lescol)?
  • Where can I get more information?

What is fluvastatin (Lescol)?

Fluvastatin is in a group of drugs called HMG CoA reductase inhibitors, or "statins." Fluvastatin reduces levels of "bad" cholesterol (low-density lipoprotein, or LDL) and triglycerides in the blood, while increasing levels of "good" cholesterol (high-density lipoprotein, or HDL).

Fluvastatin is used to treat high cholesterol in adults and children who are at least 10 years old. Lowering your cholesterol can help prevent heart disease and hardening of the arteries, conditions that can lead to heart attack, stroke, and vascular disease.

Fluvastatin may also be used for purposes not listed in this medication guide.

Lescol 20 mg

capsule, brown, imprinted with S 20, LESCOL

What are the possible side effects of fluvastatin (Lescol)?

Get emergency medical help if you have any of these signs of an allergic reaction: hives; difficulty breathing; swelling of your face, lips, tongue, or throat.

Stop taking fluvastatin and call your doctor at once if you have any of these serious side effects:

  • unexplained muscle pain, tenderness, or weakness;
  • confusion, memory problems;
  • fever, unusual tiredness, and dark colored urine;
  • pain or burning when you urinate;
  • swelling, weight gain, urinating less than usual or not at all;
  • increased thirst, increased urination, hunger, dry mouth, fruity breath odor, drowsiness, dry skin, blurred vision, weight loss); or
  • nausea, upper stomach pain, itching, loss of appetite, dark urine, clay-colored stools, jaundice (yellowing of the skin or eyes).

Less serious side effects may include:

  • headache;
  • mild muscle pain;
  • diarrhea;
  • mild nausea;
  • stomach pain or indigestion;
  • sleep problems (insomnia); or
  • cold symptoms such as stuffy nose, sneezing, sore throat.

This is not a complete list of side effects and others may occur. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.

Read the Lescol (fluvastatin sodium) Side Effects Center for a complete guide to possible side effects

Learn More »

What is the most important information I should know about fluvastatin (Lescol)?

You should not take fluvastatin if you are allergic to it, if you are pregnant or breast-feeding, or if you have liver disease.

Stop taking this medication and tell your doctor right away if you become pregnant.

Before taking fluvastatin, tell your doctor if you have ever had liver or kidney disease, diabetes, or a thyroid disorder, or if you drink more than 2 alcoholic beverages daily.

In rare cases, fluvastatin can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. Call your doctor right away if you have unexplained muscle pain, tenderness, or weakness especially if you also have fever, unusual tiredness, and dark colored urine.

Avoid eating foods that are high in fat or cholesterol. Fluvastatin will not be as effective in lowering your cholesterol if you do not follow a cholesterol-lowering diet plan.

Avoid drinking alcohol. It can raise triglyceride levels and may increase your risk of liver damage.

There are many other drugs that can increase your risk of serious medical problems if you take them together with fluvastatin. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor. Keep a list of all your medicines and show it to any healthcare provider who treats you.

Fluvastatin is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

Side Effects Centers
  • Lescol

Patient Detailed How Take

What should I discuss with my healthcare provider before taking fluvastatin (Lescol)?

You should not take fluvastatin if you are allergic to it, if you are pregnant or breast-feeding, or if you have liver disease.

To make sure you can safely take fluvastatin, tell your doctor if you have any of these other conditions:

  • history of liver disease;
  • history of kidney disease;
  • diabetes;
  • a thyroid disorder; or
  • if you drink more than 2 alcoholic beverages daily.

In rare cases, fluvastatin can cause a condition that results in the breakdown of skeletal muscle tissue, leading to kidney failure. This condition may be more likely to occur in older adults and in people who have kidney disease or poorly controlled hypothyroidism (underactive thyroid).

Tell your doctor about all other medications you use. Certain other drugs can increase your risk of serious muscle problems, and it is very important that your doctor knows if you are using any of them:

  • erythromycin (E.E.S., EryPed, Ery-Tab, Erythrocin, Pediazole);
  • fluconazole (Diflucan)
  • gemfibrozil (Lopid), fenofibric acid (Fibricor, Trilipix), or fenofibrate (Antara, Fenoglide, Lipofen, Lofibra, Tricor, Triglide);
  • medicines that contain niacin (Advicor, Niaspan, Niacor, Simcor, Slo-Niacin, and others); or
  • drugs that weaken your immune system, such as steroids, cancer medicine, or medicines used to prevent organ transplant rejection, such as cyclosporine (Gengraf, Neoral, Sandimmune), sirolimus (Rapamune), or tacrolimus (Prograf).

FDA pregnancy category X. This medication can harm an unborn baby or cause birth defects. Do not take fluvastatin if you are pregnant.Stop taking this medication and tell your doctor right away if you become pregnant. Use effective birth control to avoid pregnancy while you are taking fluvastatin.

Fluvastatin may pass into breast milk and could harm a nursing baby. Do not breast-feed while you are taking fluvastatin.

How should I take fluvastatin (Lescol)?

Take exactly as prescribed by your doctor. Do not take in larger or smaller amounts or for longer than recommended. Follow the directions on your prescription label.

Fluvastatin is usually taken once or twice daily, with or without food. Take the medicine at the same time each day. Your doctor may occasionally change your dose to make sure you get the best results.

Do not crush, chew, break, or open a fluvastatin tablet or capsule. Swallow it whole. Tell your doctor if you have trouble swallowing the pill.

You may need to stop using fluvastatin for a short time if you have:

  • uncontrolled seizures;
  • an electrolyte imbalance (such as high or low potassium levels in your blood);
  • severely low blood pressure;
  • a severe infection or illness; or
  • surgery or a medical emergency.

To be sure this medicine is helping your condition and is not causing harmful effects, your blood will need to be tested often. Visit your doctor regularly.

Fluvastatin is only part of a complete program of treatment that also includes diet, exercise, and weight control. Follow your diet, medication, and exercise routines very closely.

You may need to take fluvastatin on a long-term basis for the treatment of high cholesterol.

Store at room temperature away from moisture, heat, and light.

Side Effects Centers
  • Lescol

Patient Detailed Avoid Taking

What happens if I miss a dose (Lescol)?

Take the missed dose as soon as you remember. Skip the missed dose if your next dose is less than 12 hours away. Do not take extra medicine to make up the missed dose.

What happens if I overdose (Lescol)?

Seek emergency medical attention or call the Poison Help line at 1-800-222-1222.

What should I avoid while taking fluvastatin (Lescol)?

If you also take cholestyramine (Prevalite, Questran) or colestipol (Colestid), avoid taking them within 2 hours before you take fluvastatin.

Avoid eating foods that are high in fat or cholesterol. Fluvastatin will not be as effective in lowering your cholesterol if you do not follow a cholesterol-lowering diet plan.

Avoid drinking alcohol. It can raise triglyceride levels and may increase your risk of liver damage.

What other drugs will affect fluvastatin (Lescol)?

Tell your doctor about all other medications you use, especially:

  • cimetidine (Tagamet);
  • a blood thinner such as warfarin (Coumadin, Jantoven);
  • glyburide (DiaBeta, Glynase, Micronase);
  • omeprazole (Prilosec);
  • phenytoin (Dilantin);
  • ranitidine (Zantac);
  • spironolactone (Aldactone, Aldactazide); or
  • any other "statin" medication such as atorvastatin (Lipitor, Caduet), lovastatin (Altoprev, Mevacor), pravastatin (Pravachol), rosuvastatin (Crestor), or simvastatin (Zocor, Simcor, Vytorin).

This list is not complete and other drugs may interact with fluvastatin. Tell your doctor about all medications you use. This includes prescription, over-the-counter, vitamin, and herbal products. Do not start a new medication without telling your doctor.

Where can I get more information?

Your pharmacist can provide more information about fluvastatin.


Remember, keep this and all other medicines out of the reach of children, never share your medicines with others, and use this medication only for the indication prescribed.

Every effort has been made to ensure that the information provided by Cerner Multum, Inc. ('Multum') is accurate, up-to-date, and complete, but no guarantee is made to that effect. Drug information contained herein may be time sensitive. Multum information has been compiled for use by healthcare practitioners and consumers in the United States and therefore Multum does not warrant that uses outside of the United States are appropriate, unless specifically indicated otherwise. Multum's drug information does not endorse drugs, diagnose patients or recommend therapy. Multum's drug information is an informational resource designed to assist licensed healthcare practitioners in caring for their patients and/or to serve consumers viewing this service as a supplement to, and not a substitute for, the expertise, skill, knowledge and judgment of healthcare practitioners. The absence of a warning for a given drug or drug combination in no way should be construed to indicate that the drug or drug combination is safe, effective or appropriate for any given patient. Multum does not assume any responsibility for any aspect of healthcare administered with the aid of information Multum provides. The information contained herein is not intended to cover all possible uses, directions, precautions, warnings, drug interactions, allergic reactions, or adverse effects. If you have questions about the drugs you are taking, check with your doctor, nurse or pharmacist.

Copyright 1996-2013 Cerner Multum, Inc. Version: 11.02. Revision date: 7/24/2012.

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Side Effects Centers
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