pharmacopeia
GET
/api/v1/drug/fluvastatin
2D structure
(E,3S,5R)-7-[3-(4-fluorophenyl)-1-propan-2-ylindol-2-yl]-3,5-dihydroxyhept-6-enoic acid
SMILES CC(C)N1C2=CC=CC=C2C(=C1/C=C/[C@@H](C[C@@H](CC(=O)O)O)O)C3=CC=C(C=C3)F
InChIKey FJLGEFLZQAZZCD-JUFISIKESA-N

Mechanism of action

Sourced from openFDA

Fluvastatin sodium 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.

Hydroxymethylglutaryl-CoA Reductase

Indications

Sourced from openFDA
  • 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.ICD-10: E78.00

Contraindications

Sourced from openFDA
  • Hypersensitivity to any component of this medication ( 4 ) Active liver disease or unexplained, persistent elevations in serum transaminases ( 4 , 5.3 ) Women who are pregnant or may become pregnant ( 4 , 8.1 ) Nursing mothers ( 4 , 8.3 ) 4.1 Hypersensitivity to any Component of This Medication Fluvastatin capsules are contraindicated in patients with hypersensitivity to any component of this medication. 4.2 Active Liver Disease Fluvastatin capsules are contraindicated in patients with active liver disease or unexplained, persistent elevations in serum transaminases [see Warnings and Precautions ( 5.3 )] .contraindicated

Dosage & administration

Sourced from openFDA

Dose range: 20 mg to 80 mg/day ( 2.1 ) Fluvastatin capsules can be taken with or without food. ( 2.1 ) Do not open fluvastatin capsules prior to administration ( 2.1 ) Adults: the recommended starting dose is 40 mg to 80 mg (administered as one fluvastatin capsule, 40 mg twice daily) ( 2.2 ) Do not take two fluvastatin capsules, 40 mg at one time Children with heterozygous familial hypercholesterolemia (ages 10 to 16, inclusive): the recommended starting dose is fluvastatin capsule, 20 mg once daily ( 2.3 ) 2.1 General Dosing Information Dose range: 20 mg to 80 mg/day. Fluvastatin capsules can be administered orally as a single dose, with or without food. Do not open fluvastatin capsules prior to administration. Do not take two fluvastatin capsules, 40 mg 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, 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 Dyslipidemia Adult patients can be started on fluvastatin capsules.

Warnings & precautions

Sourced from openFDA

Skeletal muscle effects (e.g., myopathy and rhabdomyolysis): Risks increase with advanced age (≥ 65), uncontrolled hypothyroidism, renal impairment, and combination use with cyclosporine,or gemfibrozil. Advise patients to promptly report to their physician unexplained and/or persistent muscle pain, tenderness, or weakness and discontinue fluvastatin if myopathy is diagnosed or suspected. ( 5.1 , 8.5 , 8.7 ) Patients should be advised to report promptly any symptoms of myopathy. Fluvastatin capsules therapy should be discontinued if myopathy is diagnosed or suspected ( 5.1 ) Immune-Mediated Necrotizing Myopathy (IMNM): There have been rare reports of IMNM, an autoimmune myopathy, associated with statin use. IMNM is characterized by: proximal muscle weakness and elevated serum creatine kinase, which persist despite discontinuation of statin treatment; positive anti-HMG CoA reductase antibody; muscle biopsy showing necrotizing myopathy; and improvement with immunosuppressive agents. ( 5.2 ) Liver enzyme abnormalities: Persistent elevations in hepatic transaminases can occur. Check liver enzyme tests before initiating therapy and as clinically indicated thereafter ( 5.3 ) 5.1 Skeletal Muscle Rhabdomyolysis with acute renal failure secondary to myoglobinuria have been reported with fluvastatin capsules and other drugs in this class. Fluvastatin capsules 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.

Adverse reactions

Sourced from openFDA

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 ( 5.1 ) ]. Liver Enzyme Abnormalities [ see Warnings and Precautions ( 5.3 ) ]. Most frequent adverse reactions (rate ≥ 2% and > placebo) are: headache, dyspepsia, myalgia, abdominal pain and nausea ( 6.1 ) To report SUSPECTED ADVERSE REACTIONS, contact Teva at 1-888-838-2872 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch. 6.1 Clinical Studies Experience in Adult Patients Because clinical studies on fluvastatin capsules are conducted in varying study populations and study designs, the frequency of adverse reactions observed in the clinical studies of fluvastatin capsules 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 fluvastatin capsules placebo-controlled clinical trials database of 2326 patients treated with fluvastatin capsules 1 (age range 18 to 75 years, 44% women, 94% Caucasians, 4% Blacks, 2% other ethnicities) with a median treatment duration of 24 weeks, 3.4% of patients on fluvastatin capsules and 2.3% patients on placebo discontinued due to adverse reactions regardless of causality.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Pregnancy Category X Fluvastatin sodium is contraindicated in women who are or may become pregnant [see Contraindications ( 4 )]. 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 fluvastatin sodium during pregnancy. Rare reports of congenital anomalies have been received following intrauterine exposure to other statins. In a review 2 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.

Pharmacokinetics

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

Overdosage

Sourced from openFDA

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 ( 5 )]. 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 fluvastatin tablets in infants up to 3 years of age. In one case, increased serum CPK values were noted.

Approval history

Sourced from openFDA
  • Oct 6, 2000NDANDA021192Sandoz
  • Apr 11, 2012ANDAANDA090595Mylan Pharms Inc
  • Jun 12, 2012ANDAANDA078407Teva Pharms
  • Jan 27, 2016ANDAANDA079011Teva Pharms Usa
  • Apr 26, 2021ANDAANDA209397Beijing

FAERS reports

View JSON
Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
7,471 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Myalgia88012%
  2. 2Dizziness5607.5%
  3. 3Nausea5607.5%
  4. 4Diarrhoea5357.2%
  5. 5Dyspnoea5076.8%
  6. 6Fatigue5026.7%
  7. 7Asthenia4536.1%
  8. 8Headache4516.0%
  9. 9Fall4476.0%
  10. 10Arthralgia4435.9%
  11. 11Vomiting4305.8%
  12. 12Pyrexia4145.5%
  13. 13Pruritus3915.2%
  14. 14Malaise3684.9%
  15. 15Abdominal Pain3574.8%

Literature

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Recent PubMed references pinned to Fluvastatin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 74 ClinicalTrials.gov registrations naming Fluvastatin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Pharmacogenomics

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CPIC-curated drug–gene pairs for Fluvastatin. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.

Frequently asked questions

How does Fluvastatin work?
Fluvastatin sodium 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.
What is Fluvastatin used for?
According to FDA labeling, Fluvastatin carries indications including: 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.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Fluvastatin?
Fluvastatin is classified as HMG CoA reductase inhibitors, HMG-CoA Reductase Inhibitor, Hydroxymethylglutaryl-CoA Reductase Inhibitors, Decreased Cholesterol Synthesis.
What are the brand names for Fluvastatin?
Fluvastatin is marketed under brand names including Lescol.
What are the contraindications for Fluvastatin?
Fluvastatin labeling lists contraindications including: Hypersensitivity to any component of this medication ( 4 ) Active liver disease or unexplained, persistent elevations in serum transaminases ( 4 , 5.3 ) Women who are pregnant or may become pregnant ( 4 , 8.1 ) Nursing mothers ( 4 , 8.3 ) 4.1 Hypersensitivity to any Component of This Medication Fluvastatin capsules are contraindicated in patients with hypersensitivity to any component of this medication. 4.2 Active Liver Disease Fluvastatin capsules are contraindicated in patients with active liver disease or unexplained, persistent elevations in serum transaminases [see Warnings and Precautions ( 5.3 )] .. Always consult the full prescribing information and a clinician.
Note. Data for fluvastatin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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