Fluvastatin

Fluvastatin Brand Names- Lescol | Lescol XL

What is Fluvastatin

Fluvastatin is an oral antilipemic agent indicated for the treatment of primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb).

Fluvastatin doses of 20—40 mg once daily result in mean LDL reductions ranging from 22—25%; whereas, the extended-release formulation (Lescol XL 80 mg) reduces LDL by about 36%.

Fluvastatin is a HMG-CoA reductase inhibitor and was the first to be synthetically prepared. It has some similarities to lovastatin, simvastatin, and pravastatin, but it is structurally distinct, resulting in unique biopharmaceutic properties.

Purported advantages of fluvastatin over the other HMG-CoA reductase inhibitors include short half-life with no active metabolites, extensive protein binding, and minimal CSF penetration.

These criteria suggest fluvastatin may be less likely to cause systemic adverse reactions than the other agents in this class.

Fluvastatin is primarily used as an adjunct to diet to lower cholesterol and triglyceride levels associated with primary hypercholesterolemia and mixed dyslipidemia (Fredrickson types IIa and IIb).

Based on results from the Lipoprotein and Coronary Atherosclerosis Study,

the FDA approved fluvastatin for slowing of progression of coronary atherosclerosis in patients with coronary artery disease.

The FDA also approved Lescol and Lescol XL for secondary prevention of coronary events in patients with coronary heart disease based on the findings of the LIPS trial.

The LIPS trial demonstrated that initiation of fluvastatin 80 mg/day within days following PCI significantly reduces the risk of major cardiac events (cardiac death, nonfatal MI, coronary revascularization).

Additionally, a large retrospective study demonstrated that continuation of statin therapy provides an ongoing reduction in all-cause mortality in patients with and without known coronary heart disease (CHD), with the greatest risk reduction among patients with a baseline LDL-C >= 190 mg/dL and patients initiated on higher efficacy statins (i.e., simvastatin, pravastatin, or lovastatin 80 mg/day; atorvastatin >= 20 mg/day; rosuvastatin >= 10 mg/day).

Among patients with a proportion of days covered (PDC) of >= 90%, determined by the number of statin prescriptions dispensed during the time between the first statin prescription and the end of follow up, there was a 45% and 51% lower mortality risk in the primary (patients without known CHD) and secondary (patients with known CHD) prevention groups, respectively, compared to patients with a PDC <= 10%.

The mean length of follow up was 4 and 5 years in the primary and secondary prevention groups, respectively, with a maximum length of follow up of 9.5 years.

Fluvastatin (Lescol) was approved by the FDA in December 1993.

An extended-release product (Lescol XL) was approved by the FDA in October 2000.

Indications

  1. hypercholesterolemia
  2. hyperlipoproteinemia
  3. hypertriglyceridemia
  4. myocardial infarction prophylaxis
  5. stroke prophylaxis

For the treatment of hypercholesterolemia, including hyperlipidemia, hyperlipoproteinemia, or hypertriglyceridemia, as an adjunct to dietary controll, for the purpose of reducing the risk of cardiovascular events (e.g., myocardial infarction prophylaxis, stroke prophylaxis)

Side Effects

  1. abdominal pain
  2. alopecia
  3. amnesia
  4. anaphylactoid reactions
  5. angioedema
  6. anorexia
  7. anxiety
  8. arthralgia
  9. arthropathy
  10. atrial fibrillation
  11. chills
  12. cholestasis
  13. cirrhosis
  14. Co-Enzyme Q-10 deficiency
  15. confusion
  16. constipation
  17. cranial nerve palsies
  18. depression
  19. diabetes mellitus
  20. diarrhea
  21. dizziness
  22. drowsiness
  23. dysarthria
  24. dysesthesia
  25. dysgeusia
  26. dyspepsia
  27. dysphagia
  28. dyspnea
  29. elevated hepatic enzymes
  30. eosinophilia
  31. erythema multiforme
  32. fatigue
  33. fever
  34. flatulence
  35. flushing
  36. gynecomastia
  37. headache
  38. hemolytic anemia
  39. hepatic failure
  40. hepatic necrosis
  41. hepatitis
  42. hyperglycemia
  43. hypertension
  44. hypoesthesia
  45. immune-mediated necrotizing myopathy
  46. impotence (erectile dysfunction)
  47. infection
  48. influenza
  49. insomnia
  50. jaundice
  51. leukopenia
  52. libido decrease
  53. lupus-like symptoms
  54. malaise
  55. memory impairment
  56. muscle cramps
  57. muscle paralysis
  58. myalgia
  59. myasthenia
  60. myoglobinuria
  61. myopathy
  62. nausea
  63. pancreatitis
  64. paresthesias
  65. peripheral edema
  66. peripheral neuropathy
  67. pharyngitis
  68. photosensitivity
  69. pruritus
  70. purpura
  71. rash
  72. rhabdomyolysis
  73. sinusitis
  74. Stevens-Johnson syndrome
  75. syncope
  76. thrombocytopenia
  77. toxic epidermal necrolysis
  78. tremor
  79. urticaria
  80. vasculitis
  81. vertigo
  82. vomiting
  83. weakness

Monitoring Parameters

  • creatine phosphokinase (CPK)
  • LFTs
  • serum cholesterol profile

Contraindications

  • alcoholism
  • breast-feeding
  • children
  • cholestasis
  • contraception requirements
  • diabetes mellitus
  • electrolyte imbalance
  • endocrine disease
  • females
  • geriatric
  • hepatic disease
  • hepatic encephalopathy
  • hepatitis
  • hypotension
  • hypothyroidism
  • infants
  • infection
  • jaundice
  • myopathy
  • organ transplant
  • pregnancy
  • renal disease
  • renal failure
  • renal impairment
  • rhabdomyolysis
  • seizure disorder
  • surgery
  • trauma

Interactions

  • Amiodarone
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Omeprazole
  • Atazanavir
  • Atazanavir; Cobicistat
  • Bortezomib
  • Cholestyramine
  • Cimetidine
  • Clarithromycin
  • Cobicistat
  • Colchicine
  • Colchicine; Probenecid
  • Cyclosporine
  • Daclatasvir
  • Daptomycin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Deferasirox
  • Delavirdine
  • Diclofenac
  • Diclofenac; Misoprostol
  • Digoxin
  • Dronabinol
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • Eltrombopag
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Esomeprazole
  • Esomeprazole; Naproxen
  • Ethanol
  • Etravirine
  • Everolimus
  • Fenofibrate
  • Fenofibric Acid
  • Fluconazole
  • Fluoxetine
  • Fluoxetine; Olanzapine
  • Fluvoxamine
  • food
  • Fosamprenavir
  • Fosphenytoin
  • Fostemsavir
  • Gemfibrozil
  • Glecaprevir; Pibrentasvir
  • Glimepiride
  • Glimepiride; Pioglitazone
  • Glimepiride; Rosiglitazone
  • Glyburide
  • Glyburide; Metformin
  • Imatinib
  • Indinavir
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Ivacaftor
  • Lanthanum Carbonate
  • Leflunomide
  • Lesinurad
  • Lesinurad; Allopurinol
  • Letermovir
  • Lopinavir; Ritonavir
  • Lovastatin; Niacin
  • Lumacaftor; Ivacaftor
  • Meloxicam
  • Mifepristone
  • Nelfinavir
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole
  • Omeprazole; Amoxicillin; Rifabutin
  • Omeprazole; Sodium Bicarbonate
  • Oritavancin
  • Phenytoin
  • Raltegravir
  • Ranitidine
  • Red Yeast Rice
  • Regorafenib
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Rucaparib
  • Saquinavir
  • Simeprevir
  • Sirolimus
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Sulfinpyrazone
  • Sulfonamides
  • Tacrolimus
  • Telaprevir
  • Telbivudine
  • Telithromycin
  • Terbinafine
  • Teriflunomide
  • Tezacaftor; Ivacaftor
  • Tipranavir
  • Tolvaptan
  • Vemurafenib
  • Voriconazole
  • Warfarin
  • Zafirlukast