Lovastatin

Lovastatin Brand Names- Altoprev | Mevacor

What is Lovastatin

Lovastatin is an oral antilipemic agent produced by fermentation of Aspergillus terreus.

Lovastatin represents the first HMG-CoA reductase inhibitor to be introduced.

Lovastatin was developed as a prodrug to concentrate active drug in the liver during first-pass circulation.

Simvastatin is also a prodrug, but pravastatin and fluvastatin are not.

Lovastatin (Mevacor) doses of 10—80 mg/day, given in 1—2 divided doses, result in mean LDL reductions ranging from 21—42%.

Lovastatin (Mevacor) was approved by the FDA for the treatment of hypercholesterolemia in August 1987.

Since that time, its indications have been expanded to include slowing the progression of coronary atherosclerosis, primary prevention (myocardial infarction prophylaxis), and stroke prophylaxis.

In the AFCAPS/TexCAPS primary prevention study, lovastatin reduced the risk for the first acute major coronary event in adult men and women with average total and LDL cholesterol levels and below average HDL cholesterol levels.

After an average of 5.2 years, lovastatin reduced the incidence of first acute major coronary event by 37%, fatal or nonfatal myocardial infarction by 40%, unstable angina by 32%, and coronary revascularization procedures by 33%, respectively.

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.

Several generic equivalents for Mevacor were approved in December, 2001. Advicor (see separate monograph), a combination product for lovastatin and niacin, was approved by the FDA in December, 2001.

The FDA approved an extended-release formulation of lovastatin, Altocor, on June 26, 2002. The proprietary name for Altocor lovastatin extended-release tablets was changed to Aloprev by the FDA on July 21, 2004. An FDA advisory committee voted 20 to 3 against marketing lovastatin 20 mg as an OTC product during January 2005.

Although favorable results were reported by the manufacturer-sponsored CUSTOM study in regard to OTC lovastatin use, the FDA advisory committee raised concerns of inappropriate self-selection (self-diagnosis) by the study participants.

In December 2007, an FDA advisory panel again voted 10 to 2 against the OTC marketing of lovastatin citing concern that patients would not be able to properly follow instructions to safely use lovastatin without a prescription.

Indications

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

For the treatment of hypercholesterolemia, including hyperlipidemia, hyperlipoproteinemia, or hypertriglyceridemia, as an adjunct to dietary control

Side Effects

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

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
  • pregnancy
  • renal disease
  • renal failure
  • renal impairment
  • rhabdomyolysis
  • seizure disorder
  • surgery
  • trauma

Interactions

  • Aliskiren; Amlodipine
  • Aliskiren; Amlodipine; Hydrochlorothiazide, HCTZ
  • Amiodarone
  • Amlodipine
  • Amlodipine; Atorvastatin
  • Amlodipine; Benazepril
  • Amlodipine; Celecoxib
  • Amlodipine; Hydrochlorothiazide, HCTZ; Olmesartan
  • Amlodipine; Hydrochlorothiazide, HCTZ; Valsartan
  • Amlodipine; Olmesartan
  • Amlodipine; Telmisartan
  • Amlodipine; Valsartan
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Amprenavir
  • Aprepitant, Fosaprepitant
  • Atazanavir
  • Atazanavir; Cobicistat
  • Barbiturates
  • Boceprevir
  • Bortezomib
  • Bosentan
  • Carbamazepine
  • Ceritinib
  • Cilostazol
  • Cimetidine
  • Clarithromycin
  • Cobicistat
  • Colchicine
  • Colchicine; Probenecid
  • Conivaptan
  • Crizotinib
  • Cyclosporine
  • Dabigatran
  • Dabrafenib
  • Daclatasvir
  • Danazol
  • Daptomycin
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Delavirdine
  • Diltiazem
  • Dronedarone
  • Duvelisib
  • Efavirenz
  • Efavirenz; Emtricitabine; Tenofovir
  • Efavirenz; Lamivudine; Tenofovir Disoproxil Fumarate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Encorafenib
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Ethanol
  • Etravirine
  • Everolimus
  • Fedratinib
  • Fenofibrate
  • Fenofibric Acid
  • Fluconazole
  • Fosamprenavir
  • Fosphenytoin
  • Fostemsavir
  • Gemfibrozil
  • Glecaprevir; Pibrentasvir
  • grapefruit juice
  • Idelalisib
  • Imatinib
  • Indinavir
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Isradipine
  • Itraconazole
  • Ivacaftor
  • Ivosidenib
  • Ketoconazole
  • Lanthanum Carbonate
  • Lefamulin
  • Leflunomide
  • Letermovir
  • Lomitapide
  • Lopinavir; Ritonavir
  • Lovastatin; Niacin
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Mefenamic Acid
  • Mifepristone
  • Mitotane
  • Nefazodone
  • Nelfinavir
  • Nevirapine
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicardipine
  • Nilotinib
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oritavancin
  • Oxcarbazepine
  • Pazopanib
  • Perindopril; Amlodipine
  • Phenytoin
  • Posaconazole
  • Protease inhibitors
  • Quetiapine
  • Quinine
  • Raltegravir
  • Ranolazine
  • Red Yeast Rice
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Ritonavir
  • Saquinavir
  • Sarilumab
  • Siltuximab
  • Simeprevir
  • Sirolimus
  • St. John’s Wort, Hypericum perforatum
  • Tacrolimus
  • Telaprevir
  • Telbivudine
  • Telithromycin
  • Teriflunomide
  • Tezacaftor; Ivacaftor
  • Ticagrelor
  • Tipranavir
  • Tocilizumab
  • Tolvaptan
  • Trandolapril; Verapamil
  • Tucatinib
  • Verapamil
  • Voriconazole
  • Warfarin
  • Zafirlukast
  • Zileuton
You cannot copy content of this page