Simvastatin

What is Simvastatin

Simvastatin is an oral antilipemic agent which inhibits HMG-CoA reductase. Simvastatin is the methylated form of lovastatin.

Both simvastatin and lovastatin are prodrugs that require hydrolysis for activation. Simvastatin is used in the treatment of primary hypercholesterolemia and is effective in reducing total and LDL-cholesterol as well as plasma triglycerides and apolipoprotein B.

Simvastatin has a high affinity for HMG-CoA reductase. At therapeutic doses of 5 to 80 mg once daily, simvastatin reduces mean LDL concentrations by approximately 26—47%.

Simvastatin was approved by the FDA in December 1991. As a result of the Scandinavian Simvastatin Survival Study, on July 5, 1995, the FDA approved simvastatin for use, in combination with diet, to prevent myocardial infarction in patients with hypercholesterolemia and preexisting coronary artery disease.

In April 2003, the FDA approved simvastatin 40 mg as a starting dose for a broad population of patients at high risk for coronary events, including patients with existing coronary heart disease, diabetes, peripheral vessel disease, or patients with a history of stroke or other cerebrovascular disease

Brand Name

  • FloLipid
  • Zocor

Indications & Dosage

  • atherosclerosis
  • cerebral vasospasm prophylaxis
  • hypercholesterolemia
  • hyperlipoproteinemia
  • hypertriglyceridemia
  • myocardial infarction prophylaxis
  • stroke prophylaxis

For the treatment of hypercholesterolemia, including hyperlipidemia, hyperlipoproteinemia, or hypertriglyceridemia, as an adjunct to dietary control; and for reduction in cardiovascular mortality, including myocardial infarction prophylaxis and stroke prophylaxis

Side Effects

  1. abdominal pain
  2. alopecia
  3. amnesia
  4. anaphylactoid reactions
  5. angioedema
  6. arthralgia
  7. asthenia
  8. atrial fibrillation
  9. chills
  10. cholestasis
  11. cirrhosis
  12. Co-Enzyme Q-10 deficiency
  13. confusion
  14. constipation
  15. depression
  16. diabetes mellitus
  17. diarrhea
  18. dizziness
  19. drowsiness
  20. dyspepsia
  21. dyspnea
  22. edema
  23. elevated hepatic enzymes
  24. eosinophilia
  25. erythema multiforme
  26. fatigue
  27. fever
  28. flatulence
  29. flushing
  30. gastritis
  31. headache
  32. hemolytic anemia
  33. hepatic failure
  34. hepatic necrosis
  35. hepatitis
  36. hyperbilirubinemia
  37. hyperglycemia
  38. immune-mediated necrotizing myopathy
  39. impotence (erectile dysfunction)
  40. infection
  41. insomnia
  42. interstitial lung disease
  43. jaundice
  44. leukopenia
  45. lupus-like symptoms
  46. malaise
  47. memory impairment
  48. muscle cramps
  49. musculoskeletal pain
  50. myalgia
  51. myasthenia
  52. myoglobinuria
  53. myopathy
  54. nausea
  55. pancreatitis
  56. paresthesias
  57. peripheral neuropathy
  58. photosensitivity
  59. pruritus
  60. purpura
  61. rash
  62. rhabdomyolysis
  63. sinusitis
  64. Stevens-Johnson syndrome
  65. thrombocytopenia
  66. toxic epidermal necrolysis
  67. urticaria
  68. vasculitis
  69. vertigo
  70. vomiting

Monitoring Parameters

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

Contraindications

  • alcoholism
  • Asian patients
  • 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

  • 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
  • Bempedoic Acid
  • Bempedoic Acid; Ezetimibe
  • Boceprevir
  • Bortezomib
  • Bosentan
  • Carbamazepine
  • Ceritinib
  • Chlorzoxazone
  • Cimetidine
  • Ciprofloxacin
  • 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
  • Deferasirox
  • Delavirdine
  • Digoxin
  • Diltiazem
  • Dronedarone
  • Duvelisib
  • 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
  • Encorafenib
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Eslicarbazepine
  • Etravirine
  • Everolimus
  • Fedratinib
  • Fenofibrate
  • Fenofibric Acid
  • Flibanserin
  • Fluconazole
  • Fluvoxamine
  • Fosamprenavir
  • Fostamatinib
  • Gemfibrozil
  • Glecaprevir; Pibrentasvir
  • grapefruit juice
  • Hydantoins
  • Hydrochlorothiazide, HCTZ; Propranolol
  • Idelalisib
  • Imatinib
  • Indinavir
  • Isavuconazonium
  • Isoniazid, INH; Pyrazinamide, PZA; Rifampin
  • Isoniazid, INH; Rifampin
  • Itraconazole
  • Ivacaftor
  • Ivosidenib
  • Ketoconazole
  • Lanthanum Carbonate
  • Lefamulin
  • Leflunomide
  • Letermovir
  • Lomitapide
  • Lopinavir; Ritonavir
  • Lovastatin; Niacin
  • Lumacaftor; Ivacaftor
  • Lumacaftor; Ivacaftor
  • Metformin; Repaglinide
  • Mifepristone
  • Mitotane
  • Nefazodone
  • Nelfinavir
  • Netupitant, Fosnetupitant; Palonosetron
  • Nevirapine
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Nicardipine
  • Obeticholic Acid
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Amoxicillin; Rifabutin
  • Oxcarbazepine
  • Pazopanib
  • Perindopril; Amlodipine
  • Pexidartinib
  • Posaconazole
  • Propranolol
  • Protease inhibitors
  • Quinine
  • Raltegravir
  • Ranolazine
  • Red Yeast Rice
  • Repaglinide
  • Ribociclib
  • Ribociclib; Letrozole
  • Rifabutin
  • Rifampin
  • Rifapentine
  • Riluzole
  • Ritonavir
  • Saquinavir
  • Sarilumab
  • Siltuximab
  • Simeprevir
  • Sirolimus
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • St. John’s Wort, Hypericum perforatum
  • Tacrolimus
  • Telaprevir
  • Telbivudine
  • Telithromycin
  • Teriflunomide
  • Tesamorelin
  • Tezacaftor; Ivacaftor
  • Ticagrelor
  • Tipranavir
  • Tocilizumab
  • Tolvaptan
  • Trandolapril; Verapamil
  • Tucatinib
  • Verapamil
  • Voriconazole
  • Warfarin
  • Zafirlukast
  • Zileuton
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