Rosuvastatin

What is Rosuvastatin

Rosuvastatin is a selective, competitive, HMG-CoA reductase inhibitor. It potently reduces total and LDL cholesterol and lowers plasma triglycerides and apolipoprotein B (Apo-B).

Because of its chemical structure binding sites and relatively greater hydrophilicity, it appears to better penetrate the hepatocyte and bind to HMG-CoA reductase with a higher affinity than other statins.

In adult patients with primary hypercholesterolemia, dose-related LDL-reduction is 45% with 5 mg, 52% with 10mg, 55% with 20 mg, and 63% with 40 mg; doses of 5 to 40 mg/day lower triglycerides by 21% to 43%. Similar to other statins, rosuvastatin produces modest increases in HDL (8% to 12%). 

Brand Names

  • Crestor
  • Ezallor

Indications

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

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

for reduction of elevated total cholesterol, LDL-cholesterol, apolipoprotein B, and triglyceride concentrations, and to increase HDL-cholesterol in patients with primary hypercholesterolemia (heterozygous familial and nonfamilial) or mixed dyslipidemia (Fredrickson types IIa or IIb); or to treat Fredrickson Type IV (hypertriglyceridemia, increased VLDL); or to treat primary dysbetalipoproteinemia (Type III hyperlipoproteinemia)

Side Effects

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

Monitoring Parameters

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

Contraindications

  • alcoholism
  • Asian patients
  • breast-feeding
  • children
  • 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
  • reproductive risk
  • rhabdomyolysis
  • seizure disorder
  • surgery
  • trauma

Interactions

  • Acalabrutinib
  • Amoxicillin; Clarithromycin; Lansoprazole
  • Amoxicillin; Clarithromycin; Omeprazole
  • Antacids
  • Aprepitant, Fosaprepitant
  • Aspirin, ASA; Citric Acid; Sodium Bicarbonate
  • Atazanavir
  • Atazanavir; Cobicistat
  • Bortezomib
  • Calcium Carbonate
  • Calcium Carbonate; Magnesium Hydroxide
  • Calcium Carbonate; Risedronate
  • Calcium Carbonate; Simethicone
  • Capmatinib
  • Cimetidine
  • Clarithromycin
  • Clofarabine
  • Cobicistat
  • Colchicine
  • Colchicine; Probenecid
  • Cyclosporine
  • Daclatasvir
  • Daptomycin
  • Darolutamide
  • Darunavir
  • Darunavir; Cobicistat
  • Darunavir; Cobicistat; Emtricitabine; Tenofovir alafenamide
  • Dasabuvir; Ombitasvir; Paritaprevir; Ritonavir
  • Drospirenone; Ethinyl Estradiol
  • Drospirenone; Ethinyl Estradiol; Levomefolate
  • Elagolix
  • Elagolix; Estradiol; Norethindrone acetate
  • Elbasvir; Grazoprevir
  • Elexacaftor; tezacaftor; ivacaftor
  • Eltrombopag
  • Eluxadoline
  • Elvitegravir
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Alafenamide
  • Elvitegravir; Cobicistat; Emtricitabine; Tenofovir Disoproxil Fumarate
  • Erythromycin
  • Erythromycin; Sulfisoxazole
  • Ethinyl Estradiol
  • Ethinyl Estradiol; Desogestrel
  • Ethinyl Estradiol; Ethynodiol Diacetate
  • Ethinyl Estradiol; Etonogestrel
  • Ethinyl Estradiol; Levonorgestrel
  • Ethinyl Estradiol; Levonorgestrel; Ferrous bisglycinate
  • Ethinyl Estradiol; Levonorgestrel; Folic Acid; Levomefolate
  • Ethinyl Estradiol; Norelgestromin
  • Ethinyl Estradiol; Norethindrone
  • Ethinyl Estradiol; Norethindrone Acetate
  • Ethinyl Estradiol; Norethindrone Acetate; Ferrous fumarate
  • Ethinyl Estradiol; Norethindrone; Ferrous fumarate
  • Ethinyl Estradiol; Norgestimate
  • Ethinyl Estradiol; Norgestrel
  • Etravirine
  • Fenofibrate
  • Fenofibric Acid
  • Fosamprenavir
  • Fostamatinib
  • Gemfibrozil
  • Glecaprevir; Pibrentasvir
  • Indinavir
  • Itraconazole
  • Lanthanum Carbonate
  • Ledipasvir; Sofosbuvir
  • Leflunomide
  • Letermovir
  • Lopinavir; Ritonavir
  • Lovastatin; Niacin
  • Mestranol; Norethindrone
  • Nelfinavir
  • Niacin, Niacinamide
  • Niacin; Simvastatin
  • Norgestrel
  • Obeticholic Acid
  • Ombitasvir; Paritaprevir; Ritonavir
  • Omeprazole; Sodium Bicarbonate
  • Oritavancin
  • Osimertinib
  • Ponatinib
  • Raltegravir
  • Red Yeast Rice
  • Regorafenib
  • Ritonavir
  • Rolapitant
  • Safinamide
  • Saquinavir
  • Segesterone Acetate; Ethinyl Estradiol
  • Simeprevir
  • Sodium Bicarbonate
  • Sofosbuvir; Velpatasvir
  • Sofosbuvir; Velpatasvir; Voxilaprevir
  • Tacrolimus
  • Tafamidis
  • Tedizolid
  • Telaprevir
  • Telbivudine
  • Telithromycin
  • Teriflunomide
  • Tipranavir
  • Tolvaptan
  • Warfarin
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