User:Mr. Ibrahem/Rosuvastatin

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Mr. Ibrahem/Rosuvastatin
Clinical data
Pronunciation/rˈsvəstætɪn/ roh-SOO-və-stat-in
Trade namesCrestor, Rosulip, Zuvamor, others
Other namesRosuvastatin calcium (USAN US)
AHFS/Drugs.comMonograph
MedlinePlusa603033
License data
Pregnancy
category
Routes of
administration
By mouth (tablets)
Legal status
Legal status
  • AU: S4 (Prescription only)
  • UK: POM (Prescription only)
  • US: ℞-only
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability20%[2][3]
Protein binding88%[2][3]
MetabolismLiver: CYP2C9 (major) and CYP2C19-mediated; ~10% metabolized[2][3]
MetabolitesN-desmethyl rosuvastatin (major; 1/6–1/9 of rosuvastatin activity)[4]
Elimination half-life19 hours[2][3]
ExcretionFeces (90%)[2][3]
Identifiers
  • (3R,5S,6E)-7-[4-(4-Fluorophenyl)-2-(N-methylmethanesulfonamido)-6-(propan-2-yl)pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid
Chemical and physical data
FormulaC22H28FN3O6S
Molar mass481.539 g·mol−1
3D model (JSmol)
  • OC(=O)C[C@H](O)C[C@H](O)\C=C\c1c(C(C)C)nc(N(C)S(=O)(=O)C)nc1c2ccc(F)cc2
  • InChI=1S/C22H28FN3O6S/c1-13(2)20-18(10-9-16(27)11-17(28)12-19(29)30)21(14-5-7-15(23)8-6-14)25-22(24-20)26(3)33(4,31)32/h5-10,13,16-17,27-28H,11-12H2,1-4H3,(H,29,30)/b10-9+/t16-,17-/m1/s1 ☒N
  • Key:BPRHUIZQVSMCRT-VEUZHWNKSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Rosuvastatin, sold under the trade name Crestor among others, is a statin medication, used to prevent cardiovascular disease in those at high risk and treat abnormal lipids.[3] It is recommended to be used together with dietary changes, exercise, and weight loss.[3] It is taken by mouth.[3]

Common side effects include abdominal pain, nausea, headaches, and muscle pains.[3] Serious side effects may include rhabdomyolysis, liver problems, and diabetes.[3] Use during pregnancy may harm the baby.[3] Like all statins, rosuvastatin works by inhibiting HMG-CoA reductase, an enzyme found in the liver that plays a role in producing cholesterol.[3]

Rosuvastatin was patented in 1991, and approved for medical use in the United States in 2003.[3][6] It is available as a generic medication.[3] In the United States, the wholesale cost per dose is less than US$0.15 as of 2018.[7] In the United Kingdom, it costs the NHS one to two pounds for one month's treatment as of 2020.[8] In 2017, it was the 39th most commonly prescribed medication in the United States, with more than 19 million prescriptions.[9][10]

References[edit]

  1. ^ a b "Rosuvastatin Use During Pregnancy". Drugs.com. 27 September 2019. Archived from the original on 30 November 2020. Retrieved 14 March 2020.
  2. ^ a b c d e Aggarwal, RK; Showkathali, R (June 2013). "Rosuvastatin calcium in acute coronary syndromes". Expert Opinion on Pharmacotherapy. 14 (9): 1215–1227. doi:10.1517/14656566.2013.789860. PMID 23574635. Archived from the original on 29 August 2021. Retrieved 29 November 2019.
  3. ^ a b c d e f g h i j k l m n "Rosuvastatin Calcium Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists (AHFS). Archived from the original on 24 December 2018. Retrieved 24 December 2018.
  4. ^ "Crestor- rosuvastatin calcium tablet, film coated". DailyMed. 9 November 2018. Archived from the original on 25 September 2020. Retrieved 14 March 2020.
  5. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 20 September 2020. Retrieved 9 September 2020.
  6. ^ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 473. ISBN 9783527607495. Archived from the original on 24 December 2018. Retrieved 24 December 2018.
  7. ^ "NADAC as of 2018-12-19". Centers for Medicare and Medicaid Services (CMS). Archived from the original on 19 December 2018. Retrieved 22 December 2018.
  8. ^ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 217. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  9. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 18 March 2020. Retrieved 14 March 2020.
  10. ^ "Rosuvastatin - Drug Usage Statistics". ClinCalc. 23 December 2019. Archived from the original on 11 April 2020. Retrieved 11 April 2020.