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User:Mr. Ibrahem/Bisoprolol

< User:Mr. Ibrahem
Mr. Ibrahem/Bisoprolol
Clinical data
Trade namesZebeta, Concor, Selecta, others
AHFS/Drugs.comMonograph
MedlinePlusa693024
License data
Pregnancy
category
  • AU: C
Routes of
administration		By mouth
Drug classBeta blocker[1]
Legal status
Legal status
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability>90%
Protein binding30%[2]
Metabolism50% liver, CYP2D6, CYP3A4[4]
Elimination half-life10–12 hours[3]
Identifiers
  • (RS)-1-{4-[(2-Isopropoxyethoxy)methyl]phenoxy}-
    3-(isopropylamino)propan-2-ol
Chemical and physical data
FormulaC18H31NO4
Molar mass325.449 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O(c1ccc(cc1)COCCOC(C)C)CC(O)CNC(C)C
  • InChI=1S/C18H31NO4/c1-14(2)19-11-17(20)13-23-18-7-5-16(6-8-18)12-21-9-10-22-15(3)4/h5-8,14-15,17,19-20H,9-13H2,1-4H3 checkY
  • Key:VHYCDWMUTMEGQY-UHFFFAOYSA-N checkY
  (verify)

Bisoprolol, marketed under the tradename Zebeta among others, is a medication of the beta blocker type most commonly used for heart diseases.[1] This specifically includes high blood pressure, chest pain from not enough blood flow to the heart, and heart failure.[1][5] It is taken by mouth.[1]

Common side effects include headache, feeling tired, diarrhea, and swelling in the legs.[1] More severe side effects include worsening asthma, blocking the ability to recognize low blood sugar, and worsening heart failure.[7] There are concerns that use during pregnancy may be harmful to the baby.[8] Bisoprolol is in the beta blocker family of medications, specifically the β1 selective type.[1]

Bisoprolol was patented in 1976 and approved for medical use in 1986.[9] It is on the World Health Organization's List of Essential Medicines.[10] Bisoprolol is available as a generic medication.[1] The wholesale cost in the developing world is about US$3–5 per month.[11] In the UK it costs the NHS just less than £1 per month as of 2020.[12] In the United States, as of 2015, it costs about $25–50 a month.[13] In 2017, it was the 268th most commonly prescribed medication in the United States, with more than one million prescriptions.[14][15]


References

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  1. ^ a b c d e f g h i "Bisoprolol Fumarate". The American Society of Health-System Pharmacists. Archived from the original on 21 December 2016. Retrieved 8 December 2016.
  2. ^ Bühring KU, Sailer H, Faro HP, Leopold G, Pabst J, Garbe A (1986). "Pharmacokinetics and metabolism of bisoprolol-14C in three animal species and in humans". J. Cardiovasc. Pharmacol. 8 Suppl 11: S21–8. doi:10.1097/00005344-198511001-00004. PMID 2439794.
  3. ^ Leopold G (1986). "Balanced pharmacokinetics and metabolism of bisoprolol". J. Cardiovasc. Pharmacol. 8 Suppl 11: S16–20. doi:10.1097/00005344-198511001-00003. PMID 2439789.
  4. ^ Yuji Horikiri; Takehiko Suzuki; Masakazu Mizobe (March 1998). "Pharmacokinetics and metabolism of bisoprolol enantiomers in humans". Journal of Pharmaceutical Sciences. 87 (3): 289–294. doi:10.1021/js970316d. PMID 9523980.
  5. ^ a b "Bisoprolol 2.5mg/5mg/10mg film coated tablet - Summary of Product Characteristics (SPC) - (eMC)". www.medicines.org.uk. 18 February 2014. Archived from the original on 20 December 2016. Retrieved 14 December 2016.
  6. ^ "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 29 October 2020. Retrieved 26 August 2020.
  7. ^ "Bisoprolol - FDA prescribing information, side effects and uses". www.drugs.com. Archived from the original on 21 December 2016. Retrieved 14 December 2016.
  8. ^ "Bisoprolol (Zebeta) Use During Pregnancy". www.drugs.com. Archived from the original on 21 December 2016. Retrieved 14 December 2016.
  9. ^ Fischer, Janos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 461. ISBN 9783527607495. Archived from the original on 2017-09-08.
  10. ^ World Health Organization (2019). World Health Organization model list of essential medicines: 21st list 2019. Geneva: World Health Organization. hdl:10665/325771. WHO/MVP/EMP/IAU/2019.06. License: CC BY-NC-SA 3.0 IGO.
  11. ^ "Bisoprolol". International Drug Price Indicator Guide. Archived from the original on 13 October 2018. Retrieved 8 December 2016.
  12. ^ BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 165. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  13. ^ Hamilton, Richart (2015). Tarascon Pocket Pharmacopoeia 2015 Deluxe Lab-Coat Edition. Jones & Bartlett Learning. p. 151. ISBN 9781284057560.
  14. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  15. ^ "Bisoprolol Fumarate - Drug Usage Statistics". ClinCalc. Archived from the original on 11 April 2020. Retrieved 11 April 2020.
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