Mr. Ibrahem/Labetalol
Clinical data
Pronunciation/ləˈbɛtəlɔːl/
Trade namesNormodyne, Trandate, others
AHFS/Drugs.comMonograph
MedlinePlusa685034
License data
Pregnancy
category
  • C
    One of few drugs used for PIH
Routes of
administration
By mouth, intravenous
Drug classBeta blocker[1]
Legal status
Legal status
  • AU: S4 (Prescription only)
  • In general: ℞ (Prescription only)
Pharmacokinetic data
Bioavailability25%
Protein binding50%
MetabolismLiver pass metabolism,
Onset of actionWithin 10 min (iv)[2]
Elimination half-lifeTablet: 6-8 hours; IV: 5.5 hours
Duration of actionUp to 6 hrs (iv)[2]
ExcretionExcreted in urine, not removed by hemodialysis
Identifiers
  • (RS)-2-Hydroxy-5-[1-hydroxy-2-[(4-phenylbutan-2-yl)amino]ethyl]benzamide
Chemical and physical data
FormulaC19H24N2O3
Molar mass328.412 g·mol−1
3D model (JSmol)
ChiralityRacemic mixture
  • O=C(c1cc(ccc1O)C(O)CNC(C)CCc2ccccc2)N
  • InChI=1S/C19H24N2O3/c1-13(7-8-14-5-3-2-4-6-14)21-12-18(23)15-9-10-17(22)16(11-15)19(20)24/h2-6,9-11,13,18,21-23H,7-8,12H2,1H3,(H2,20,24) checkY
  • Key:SGUAFYQXFOLMHL-UHFFFAOYSA-N checkY
  (verify)

Labetalol is a medication used to treat high blood pressure and in long term management of angina.[1][5] This includes essential hypertension, hypertensive emergencies, and hypertension of pregnancy.[5] In essential hypertension it is generally less preferred than a number of other blood pressure medications.[1] It can be given by mouth or by injection into a vein.[1]

Common side effects include low blood pressure with standing, dizziness, feeling tired, and nausea.[1] Serious side effects may include low blood pressure, liver problems, heart failure, and bronchospasm.[1] Use appears safe in the latter part of pregnancy and it is not expected to cause problems during breastfeeding.[5][6] It works by blocking the activation of both α-receptors and β-receptors.[7]

Labetalol was patented in 1966 and came into medical use in 1977.[8] It is available as a generic medication.[5] A month supply of labetalol at 200mg three times daily, in the United Kingdom, costs the NHS less than £15 as of 2020.[5] In the United States the same dose for a month costs just less than US$24.[9] In 2017, it was the 211th most commonly prescribed medication in the United States, with more than two million prescriptions.[10][11]

References

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  1. ^ a b c d e f g "Labetalol Monograph for Professionals". Drugs.com. American Society of Health-System Pharmacists. Archived from the original on 15 February 2021. Retrieved 15 February 2021.
  2. ^ a b Cite error: The named reference EMCrit2024 was invoked but never defined (see the help page).
  3. ^ Cite error: The named reference MSF2020 was invoked but never defined (see the help page).
  4. ^ Cite error: The named reference WHO2020DDD was invoked but never defined (see the help page).
  5. ^ a b c d e BNF (80 ed.). BMJ Group and the Pharmaceutical Press. September 2020 – March 2021. p. 160-161. ISBN 978-0-85711-369-6.{{cite book}}: CS1 maint: date format (link)
  6. ^ "Labetalol Use During Pregnancy". Drugs.com. Archived from the original on 29 November 2020. Retrieved 11 March 2019.
  7. ^ Ritter, Professor of Clinical Pharmacology Guy's King's and St Thomas's Medical Schools James M.; Flower, Rod J.; Henderson, Graeme; Loke, Yoon Kong; MacEwan, David; Rang, Humphrey P. (2020). "15. Noradrenergic transmission". Rang & Dale's Pharmacology. Elsevier. p. 210. ISBN 978-0-7020-7448-6. Archived from the original on 2021-08-28. Retrieved 2021-03-01.
  8. ^ Fischer, Jnos; Ganellin, C. Robin (2006). Analogue-based Drug Discovery. John Wiley & Sons. p. 463. ISBN 9783527607495. Archived from the original on 2018-12-24. Retrieved 2019-03-01.
  9. ^ "Labetalol Prices, Coupons & Patient Assistance Programs". Drugs.com. Archived from the original on 15 February 2021. Retrieved 15 February 2021.
  10. ^ "The Top 300 of 2020". ClinCalc. Archived from the original on 12 February 2021. Retrieved 11 April 2020.
  11. ^ "Labetalol - Drug Usage Statistics". ClinCalc. Archived from the original on 11 April 2020. Retrieved 11 April 2020.