Norepinephrine (medication) explained

Verifiedrevid:595681188
Drug Name:Norepinephrine
Width:180
Tradename:Levarterenol, Levophed, Norepin, other
Dailymedid:Norepinephrine
Licence Us:Norepinephrine
Pregnancy Au:B3
Pregnancy Us:C
Routes Of Administration:Intravenous
Atc Prefix:C01
Atc Suffix:CA03
Source Tissues:Locus coeruleus
sympathetic nervous system; adrenal medulla
Target Tissues:System-wide
Receptors:α1, α2, β1, β3
Agonists:Sympathomimetic drugs, clonidine, isoprenaline
Antagonists:Tricyclic antidepressants, Beta blockers, antipsychotics
Legal Au:S4
Legal Ca:OTC
Legal Uk:POM
Legal Us:Rx-only
Metabolism:MAO-A
COMT
Excretion:Urine (84–96%)
Index2 Label:as salt
Cas Number:51-41-2
Pubchem:439260
Iuphar Ligand:505
Drugbank:DB00368
Chemspiderid:388394
Unii:X4W3ENH1CV
Kegg:D00076
Kegg2:D05206
Chebi:18357
Chembl:1437
Synonyms:Noradrenaline
(R)-(–)-Norepinephrine
l-1-(3,4-Dihydroxyphenyl)-2-aminoethanol
3,4,β-Trihydroxyphenethylamine
Iupac Name:4-[(1''R'')-2-amino-1-hydroxyethyl]benzene-1,2-diol
C:8
H:11
N:1
O:3
Smiles:Oc1ccc(cc1O)[C@@H](O)CN
Stdinchi:1S/C8H11NO3/c9-4-8(12)5-1-2-6(10)7(11)3-5/h1-3,8,10-12H,4,9H2/t8-/m0/s1
Stdinchikey:SFLSHLFXELFNJZ-QMMMGPOBSA-N
Density:1.397±0.06
Melting Point:217
Melting Notes:(decomposes)
Boiling Point:442.6
Boiling Notes:±40.0°C

Norepinephrine, also known as noradrenaline, is a medication used to treat people with very low blood pressure. It is the typical medication used in sepsis if low blood pressure does not improve following intravenous fluids.[1] It is the same molecule as the hormone and neurotransmitter norepinephrine. It is given by slow injection into a vein.[2]

Common side effects include headache, slow heart rate, and anxiety.[2] Other side effects include an irregular heartbeat.[2] If it leaks out of the vein at the site it is being given, norepinephrine can result in limb ischemia.[2] If leakage occurs the use of phentolamine in the area affected may improve outcomes.[2] Norepinephrine works by binding and activating alpha adrenergic receptors.[2]

Norepinephrine was discovered in 1946 and was approved for medical use in the United States in 1950.[2] [3] It is available as a generic medication.[2]

Medical uses

Norepinephrine is used mainly as a sympathomimetic drug to treat people in vasodilatory shock states such as septic shock and neurogenic shock, while showing fewer adverse side-effects compared to dopamine treatment.[4] [5]

Pharmacology

Mechanism of action

It stimulates α1 and α2 adrenergic receptors to cause blood vessel contraction, thus increases peripheral vascular resistance and resulted in increased blood pressure. This effect also reduces the blood supply to gastrointestinal tract and kidneys. Norepinephrine acts on beta-1 adrenergic receptors, causing increase in heart rate and cardiac output.[6] However, the elevation in heart rate is only transient, as baroreceptor response to the rise in blood pressure as well as enhanced vagal tone ultimately result in a sustained decrease in heart rate.[7] Norepinephrine acts more on alpha receptors than the beta receptors.[8]

Pharmacokinetics

Norepinephrine does not cross the blood–brain barrier under normal circumstances and hence is a peripherally selective drug.[9]

Society and culture

Names

Norepinephrine is the INN while noradrenaline is the BAN.

External links

Notes and References

  1. Book: Latifi R . Surgical Decision Making: Beyond the Evidence Based Surgery. 2016. Springer. 9783319298245. 67. en. live. https://web.archive.org/web/20170327165820/https://books.google.ca/books?id=2Z8YDAAAQBAJ&pg=PA67. 2017-03-27.
  2. Web site: Norepinephrine Bitartrate. The American Society of Health-System Pharmacists. 26 March 2017. live. https://web.archive.org/web/20170326230032/https://www.drugs.com/monograph/norepinephrine-bitartrate.html. 26 March 2017.
  3. Book: Encyclopedia of the Neurological Sciences. 2014. Academic Press. 9780123851581. 224. en. live. https://web.archive.org/web/20170327165724/https://books.google.ca/books?id=hfjSVIWViRUC&pg=RA1-PA224. 2017-03-27.
  4. Rhodes A, Evans LE, Alhazzani W, Levy MM, Antonelli M, Ferrer R, Kumar A, Sevransky JE, Sprung CL, Nunnally ME, Rochwerg B, Rubenfeld GD, Angus DC, Annane D, Beale RJ, Bellinghan GJ, Bernard GR, Chiche JD, Coopersmith C, De Backer DP, French CJ, Fujishima S, Gerlach H, Hidalgo JL, Hollenberg SM, Jones AE, Karnad DR, Kleinpell RM, Koh Y, Lisboa TC, Machado FR, Marini JJ, Marshall JC, Mazuski JE, McIntyre LA, McLean AS, Mehta S, Moreno RP, Myburgh J, Navalesi P, Nishida O, Osborn TM, Perner A, Plunkett CM, Ranieri M, Schorr CA, Seckel MA, Seymour CW, Shieh L, Shukri KA, Simpson SQ, Singer M, Thompson BT, Townsend SR, Van der Poll T, Vincent JL, Wiersinga WJ, Zimmerman JL, Dellinger RP . 6 . Surviving Sepsis Campaign: International Guidelines for Management of Sepsis and Septic Shock: 2016 . Critical Care Medicine . 45 . 3 . 486–552 . March 2017 . 28098591 . 10.1097/CCM.0000000000002255 . free . We recommend norepinephrine as the first-choice vasopressor (strong recommendation, moderate quality of evidence). . 52827184 . 10281/267577 .
  5. De Backer D, Biston P, Devriendt J, Madl C, Chochrad D, Aldecoa C, Brasseur A, Defrance P, Gottignies P, Vincent JL . 6 . Comparison of dopamine and norepinephrine in the treatment of shock . The New England Journal of Medicine . 362 . 9 . 779–789 . March 2010 . 20200382 . 10.1056/nejmoa0907118 . free .
  6. Book: Moore JI . Pharmacology. 6 December 2012. Springer Science and Business Media. 9781468405248. 39. 3rd . 19 November 2017.
  7. Web site: Klabunde RE . 7 December 2022 . Circulating Catecholamines . CV Physiology . 2019-02-27.
  8. Pollard S, Edwin SB, Alaniz C . Vasopressor and Inotropic Management Of Patients With Septic Shock . P & T . 40 . 7 . 438–450 . July 2015 . 26185405 . 4495871 .
  9. Froese L, Dian J, Gomez A, Unger B, Zeiler FA . The cerebrovascular response to norepinephrine: A scoping systematic review of the animal and human literature . Pharmacol Res Perspect . 8 . 5 . e00655 . October 2020 . 32965778 . 10.1002/prp2.655 . 7510331 .