Norepinephrine

This article is about the medication. For the neurotransmitter, see norepinephrine (neurotransmitter).
Norepinephrine
Names
Trade namesLevarterenol, Levophed, Norepin, other
Other namesNoradrenaline
(R)-(–)-Norepinephrine
l-1-(3,4-Dihydroxyphenyl)-2-aminoethanol
IUPAC name
  • 4-[(1R)-2-amino-1-hydroxyethyl]benzene-1,2-diol
Clinical data
Drug classAdrenergic agonist (alpha and beta)[1]
Main usesLow blood pressure[1]
Side effectsHeadache, slow heart rate, anxiety[1]
WHO AWaReUnlinkedWikibase error: ⧼unlinkedwikibase-error-statements-entity-not-set⧽
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
    Routes of
    use    		Intravenous
    Defined daily dose6 mg[2]
    Typical dose2 to 80 mcg/min (adults)[3][4]
    External links
    AHFS/Drugs.comMonograph
    Physiological data
    Target tissuesSystem-wide
    Receptorsα1, α2, β1, β3
    AgonistsSympathomimetic drugs, clonidine, isoprenaline
    AntagonistsTricyclic antidepressants, Beta blockers, antipsychotics
    MetabolismMAO-A; COMT
    Legal
    License data
    Legal status
    Pharmacokinetics
    MetabolismMAO-A; COMT
    ExcretionUrine (84–96%)
    Chemical and physical data
    FormulaC8H11NO3
    Molar mass169.180 g·mol−1
    3D model (JSmol)
    Density1.397±0.06 g/cm3
    Melting point217 °C (423 °F) (decomposes)
    Boiling point442.6 °C (828.7 °F) ±40.0°C
    SMILES
    • Oc1ccc(cc1O)[C@@H](O)CN
    InChI
    • InChI=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 checkY
    • Key:SFLSHLFXELFNJZ-QMMMGPOBSA-N checkY

    Norepinephrine, also known as noradrenaline, is a medication used to treat people with very low blood pressure.[1] It is the typical medication used in sepsis if low blood pressure does not improve following intravenous fluids.[5] It is the same molecule as the hormone and neurotransmitter norepinephrine.[1] It is given by slow injection into a vein.[1]

    Common side effects include headache, slow heart rate, and anxiety.[1] Other side effects include an irregular heartbeat.[1] If it leaks out of the vein at the site it is being given, norepinephrine can result in limb ischemia.[1] If leakage occurs the use of phentolamine in the area affected may improve outcomes.[1] Norepinephrine works by binding and activating alpha adrenergic receptors.[1]

    Norepinephrine was discovered in 1946 and was approved for medical use in the United States in 1950.[1][6] It is available as a generic medication.[1] The wholesale cost in the developing world as of 2015 is about 0.42 USD per vial of four milligrams.[7] In the United Kingdom this amount costs the NHS about 4.40 pounds.[8]

    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.[9][10]

    Dosage

    It is generally started at 2 to 15 mcg/min with titration up to 80 to 250 mcg/min.[3][4] The dose may be increased every two to five minutes.[3] If more than 15 mcg/min is required, vasopressin is than often started at 0.03 units per minute (1.8 units/hr).[4][11]

    In children it may be used at 0.05 to 0.1 mcg/kg/min and may be increased up to 2 mcg/kg/min.[3]

    The defined daily dose is 6 mg by infusion.[2]

    • A vial of norepinephrine
      A vial of norepinephrine

    Side effects

    Side effects may include anxiety, headache, shortness of breath, and an irregular heart rate.[3]

    If it enters into soft tissues rather than a vein tissue death may occur.[1] This situation may be treated with phentolamine 0.1 to 0.2 mg/kg (up to 10 mg) injected under the skin at the site this occurred.[3] The phentolamine should be mixed with 10 to 15 ml of normal saline.[1]

    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.[12] 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.[13] Norepinephrine acts more on alpha receptors than the beta receptors.[14]

    Names

    Norepinephrine is the INN while noradrenaline is the BAN.

    References

    1. 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 "Norepinephrine Bitartrate". The American Society of Health-System Pharmacists. Archived from the original on 26 March 2017. Retrieved 26 March 2017.
    2. 1 2 "WHOCC - ATC/DDD Index". www.whocc.no. Archived from the original on 1 December 2020. Retrieved 9 September 2020.
    3. 1 2 3 4 5 6 "Norepinephrine - WikEM". wikem.org. Archived from the original on 26 August 2017. Retrieved 9 September 2020.
    4. 1 2 3 "UpToDate". www.uptodate.com. Archived from the original on 13 October 2022. Retrieved 25 May 2023.
    5. ↑ Latifi, Rifat (2016). Surgical Decision Making: Beyond the Evidence Based Surgery. Springer. p. 67. ISBN 9783319298245. Archived from the original on 2017-03-27.
    6. ↑ Encyclopedia of the Neurological Sciences. Academic Press. 2014. p. 224. ISBN 9780123851581. Archived from the original on 2017-03-27.
    7. ↑ "Norepinephrine". mshpriceguide.org. Archived from the original on 26 March 2017. Retrieved 26 March 2017.
    8. ↑ British national formulary : BNF 69 (69 ed.). British Medical Association. 2015. p. 145. ISBN 9780857111562.
    9. ↑ Rhodes, Andrew; Evans, Laura E (March 2017). "Surviving Sepsis Campaign: International Guidelines for Management of Sepsis and Septic Shock 2016". Critical Care Medicine. 45 (3): 486–552. doi:10.1097/CCM.0000000000002255. hdl:10281/267577. PMID 28098591. We recommend norepinephrine as the first-choice vasopressor (strong recommendation, moderate quality of evidence).
    10. ↑ De Backer D, Biston P, Devriendt J, Madl C, Chochrad D, Aldecoa C, Brasseur A, Defrance P, Gottignies P, Vincent JL (March 2010). "Comparison of dopamine and norepinephrine in the treatment of shock". The New England Journal of Medicine. 362 (9): 779–89. doi:10.1056/nejmoa0907118. PMID 20200382.
    11. ↑ "BC Sepsis Network Guidelines" (PDF). Archived (PDF) from the original on 20 October 2023. Retrieved 13 October 2023.
    12. ↑ I Moore, Joanne (6 December 2012). Pharmacology (3 ed.). Springer Science and Business Media. p. 39. ISBN 9781468405248. Archived from the original on 28 August 2021. Retrieved 19 November 2017.
    13. ↑ "CV Physiology | Circulating Catecholamines". cvphysiology.com. Archived from the original on 2019-02-28. Retrieved 2019-02-27.
    14. ↑ Sacha, Pollard; Stephenie, B Edwin; Cesar, Alaniz (July 2015). "Vasopressor and Inotropic Management Of Patients With Septic Shock". Physical Therapy. 40 (7): 449–450. PMC 4495871. PMID 26185405.
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