Norepinephrine (medication)

From WikiProjectMed
Jump to navigation Jump to search
Norepinephrine
Norepinephrine.svg
Norepinephrine ball-and-stick model.png
Names
Trade namesLevarterenol, Levophed, Norepin, other
Other namesNoradrenaline
(R)-(–)-Norepinephrine
l-1-(3,4-Dihydroxyphenyl)-2-aminoethanol
Clinical data
Pregnancy
category
  • AU: B3
  • US: C (Risk not ruled out)
Routes of
use
Intravenous
Defined daily dose6 mg[1]
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
  (verify)

Norepinephrine, also known as noradrenaline, is a medication used to treat people with very low blood pressure.[2] It is the typical medication used in sepsis if low blood pressure does not improve following intravenous fluids.[3] It is the same molecule as the hormone and neurotransmitter norepinephrine.[2] 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][4] It is available as a generic medication.[2] The wholesale cost in the developing world as of 2015 is about 0.42 USD per vial of four milligrams.[5] In the United Kingdom this amount costs the NHS about 4.40 pounds.[6]

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.[7][8]

Dosage

The defined daily dose is 6 mg by infusion.[1] It is generally started at 2 to 4 mcg/min with titration up to 25 mcg/min.[9] The dose may be increased every two to five minutes.[9]

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.[9]

Side effects

Side effects may include anxiety, headache, shortness of breath, and an irregular heart rate.[9]

If it enters into soft tissues rather than a vein tissue death may occur.[2] 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.[9] The phentolamine should be mixed with 10 to 15 ml of normal saline.[2]

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.[10] 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.[11] Norepinephrine acts more on alpha receptors than the beta receptors.[12]

Names

Norepinephrine is the INN while noradrenaline is the BAN.

References

  1. 1.0 1.1 "WHOCC - ATC/DDD Index". www.whocc.no. Retrieved 9 September 2020.
  2. 2.00 2.01 2.02 2.03 2.04 2.05 2.06 2.07 2.08 2.09 2.10 2.11 "Norepinephrine Bitartrate". The American Society of Health-System Pharmacists. Archived from the original on 26 March 2017. Retrieved 26 March 2017.
  3. Latifi, Rifat (2016). Surgical Decision Making: Beyond the Evidence Based Surgery. Springer. p. 67. ISBN 9783319298245. Archived from the original on 2017-03-27.
  4. Encyclopedia of the Neurological Sciences. Academic Press. 2014. p. 224. ISBN 9780123851581. Archived from the original on 2017-03-27.
  5. "Norepinephrine". mshpriceguide.org. Archived from the original on 26 March 2017. Retrieved 26 March 2017.
  6. British national formulary : BNF 69 (69 ed.). British Medical Association. 2015. p. 145. ISBN 9780857111562.
  7. 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).
  8. 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.
  9. 9.0 9.1 9.2 9.3 9.4 "Norepinephrine - WikEM". wikem.org. Retrieved 9 September 2020.
  10. I Moore, Joanne (6 December 2012). Pharmacology (3 ed.). Springer Science and Business Media. p. 39. ISBN 9781468405248. Retrieved 19 November 2017.
  11. "CV Physiology | Circulating Catecholamines". cvphysiology.com. Retrieved 2019-02-27.
  12. 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.

External links

Identifiers: