Chemistry:Tolazoline

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Short description: An α2 adrenoceptor antagonist
Tolazoline
Tolazoline.svg
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
IV
ATC code
Identifiers
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
Chemical and physical data
FormulaC10H12N2
Molar mass160.220 g·mol−1
3D model (JSmol)
  (verify)


Tolazoline is a non-selective competitive α-adrenergic receptor antagonist.[1] It is a vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis). It has also been used (in conjunction with sodium nitroprusside) successfully as an antidote to reverse the severe peripheral vasoconstriction which can occur as a result of overdose with certain 5-HT2A agonist drugs such as 25I-NBOMe,[2] DOB and Bromodragonfly (prolonged severe vasoconstriction can lead to gangrene if untreated).[3][4]

It is however most commonly used in veterinary medicine, to reverse xylazine-induced sedation.[5][6]

References

  1. Aronson, J. K. (2016). Meyler's side effects of drugs : the international encyclopedia of adverse drug reactions and interactions. Amsterdam: Elsevier Science. ISBN 978-0-444-53717-1. OCLC 927102885. "Tolazoline is an α2 adrenoceptor antagonist that increases skin blood flow in healthy subjects and has been used to relieve acute vasospasm." 
  2. "Human Metabolome Database: Showing metabocard for Tolazoline (HMDB0014935)". https://hmdb.ca/metabolites/HMDB0014935. 
  3. "Diffuse vascular spasm associated with 4-bromo-2,5-dimethoxyamphetamine ingestion". JAMA 249 (11): 1477–9. March 1983. doi:10.1001/jama.1983.03330350053028. PMID 6827726. 
  4. "[Bromo-dragon fly--life-threatening drug. Can cause tissue necrosis as demonstrated by the first described case]" (in sv). Läkartidningen 105 (16): 1199–200. 2008. PMID 18522262. 
  5. "Anticonvulsant drugs and analeptic agents". Veterinary pharmacology and therapeutics. Ames: Iowa State University Press. 2001. pp. 378–9. ISBN 0-8138-1743-9. https://books.google.com/books?id=2CUbc0RXvb8C. Retrieved 8 September 2008. 
  6. "Principles of sedation, analgesia and premedication". Veterinary anaesthesia. Philadelphia: W.B. Saunders. 2001. pp. 90–1. ISBN 0-7020-2035-4.