Tolazoline

Tolazoline
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration		IV
ATC code
Identifiers
  • 2-Benzyl-4,5-dihydro-1H-imidazole
CAS Number
PubChem CID
IUPHAR/BPS
DrugBank
ChemSpider
UNII
KEGG
ChEBI
ChEMBL
CompTox Dashboard (EPA)
ECHA InfoCard100.000.408 Edit this at Wikidata
Chemical and physical data
FormulaC10H12N2
Molar mass160.220 g·mol−1
3D model (JSmol)
  • N\1=C(\NCC/1)Cc2ccccc2
  • InChI=1S/C10H12N2/c1-2-4-9(5-3-1)8-10-11-6-7-12-10/h1-5H,6-8H2,(H,11,12) checkY
  • Key:JIVZKJJQOZQXQB-UHFFFAOYSA-N checkY
  (verify)
For other uses, see Adrenergics.

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)". hmdb.ca. Retrieved 2022-02-03.
  3. ^ Bowen JS, Davis GB, Kearney TE, Bardin J (March 1983). "Diffuse vascular spasm associated with 4-bromo-2,5-dimethoxyamphetamine ingestion". JAMA. 249 (11): 1477–9. doi:10.1001/jama.1983.03330350053028. PMID 6827726.
  4. ^ Thorlacius K, Borna C, Personne M (2008). "[Bromo-dragon fly--life-threatening drug. Can cause tissue necrosis as demonstrated by the first described case]". Läkartidningen (in Swedish). 105 (16): 1199–200. PMID 18522262.
  5. ^ Boothe DM (2001). "Anticonvulsant drugs and analeptic agents". In Adams HR (ed.). Veterinary pharmacology and therapeutics. Ames: Iowa State University Press. pp. 378–9. ISBN 0-8138-1743-9. Retrieved 8 September 2008.
  6. ^ Hall LW, Clarke KW, Trim CM (2001). "Principles of sedation, analgesia and premedication". Veterinary anaesthesia. Philadelphia: W.B. Saunders. pp. 90–1. ISBN 0-7020-2035-4.