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Tolazoline
Systematic (IUPAC) name
2-benzyl-4,5-dihydro-1H-imidazole
Identifiers
CAS number 59-98-3
ATC code C04AB02 M02AX02
PubChem 5504
DrugBank APRD00170
Chemical data
Formula C 10H12N2  
Mol. mass 160.216 g/mol
Pharmacokinetic data
Bioavailability  ?
Metabolism  ?
Half life  ?
Excretion  ?
Therapeutic considerations
Pregnancy cat.  ?
Legal status
Routes IV

Tolazoline is a non-selective competitive α-adrenergic receptor antagonist. It is a vasodilator that is used to treat spasms of peripheral blood vessels (as in acrocyanosis). It has also been used 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 LSD, DOB and Bromodragonfly and can lead to gangrene if untreated.[1][2]

It is however most commonly used in veterinary medicine, to reverse xylazine-induced sedation.[3][4]

References

  1. ^ Bowen JS, Davis GB, Kearney TE, Bardin J. Diffuse vascular spasm associated with 4-bromo-2,5-dimethoxyamphetamine ingestion. Journal of the American Medical Association 1983 Mar 18;249(11):1477-9. PMID 6827726
  2. ^ Thorlacius K, Borna C, Personne M. Bromo-dragon fly--life-threatening drug. Can cause tissue necrosis as demonstrated by the first described case. (Swedish) Lakartidningen. 2008 Apr 16-22;105(16):1199-200. PMID 18522262
  3. ^ 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. http://books.google.com/books?id=2CUbc0RXvb8C.   Retrieved September 8, 2008 through Google Book Search.
  4. ^ 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.   Retrieved September 8, 2008 through Google Book Search.
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