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Tolazoline

Chemical compound

Chemical compound

| Drugs.com =

| elimination_half-life =

Tolazoline is a non-selective competitive α2-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 (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 receptor agonist drugs such as 25I-NBOMe, DOB, and Bromodragonfly.

History

Tolazoline was first used in the 1980s as an alternative reversal agent for xylazine.

Use

Tolazoline is used in large animal medicine to reverse the effects of α2-adrenergic receptor agonists, typically xylazine. Large doses of intravenous tolazoline in cattle can cause hyperesthesia and opisthotonos and other routes such as intramusucular are preferred.

Pharmacology

Tolazoline binds to the a2 adrenergic receptor at a ratio of 4:1, the lowest of all a2 adrenergic receptor antagonists. Tolazoline activates the imidazoline receptor.

IV tolazoline has slow elimination and a large distribution in the horse.

References

References

  1. (2016). "Meyler's side effects of drugs : the international encyclopedia of adverse drug reactions and interactions". Elsevier Science.
  2. "Human Metabolome Database: Showing metabocard for Tolazoline (HMDB0014935)".
  3. (March 1983). "Diffuse vascular spasm associated with 4-bromo-2,5-dimethoxyamphetamine ingestion". JAMA.
  4. (2008). "[Bromo-dragon fly--life-threatening drug. Can cause tissue necrosis as demonstrated by the first described case]". Läkartidningen.
  5. "Veterinary Anesthesia and Analgesia, The 6th Edition of Lumb and Jones". Wiley Blackwell.
  6. (2013). "Pharmacokinetics and pharmacodynamic effects of tolazoline following intravenous administration to horses". The Veterinary Journal.
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alpha-1-blockers alpha-2-blockers disulfiram-like-drugs imidazolines vasodilators veterinary-drugs
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