Atipamezole for Animals

Atipamezole

Atipamezole is a selective alpha2-adrenergic antagonist used to reverse the effects of alpha2-agonist sedatives. Its main veterinary application is reversal of medetomidine or dexmedetomidine in dogs, with additional species-specific and extra-label uses. It also has a role in selected intoxications that produce clinically important alpha2-mediated effects.

Group

Alpha-2 adrenergic antagonist

Mechanism of Action

Atipamezole competitively blocks alpha2-adrenoceptors and removes agonist-induced inhibition of norepinephrine release. Restoration of noradrenergic signaling promotes arousal and reverses alpha2-mediated sedation, analgesia and autonomic changes. The degree of reversal depends on receptor occupancy, the agonist involved and concurrent drugs. In amitraz intoxication, antagonism addresses the alpha2 activity of amitraz and its metabolites.

Dose Rates

Dogs

Use / stageDoseRouteScheduleInstructions
Dexmedetomidine reversal0.2 mg/kgIM, IVOnce
Amitraz toxicosis0.05 mg/kgIMEvery 4–6 hReassess for recurrence because amitraz may outlast the antagonist.
Medetomidine reversalReference onlyIMFor 5 mg/mL atipamezole and 1 mg/mL medetomidine, the source describes equal IM volumes. Prior agonist dose determines antagonist amount; retain the concentration-specific ratio.

Cats

Use / stageDoseRouteScheduleInstructions
Dexmedetomidine reversal0.2 mg/kgIM, IVOnce
Medetomidine reversalReference onlyIMFor 5 mg/mL atipamezole and 1 mg/mL medetomidine, the source describes equal IM volumes. Prior agonist dose determines antagonist amount; retain the concentration-specific ratio.

Rabbits

Use / stageDoseRouteScheduleInstructions
Medetomidine reversal0.5 mg/kgIM, SCOnce
Medetomidine reversal0.25 mg/kgIVOnce

Mice

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.1–1 mg/kgIM, IP, IV, SCOnce

Rats

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.1–1 mg/kgIM, IP, IV, SCOnce

Gerbils

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.1–1 mg/kgIM, IP, IV, SCOnce

Hamsters

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.1–1 mg/kgIM, IP, IV, SCOnce

Guinea pigs

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.1–1 mg/kgIM, IP, IV, SCOnce

Cattle

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.02–0.1 mg/kgIVOnceTitrate to effect.

Sheep

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.02–0.1 mg/kgIVOnceTitrate to effect.
Alpha-2 agonist reversal – alternative0.1–0.2 mg/kgIV, IMOnceIf IV, give slowly; observe the delay after dissociative combinations.

Goats

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.02–0.1 mg/kgIVOnceTitrate to effect.
Alpha-2 agonist reversal – alternative0.1–0.2 mg/kgIV, IMOnceIf IV, give slowly; observe the delay after dissociative combinations.

Llamas

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.02–0.1 mg/kgIVOnceTitrate to effect.
Alpha-2 agonist reversal – alternative0.1–0.2 mg/kgIV, IMOnceIf IV, give slowly; observe the delay after dissociative combinations.

Alpacas

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.02–0.1 mg/kgIVOnceTitrate to effect.
Alpha-2 agonist reversal – alternative0.1–0.2 mg/kgIV, IMOnceIf IV, give slowly; observe the delay after dissociative combinations.

Birds

Use / stageDoseRouteScheduleInstructions
Alpha-2 agonist reversal0.5 mg/kgIMOnce

Reptiles

Use / stageDoseRouteScheduleInstructions
Medetomidine reversalReference onlyIMAtipamezole amount 4-5 times the medetomidine dose in the ketamine/medetomidine protocol; reversal may take up to one hour. Do not give IV.

Indications

  • Reversal of medetomidine- or dexmedetomidine-associated sedation and related effects in dogs.
  • Reversal of selected alpha2-agonist effects in cats, horses or other veterinary species using a supported protocol.
  • Adjunctive reversal of clinically significant alpha2-mediated effects in selected amitraz poisoning.
  • Specialist treatment of selected intoxications involving other alpha2 agonists, with agent-specific evidence.

Contraindications

  • Avoid IV administration in reptiles because profound hypotension can occur.
  • Pregnancy, lactation and breeding safety are inadequately established.

Interactions

  • Antagonises alpha-2 agonists; removal of their analgesia may expose untreated pain.
  • Partial alpha-1 effects may interfere with prazosin.

Adverse effects

  • Vomiting, diarrhoea, salivation, tremor and abrupt excitation or aggression.

Toxicity

Overdose usually causes transient excitement, panting, vomiting or tremor. Monitor cardiovascular status.

Preparations

PreparationFormStrengthRoute
Antisedan 5 mg/mL
Strength expressed as atipamezole hydrochloride. Source IV protocols are extralabel and do not change the labelled product route.
Injection5 mg / mLIM

Monitoring and Administration

Provide alternative analgesia before reversing a painful patient. Protect recovering animals from falls and observe for resedation.

After ketamine/tiletamine combinations in small ruminants or camelids, do not reverse too early: allow at least 30, preferably 60, minutes for the dissociative component to diminish.

The equal-volume rule applies only to the specified agonist and antagonist concentrations; it is not a universal volume rule.

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