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Atipamezole
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Atipamezole
Atipamezole , sold under the brand name Antisedan among others, is a synthetic α2 adrenergic receptor antagonist used for the reversal of the sedative and analgesic effects of dexmedetomidine and medetomidine in dogs. Its reversal effect works by competing with the sedative for α2-adrenergic receptors and displacing them. It is mainly used in veterinary medicine, and while it is only licensed for dogs and for intramuscular use, it has been used intravenously, as well as in cats and other animals (intravenous use in cats and dogs is not recommended due to the potential for cardiovascular collapse. This occurs due to profound hypotension caused by reversal of the alpha 1 effects while the reflex bradycardia is still in effect.). There is a low rate of side effects, largely due to atipamezole's high specificity for the α2-adrenergic receptor. Atipamezole has a very quick onset, usually waking an animal up within 5 to 10 minutes.[medical citation needed]
It was originally released in 1996. It is available in as a generic medication.
Atipamezole was first sold in 1996 as a reversal agent for medetomidine. Although developed specifically for medetomidine it also reverses other alpha2 adrenergic receptor agonists. While it reverses both the sedative and analgesic (pain-relieving) effects of dexmedetomidine, atipamezole may not entirely reverse the cardiovascular depression that dexmedetomidine causes.
Atipamezole is licensed in the United States for intramuscular injection (IM) in dogs; it is, however, used off-label in cats, rabbits, and farm animals such as horses and cows, as well as in zoo medicine for reptiles (including tortoises, turtles, and alligators), armadillos, hippopotamuses, giraffes, okapi, and others. It has been given intravenously (IV), subcutaneously, intraperitoneally and, in red-eared sliders, intranasally. Atipamezole has mostly displaced yohimbine and tolazoline in small animal medicine but not large animal medicine.
Atipamezole has also been used as an antidote for various toxicities in dogs. For example, the anti-tick medication amitraz is commonly ingested by dogs who eat their anti-tick collars. Amitraz works by the same mechanism as dexmedetomidine and is thus easily reversed by atipamezole. Atipamezole also reverses the hypotension caused by tizanidine (a muscle relaxant) toxicity, and relieves toxicity from decongestants such as ephedrine and pseudoephedrine.
Intramuscular administration of atipamezole in the dog has quick absorption with the drug's half-life elimination being an hour following IM administration. In the dog atipamezole is metabolised in the liver by hydroxylation.
Atipamezole is sold at 5 mg/mL for ease of use: 5 times as much atipamezole as medetomidine is needed for full reversal, and because medetomidine is sold as 1 mg/mL, 1 mL of atipamezole reverses 1 mL of medetomidine. When the enantiomerically pure version of medetomidine (dexmedetomidine) was released, it was sold at 0.5 mg/mL, because it was twice as strong as medetomidine. As such, 1 mL of atipamezole also reverses 1 mL of dexmedetomidine.
Atipamezole is not recommended for animals that are pregnant, lactating, or slated for breeding.
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Atipamezole
Atipamezole , sold under the brand name Antisedan among others, is a synthetic α2 adrenergic receptor antagonist used for the reversal of the sedative and analgesic effects of dexmedetomidine and medetomidine in dogs. Its reversal effect works by competing with the sedative for α2-adrenergic receptors and displacing them. It is mainly used in veterinary medicine, and while it is only licensed for dogs and for intramuscular use, it has been used intravenously, as well as in cats and other animals (intravenous use in cats and dogs is not recommended due to the potential for cardiovascular collapse. This occurs due to profound hypotension caused by reversal of the alpha 1 effects while the reflex bradycardia is still in effect.). There is a low rate of side effects, largely due to atipamezole's high specificity for the α2-adrenergic receptor. Atipamezole has a very quick onset, usually waking an animal up within 5 to 10 minutes.[medical citation needed]
It was originally released in 1996. It is available in as a generic medication.
Atipamezole was first sold in 1996 as a reversal agent for medetomidine. Although developed specifically for medetomidine it also reverses other alpha2 adrenergic receptor agonists. While it reverses both the sedative and analgesic (pain-relieving) effects of dexmedetomidine, atipamezole may not entirely reverse the cardiovascular depression that dexmedetomidine causes.
Atipamezole is licensed in the United States for intramuscular injection (IM) in dogs; it is, however, used off-label in cats, rabbits, and farm animals such as horses and cows, as well as in zoo medicine for reptiles (including tortoises, turtles, and alligators), armadillos, hippopotamuses, giraffes, okapi, and others. It has been given intravenously (IV), subcutaneously, intraperitoneally and, in red-eared sliders, intranasally. Atipamezole has mostly displaced yohimbine and tolazoline in small animal medicine but not large animal medicine.
Atipamezole has also been used as an antidote for various toxicities in dogs. For example, the anti-tick medication amitraz is commonly ingested by dogs who eat their anti-tick collars. Amitraz works by the same mechanism as dexmedetomidine and is thus easily reversed by atipamezole. Atipamezole also reverses the hypotension caused by tizanidine (a muscle relaxant) toxicity, and relieves toxicity from decongestants such as ephedrine and pseudoephedrine.
Intramuscular administration of atipamezole in the dog has quick absorption with the drug's half-life elimination being an hour following IM administration. In the dog atipamezole is metabolised in the liver by hydroxylation.
Atipamezole is sold at 5 mg/mL for ease of use: 5 times as much atipamezole as medetomidine is needed for full reversal, and because medetomidine is sold as 1 mg/mL, 1 mL of atipamezole reverses 1 mL of medetomidine. When the enantiomerically pure version of medetomidine (dexmedetomidine) was released, it was sold at 0.5 mg/mL, because it was twice as strong as medetomidine. As such, 1 mL of atipamezole also reverses 1 mL of dexmedetomidine.
Atipamezole is not recommended for animals that are pregnant, lactating, or slated for breeding.
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