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Maropitant

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Maropitant
Clinical data
AHFS/Drugs.comInternational Drug Names
Routes of
administration
Oral, subcutaneous
ATCvet code
Legal status
Legal status
  • Veterinary use only
Identifiers
  • (7R,8S)-N-[(5-tert-Butyl-2-methoxyphenyl)methyl]-7-[di(phenyl)methyl]-1-azabicyclo[2.2.2]octan-8-amine
PubChem CID
ChemSpider
UNII
CompTox Dashboard (EPA)
Chemical and physical data
FormulaC32H40N2O
Molar mass468.67 g/mol g·mol−1
3D model (JSmol)
  • O=C(O)C(O)(CC(=O)O)CC(=O)O.O.O(c1ccc(cc1CN[C@@H]2[C@@H](N3CCC2CC3)C(c4ccccc4)c5ccccc5)C(C)(C)C)C
  • InChI=1S/C32H40N2O.C6H8O7.H2O/c1-32(2,3)27-15-16-28(35-4)26(21-27)22-33-30-25-17-19-34(20-18-25)31(30)29(23-11-7-5-8-12-23)24-13-9-6-10-14-24;7-3(8)1-6(13,5(11)12)2-4(9)10;/h5-16,21,25,29-31,33H,17-20,22H2,1-4H3;13H,1-2H2,(H,7,8)(H,9,10)(H,11,12);1H2/t30-,31-;;/m0../s1 checkY
  • Key:PGVSXRHFXJOMGW-YBZGWEFGSA-N checkY
  (verify)

Maropitant (trade name Cerenia in the US and other countries), used as maropitant citrate (USAN), is a neurokinin (NK1) receptor antagonist, which was developed by Zoetis specifically for the treatment of motion sickness and vomiting in dogs. It was approved by the FDA in 2007 for use in dogs,[1][2] and more recently has also been approved for use in cats.[3]

Maropitant also has anti-nociceptive (analgesic) properties. In a 2012 study, parenteral maropitant decreased the minimum alveolar concentration (MAC) of sevoflurane in a pain-response model.[citation needed] Epidural administration had no effect. It has also been shown to decrease the MAC of sevoflurane in a cat spay and dog spay model. Whether it has analgesic properties in awake animals remains to be proven, but anecdotal evidence indicates that it is being used for analgesia by many veterinarians. Its mode of action is through inhibition of substance P binding at the NK1 receptor.

See also

References

  1. ^ "Cerenia (maropitant citrate) Injectable Solution, Dogs" (pdf). Retrieved 2011-04-19.
  2. ^ Package Insert for Cerenia at Pfizer Animal Health (full detailed drug information)
  3. ^ "Cerenia (maropitant citrate) information at Pfizer Animal Health".

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