Details
Stereochemistry | ABSOLUTE |
Molecular Formula | C32H40N2O.C6H8O7 |
Molecular Weight | 660.7963 |
Optical Activity | UNSPECIFIED |
Defined Stereocenters | 2 / 2 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
OC(=O)CC(O)(CC(O)=O)C(O)=O.COC1=CC=C(C=C1CN[C@H]2C3CCN(CC3)[C@H]2C(C4=CC=CC=C4)C5=CC=CC=C5)C(C)(C)C
InChI
InChIKey=XDZPFSKCXRGRIO-PNXDLZEOSA-N
InChI=1S/C32H40N2O.C6H8O7/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)/t30-,31-;/m0./s1
DescriptionSources: https://www.drugs.com/pro/cerenia.htmlCurator's Comment: Description was created based on several sources, including
http://cerenia.com/
http://www.fda.gov/downloads/AnimalVeterinary/ucm062313.pdf
Sources: https://www.drugs.com/pro/cerenia.html
Curator's Comment: Description was created based on several sources, including
http://cerenia.com/
http://www.fda.gov/downloads/AnimalVeterinary/ucm062313.pdf
Maropitant (trade name Cerenia in the U.S. and other countries), used as maropitant citrate 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, and was later approved for use in cats. Maropitant also has anti-nociceptive (analgesic) properties. Maropitant inhibits binding of substance P to NK-1 receptors. Substance P is an emetogen experimentally, and is found endogenously, along with NK-1 receptors, in the emetic center, chemoreceptor trigger zone, and in vagal afferent nerves in the gastrointestinal tract.
CNS Activity
Sources: https://www.drugs.com/pro/cerenia.html
Curator's Comment: Maropitant, a lipophilic compound, crosses the blood-brain barrier http://veterinarymedicine.dvm360.com/maropitants-pharmacokinetics-and-pharmacology
Maropitant is a neurokinin (NK1) receptor antagonist that blocks the pharmacological action of substance P in the central nervous system (CNS).
Originator
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
---|---|---|---|
Target ID: Q5DUB3 Gene ID: 403815.0 Gene Symbol: TACR1 Target Organism: Canis lupus familiaris (Dog) (Canis familiaris) |
Conditions
Condition | Modality | Targets | Highest Phase | Product |
---|---|---|---|---|
Sources: http://cerenia.com/ |
Preventing | Cerenia Approved UseCerenia is indicated for the prevention of acute vomiting and the prevention of vomiting due to motion sickness in dogs. Launch Date2007 |
PubMed
Title | Date | PubMed |
---|---|---|
The pharmacokinetics of maropitant, a novel neurokinin type-1 receptor antagonist, in dogs. | 2007 Aug |
|
The neurokinin-1 antagonist activity of maropitant, an antiemetic drug for dogs, in a gerbil model. | 2007 Aug |
|
The anti-emetic efficacy of maropitant (Cerenia) in the treatment of ongoing emesis caused by a wide range of underlying clinical aetiologies in canine patients in Europe. | 2007 Feb |
|
Efficacy of maropitant for treatment and prevention of emesis caused by intravenous infusion of cisplatin in dogs. | 2007 Jan |
|
Efficacy of injectable maropitant (Cerenia) in a randomized clinical trial for prevention and treatment of cisplatin-induced emesis in dogs presented as veterinary patients. | 2007 Mar |
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[New antiemetics: maropitant citrate]. | 2007 May 15 |
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Efficacy of maropitant for preventing vomiting associated with motion sickness in dogs. | 2007 Sep 29 |
|
Safety and efficacy of injectable and oral maropitant, a selective neurokinin 1 receptor antagonist, in a randomized clinical trial for treatment of vomiting in dogs. | 2008 Dec |
|
Comparative efficacy of maropitant and selected drugs in preventing emesis induced by centrally or peripherally acting emetogens in dogs. | 2008 Dec |
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Efficacy and safety of maropitant, a selective neurokinin 1 receptor antagonist, in two randomized clinical trials for prevention of vomiting due to motion sickness in dogs. | 2008 Dec |
|
Safety, pharmacokinetics and use of the novel NK-1 receptor antagonist maropitant (Cerenia) for the prevention of emesis and motion sickness in cats. | 2008 Jun |
|
Effect of refrigeration of the antiemetic Cerenia (maropitant) on pain on injection. | 2009 Fall |
|
Acute pancreatitis attributed to dietary indiscretion in a female mixed breed canine. | 2010 Feb |
|
Acute vomiting in cats: rational treatment selection. | 2010 Mar |
|
Efficacy of maropitant in the prevention of delayed vomiting associated with administration of doxorubicin to dogs. | 2010 Nov-Dec |
|
In vivo assessment of antiemetic drugs and mechanism of lycorine-induced nausea and emesis. | 2011 Dec |
Sample Use Guides
In Vivo Use Guide
Sources: https://www.drugs.com/pro/cerenia.html
Curator's Comment: Can also be injected subcutaneously
http://www.fda.gov/downloads/AnimalVeterinary/ucm062313.pdf
For Prevention of Vomiting Due to Motion Sickness
Administer Cerenia (Maropitant) Tablets orally at a minimum dose of 8 mg/kg (3.6 mg/lb) body weight once daily for up to 2 consecutive days. Dogs should be fasted 1 hour prior to administration of Cerenia Tablets. Administer Cerenia Tablets 2 hours prior to travel.
Route of Administration:
Oral
In Vitro Use Guide
Sources: https://www.ncbi.nlm.nih.gov/pubmed/25947563
Maropitant (0.1-10 uM) increased frequency of whole murine intestine contraction, decreased amplitude of contraction and totally inhibited motility index in a concentration-dependent manner.
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ACTIVE MOIETY
SUBSTANCE RECORD