Firocoxib

Bezeichnung:Firocoxib

CAS-Nr189954-96-9

Englisch Name:Firocoxib

CBNumberCB71011736

SummenformelC17H20O5S

Molgewicht336.4

MOL-Datei189954-96-9.mol

Firocoxib physikalisch-chemischer Eigenschaften

Schmelzpunkt	78-80°C
Siedepunkt	563.9±50.0 °C(Predicted)
Dichte	1.31
storage temp.	Sealed in dry,Store in freezer, under -20°C
Löslichkeit	Chloroform (Slightly), Ethyl Acetate (Slightly), Methanol (Slightly)
Aggregatzustand	Solid
Farbe	White to Off-White
InChI	InChI=1S/C17H20O5S/c1-17(2)14(12-6-8-13(9-7-12)23(3,19)20)15(16(18)22-17)21-10-11-4-5-11/h6-9,11H,4-5,10H2,1-3H3
InChIKey	FULAPETWGIGNMT-UHFFFAOYSA-N
SMILES	O1C(C)(C)C(C2=CC=C(S(C)(=O)=O)C=C2)=C(OCC2CC2)C1=O

Gefahreninformationscode (GHS)

Firocoxib Chemische Eigenschaften,Einsatz,Produktion Methoden

Beschreibung
Firocoxib is a selective inhibitor of COX-2 (IC₅₀s = 0.13 and 7.5 μM for COX-2 and COX-1, respectively, in isolated cat blood). It inhibits LPS-induced production of prostaglandin E₂ (PGE₂; ) in isolated dog, horse, and cat whole blood ex vivo. Firocoxib decreases lameness, induces analgesia, and improves range of motion in dogs and horses with osteoarthritis when administered at doses of 5 and 0.1 mg/kg per day, respectively. Formulations containing firocoxib have been used in dogs and horses with osteoarthritis.
Chemische Eigenschaften
White Solid
Verwenden
A selective cyclooxygenase-2-(COX-2) inhibitor. Anti-inflammatory; analgesic.
Verwenden
antibacterial
Definition
ChEBI: An enol ether that is the cyclopropylmethyl ether of 3-hydroxy-5,5-dimethyl-4-[4-(methylsulfonyl)phenyl]furan-2-one. A selective cyclooxygenase 2 inhibitor, it is used in veterinary medicine for the control of pain and inflammation associated with osteoart ritis in horses and dogs.
Trademarks
Equioxx (Merial).
Mechanism of action
Firocoxib is a non-steroidal anti-inflammatory drug (NSAID) belonging to the Coxib group, which acts by selective inhibition of cyclooxygenase-2 (COX-2)-mediated prostaglandin synthesis. Cyclooxygenase is responsible for the generation of prostaglandins. COX-2 is the isoform of the enzyme induced by pro-inflammatory stimuli and has been postulated to be primarily responsible for synthesizing prostanoid mediators of pain, inflammation, and fever. Coxibs, therefore, display analgesic, anti-inflammatory, and antipyretic properties. COX-2 is also thought to be involved in ovulation, implantation, and closure of the ductus arteriosus and central nervous system functions (fever induction, pain perception, and cognitive function).
Pharmakokinetik
Firocoxib has a half-life of 7.8 hours in dogs, 9-12 hours in cats, 11 hours in foals, 30-40 hours in adult horses, and 6.7 hours in calves. Because of shorter half-life, the concentrations are lower in foals compared to adult horses. It is highly protein bound (96%-98%). Oral absorption is 38% in dogs, 79%-100% in horses, approximately 100% in calves, and 54%-70% in cats. Feeding delays absorption but does not diminish overall absorption. In horses, oral absorption is 79%-100% with oral paste at a dose of 0.1 mg/kg, and 88% when the canine tablets are administered (no significant difference in absorption between oral paste and tablets). Fasted horses have higher absorption than fed horses[1].
Veterinary Drugs and Treatments
Firocoxib is indicated in dogs and horses for the control of pain and inflammation associated with osteoarthritis. A chewable tablet form for dogs and an oral paste for horses are available.
Like other NSAIDs, firocoxib can be useful for treating fever, pain, and/or inflammation associated with other conditions, postsurgery, trauma, etc.
Firocoxib may also be useful in other species, but information is scant regarding its safety and efficacy. One study in cats (McCann, Rickes et al. 2005) evaluating firocoxib in experimentally induced pyrexia, demonstrated that the drug was effective after a single oral dose in preventing or attenuating pyrexia at all doses studied (0.75 – 3 mg/kg).
Einzelnachweise
[1] Mark G. Papich DVM. “Firocoxib.”Saunders Handbook of Veterinary Drugs (Fourth Edition) (2016): 324-327.

Firocoxib Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

189954-96-9, Firocoxib Verwandte Suche:

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