PARECOXIB SODIUM
- CAS NO.:198470-85-8
- Empirical Formula: C19H19N2NaO4S
- Molecular Weight: 394.42
- EINECS: 813-689-5
- SAFETY DATA SHEET (SDS)
- Update Date: 2024-11-20 15:18:15
What is PARECOXIB SODIUM?
Description
Parecoxib is a prodrug form of the COX-2 inhibitor valdecoxib . It is converted to valdecoxib by human liver microsomes in vitro and in vivo in rats, dogs, and cynomolgous monkeys. Parecoxib is also a cannabinoid (CB) receptor 1 agonist with an EC50 value of 2.4 μM in HEK293 cells. It reduces hyperalgesia in a rat model of carrageenan-induced foot pad edema (ED50 = 5 mg/kg) and decreases inflammation in a rat model of M. butyricum-induced arthritis (ED50 = 0.08 mg/kg).
Chemical properties
White Solid
The Uses of PARECOXIB SODIUM
Anti-inflammatory, analgesic.
What are the applications of Application
Parecoxib sodium is a water-soluble sodium salt of the amide prodrug of valdecoxib. Parecoxibundergoes enzymatic hydrolysis in vivo to the active moiety valdecoxib, and is formulated as apowder for solution for parenteral administration. Valdecoxib is a selective inhibitor of the enzymeCOX-2.
Indications
For the short-term treatment of acute pain and post-operative pain i.e., oral surgery, abdominal hysterectomy, myomectomy, total knee replacement, total hip arthroplasty, laparoscopic cholecystectomy, inguinal hernia repair and other general surgery like diagnostic laparoscopy, gastrectomy, hernioplasty, appendectomy, hemithyroidectomy and splenectomy. Parecoxib Sodium may be used pre-operatively to prevent or reduce post-operative pain and it can reduce opioid requirements when they are used concomitantly.
Biological Functions
A water-soluble, injectable sodium salt form of parecoxib, an amide prodrug of the cyclooxygenase II (COX-2) selective, non-steroidal anti-inflammatory drug (NSAID) valdecoxib, with anti-inflammatory, analgesic, and antipyretic activities. Valdecoxib selectively binds to and inhibits COX-2. This prevents the conversion of arachidonic acid into prostaglandins, which are involved in the regulation of pain, inflammation, and fever. This NSAID does not inhibit COX-1 at therapeutic concentrations and, therefore, does not interfere with blood coagulation.
Pharmacokinetics
Parecoxib (Dynastat) is a prodrug of valdecoxib. Valdecoxib is an NSAID that exhibits antiinflammatory, analgesic and antipyretic properties in animal models. The mechanism of action is believed to be due to inhibition of prostaglandin synthesis primarily through inhibition of COX-2. At therapeutic plasma concentrations in humans valdecoxib does not inhibit cyclooxygenase-1 (COX-1).
Properties of PARECOXIB SODIUM
Melting point: | 273-275°C |
storage temp. | Inert atmosphere,2-8°C |
solubility | DMF: 10mg/mL; DMSO: 15mg/mL; Ethanol: 3mg/mL; PBS (pH 7.2): 5mg/mL |
form | Powder |
color | White to off-white |
InChI | InChI=1S/C19H18N2O4S.Na.H/c1-3-17(22)21-26(23,24)16-11-9-14(10-12-16)18-13(2)25-20-19(18)15-7-5-4-6-8-15;;/h4-12H,3H2,1-2H3,(H,21,22);; |
Safety information for PARECOXIB SODIUM
Signal word | Danger |
Pictogram(s) |
Flame Flammables GHS02 Exclamation Mark Irritant GHS07 |
GHS Hazard Statements |
H225:Flammable liquids H315:Skin corrosion/irritation H319:Serious eye damage/eye irritation H335:Specific target organ toxicity, single exposure;Respiratory tract irritation |
Precautionary Statement Codes |
P261:Avoid breathing dust/fume/gas/mist/vapours/spray. P305+P351+P338:IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing. |
Computed Descriptors for PARECOXIB SODIUM
InChIKey | OGSQVUBPCQXSGW-UHFFFAOYSA-N |
SMILES | CC1ON=C(C2C=CC=CC=2)C=1C1C=CC(S(=O)(=O)NC(=O)CC)=CC=1.[NaH] |
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Nuray Chemicals Pvt Ltd
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