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PARECOXIB NA

CAS No.
197502-82-2
Chemical Name:
PARECOXIB NA
Synonyms
PARECOXIB NA
CBNumber:
CB6117568
Molecular Formula:
C19H17N2NaO4S
Molecular Weight:
392.4
MDL Number:
MFCD04972608
MOL File:
197502-82-2.mol

PARECOXIB NA Chemical Properties,Uses,Production

Description

Parecoxib sodium is an injectable COX-2 inhibitor, launched as an anti-inflammatory agent and for the management of acute pain. Parecoxib is an amide prodrug of Pharmacia’s valdecoxib. It can be administered by either i.m. or i.v. routes, in contrast to other currently available COX-2 inhibitors which are poorly watersoluble. Parecoxib sodium can be prepared from valdecoxib by acylation of the sulfonamide with propionic anhydride. Parecoxib sodium exhibited potent acute and chronic antiinflammatory activity in rats, as demonstrated in the carrageenan air pouch model, where 98% of inhibition was achieved with the dose of 0.3mg/kg, and in the adjuvant arthritis model (ED50 = 0.08mglkg). Moreover, in the carrageenan footpad edema model, parecoxib sodium showed excellent efficacy (ED50 = Smglkg) and a rapid onset of action comparable with the most potent analgesic ketorolac. In this model, it produced a complete blockade of the carrageenan-induced hyperalgesia within 1 h after iv. administration. Pharmacokinetic studies indicated that parecoxib sodium completely and rapidly converted in valdecoxib with bioequivalence found between parenterally administered parecoxib sodium and orally administered valdecoxib. The maximum plasma concentrations of valdecoxib were 2530% greater after iv. than i.m. administration of parecoxib and tnax was respectively 0.5 h after iv. and 1.5 h after i.m. administration. Parecoxib sodium had greater gastrointestinal tolerance than ketorolac and had no significant effect on platelet aggregation. Parecoxib sodium was as effective as ketorolac or even superior to morphine and placebo in the treatment of severe pain (such as that observed following gynaecologic or orthopaedic surgery). Mean times to rescue medication were longer with parecoxib compared to morphine. Parecoxib sodium works 12-14 min after i.v. administration and a dose of 40 mg provides good or excellent relief of pain in approximately 90% of patients. Thus, parecoxib sodium is a non-narcotic, specific COX-2 inhibitor, which provides potent analgesic ability and fulfils some important requirements for the pain management in the post-operative period such as i.v. formulation, rapidity of action, and short half-life. Furthermore, although valdecoxib is a substrate for CYP3A4 as other drugs used in the perioperative period, it does not interfere either with the metabolism of the sedative/tranquilizer, midazolam, or with the intravenous anesthetic propofol.

Originator

Pharmacia (Searle) (USA)

Uses

Anti-inflammatory; analgesic (cyclooxygenase).

brand name

Dynastat

PARECOXIB NA Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 9)Suppliers
Supplier Tel Email Country ProdList Advantage
Hangzhou FandaChem Co.,Ltd.
008657128800458; +8615858145714 fandachem@gmail.com China 9341 55
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
SPIRO PHARMA eric_feng1954@126.com China 9254 55
Wuhan Noble Pharmaceutical&Chemical Co.Ltd. 027-87827088 13907152521 3085654926@QQ.COM China 1973 58

View Lastest Price from PARECOXIB NA manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
	PARECOXIB NA pictures 2019-09-02 PARECOXIB NA
197502-82-2
US $7.00 / KG 1KG 99% JD 499 Career Henan Chemical Co
PARECOXIB NA 197502-82-2 Active Pharmaceutical Ingredients