Parecoxib

Indications
 Parenteral
Postoperative pain
Adult: 40 mg slow IM or IV inj, then 20 or 40 mg every 6-12 hr as required. Max dose: 80 mg/day.
Child: <18 yr: Not recommended.
Elderly: <50 kg: 20 mg slow IV or IM inj, repeat to a max of 40 mg/day.
Hepatic impairment: Mild impairment (Child-Pugh score 5-6): No dosage adjustment. Moderate impairment (Child-Pugh score 7-9): Half the usual dose, repeat to a max of 40 mg/day. Severe impairment (Child-Pugh score >9): Not recommended.

Special Populations: Moderate hepatic impairment: Halved dose, max 40 mg/day.

Reconstitution: Reconstitute with sodium chloride 0.9%, glucose 5%, or sodium chloride 0.45% with glucose 5%.
Contraindications
 Aspirin or NSAID hypersensitivity; allergy to sulphonamides; inflammatory bowel disease; moderate to severe heart failure; ischaemic heart disease, peripheral arterial disease, or cerebrovascular disease; following CABG; active peptic ulceration; severe hepatic impairment (Child-Pugh score ≥10); pregnancy (3rd trimester) and lactation.
Warnings / Precautions
 Elderly, children ; history of GI ulceration, perforation or bleed; oedema; dehydration; hyperlipidaemia; DM; hypertension; liver or kidney disease; concurrent infection. May impair ability to drive or operate machinery.
Adverse Reactions
 Rash, ulcerations or any other signs of an allergic reaction; GI disturbances and bleeding; hypotension; hypertension; back pain; oedema; numbness; agitation or sleeping difficulties; anaemia; sore throat or difficulty breathing; pruritus; decreased urine output; jaundice, abnormal liver function; low platelet count; skin swelling, blistering or peeling; kidney failure; heart failure, heart attack, bradycardia, arrhythmia.
Potentially Fatal: Anaphylaxis, Steven-Johnson syndrome, toxic epidermal necrolysis.
Drug Interactions
 Enhances effects of oral anticoagulants (azapropazone and phenylbutazone); increases plasma concentrations of lithium, methotrexate, and cardiac glycosides; increased risk of nephrotoxicity with ACE inhibitors, ciclosporin, tacrolimus, or diuretics; reduces antihypertensive effects of some antihypertensives (ACE inhibitors, beta blockers, diuretics); occurrence of convulsions with quinolones; increases effects of phenytoin and sulfonylurea antidiabetics; increased risk of adverse effects with other NSAIDs (including aspirin) and misoprostol; risk of GI bleeding and ulceration increased with corticosteroids, SSRIs, the SNRI venlafaxine, the antiplatelets clopidogrel and ticlopidine, iloprost, erlotinib, sibutramine, alcohol, bisphosphonates, or pentoxifylline; increased risk of haematotoxicity with zidovudine; increased plasma concentrations with ritonavir; may alter the efficacy of mifepristone; metabolism may be decreased with CYP3A4 (e.g ketoconazole) and CYP2C9 inhibitors (e.g. fluconazole), or increased with enzyme inducers (e.g. carbamazepine, dexamethasone).
See Below for More parecoxib Drug Interactions
Mechanism of Actions
 Parecoxib is the prodrug of valdecoxib. It has a very high selectivity for inhibiting cyclo-oxygenase-2 (COX-2) mediated prostaglandin synthesis to reduce mediators of pain and inflammation. The selective inhibition of COX-2 is coupled with reduced GI toxicity, but associated increased risk for thrombotic events and renal impairment have been noted.
Distribution: Plasma protein binding: approx 98%.
Metabolism: Hydrolysed in the liver to its active metabolite, valdecoxib, and propionic acid; plasma half-life: 22 min.
Excretion: Via urine; approx 70% of a dose appearing as inactive metabolites, <5% of a dose appears as unchanged valdecoxib in the urine. Trace amounts of unchanged drug in faeces. Elimination half-life: 8 hr.
ATC Classification
 M01AH04 - parecoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Available As
  • Parecoxib 40 mg
  • Parecoxib 50 mg

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