Patients at high risk of NSAID-induced GI adverse events or surgical/traumatic bleeding

Parecoxib is a parenteral pro-drug for valdecoxib, a highly selective cyclo-oxygenase-2 (COX-2) inhibitor. COX-2 is the inducible isoform of cyclo-oxygenase whose expression is markedly increased in response to inflammatory stressors. In contrast, COX-1 is the constitutive isoform whose activity predominates during normal physiological conditions. The therapeutic and anti-inflammatory activity of NSAIDs results primarily from their inhibition of COX-2 whereas their toxicity, antiplatelet activity and adverse effects result mainly from COX-1 inhibition.

• similar analgesic efficacy to ketorolac 30mg IV or 60mg IM, a conventional non-selective parenteral NSAID
• has a significant opioid-sparing effect, therefore reducing opioid side effects
• causes significantly less erosion and ulceration of the gastroduodenal mucosa and fewer clinical gastrointestinal adverse events than ketorolac
• has no antiplatelet activity and therefore, unlike ketorolac, it does not affect peri-operative or traumatic blood loss
• has a rapid onset (13 minutes) and long duration of action (more than 15 hours IV)
• It is indicated for short-term management of acute postoperative pain and should be considered for parenteral short-term management of acute pain of moderate severity in patients:
  • for whom oral medication is inappropriate
  • who would be at high risk of gastrointestinal adverse events if prescribed ketorolac
  • in whom any antiplatelet effect must be minimised

Contraindications include:

• hypersensitivity to aspirin or any other NSAID, or sulphonamide hypersensitivity
• active peptic ulcer disease (i.e. patients on treatment) or GI bleeding
• established ischaemic heart disease or cerebrovascular disease
• mild to severe heart failure
• peripheral arterial disease
• inflammatory bowel disease

Caution should be observed in:

• patients with dehydration
• renal impairment
• hepatic impairment or predisposed to fluid retention
• oedema
• the elderly
• hypertension
• left ventricular dysfunction
• cardiac impairment
• following coronary artery bypass surgery
• allergic disorders
• coagulation defects and alternative therapy considered.
• avoid in pregnancy, breast feeding, severe liver disease.

Rare but potentially serious or fatal hypersensitivity and severe skin reactions are possible with COX II inhibitors – this risk is increased in patients with a history of drug allergy. The drug should be immediately discontinued if an adverse drug reaction of this type occurs.