PARECOXIB 40 AFT

Indications

• Short-term management of moderate to severe acute postoperative pain

Dosage

Adults: Initially, 10 mg by intramuscular or intravenous injection, then 10–30 mg every 4–6 hours as required, with a maximum duration of treatment of 2 days. Frequency may be increased to up to every 2 hours during the initial postoperative period, with a maximum of 60 mg per day.

Mechanism of action

Parecoxib selectively inhibits cyclooxygenase-2 (COX-2), an enzyme responsible for the formation of prostanoids, which are involved in the inflammatory response. By blocking COX-2, parecoxib reduces the synthesis of prostaglandins, leading to decreased inflammation, pain, and fever.

Pharmacodynamics

The analgesic effect of parecoxib occurs through its inhibition of COX-2, which reduces pain signaling pathways. This action is beneficial in managing postoperative pain, allowing for improved recovery and comfort for patients.

Pharmacokinetics

Parecoxib is rapidly absorbed after intramuscular administration, with peak plasma concentrations occurring within 30 minutes. It has a half-life of approximately 8 to 11 hours. The drug is metabolized primarily in the liver by cytochrome P450 enzymes, and its active metabolite, valdecoxib, is also eliminated via hepatic pathways. Renal impairment may affect drug clearance, and caution is advised in patients with hepatic impairment.

Contra-indications

• History of hypersensitivity to aspirin or any other NSAID
• Severe hepatic impairment
• Active gastrointestinal bleeding
• History of gastrointestinal ulceration or bleeding related to previous NSAID therapy
• Severe renal impairment
• Hypertension that is uncontrolled

Adverse effects

• Gastrointestinal disturbances
• Nausea
• Vomiting
• Weight increase
• Dizziness
• Anxiety
• Angioedema
• Hemorrhage
• Aggravation of asthma symptoms

Interactions

• Other NSAIDs may increase risk of gastrointestinal side effects
• Anticoagulants may enhance the risk of bleeding
• Caution with diuretics due to risk of renal impairment
• Caution with antihypertensives as NSAIDs may reduce their effectiveness

Precautions

• Use with caution in patients with allergic disorders
• Cardiac impairment
• Caution in patients with a history of gastritis or peptic ulcers
• Elderly patients may be more susceptible to adverse effects

Pregnancy

Use only if the potential benefit justifies the risk, especially avoid during the third trimester due to risk of fetal ductus arteriosus closure and potential pulmonary hypertension in the newborn.

Breast-feeding

Amount excreted in breast milk is too small to be harmful.

Storage

Store in a cool, dry place, away from direct sunlight.

Formulations

• Intravenous solution: 30 mg/1 ml
• Intramuscular injection ampoules: 30 mg/1 ml