Pharmacology: Pharmacodynamics: Etoricoxib, an NSAID, is a selective cyclo-oxygenase-2 (COX-2) inhibitor. Its anti-inflammatory and analgesic action is exhibited by inhibition of prostaglandin synthesis via inhibition of COX-2.
Pharmacokinetics: Absorption: Well absorbed from the gastrointestinal tract, food delays rate of absorption.
Absolute bioavailability: Approx 100%.
Time to peak plasma concentrations: Approx 1 hour (without food), 2 hours (with food).
Distribution: Volume of distribution: 120 L.
Plasma protein binding: Approx 92%.
Metabolism: Extensively metabolised via CYP3A4 isoenzyme to form 6'-hydroxymethyl derivative of etoricoxib, then oxidised to 6'-carboxylic acid derivative (major metabolite).
Excretion: Mainly via urine (70%), 20% in faeces, <2% as unchanged drug.
Elimination half-life: Approx 22 hours.
Ankylosing spondylitis, Rheumatoid arthritis.
Osteoarthritis.
Acute gouty arthritis.
Pain and inflammation associated with dental surgery.
Ankylosing spondylitis, Rheumatoid arthritis: Adult: 60 mg once daily, may increase to 90 mg once daily as necessary. Once patient is clinically stable, may reduce dose to 60 mg once daily.
Osteoarthritis: Adult: 30 mg once daily, may increase to 60 mg once daily as necessary.
Acute gouty arthritis: Adult: 120 mg once daily. Max duration: 8 days.
Pain and inflammation associated with dental surgery: Adult: 90 mg once daily. Max duration: 3 days.
Renal Impairment: See table.
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Hepatic Impairment: Mild (Child-Pugh score 5-6): Max: 60 mg once daily.
Moderate (Child-Pugh score 7-9): Max: 30 mg once daily.
Severe (Child-Pugh score ≥10): Contraindicated.
Administration: May be taken with or without food.
Symptoms: Gastrointestinal events, cardiorenal events.
Management: Supportive treatment e.g. removal of unabsorbed drug from the gastrointestinal tract and clinical monitoring.
Hypersensitivity. Patient with active peptic ulceration or gastrointestinal bleeding, inflammatory bowel disease, congestive heart failure (NYHA II-IV), uncontrolled hypertension or with persistently high blood pressure (>140/90 mmHg), ischaemic heart disease, peripheral arterial disease, cerebrovascular disease, history of bronchospasm, acute rhinitis, nasal polyps, angioneurotic oedema, urticaria or allergic-type reactions after taking aspirin, NSAIDs including COX-2 inhibitors. Children and adolescent <16 years. Renal (CrCl <30 mL/min) and severe hepatic (Child-Pugh ≥10) impairment. Pregnancy.
Patient with history of gastrointestinal disease (e.g. ulceration, gastrointestinal bleeding), with risk factors for cardiovascular events (e.g. hyperlipidaemia, hypertension, diabetes mellitus, smoking), uncompensated heart failure, cirrhosis, history of cardiac failure, left ventricular dysfunction, pre-existing oedema, dehydration. Mild to moderate hepatic impairment. Elderly. Lactation.
Use in Pregnancy: PO: Z (NSAIDs use in >20 weeks gestation may cause oligohydramnios and fetal renal impairment. Fetal ductus arteriosus premature closure and persistent pulmonary hypertension may occur >30 weeks gestation. Avoid NSAIDs 30 weeks and later. If an NSAID is needed during 20-30 weeks, use lowest effective dose for shortest duration.).
Significant: Fluid retention, oedema, hypertension, increased ALT or AST, hypersensitivity reactions including anaphylaxis and angioedema.
Cardiac disorders: Palpitations, arrhythmia.
Gastrointestinal disorders: Abdominal pain, constipation, flatulence, gastritis, heartburn, diarrhoea, dyspepsia, nausea, vomiting, oesophagitis, oral ulcer.
General disorders and admin site conditions: Asthenia, flu-like disease.
Infections and infestations: Alveolar osteitis.
Nervous system disorders: Headache.
Respiratory, thoracic and mediastinal disorders: Bronchospasm.
Potentially Fatal: Gastrointestinal perforations, ulcers or bleedings, exfoliative dermatitis, Stevens-Johnson syndrome (SJS), toxic epidermal necrolysis (TEN).
Increased INR with anticoagulants (e.g. warfarin). May decrease effect of diuretics and antihypertensive agents. Concomitant use with ACE inhibitor or angiotensin II antagonist may further deteriorate renal function. May increase rate of gastrointestinal ulceration with concomitant low dose acetylsalicylic acid. Increased plasma concentrations of ethinylestradiol, lithium, methotrexate, and other drugs metabolised by human sulfotransferases (e.g. oral salbutamol, minoxidil). Decreased plasma concentrations with rifampicin.
M01AH05 - etoricoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Intoricoxib FC tab 90 mg
30's;7's
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