Etocox (Etoricoxib)

	Composition Etocox 60, 90, 120: Each film coated tablet contains Etoricoxib INN 60 mg, 90 mg and 120 mg respectively.
Chemical Structure Etoricoxib is described chemically as 5-chloro-6'-methyl-3-[4-(methylsulfonyl) phenyl]-2, 3'-bipyridine. The empirical formula is C18H15ClN2O2S. The molecular weight is 358.84.

Pharmacology Etoricoxib exhibits anti-inflammatory, analgesic and antipyretic activities. Etoricoxib is a potent, orally active, highly selective	Click Here to Enlarge Image
cyclooxygenase-2 (COX-2) inhibitor.Two isoforms of cyclooxygenase (COX) have been identified: COX-1 and COX-2. COX-1 is responsible for prostaglandin mediated normal physiologic functions such as gastric cytoprotection and platelet aggregation. Inhibition of COX-1 by nonselective NSAIDs has been associated with gastric damage and platelet inhibition. COX-2 has been shown to be primarily responsible for the synthesis of prostanoid mediators of pain, inflammation and fever. Selective inhibition of COX-2 by Etoricoxib decreases these clinical signs and symptoms with decreased Gastro-intestinal toxicity and without effects on platelet function.
Pharmacokinetics Absorption Orally administered Etoricoxib is well absorbed. The mean oral bioavailability of Etoricoxib is approximately 100%. The onset of action of Etoricoxib occurs as early as 24 minutes after dosing. Following 120 mg once daily dosing to steady state, the peak plasma concentration (Cmax = 3.6 µg/mL) is observed at approximately 1 hour (Tmax) after administration to fasted adults & the AUC0-24hr is 37.8 µg•hr/mL. Distribution The volume of distribution at steady state is approximately 120 L in humans. Plasma protein binding Etoricoxib is approximately 92% bound to human plasma protein over the range of concentrations of 0.05-5 µg/mL. Metabolism Etoricoxib is extensively metabolized. Metabolism of Etoricoxib is catalyzed by cytochrome P-450 enzymes. Five metabolites have been identified in man. These metabolites are only weakly active as COX-2 inhibitors. Elimination half- life The elimination half-life of Etoricoxib is approximately 22 hours. Excretion Elimination of Etoricoxib occurs almost exclusively through metabolism followed by renal excretion. The plasma clearance is estimated to be approximately 50 mL/min. Indications Acute pain and inflammation, chronic musculo-skeletal pain, osteoarthritis, rheumatoid arthritis, acute gouty arthritis, primary dysmenorrhoea, ankylosing spondylitis. Dosage and Administration For adult and adolescent (over 16 years) Arthritis, osteoarthritis: 60 mg once daily. Rheumatoid arthritis: 90 mg once daily. Acute gouty arthritis: 120 mg once daily. Analgesia, Acute pain associated with dental surgery: 120 mg once daily.

Precautions
Decreased kidney function and liver function, dehydration, hypertension, history of heart failure, perforation and people over 65 years of age.

Side Effects
Common side effects are dizziness, headache, gastro intestinal disorders (e.g. abdominal pain, flatulence and heartburn), diarrhoea, dyspepsia, nausea, asthenia, fatigue, flu-like symptoms. Rare side effects are oedema, weight gain, anxiety, blurred vision, hypertension, epistaxis, dyspnoea, constipation, vomiting, muscle cramps, chest pain.

Use in Pregnancy and Lactation

Not recommended.

Special Conditions

Geriatrics:
No dosage adjustment is necessary for the healthy old patients.
Renal Impairment:
Dosage adjustment is not recommended in patients with moderate to severe renal insufficiency and patients with end-stage renal disease on hemodialysis.
Hepatic Impairment:
There is no clinical or pharmacokinetic data in patients with severe hepatic insufficiency. But in patients with mild & moderate hepatic insufficiency, a dose of 60 mg once daily should not be exceeded.

Drug Interactions
Rifampicin: Co-administration of Etoricoxib with rifampicin produced a 65% decrease in Etoricoxib plasma area under the curve (AUC).
Angiotensin Converting Enzyme (ACE) Inhibitors: Etoricoxib may diminish the anti hypertensive effect of ACE inhibitors.
Methotrexate: Etoricoxib may increase methotrexate plasma concentrations and reduce renal clearance of methotrexate when Etoricoxib at doses greater than 90 mg daily and methotrexate are administered concomitantly.
Aspirin: Concomitant administration of low-dose aspirin with Etoricoxib results in an increased rate of gastro intestinal ulceration or other complications compared to use of Etoricoxib alone.
Lithium: Etoricoxib may increase the plasma concentration of lithium.
Oral Contraceptives: Concomitant administration of Etoricoxib with an oral contraceptive containing ethinyl estradiol (EE) and norethindrone increases the steady state AUC0-24hr of EE.
Digoxin: Etoricoxib may increase the plasma concentration of digoxin.

How Supplied
Etocox 60: Each box contains 3 blister strips of 10 film coated tablets.
Etocox 90: Each box contains 2 blister strips of 10 film coated tablets.
Etocox 120: Each box contains 1 blister strip of 10 film coated tablets.