Etoricon

White to off white biconvex, rectangular film-coated tablet engraved 'ACME' on one face and breakline on the other face.
Each film-coated tablet contains: Etoricoxib 120 mg.

Coxib.
Pharmacology: Pharmacodynamics: Etoricoxib is an oral, selective cyclo-oxygenase-2 (COX-2) inhibitor. Etoricoxib produced dose dependent inhibition of COX-2 without inhibition of COX-1 at doses up to 150 mg daily. COX-2 is the isoform of the enzyme that has been shown to be induced by pro-inflammatory stimuli and has been postulated to be primarily responsible for the synthesis of prostanoid mediators of pain, inflammation and fever. COX-2 is also involved in ovulation, implantation and closure of ductus arteriosus, regulation of renal function and central nervous system functions (fever induction, pain perception, and cognitive function). It may also play a role in ulcer healing. COX-2 has been identified in tissue around gastric ulcers in man but its relevance to ulcer healing has not been established. Etoricoxib did not inhibit gastric prostaglandin synthesis and had no effect on platelet function.
Pharmacokinetics: Absorption: Orally administered Etoricoxib is well absorbed. The absolute bioavailability approximately 100%. Following 120 mg once-daily to steady state, the peak plasma concentration (geometric mean Cmax = 3.6 μg/mL) was observed at approximately 1 hour (Tmax) after administration to fasted adults.
Dosing with food (high fat meal) had no effect on the extent of absorption of Etoricoxib after administration of 120 mg-dose. The rate of absorption was affected, resulting in a 36% decrease in Cmax and an increase in Tmax by 2 hours. These data are not considered clinically significant.
Distribution: Etoricoxib is approximately 92% bound to human plasma protein over the range of concentrations of 0.05 to 5 μg/mL. The volume of distribution at steady state (V_dss) was approximately 120 L in humans.
Metabolism: Etoricoxib is extensively metabolized with <1% of a dose recovered in urine as the parent drug. The major route of metabolism to form the 6'-hydroxymethyl derivative is catalyzed by CYP enzymes. CYP3A4 appears to contribute the metabolism of Etoricoxib in vivo. In vitro studies indicate that CYP2D6, CYP2C9, CYP1A2, and CYP2C19 also can catalyze the main metabolic pathway but their quantitative roles in vivo have not been studied.
Five metabolites have been identified for Etoricoxib in man. The principal metabolite is 6'-carboxylic acid derivative of Etoricoxib formed by further oxidation of 6'-hydroxymethyl derivative. These principal metabolites either demonstrate no measurable activity or are only weakly active as COX-2 inhibitors.
Elimination: Less than 2% remain as unchanged drug. Elimination of Etoricoxib occurs almost exclusively through metabolism followed by renal excretion. Steady state concentrations of Etoricoxib are reached within seven days of once daily administration of 120 mg, with an accumulation ratio of approximately 2, corresponding to a half-life of approximately 22 hours. The plasma clearance after a 25 mg intravenous dose is estimated to be approximately 50 mL/min.

Etoricoxib (Etoricon) is indicated for relief of pain and inflammation in: Osteoarthritis; Rheumatoid Arthritis; Ankylosing spondylitis; Acute gout; Dysmenorrhea; Other chronic musculoskeletal disorders; Following dental surgery.

Osteoarthritis, Dysmenorrhea & Chronic musculoskeletal disorders: 60 mg, once daily.
Rheumatoid arthritis, ankylosing spondylitis: 90 mg, once daily.
Pain following dental surgery and acute gout: 120 mg, once daily.
Or as directed by the physician.

Administration of single doses of Etoricoxib up to 500 mg and multiple doses up to 150 mg/day for 21 days did not result in significant toxicity. For reports of acute overdosage with Etoricoxib, adverse events were not reported for majority of the cases. In the event of overdose, usual supportive measures such as removal of unabsorbed material from GI tract, employment of clinical monitoring and institute of supportive therapy (if required) can be done.

Etoricoxib (Etoricon) is contraindicated to patients with known hypersensitivity to Etoricoxib. Patients with active peptic ulceration or gastro-intestinal (GI) bleeding, severe hepatic dysfunction. Patient having inflammatory bowel disease and severe congestive heart failure. Children under 16 years of age.

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

Pregnancy: Etoricoxib should be avoided in late pregnancy because it may cause premature closure of ductus arteriosus.
Lactation: As it is excreted in breast milk, use of Etoricoxib should be avoided during lactation.

Infections and infestations: Common: Alveolar osteitis.
Uncommon: Gastroenteritis, upper respiratory infection, urinary tract infection.
Blood and lymphatic system disorder: Common: Anemia (primarily associated with gastrointestinal bleeding), leukopenia, thrombocytopenia.
Immune system disorder: Uncommon: Hypersensitivity.
Rare: Angioedema/anaphylactic/anaphylactoid reactions, including shock.
Metabolism and nutrition disorders: Common: Edema/fluid retention.
Uncommon: Appetite increase or decrease, weight gain.
Psychiatric disorders: Uncommon: Anxiety, depression, mental acuity decreased, hallucinations.
Rare: Confusion, restlessness.
Nervous system disorders: Common: Dizziness, headache.
Uncommon: Dysgeusia, insomnia, paresthesia/hypoaesthesia, somnolence.
Eye disorders: Uncommon: Blurred vision, conjunctivitis.
Ear and labyrinth disorders: Uncommon: Tinnitus, vertigo.
Cardiac disorders: Common: Palpitations, arrhythmia.
Uncommon: Atrial fibrillation, tachycardia, congestive heart failure, non-specific ECG changes, angina pectoris, myocardial infarction.
Vascular disorders: Common: Hypertension.
Uncommon: Flushing, cerebrovascular accident, transient ischemic attack, hypertensive crisis, vasculitis.
Respiratory, thoracic, and mediastinal disorders: Common: Bronchospasm.
Uncommon: Cough, dyspnea, epistaxis.
Gastrointestinal disorders: Very common: abdominal pain.
Common: Constipation, flatulence, gastritis, heartburn/acid reflux, diarrhea, dyspepsia/epigastric discomfort, nausea, vomiting, oesophagitis, oral ulcer.
Uncommon: abdominal distention, bowel movement pattern change, dry mouth, gastroduodenal ulcer, peptic ulcers including gastrointestinal perforation and bleeding, irritable bowel syndrome, pancreatitis.
Hepatobiliary disorders: Common: ALT increased, AST increased.
Rare: Hepatitis, hepatic failure, jaundice.
Skin and subcutaneous tissue disorders: Common: Ecchymosis.
Uncommon: Facial edema, pruritus, rash, erythema, urticaria.
Rare: Stevens-Johnson syndrome, toxic epidermal necrolysis, fixed drug eruption.
Musculoskeletal and connective tissue disorders: Uncommon: Muscular cramp/spasm, musculoskeletal pain/stiffness.
Renal and urinary disorders: Uncommon: Proteinuria, serum creatinine increased, renal failure/renal insufficiency.
General disorders and administration site conditions: Common: Asthenia/fatigue, flu-like disease.
Uncommon: Chest pain.
Investigations: Uncommon: Blood urea nitrogen increased, creatine phosphokinase increased, hyperkalemia, uric acid increased.
Rare: Blood sodium decreased.

Oral anticoagulants, diuretics, ACE inhibitors, acetylsalicylic acid, cyclosporine, lithium, methotrexate, oral contraceptives, prednisone/prednisolone, digoxin, ethinyl estradiol drugs metabolized by CYP iso-enzymes, ketoconazole, rifampicin and antacids have interaction with Etoricoxib.

Special Precautions for Handling and Disposal: Any unused medicine should be disposed properly. Consult the pharmacist or local waste management center for more details about how to safely discard expired or unused medicines.

Store at temperatures not exceeding 30°C.

Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)

M01AH05 - etoricoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.

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