Torcozia

Etoricoxib.

White, unequal hexagonal, rounded corners, biconvex film-coated tablet. One side has letter "XC" and on the other side no letter.
Each film-coated tablet contains Etoricoxib 90 mg.

Pharmacology: Pharmacodynamics: Mechanism of action: Etoricoxib is a nonsteroidal anti-inflammatory agent (dipyridinyl derivative) for oral administration. It is a selective inhibitor of cyclooxygenase-2 (COX-2). Decreases synthesis of prostaglandins due to selective inhibition of cyclooxygenase-2 (COX-2) enzyme; has antipyretic, analgesic, and anti-inflammatory properties. Etoricoxib does not inhibit cyclooxygenase-1 (COX-1) at therapeutic concentrations.
Pharmacokinetics: Etoricoxib is well absorbed from the gastrointestinal tract after oral doses. Peak plasma concentrations are reached in about 1 hour in fasted adults; food delays absorption by about 2 hours, although it has no effect on the extent of absorption. Plasma protein binding is about 92%. At steady state the half-life of etoricoxib is about 22 hours. Etoricoxib is extensively metabolized with less than 2% of a dose recovered in the urine as the parent drug. The major route of metabolism is via cytochrome P450 isoenzymes including CYP3A4 to form the 6'-hydroxymethyl derivative of etoricoxib, which is then oxidized to the 6'-carboxylic acid derivative, the major metabolite. Both are inactive or only weak cyclo-oxygenase-2 (COX-2) inhibitors. Excretion is mainly via the urine (70%) with only 20% of a dose appearing in the faeces. Studies in animals suggest that etoricoxib may cross the placenta and that some is distributed into breast milk.

Etoricoxib 90 mg film-coated tablets are indicated for: Acute and chronic treatment of the signs and symptoms of osteoarthritis (OA) and rheumatoid arthritis (RA); Treatment of ankylosing spondylitis (AS); Treatment of acute gouty arthritis, Relief of chronic musculo-skeletal pain, including chronic low back pain; Relief of acute pain including dental surgery; Treatment of primary dysmenorrhea; Treatment of moderate to severe acute post-operative pain associated with abdominal gynecological surgery.

Rheumatoid arthritis: The recommended dose is 90 mg once daily.
Ankylosing spondylitis: The recommended dose is 90 mg once daily.
Acute pain: For acute pain conditions, TORCOZIA 90 MG should be used only for the acute symptomatic period.
Post-operative dental pain: The recommended dose is 90 mg once daily for up to 3 days.
Post-operative gynecological pain: The recommended dose is 90 mg once daily for up to 5 days. The initial dose should be administered shortly before surgery. The dose can be increased to a maximum 120 mg once daily.
Hepatic insufficiency: Etoricoxib 90 mg tablet is not for use in patients with mild or moderate hepatic insufficiency.
In patients with mild hepatic insufficiency (Child-Pugh score 5-6), a dose of 60 mg once daily should not be exceeded.
In patients with moderate hepatic insufficiency (Child-Pugh score 7-9), the dose should be reduced; a dose of 60 mg every other day should not be exceeded, administration of 30 mg once daily can also be considered.
There are no clinical or pharmacokinetic data in patients with severe hepatic insufficiency (Child-Pugh score >9).
Use is contraindicated in severe hepatic insufficiency.
Renal Insufficiency: Creatinine clearance <30 mL/min: Use is contraindicated.
Creatinine clearance ≥30 mL/min: No dosage adjustment necessary.
Mode of Administration: TORCOZIA 90 MG is administered orally. TORCOZIA 90 MG may be administered without regard to meal.

Overdose and Treatment: There have been reports of acute overdosage with etoricoxib, although adverse experiences were not reported in the majority of cases. The most frequently observed adverse experiences were consistent with the safety profile for etoricoxib (e.g. gastrointestinal events, renovascular events).
In the event of overdose, it is reasonable to employ the usual supportive measures, e.g., remove unabsorbed material from the gastrointestinal tract, employ clinical monitoring, and institute supportive therapy, if required. Etoricoxib is not dialyzable by hemodialysis; it is not known whether etoricoxib is dialyzable by peritoneal dialysis.

Etoricoxib is contraindicated in patients with a history of hypersensitivity to etoricoxib or any component of the formulation.
Etoricoxib is contraindicated in patients with congestive heart failure (NYHA class II-IV).
Etoricoxib is contraindicated in patients with active peptic ulceration or gastrointestinal (Gl) bleeding.
Etoricoxib is contraindicated in patients with severe hepatic dysfunction (Child-Pugh score >9).
Etoricoxib is contraindicated in patients with severe renal impairment (CrCl <30 ml/min).
Etoricoxib is contraindicated in patients with a history of allergic-type reaction (eg, bronchospasm, acute rhinitis, nasal polyps, angioedema, urticaria) to aspirin or other non-steroidal anti-inflammatory drugs (NSAIDS).
Etoricoxib is contraindicated in pregnancy and lactation.
Etoricoxib is contraindicated in children under 16 years of age.
Etoricoxib is contraindicated in patients with inflammatory bowel disease.
Etoricoxib is contraindicated in patients with established ischemic heart disease, peripheral artery disease and/or cerebrovascular disease (including patients who have recently undergone coronary artery bypass graft surgery or angioplasty).
Etoricoxib is contraindicated in patients with persistent uncontrolled hypertension.

Etoricoxib should be used with caution in patients with significant risk factors for cardiovascular disease such as hypertension, hyperlipidaemia and diabetes mellitus.
Etoricoxib should be avoided in patients who have a history of mild allergic phenomena related to ingestion of other nonsteroidal anti-inflammatory drugs eg, rash.
Etoricoxib should be avoided in patients who have conditions predisposing to gastrointestinal events (eg, history of peptic ulcer, upper gastrointestinal disease, ulcerative colitis; smoking; advancing age; concurrent aspirin or corticosteroids; alcohol abuse; stress).
Etoricoxib should be avoided in patients with bleeding disorders (potential exacerbation).

Pregnancy: Etoricoxib is contraindicated in women who are pregnant or who may become pregnant.
Lactation: The use of etoricoxib is contraindicated during lactation. It is not known whether etoricoxib is excreted in human milk. Etoricoxib is excreted in milk of lactating rats. Women who use etoricoxib must not breast feed.

1% to 10%: Cardiovascular: Edema, hypertension, palpitations.
Central nervous system: Dizziness, fatigue, headache.
Dermatologic: Bruising.
Gastrointestinal: Abdominal pain, diarrhea, dyspepsia, flatulence, heartburn, nausea.
Hepatic: ALT increased, AST increased.
Neuromuscular & skeletal: Weakness.
Miscellaneous: Alveolar osteitis, flu-like syndrome.
<1%, postmarketing and/or case reports: Abnormal taste, anaphylactic/anaphylactoid reactions, anemia, angina pectoris, angioedema, anxiety, appetite increase/decrease, arrhythmia, atrial fibrillation, blurred vision, bronchospasm, BUN increased, cerebrovascular accident, chest pain, confusion, congestive heart failure, conjunctivitis, constipation, cough, CPK increased, depression, dyspnea, ECG changes, epistaxis, esophagitis, erythema, facial edema, fixed drug eruption, flushing, gastritis, gastroduodenal ulcer, gastroenteritis, gastroesophageal reflux, gastrointestinal bleeding, gastrointestinal perforation, hallucinations, hepatic failure, hepatitis, hyperkalemia, hypersensitivity reactions, hypertensive crisis, hypoesthesia, hyponatremia, insomnia, interstitial nephritis, jaundice, leukopenia, myocardial infarction, muscle pain, muscle spasm, nephrotic syndrome, oral ulceration, pancreatitis, paresthesia, peptic ulcers, proteinuria, pruritus, rash, renal insufficiency (including renal failure), serum creatinine increased, shock, somnolence, Stevens-Johnson syndrome (SJS), tachycardia, taste abnormal, thrombocytopenia, tinnitus, toxic epidermal necrolysis (TEN), transient ischemic attack, upper respiratory infection, uric acid levels increased, urinary tract infection, urticaria, vasculitis, vertigo, vomiting, weight gain, xerostomia.

Concomitant use of etoricoxib and warfarin has resulted in increased serum concentration of warfarin.
Concomitant administration of etoricoxib with rifampicin, a potent inducer of CYP isoenzymes has produced decreased plasma concentrations of etoricoxib.
Concomitant use of etoricoxib and diuretics, angiotensin converting enzyme (ACE) inhibitors and angiotensin II antagonists (AIIAs) may decrease the antihypertensive effect.
Etoricoxib is an inhibitor of human sulfotransferase activity and has been shown to increase the plasma concentration of ethinylestradiol.

Store at a temperature below 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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