Nacoxib

Nacoxib

etoricoxib

Manufacturer:

Bangkok Lab & Cosmetic

Distributor:

Bangkok Drug
Full Prescribing Info
Contents
Etoricoxib.
Description
Each film-coated tablet contains Etoricoxib 90 mg.
Action
Pharmacology: Pharmacodynamics: 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: Absorption: Rapid and complete.
Distribution: The volume of distribution (Vd) ~120 L.
Protein binding: 92%.
Metabolism: Extensive hepatic metabolism via CYP3A4 (In vitro data suggest that 2D6, 2C9, 2C19, and 1A2 may also play a role in metabolism); forms five metabolites with minimal inhibition of COX-2 and no inhibition of COX-1. The major metabolite is the 6'carboxylic acid derivative of etoricoxib formed by further oxidation of the 6'-hydroxymethyl derivative.
Bioavailability: ~100%; AUC increased 16% with mild hepatic impairment and ~twofold with moderate hepatic impairment.
Half-life Elimination: ~22 hours.
Time to peak: ~1 hour (fasted).
Excretion: Urine (70% as metabolites, <2% as unchanged drug); feces (20% as metabolites, <2% as unchanged drug).
Indications/Uses
Etoricoxib is indicated for: the symptomatic relief of osteoarthritis (OA) and rheumatoid arthritis (RA); the symptomatic relief of ankylosing spondylitis; the symptomatic relief of the pain and inflammation associated with acute gouty arthritis; treatment of acute pain including moderate to severe pain following minor dental procedures and gynecological surgery, and pain related to primary dysmenorrhea; treatment of chronic pain.
Dosage/Direction for Use
Use the lowest effective dose for the shortest duration of time, consistent with individual patient treatment goal.
Osteoarthritis: 30 to 60 mg once daily (should not exceed 60 mg daily).
Rheumatoid arthritis: 60 to 90 mg once daily (should not exceed 90 mg daily).
Ankylosing spondylitis: 60 to 90 mg once daily (should not exceed 90 mg daily).
Acute gouty arthritis: 120 mg once daily (initial and maximum dose) for ≤ 8 days.
Acute pain conditions: Acute pain conditions: 90 mg or 120 mg once daily for ≤ 8 days (should not exceed 120 mg daily).
Postoperative dental surgery pain: 90 mg once daily (initial and maximum dose) for ≤ 3 days.
Primary dysmenorrhea pain: 120 mg once daily (initial and maximum dose) for ≤ 8 days.
Postoperative gynecological surgery pain: 90 mg once daily (initial and maximum dose) for ≤ 5 days.
Chronic pain: 60 mg once daily (initial and maximum dose).
Special populations: Elderly patients: No dosage adjustment necessary; use with caution.
Patients with hepatic impairment: Mild hepatic dysfunction (Child-Pugh score 5-6/class A): Do not exceed 60 mg once daily.
Moderate hepatic dysfunction (Child-Pugh score 7-9/class B): Do not exceed 30 mg once daily or 60 mg every other day; use with caution.
Severe hepatic dysfunction (Child-Pugh score10/class C): Use is contraindicated.
Patients with renal impairment: creatinine clearance ≥30 ml/min: No dosage adjustment necessary.
creatinine clearance <30 ml/min: Use is contraindicated.
Pediatric: Adolescents ≥ 16 years; Refer to adult dosing.
Mode of Administration: Etoricoxib is administered orally and may be taken without regard to meals.
Overdosage
In general, symptoms of NSAIDs poisoning are mild, and usually include nausea and vomiting, epigastric pain, tinnitus, headache, drowsiness, blurred vision, and dizziness. Gastrointestinal bleeding may also occur. There have been isolated case reports of more serious toxicity, including seizures, hypotension, apnea, coma, and renal failure, although usually after ingestion of substantial quantities.
Treatment of NSAIDs overdosage is entirely supportive. The benefit of gastric decontamination is uncertain although activated charcoal may be of benefit within 1 hour of ingestion of potentially toxic amount. Forced diuresis, hemodialysis, or hemoperfusion are unlikely to be of benefit for NSAIDs overdosage, although hemodialysis may be required if oliguric renal failure develops.
Contraindications
Patients with known hypersensitivity to the etoricoxib or any excipients of this product.
Patients with congestive heart failure (NYHA II-IV).
Patients with established ischemic heart disease, peripheral arterial disease, and/or cerebrovascular disease.
Patients who, after taking aspirin or NSAIDs including COX-2 (cyclooxygenase-2) inhibitors, experience bronchospasm, acute rhinitis, nasal polyps, angioedema, urticaria, or all ergictype reactions.
Patients with active peptic ulceration or active gastrointestinal (GI) bleeding.
Pregnancy and lactation.
Patients with severe hepatic dysfunction (serum albumin <25 g/l or Child-Pugh score ≥10/class C).
Patients with estimated renal creatinine clearance <30 ml/min.
Children and adolescents under 16 years of age.
Patients with inflammatory bowel disease.
Patients with hypertension whose blood pressure is persistently elevated above 140/90 mmHg and has not been adequately controlled.
Warnings
Contraindicate in patients with known hypersensitivity to any component of this product, pregnancy and lactation.
Contraindicate in patients who have recently undergone coronary artery bypass graft surgery.
Contraindicate in patients with cardiovascular or cerebrovascular disease.
Contraindicate in patients with uncontrolled hypertension.
Contraindicate in patients with myocardial infarction or congestive heart failure NYHA II-IV.
Contraindicate in patients with history of ischemic heart disease of history of paralysis from cerebrovascular disease.
Caution should be used in patients with risk factors for cardiovascular events e.g. hypertension, hyperlipidemia, diabetes mellitus, smoking, elderly.
Caution should be used in patients with liver or renal disease.
Special Precautions
Use the lowest effective dose for the shortest duration of time, consistent with individual patient goals, to reduce risk of serious gastrointestinal (GI) and cardiovascular adverse events.
Serious (some fatal) upper GI complications including perforations, ulcers, and bleeding have occurred. Use caution with a history of GI disease (bleeding or ulcers), concurrent therapy with aspirin or other NSAIDs, anticoagulants and/or corticosteroids, smoking, alcohol, and the elderly or debilitated patients. When used concomitantly with aspirin (even at low doses), gastroprotective therapy (e.g. proton pump inhibitors, misoprostol) is recommended.
NSAIDs are associated with an increased risk of serious (and potentially fatal) adverse cardiovascular thrombotic events, including Ml and stroke. Risk may be increased with long-term use or preexisting cardiac risk factors (e.g. hypertension, hyperlipidemia, diabetes, smoking). Carefully evaluate individual cardiovascular profiles prior to prescribing and periodically re-evaluate the need for symptomatic relief and response to therapy.
Risk of Ml and stroke may be increased with use following coronary artery bypass graft (CABG) surgery; NSAIDs, including COX-2 setective inhibitors, are not recommended for treatment of perioperative pain in the setting of CABG.
New-onset or worsening hypertension may occur; maintain blood pressure <140/90 mmHg prior to initiation and monitor carefully throughout therapy. New-onset or worsening edema and heart failure may occur; use caution with preexisting edema (any cause), left ventricular dysfunction, or NYHA class I heart failure; use is contraindicated with NYHA class II- IV heart failure. Discontinue use if worsening heart failure, edema, or uncontrolled/severe hypertension occurs; consider alternate therapies for high risk patients.
Serious hypersensitivity reactions, including anaphylaxis, angioedema, Stevens- Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN) have been (rarely) reported with etoricoxib; discontinue use at first appearance of skin rash, mucosal lesions, or any other sign of hypersensitivity. Do not use in patients who experience bronchospasm, asthma, rhinitis, or urticaria with NSAIDs or aspirin therapy.
Use with caution in mild-to-moderate hepatic impairment; dosage adjustment recommended. Use is contraindicated in severe hepatic impairment. Elevations in transaminases (>3 times the upper limit of normal) may occur; monitor hepatic function closely in patients with previous abnormal hepatic function test or signs/symptoms of hepatic dysfunction. Severe hepatic reactions (e. g. hepatitis, jaundice, liver failure) have (rarely) occurred with use; discontinue if signs or symptoms of hepatic disease develop, if systemic manifestations occur, or with persistent or worsening abnormal hepatic function tests.
NSAIDs use may compromise existing renal function through a dose-dependent decrease in prostaglandin synthesis, resulting in a reduction in renal blood flow which may cause renal decompensation (usually reversible). Patients with impaired renal function, dehydration, heart failure, liver dysfunction; those taking diuretics, ACE inhibitors, angiotensin II receptor blockers; and the elderly are at greater risk for renal toxicity. Patients should be adequately hydrated prior to initiation of therapy. Monitor renal function closely; discontinue use with persistent or worsening abnormal renal function test. Use is contraindicated with severe renal impairment (CrCl <30 ml/minute). Long-term NSAIDs use may result in renal papillary necrosis.
NACOXIB-90MG tablets contain lactose. Patients with galactose intolerance or glucose-galactose malabsorption should not take this medicine.
Use In Pregnancy & Lactation
Pregnancy: Adverse events have been observed in animal reproduction studies. Etoricoxib is an NSAID that selectively inhibits COX-2, The effects of selective inhibition to the fetus have not been well studies, and no specific data for etoricoxib is available. Etoricoxib,as with other medicinal products inhibiting prostaglandin synthesis, may cause uterine inertia, premature closure of the ductus arteriosus, adverse fetal events, and may affect fertility. Etoricoxib is contraindicated in pregnancy; use in women who wish become pregnant is not recommended.
Lactation: It is not known whether etoricoxib is excreted in human milk. Etoricoxib is excreted in the milk of lactating rats. Breast-feeding is contraindicated.
Adverse Reactions
1%-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%: 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 failure/renal insufficiency, serum creatinine increased, shock, somnolence, Stevens-Johnson syndrome (SJS), tachycardia, thrombocytopenia, tinnitus, toxic epidermal necrolysis (TEN), transient ischemic attack, upper respiratory infection, uric acid increased, urinary tract infection, urticaria, vasculitis, vertigo, vomiting, weight gain, xerostomia.
Drug Interactions
The metabolism of etoricoxib is mediated by the cytochrome P450 isoenzyme CYP3A4. Use with other drugs that inhibit or induce this isoenzyme may result in changes in plasma concentration of etoricoxib. In addition, in vitro studies suggest that several other isoenzymes may also mediate the main metabolic pathway of etoricoxib. Rifampicin, a potent inducer of CYP isoenzymes, has produced decreased plasma concentration of etoricoxib.
Etoricoxib is an inhibitor of human sulfotransferase activity and has been shown to increase the plasma concentration of ethinylestradiol. Interactions with other drugs, such as oral salbutamol and minoxidil, also metabolised by this enzyme may be a possibility.
Interactions involving NSAIDs include enhancement of the effects of oral anticoagulants and increase plasma concentrations of lithium, methotrexate, and cardiac glycosides.
The risk of nephrotoxicity may be increased if given with ACE inhibitors, cyclosporin, tacrolimus, or diuretics. Effects on renal function may lead to reduced excretion of some drugs.
There may also be an increased risk of hyperkalemia with ACE inhibitors and some diuretics, including potassium sparing diuretics.
The antihypertensive effects of some antihypertensives including ACE inhibitors, beta blockers, and diuretics may be reduced. Convulsions may occur due to an interaction with quinolones. NSAIDs may increase the effect of phenytoin and sulfonylurea antidiabetics.
Use of more the one NSAID together (including aspirin) should be avoided because of the increased risk of adverse effects. The risk of gastrointestinal bleeding and ulceration associated with NSAIDs is increased when use with corticosteroids, the SSRls, the SNRI venlafaxine, the antiplatelets clopidogrel and ticlopidine, iloprost, erlotinib, sibutramine, or, possibly, alcohol, bisphosphonates, or pentoxifylline.
There may be an increased risk of hematotoxicity if zidovudine is use with NSAIDs. Ritonavir may increase the plasma concentrations of NSAIDs.
Storage
Store at the temperature below 30°C.
ATC Classification
M01AH05 - etoricoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Presentation/Packing
FC tab 90 mg (square, biconvex white with smooth on both sides) 3 x 10's.
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