Etoxib

Etoxib

etoricoxib

Manufacturer:

Micro Labs

Distributor:

Atlanta Medicare

Marketer:

Atlanta Medicare
Full Prescribing Info
Contents
Etoricoxib.
Description
Etoricoxib Tablets 30/60/90/120.
Action
Pharmacology: PHARMACODYNAMICS: Etoricoxib is an oral, selective cyclo-oxygenase-2 (COX-2) inhibitor within the clinical dose range.
Across clinical pharmacology studies, Etoricoxib produced dose-dependent inhibition of COX-2 without inhibition of COX-1 at doses up to 150 mg daily. Etoricoxib did not inhibit gastric prostaglandin synthesis and had no effect on platelet function.
Cyclooxygenase is responsible for generation of prostaglandins. Two isoforms, COX-1 and COX-2, have been identified. 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 the 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.
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 metabolised 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.
Indications/Uses
Etoricoxib is indicated for symptomatic treatment of: Pain and inflammation in osteoarthritis; Pain and inflammation in rheumatoid arthritis; Ankylosing spondylitis; Acute gout.
Dosage/Direction for Use
RECOMMENDED DOSE: Pain and inflammation in osteoarthritis: By mouth: Child 16-17 years: 30 mg once daily, increased if necessary to 60 mg once daily.
Adult: 30 mg once daily, increased if necessary to 60 mg once daily.
Pain and inflammation in rheumatoid arthritis, Ankylosing spondylitis: By mouth: Child 16-17 years: 60 mg once daily, increased if necessary to 90 mg once daily.
Adult: 60 mg once daily, increased if necessary to 90 mg once daily.
Acute gout: By mouth: Child 16-17 years: 120 mg once daily for maximum 8 days.
Adult: 120 mg once daily for maximum 8 days.
Administration in hepatic impairment: The maximum oral dose of etoricoxib in patients with mild hepatic impairment (Child-Pugh score of 5 to 6), regardless of indication, is 60 mg once daily; those with moderate impairment (Child-Pugh 7 to 9) should be given a maximum of 60 mg every other day or 30 mg once daily. Etoricoxib should not be given to patients with severe hepatic impairment (Child-Pugh 10 or more).
Musculoskeletal and joint disorders: The selective cyclooxygenase-2 (COX-2) inhibitor etoricoxib is used in the treatment of the musculoskeletal disorders, osteoarthritis and rheumatoid arthritis.
Etoricoxib is also used in gouty arthritis and has been tried in the treatment of ankylosing spondylitis.
MODE OF ADMINISTRATION: Orally, once a day.
Overdosage
In clinical studies, 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. There have been reports of acute overdosage with Etoricoxib, although adverse experiences were not reported in the majority or cases. The most frequently observed adverse experiences were consistent with the safety profile for Etoricoxib (e.g. gastrointestinal events, cardiorenal events).
In the event of overdose, it is reasonable to employ the usual supportive measures, e.g. remove unabsorbed material from the GI 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.
Contraindications
Active gastro-intestinal bleeding; active gastro-intestinal ulceration; cerebrovascular disease; inflammatory bowel disease; ischaemic heart disease; mild to severe heart failure; peripheral arterial disease; uncontrolled hypertension (persistently above 140/90 mmHg).
Special Precautions
Allergic disorders; cardiac impairment (NSAIDs may impair renal function); coagulation defects; connective-tissue disorders; Crohn's disease (may be exacerbated); dehydration; history of cardiac failure; hypertension; left ventricular dysfunction; oedema; risk factors for cardiovascular events; ulcerative colitis (may be exacerbated).
Hepatic impairment: Max. 60 mg daily in mild impairment.
Max. 60 mg on alternate days or 30 mg once daily in moderate impairment.
Use with caution; there is an increased risk of gastro-intestinal bleeding and fluid retention.
Avoid in severe liver disease.
Renal impairment: The lowest effective dose should be used for the shortest possible duration.
Avoid if possible or use with caution.
With systemic use in adults: Avoid if eGFR less than 30 mL/minute/1.73 m2.
Use in Children: Avoid if estimated glomerular filtration rate less than 30 mL/ minute/1.73 m2.
In renal impairment monitor renal function; sodium and water retention may occur and renal function may deteriorate, possibly leading to renal failure.
Use in the Elderly: With systemic use: elderly (risk of serious side-effects and fatalities) (in adults).
Use In Pregnancy & Lactation
Pregnancy: Avoid during the third trimester (risk of closure of fetal ductus arteriosus in utero and possibly persistent pulmonary hypertension of the newborn); onset of labour may be delayed and duration may be increased.
Lactation: Use with caution during breast-feeding.
Adverse Reactions
Common or very common: Ecchymosis; fatigue; influenza-like symptoms; palpitation.
Uncommon: Anxiety; appetite change; arthralgia; atrial fibrillation; chest pain; cough; dry mouth; dyspnoea; electrolyte disturbance; epistaxis; flushing; mental acuity impaired; mouth ulcer; myalgia; paraesthesia; taste disturbance; transient ischaemic attack; weight change.
Rare: Alveolitis; aseptic meningitis (patients with connective-tissue disorders such as systemic lupus erythematosus may be especially susceptible); hepatic damage; interstitial fibrosis associated with NSAIDs can lead to renal failure; pancreatitis; papillary necrosis associated with NSAIDs can lead to renal failure; pulmonary eosinophilia; Stevens-Johnson syndrome; toxic epidermal necrolysis; visual disturbances.
Very rare: Confusion; hallucinations.
Frequency not known: Angioedema; blood disorders; bronchospasm; colitis (induction of or exacerbation of); Crohn's disease (induction of or exacerbation of); depression; diarrhoea; dizziness; drowsiness; fluid retention (rarely precipitating congestive heart failure); gastro-intestinal bleeding; gastro-intestinal discomfort; gastro-intestinal disturbances; gastro-intestinal ulceration; haematuria; headache; hearing disturbances; hypersensitivity reactions; insomnia; nausea; nervousness; photosensitivity; raised blood pressure; rashes; renal failure (especially in patients with pre-existing renal impairment); tinnitus; vertigo.
Side-effects, further information: NSAIDs and cardiovascular events: All NSAID use (including cyclo-oxygenase-2 selective inhibitors) can, to varying degrees, be associated with a small increased risk of thrombotic events (e.g. myocardial infarction and stroke) independent of baseline cardiovascular risk factors or duration of NSAID use; however, the greatest risk may be in those receiving high doses long term.
Cyclo-oxygenase-2 selective inhibitors, diclofenac (150 mg daily) and ibuprofen (2.4 g daily) are associated with an increased risk of thrombotic events. Although there are limited data regarding the thrombotic effects of Aceclofenac, treatment advice has been updated in line with diclofenac, based on aceclofenac's structural similarity to diclofenac and its metabolism to diclofenac. The increased risk for diclofenac is similar to that of licensed doses of etoricoxib. Naproxen (1 g daily) is associated with a lower thrombotic risk and low doses of ibuprofen (1.2 g daily or less) have not been associated with an increased risk of myocardial infarction.
The lowest effective dose of NSAID should be prescribed for the shortest period of time to control symptoms and the need for long-term treatment should be reviewed periodically.
NSAIDs and gastro-intestinal events: All NSAIDs are associated with serious gastro-intestinal toxicity; the risk is higher in the elderly. Evidence on the relative safety of non-selective NSAIDs indicates differences in the risks of serious upper gastro-intestinal side effects - piroxicam, ketoprofen, and ketorolac trometamol are associated with the highest risk; indomethacin, diclofenac, and naproxen are associated with intermediate risk, and ibuprofen with the lowest risk (although high doses of ibuprofen have been associated with intermediate risk). Selective inhibitors of cyclooxygenase-2 are associated with a lower risk of serious upper gastro-intestinal side-effects than non-selective NSAIDs.
Recommendations are that NSAIDs associated with a low risk e.g. ibuprofen are generally preferred, to start at the lowest recommended dose and not to use more than one oral NSAID at a time.
The combination of a NSAID and low-dose aspirin can increase the risk of gastro-intestinal side-effects; this combination should be used only if absolutely necessary and the patient should be monitored closely.
While it is preferable to avoid NSAIDs in patients with active or previous gastro-intestinal ulceration or bleeding, and to withdraw them if gastro-intestinal lesions develop, nevertheless patients with serious rheumatic diseases (e.g. rheumatoid arthritis) are usually dependent on NSAIDs for effective relief of pain and stiffness.
Patients at risk of gastro-intestinal ulceration (including the elderly), who need NSAID treatment should receive gastro protective treatment.
Systemic as well as local effects of NSAIDs contribute to gastro-intestinal damage, taking oral formulations with milk or food, or using enteric-coated formulations, or changing the route of administration may only partially reduce symptoms such as dyspepsia.
NSAIDs and alcohol: Alcohol increases the risk of gastro-intestinal haemorrhage associated with NSAIDs. Specialist sources recommend that concurrent use need not be avoided with moderate alcohol intake, but greater caution is warranted in those who drink more than the recommended daily limits. Some cases of acute kidney injury have been attributed to use of NSAIDs and acute excessive alcohol consumption.
Drug Interactions
Etoricoxib has the following interaction information: See Table 1.

Click on icon to see table/diagram/image

Etoricoxib belongs to NSAIDS and will have the following interaction information.
Note: See also Aspirin in Table 2 as follows. Interactions do not generally apply to topical NSAIDs. (See Table 2.)

Click on icon to see table/diagram/image
Storage
Store below 30°C.
MIMS Class
Nonsteroidal Anti-Inflammatory Drugs (NSAIDs)
ATC Classification
M01AH05 - etoricoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Presentation/Packing
FC tab 30 mg (blue-green, apple-shaped, biconvex, engraved '30' on one face and other face plain) x 3 x 10's. 60 mg (dark-green, apple-shaped, biconvex, engraved '60' on one face and other face plain) x 3 x 10's. 90 mg (white, apple-shaped, biconvex, engraved '90' on one face and other face plain) x 3 x 10's. 120 mg (pale-green, apple-shaped, biconvex, engraved '120' on one face and other face plain) x 3 x 10's.
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