Mexib

Mexib

etoricoxib

Manufacturer:

Mepro Pharma

Distributor:

Royal Distribution

Marketer:

ESTI Pharma
Full Prescribing Info
Contents
Etoricoxib.
Description
Each film-coated tablet contains: Etoricoxib 60 mg and 90 mg.
Mexib is described chemically as 5-chloro-6'-methyl-3-[4-methylsulfonyl) phenyl]-2,3'-bipyridine. The empirical formula is C18H15CIN2O2S. The molecular weight is 358.84.
Action
Pharmacology: Pharmacodynamics: MEXIB is a nonsteroidal anti-inflammatory drug (NSAID) with a potent highly selective cyclooxygenase-2 (COX-2) inhibitor activity. The drug exhibits anti-inflammatory, analgesic and antipyretic activities in animal models. Since 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 GI toxicity and without effects on platelet function.
Pharmacokinetics: Orally administered etoricoxib is well absorbed. The mean oral bioavailability is approximately 100%. The pharmacokinetics of etoricoxib is linear across the clinical dose range. In some studies, the onset of action of etoricoxib is reported to have occurred as early as 24 minutes after dosing.
Etoricoxib is approximately 92% bound to human plasma protein.
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 cytochrome P450 (CYP) enzymes.
Elimination of etoricoxib occurs almost exclusively through metabolism followed by renal excretion.
Hepatic insufficiency: Patients with mild/moderate hepatic insufficiency are reported to have similar mean AUC compared to the healthy subjects. There are no clinical or pharmacokinetic data in patients with severe hepatic insufficiency (Child-Pugh score >9).
Renal insufficiency: The pharmacokinetics of etoricoxib in patients with moderate to severe renal insufficiency and patients with end-stage renal disease on Hemodialysis were not reported to be significantly different from those in healthy subjects.
Pediatric Patients: Safety and effectiveness of etoricoxib in paediatric patients (<12 years) have not been established.
Toxicology: Carcinogenicity, mutagenicity and impairment of fertility: This drug was neither found to be carcinogenic nor mutagenic. It is also not reported to impair fertility.
Indications/Uses
Acute and chronic treatment of the signs and symptoms of osteoarthritis (OA) and rheumatoid arthritis (RA).
Treatment of acute gouty arthritis.
Relief of acute pain.
Relief of chronic musculoskeletal pain.
Dosage/Direction for Use
Etoricoxib is administered orally with or without food.
Arthritis: Osteoarthritis: 60 mg once daily.
Rheumatoid Arthritis: 90 mg once daily.
Acute Gouty Arthritis: 120 mg once daily.
Etoricoxib 120 mg should be used only for the acute symptomatic period.
Analgesia: Acute pain: The recommended dose is 120 mg once daily.
Chronic Musculoskeletal Pain: 60 mg once daily.
No dosage adjustment is necessary for the elderly.
Hepatic insufficiency: Mild hepatic insufficiency: a dose of 60 mg once daily should not be exceeded. Moderate hepatic insufficiency (Child-Pugh score 7-9) a dose of 60 mg every alternate day should not be exceeded.
Severe hepatic insufficiency (Child-Pugh score >9): No data available.
Renal insufficiency: Not recommended in advanced renal disease (creatinine clearance <30 ml/min).
No dosage adjustment is necessary for patients with lesser degrees of renal insufficiency.
Overdosage
In the event of overdose, employ the usual supportive measures.
Contraindications
Hypersensitivity to any component of this preparation.
Warnings
This drug should be used with caution in patients suffering from coronary heart disease (CHD)/Cardiovascular disorder.
Special Precautions
In patients with advanced renal disease, treatment with etoricoxib is not recommended: If therapy must be initiated in such patients, close monitoring of the renal function is advisable.
Patients with pre-existing severely impaired renal function, uncompensated heart failure or cirrhosis should be treated with utmost caution because under conditions of compromised renal perfusion, administration of etoricoxib may cause a reduction in prostaglandin formation and secondary in renal blood flow, and thereby impair renal function. Monitoring of renal function in such patients should be considered, and if need be, therapy should be discontinued to allow recovery to the pretreatment state.
In patients with considerable dehydration, it is advisable to rehydrate patients prior to starting therapy with etoricoxib.
As with other drugs known to inhibit prostaglandin synthesis the possibility of fluid retention, oedema or hypertension should be taken into consideration when etoricoxib is used in patents with pre-existing oedema, hypertension or heart failure.
While on treatment with etoricoxib, antiplatelet therapy if ongoing, should not be discontinued and, if indicated, should be considered in patients at risk for or with a history or cardiovascular or other thrombotic effects.
Caution should be exercised in patients with a medical history of ischemic heart disease because of the pharmacodynamic profile of COX-2 selective inhibitors.
Physicians should be aware that upper gastrointestinal (GI) ulcers/ulcer complications have occurred in patients treated with etoricoxib. Independent of treatment, complications have occurred in patients treated with etoricoxib. Independent of treatment, patients with a prior history of GI perforation ulcers and bleeding (PUB) and patients >65 years of age are known to be at a higher risk for a PUB.
Elevations of alanine aminotransferase (ALT) and/or aspartate aminotransferase (AST) (approximately three or more times the upper limit of normal have been reported in a very few patients up to one year period.
Caution to be exercised in treating patients with symptoms and signs of liver dysfunction or in whom an abnormal liver function test has occurred.
The drug should be used with caution in patients who have previously experienced acute asthmatic attacks, urticaria, or rhinitis, which were precipitated by salicylate or non-selective cyclooxygenase inhibitors.
Etoricoxib may mask fever which is a sign of infection. The physician should be aware of this when using the drug in those treated for infection.
Paediatric use: Safety and effectiveness of etoricoxib in paediatric patients have not been established.
Use In Pregnancy & Lactation
Pregnancy: There are no adequate and well-controlled studies in pregnant women. The drug should be used during the first two trimesters of pregnancy only if the potential benefit justifies the potential risk to the foetus. As with other drugs known to inhibit prostaglandin synthesis, use of etoricoxib should be avoided in late pregnancy because it may cause premature closure of the ducts arteriosus.
Nursing Mothers: A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother.
Adverse Reactions
Generally well tolerated. Commonly reported adverse effects include: asthenia, fatigue, dizziness, lower extremity oedema, hypertension, dyspepsia, heartburn, nausea, and headache. Hypersensitivity reactions, including anaphylactic/anaphylactoid reaction, insomnia, dysgeusia, somnolence, congestive heart failure, bronchospasm, abdominal pain, oral ulcers, peptic ulcer including perforation and bleeding (mainly in elderly patients) vomiting, angioedema, rash, pruritus, urticaria, renal insufficiency, including renal failure have also been reported.
Drug Interactions
Warfarin: Monitoring of INR values should be done when etoricoxib treatment is initiated or changed particularly in the first few days, in patients receiving warfarin or similar agents.
Rifampin: Co-administration with rifampin may cause decrease in etoricoxib plasma area under the curve (AUC).
Methotrexate: Monitoring for methotrexate-related toxicity should be considered when etoricoxib at doses greater than 90 mg daily and methotrexate are administered concomitantly.
Angiotensin Converting Enzyme (ACE) inhibitors: COX-2 selective inhibitors may diminish the antihypertensive effect of ACE inhibitors.
Lithium: COX-2 selective inhibitors may increase plasma lithium levels.
Aspirin: etoricoxib can be used concomitantly with low dose aspirin for cardiovascular prophylaxis. However, it may result in an increased rate of GI ulceration or other complications compared to use of etoricoxib alone.
Oral contraceptives: Increase in ethinyl estradiol (EE) concentration is reported when concomitantly used with etoricoxib.
Antacids and ketoconazole (a potent inhibitor of CYP3A4) reportedly did not have clinically important effects on the pharmacokinetics of etoricoxib.
Storage
Store at temperature not exceeding 30°C. Protect from light.
ATC Classification
M01AH05 - etoricoxib ; Belongs to the class of non-steroidal antiinflammatory and antirheumatic products, coxibs.
Presentation/Packing
FC tab 60 mg x 3 x 10's. 90 mg x 3 x 10's.
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