Etoricoxib

Etoricoxib is a Cyclooxygenase-2 (COX-2) inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs) belonging to Analgesic class.

Etoricoxib is a selective COX-2 inhibitor used to relieve moderate post-surgical dental pain as a short-term treatment and inflammatory and painful symptoms of various forms of arthritis.

Etoricoxib is absorbed well from the gastrointestinal tract. Its Absolute bioavailability is approximately 100%. The time taken to reach peak plasma concentrations is Approximately 1 hour. Etoricoxib is 92% bound to proteins. Etoricoxib is metabolized via Hepatic, primarily via CYP3A4. Extensively metabolized by the CYP3A4 isoenzyme to form the 6'-hydroxymethyl derivative of etoricoxib, which undergoes further oxidation to form the major metabolite 6'-carboxylic acid derivative. It is Mainly excreted via urine as (70% as metabolites and <2% as unchanged drug) and in faeces as (20% as metabolites <2% as unchanged drug).

Etoricoxib shows side effects like Nausea or vomiting, Headache, Dizziness, Stomach pain, swelling of face, lips, eyelids, tongue, hands and feet, Yellowing of skin and eyes, Blurred vision, Increase in blood pressure, Urinary tract infection, Indigestion, Diarrhea, Drowsiness, Swelling of feet and lower legs.

Etoricoxib is available in the form of Oral Tablet and Oral capsule.

Etoricoxib is available in India, China, Austria, Finland, Singapore, France, Italy, Malaysia, Portugal and Spain.

Etoricoxib is an Analgesic a belonging to the class Cyclooxygenase-2 (COX-2) inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs).

Etoricoxib is a COX-2 selective inhibitor. Current therapeutic indications are: treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout. Like any other COX-2 selective inhibitor, Etoricoxib selectively inhibits isoform 2 of cyclo-oxigenase enzyme (COX-2) to reduce the generation of prostaglandins (PGs) from arachidonic acid.

The onset and duration of action for Etoricoxib is not known.

The Tmax of Etoricoxib is about 1 hour.

Etoricoxib is available in the form of an Oral Tablet and Oral capsule.

Etoricoxib tablet and capsule is taken orally usually once daily.

Etoricoxib is a selective COX-2 inhibitor used to relieve moderate post-surgical dental pain as a short-term treatment and inflammatory and painful symptoms of various forms of arthritis.

Etoricoxib is a Cyclooxygenase-2 (COX-2) inhibitor / non-steroidal anti-inflammatory drugs (NSAIDs) belonging to Analgesic class.

Etoricoxib, an NSAID, is an orally active, highly selective cyclo-oxygenase-2 (COX-2) inhibitor. Its anti-inflammatory and analgesic action is exhibited by inhibition of prostaglandin synthesis via inhibition of COX-2.

Etoricoxib is approved for use in the following clinical indications

• For the treatment of rheumatoid arthritis, osteoarthritis, ankylosing spondylitis, chronic low back pain, acute pain and gout.

• Osteoarthritis

Adult: 30 mg once daily, may increase to 60 mg once daily as necessary. Use the lowest effective dose and follow the shortest possible duration of treatment.

Child: ≥16 years Same as adult dose.

• Rheumatoid arthritis

Adult: 60 mg once daily, may increase to 90 mg once daily as necessary. Once patient is clinically stable, may reduce dose to 60 mg once daily. Use the lowest effective dose and follow the shortest possible duration of treatment.

Child: ≥16 years Same as adult dose.

• Ankylosing spondylitis

Adult: 60 mg once daily, may increase to 90 mg once daily as necessary. Once patient is clinically stable, may reduce dose to 60 mg once daily. Use the lowest effective dose and follow the shortest possible duration of treatment.

Child: ≥16 years Same as adult dose.

• Acute gouty arthritis

Adult: 120 mg once daily. Max treatment duration: 8 days.

Child: ≥16 years Same as adult dose.

• Acute pain

Adult: For the treatment of postoperative dental surgery pain: 90 mg once daily. Max treatment duration: 3 days. Doses should only be given during the acute symptomatic period.

Child: ≥16 years Same as adult dose.

• Primary dysmenorrhoea

Adult: For the treatment of acute pain: 120 mg once daily. Max treatment duration: 8 days. Doses should only be given during the acute symptomatic period.

Child: ≥16 years Same as adult dose.

Etoricoxib is available in various strengths as 30mg, 60mg, 90mg and 120mg.

Etoricoxib is available in the form of Oral tablet and Oral capsule.

• Dosage Adjustment in Kidney Patient

Etoricoxib is contraindicated with history of kidney disease.

• Dosage Adjustment in Hepatic impairment Patient

Etoricoxib is contraindicated with history of liver disease.

Etoricoxib is contraindicated in patients with

• Caution should be exercised in patients with a history of heart, liver, kidney disease, high blood pressure, blood clotting disorder, any allergy, children, elderly, during pregnancy and breast feeding.
• Drink adequate fluid to avoid dehydration.
• Stop the medication immediately if gastrointestinal lesions occur.
• Monitor blood pressure regularly while taking Etoricoxib.

• Allergy

Avoid taking Etoricoxib if you are allergic to it. Serious allergic reactions to this medicine are rare. However, seek immediate medical attention if you notice any symptoms such as skin rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, breathing difficulty, etc. It is also not recommended if you are allergic to other similar medicines like Paracetamol, Ibuprofen, Aspirin, etc.

• Gastrointestinal bleeding

Etoricoxib can cause stomach and intestinal bleeding. Therefore, this medicine is not recommended if you have peptic ulcers (sores in the lining of the stomach, small intestine, and food pipe) or bleeding in the stomach and intestine as it may worsen your health condition.

• Severe Liver/Kidney Impairment

Etoricoxib is not recommended for use if you have severe liver and/or kidney problems. This medicine may further damage your liver and/or kidneys and worsen your condition.

• Heart diseases

Etoricoxib is not recommended for use if you have heart problems such as heart failure (a condition in which your heart is unable to pump a sufficient amount of blood), ischaemic heart diseases (heart problems due to narrowing of the blood vessels that supply oxygen to the heart), high blood pressure that has not been adequately controlled or if you have undergone a coronary artery bypass graft surgery (a surgical procedure that diverts the blood from narrowed or blocked vessels in the heart to improve its blood supply). Taking this medicine may increase your risk of heart attack and stroke (a condition that occurs due to reduced blood supply to the brain).

• Diabetes or high cholesterol levels

Etoricoxib should be used with caution if you have diabetes (a condition of high sugar levels in your blood) or high blood cholesterol (fat) levels as it may increase the risk of heart problems.

Alcohol intake may increase the risk of heart problems when using Etoricoxib.

Etoricoxib should be used with caution in breastfeeding mothers.

Etoricoxib having pregnancy category C. It shows toxic effects on the fetus when given to pregnant women.

• Common

Fluid retention, new-onset or exacerbation of oedema, hypertension, new-onset or recurrent CHF, increased ALT or AST, hypersensitivity reactions (e.g. anaphylaxis, angioedema), Palpitations, arrhythmia, Abdominal pain, constipation, flatulence, gastritis, acid reflux, diarrhea, dyspepsia, epigastric discomfort, nausea, vomiting, oesophagitis, oral ulcer, Asthenia, fatigue, flu-like disease, Alveolar osteitis, Headache, dizziness, Bronchospasm, Ecchymosis.

• Rare

Gastrointestinal perforations, ulcers, hemorrhage, CV thrombotic events (e.g. MI, stroke). Rarely, exfoliative dermatitis, Stevens-Johnson syndrome, and toxic epidermal necrolysis.

• Anticoagulants:

Increased INR with anticoagulants (e.g. warfarin).

• Diuretics and antihypertensive agents:

May diminish the therapeutic effect of diuretics and antihypertensive agents.

• Aspirin:

May increase the risk of gastrointestinal ulceration with aspirin (even at low doses).

• Rifampicin:

Decreased plasma concentrations with rifampicin.

• Increased plasma concentrations of ethinylestradiol, lithium, methotrexate, and other drugs metabolized by human sulfotransferases (e.g. oral salbutamol, minoxidil).

The common side effects of Etoricoxib include the following

Common side effects

Nausea or vomiting, Headache, Dizziness, Stomach pain, swelling of face, lips, eyelids, tongue, hands and feet, Yellowing of skin and eyes, Blurred vision, Increase in blood pressure, Urinary tract infection, Indigestion, Diarrhea, Drowsiness, Swelling of feet and lower legs.

• Pregnancy

Pregnancy Category C

Etoricoxib should not be used in Pregnant women as it shows toxic effects on the fetus when given to pregnant women.

• Nursing Mothers

Etoricoxib should be used with caution in breastfeeding mothers.

• Pediatric Use

Etoricoxib is not recommended for children under 16 years of age.

Symptoms: Gastrointestinal or cardiorenal events.

Management: Supportive treatment. Remove unabsorbed drug from the gastrointestinal tract. Perform clinical monitoring.

• Pharmacodynamic

Etoricoxib, an NSAID, is an orally active, highly selective cyclo-oxygenase-2 (COX-2) inhibitor. Its anti-inflammatory and analgesic action is exhibited by inhibition of prostaglandin synthesis via inhibition of COX-2.

• Pharmacokinetics

Absorption

Etoricoxib is Well absorbed from the gastrointestinal tract. Its Absolute bioavailability is Approximately 100%. Time taken to reach peak plasma concentrations is Approximately 1 hour.

Distribution

Etoricoxib is 92% bound to proteins.

Metabolism and Excretion

Etoricoxib is metabolized via Hepatic, primarily via CYP3A4. Extensively metabolised by the CYP3A4 isoenzyme to form the 6'-hydroxymethyl derivative of etoricoxib, which undergoes further oxidation to form the major metabolite 6'-carboxylic acid derivative.It is Mainly excreted via urine as (70% as metabolites and <2% as unchanged drug) and in faeces as (20% as metabolites <2% as unchanged drug).

• https://www.apollopharmacy.in/salt/ETORICOXIB
• https://go.drugbank.com/drugs/DB01628
• https://www.medscape.co.uk/drug/etoricoxib-oral-69880-69880
• https://www.medindia.net/doctors/drug_information/etoricoxib.htm#Contraindications