Etoricoxib

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[edit] BRAND NAMES

[edit] STRUCTURE

Etoricoxib.jpg

[edit] MECHANISM OF ACTION

Etoricoxib is a non-steroidal anti-inflammatory drug (NSAID) of the coxib class. It is a selective inhibitor of the cyclooxygenase 2 enzyme (COX-2) at doses up to 150 mg daily.

Two forms of cyclooxygenase have been described in mammals:

  • The constitutive cyclooxygenase, COX-1, synthesizes prostaglandins necessary for normal gastrointestinal and renal function.
  • The inducible cyclooxygenase, COX-2, is responsible for the production of mediators including PGE2 which induce pain, inflammation or fever..

Inhibition of COX-1 is thought to be associated with gastrointestinal and renal toxicity while inhibition of COX-2 reduces pain and inflammation associated with musculoskeletal disorders.

[edit] INDICATIONS

For the symptomatic relief of osteoarthritis, rheumatoid arthritis, ankylosing spondylitis, and the pain and signs of inflammation associated with acute gouty arthritis.

The decision to prescribe a selective COX-2 inhibitor should be based on an assessment of the individual patient's overall risks

[edit] DOSAGE

Etoricoxib is administered orally and may be taken with or without food. The onset of the effect may be faster when Etoricoxib is administered without food. This should be considered when rapid symptomatic relief is needed.

As the cardiovascular risks of etoricoxib may increase with dose and duration of exposure, the shortest duration possible and the lowest effective daily dose should be used.

  • Osteoarthritis: The recommended dose is 30 mg once daily. In some patients with insufficient relief from symptoms, an increased dose of 60 mg once daily may increase efficacy. In the absence of an increase in therapeutic benefit, other therapeutic options should be considered.
  • Rheumatoid arthritis: The recommended dose is 90 mg once daily.
  • Acute gouty arthritis: The recommended dose is 120 mg once daily. Etoricoxib 120 mg should be used only for the acute symptomatic period, for a maximum of 8 days treatment.
  • Ankylosing spondylitis: The recommended dose is 90 mg once daily.

[edit] CONTRAINDICATIONS

  • Known hypersensitivity to Etoricoxib
  • History of asthma, urticaria, or other allergic-type reactions after taking aspirin or other NSAIDs
  • Active gastrointestinal bleeding
  • Pregnancy and lactation
  • Severe hepatic dysfunction (serum albumin <25 g/l or Child-Pugh score ≥10).
  • Estimated renal creatinine clearance <30 ml/min.
  • Children and adolescents under 16 years of age.
  • Inflammatory bowel disease.
  • Congestive heart failure (NYHA II-IV).
  • Patients with hypertension whose blood pressure is persistently elevated above 140/90mmHg and has not been adequately controlled.
  • Established ischemic heart disease, peripheral arterial disease, and/or cerebrovascular disease.

[edit] WARNINGS AND PRECAUTIONS

  • Cardiovascular Thrombotic Events: Etoricoxib may cause an increased risk of cardiovascular thrombotic events, myocardial infarction, and stroke. All nonsteroidal anti-inflammatory drugs (NSAIDs) may have a similar risk. This risk may increase with duration of use. Patients with cardiovascular disease or risk factors for cardiovascular disease (e.g. hypertension, hyperlipidaemia, diabetes mellitus, smoking) may be at greater risk. To minimize the potential risk for an adverse cardiovascular event, the lowest effective dose should be used for the shortest duration consistent with individual patient treatment goals. Therapy should be re-evaluated periodically, especially in patients with osteoarthritis.
  • Hypertension: NSAIDs can lead to onset of new hypertension or worsening of preexisting hypertension, either of which may contribute to the increased incidence of cardiovascular events. Etoricoxib may be associated with more frequent and severe hypertension than some other NSAIDs and selective COX-2 inhibitors, particularly at high doses. Therefore, hypertension should be controlled before treatment with etoricoxib and special attention should be paid to blood pressure monitoring during treatment with etoricoxib. Blood pressure should be monitored within two weeks after initiation of treatment and periodically thereafter. If blood pressure rises significantly, alternative treatment should be considered.
  • Heart failure and edema: Fluid retention and edema have been observed in some patients taking NSAIDs, including Etoricoxib, therefore caution is advised in patients with fluid retention or heart failure.
  • Gastrointestinal effects: NSAIDs, including Etoricoxib, can cause serious gastrointestinal events including bleeding, ulceration, and perforation of the stomach, small intestine or large intestine, which can be fatal. The risk is greater in patients with a prior history of ulcer disease or GI bleeding, in patients at high risk for GI events, especially the elderly, and when etoricoxib is taken concomitantly with acetylsalicylic acid (even at low doses).
  • Hepatic Effects: Elevated liver enzymes have been reported in approximately 1% of patients in clinical trials treated for up to one year with etoricoxib 30, 60 and 90 mg daily. Discontinue use of Etoricoxib immediately if abnormal liver enzymes (three times the upper limit of normal) persist or worsen.
  • Renal Effects: Etoricoxib may cause a reduction in prostaglandin formation and, secondarily, in renal blood flow, and thereby impair renal function. Use Etoricoxib with caution in the elderly, those with impaired renal function, heart failure, and liver dysfunction.
  • Anaphylactoid Reactions: Serious hypersensitivity reactions (such as anaphylaxis and angioedema) have been reported in patients receiving etoricoxib.
  • Skin Reactions: Rare cases of serious skin adverse events such as exfoliative dermatitis, Stevens-Johnson syndrome (SJS), and toxic epidermal necrolysis (TEN), have been reported in association with the use of NSAIDs and some selective COX-2 inhibitors, and can occur without warning. . Patients appear to be at highest risk for these reactions early in the course of therapy with the onset of the reaction occurring in the majority of cases within the first month of treatment. Discontinue Etoricoxib at first appearance of rash or skin reactions.

[edit] INTERACTIONS

  • Diuretics, ACE Inhibitors and Angiotensin II antagonists: Etoricoxib may reduce the antihypertensive effect. Concomitant use of Etoricoxib with ACE Inhibitors or Angiotensin II antagonists in elderly or volume depleted or renally compromised patients may result in deterioration of renal function, including acute renal failure.
  • Lithium carbonate: Reports suggest that non-selective NSAIDs and selective COX-2 inhibitors may increase plasma lithium levels. This interaction should be given consideration in patients taking Etoricoxib concomitantly with lithium.
  • Aspirin: concomitant administration of low-dose aspirin with Etoricoxib results in an increased rate of GI ulceration or other complications.
  • Oral Contraceptives: Etoricoxib increases plasma concentrations of ethinyl estradiol (EE). This increase should be considered when selecting an appropriate oral contraceptive for use with Etoricoxib.

[edit] PREGNANCY AND LACTATION

  • Pregnancy: Etoricoxib is contraindicated in pregnancy. If a woman becomes pregnant during treatment, etoricoxib must be discontinued.
  • Lactation: It is not known whether etoricoxib is excreted in human milk. Etoricoxib is excreted in the milk of lactating rats. Women who use etoricoxib must not breast feed

[edit] SIDE EFFECTS

Common (occurring in greater than 1 out of 100 and less than 1 out of 10 people)
Weakness and fatigue, dizziness, headache, flu-like illness, diarrhoea, wind, nausea, indigestion (dyspepsia), stomach pain or discomfort, heartburn, changes in blood tests related to your liver, swelling of the legs and/or feet due to fluid retention (oedema), increased blood pressure, palpitations, bruising.

Uncommon (occurring in greater than 1 out of 1000 and less than 1 out of 100 people)
Stomach or bowel bloating, chest pain, heart failure, heart attack, stroke, mini-stroke (transient ischaemic attack), abnormal heart rhythm (atrial fibrillation), upper respiratory infection, high levels of potassium in your blood, changes in blood or urine tests relating to your kidney, changes in your bowel habits including constipation, dry mouth, mouth ulcers, taste alteration, gastroenteritis, gastritis, stomach ulcer, being sick (vomiting), irritable bowel syndrome, inflammation of the esophagus, blurred vision, eye irritation and redness, nose bleed, ringing in the ears, vertigo, appetite increases or decreases, weight gain, muscle cramp/spasm, muscle pain/stiffness, inability to sleep, sleepiness, numbness or tingling, anxiety, depression,decreases in mental sharpness, breathlessness, cough, swelling of the face, flushing, skin rash or itchy skin, urinary tract infection.

Rare (occurring in greater than 1 out of 10,000 and less than 1 out of 1000 people)
Low blood levels of sodium.

Very Rare (occurring in less than 1 out of 10,000 people)
Allergic reactions (which may be serious enough to require immediate medical attention) including hives, swelling of the face, lips, tongue, and/or throat which may cause difficulty in breathing or swallowing, bronchospasm (wheezing or shortness of breath), severe skin reactions, inflammation of the stomach lining or stomach ulcers that can become serious and may lead to bleeding, liver problems, serious kidney problems, severe increase in blood pressure, confusion, seeing, feeling or hearing things that are not there (hallucinations).

[edit] RELATED LINKS

[edit] BIBLIOGRAPHY

[edit] REFERENCES

Non-steroidal anti-inflammatory drugs (NSAIDs)
Non-selective (COX-1 and COX-2 inhibitors) Aceclofenac   Acetylsalicylic acid   Benzydamine   Diclofenac   Flurbiprofen   Ibuprofen   Indometacin   Ketoprofen   Ketorolac   Ketorolac   Lornoxicam   Mefenamic acid   Morniflumate   Nabumetone   Naproxen   Niflumic acid   Piroxicam   Tenoxicam
Relatively COX-2 selective Meloxicam   Nimesulide
COX-2 selective inhibitors (Coxibs) Celecoxib   Etoricoxib   Parecoxib
Ophthalmic NSAIDs Bromfenac (ophthalmic)   Diclofenac (ophthalmic)   Flurbiprofen (ophthalmic)   Ketorolac (ophthalmic)   Nepafenac (ophthalmic)
Veterinary use Carprofen   Deracoxib   Firocoxib   Mavacoxib   Robenacoxib