Etoricoxib

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DRUGS
Etoricoxib

Etoricoxib is a non-steroidal anti-inflammatory (NSAID) class of the drug, which is used to treat painful conditions such as arthritis, gout and dental pain after surgery. It eases the pain and reduces inflammation. Etoricoxib has been known to work by blocking the production of substances that cause pain and inflammation.

Introduction

Etoricoxib is a non-steroidal anti-inflammatory (NSAID) class of the drug, which is used to treat painful conditions such as arthritis, gout and dental pain after surgery. It eases the pain and reduces inflammation. Etoricoxib has been known to work by blocking the production of substances that cause pain and inflammation.

Pharmacological class: NSAID

Indications

  • Ankylosing spondylitis
  • Osteoarthritis
  • Rheumatoid arthritis
  • Musculoskeletal pain
  • Chronic low back pain
  • Gout

Pharamcological Action

Etoricoxib is also known as a cyclo-oxygenase-2 inhibitor. This is because it works to relieve pain and inflammation by blocking an enzyme in the body called cyclo-oxygenase-2 (COX-2). COX-2 is involved in the production of irritant substances in the body in response to disease and injury. By blocking the action of COX-2, etoricoxib reduces the symptoms of pain and inflammation.

Dosage

For Osteoarthritis - 60 mg once a day

For Rheumatoid arthritis - 90 mg once a day

For Ankylosing spondylitis - 90 mg once a day

For the relief of gout - 120 mg once a day

Musculoskeletal pain - 60 mg once a day

Pharmacokinetics

The rate of absorption of etoricoxib is moderate when given orally and the extent of absorption is similar with oral and intravenous doses. Etoricoxib is extensively protein bound, primarily to plasma albumin, and has an apparent volume of distribution of 120 L in humans. Etoricoxib is eliminated following biotransformation to carboxylic acid and glucuronide metabolites that are excreted in urine and feces, with little of the drug (<1%) being eliminated unchanged in the urine. Etoricoxib is metabolized primarily by the cytochrome P450 (CYP) 3A4 isozyme.

Contraindications

  • Contraindicated in patients with peptic ulcers.
  • Contraindicated in patients with uncontrolled hypertension
  • Contraindicated in patients with stroke.
  • Contraindicated in patients with severe heart disease.
  • Contraindicated in patients with hypersensitivity.

Drug Interactions

  • Concomitant administration of etoricoxib and warfarin causes morbidity and potentially fatal bleeding, as it increases the anti-blood clotting effect of warfarin.
  • Etoricoxib, when taken with ACE inhibitors increased the risk of renal impairment.
  • Concomitant intake of etoricoxib and diuretics increases the risk of nephrotoxicity.
  • Etoricoxib increases the risk of toxicity of methotrexate when taken concomitantly as it reduces its excretion.
  • Increased risk of bleeding when taken with venlafaxine.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Weakness and fatigue
  • Dizziness
  • Flu-like symptoms
  • Diarrhea
  • Indigestion (dyspepsia)
  • Stomach pain
  • Heartburn
  • Flatulence
  • Nausea
  • Alteration of liver-related blood tests
  • Headache
  • Edema and increased blood pressure
  • Palpitations

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Abdominal swelling
  • Chest pain
  • Swelling of the face
  • Changes of kidney-related blood or urine tests
  • Heart failure
  • Myocardial infarction
  • Cerebral infarction
  • Mini stroke (transient ischemic attacks)
  • Abnormal heart rhythm (atrial fibrillation)
  • Change in bowel movement pattern

Very Rare (affecting less than 1 in 10,000)

  • Low blood sodium level
  • Allergic reactions
  • Bronchospasm
  • Severe skin reactions
  • Severe kidney problems
  • Severe increase in blood pressure
  • Confusion
  • Hallucinations

Precautions

  • Avoid in patients who have or had history of angina, heart attack or a blocked artery in heart, narrow or blocked arteries of the extremities.
  • Avoid in patients suffering from kidney disease, liver disease.
  • Avoid in pregnant women or women having breast feeding.
  • Don’t use in patients having allergic reaction and infection to etoricoxib.
  • Avoid excess dosage of etoricoxib.

Clinic Evidence

  • In 12-week placebo and active comparator-controlled period of a randomized, double-blind study, patients were treated with etoricoxib 60 mg once daily (n = 224), naproxen 500 mg twice daily (n = 221), or placebo (n = 56). Etoricoxib 60 mg demonstrated efficacy significantly superior to placebo (p < or = 0.005) and comparable to naproxen 500 mg twice daily as assessed. Treatment effects were evident by day 2, maximal by week 2, and sustained over the entire 12 weeks. Etoricoxib was well tolerated for 12 weeks. Results showed etoricoxib have rapid and durable treatment effects in patients with OA of knee or hip and was generally well tolerated.1
  • In a randomized, double blind, active comparator controlled trial of 142 men and eight women aged 18 years or over with clinically diagnosed acute gout within 48 hours of onset, etoricoxib 120 mg was administered orally once daily for 8 days. Results concluded that etoricoxib 120 mg once daily provides rapid and effective treatment for acute gouty arthritis comparable to indomethacin 50 mg three times daily. Etoricoxib was generally safe and well tolerated in this study.2

References

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