Lumiracoxib

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Lumiracoxib

Lumiracoxib is a COX-2 selective inhibitor non-steroidal anti-inflammatory drug. It belongs to the class of organic compounds known as phenylacetic acid derivatives. It is widely used in the treatment of patients suffering from osteoarthritic pain

Introduction

Lumiracoxib is a COX-2 selective inhibitor non-steroidal anti-inflammatory drug. It belongs to the class of organic compounds known as phenylacetic acid derivatives. It is widely used in the treatment of patients suffering from osteoarthritic pain

Pharmacological class: NSAID

Indications

  • Osteoarthritis
  • Rheumatoid arthritis

Pharamcological Action

The mechanism of action of lumiracoxib involves the inhibition of prostaglandin synthesis via inhibition of cyclo-oxygenase-2 (COX-2) enzyme. Lumiracoxib does not inhibit COX-1 at therapeutic concentrations.

Dosage

Osteoarthritis: 100 to 400 mg orally per day

Rheumatoid arthritis: 200 to 400 mg orally per day

Pharmacokinetics

Lumiracoxib is rapidly absorbed, achieves mean plasma concentrations >1 microg/ml within 1 h of dosing. Unchanged drug in plasma accounts for 81 to 91% of radioactivity up to 2.5 h post dose, suggesting a modest first-pass effect; unchanged drug is the major circulating component in plasma, accounting for approximately 43% of AUC (0 to 24 h). The terminal half-life of lumiracoxib in plasma is found to be 6.5 h. Major plasma metabolites are the 5-carboxy, 4'-hydroxy, and 4'-hydroxy-5-carboxy derivatives. Excretion involves both renal (54.1%) and fecal (42.7%) routes, and dose recovery is almost complete (96.8%). It is extensively metabolized before excretion, with little unchanged drug in urine (3.3% of dose) or feces (2.0% of dose).

Contraindications

  • Contraindicated in patients with ischemic heart disease, cerebrovascular disease, or peripheral arterial disease.
  • Contraindicated in patients with history of drug-induced increases in transaminase values >3 times the upper limit of normal (ULN) or in those taking other drugs known to cause clinically significant hepatotoxicity.
  • Contraindicated in patients with inflammatory bowel disease, moderate to severe heart failure (NYHA class II-IV). 

Drug Interactions

  • May decrease the clearance of CYP2C9 substrates (e.g. phenytoin, warfarin).
  • May increase anticoagulant effect of warfarin, acenocoumarol, anisindione and dicoumarol.
  • Concomitant use with telmisartan may increase the risk of acute renal failure and hyperkalemia.
  • Tolbutamide may decrease the metabolism and clearance of lumiracoxib.
  • May antagonize the antihypertensive effect of timolol. May increase lithium serum levels.
  • May decrease antihypertensive effect of trandolapril.

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Abdominal pain
  • Acute pharyngitis
  • Constipation
  • Diarrhea
  • Dizziness
  • Dry cough
  • Dyspepsia
  • Fatigue
  • Headache
  • Influenza-like symptoms
  • Nausea
  • Edema
  • Urinary tract infection

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Abdominal distension
  • Acute myocardial infarction
  • Blocked sinuses
  • Blurred Vision
  • Chest pain
  • Dysphagia
  • Dyspnea
  • Frequency of micturition
  • Gingivitis
  • Insomnia
  • Migraine
  • Peptic ulcer symptoms
  • Rash

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

  • Acute cholecystitis
  • Acute hepatitis
  • Acute renal failure
  • Anaphylactic shock
  • Cardiac conduction disorders
  • Cholelithiasis
  • Gastrointestinal hemorrhage
  • Heart failure
  • Hyperglycemia
  • Keratitis
  • Leucopenia
  • Nephrotic syndrome
  • Neutropenia
  • Pancytopenia 

Precautions

  • Avoid in patients with asthma
  • Avoid in patients who have wheezing or difficulty breathing after taking medication like aspirin or non-steroidal anti-inflammatory drugs
  • Avoid in patients with stomach or duodenal ulcer
  • Avoid in patients with heart disease
  • Avoid in patients with liver or kidney disease
  • Avoid in patients with high blood pressure

Clinic Evidence

In a 13-week, multicenter, randomized, double-blind, double-dummy, placebo-controlled study, males or females aged >/= 18 years with primary knee OA received lumiracoxib 100 mg od, lumiracoxib 100 mg od with a loading dose of 200 mg od for the first two weeks, celecoxib 200 mg od, or placebo. All active treatments were superior to placebo for all co-primary variables. No significant differences were observed between any active treatments. Mean reductions from baseline to week 13 for lumiracoxib 100mg od, 100mg od with loading dose, celecoxib and placebo, respectively, were: OA pain intensity in the target knee: 26.8, 26.2, 26.6 and 21.4mm (all p < 0.01 vs. placebo); patient's global assessment of disease activity: 25.1, 21.9, 22.9 and 18.9 mm (all p < 0.05 vs. placebo); WOMAC total score: 15.2, 14.8, 14.7 and 11.3 (all p < 0.01 vs. placebo). Lumiracoxib was superior to placebo and similar to celecoxib for OMERACT-OARSI response and WOMAC subscale scores. Lumiracoxib was well tolerated.1

References

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