Aceclofenac

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DRUGS
Aceclofenac

Aceclofenac is an anti-inflammatory drug provides symptomatic relief in a variety of painful inflammatory conditions such as osteoarthritis, rheumatoid arthritis  and ankylosing spondylitis. It is well tolerated with improved gastrointestinal tolerability relative to other NSAIDs.

Introduction

Aceclofenac is an anti-inflammatory drug provides symptomatic relief in a variety of painful inflammatory conditions such as osteoarthritis, rheumatoid arthritis and ankylosing spondylitis. It is well tolerated with improved gastrointestinal tolerability relative to other NSAIDs.

Indications

  • Mild to moderate pain
  • Headache
  • Fever
  • Ankylosing spondylitis
  • Osteoarthritis
  • Rheumatoid arthritis
  • Lower back pain
  • Dental pain
  • Primary dysmenorrhea

Pharamcological Action

Aceclofenac is the glycolic acid ester of diclofenac and inhibits synthesis of the inhibitory cytokines interleukin-1b and tumor necrosis factor, and inhibits prostaglandin E2 production. It is also effective in reducing non-inflammatory pain. It has also shown stimulatory effects on cartilage matrix synthesis that may be linked to the ability of the drug to inhibit Interleukin-1 activity.

Dosage

Adult: 100 mg twice daily

100 mg daily in patients with hepatic impairment

Note: Not for use by children

Pharmacokinetics

Aceclofenac is rapidly and completely absorbed after oral administration and is extensively bound to plasma proteins. Peak plasma concentrations are reached within 1.25-3 hours following ingestion. It diffuses into synovial fluid after multiple dosing. The volume of distribution is about 25L. It is metabolized in renal with 70 to 80% of an administered dose found in the urine, mainly as the glucuronides of aceclofenac and its metabolites. The plasma elimination half life is approximately 4 hours and 2/3 of the administered dose is excreted via the urine, mainly as hydroxymetabolites.

Contraindications

  • Patients with active or history of recurrent peptic ulcer/or Gastrointestinal bleeding and moderate or severe renal impairment.
  • Patients with established congestive heart failure, ischemic heart disease, peripheral arterial disease and/or cerebrovascular disease
  • It should not be given to pregnant or breast-feeding mothers

Drug Interactions

  • Increased risk of plasma concentrations of lithium and digoxin
  • Increased nephrotoxicity when used with diuretics or cyclosporine
  • Increased risk of convulsion with quinolones
  • Increase risk of methotrexate toxicity when administered within
  • 24 hr of methotrexate administration

Side effects

Common (affecting between 1 in10 to 1 in 100)

  • Dizziness
  • Nausea
  • Diarrhea
  • Dyspepsia
  • Abdominal Pain
  • Flatulence

Uncommon (affecting 1 in 100 to 1 in 1000)

  • Constipation
  • Gastritis
  • Ulcerative stomatitis
  • Vomiting
  • Mouth Ulcers
  • Itching
  • Rash
  • Dermatitis
  • Increase in blood urea nitrogen
  • Increase in blood creatinine levels

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

  • Low levels of iron in the blood
  • Hypersensitivity (allergic reaction)
  • Visual disturbance
  • Shortness of breath
  • Ringing in the ears
  • Aseptic meningitis

Precautions

  • Should be given with caution to elderly patients with hepatic, renal or cardiovascular impairment and those are on other medication
  • Caution should be taken in patients with a history of hypertension and/or mild to moderate congestive heart failure, peptic ulcer, gastrointestinal toxicity, Crohn’s disease and systemic lupus erythematosus
  • It may cause dizziness or drowsiness. Driving a car or operating a machinery while taking this medication is not advised

Clinic Evidence

  • The data from in vitro studies indicate properties of particular interest with respect to cartilage matrix effects and selectivity for cyclo-oxygenase-2 have shown aceclofenac to be an effective agent in the management of pain and rheumatic disease. Its analgesic and anti-inflammatory properties provides symptomatic relief in a variety of painful conditions. In patients with osteoarthritis of the knee, the drug decreases pain, reduces disease severity and improves the functional capacity of the knee.1
  • Aceclofenac is effective in the treatment of painful inflammatory diseases and also provides effective analgesia in other indications, such as dental or gynecological pain, lower back pain and ear, nose and throat indications. The good tolerability profile of aceclofenac results in a reduced withdrawal rate and hence greater compliance with treatment.2

References

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