Aceclofenac; Uses, Dosage, Side Effects, Interactions

Aceclofenac
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Aceclofenac is a non-steroidal anti-inflammatory drug (NSAID) with marked anti-inflammatory and analgesic properties. It is reported to have a higher anti-inflammatory action or at least comparable effects than conventional NSAIDs in double-blind studies

Aceclofenac potently inhibits the cyclooxygenase enzyme (COX) that is involved in the synthesis of prostaglandins, which are inflammatory mediators that cause pain, swelling, inflammation, and fever. It is orally administered for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis, and ankylosing spondylitis. Aceclofenac belongs to BCS Class II as it possesses poor aqueous solubility. It displays high permeability to penetrate into synovial joints wherein patients with osteoarthritis and related conditions, the loss of articular cartilage in the area causes joint pain, tenderness, stiffness, crepitus, and local inflammation.

Aceclofenac belongs to the class of non-steroidal anti-inflammatory preparations for topical use. Used in the treatment of joint and muscular pains due to it muscle relaxing action.

Mechanism of Action of Aceclofenac

Through COX-2 inhibition, aceclofenac downregulates the production of various inflammatory mediators including prostaglandin E2 (PGE2), IL-1β, and TNF from the arachidonic acid (AA) pathway. Inhibition of IL-6 is thought to be mediated by diclofenac converted from aceclofenac. The suppressed action of inflammatory cytokines decreases the production of reactive oxygen species. Aceclofenac is shown to decreased production of nitrous oxide in human articular chondrocytes. In addition, aceclofenac interferes with neutrophil adhesion to endothelium by decreasing the expression of L-selectin (CD62L), which is a cell adhesion molecule expressed on lymphocytes. Aceclofenac is proposed to stimulate the synthesis of glycosaminoglycan in human osteoarthritic cartilage which may be mediated through its inhibitory action on IL-1 production and activity. The chondroprotective effects are generated by 4′-hydroxyaceclofenac which suppresses IL-1 mediated production of matrix metalloproteinase-1 and metalloproteinase-3 and interferes with the release of proteoglycan from chondrocytes

Indications of Aceclofenac

Aceclofenac tablet is used for the treatment, control, prevention, & improvement of the following diseases, conditions, and symptoms
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Contra-Indications of Aceclofenac

Hypersensitivity to  Aceclofenac Tablet is a contraindication. In addition, Aceclofenac Tablet should not be used if you have the following conditions

Dosage of Aceclofenac 

Strengths : 100 mg , 200 mg

Ankylosing spondylitis

  • 100 mg bid, in the morning and in the evening.

Rheumatoid arthritis

  • 100 mg bid, in the morning and in the evening.

Osteoarthritis

  • 100 mg bid, in the morning and in the evening.

Side Effects of Aceclofenac

The most common

More common

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Rare

Drug Interactions of Aceclofenac

Aceclofenac may interact with following drugs, supplyments & may change the efficacy of drugs

Other NSAIDs: Concomitant therapy with aspirin or other NSAIDs may increase the frequency of adverse reactions, including the risk of GI bleeding.

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Pregnancy& Lactation of Aceclofenac

FDA Pregnancy Category C 

Pregnancy

There is no information on the secretion of aceclofenac in breast milk. The use of aceclofenac should therefore be avoided during lactation unless the potential benefits to the mother outweigh the possible risks to the children. During the third trimester of pregnancy, all prostaglandin synthesis inhibitors may expose the foetus to

  • cardiopulmonary toxicity (with premature closure of the ductus arteriosus and pulmonary hypertension);
  • renal dysfunction, which may progress to renal failure with oligo-hydramnios;

the mother and the neonate, at the end of pregnancy, to

  • possible prolongation of bleeding time, an anti-aggregating effect which may occur even at very low doses.
  • inhibition of uterine contractions resulting in delayed or prolonged labor.

Consequently, aceclofenac is contraindicated during the third trimester of pregnancy

Lactation

There is no information on the secretion of aceclofenac to breast milk; there was, however, no notable transfer of radiolabelled aceclofenac to the milk of lactating rats. The use of aceclofenac should, therefore, be avoided in pregnancy and lactation unless the potential benefits to the other outweigh the possible risks to the fetus.


  1. References

Aceclofenac

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