Description

Aceclofenac  (NSAID of BCS Class II)

• A phenylacetic acid derivative with anti-inflammatory and analgesic properties.

• Highly (>99%) protein bound possessed with poor aqueous solubility circulates mainly as unchanged drug.

• Has additional properties to inhibit the synthesis of inflammatory cytokines such as interleukin-1 (IL-1), tumor necrosis factor (TNF), and Prostaglandin E2 (PGE2).

[Note: (1) TNF may promote cancer development and progression. (2) IL-1 causes fever by affecting areas of brain. (3) PGE2 causes redness, swelling, and pain.]

Mechanism

• Its mechanism of action is based on the inhibition of prostaglandin production by selectively inhibiting COX-2.

• In contrast to some other NSAIDs, aceclofenac has shown stimulatory effects on cartilage matrix synthesis.

Management of pain and inflammation

• Improved functional capacity in adults with radiologically confirmed OA; reduced joint tenderness, swelling, and erythema, and improved knee flexion and extension.

• Reduction in pain intensity from baseline almost equivalent to its competing NSAIDs diclofenac, nabumetone, naproxen, piroxicam, and paracetamol.

• Reduces joint inflammation, pain intensity and the duration of morning stiffness in patients with rheumatoid arthritis; also effective in other painful conditions (e.g. dental and gynaecological).

Safety and efficacy

• Well-tolerated, and well-accepted therapy for both acute and chronic inflammatory and degenerative diseases.

• Better tolerated than several other NSAIDs, including naproxen, piroxicam, indomethacin, and ketoprofen.

• A tolerability profile generally similar to that of tenoxicam and paracetamol.

• Significantly lower incidence of GI adverse effects compared with other NSAIDs, which may result in lower withdrawal rates and increased treatment compliance.