Aceclofenac & Thiocolchicoside

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 [A19667, A19668, A19670]. Aceclofenac potently inhibits the cyclo-oxygenase 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 [A19667]. It displays high permeability to penetrate into synovial joints where in patients with osteoarthritis and related conditions, the loss of articular cartilage in the area causes joint pain, tenderness, stiffness, crepitus, and local inflammation [A19666]. Aceclofenac is also reported to be effective in other painful conditions such as dental and gynaecological conditions [A19672]. In 1991, aceclofenac was developed as an analog of a commonly prescribed NSAID, [DB00586], via chemical modification in effort to improve the gastrointestinal tolerability of the drug. It is a more commonly prescribed drug in Europe.

Thiocolchicoside is a muscle relaxant with anti-inflammatory and analgesic effects. It acts as a competitive GABAA receptor antagonist and also glycine receptor antagonist with similar potency and nicotinic acetylcholine receptors to a much lesser extent. It has powerful convulsant activity and should not be used in seizure-prone individuals.

Adverse Effects:
The most common adverse reactions were somnolence, nasopharyngitis, fatigue, dry mouth and pharyngitis, and most were mild to moderate in intensity.

Thiocolchicoside 

Has been shown to cause chromosomal aneuploidy and male infertility. Should be avoided during all stages of pregnancy, lactation and puberty. Is a potential risk factor for cancer.

Some common adverse effects include gastro-intestinal disorders (dyspepsia, abdominal pain, nausea), rash, ruber, urticaria, symptoms of enuresis, headache, dizziness, and drowsiness [L869]. Oral LD50 value in rats is 130 mg/kg [MSDS].

Thiocolchicoside For the treatment of muscle spasms.