Product Information
Registration Status: ActiveSIN15700P
AIRTAL FILM COATED TABLETS 100mg is approved to be sold in Singapore with effective from 2019-05-29. It is marketed by ZUELLIG PHARMA PTE LTD, with the registration number of SIN15700P.
This product contains Aceclofenac 100mg in the form of TABLET, FILM COATED. It is approved for Not Available use.
This product is manufactured by Industrias Farmaceuticas Almirall. S.A. (IFA) in SPAIN.
It is a Prescription Only Medicine that can only be obtained from a doctor or a dentist, or a pharmacist with a prescription from a Singapore-registered doctor or dentist.
Product Reference
Important Note: For generic product, the SPC/PIL provided may not be brand specific.
{{/items}} {{^items}}Description
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.
Indication
Indicated for the relief of pain and inflammation in osteoarthritis, rheumatoid arthritis and ankylosing spondylitis.
Mechanism of Action
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 [A19671]. 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 [A19667]. 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 [A19673]. 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 [A19666]. The chrondroprotective effects are generated by 4'-hydroxyaceclofenac which suppresses IL-1 mediated production of promatrix metalloproteinase-1 and metalloproteinase-3 and interferes with the release of proteoglycan from chrondrocytes [A19666, A19667, A19672].
Pharmacokinetics
- Absorption
- Aceclofenac is rapidly and completely absorbed from the gastrointestinal tract and circulates mainly as unchanged drug following oral administration. Peak plasma concentrations are reached around 1.25 to 3 hours post-ingestion, and the drug penetrates into the synovial fluid where the concentration may reach up to 60% of that in the plasma [L868]. There is no accumulation in regular dosing, with similar maximum plasma concentration (Cmax) and time to reach peak plasma concentration (Tmax) after single and multiple doses [A19667].
- Distribution
- The volume of distribution is approximately 25 L [L868].
- Metabolism
- 4'-hydroxyaceclofenac is the main metabolite detected in plasma however other minor metabolites include diclofenac, 5-hydroxyaceclofenac, 5-hydroxydiclofenac, and 4'-hydroxydiclofenac [A19667]. It is probable that the metabolism of aceclofenac is mediated by CYP2C9 [A19674].
- Elimination
Clearance
The mean clearance rate is approximately 5 L/h [A19674].
Toxicity
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].
Active Ingredient/Synonyms
2-[(2,6-dichlorophenyl)amino]benzeneacetic acid carboxymethyl ester | 2-[(2,6-dichlorophenyl)amino]phenylacetoxyacetic acid | 2-[(2',6'-dichlorophenyl)amino]phenylacetoxyacetic acid | Aceclofenac | acéclofénac | Aceclofenac betadex | Aceclofenaco | Aceclofenacum | glycolic acid [o-(2,6-dichloroanilino)phenyl]acetate ester | Aceclofenac |
Source of information: Drugbank (External Link). Last updated on: 3rd July 18. *Trade Name used in the content below may not be the same as the HSA-registered product.