Alclofenacum
Alclofenacum Uses, Dosage, Side Effects, Food Interaction and all others data.
Alclofenacum is a non-steroidal anti-inflammatory drug. It was withdrawn from the market in the United Kingdom in 1979.
| Trade Name | Alclofenacum |
| Generic | Alclofenac |
| Alclofenac Other Names | Alclofénac, Alclofenac, Alclofenaco, Alclofenacum, Alclophenac |
| Type | |
| Formula | C11H11ClO3 |
| Weight | Average: 226.66 Monoisotopic: 226.0396719 |
| Protein binding | The binding to plasma proteins is 90-99%. |
| Groups | Approved, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Alclofenacum is indicated in rheumatology, in particular for the treatment of rheumatoid arthritis, ankylosing spondylitis and, as an analgesic, in painful arthritic pathologies.
How Alclofenacum works
Alclofenacum is an inhibitor of prostaglandin H2 synthase. The inhibition of the enzyme occurs through the reversible block of cyclooxygenase enzyme. Therefore, it prevents the production of inflammatory mediators (and pain) as prostacyclins and prostaglandins. Aclofenac has the ability to inhibit the biosynthesis of prostaglandins which may be an important factor in the action of these drugs, but in addition, the effect of these agents in displacing endogenous anti-inflammatory substances from plasma protein binding sites is thought to be an equally important effect in their mechanism of action
Toxicity
The lethal dose
orally: 1100 (mice), 1050 (rats) mg / kg ;
under the skin: 600 (mice), 630 (rats) mg / kg
intraperitoneally: 550 (mice), 530 (rats) mg / kg
Volume of Distribution
The volume of distribution is 0.1 L / kg
Elimination Route
The absorption of alclofenac from the gastrointestinal tract is irregular. After oral or rectal administration maximum plasma concentrations are reached within 1-4 hours.
Half Life
The plasma half-life varies between 1.5 and 5.5 hours.
Clearance
For oral dose of 500mg: Renal clearance constant (av) 35ml/min Overall clearance constant (av) 37-69ml/min
Elimination Route
Alclofenacum is excreted in the urine mainly as glucuronide and as unchanged active substance.
Innovators Monograph
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