Bufexamic Acid
Bufexamic Acid Uses, Dosage, Side Effects, Food Interaction and all others data.
Bufexamic Acid is a non-steroidal anti-inflammatory drug (NSAID) under the market name Droxaryl, Malipuran, Paraderm and Parfenac. It is typically administered topically for the treatment of subacute and chronic eczema of the skin, including atopic eczema and other inflammatory dermatoses, as well as sunburn and other minor burns, and itching. It has also been used in suppositories in combination with local anaesthetics indicated for haemorrhoids. The use of bufexamac has been discontinued in Canada and the United States, which may be due to undetermined clinical efficacy and a high prevalence of contact sensitization . Bufexamic Acid was also withdrawn by the EMA in April 2010.
Bufexamic Acid is a topically-active anti-inflammatory agent that inhibits the cyclooxygenase enzyme. In cutaneous and deep experimental inflammation, topical administration of bufexamac exerted a dose-related anti-inflammatory effect . In guinea pigs, bufexamax was shown to be more active than topical acetylsalicylic acid 5% or phenylbutazone 5% in delaying the local increase in temperature resulting from UV exposure . Bufexamic Acid is unlikely to have any effect on wound healing .
| Trade Name | Bufexamic Acid |
| Generic | Bufexamac |
| Bufexamac Other Names | Acide p-butoxyphenylacethydroxamique, Bufexamac, bufexamaco, bufexamacum, Bufexamic acid, p-Butoxyphenylacetohydroxamic acid |
| Type | |
| Formula | C12H17NO3 |
| Weight | Average: 223.272 Monoisotopic: 223.120843411 |
| Protein binding | No data available. |
| Groups | Approved, Withdrawn |
| Therapeutic Class | |
| Manufacturer | |
| Available Country | |
| Last Updated: | September 19, 2023 at 7:00 am |
Uses
Bufexamic Acid is an NSAID used to treat skin conditions like atopic eczema and inflammatory dermatoses.
Indicated for the treatment of various skin conditions, such as atopic eczema and other inflammatory dermatoses.
Bufexamic Acid is also used to associated treatment for these conditions: Anal Fissures, Hemorrhoids, Pruritus Ani
How Bufexamic Acid works
The full mechanism of action is unclear. It is proposed that bufexamac acts similarly to other non-steroidal anti-inflammatory drugs to inhibit prostaglandin biosynthesis in vitro, via inhibiting cyclo-oxygenase (COX) enzymes . Systematically administered bufexamac may accumulate preferentially in the adrenal cortex of rats and may play a role in adrenal stimulation; however its topical anti-inflammatory action is likely to be independent of this effect .
Toxicity
The LD50 in rat following oral and intraperitoneal administration is 3370 mg/kg and 805 mg/kg, respectively . Subcutaneous LD50 in mouse is >5000 mg/kg . Mild skin irritation was seen in rabbits following dermal application of 750 mg/30d(l) . Non-steroidal anti-inflammatory drug (NSAID) overdose may produce nausea, vomiting, indigestion and upper abdominal pain. Other effects may include drowsiness, dizziness, confusion, disorientation, lethargy .
Food Interaction
No interactions found.Volume of Distribution
No data available.
Elimination Route
Method of application affects the extent of cutaneous absorption . Following rectal administration as suppositories, the systemic absorption was reported to be low .
Half Life
No data available.
Clearance
No data available.
Elimination Route
Following topical administration of 5% bufexamac, the recovery in the urine was 3.5% of the applied dose within 144 hours . Studies in healthy volunteers receiving an oral dose of 125 to 500 mg indicate that an average of 80% of the total dose is excreted in the urine within 48 hours .
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