Bufexamac

Bufexamac is Non-steroidal Anti inflammatory drug belonging to anti-pyretic agents.

Bufexamac is used in the treatment of various skin conditions, such as atopic eczema and other inflammatory dermatoses.

Bufexamac can be absorbed through intact skin but has limited systemic absorption. It primarily acts locally at the site of application. Bufexamac remains primarily in the tissues near the site of application. It does not exhibit significant distribution throughout the body. Bufexamac undergoes metabolism in the skin tissues. The exact metabolic pathways and metabolites produced are not extensively studied or well-documented. Bufexamac is eliminated from the body primarily through the urine and feces. The elimination half-life of bufexamac is relatively short, typically ranging from a few hours to a day.

Bufexamac is available in creams or ointments

Bufexamac is available in India, Germany, Canada, France, USA.

Bufexamac 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, bufexamac 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 . Bufexamac is unlikely to have any effect on wound healing.

Bufexamac is available in the form of creams or ointments.

Bufexamac is used in the treatment of various skin conditions, such as atopic eczema and other inflammatory dermatoses.

Bufexamac is approved for use in the following clinical indications

Various skin conditions, such as atopic eczema and other inflammatory dermatoses.

Bufexamac is available in the dosage strength of 1%, 5 %

Bufexamac is available in the form of creams or ointments.

Bufexamac is contraindicated in patients with:

Hypersensitivity (eg, anaphylactic reaction) to Bufexamac or any component of the formulation.

• Allergy or sensitivity: Some individuals may be allergic or hypersensitive to bufexamac or other components of the formulation. Open wounds or damaged skin: Bufexamac should not be applied to open wounds, broken skin, or areas with extensive skin damage, as it may be absorbed more readily and potentially cause systemic effects.
• Skin irritation or sensitization: Bufexamac can cause skin irritation or sensitization in some individuals.
• Avoid contact with eyes and mucous membranes: Bufexamac should not come into contact with the eyes or mucous membranes. If accidental contact occurs, rinse thoroughly with water.
• Use in pregnancy and breastfeeding: Limited information is available regarding the use of bufexamac during pregnancy or while breastfeeding. It is recommended to consult with a healthcare professional before using bufexamac in these situations.
• Drug interactions: Bufexamac is primarily used topically, which reduces the likelihood of significant drug interactions.
• Pediatric use: Safety and effectiveness of bufexamac in pediatric populations have not been well-established.

Bufexamac may cause liver problems, and using it with substantial quantities of ethanol may increase that risk.

Bufexamac is used off label to enhance leflunomide elimination. Use of the enhanced elimination procedure is recommended in all females of reproductive potential upon discontinuation of leflunomide. Pregnancy should be avoided until undetectable serum concentrations (<0.02 mg/L) of leflunomide are verified.

• Common Adverse effects:

Nausea, vomiting; redness of rectal mucus membranes

• Less Common Adverse effects:

Rash, pruritus, erythema, urticaria.

Vascular disorders: Hypotension, hypertension, flushing.

• Rare Adverse effects

Insomnia, anxiety.

The common side effects of Bufexamac include the following :

Severe contact dermatitis

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 .

• Pharmacodynamic

Bufexamac is a para-aminophenol derivative that exhibits analgesic and antipyretic actions and weak anti-inflammatory activity. The mechanism of its analgesic effect has not been fully determined but may be associated with the inhibition of prostaglandin synthesis in the CNS and to a lesser extent, through peripheral blockage of pain-impulse generation. It produces antipyresis by inhibiting the hypothalamic heat-regulating centre.

• Pharmacokinetics

Absorption: Bufexamac can be absorbed through intact skin but has limited systemic absorption. It primarily acts locally at the site of application.

Distribution: Bufexamac remains primarily in the tissues near the site of application. It does not exhibit significant distribution throughout the body.

Metabolism: Bufexamac undergoes metabolism in the skin tissues. The exact metabolic pathways and metabolites produced are not extensively studied or well-documented.

Elimination: Bufexamac is eliminated from the body primarily through the urine and feces. The elimination half-life of bufexamac is relatively short, typically ranging from a few hours to a day.

1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC1364710/
2. https://reference.medscape.com/drug/colestid-Bufexamac -342452
3. https://go.drugbank.com/drugs/DB00375
4. https://www.sciencedirect.com/topics/medicine-and-dentistry/Bufexamac
5. https://europepmc.org/article/med/6988203