Bufexamac
Encyclopedia
Bufexamac is a drug used as an anti-inflammatory
agent on the skin, as well as rectally. Common brand names include Paraderm and Parfenac.
of the skin, including atopic eczema, as well as sunburn
and other minor burns, and itch
ing. Suppositories containing bufexamac in combination with local anaesthetics are used against haemorrhoids.
, which would make it an non-steroidal anti-inflammatory drug
. Evidence on the mechanism of action is scarce.
Furthermore, bufexamac was identified as a specific inhibitor of class IIB histone deacetylase
s (HDAC6
and HDAC10
), which may contribute to its clinical efficacy.
which is often hard to distinguish from the initial condition. As a consequence, the European Medicines Agency
recommended to withdraw the marketing approval in April 2010.
Anti-inflammatory
Anti-inflammatory refers to the property of a substance or treatment that reduces inflammation. Anti-inflammatory drugs make up about half of analgesics, remedying pain by reducing inflammation as opposed to opioids, which affect the central nervous system....
agent on the skin, as well as rectally. Common brand names include Paraderm and Parfenac.
Indications
Ointments and lotions containing bufexamac are used for the treatment of subacute and chronic eczemaEczema
Eczema is a form of dermatitis, or inflammation of the epidermis . In England, an estimated 5.7 million or about one in every nine people have been diagnosed with the disease by a clinician at some point in their lives.The term eczema is broadly applied to a range of persistent skin conditions...
of the skin, including atopic eczema, as well as sunburn
Sunburn
A sunburn is a burn to living tissue, such as skin, which is produced by overexposure to ultraviolet radiation, commonly from the sun's rays. Usual mild symptoms in humans and other animals include red or reddish skin that is hot to the touch, general fatigue, and mild dizziness. An excess of UV...
and other minor burns, and itch
Itch
Itch is a sensation that causes the desire or reflex to scratch. Itch has resisted many attempts to classify it as any one type of sensory experience. Modern science has shown that itch has many similarities to pain, and while both are unpleasant sensory experiences, their behavioral response...
ing. Suppositories containing bufexamac in combination with local anaesthetics are used against haemorrhoids.
Pharmacology
Bufexamac is thought to act by inhibiting the enzyme cyclooxygenaseCyclooxygenase
Cyclooxygenase is an enzyme that is responsible for formation of important biological mediators called prostanoids, including prostaglandins, prostacyclin and thromboxane. Pharmacological inhibition of COX can provide relief from the symptoms of inflammation and pain...
, which would make it an non-steroidal anti-inflammatory drug
Non-steroidal anti-inflammatory drug
Nonsteroidal anti-inflammatory drugs, usually abbreviated to NSAIDs or NAIDs, but also referred to as nonsteroidal anti-inflammatory agents/analgesics or nonsteroidal Anti-inflammatory medicines , are drugs with analgesic and antipyretic effects and which have, in higher doses, anti-inflammatory...
. Evidence on the mechanism of action is scarce.
Furthermore, bufexamac was identified as a specific inhibitor of class IIB histone deacetylase
Histone deacetylase
Histone deacetylases are a class of enzymes that remove acetyl groups from an ε-N-acetyl lysine amino acid on a histone. This is important because DNA is wrapped around histones, and DNA expression is regulated by acetylation and de-acetylation. Its action is opposite to that of histone...
s (HDAC6
HDAC6
Histone deacetylase 6 is an enzyme that in humans is encoded by the HDAC6 gene.-Interactions:HDAC6 has been shown to interact with HDAC11 and Zinc finger and BTB domain-containing protein 16.-Further reading: -External links:...
and HDAC10
HDAC10
Histone deacetylase 10 is an enzyme that in humans is encoded by the HDAC10 gene.-Interactions:HDAC10 has been shown to interact with Histone deacetylase 2 and Nuclear receptor co-repressor 2....
), which may contribute to its clinical efficacy.
Side effects
Bufexamac can cause severe contact dermatitisContact dermatitis
Contact dermatitis is a term for a skin reaction resulting from exposure to allergens or irritants . Phototoxic dermatitis occurs when the allergen or irritant is activated by sunlight....
which is often hard to distinguish from the initial condition. As a consequence, the European Medicines Agency
European Medicines Agency
The European Medicines Agency is a European agency for the evaluation of medicinal products. From 1995 to 2004, the European Medicines Agency was known as European Agency for the Evaluation of Medicinal Products.Roughly parallel to the U.S...
recommended to withdraw the marketing approval in April 2010.