Bufexamac is a drug used as an

anti-inflammatory Anti-inflammatory is the property of a substance or treatment that reduces inflammation, fever or swelling. Anti-inflammatory drugs, also called anti-inflammatories, make up about half of analgesics. These drugs reduce pain by inhibiting mechan ...

agent on the skin, as well as

rectal The rectum (: rectums or recta) is the final straight portion of the large intestine in humans and some other mammals, and the Gastrointestinal tract, gut in others. Before expulsion through the anus or cloaca, the rectum stores the feces te ...

ly. Common brand names include Paraderm and Parfenac. It was withdrawn in Europe and Australia because of allergic reactions.

Indications

Ointments and lotions containing bufexamac are used for the treatment of subacute and chronic

eczema Dermatitis is a term used for different types of skin inflammation, typically characterized by itchiness, redness and a rash. In cases of short duration, there may be small blisters, while in long-term cases the skin may become thickened ...

of the skin, including atopic eczema, as well as

sunburn Sunburn is a form of radiation burn that affects living tissue, such as skin, that results from an overexposure to ultraviolet (UV) radiation, usually from the Sun. Common symptoms in humans and other animals include red or reddish skin tha ...

and other minor burns, and

itch An itch (also known as pruritus) is a sensation that causes a strong desire or reflex to scratch. Itches have resisted many attempts to be classified as any one type of sensory experience. Itches have many similarities to pain, and while both ...

ing.

Suppositories A suppository is a dosage form used to deliver pharmaceutical drug, medications by insertion into a body orifice (any opening in the body), where it dissolves or melts to exert local or systemic effects. There are three types of suppositories, eac ...

containing bufexamac in combination with

local anaesthetic A local anesthetic (LA) is a medication that causes absence of all sense, sensation (including pain) in a specific body part without loss of consciousness, providing local anesthesia, as opposed to a general anesthetic, which eliminates all sen ...

s are used against haemorrhoids.

Pharmacology

Bufexamac is thought to act by inhibiting the enzyme

cyclooxygenase Cyclooxygenase (COX), officially known as prostaglandin-endoperoxide synthase (PTGS), is an enzyme (specifically, a family of isozymes, ) that is responsible for biosynthesis of prostanoids, including thromboxane and prostaglandins such a ...

, which would make it a

non-steroidal anti-inflammatory drug Non-steroidal anti-inflammatory drugs (NSAID) are members of a therapeutic drug class which reduces pain, decreases inflammation, decreases fever, and prevents blood clots. Side effects depend on the specific drug, its dose and duration of ...

. Evidence on the mechanism of action is scarce. Furthermore, bufexamac was identified as a specific inhibitor of class IIB

histone deacetylase Histone deacetylases (, HDAC) are a class of enzymes that remove acetyl groups (O=C-CH3) from an ε-N-acetyl lysine amino acid on both histone and non-histone proteins. HDACs allow histones to wrap the DNA more tightly. This is important becaus ...

s ( HDAC6 and HDAC10).

Side effects

Bufexamac can cause severe

contact dermatitis Contact dermatitis is a type of acute or chronic inflammation of the skin caused by exposure to chemical or physical agents. Symptoms of contact dermatitis can include itchy or dry skin, a red rash, bumps, blisters, or swelling. These rashes ...

which is often hard to distinguish from the initial condition. As a consequence, the

European Medicines Agency The European Medicines Agency (EMA) is an agency of the European Union (EU) in charge of the evaluation and supervision of pharmaceutical products. Prior to 2004, it was known as the European Agency for the Evaluation of Medicinal Products ...

recommended to withdraw the marketing approval in April 2010.

References

{{Prostanoidergics Anti-inflammatory agents Hydroxamic acids Phenol ethers Withdrawn drugs