Bromfenac

Bromfenac is a non-steroidal anti-inflammatory agent and is used locally on the eye after cataract surgery to treat ocular inflammation. The substance exhibits an anti-inflammatory effect. This surgery is mainly performed on elderly patients suffering from lens opacity (cataract) that develops with age. The effect of Bromfenac is due to the inhibition of prostaglandins, which are involved in local pain mediation as well as inflammatory processes, among others.

Uses and indications

Bromfenac is commercially available as a solution in the form of eye drops under the name Yellox®.

The eye drops are applied to the affected eye twice a day (in the morning and in the evening) at the rate of one drop on the day after surgery. This dose, as well as the use of this drug for a period of two weeks, should not be exceeded.

History

In Japan, bromfenac has been available in the form of eye drops since 2000.

The drug was approved by the FDA for ophthalmic use in the United States under Xibrom in 2005. Prior to this, in 1997, it was available on the market as an oral pain reliever under the name Duract. However, this was withdrawn only after a year because many patients took it for more than the recommended maximum 10-day period. As a result, it was reported to have caused hepatotoxicity (liver toxicity) according to numerous reports.

Bromfenac has also been available as eye drops in the EU since 2011 and is now available worldwide.

Pharmacodynamics/mechanism of action

As a non-steroidal anti-inflammatory drug, bromfenac blocks the generation of prostaglandins by inhibiting cyclooxygenase. Cyclooxygenase is an enzyme that synthesizes the prostaglandins involved in the generation of pain during inflammation. A distinction is made between COX-1, which is expressed almost ubiquitously in the healthy organism, and COX-2, which is increasingly expressed in damaged and inflamed tissue. COX-2 then forms the prostaglandins in these tissues that maintain or increase inflammation there.

Bromfenac inhibits COX-1 only slightly, but inhibits COX-2 much more strongly. By inhibiting COX-2, prostaglandins are not produced and thus the inflammatory process is alleviated.

Pharmacokinetics

Bromfenac is structurally derived from the non-steroidal anti-inflammatory drug amfenac by an additional bromine atom. Of these, bromfenac is characterized by a higher lipophilicity, which plays a crucial role in its action. Meanwhile, bromfenac is absorbed within only 15 minutes after application, as it is very well absorbed by the cornea as well as by the ocular tissue behind it.

After 150-180 minutes of a single dose, the maximum concentration of the active ingredient is reached in the aqueous humor, which is located in the anterior and posterior chambers of the eye. These maximum levels are maintained for twelve hours.

The active ingredient is almost completely bound to plasma proteins.

It is metabolized mainly by the enzyme CYP2C9 and subsequently excreted in the urine.

Interactions

With the current state of science, no interactions are known.

Contraindications & precautions

The drug should not be used in case of allergy to bromfenac or any other ingredient of the formulation and should not be used in that case.

Simultaneous use of bromfenac with other NSAIDs such as acetylsalicylic acid or ibuprofen may cause asthma, skin allergy or severe nasal inflammation. If this is the case, the drug must not be used as well. Therefore, initial caution is advised.

If steroids such as cortisone are used at the same time, this may lead to undesirable side effects.

Furthermore, caution is advised in case of:

• Bleeding disorders or if medicines that may prolong bleeding time such as warfarin or acetylsalicylic acid have been taken in the past.
• existing eye problems
• Diabetes (diabetes )
• rheumatoid arthritis
• repeated eye surgery within a short period of time

Yellox® should not be used in children and adolescents!

Before taking Yellox® with other medicines, a doctor or pharmacist should be consulted for preliminary clarification.

Side effects

The side effects listed below may or may not occur. On the whole, Bromfenac eye drops are well tolerated.

Side effects that may occasionally occur include:

• Foreign body sensation in the eye
• Redness and inflammation of the eye
• Itching, irritation or pain of the eye
• Swelling or bleeding of the eyelid
• Impaired vision
• Moving spots in front of the eyes
• Decreasing vision
• Eye discomfort
• Light discomfort
• Limited or blurred vision
• Facial swelling

In rare cases, ocular surface damage or asthma may also occur.

Pregnancy and lactation

During pregnancy, administration of the drug Yellox® with the active ingredient bromfenac is allowed only if the doctor prescribes it, but it is generally not recommended. In the last three months of pregnancy, administration is not allowed. Nursing mothers are allowed to use Yellox®.