Prolensa

Ophthalmological Non-steroidal Anti-inflammatories

Apply topically to the eye.
Remove contact lenses before instillation of solution; lenses may be reinserted 10 minutes after administration.
Instruct patient on proper instillation of eye solution.
Do not touch the tip of the dropper to the eye, fingertips, or other surface.
If more than one ophthalmic medication is being used, separate administration by at least 5 minutes.
Do not share bottle with other patients.

ocular hypertension / Delayed / 1.0-8.0
corneal erosion / Delayed / Incidence not known
keratitis / Delayed / Incidence not known

photophobia / Early / 3.0-8.0
iritis / Delayed / 1.0-8.0
blurred vision / Early / 3.0-8.0
conjunctival hyperemia / Early / 2.0-7.0
hyphema / Delayed / Incidence not known
impaired wound healing / Delayed / Incidence not known

ocular pain / Early / 1.0-8.0
foreign body sensation / Rapid / 3.0-8.0
headache / Early / 1.0-8.0
ocular pruritus / Rapid / 2.0-7.0
ocular irritation / Rapid / 2.0-7.0

Bromday, BromSite, Prolensa, Xibrom

Rx

Ophthalmic benzene acetic acid NSAID
Used for the treatment of ocular pain and inflammation following cataract surgery
Use may result in keratitis; monitor patients closely for corneal health

One drop (0.07 mg or 0.09 mg) instilled into affected eye(s) once daily beginning 24 hours prior to cataract surgery, continued on the day of surgery, and through the first 14 days of the postoperative period.

One drop (0.09 mg) instilled into affected eye(s) twice daily beginning 24 hours after cataract surgery, continued through the first 14 days of the postoperative period.

One drop (0.075 mg) instilled into affected eye(s) twice daily beginning 1 day prior to surgery, continued on the day of surgery, and through the first 14 days of the postoperative period.

Specific guidelines for dosage adjustments of the ophthalmic solution in hepatic impairment are not available; it appears that no dosage adjustments are needed.

Specific guidelines for dosage adjustments of the ophthalmic solution in renal impairment are not available; it appears that no dosage adjustments are needed.

There are no drug interactions associated with Bromfenac products.

Bromday/Bromfenac/Bromfenac Sodium/BromSite/Prolensa/Xibrom Ophthalmic Sol: 0.07%, 0.075%, 0.09%

1 drop/day per affected eye for Bromday or Prolensa solutions; 2 drops/day per affected eye for Bromsite or Xibrom solutions.

1 drop/day per affected eye for Bromday or Prolensa solutions; 2 drops/day per affected eye for Bromsite or Xibrom solutions.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

Safety and efficacy have not been established.

The analgesic effects of bromfenac are due to the inhibition of the enzyme cyclooxygenase (COX). The enzymes COX-1 and COX-2 catalyze the conversion of arachidonic acid to prostaglandin G2 (PGG2), which is the first step in the synthesis of prostaglandins and thromboxanes that are involved in rapid physiological responses. COX isoenzymes are also responsible for a peroxidase reaction, which is not affected by NSAIDs. In addition, NSAIDs do not suppress leukotriene synthesis by lipoxygenase pathways. Because prostaglandins sensitize pain receptors, inhibition of prostaglandin synthesis (via cyclooxygenase inhibition) is believed to be responsible for the analgesic effects of bromfenac. Most NSAIDs do not alter the pain threshold or affect existing prostaglandins, so the analgesic action is most likely peripheral. The anti-inflammatory effects of bromfenac may also result from inhibition of prostaglandin synthesis as well as inhibition of leukocyte migration. Antipyresis can occur due to peripheral dilation caused by a central action on the hypothalamus. This results in an increased cutaneous blood flow and subsequent heat loss. COX-1 is constitutively expressed in almost all tissues, while COX-2 appears to only be constitutively expressed in the brain, kidney, bones, reproductive organs, and some neoplasms (e.g., colon and prostate cancers). COX-1 is responsible for prostaglandin synthesis in response to stimulation by circulating hormones, as well as maintenance of normal renal function, gastric mucosal integrity, and hemostasis. However, COX-2 is inducible in many cells in response to certain mediators of inflammation (e.g., interleukin-1, tumor necrosis factor, lipopolysaccharide, mitogens, and reactive oxygen intermediates).
•Ophthalmic Activity: Following topical application to the eye, bromfenac inhibits miosis by inhibiting the biosynthesis of ocular prostaglandins. Prostaglandins play a role in the miotic response produced during ocular surgery by constricting the iris sphincter independently of cholinergic mechanisms. In the eye, prostaglandins also have been shown to disrupt the blood-aqueous humor barrier, cause vasodilation, increase vascular permeability, promote leukocytosis, and increase intraocular pressure (IOP). The degree of ocular inflammatory response is correlated with prostaglandin-induced increases in ciliary epithelium permeability. When applied topically to the eye, NSAIDs inhibit the synthesis of prostaglandins in the iris, ciliary body, and conjunctiva. Thus, NSAIDs may prevent many of the manifestations of ocular inflammation. Bromfenac does not affect intraocular pressure or tonographic aqueous outflow resistance and does not interfere with the action of acetylcholine administered during ocular surgery. Bromfenac also does not prevent increases in intraocular pressure or decreases in aqueous outflow induced by topical corticosteroids.

Bromfenac is administered topically as an ophthalmic solution. Systemic exposure following ophthalmic administration is low. The metabolism and elimination of ophthalmically-administered bromfenac have not been characterized.
 
Affected cytochrome P450 isoenzymes: none

Ophthalmic Route
Bromfenac serum concentrations are expected to be below the quantification limit (50 ng/mL) after ophthalmic administration of 0.09 mg to each eye twice daily. Following administration of twice daily bromfenac 0.075% solution, bromfenac plasma concentrations ranged from below the limit of quantification (0.2 ng/mL) to 2.42 ng/mL at 30 to 60 minutes post-dose.

There are no data on the presence of ophthalmic bromfenac in human milk, the effects of the drug on the breast-fed infant, or the effects of the drug on milk production. Caution should be exercised if bromfenac ophthalmic solution is given to a woman who is breast-feeding. Because only very small amounts are present in systemic circulation after ophthalmic administration, the amount of drug excreted into human milk is not expected to be clinically significant. Other orally administered NSAIDs (e.g., ibuprofen) are considered compatible with breast-feeding; therefore, it is likely that ophthalmically administered bromfenac would also be compatible. However, due to the lack of well-controlled studies specific to the use of bromfenac in lactating women, its use should be approached with caution. Consider the developmental and health benefits of breast-feeding along with the mother's clinical need for bromfenac and any potential adverse effects on the breast-fed infant from bromfenac or the underlying maternal condition.