Diclofenac 0.

1% Ophthalmic Solution (5 mL)

Indication(s)
 For the treatment of postoperative ocular inflammation following cataract extraction
 For the reduction of photophobia and ocular pain following corneal refractive surgery
Pharmacological Classification
 Analgesic - Ophthalmic Nonsteroidal Anti-inflammatory Drug (NSAID)
Mechanism of Action
 Diclofenac competitively inhibits both COX-1 and COX-2 enzymes by blocking
arachidonate binding. Following topical application to the eye, diclofenac inhibits miosis
(constriction of the pupil) by inhibiting the biosynthesis of ocular prostaglandins. Thus,
NSAIDs may prevent ocular inflammation.
Pharmacokinetics (ADME)
 Absorption: Systemic absorption from the ophthalmic formulation is not clinically
significant.
 Distribution: It is widely distributed, with significant amounts in synovial fluid. Protein
binding is roughly 99%, primarily to albumin. No significant distribution into breast milk.
 Metabolism: Metabolized via hepatic CYP450 2C9 and 3A4. UGT2B7 and CYP2C8 may
also play a role in metabolism.
 Excretion: Metabolites are excreted through urinary and biliary pathway: about 65% in
the urine and about 35% in the bile. Less than 1% is excreted in the urine unchanged,
with the remainder as metabolites or conjugates of the drug. Conjugates of unchanged
diclofenac account for 5 to 10% of the dose excreted in the urine and less than 5%
excreted in the bile. Little or no unchanged unconjugated drug is excreted.
Dosage & Administration
 Postoperative Ocular Inflammation Following Cataract Extraction:
o Adults: Instill 1 drop of 0.1% solution into the affected eye(s) 4 times daily,
starting 24 hrs after cataract surgery and continue for 2 wks
 Photophobia and Ocular Pain Following Corneal Refractive Surgery:
o Adults: Instill 1 to 2 drops of 0.1% solution into the affected eye(s) within 1 hr
prior to surgery, then 1 to 2 drops 15 mins after surgery, and then 4 times daily
beginning 4 to 6 hrs after surgery and continue for up to 3 days as needed
Off Label Uses
 corneal abrasion
 discomfort and inflammation with epidemic keratoconjunctivitis
o Instill 1 drop four times daily for 4-7 days during the acute phase of infection
 cystoid macular edema after cataract surgery
o Instill 1 drop four times daily for 4-6 weeks in combination with Pred Forte
Ophthalmic (Prednisolone) and taper slowly after the initial treatment period
 various mild anterior segment inflammatory conditions
 Recent studies have looked at the potential for treating acute seasonal allergic
conjunctivitis. The results were promising: less inflammation and improved comfort.
Contraindications
  Topical diclofenac is contraindicated in patients with salicylate hypersensitivity or NSAID
hypersensitivity who have experienced asthma, urticaria, or other allergic reactions after
taking aspirin or other NSAIDs.
Warnings & Precautions
 Diclofenac ophthalmic solution should be used with caution in ocular surgery patients
with known bleeding tendencies or patients receiving other medications that may
prolong bleeding time.
 Ocular diclofenac is recommended to be used with caution in patients with diabetes,
corneal denervation, corneal epithelial defects, xerophthalmia, rheumatoid arthritis, or
repeat ocular surgery within a short time period, as they may be at greater risk for
corneal adverse events (possibly sight-threatening).
 Patients who are wearers of hydrogel soft contact lenses should use the diclofenac
ophthalmic preparation with caution; use of ophthalmic diclofenac has caused ocular
irritation, erythema, and burning in this patient population.
Drug Interactions
 Corticosteroids (Ophthalmic) - NSAIDs (ophthalmic) may enhance the adverse/toxic
effect of corticosteroids (ophthalmic). The concomitant use of ophthalmic
corticosteroids and ophthalmic NSAIDs may negatively affect the healing process of
ophthalmic tissue, as each class of medications has been associated with delayed wound
healing. Additionally, in a small retrospective study, concurrent ophthalmic
corticosteroids use was reported to be a risk factor for ophthalmic NSAID-induced
corneal erosion and perforation.
 monitor for delayed/slow healing of ophthalmic tissue during concomitant use
 Prostaglandins (Ophthalmic) – NSAIDs (ophthalmic) may enhance or diminish the
therapeutic effect of Prostaglandins (ophthalmic).
 monitor the clinical intraocular pressure lowering response to ophthalmic
prostaglandins closely in patients who are also using ophthalmic NSAIDs
Black Box Warning
 N/A
REMS
 N/A
Use in Specific Populations
 It is unknown whether diclofenac reaches detectable quantities in breast milk following
ophthalmic administration. Fetal risk cannot be ruled out.
 Infant risk cannot be ruled out.
Pediatric Patients
 Safety and effectiveness have not been established.
Adverse Effects
 burning sensation in eye (15%)
 keratitis (up to 28%) - possibly due to cataract surgery
 lacrimation and lacrimal drainage (up to 30%)
 raised intraocular pressure (up to 15%) - possibly due to cataract surgery
 dizziness (1%), headache (1%), chills (less than 3%), insomnia (6% or less)
  unspecified infections and associated symptoms (10% or less)
 viral infection (less than 3%)
 conjunctivitis (10% or less)
 corneal erosion
o may lead to sight threatening ulceration or perforation
o immediately discontinue use when there is evidence of corneal breakdown
 ocular irritation (10% or less)
 ocular pruritus (10% or less)
 ocular allergy (10% or less)
 iritis (10% or less)
 eyelid swelling (10% or less)
 eye redness (10% or less)
 corneal edema (10% or less)
 corneal opacification (10% or less)
 corneal deposits (10% or less)
 corneal lesion (10% or less)
 ocular discharge (10% or less)
 Counsel patients that adherence to the dosing recommendation may reduce the risk of
serious adverse events.
Monitoring
 Monitor for relief of postoperative ophthalmic inflammation and temporary relief of
pain and photophobia during surgery indicating efficacy.
 Refractive stability; in patients treated with diclofenac during corneal refractive
procedures; for 1 year after treatment
 liver function tests
 serum creatinine/BUN
Storage & Handling
 Store at room temperature between 15 and 25 degrees C (59 and 77 degrees F).
 Protect from light.
 Throw away any unused eye solution after one month.
 Keep out of the reach of children.
Patient Education
 This medicine is only for use in the eye. Do not take by mouth.
 Follow the directions on the prescription label. Wash hands before and after use.
 Tilt your head back slightly and pull your lower eyelid down with your index finger to
form a pouch. Try not to touch the tip of the dropper to your eye, fingertips, or any
other surface. Squeeze the prescribed number of drops into the pouch. Close the eye
gently to spread the drops.
 Your vision may blur for a few minutes.
 Use your doses at regular intervals. Do not use your medicine more often than directed.
 If you have soft contact lenses, you should not wear them while you are using this
medicine.
 Talk to your pediatrician regarding the use of this medicine in children. Special care may
be needed.
 This medicine is only for you. Do not share this medicine with others.
 Inform your physician if you have any of the following conditions prior to use: bleeding
problems, diabetes, dry eye syndrome, other eye problems, or recent eye surgery,
rheumatoid arthritis, wear soft contact lenses, an unusual or allergic reaction to
diclofenac, aspirin, other NSAIDs, other medicines, foods, dyes, or preservatives,
pregnant or trying to get pregnant, breast-feeding
 Tell your doctor or health care professional if your eye symptoms do not get better
within 2 to 3 days. Do not use for longer than directed by your doctor or health care
professional.
 You may have to wear a special bandage for up to 3 days after your eye surgery.
 Wear sunglasses if your eyes are more sensitive to light.
 If you miss a dose, use it as soon as you can. If it is almost time for your next dose, use
only that dose. Do not use double or extra doses.
 If you think you have taken too much of this medicine contact a poison control center or
emergency room at once.

References
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