Opthalmolo

gy Module
Product Knowledge
Dr. Ahmed Talaat (Senior GPM)
Idelox
 Composition

 Each one ml of Idelox solution contains 5 mg of Moxifloxacin

(0.5%).
 Mechanism of Action

 Moxifloxacin, a fourth-generation fluoroquinolone, inhibits

the DNA gyrase and topoisomerase IV required for bacterial
DNA replication.
 Indications

 Idelox is indicated for:

1) the treatment of bacterial conjunctivitis, blepharitis,
keratitis (including corneal ulcer) caused by susceptible
strains
2) Preoperative and postoperative prophylaxis.
 Susceptible Strains
Aerobic Gram‐positive microorganisms:
 Corynebacterium species
 Staphylococcus aureus
 Staphylococcus epidermidis
 Other Staphylococcus Species
Aerobic Gram‐negative microorganisms:
 Haemophilus influenzae
 Klebsiella Species
 Moraxella catarrhalis
 Proteus mirabilis & vulgaris
 Pseudomonas aeruginosa
Other microorganisms:
 Chlamydia trachomatis
 Bacterial Resistance

 Idelox Uniquely designed to reduce resistance.

 With topical Moxifloxacin, bacterial resistance development
is not observed because topical Moxifloxacin:
1) Achieves very high ocular surface concentrations (20 min.
after single dose, concentrations of Moxifloxacin in
conjunctiva (18.0 mg/g) are higher than for Ciprofloxacin,
Gatifloxacin, Ofloxacin & Levofloxacin).
2) Dual-step mutation required (two mutations in the DNA
Gyrase and Topoisomerase genes means that resistance to
Moxifloxacin develops at a slower rate).
Dosage & Method of Administration
 For blepharitis, conjunctivitis & keratitis (including corneal
ulcer): Usually instill one drop in the affected eye (s) 3 times a
day.

 For preoperative and postoperative prophylaxis: Usually,

instill one drop in the affected eye (s) 5 times per day for 2
days before operation, and 3 times a day up to 14 days after
operation.

 Patients should be instructed to leave at least 5 minutes

 Safety Profile – Use in Special Population

 Common Side Effects: Eye Pain – Eye Irritation

 Pediatric Use: The safety and effectiveness of Idelox solution in bacterial
conjunctivitis have been established in all ages including children and
neonates.
 Geriatric Use: No overall differences in safety and effectiveness.
 Pregnancy: There are no studies with Idelox in pregnant women to inform
a product-associated risk. However, no effects on pregnancy are anticipated
since the systemic exposure is negligible.
 Breast-feeding: It is not known if moxifloxacin is transferred into human
milk. However, at therapeutic doses of Idelox solution no effects on the
child are anticipated.
Brochure
Trials
Clinical Studies – High Potency
Clinical Studies – High Penetration Power
Conclusion

● In this study, significantly greater target tissue

penetration was evident with moxifloxacin than with
the other 4 fluoroquinolones. Moxifloxacin is a potent
antibiotic against the pathogens causing
conjunctivitis and is a superior treatment option
when penetration of therapeutic concentrations to
the conjunctiva is necessary.
Clinical Studies – High Penetration Power / Cataract
Surgery
 High High
High
Summary of Benefits Cure Rate
Penetration
Power
Safety
Profile

 Idelox shows lower MIC 90 for all gram-positive bacteria compared to

Ofloxacin, Ciprofloxacin, Levofloxacin and Gatifloxacin.

 Idelox has statistically significant higher conjunctival levels compared to

other fluoroquinolones.

 Idelox achieves significantly higher aqueous humour concentration

compared to Gatifloxacin in cataract patients.

 Idelox is safe in pediatric patients under one month of age.

Ramedafenac
 Composition

 Each one ml of Ramedafenac solution contains 1 mg of

Nepafenac (0.1%).
 Mechanism of Action

 Nepafenac is a non-steroidal anti-inflammatory and analgesic

prodrug (Better Penetration).

 After topical ocular dosing, Nepafenac penetrates the cornea and

is converted by ocular tissue hydrolases to Amfenac, a
nonsteroidal anti-inflammatory drug.

 Amfenac inhibits the action of prostaglandin H synthase

(cyclooxygenase), an enzyme required for prostaglandin
production.
 Indications

 Ramedafenac is indicated in adults for:

Prevention and treatment of postoperative pain &
inflammation associated with cataract surgery.
Reduction in the risk of postoperative macular edema
associated with cataract surgery in diabetic patients.
 Dosage & Method of Administration

 The dose is 1 drop in the conjunctival sac of the affected eye(s) 3 times daily
beginning 1 day prior to cataract surgery, continued on the day of surgery and
up to 21 days of the postoperative period.
 An additional drop should be administered 30 to 120 minutes prior to surgery.
 For the reduction in the risk of Macular Edema: The dose is 1 drop in the
conjunctival sac of the affected eye(s) 3 times daily beginning 1 day prior to
cataract surgery, continued on the day of surgery and up to 60 days of the
postoperative period.
 If more than one topical ophthalmic drug is being used, the drugs should be
administered at least five minutes apart.
 Use with Contact Lenses: Contact lenses should be removed before using
Ramedafenac & put them back 10-15 minutes afterwards as Benzalkonium
chloride (preservative) may change the color of contact lenses.
 Safety Profile – Use in Special Population

 Common Side Effects: Keratitis – Eye Pain - Eyelid margin crusting.

 Pediatric Use: No data are available.
 Geriatric Use: No differences in safety / efficacy were observed between elderly &
younger patients.
 Pregnancy: Not Recommended.
 Breast-feeding: can be used during breast-feeding.
 Renal & hepatic Patients: No Dose Adjustment.
 Contraindications

 (1) Patients in whom attacks of asthma, urticaria, or acute rhinitis are precipitated
by acetylsalicylic acid or other NSAIDs.
 (2) Hypersensitivity to any component of this product or to other NSAIDs.
 Warnings

 Patients should be instructed to avoid sunlight during treatment with Ramedafenac.

 In some susceptible patients, continued use of topical NSAIDs may result in
epithelial breakdown, corneal thinning, corneal erosion, corneal ulceration or
corneal perforation.
 Caution should be exercised if Ramedafenac is administered concomitantly with
corticosteroids, particularly in patients at high risk for corneal adverse reactions
described below.
 An acute ocular infection may be masked by the topical use of anti-inflammatory
medicines.
Brochure
Trials
 Clinical Studies – Effect on Pain
Ramedafenac onset of action is around 15 minutes &
duration of action is greater than 8 hours.
At Day 14, Over 90% of patients treated with Ramedafenac
reported no
Pain (highly effective in the treatment of pain related to
cataract surgery).
Clinical Studies – Cure Rate

At Day 14, Over 75% of patients treated with Ramedafenac

reported as totally cured.

Corneal permeability of Ramedafenac (prodrug) is

approximately 4,19, and 28 times greater than Diclofenac,
Bromfenac, and Ketorolac respectively.
 Summary of Benefits

 Ramedafenac has fast onset of action (around 15 minutes) & duratio

of action which is greater than 8 hours.
 Ramedafenac is effective in the treatment of pain related to catarac
surgery.
 Ramedafenac offers high cure rate.
 Ramedafenac has greater corneal permeability than diclofenac,
bromfenac & ketorolac.
Sustained
Rapid High
Anti- High Cure
Analgesic Penetration
inflammatory Rate
Effect Power
Effect
Olopalite
 Composition

 Each one ml of Olopalite solution contains 1 mg of

Olopatadine (0.1%).
 Mechanism of Action

 Olopatadine is a potent selective anti-allergic/antihistaminic

agent that exerts its effects through multiple distinct
mechanisms of action (Dual Action).
1) It antagonizes histamine (the primary mediator of allergic
response) and prevents histamine induced inflammatory
cytokine production by human conjunctival epithelial cells
(Fast Initial Relief after 3 minutes).
2) it may act on human conjunctival mast cells to inhibit the
release of pro-inflammatory mediators (preventing further
waves of mast cell activation).
 Indications

 Olopalite is indicated for:

Treatment of ocular signs and symptoms of seasonal allergic
conjunctivitis.
Dosage & Method of Administration

 The dose is one drop in the conjunctival sac of the affected

eye(s) twice daily, morning and evening.
 Treatment may be maintained for up to 4 months, if
considered necessary.
 In case of concomitant therapy with other ocular medicines,
an interval of five minutes should be allowed between
successive applications.
 Use with Contact Lenses: Contact lenses should be
removed before using Olopalite & put them back 15 minutes
 Safety Profile – Use in Special Population

 Common Side Effects: eye pain – eye irritation – dry eye.

 Pediatric Use: Olopalite may be used in pediatric patients three years of age and
older at the same dose as in adults.
 The safety and efficacy in children under 3 years has not been established. No data
are available.
 Geriatric Use: No dosage adjustment.
 Hepatic & Renal Patients: No dosage adjustment.
 Pregnancy: There are no or limited amount of data from the use of ophthalmic
Olopatadine in pregnant women – Not Recommended.
 Breast-feeding: Olopalite should not be used during breast-feeding.
Brochure
Trials
 Study Design
● Single-center, prospective, three-visit, randomized, placebo and active contralateral
treatment controlled phase IV study designed to compare the efficacy of a single dose
of olopatadine to a single dose of epinastine in the prevention of itching and
conjunctival redness in the conjunctival allergen challenge model.
● The patients followed 3 visits during the trial:
1. Visit 1 “Baseline Screening” at Day 0: A conjunctival allergen challenge was
performed bilaterally with an allergen (i.e., cats, grasses, trees, or ragweed) to
which the subject tested positive in a skin test. The allergen concentration was
increased until a positive reaction (defined as ≥ 2.0+ itching and ≥ 2.0+
hyperemia in at least one vessel bed) was elicited bilaterally. Itching was evaluated
by subjects using a standardized scale (i.e., 0 = no itching; 4 = severe itching).
Redness and chemosis were evaluated by investigators using standardized scales
(i.e., 0 = none; 4 = severe). Any subject who did not react positively was exited
from the study.
2. Visit 2 “Confirmatory” at Day 7 ±2: A technician instilled bilaterally the
appropriate allergen at the appropriate concentration that elicited a positive
reaction. Subjective grading of ocular itching occurred at 3 min, 5 min, and 7 min
following challenge (scale described above). The investigator graded redness in
each of the three vessel beds and chemosis at 10 min,15 min, and 20 min
following challenge (scales described above).
3. Visit 3 “Drug Evaluation” at Day 21±3:. Randomization of subject
numbers into treatment groups was performed prior to commencement of all
other study procedures by an independent technician not involved in any
other aspect of the study. Subjects were randomized into one of the three
treatment groups listed below in an 8:1:1 fashion:
○ Olopatadine 0.1% in one (left or right) eye and epinastine 0.05% in
the fellow eye.
○ Olopatadine 0.1% in one (left or right) eye and placebo (artificial
tears) in the fellow eye.
○ Epinastine 0.05% in one eye (left or right) and placebo (artificial
tears) in the fellow eye.
● A technician instilled a drop of the study medication in each eye according to the
defined randomization scheme. Study medications were masked in identical
containers. Five minutes after instillation, a conjunctival allergen challenge was
performed bilaterally using the same concentration and allergen that elicited a
positive allergic response at Visits 1 and 2. Ocular itching, redness, and chemosis
grading was performed at the same time points as described (above).
 Clinical Studies – Effect on Ocular Itching
Olopalite is more effective than epinastine in controlling
itching associated with allergic conjunctivitis
 Clinical Studies – Effect on Ocular
Redness
Olopalite is more effective than epinastine in controlling
redness associated with allergic conjunctivitis
Clinical Studies – Comparison VS
Ketotifen

Olopalite was shown to be significantly more effective than

Ketotifen (p < 0.05) in reducing ocular itching induced by a
conjunctival antigen 12 hour after instillation.

73% of patients identified Olopalite as the more tolerable

formulation
compared to Ketotifen.
 Summary of Benefits
 Olopalite is more effective than epinastine in controlling
itching, redness &
chemosis associated with allergic conjunctivitis.
 Olopalite is significantly more effective than Ketotifen in
reducing ocular
itching.
 Olopalite is more tolerable compared to Ketotifen.
Fast Relief Long-term High
Dual
of Symptoms Safety
Action
Symptoms Control Profile