OCULAR PHARMACOLOGY that is very painful, prescribe analgesics to relieve

Dr. Nathaniel Chan the eye pain because it is toxic to the corneal
February 13, 2015 endothelium and it could cause toxic keratitis with
Grupo ni Michelle TENte prolonged use
 Toxic to the corneal epithelium when used
COMMON EYE MEDICATIONS habitually; can cause
 Anesthetic agents o Punctate keratitis
 Dyes o Injury
 Anti-infective drugs
 Anti-inflammatory agents Topical anesthetics should never be prescribed for
home use, since prolonged application may cause
 Mydriatic/Cyclopegic agents
corneal complications and mask serious ocular
o Pupil dilators disease.
 Glaucoma medications
 Decongestant, vasoconstrictive, and anti-allergy
agents Local Anesthetics for Injection
 Lubricating agents and tear substitutes  Common agents
 Corneal dehydration medications o Lidocaine (Lignocaine) – most commonly used
local anesthetic
Modes of Delivery / Preparations o Procaine hydrochloride (Novocaine)
 Topical drops or ointment o Mepivacaine hydrochloride longer acting than
o Most common lidocaine
 Thin drug o Bupivacaine hydrochloride (Marcaine,
o containing wafers deposited in the conjunctival Sensorcaine)
sac o Etidocaine hydrochloride
 Injectable drugs o The first three are the short-acting. They have a
o Subconjunctiva faster onset of action but they only last for 1-2
hours.
o Vitreous cavity – injected underneath the
conjunctiva like in age-related macular o The last two are longer-acting. Some would last
for 6-10 hours
degeneration
o Sub-Tenon’s capsule - steroids  Differ in length of action
o Peribulbar or retrobulbar spaces – like in  Used in ophthalmic surgeries, i.e. cataract
cataract or intraocular surgeries, we inject extraction, etc.
anesthetics o Lidocaine and Mepivacaine in equal amounts to
 Systemic medications anesthetize the eye and paralyze the extraocular
muscles so that they are not able to move to
ANESTHETIC AGENTS have a steady or fixed eye during the procedure
 used prior to removal of foreign bodies
DYES
Topical Anesthetics  Used for ophthalmic diagnosis (not to treat)
 Used when performing diagnostic and therapeutic  Common agents
procedures, because there are many nerve endings  Biologic Dyes
in the cornea so manipulation would be painful 1. Fluorescein dye – yellow-orange dye (When
 Most common preparation exposed to blue light will turn green)
 In the form of eye drops - Stain attached to epithelium
 Common agents:  Uses
o Tetracaine HCl- (Pontocaine)  Applanation tonometry to diagnose
o Proparacaine HCl – most widely used corneal abrasions if the epithelium is
because it is the least irritating sloughed off the dye will stain the
o Benoxinate with fluorescein anterior stromal layer and will appear
green on slit-lamp exam, punctate
o Cocaine
epithelial erosions, and other epithelial
 Not given habitually, not prescribed, only used in
the clinics, so if the patient has corneal abrasion
References: Doc’s Lecture, Audio, JAX notes, Book notes (Ophthalmic Therapeutics by Flach and Fraunfelder) Page 1 of 6
 defects. An intact cornea will not stain o Gentamicin
with fluorescein dye, only the stroma. o Tobramycin – treatment of Pseudomonas
 Fluorescein angiography- presence of keratitis , common in contact lens users due to
ischemia or constriction washing of the lenses with tap water
 Dye is injected into the veins o Chloramphenicol – seldom used
 To visualize the retinal vasculature o Fluoroquinolones- broad spectrum usually used
 Pictures will be taken during the for prophylaxis for post-op infections, reserved
time the dye is traveling in the for severe bacterial eye infections or resistant
circulation organisms
 Contact lens fitting  Ciprofloxacin
 how the lens fit  Gatifloxacin
2. Rose Bengal – red dye  Moxifloxacin
 Used in the diagnosis of keratoconjunctivitis o Sulfacetamide sodium
sicca (dry eyes)  Sulfonamide derivative most commonly
 Stains devitalized epithelium and mucus used in bacterial conjunctivitis
shreds unlike fluorescein dye it does not
need an exposed epithelium to stain the Antifungal Agents
cornea.  Not readily available in topical forms – oral
 Trypan blue- used to visualize anterior antifungal is mixed with artificial tears and used as
capsule especially in capsulorhexis in topical eyedrops, but can precipitate and cause
cataract operation foreign body sensation due to the granules
 Natamycin
ANTI-INFECTIVE AGENTS o effective against filamentary and yeast forms;
 Three general classes initial drug of choice for most fungal ulcers
1. Antibacterial o the only topical antifungal agent
2. Antiviral o Fungal ulcers are not very common because
3. Antifungal they are due to organic injuries from plants and
*most of these are in topical formation soil
o Most commonly used
Antibiotics / Antibacterial o Very hard to source, in India, not FDA-approved
in Phils
 Used in the treatment of eye infections
o Bacterial conjunctivitis  Nystatin
o Hordeolum/Stye  Amphotericin B
o Blepharitis o very expensive (~P10,000/bottle)
o Bacterial corneal ulcers o for systemic fungal infections
o Endophthalmitis – all of the eye is infected o IV
(panophthalmic infection)  Miconazole
 As prophylaxis post-op  Itraconazole
In cataract surgery, it is given 3-5 days before
surgery to make sure eye is sterile and risk of Antiviral Agents
infection is reduced No readily available antiviral agents in the Philippines,
 Most of these drugs are packaged as pure antibiotics viral infections in the eye are rare in the Philippines
or in combination with steroids. Steroids should not  Idoxuridine
be given in fungal or bacterial infections because it o for the treatment of herpes simplex keratitis
would retard wound healing and promote growth of  Vidarabine
these microorganisms. If you’re not sure, don’t give o for treatment of herpetic keratitis
combination drugs.  Trifluridine
 Common antibiotic eyedrops  Acyclovir
o Bacitracin- neomycin-polymyxin B o Available as oral and topical preparations
o Erythromycin – prophylaxis for ophthalmia o given orally for 7-10 days
neonatorum - hard to procure, most effective, o for herpes zoster ophthalmicus (presence of
tetracycline as an alternative vesicopapular lesions around the eyelids and

References: Doc’s Lecture, Audio, JAX notes, Book notes (Ophthalmic Therapeutics by Flach and Fraunfelder) Page 2 of 6
 later on turn to scabs due to the reactivation of o Open-angle glaucoma more common side effect
chicken pox and affects a specific nerve; most than cataracts
commonly involved is the 1st branch/ophthalmic o Delayed wound healing
branch of the trigeminal nerve) o Corneal melting, corneal ulcers
 Ganciclovir o Prolongation of the natural duration of the
o Used in cases of HIV when they have very low disease
CD4 counts and CMV retinitis o Mydriasis and ptosis – rare complications

ANTI-INFLAMMATORY AGENTS Non-Steroidal Anti-Inflammatory Drugs

Two general categories  Indications
1. Corticosteroids Substitute for patients who are not good candidates
2. Non Steroidal Anti-Inflammatory Drugs for steroid treatment
o Reduce inflammation
Corticosteroids o Reduce pupillary constriction during surgery- in
 Not given for corneal ulcers cataract surgery, gives better exposure of lens
 Topical o one of the most important uses of NSAIDs
 Systemic o Especially during cataract surgery because the
 Used to reduce ocular inflammation in pupils should be dilated intraoperatively
o Allergic conjunctivitis – not first line, usually give o Given a few hours before the procedure
antihistamine first, followed by mast cell o Ocular allergies
stabilizers, then topical steroids; short term  Available topical NSAIDs
treatment o Flurbiprofen
o Uveitis o Ketorolac
o Episcleritis o Diclofenac Na
o Scleritis o Nepafenac
o Phylytecnulosis
o Non-infectious and infectious keratitis GLAUCOMA MEDICATIONS
 Steroids are not given in fungal or herpetic  Classes:
keratitis because it might lead to corneal o Cholinergic drugs
melting or increase in the size of the ulcer, o Adrenergic drugs
delay wound healing and increase viral or o Beta-adrenergic blocking agents
fungal load o Carbonic anhydrase inhibitors
 After antibiotic therapy when you are sure o Hyperosmotic agents
that the patient is almost healed, you may Dose and frequency of administration of therapy should
give steroid to deal with interstitial keratitis be individualized according to measurements of
(not epithelial) intraocular pressure. The minimum treatment being used
 Never give if epithelium is not closed that sufficiently controls the intraocular pressure to
 Available topical steroids prevent optic nerve damage.
Increases Intraocular pressure o Prostaglandin analogues
Loteprednol is used in patients with increased o Combination drugs
intraocular pressure (glaucoma)  Usually have actions on the sympathetic or the
o Prednisolone – most potent parasympathetic autonomic nervous system
o Dexamethasone  Review the autonomic nervous system because we
o Progesterone-like agents are dealing with drugs that affects it. This might
Medrysone come out in doc’s exams.
Fluorometholone
 Side-effects and complications Cholinergic Agonists
o Can enhance activity of herpes simplex virus
o Fungal overgrowth Topical direct-acting cholinergic agonist
o Cataract formation (posterior subcapsular type)- (parasympathomimetics) decrease intraocular pressure
by increasing the outflow of aqueous through the
in long term use
trabecular meshwork.
 Miotics or parasympathomimetics
References: Doc’s Lecture, Audio, JAX notes, Book notes (Ophthalmic Therapeutics by Flach and Fraunfelder) Page 3 of 6
 Increase outflow of aqueous humor- aqueous humor o Tachycardia
is produced by ciliary body o Hypertension
 Increases eye pressure o Tremor
o due to pupillary constriction (peripheral iris o Anxiety
would be stretched and the angle would o Premature ventricular contractions
increase)
 Examples: Beta-Adrenergic Receptor Antagonists (sympatholytics)
o Pilocarpine most readily available, used for acute Beta-Adrenergic blocking agents reduce intraocular
angle glaucoma pressure by suppressing aqueous production.
o Carbachol –intra-op to constrict pupils, used to
reconstrict pupil after cataract surgery
 Elicit history of asthma before prescribing
o Demecarium bromide
o Echothiophate iodide  Beta-blockers
o Isoflurophate  Reduces aqueous production in the ciliary
 Side effects epithelium
o Pupillary constriction-narrow visual field may be  Examples:
mistaken as advanced glaucoma o Timolol maleate most widely used in the market-
o Its action is also its side effect Be careful when administering to those with
o Ciliary spasm – brow ache and myopic shift; pulmonary asthma or COPD
when there’s contraction in ciliary spasm, the o Levobunolol hydrochloride
zonules relax, thus increasing the AP diameter o Betaxolol hydrochloride
(myopia)  greater selectivity for β1 receptors no action
on β2 receptors
Adrenergic Agonists  Safer to use in patients with pulmonary
conditions; no pulmonary side effects
Topical Adrenergic receptor Agonists- Sympathomimetic drugs o Metipranolol hydrochloride
which reduce intraocular pressure by variable effects on
production and drainage of aqueous, comprise the α2-
o Carteolol hydrochloride
adrenergic agonist apraclonidine and bromonidine, and Same drugs given to hypertensives
dipivefrin, a pro-drug of non-selective agonist epinephrine.  Side effects
o Bradycardia
o Decreased cardiac output
 Sympathomimetics – dilates the pupil
o Exercise intolerance –due to cardiac effects
 Reduce production of aqueous humor and opens
o Bronchiolar spasm – not given to asthmatic
outflow pathways
patients
 Decrease eye pressure
o Hypotension
 Examples:
o Syncope
o Epinephrine
o Decreased libido – a concern for male elderly
o Dipivefrin
patients
o Apraclonidine – only use is to prevent sudden
o Lethargy
increase in IOP from post-op laser
o Depression
o Brimonidine – most commoly used, only
adrenergic agonist used regularly as a topical
Carbonic Anhydrase Inhibitors
medication
 Reduce aqueous production by inhibiting the
 Side effects
enzyme carbonic anhydrase
o Ocular
 Very potent anti glaucoma medication if given
o Rebound hyperemia – it will constrict
systematically
conjunctival vessels, causes eye redness that can
 Rarely used due to its many side effects
be mistaken as sore eyes
 Sulfonamide derivatives
o because of vasoconstriction with rebound
dilatation o acetazolamide- commonly used in the Phil.
(250mg/tab, 1 tablet TID-QID)
o Cystoid macular edema - Brimonidine
o methazolamide
o Systemic – press nasolacrimal system to prevent
o dichlorphenamide
systemic absorption

References: Doc’s Lecture, Audio, JAX notes, Book notes (Ophthalmic Therapeutics by Flach and Fraunfelder) Page 4 of 6
 o Given in acute open angle glaucoma because of  Good efficacy in decreasing the intraocular pressure
very high IOP
o To lower the pressure very fast, give oral. Cycloplegics – Parasympatholytics
o Not given for a long time, not used as o Atropine is an effective and long-acting
maintenance medication because of the cycloplegic. Used to maintain dilated pupil after
hypokalemia side effect which can lead to intraocular surgical procedure.
cardiac arrest o Scopolamine hydrobromide, Homatropinede
 Topical hydrobromide, Cyclopentolate Hydrochloride,
Topicals were developed since we cannot use Tropicamide, Cyclopentolate Hydrochloride-
systemic drugs long term Phenylephrine Hydrochloride
o Dorzolamide
o Brinzolamide  Increases uveoscleral otflow (alternative outflow of
o not as strong as systemic form aqueous)
o used only as adjunct to β-blocker or o has replaced Timolol as the first-line drug for
prostaglandin analogues glaucoma because Timolol has more
 Side effects complications
o nausea  Examples
o tingling of the fingers and toes o Latanoprost
o anorexia o Travoprost- newest, less hyperemic side effects
o peculiar taste sensations o Bimatoprost
o hypokalemia- sometimes Kalium durule or  Side effects
potassium prep is given, esp for systemic o Iris hyperpigmentation
carbonic anhydrase inhibitors  not a concern for Asians because we are
o renal lithiasis; can cause sudden death already brown-eyed
o acidosis o Bitter taste
o lethargy o Conjunctival hyperemia
o loss of libido  more common side effect
o depression o Burning, stinging, itching
o aplastic anemia – rare o Anterior uveitis
o Cystoid macular edema
Hyperosmotic Agents/ Systemic Osmotic Agents o Epithelial toxicity
o Lengthens eyelashes
Used in the management of acute (angle closure)
glaucoma and occasionally preoperatively. MYDRIATIC/CYCLOPLEGIC AGENTS
 Actions
 Reduce IOP by making the plasma hypertonic to o Mydriasis by either paralyzing the iris sphincter
aqueous and vitreous humor (osmotic gradient) (cycloplegics) or stimulating the iris dilators
 Fluid from aqueous and vitreous will flow into the (mydriatics) - sympathomimetics
intravascular space o Paralyzes the ciliary muscle (cycloplegics)
 Given orally or via IV in cases of acute glaucoma and o Increases iris size
pre- or post-operatively in selected patients  Uses:
 Examples o Pupillary dilation for ophthalmoscopy and
o Urea cataract surgery provides easy access to the
o Glycerin lens
o Isosorbide o Refraction in children- for children <10 years;
o Mannitol – most common dry refraction
 Given with caution in patients with DM, CHF, o Relieves ciliary muscle spasm
and kidney damage (eliminated by kidneys)  Antidote to pilocarpine
Can lead to congestion due to increased intravascular  Examples
volume o Phenylephrine – purely mydriatic with no
cycloplegic effect.
Prostaglandin Analogues o Atropine sulfate – longest acting cycloplegic,
 Initial drug of choice for open angle glaucoma within 1 week after instillation
References: Doc’s Lecture, Audio, JAX notes, Book notes (Ophthalmic Therapeutics by Flach and Fraunfelder) Page 5 of 6
 o Scopolamine  Post-op : very traumatic cataract,
o Homatropine edematous
o Cyclopentolate  acute closure –angle glaucoma, to clear
o Tropicamide corneal haziness
 patient might claim a stinging sensation
Phenylephrine is used both singly and with
cycloplegics to facilitate ophthalmology, in
treatment of uveitis, and to dilate the pupil prior to
POSSIBLE ADVERSE EFFECTS OF SYSTEMIC DRUGS
cataract surgery.  Allopurinol – cataract
 Cardiac glycosides – retinal degeneration
DECONGESTANTS, VASOCONSTRICTIVE, AND ANTI-  Chloramphenicol – optic atrophy, optic neuritis
ALLERGY AGENTS  Corticosteroids – glaucoma, cataract
 Ethambutol – optic neuritis quite common;
 EyeMo, Visine, etc.
sometimes reversible, sometimes not
 Can cause rebound eye redness as it dilates the eye
if discontinued after prolong used  Haloperidol – cataract
 Isoniazid – optic neuritis
 Already pulled out in pharmacies
 Not usually prescribed by ophthalmologists as it  Morphine - optic neuritis
causes vasoconstriction leading to rebound  Rifampin - optic neuritis
vasodilation  Salicylates – nystagmus, retinal hemorrhage
 Reduces ocular redness, itching and irritation  Tetracycline – papilledema
 Most contain ephedrine and naphazoline,
tetrahydrozoline or phenylephrine END
 May also contain antihistamine like pheniramine
maleate or antazoline phosphate (for ocular Happy Valentine’s Day!
allergies) 
 Newer agents are the mast cell stabilizers- prevents
release of allergic mediators
o Cromolyn sodium
o Ketotifen
o Lodoxamine
o Olopatadine
 Available in the Philippines are only Ketotifen and
Olopatadine

LUBRICATING MEDICATIONS AND TEAR SUBSTITUTES

 Most prescribed eye drops
 Used for treatment of dry eyes
 Used as ophthalmic lubricants in certain
examinations using contact lenses
 Basic ingredients
o Hypotonic or isotonic buffered solution
o Surfactants
o Viscous agents – methylcellulose

CORNEAL DEHYDRATION MEDICATIONS

Cornea is a dry structure, when with water it becomes
edematous causing haziness
 Hypertonic medications instilled on the eye
 Clear corneal edema osmotically
 Examples
o Anyhydrous glycerine solution
o Hypertonic sodium chloride 2% and 5%

References: Doc’s Lecture, Audio, JAX notes, Book notes (Ophthalmic Therapeutics by Flach and Fraunfelder) Page 6 of 6