Far Eastern University – Nicanor Reyes Medical Foundation
OPHTHALMOLOGY – OCULAR PHARMACOLOGY
Miriam Louella D. Fermin, RPh, MD
CLINICAL PHARMACOLOGY
• Uses drugs to treat, prevent and diagnose disease
• PHARMACODYNAMICS
o Interactions between the body systems through its
chemical components with foreign chemicals
o “What the DRUG does to the body”
• PHARMACOKINETICS
o “What the BODY does to the drug”
1. Absorption: process of uptake of the compound from
the site of administration into the systemic circulation
2. Distribution: stage when a drug moves from the site of
entry to other organs/areas of the body
3. Metabolism: when the body transforms the drug into
metabolites
4. Elimination or Excretion: process wherein the parent
drug and its metabolites leave the body
OCULAR SRUCTURES AND PHARMACOKINETICS
a. Cornea: acts as major functional barrier for ocular
penetration. For effective penetration, drugs must have
hydrophilic and lipophilic properties.
b. Conjunctiva and Sclera: major depot of drugs
c. Iris: drug response varies depending on the amount of iris
pigmentation.
d. Lens: barrier for rapid penetration of drugs from aqueous
and vitreous humor
e. Vitreous: reservoir of drugs and temporary storage depot of
metabolites
f. Retina: forms the Blood Retinal Barrier (BRB) that does not
allow passive diffusion of drug molecule into the ocular
tissue.
FACTORS AFFECTING DRUG PENETRATION INTO OCULAR TISSUES
• Drug concentration and solubility: higher concentration,
better penetration
• Viscosity: addition of methylcellulose and polyvinyl alcohol
increases drug viscosity and penetration by increasing
contact time with the cornea and altering corneal
epithelium.
• Lipid solubility: higher lipid solubility, better penetration.
• Surfactants: preservatives (benzalkonium and thiomersal)
used in ocular preparations alter corneal cell membrane
and increase drug permeability.
• pH: ocular drugs must be formulated to be within a pH
range that is non-irritating (pH 4.3-8.4) and non-corrosive
(pH 2-11.5)
• Osmolarity: ocular drugs must be formulated with a non-
irritating osmolarity (<500 mOsm)
• Molecular weight and size: lower molecular weight and
size, better penetration.
ROUTES OF DRUG ADMINISTRATION
A. TOPICAL
• instilled directly into the eye
Solutions & • eye drops – most common
suspensions • Advantage: easier to instill, can cause less
blurring of vision
• Disadvantage: because it is less viscous, it
has lesser contact time, inc. risk of
contamination, may cause ocular injury
from careless instillation.
Ointments • Advantages: prolonged ocular contact
time allowing less frequent dosing of the
medication
• Disadvantages: complain of blurred vision
or oily skin after application; because of its
prolonged contact time, some may
develop hypersensitivity reaction to the
preservatives
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Lid Scrubs • Application of a solution ointment or
detergent is helpful in treatment of
seborrheic/infective blepharitis.
• This aids in the removal of oils, debris,
desquamated skin in the inflamed lid.
Gels • Gelling agents transform from gel to liquid
upon contact with your eye rendering the
drug hydrophilic and minimizing complaints
of blurring of vision.
“DOUBLE DOT” TECHNIQUE
1. Digital Occlusion Technique
• Wash your hands
• Pull lower lid using index finger
• Ask patient to look up and instill eyedrops
• Ask patient to close eyes → It forms a negative
pressure in the lacrimal drainage system for better
penetration
• Press the inside corner (inner canthal area) of the eye
2. Don’t Open Technique
• Don’t’ open eye for at least 3 minutes
B. SYSTEMIC:
a. Oral (P.O.): drug taken by mouth
b. Intravenous (IV): drug injected directly into the blood
stream
c. Intramuscular (IM): drug injected into skeletal muscle
d. Subcutaneous (SC): drug injected into subcutaneous
tissue
C. PERIOCULAR
a. Subconjunctival injection
b. Subtenon’s injection
c. Retrobulbar injection: drug injected into the muscle cone
o Used in anesthesia injection during cataract surgery
This is preferred route for anesthesia to prevent
movement of the eyes
o Drugs are injected in the intraconal space include
anesthetics, steroids, phenols and alcohol.
o Provides rapid onset of anesthesia and akinesia for
anterior segment and vitreoretinal surgery
o This technique is a blind procedure where the
needle is placed near the globe while aiming for
the muscle cone which contains vital structure such
as the optic nerve.
o Potential risks include inadvertent globe
penetration, retrobulbar hemorrhage, direct injury
to the optic nerve
d. Peribulbar injection: drug injected above and below the
orbit
o Also used in anesthesia procedures
o It is also a blind procedure, involves one
or more injections around the globe without directly
aiming for the muscle cone.
o A rather safer technique, and provides similar
anesthesia and akinesia but with a lesser rapid onset
as compared with the retrobulbar anesthesia
D. INTRAOCULAR
a. Intracameral: drug injected into the eye (aqueous) cavity
o Used to inject intraocular antibiotics (for intraocular
infections and for post- cataract operation)
o Involves directly placing a drug in the anterior
chamber
b. Intravitreal
o Injection in the vitreous cavity in about 4mm in the
limbal area (in the junction of cornea and sclera)
o Used in endophthalmitis, posterior segment infection
o Also used for the injection of anti-VEGF in the retina
(for neovascularization like in diabetic retinopathy)
 OPHTALMOLOGY –OCULAR PHARMACOLOGY
MOA
OCULAR DIAGNOSTIC DRUGS
A. FLUORESCEIN DYE • Water soluble, orange-
yellow, non-irritating dye that
becomes brilliant green
when viewed under cobalt
blue or fluorescent light.
B. TOPICAL ANESTHETICS
C. MYDRIATICS AND • These drugs produce
CYCLOPLEGICS pupillary dilatation that aids
adequate examination of
the fundus and reduce the
incidence of posterior
synechiae formation in
uveitis. They are also used
pre-operatively in cataract
surgery.
D. CHOLINERGIC • These agents cause pupillary
BLOCKING AGENTS constriction or miosis.
1. Direct Acting • Parasympathomimetic
Cholinergic Blocking Stimulates the ciliary muscle
Agents and subsequently increases
• aqueous humor outflow.
2. Anti-Cholinesterase • Constriction of iris sphincter
(Cholinergic Blocking (miosis)
Agent) • Ciliary muscle (ciliary muscle
spasm)
3. Adrenergic • Vasoconstriction
Stimulating Drugs • Ocular pressure reduction
TOPICAL OCULAR THERAPEUTIC DRUGS
A. DECONGESTANTS • Vasoconstriction of
conjunctival blood vessels
B. ANTIHISTAMINES • Inhibits histamine release
from mast cells
C. ARTIFICIAL TEARS or • Lubricates ocular surface,
LUBRICANTS reduce tear osmolarity and
protect the ocular surface
from desiccation
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INDICATIONS SIDE EFFECTS EXAMPLES
• Diagnosis of corneal abrasion and post-
surgical aqueous leak
• Tear layer evaluation in dry eye or
contact lens fitting
• Assessment of lacrimal drainage
• Intraocular (IOP) determination using
applanation tonometry
• Angiographic procedure for the retina
(Fluorescein Angiography)
• Removal of foreign body/sutures mildly toxic to the cornea and retards • Proparacaine HCl 0.5%,
• Applanation tonometry healing • Tetracaine HCl 0.5%,
• Local anesthesia for ocular • Lidocaine 1.0%
procedures/surgeries • Oxybupavacaine 0.4%
• paralyze accommodation in The stronger mydriatics (cycloplegics) • Sympathomimetic:
cycloplegic refraction, iritis, cyclitis and paralyze the ciliary body. Phenylephrine 2.5%
diffuse uveitis • Parasympatholytic: Atropine
1%, Cyclopentolate 1%,
Tropicamide 0.5%
• acute angle closure glaucoma • Pilocarpine HCl eye drops
1%,2%, 4%
• Isofluorophate
• Echothiopate iodide
• Domecanium bromide
• Physostigmine salicylate
• Neostigmine bromide
• Post trabeculoplasty glaucoma patients • Epinephrine
• Dipivefrine
• Apraclonidine eye drops
(not available in PH and
expensive)
• Short term relief of red and irritated eyes • Angle closure in narrow angles • Naphazoline HCl,
• Keratitis sicca (dry eye disease) • Tetrahydrozoline HCl
(Visine/EyeMo)
• allergic conjunctivitis • Burning, stinging, redness, drying, • Olopatadine
irritation and itchiness of the eyes • Pemirolast
• Pheniramine maleate
• Dry eye and ocular surface disease • Blurring of vision, eye redness, • Carboxymethylcellulose
discomfort and irritation, increased • Hypromellose
sensitivity to light, matting of • Sodium hyaluronate
eyelashes, excessive tearing • Polyethylene glycol
• Carbomer
• Lipid emulsion
 OPHTALMOLOGY –OCULAR PHARMACOLOGY
D. ANTI-INFLAMMATORY AGENTS
1. Non-Steroidal Anti- • Inhibition of prostaglandin
Inflammatory Agents biosynthesis inhibits action of
(NSAIDs) cyclooxygenase →
responsible for conversion to
prostaglandin – responsible
for pain
2. Corticosteroids • Decrease local generation
of prostaglandin and
leukotrienes
• Anti-inflammatory
3. Antibacterial Drugs • Bactericidal (kills) or
bacteriostatic (prevents
growth) by inhibition of
protein/ mucopeptide/ cell
wall/folic acid synthesis
4. Antiviral Agents • inhibits viral nucleic acid
synthesis
5. Antifungal Agents • fungicidal or fungistatic by
inhibition of ergosterol
synthesis (ergosterol – major
sterol of fungi backbone)
6. Intraocular Pressure
Lowering Agents
a. Beta Adrenergic • Reduce IOP by suppressing
Blocking Agents aqueous production.
• IOP reduction: 15-20%
b. Cholinergic • Increasing outflow facility by
Stimulating Drugs stimulating contraction of
the longitudinal ciliary
muscle.
• IOP reduction: 20-25%
c. Adrenergic Agonist • increase aqueous outflow
and decrease aqueous
production
• IOP reduction: 20-25%
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• Prevention of intra-operative miosis,
control of post- operative and
traumatic inflammation, vernal
keratoconjunctivitis, uveitis and scleritis
• post-operative inflammation, anterior
uveitis, severe allergic reactions
• For external eye infections (e.g.
conjunctivitis)
• Viral keratitis, viral conjunctivitis
• Fungal keratitis
• Open angle glaucoma
• Acute angle closure glaucoma
• vasoconstriction
• reduction of intra-ocular pressure
Contraindication:
patients taking MAO inhibitors (stimulates
the release of catecholamines → can
induce hypertension)
• Transient stinging and burning on • Diclofenac
instillation, ocular irritation, allergic • Nepafenac
reactions • Ketorolac
• steroid induced glaucoma • Prednisolone
• can induce elevation of intraocular • Dexamethasone
pressure, cataract, activation of • Fluorometholone
infection and corneal perforation
(with prolonged use)
• local conjunctival irritation, stinging, • Aminoglycosides (Topical:
burning, allergic reactions, Tobramycin)
sensitization • Bacitracin
• Chloramphenicol eyedrops
• Erythromycin eye ointment
• Quinolones (4th generation:
levofloxacin and
moxifloxacin – inhibits DNA
gyrase)
• Sulfonamides
• Polymyxin B
• nausea, diarrhea, fever, rash, • Ganciclovir (ointment
peripheral neuropathy
• • Natamycin, Voriconazole
• Transient ocular burning, stinging, • Timolol Maleate, Betaxolol
itching, discomfort, dryness HCl
• Systemic hypotension,
bronchospasm, diarrhea, amnesia
May penetrate systemic circulation
thus it is important to ask for history
of asthma, COPD
• Local → brow ache, blurring of • Pilocarpine 1-4% (available
vision, increase risk of pupillary block in the market is 2%)
due to forward shift of lens,
cataract, uveitis, retinal
detachment,
• Systemic → salivation, nausea,
vomiting, bronchospasm, intestinal
cramps, frequent urination
• dry mouth, blepharitis, conjunctival • Brimonidine
hyperemia, foreign body sensation, • Apraclonidine
drowsiness, dizziness, apnea in
children
 OPHTALMOLOGY –OCULAR PHARMACOLOGY
d. Prostaglandin • Decrease IOP by increasing • Primary open angle glaucoma, ocular • hypertrichosis, increase • Latanoporst
Analogs uveo-scleral outflow hypertension pigmentation of eyelid skin and iris • Bimatoprost
• IOP reduction: 25-30% • IOP >21mmHg with no evidence of color, conjunctival hyperemia, • Travoprost
optic nerve damage and no visual field cystoid macular edema, corneal • Taflotan
defect erosion, allergy
e. Carbonic Anhydrase reduces aqueous
• • stinging sensation, toxic keratitis, • Brinzolamide
Inhibitors production corneal endothelial dysfunction • Dorzolamide
• IOP reduction: 15-20%
SYSTEMIC DRUGS USED FOR OPHTHALMIC CONDITIONS
A. GLAUCOMA MEDICATIONS
1. Carbonic Anhydrase • IOP reduction: 40-50% • tingling sensation, nausea, vomiting, • Acetazolamide 250 mg/tab
Inhibitors • Draws out water from diarrhea, metabolic acidosis, blood
vitreous dyscrasia
• Can cause electrolyte imbalance →
advise to take meds with banana or
any fruit with high potassium
2. Osmotic Agents Increase serum osmolarity to
• • Acute angle closure glaucoma • Caution: CHF • Glycerol 50% oral
reduce intra-ocular water • Contraindication: Diabetes in • Mannitol 20% IV
• content glycerol use
B. ANTI-INFLAMMATORY AGENTS
1. Non-Steroidal Anti- • Inhibition of prostaglandin • ocular inflammation where steroids are • Gastric irritation, hyperacidity • Aspirin
Inflammatory Agents biosynthesis contraindicated • Indomethacin (selective
(Nsaids) action – COX-2 isozyme at
the site of inflammation → GI
friendly)
2. Corticosteroids • decrease local generation • posterior uveitis • moon facies, buffalo hump, acne, • Prednisone
of prostaglandin and • optic neuritis hyperglycemia, weight • IV Methylprednisone
leukotrienes • sympathetic ophthalmia • gain, hyperacidity • Dexamethasone
• anti-inflammatory • Hydrocortisone
Contraindications:
Diabetes Mellitus, hypertension,
hypothyroidism, cirrhosis, renal failure,
systemic and localized respiratory infection,
immunocompromised patients
C. ANTIBACTERIAL • Bactericidal or bacteriostatic • Severe intra-ocular infections, bacterial • Renal toxicity, hepatic toxicity, • Aminoglycosides, Penicillin,
DRUGS by inhibition of endophthalmitis, infections of the allergic reactions, nausea, vomiting Sulfonamides,
protein/mucopeptide/ cell adnexae and orbit or diarrhea Cephalosporins,
wall/folic acid synthesis Tetracycline,
Chloramphenicol,
Lincosamide
D. ANTIVIRAL AGENTS • inhibits viral nucleic acid • CMV retinitis, systemic viral infection • nausea, diarrhea, fever, headache, • Acyclovir, Ganciclovir
synthesis insomnia, rash, peripheral
neuropathy
E. ANTIFUNGAL AGENTS • fungicidal or fungistatic by • Fungal endophthalmitis, systemic fungal • Fluconazole, Itraconazole,
inhibiton of ergosterol infection Amphotericin B IV,
synthesis Ketoconazole

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OPHTALMOLOGY –OCULAR PHARMACOLOGY
OCULAR SIDE EFFECTS OF SYSTEMIC DRUGS
DRUG CLASSIFICATION OCULAR SIDE EFFECT
Allopurinol Anti-gout • Cataract
Amiodarone Anti-arrhythmic • Optic neuropathy
• Verticillata (whorl-
shaped pigmented
deposits in corneal
epithelium)
Biphosphonates Osteoclast • Conjunctivitis
inhibitor • Scleritis,
• uveitis
• orbital inflammation
Chloroquine/ Anti-malaria • Bull’s eye
Hydroxychloroquine maculopathy
• Retinopathy
• corneal deposits
Chlorpromazine Anti-psychotic • Corneal
• lenticular opacities
Corticosteroids Anti-inflammatory • Posterior subcapsular
cataract
• steroid induced
glaucoma
• acute and
aggravate acute
chronic serous
retinopathy
Digitalis Cardiac glycoside • Visual disturbance
(blurring of vision and
abnormality in color
vision)
Diphenylhydantoin Anticonvulsant • Nystagmus diplopia
• ophthalmoplegia
Ethambutol Anti-Koch’s • Toxic optic
neuropathy
HMG-COA Cholesterol • Cataract
reductase inhibitors lowering agent
(statins)
Rifabutin Anti-retroviral • Severe uveitis in
immunocompromised
patients
Sildenafil Phosphodiesterase • Color discrimination
inhibitor (blue color tinge of
vision)
• Non-arteritic ischemic
optic neuropathy
• Central serous
retinopathy
Tamoxifen Estrogen receptor • Corneal changes
antagonist (whorl-like opacities),
• Inner retinal crystalline
deposits
• Macular edema,
cataract
• Optic neuritis
Tamsulosin Alpha 1 • Flaccid iris
antagonist • Poor pupillary dilation
Thioridazine Anti-psychotic • Pigmentary
retinopathy
Topiramate Anti-seizure • Induce acute
bilateral angle
closure glaucoma

Sources:
• RER RGAR Trans 2020
• Lecture Guide in Ophthalmology

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