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OCULAR

PHARMACOLOGY
(SHORT NOTES)

Inaam Niyas
Batch of August 2013
Manipal College of Medical Sciences
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
CONTENTS
Anaesthetic Lignocaine & Bupivacaine
Antibiotics Ciprofloxacin
Polymyxin B
Antifungals Fluconazole
Natamycin
Antiglaucoma Acetazolamide
Dorzolamide
Brimonidine Tatrate
Levobunalol, Timolol & Betaxolol
Pilocarpine
Mannitol
Anti-inflammatory Dexamethosone
Flurbiprofen
Antivirals Acyclovir
Mydriatics Atropine
Tropicamide
Phenylephrine
Miscellaneous Carboxymethyl Cellulose
Catarest Eye Drops
Napahzoline

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


ANAESTHETICS
LIDOCAINE / LIGNOCAINE / XYLOCAINE & BUPIVACAINE

1. Group and Mechanism of Action


a. Group – Local Anesthetic (LA)
b. Mechanism of Action – LA travels across the axon membrane in its unionized form to enter the
axoplasm. It then reionizes and binds with the LA receptor, within the intracellular mouth of the
Na+ channel. The receptor has higher affinity, or is more accessible to the LA in the activated as
well as inactivated states compared to the resting state. Binding of LA to its receptor stabilizes
the channel in the inactivated state and thus reduces the probability of channel opening.
2. Concentration, Dose and Duration
a. Concentration – 2% - 4%
b. Dose and Duration
 Topical Effect -1drop 4times every 4min
 Van Lint‟s Nv. block – 1-2% 2.5ml inj
 Facial Nv. trunk block – 1-2% 4-6ml inj
 Retrobulbar block – 2ml of solution (consisting of 2% lignocaine)
 Peribulbar block – 6-7ml of solution (consisting of 2% lignocaine)
3. Combinations and Uses
a. Combinations –
 Adrenaline – to achieve bloodless field and to extend duration of anesthetic while
reducing systemic effect (Lignocaine + 1:100,000 Adrenaline)
 Hyaluronidase – (in peribulbar block, 5IU/ml) degrade the connective tissue of the
peripheral spaces so that anesthesia can reach the retrobulbar space.
 Bupivacaine - (in peribulbar block, 0.5-0.75%) (Ligno:bupi=2:1). Is long acting but with
slow onset, so the combination results is rapid onset, long acting anesthesia.
b. Uses –
i. All ocular Surgeries
ii. Before scraping corneal ulcer to obtain sample for culture an microscopy
iii. Before Laser procedure
iv. Before Lacrimal Syringing
v. Before removing corneal foreign body, foreign body impacted in bulbar conjunctiva
4. Side Effects
a. Ocular –
 Healing Delay, Burning, Itching, Stinging
 Conjunctival Hyperaemia, Corneal Epithelial Changes
b. Systemic –
 Dizziness
 Disorientation
 Oculocardiac Reflex (Bradycardia / Cardiac Arrhythmia / Hypotension)
 Headache
 Contact sensitization
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
5. Contraindications
a. Hypersensitivity to amide local anaesthetics

NOTE:

 Bupivacaine is same as Lignocaine but given as 0.5-0.75% concentration, usually in combination


with Lignocaine
 Effects of Anaesthesia
o Anaesthesia (Lack of sensation)
o Analgesia (Lack of pain)
o Akinesia (Lack of movement)
o Decreased IOP
o Mydriasis
o White eye (Decreased congestion)

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


ANTIBIOTICS
CIPROFLOXACIN
1. Group and Mechanism of Action
a. Group – First Generation Flouroquinolone
b. Mechanism of Action – Bactericidal (Primarily against gram negative)
 In Gram Negative Bacteria FQs inhibit the enzyme bacterial DNA gyrase (primarily
active in gram negative bacteria), which nicks double stranded DNA, introduces negative
supercoils and then reseals the nicked ends. This is necessary to prevent excessive
positive supercoiling of the strands when they separate.
 In Gram Positive Bacteria the major target of FQ action is a similar enzyme
topoisomerase IV which nicks and separates daughter DNA strands after DNA
replication.
2. Concentration, Dose and Duration
a. Concentration –
 3mg/ml (0.3%) solution
 3.3mg/g ointment
b. Dose and Duration -
 Drops: 1-2 drops every 1-4 hourly
 Ointment: 1.25cm ribbon applied to conjunctival sac every 8-12 hourly
3. Combinations and Uses
a. Combinations – Ciprofloxacin 0.3% + Dexamethosone 0.1%
b. Uses –
 Bacterial ocular infections like Conjunctivitis, Ulcerative and Non-Ulcerative Keratitis,
Infectious Scleritis, Purulent Uveitis, Bacterial Blepharitis
 As an umbrella cover when using steroids for allergic conjunctivitis, iridocyclitis etc.
 To prevent bacterial superinfection in viral infections
4. Side Effects
a. Ocular –
 Burning, Itching, Stinging
 Ciprofloxacin precipitate in superficial portion of corneal defect
 Conjunctival hyperemia
 Crystals or scales on eyelashes
 Foreign-body sensation
b. Systemic –
 Headache, Dysgeusia, Nausea
 Rarely: Hypersensitivity, Dermatitis, Dizziness
5. Contraindications
a. Hypersensitivity to the active substance 0.06mg of benzalkonium chloride
b. Hypersensitivity to quinolones.

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


POLYMYXIN B
1. Group and Mechanism of Action
a. Group – Polypeptide Antibiotic
b. Mechanism of Action – A rapidly acting bactericidal agent; have a detergent-like action on the
cell membrane. They have high affinity for phospholipids. The peptide molecules (or their
aggregates) orient between the phospholipid and protein films in gram-negative bacterial cell
membrane causing membrane distortion or pseudopore formation. As a result ions, amino acids,
etc. leak out.
2. Concentration, Dose and Duration
a. Concentration – Available in 5,000IU – 10,000IU
b. Dose and Duration - 1drop x 8hrly x 7-10 days
3. Combinations and Uses
a. Combinations - Exhibit synergism with many other antimicrobials by improving their
penetration into the bacterial cell. Can be combined with
 Other Antibiotics - Chloramphenicol, Neomycin, Bacitracin, Gramicidin
 Corticosteroids - Dexamethasone, Hydrocortisone
b. Uses –
 Used for gram negative infections especially Pseudomonas. Nowadays it is almost
exclusively used for Pseudomonas infection.
 Bacterial ocular infections like Conjunctivitis, Ulcerative and Non-Ulcerative Keratitis,
Infectious Scleritis, Purulent Uveitis, Bacterial Blepharitis
 As an umbrella cover when using steroids for allergic conjunctivitis, iridocyclitis etc.
 To prevent bacterial superinfection in viral infections
4. Side Effects
a. Ocular –
 Blurry vision
 Hypersensitivity (Lid Edema, Itching, Increased redness, Tearing, Circumcorneal rash)
 Local irritation
b. Systemic –
 IV - Flushing, Parasthesia, Kidney Damage, Neurological disturbances, Neuromuscular
blockade.
 Oral – Nausea, Vomiting, Diarrhea
5. Contraindications
a. No effect on gram positive organisms
b. Relative contraindications in CKD, Myasthenia gravis
c. Absolutely contraindicated in known hypersensitivity to polypeptide antibiotics (Polymyxin and
Colistin)

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


ANTIFUNGAL AGENTS
CLASSIFICATION
1. Polyene Antifungals
a. Nystatin
b. Natamycin
c. Amphoteracin B
2. Imidazole Antifungals
a. Miconazole
b. Econazole
c. Clotrimazole
d. Fluconazole
e. Ketoconazole
f. Itracnzole
3. Pyridine Antifungals
a. Flucystosine
4. Silver Compounds
a. Silver Sufadiazine

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


FLUCONAZOLE
1. Group and Mechanism of Action
a. Group – First Generation Triazole Antifungal
b. Mechanism of Action – Inhibits the fungal cytochrome P450 enzyme “lanosterol 14α-
demethylase”. This inhibition prevents the conversion of lanosterol to ergosterol, an essential
component of the fungal cytoplasmic membrane. Fluconazole is primarily fungistatic; however,
it may be fungicidal against certain organisms in a dose-dependent manner,
specifically Cryptococcus.
2. Concentration, Dose and Duration
a. Concentration –
 Topical: 0.3%
 Oral: 50, 100, 150, 200mg tablets
 IV: 200mg/100ml
b. Dose and Duration –
 In Fungal Ketatitis - One drop 2 hourly initially then reduce to One drop 6 to 8 times
daily after 3 to 4 days..Therapy should generally be continued for 14 to 21 days or until
there is resolution of active fungal keratitis.
 In Fungal Blepharitis and conjunctivitis - Less frequent initial dosage (4 to 6 daily
applications) may be sufficient
3. Combinations and Uses
a. Combinations –
b. Uses –
 Fungal keratitis / Corneal Ulcer
 Used against Candida, Aspergillus, Cryptococcus
4. Side Effects
a. Ocular –
 Burning, Itching, Stinging
b. Systemic –
 Headache
 Stomach discomfort, Gastritis
 Cardiac arrhythmias
 Hepatotoxicity
5. Contraindications
a. Known hypersensitivity to other azole medicines such as ketoconazole
b. If patient is also on Terfenadine, Quinidine, SSRIs such as fluoxetine or sertraline.

Caution: High doses of fluconazole during the first trimester of pregnancy may be associated with a rare
and distinct set of birth defects in infants.

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


NATAMYCIN
1. Group and Mechanism of Action
a. Group – Antifungal drug (Polyene)
b. Mechanism of Action – It binds to the sterol moiety of the fungal cell membrane. The
polyenesterol complex alters the permeability of the membrane to produce depletion of essential
cellular constituents. Although the activity against fungi is dose-related, Natamycin is
predominantly fungicidal.
2. Concentration, Dose and Duration
a. Concentration –5% suspension
b. Dose and Duration –
 In Fungal Ketatitis - One drop 2 hourly initially then reduce to One drop 6 to 8 times
daily after 3 to 4 days..Therapy should generally be continued for 14 to 21 days or until
there is resolution of active fungal keratitis.
 In Fungal Blepharitis and conjunctivitis - Less frequent initial dosage (4 to 6 daily
applications) may be sufficient
3. Combinations and Uses
a. Combinations –
b. Uses –
 Fungal keratitis
 Fungal blepharitis
 Fungal conjunctivitis
 Used against Aspergillus, Fusarium, Cephalosporium
4. Side Effects
a. Ocular –
 Mild eye irritation or discomfort (redness stinging or burning)
 Allergic reaction
 Change in vision
 Corneal opacity
 Eye swelling
 Eye pain
 Weakness
b. Systemic –
 Chest Pain
 Shortness of Breath
5. Contraindications
a. Hypersensitivity to Natamycin or any of its components

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


ANTIVIRALS
ACYCLOVIR
1. Group and Mechanism of Action
a. Group - Antivirals
b. Mechanism of Action – It inhibits the viral
DNA, preferentially entering the infected cells,
with little effects on normal cells. It penetrates
int the deep layers and thus is very effetive in
stromal keratitis.

2. Concentration & Dose


a. Concentration:
i. Ointment ( 3%, 5% cream)
ii. Tablet (200 mg, 400mg, 800mg)
iii. Injections for IV
b. Dose:
i. Herpes simplex infections: 400 mg 5 times a day for 4-5 days
ii. Herpes zoster infections :
 Tablet 800 mg 5 times a day for 10 days
 Ointment 3% 5 times a day for 2 weeks
iii. Varicella zoster: 4times a day for 5 days
 dose:
 >6 yrs: 800 mg
 2-5yeras: 400 mg
 <2 years: 200 mg
iv. For immunocompromised and serious cases such as herpetic encephalitis, acyclovir is
given intravenously.
3. Combination & Uses
a. Combination
i. With corticosteroid
b. Uses
i. Topically:
 Stromal herpes simplex keratitis
 Cold sores/ fever blisters (herpes labialis)
ii. Oral:
 Penetrating keratopathy in patients suffeing from herpes simplex keratitis
 Recalcitrant stromal or uveal disease cause by herpes simplex virus
 To reduce complications of keratitis and uveitis in herpes zoster opthalmicus.
4. Side Effects
 Slight punctate epithelial keratitis which ceases once the drug is stopped.
 Other effects include headache, diarrhoea, rashes, itching, sensitivity to light, alopecia etc.
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
ANTIGLAUCOMA DRUGS
6. Prostaglandin Analogues
Classification  Latanoprost, Bimatoprost,
1. Parasympathomimetic Drugs Travoprost, Unoprostone
a. Direct Acting (Agnonists)
 Pilocarpine Mechanism of Action of Antiglaucoma Drugs
b. Indirect Acting (Cholinesterase 1. Increase Trabecular Outflow
Inhibitors) a. Miotics
 Reversible (Physostigmine) b. Epinephine, Dipivefrine
 Irreversible (Echothiophate c. Bimatoprost
iodide, Demecarium 2. Increase Uveoscleral Outflow
bromide) a. Latanoprost
c. Dual Action (Both Muscarinic b. Epinephrine, Dipivefrine
Agonist + Weak Cholinesterase c. Brimonidine
Inhibitor) d. Apraclonidine
 Carbachol 3. Decrease Aqueous Production
2. Sympathomimetic Drugs a. CA Inhibitors (Acetazolamide,
a. Both Alpha and Beta Stimulators Dorzolamide)
 Epinephrine, Dipivefrine b. Beta Blockers (Timolol, Betaxolol,
(Prodrug converted to Epi) Levobunolol)
b. Selective Alpha Stimulators c. Alpha Receptor Stimulators
 Clonidine, Apraclonidine, (Epinephrine, Dipivefrine,
Brimonidine Brimonidine, Clonidine,
3. Beta Blockers Apraclonidine)
a. Non-selective Beta Blockers 4. Hyperosmotic Agents
 Timolol, Levobunolol a. Glycerol
b. Selective Beta-1 Blockers b. Mannitol
 Betaxolol
4. Carbonic Anhydrase Inhibitors
a. Systemic CA Inhibitors
 Acetazolamide,
Dichlorphenamide,
Methazolamide,,
Ethoxzolamide
b. Topical CAS Inhibitors
 Dorzolamide, Brinzolamide
5. Hyperosmotic Agents
a. Oral
 Glycerol, Isosorbide
b. Intravenous
 Mannitol, Urea

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


ACETAZOLAMIDE

1. Group and Mechanism of Action


a. Group – Systemic Carbonic Anhydrase Inhibitor
b. Mechanism of Action – It inhibits the Carbonic Anhydrase enzyme present in the ciliary body
which results in decreased aqueous humor formation. Acetazolamide reduces the production of
aqueous by 30-40% and substantially lowers the intraocular pressure.
2. Concentration & Dose
Available as 250 mg tablets (250–1000 mg daily in divided doses), sustained-release 250 mg
capsules (250–500 mg daily) and 500 mg powder vials for injection (single dose, typically used
in acute angle-closure glaucoma)
Usually given at mornings
3. Uses
i. Commonly used in acute angle-closure glaucoma
500mg IV Stat followed by 250mg TDS
ii. Secondary glaucomas.( long-term use is reserved for patients at high risk of visual loss)
iii. Used for controlling very high intraocular pressures in acute cases for short term in other
glaucoma. Usually treatment not given longer than 3 days.
iv. Long-term use is reserved for patients at high risk of visual loss
v. Congenital Glaucoma: to lower the IOP till surgery is taken up
4. Side Effects
a. Ocular –
i. Choroidal effusion, particularly after cataract surgery. Angle closure may result
b. Systemic –
i. Parasthesia
ii. Urinary Frequency
iii. Potassium Depletion
Seen if simultaneously taking corticosteroids, aspirin or thiazide.
iv. Bicarbonate Depletion  Metabolic Acidosis
v. GI Symptom Complex: Abdominal discomfort, gastric irritation, nausea, diarrhoea
vi. Sulfonamide Related (rare)
Renal calculi, blood dyscrasias, SJS
5. Contraindications
a. Sulfonamide („sulfa‟) allergy is a relative contraindication.
b. Patients of BPH and Renal Failure
c. Patients with cirrhosis as may contribute to development of hepatic encephalopathy and
hyperammonemia
6. Alternative Agents
a. Dichlorphenamide 50 mg tablets (50–100 mg two or three times daily).
Less metabolic acidosis
b. Methazolamide 50 mg tablets (50–100 mg two or three times daily); this has a longer duration of
action than acetazolamide. Also less likelyto cause renal stones and acidosis as compared to
acetazolamide

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


DORZOLAMIDE

1. Group and Mechanism of action


a. Group :- Carbonic Anhydrase Inhibitors
b. MOA: - Carbonic Anhydrase is an enzyme that‟s present in the ciliary body of the eye. It functions
in carbon dioxide and bicarbonate transport and H+ ion secretion. Direct antagonistic activity on the
ciliary epithelium CA enzyme decreases the production of aqueous which in turn lead to the
decrease in intraocular pressure.

It is a topically useful carbonic anhydrase inhibitor developed to avoid the systemic side effects of
Acetazolamide. It lowers the intraocular pressure by around 20%, somewhat less efficacious than
Timolol.

2. Concentration, Dose and Duration


a. Concentration:- 2%
b. Dose and duration:- 1 eye drop X 3 times or X 2 times

3. Combinations and Uses


a. Combinations :- Can be combined with topical beta blockers and prostaglandin analogues
b. Uses :- for treatment of open angle glaucoma
Used only as add on drug to topical beta blockers and PG analogues or when these drugs are
contraindicated.

4. Side Effects
a. Ocular :- ocular stinging, burning sensation, itching, punctate keratitis, lacrimation, corneal oedema,
b. Systemic :- headache, paresthesia, sinusitis, malaise, fatigue, depression, gastric irritation, metallic
taste, diarrhoea, hypersensitivity reactions, epistaxis, urolithiasis, Stevens Johnsons syndrome

5. Contraindications
a. Hypersensitivity
b. Severe renal impairment
c. Metabolic acidosis
d. Lactation
e. Endothelial dysfunction

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


BRIMONIDINE TARTRATE

1. Group and Mechanism of Action


a. Group – Selective Alpha 2 Adrenergic Agnoist
b. Mechanism of Action – It decreases the aqueous synthesis and increases the amount of aqueous
drain from eye through uveoscleral flow. Also has a vasoconstrictor effect
2. Concentration & Dose
a. Concentration: 0.2%, 0.5%
b. Dose: 1 drop 2 times a day
3. Combination & Uses
a. Combination
i. With other Anti-Glaucomna drugs (Timolol, Latanoprost)
b. Uses
i. POAG
ii. Ocular HTN
4. Side Effects
a. Systemic –
i. Oral dryness
ii. Headache
iii. Upper Respiratory Symptoms
b. Ocular –
i. A – Allergic Blepharoconjunctivitis
ii. B –
1. Blurred Vision
2. Burning Sensation
iii. C –
1. Conjunctival Hyperaemia
2. Conjunctival Pigmentation
3. CME (in Aphakics)
iv. Mydriasis
5. Contraindications
a. Hypersensitivity to Brimonidine or it‟s components
b. Patients on Monoamine Oxidase (MAO) Inhibitor Therapy

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


LEVOBUNOLOL HYDROCHLORIDE & TIMOLOL MALEATE
1. Group and Mechanism of Action
a. Group – Beta adrenergic blocker
b. Mechanism of Action –Nonselective beta 1(cardiac) and beta 2 ( smooth muscle) blocker.
Lowers IOP by blockade of beta 2 receptors in ciliary process causing decreased aqueous
production by blockade of catecholamine stimulated increases in cyclic adenosine
monophosphate (cAMP) concentrations within the ciliary processes. Also decrease the ocular
blood flow which decreases ultrafiltration responsible for aqueous production.
2. Concentration, Dose and Duration
a. Concentration – Available in 0.25% and 0.5%solution
b. Dose- One to two drops in the affected eye(s) twice a day
3. Combinations and Uses
a. Combinations - Dipivefrine, epinephrine, pilocarpine and other miotics, prostaglandin analogues,
brimonidine.
b. Uses –
 All types of glaucoma - developmental, primary, secondary, open or closed angle, first
choice drug if prostaglandin analogues are unaffordable
 Ocular hypertension
 To lower IOP in Corneal Ulcer with impending perforation, CRAO / CRVO
4. Side Effects
a. Ocular –
 Burning and conjunctival hyperemia
 Superficial punctate keratopathy
 Corneal anesthesia
b. Systemic –
 Cardiovascular (due to Beta 1) -bradycardia, arrhythmias, heart failure and syncope
 Pulmonary(due to Beta 2) - bronchospasm and airways obstruction
 Central nervous system - anxiety, depression, confusion, drowsiness, hallucination,
emotional liability
 Miscellaneous - nausea, diarrhoea, impotence, skin rashes, alopecia, exacerbation of
myasthenia gravis
5. Contraindications
a. Relative contraindications - depends on the severity of bronchial asthma, emphysema, COPD,
heart blocks, congestive heart failure, cardiomyopathy.
b. Absolutecontraindication-Drug allergy

NOTE: Timolol has phenomenon of short term escape & long term drift.
 Short term escape - implies marked initial fall in IOP followed by transient rise with continued
moderate fall in IOP.
 Long term drift -implies slow rise in IOP in patients who were well controlled with many months
of therapy.
Betaxolol is a cardioselective Beta Blocker and thus can be safely used in patients with Pulmonary Ds.

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


MANNITOL
1. Group and Mechanism of Action
a. Group – Hyperosmotic Agent
b. Mechanism of Action – It increases the plasma tonicity .The osmotic pressure gradient created
between the blood and vitreous draws sufficient water out of the eye ball thereby significantly
lowering the IOP
2. Concentration, Dose and Duration
a. Concentration – Available as a 20% solution
b. Dose- 1-2g/kg body weight administered very rapidly over 20-30 minutes
3. Combinations and Uses
a. Combinations - None
b. Uses –
 All types of glaucoma - Increased IOP – (acute congestive glaucoma, Secondary
glaucoma)
 Increased intracranial tension / Cerebral Edema
 Impending acute renal failure
 Dialysis disequilibrium
4. Side Effects
 Headache
 Nausea
 Hypersensitivity Reactions
5. Contraindications
a. Relative contraindications – should be used cautiously in hypertensive patients
b. Absolute contraindication-
 Drug allergy
 Renal Failure
 Congestive Cardiac Failure
 Pulmonary edema
 Cerebral hemorrhage

NOTE: Unlike Oral Glycerol, Mannitol is not metabolized into glucose, thus it is not contraindicated in
Diabetics.

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


PILOCARPINE
1. Group and Mechanism of Action
a. Group – Antiglaucoma (Direct Acting Parasympathomimetic)
b. Mechanism of Action –
 In POAG- Contraction of the longitudinal muscle of ciliary body, which exerts a pull on
scleral spur, cause changes in the trabecular meshwork, enhance outflow, reduce IOP
 In PACG- Miotic action of pilocarpine involved. Mechanical contraction of the pupil,
moves the peripheral iris away from trabecular meshwork.
2. Concentration, Dose and Duration
a. Concentration –
 Eye drops- 1% , 2%, 4%
 Ocuserts (pilo-20,pilo-40) - they are changed every week
 Pilocarpine gel (4%)
b. Dose and Duration –
3. Combinations and Uses
a. Combinations – With other antiglaucoma drugs (Eg:Timolol, Latanoprost)
b. Uses –
 POAG
 Acute ACG
 Chronic Synechial ACG
 Due to availability of many better drugs it is no longer considered a first line treatment.
Sometimes still used when a cardiac diseased person is undergoing glaucoma surgery
4. Side Effects
a. Ocular –
 Due to miosis - Reduced visual acuity in the presence of polar cataracts, Impairment of
night vision, Generalized constriction o visual fields
 Due to spasm of accommodation - Myopia, Frontal Headache
 Retinal Detachment
 Lenticular opacities (Anterior Subcapsular Cataract)
 Iris Cyst formation
 Mild Iritis
 Lacrimation (prolonged use can also cause punctual occlusion  Lacrimation)
 Follicular conjunctivitis
b. Systemic –
 Bradycardia, Sweating, Diarrhoea, Excessive salivation, Anxiety
5. Contraindications
a. Absolulte Contraindications
 Inflammatory Glaucoma and Malignant Glaucoma
 Hypersensitivity to any of it‟s components
b. Relative Contraindications
 Children – do not tolerate spasm of accommodation
 Adults with Cataract (Nuclear or Central Cortical Opacity) – marked visual disturbance
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
ANTI-INFLAMMATORY
DEXAMETHASONE
1. Group and Mechanism of Action
a. Group – Corticosteroid (Long Acting)
b. Mechanism of Action –
 Suppress the formation of arachadonic acid and other inflammatory mediators by
induction of phospholipase A2 inhibitory proteins (lipocortins). Lysosomal membranes
are stabilized and the production of leukotrienes and prostaglandins decreased.
 Anti-inflamatory, Anti-allergic and Anti-fibrotic action
2. Concentration, Dose and Duration
a. Concentration –
 Eye drops- 0.1%
 Ointment - 0.5%
 Tablets – 0.5, 1, 2, 4mg
 IV – 4mg/ml solution
b. Dose and Duration –
 Eye drops 4-6 times a day and eye ointment at bed time
3. Combinations and Uses
a. Combinations – With antibiotics (Eg:Neomycin, Chloramphenicol, Polymyxin B)
b. Uses –
 Uveitis (Anterior, Intermediate and Posterior), Sympathetic Ophthalmitis
 Non-infectious Scleritis
 Allergic Conjunctivitis and Keratitis
 Herpes Zoster Keratitis, Iridocyclitis and Scleritis
 Endophthalmitis (24-48 hrs after control of infection to limit the tissue damage)
 Acute Congestive Glaucoma to reduce inflammation
 Chemical Injury to Eye (Not used for more than 2 weeks)
 Cystoid Macular Edema
 After intraocular surgery
4. Side Effects
a. Ocular –
 Steroid induced glaucoma
 Drug induced Cataract (Posterior subcapsular cataract)
 Activation of infection
 Dry Eye
 Ptosis
 Central Retinal Vein Occlusion
 Delayed wound healing
b. Systemic – CUSHINGOID
 C – Central obesity
 U – Peptic Ulcers
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
 S – Skin: striae, thinning, bruising
 H – Hypertension/ Hirsutism/ Hyperglycemia
 I – Infections
 N – Necrosis (Avascular necrosis of the femoral head)
 G – Glycosuria
 O – Osteoporosis
 I – Immunosuppression
 D –Diabetes
5. Contraindications
 Ocular infections

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


FLURBIPROFEN
1. Group and Mechanism of Action
a. Group – NSAID (Non-Selective COX Inhibitor)
b. Mechanism of Action –
 They act by irreversibly blocking the enzyme cyclo-oxygenase 1 & 2, thus inhibiting
prostaglandin biosynthesis which gives rise to its antipyretic, analgesic and anti-
inflammatory action.
2. Concentration, Dose and Duration
a. Concentration –
 Eye drops- 0.3%
 Tablets – 50, 100 150mg
b. Dose and Duration –
 Eye drops – 1 drop 6 hrly
 Tablets – BD or QID
3. Combinations and Uses
a. Combinations –
 With Hydroxypropylmethyl Cellulose
 With Antibiotics like Gatifloxacin and Chloramphenicol
b. Uses –
 Preventing post-op CME in cataract surgery
 To maintain dilatation of pupil in cataract surgery
 Episcleritis and Scleritis
 Uveitis (Not as a primary agent but as long term therapy in recurrent uveitis initially
controlled by steroids)
 Conjunctivitis, Pingiculitis, Inflamed Pterygium
 Stye, Hordeolum Internum
 Corneal Ulcers
4. Side Effects
a. Ocular –
 Burning, Itching, Stinging
 Slows corneal wound healing
 Fibrosis
b. Systemic –
 Nausea Vomiting, Gastric discomfort
 Dizziness, Headache, Tinnitus
5. Contraindications
 N – Nursing mother (Pregnancy)
 S – Severe Bleeding
 A – Allergic to NSAIDs / Asthmatic Patients / Angioedema
 I – Impaired Renal Function
 D – Drugs (Anticoagulants)

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


MYDRIATICS
ATROPINE
1. Group and Mechanism of Action
a. Group – Anticholinergic (Natural Alkaloid)
b. Mechanism of Action –
 Dilates pupil causing mydriasis and impair accommodation leading to cyclopegia
(paralysis of the ciliary muscle)
 Atropine causes mydriasis by blocking contraction of the circular sphincter pupillae
muscle which is normally stimulated by Ach release, thereby allowing the unopposed
action of radial dilator pupillae muscle to contract and dilate the pupil
 Peak Effect  2-3 days
 Effect lasts for  10-20 days
2. Concentration, Dose and Duration
a. Concentration –
 1% Eye Ointment
 1% Eye Drops
b. Dose and Duration –
 For retinoscopy - Ointment applied TDS for 3 days and Retinoscopy performed on the 4 th
day
 For Keratitis / Uveitis – Ointment or drops BD-TDS applied for at least 2-3weeks after
the eye becomes quiet
3. Combinations and Uses
a. Combinations –
 With Prednisolone / Dexamethasone
 With Antibiotics like Chloramphenicol
 With Chlorobutanol (Preservative and weak local anaesthetic)
b. Uses –
 Diagnostic
 For refraction / retinoscopy in children <5 yrs (hypermetropia)
 For fundus examination in children <5 yrs
 Therapeutic
 In iridocyclitis / keratitis
a. Gives comfort and rest to the eye by relieving spasm of iris sphincter and
ciliary muscles
b. Prevents the formation of synechiae and breaks already formed synechiae
c. Reduces exudation by decreasing vascular permeability
d. Increases blood supply to the anterior uvea by relieving pressure on the
anterior ciliary arteries. As a result, more antibodies reach the target
tissues and more toxins are absorbed
 For Atropine Penalization in children with Amblyopia
 Hyphaema / Vitreous Hemorrhage
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
 Postoperatively after cataract surgery
 Used IV/IM in Mushroom/ OP Poisoning
4. Side Effects
a. Ocular –
 Diplopia, Blurring of vision
 Photophobia
 May precipitate angle closure -> Increased IOP
 Allergic Reactions
b. Systemic –
 Dryness of mouth
 Dry hot skin
 Dysarthria
 Dysphagia
 Dilatation of cutaneous blood vessels (Facial Flushing)
 Drunken gait
 Delirium
 Drowsiness
 On Examination:
 Diminished bowel sounds
 Distension of urinary bladder with urinary retension
 Rapid pulse and Respiratory Rate
 Scarlatiniform rash over the body

5. Contraindications
a. Rupture of papillary margins
b. Subluxation of lens
c. Elderly patients with shallow anterior chamber / Hypermetropia
d. Primary Angle Closure Suspects
e. Prostate hypertrophy

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


TROPICAMIDE
1. Group and Mechanism of Action
a. Group – Mydriatics / Cycloplegics
b. Mechanism of Action –
 Dilates pupil causing mydriasis and impair accommodation leading to cyclopegia
(paralysis of the ciliary muscle)
 Atropine causes mydriasis by blocking contraction of the circular sphincter pupillae
muscle which is normally stimulated by Ach release, thereby allowing the unopposed
action of radial dilator pupillae muscle to contract and dilate the pupil
 Peak Effect  20-40 min
 Effect lasts for  4-6 hrs
2. Concentration, Dose & Duration
a. Concentration:
i. Eye Drops – 0.5%, 1%
b. Dose and Duration –
i. For Retinoscopy – 1 drop every 15 minutes for 4 times
ii. Ocular surgery- Phenylephrine 2.5% + Tropicamide 1% Every 15 minutes for 4 times
iii. For Keratitis / Uveitis – 3-4 times a day for at least 2-3weeks after the eye becomes quiet
3. Combination & Uses
a. Combination
i. With tropicamide (to produce mydriasis before ocular surgery)
b. Uses
 For refraction / retinoscopy / fundus examination – Not used as a cycloplegic but only for
mydriasis
 To produce mydriasis before ocular surgery
 To produce mydriais in patients with small central lenticular opacity
 For mydriatic provocation test in Primary Angle Closure Suspect
4. Side Effects
a. Ocular –
i. Diplopia / Blurred Vision
ii. Photophobia
iii. May precipitate angle closure -> Increased IOP
iv. Allergic Reactions
v. Transient stinging
b. Systemic –
i. Dry mouth
ii. Tachycardia
iii. Headache
5. Contraindications
a. Rupture of papillary margins
b. Subluxation of lens
c. Elderly patients with shallow anterior chamber / hypermetopia
d. Primary Angle Closure Suspects
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
PHENYLEPHRINE

1. Group and Mechanism of Action


a. Group –Mydriatics, alpha-agonists
b. Mechanism of Action – Acts directly on alpha-adrenergic receptors in eye producing contraction
of dilator muscle of pupil and constriction of arterioles in conjunctiva.
 Peak Effect  30-40 min
 Effect lasts for  4-6 hrs
2. Concentration, Dose and Duration
a. Concentration – Available as 5% and 10% eye drops
b. Dose and Duration –
i. For Retinoscopy – 1 drop every 15 minutes for 4 times
ii. Ocular surgery- Phenylephrine 2.5% + Tropicamide 1% Every 15 minutes for 4 times
3. Combinations and Uses
a. Combinations –
i. With atropine (in anterior uveitis to prevent posterior synechiae)
ii. With tropicamide (to produce mydriasis before ocular surgery)
iii. With naphazoline (before ocular surgeries)
b. Uses –
i. For mydriasis production (for ophthalmoscopy, before ocular surgeries)
ii. For posterior synechiae prevention (in anterior uveitis and post-iridectomy)
iii. To produce mydriais in patients with small central lenticular opacity
iv. For mydriatic provocation test in Primary Angle Closure Suspect
v. In eye redness (to decrease the redness of eye)
4. Side Effects
a. Ocular –
i. Transient burning or stinging
ii. Blurred vision
iii. Rebound miosis
iv. Transient keratitis
v. Allergic conjunctivitis
vi. Sensitivity to light
b. Systemic –
i. Arrhythmia
ii. Myocardial infarction
iii. Subarachnoid haemorrhage
iv. Headache or browache
5. Contraindications
a. Rupture of papillary margins
b. Subluxation of lens
c. Elderly patients with shallow anterior chamber / Hypermetropia
d. Primary Angle Closure Suspects
e. Hypersensitivity
f. Hypertension
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
MISCELLANEOUS
CARBOXYMETHYL CELLULOSE
1. Group and Mechanism of Action
a. Group – Lubricating Agents / Teat Substitutes / Artificial Tears
b. Mechanism of Action – Each ingredient has a specific function
 Ingredients -
 Balanced amount of inorganic electrolytes- maintain ocular tonicity (0.9% NaCl)
 Buffers – boric acid – adjust pH
 Viscosity agents (water soluble polymer) - MAIN ingredient. Enhance viscosity
and promote tear film stability. Carboxymethyl Cellulose.
 Preservative – maintain solution sterility- benzalkonium chloride, chlorobutanal,
thimerosal
2. Concentration, Dose and Duration
a. Concentration – 0.5%
b. Dose and Duration – 1-2 drops as needed in the affected eye
3. Combinations and Uses
a. Combinations –
 With polyvinyl pyrrolidone and/or other polymers
 With Vitamin A
 With certain lipids
b. Uses –
 Dry Eye
 Aqueous Deficiency Dry Eye
a. Sjogren‟s Syndrome (Primary Keratoconjunctivits Sicca)
b. Non-Sjogren‟s Keratoconjunctivitis Sicca
i. Primary Age Related Hyposecretion
ii. Lacrimal Gland Deficiencies
1. Congenital Alacrima
2. Infiltrations of the lacrimal gland by tumour, sarcoid, post-
radiation fibrosis
3. Surgical Removall
iii. Lacrimal Gland Duct Obstruction
1. Cicatrizing Trachoma
2. Thermal and Chemical Burns
3. SJS, Cicatricial Pemphigoid
iv. Reflex Hyposecretion
1. Familial Dysautonomia (Riley Day Syndrome)
2. Parkinson‟s Disease
3. Reflex Sensory Block
4. Reflex Motor Blade
5. Paralysis of Facial Nerve
OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas
6. Reduced Corneal Sensation
 Evaporative Dry Eye
a. Meibomian Gland Dysfunction
i. Chronic Posterior Blepharitis
ii. Rosacea
iii. Congenital Absence of Meibomian Glands
b. Lagophthalmos
i. Facial Nerve Palsy
ii. Severe Proptosis
iii. Symblepharon
c. Defective Blinking such as low blink rate in computer users
d. Vitamin A Deficiency
e. Others
i. Topical Drugs
ii. Contact Lens Wear
iii. Ocular Surface Allergic Diseases and Scarring Disorders
 Preventing recurrences of Pterygium
 Symptomatic relief in Corneal Ulcers, Conjunctivitis
4. Side Effects
a. Ocular –
 Rarely slight irritation and blurring of vision
b. Systemic –
 None
5. Contraindications
a. Do not drive or operate machinery until vision is clear

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


CATAREST EYE DROPS
Composition: Sodium Chloride (0.83%)
Calcium Chloride (1%)
Potassium Iodide (3.3%)
Mechanism of Action: Maintain proper fluid balance and keep tissue hydrated
Increase calcium levels
Reducing the chance of radioactive iodine swallowing
Uses:
1) Early stages of cataract to delay progression
2) Low sodium levels
3) Low potassium levels
4) Low calcium levels
5) Blood and fluid loss
6) Protect thyroid gland from toxic effects of radioactive iodine
Side effects:
1) Reduced Salivation
2) Fever
3) Flow of tears
4) Hypernatraemia
5) Thirst
6) Coma
Contraindications:
1) Abnormal growths on the thyroid gland
2) Acidic body fluids due to lung insufficiency
3) Allergic
4) Congestive heart failure
5) Cor pulmonale
6) Decreased urination

NOTE: Not commonly asked. Just remember it’s used to delay cataract progression.

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas


NAPHAZOLINE
1. Group and Mechanism of Action
a. Group - Anti allergic and vasoconstrictors (decongestant)
b. Mechanism of Action - A direct-acting sympathomimetic drug. Acts on alpha-adrenergic
receptors in the arterioles of the conjunctiva to produce vasoconstriction, resulting in decreased
conjunctival congestion.
2. Concentration, Dose & Duration
a. Concentration:
i. Eye Drops – 0.5%, 1%
c. Dose and Duration –
i. Naphazoline Hydrochloride- 0.012% - 1 to 2 drops in affected eye 1-2 times daily.
ii. Naphazoline/Pheniramine: 0.25% / 0.3% - 1 to 2 drops in affected eye 1-2 times daily.
3. Combination & Uses
a. Combination
i. With tropicamide (to produce mydriasis before ocular surgery)
b. Uses
 For refraction / retinoscopy / fundus examination – Not used as a cycloplegic but only for
mydriasis
 To produce mydriasis before ocular surgery
 To produce mydriais in patients with small central lenticular opacity
 For mydriatic provocation test in Primary Angle Closure Suspect
4. Side Effects
a. Ocular –
i. Mydriasis, irritation, discomfort, blurring, punctate keratitis, lacrimation, increased
intraocular pressure.
b. Systemic –
i. Dizziness, headache, nausea, sweating, nervousness, drowsiness, weakness, hypertension,
cardiac irregularities, and hyperglycemia.
5. Contraindications
a. Pregnancy/lactation
b. Glaucoma
c. Diabetes
d. Cardiovascular diseases (eg: HTN)

OCULAR PHARMACOLOGY SHORT NOTES – Inaam Niyas

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