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Ocular Pharmacology

The document outlines various ophthalmic medications organized into categories: 1. Anti-allergy medications including olopatadine 0.1% and naphazoline 0.1% 2. Anti-bacterial medications including chloramphenicol 0.5%, moxifloxacin 0.5%, and tobramycin 1% 3. Anti-glaucoma medications including brimonidine 0.2%, brinzolamide 1%, netarsudil 0.02%, timolol 0.25% and 0.5%, and travoprost 0.004% 4. Anti-inflammatory and immunosuppressant medications including corticosteroids

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Shahbaz AAnsari
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0% found this document useful (0 votes)
87 views20 pages

Ocular Pharmacology

The document outlines various ophthalmic medications organized into categories: 1. Anti-allergy medications including olopatadine 0.1% and naphazoline 0.1% 2. Anti-bacterial medications including chloramphenicol 0.5%, moxifloxacin 0.5%, and tobramycin 1% 3. Anti-glaucoma medications including brimonidine 0.2%, brinzolamide 1%, netarsudil 0.02%, timolol 0.25% and 0.5%, and travoprost 0.004% 4. Anti-inflammatory and immunosuppressant medications including corticosteroids

Uploaded by

Shahbaz AAnsari
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1.

Anti-Allergy Medications
i. Olopatadine 0.1%
ii. Naphazoline 0.1%

2. Anti-Bacterial Medications
i. Chloramphenicol 0.5%
ii. Moxifloxacin 0.5%
iii. Tobramycin 1%

3. Anti-Glaucoma Medications
i. Brimonidine 0.2%
ii. Brinzolamide 1% / Dorzolamide 2%
iii. Netarsudil 0.02%
iv. Timolol 0.25%, 0.5%
v. Travoprost 0.04%

4. Anti-Inflammatory and Immunosuppressant

a) Corticosteroids

i. Dexamethasone 0.1%, 0.5%, 0.5mg, 4 mg/mL


ii. Prednisolone 5mg, 10mg, 20mg/mL
iii. Hydrocortisone 0.2%, 0.5%
iv. Loteprednol 0.5%

b) NSAIDs

i. Bromfenac 0.09%
ii. Ketorolac 0.5%
iii. Nepafenac 0.1%
5. Cycloplegic & Mydriatic Drugs
a) Parasympatho-lytics
i. Homatropine 2%
ii. Tropicamide 0.5%, 1%
b) Sympatho-mimetics
i. Phenylephrine 5%, 10%

6. Lubricating and Viscoelastic Agents


i. Carboxy-Methyl-Cellulose (CMC) 0.5%
ii. Hypromellose (Hydroxy-Propyl-Methyl Cellulose – HPMC) 0.5%, 1%
iii. Sodium Hyaluronate / Hyaluronidase 0.1 to 0.3%, 1 to 1.4%, 2.3%

7. Local Anaesthesia
i. Bupivacaine 0.5%
ii. Lignocaine 2-4%
iii. Proparacaine 0.5%

1. Anti-Allergy Medications
i. Olopatadine 0.1%
MOA: H1 receptor antagonist (immediate action) + Mast cell stabilizer (long
term effect)
Indications: Allergic Conjunctivitis [Simple Allergic Conjunctivitis, Vernal
Keratoconjunctivitis, Acute Keratoconjunctivitis, Giant Papillary Conjunctivitis]
Dosage: 0.1% (w/v), 1-2 drops given twice daily in Vernal Keratoconjunctivitis
S/E: Burning or stinging of eye, dry eyes, Headache
C/I: Narrow Angle Glaucoma, Children < 3 Years Age, History of HSR

ii. Naphazoline 0.1%


MOA: Stimulate -agonists → Vasoconstriction → Relieves redness by causing
decongestion
Indications: Allergic conjunctivitis, common cold, sinusitis
Dosage: 0.1%, 1-2 drops upto 4 times a day
S/E: Ocular: Rebound congestion (after decongestion), Dryness, Blurred Vision,
Systemic: Aggravation of Hypertension, Headache, Nausea
C/I: History of allergy/ HSR, Narrow Angle Glaucoma, Severe hypertension,
Taking MAOIs or TCAs [Cheese Reaction → Hypertensive Crisis]

2. Anti-Bacterial Medications
Anti-Bacterial Medications
i. Chloramphenicol 0.5%
MOA: Broad-spectrum antibiotic, mainly bacteriostatic
In high concentration, bactericidal to H. influenzae, N. meningitidis, S.
pneumoniae
Binds reversibly to 50S ribosomal subunit → Prevents peptide bond
formation → Inhibits protein synthesis
Indications: In bacterial infections since it is broad spectrum antibiotic
having activity against Gram +ve, Gram -ve bacteria, Rickettsia, Chlamydia,
Mycoplasma
Dosage: Topically, as 0.5% Eye Drops, 1-2 drops every 4 to 6 hours.
Systemic use possible as it is lipid-soluble (resistance & toxicity limits use)
S/E: HSR, Bone Marrow Suppression, GI upset, “Gray Baby” syndrome
C/I: Bone Marrow Depression, Aplastic Anaemia, Liver Disease

ii. Moxifloxacin 0.5%


MOA: It is a 4th generation fluoro-quinolone (Gen 4 FQs) which acts by
inhibiting DNA synthesis.
Gram -ve Bacteria: Acts on Topoisomerase II (DNA Gyrase)
Gram +ve Bacteria: Acts on Topoisomerase IV
Spectrum: Highly effective against Aerobic Gram -ve (e.g., E.coli, Proteus)
More activity than Ciprofloxacin against Gram +ve like S. pneumonia, M.
tuberculosis and some anaerobes like Bacteroides fragilis.
Indications: Bacterial conjunctivitis, Corneal Ulcers
Dosage: 0.5% Eye Drops, every 1 to 4 hours (Topical)
400mg Tab Once Daily (Systemic)
S/E: GI upset; Headache, insomnia; HSR (skin rash, urticaria); ↑ QT interval
C/I: Pregnancy; young children (risk of cartilage damage)

iii. Tobramycin 1%
MOA: Belongs to Aminoglycoside group, Bactericidal by inhibiting protein
synthesis, primarily acts against Gram -ve Aerobes
Binds to 30S ribosomal subunit→ Stops Initiation of Protein Synthesis +
Causes misreading of Codon → Defective proteins formed and incorporated
→ Altered permeability, disruption of cell membrane → Bactericidal Effect
Indications: Bacterial conjunctivitis, Blepharitis, Corneal Ulcers, Ocular
infections
More activity against Pseudomonas aeruginosa, Proteus (as compared to
Gentamycin)
Dosage: 1% Eye Drops 1-2 drops every 4 to 6 hours.
S/E: Ototoxic, Nephrotoxic, Neuromuscular blockade, HSR
C/I: Pregnancy (ototoxic to fetus), Myasthenia Gravis patients, resistance to
any other amino-glycoside (share partial cross-resistance)

3. Anti-Glaucoma Medications
Anti-Glaucoma Medications
i. Brimonidine 0.2%
MOA: Selective -2 agonist. Lowers IOP by ↓ aqueous humour production
and ↑ uveo-scleral outflow. Has an additive effect with -blockers.
Peak action in 2 hours, t1/2 is 12 hours.
Indications: Various types of Glaucoma like Primary Open Angle Glaucoma
(2nd DOC), Phacolytic (Lens Protein) Glaucoma, Lens Particle Glaucoma,
Phaco-antigenic Glaucoma, Chronic Open Angle Inflammatory Glaucoma,
Pigmentary Glaucoma, Pseudo-exfoliative Glaucoma
Dosage: 0.2%, used twice daily
S/E: Ocular: Irritation, Allergy, Follicular Conjunctivitis, Ischemia
Systemic: Anxiety, Fatigue, Insomnia, Dry Mouth, Hypotension, Vaso-vagal
Attack
C/I: Primary Congenital Glaucoma

ii. Brinzolamide 1%, Dorzolamide 2%


MOA: Inhibit Carbonic Anhydrase enzyme → ↓HCO3- in ciliary epithelium →
↓Aqueous humour formation → ↓ IOP
Indications: Topically: 2nd Line Drugs, Adjunct Therapy in Primary Open Angle
Glaucoma; Ocular Hypertension
Dosage: Brinzolamide 1% BD (twice daily)
Dorzolamide 2% TDS (thrice daily) → Causes 22% ↓ in IOP, additive to Timolol
S/E: Paraesthesia, ↑ Urinary frequency (Diuresis), Serum Electrolyte
Imbalance, Gastro-intestinal symptom complex, Sulphonamide related
Adverse effects like Steven-Johnson Syndrome, Hypertensive nephropathy,
teratogenicity
C/I: COPD, Renal Disease, History of HSR

iii. Netarsudil 0.02%


MOA: -kinase inhibitor + some Neuroprotective role
Relaxation of cytoskeleton of Trabecular Meshwork + Schlemm’s Canal Cells
→ Reduced cell stiffness → ↓ in Episcleral Venous Pressure → ↑ in Trabecular
(Conventional) outflow → ↓ in IOP
Indications: POAG, Ocular Hypertension, Corneal Endothelial Dystrophies
like Fuch’s Endothelial Corneal Dystrophy
Dosage: 0.02% eye drops applied Once Daily (OD)
S/E: Eye Irritation, Blurred vision, Foreign Body Sensation, Lacrimation,
Conjunctival Hyperaemia, Corneal Erosion
C/I: Ocular Inflammation, Herpetic Keratitis, Liver Disease

iv. Timolol 0.25%, 0.5%


MOA: Non-selective -blocker
Blocks 2-receptors on ciliary epithelium → ↓ in Aqueous humour formation
→ ↓ in Ocular Blood Flow
Why preferred?
• Good synergistic action when combined with miotics (as in POAG)
• No local anaesthesia / partial agonist property
• No effect of pupil size / accommodation
• Long duration of action
• Well-tolerated
• Relatively cheap
Indications: Developmental Glaucoma
Primary Narrow and Open Angle Glaucoma
Secondary Glaucoma
DOC in Primary Open Angle Glaucoma, Secondary Glaucomas
Dosage: Timolol Maleate 0.25% or 0.5% eye drops OD or BD
Action starts in 30 min, peaks in 12 hours, lasts upto 24 hours.
S/E: Phenomenon of ‘Short-Term Escape’ and ‘Long-Term Drift’
Ocular: Superficial Punctate Keratitis, Corneal Anaesthesia
Systemic: Arrhythmia, Heart Failure; Bronchospasm; Depression, Anxiety
C/I: Bronchial Asthma, COPD, Chronic Heart Failure, Heart Blocks

v. Travoprost 0.004%
MOA: Synthetic PGF2 analogue
↑ in Uveoscleral Outflow → ↓ in IOP
Indications: DOC in POAG, also used in Acute Congestive Glaucoma
Why preferred?
• Long t1/2 (Once Daily dosing)
• High Efficacy
• Low systemic toxicity
Dosage: 0.004% Eye Drops given OD
S/E: Ocular: Iris pigmentation; Trichiasis, Distichiasis; Blurred Vision, Anterior
Uveitis
C/I: Active ocular inflammation, Corneal abrasion / erosion, Liver or Kidney
Disease

4. Anti-Inflammatory and Immunosuppressant


a) Corticosteroids
Anti-Inflammatory and Immunosuppressant
a) Corticosteroids
MOA:
Membrane Phospholipids → Action of Phospholipase A2 → Arachidonic Acid
→ Cyclo-oxygenase (COX) release PGs (Prostaglandin) + Lipo-oxygenase (LOX)
produces LTs (Leukotriene) → PGs and LTs are inflammatory mediators

Corticosteroids → Lipocortin → Phospholipase → ⨯Release of PGs, LTs


• ↓ Leukocytic & plasma exudation
• Cellular membrane integrity maintained, tissue swelling inhibited
• ⨯ Lysosome release from granules
• ↑ Stability of intra-cellular lysosomal membrane
• ↓ in number of circulating lymphocytes

Indications: Topical: Uveitis, Scleritis, Allergic Conjunctivitis (VKC, PKC),


Allergic Keratitis, Cystoid Macular Oedema (CME) , After Intra-ocular surgery
Systemic: Posterior Uveitis, Sympathetic Ophthalmia, Vogt-Koyanagi-Harada
(VKH), Papillitis, Retro-bulbar Neuritis, Anterior Ischaemic Optic Neuropathy
(AION), Scleritis, Malignant Exophthalmos, Corneal Graft Rejection
S/E: Topical: Glaucoma; Cataract; Activation of Infection like Herpes, Fungal,
Bacterial Keratitis; Dry Eye; Ptosis
Systemic: Hypertension, Aggravation of Diabetes Mellitus, Peptic Ulcer,
Osteoporosis, TB Re-activation, Cushingoid State
C/I: Glaucoma, Herpes Simplex Keratitis; Hypertension, Diabetes Mellitus,
Peptic Ulcer, Tuberculosis, Congestive Cardiac Failure, Renal Failure

i. Dexamethasone 0.1%, 0.5%, 0.5mg, 4 mg/mL


Dosage: Long-acting, highly potent anti-inflammatory drug
Topical: 0.1% solution, 0.5% Sodium Phosphate suspension
Systemic: 0.5 mg Tab, Injection solution in strength 4 mg/mL

ii. Prednisolone 5mg / 10 mg, 20 mg/mL


Dosage: Short-acting, moderate potency anti-inflammatory drug
Systemic: 5 mg / 10 mg Tab, Injection solution in strength 20 mg/mL

iii. Hydrocortisone / Cortisol 0.2%, 0.5%


Dosage: Short-acting, less potent anti-inflammatory drug
Topical: 0.5% suspension acetate and 0.2% ointment

iv. Loteprednol 0.5%


Dosage: Short-acting, least potent anti-inflammatory drug
Topical: 0.5% suspension

Relative Anti-inflammatory Potency (assuming Cortisol as standard):


Dexamethasone (25) > Prednisolone (4) > Hydrocortisone / Cortisol (1) >
Loteprednol (<1)
b) NSAIDs
b) NSAIDs
MOA:
Membrane Phospholipids → Action of Phospholipase A2 → Arachidonic Acid
→ Cyclo-oxygenase (COX-1 & COX-2) release PGs (Prostaglandin) + Lipo-
oxygenase (LOX) produces LTs (Leukotriene) → PGs and LTs are
inflammatory mediators
NSAIDs → Irreversibly non-selective COX inhibition → ↓ Inflammation
Indications: Prevention of intra-operative Miosis during cataract surgery,
Pain relief following cataract surgery, Prevention of Post cataract surgery
Cystoid Macular Oedema (CME); Episcleritis & Scleritis; Uveitis (not 1st choice)
S/E: Blurred vision, Eye irritation / discomfort, ↑ IOP, Corneal Ulcer (Rare)
C/I: History of Bleeding disorders / Anti-coagulant use, Asthma, HSR like
urticaria, skin rash
i. Bromfenac 0.09%
Dosage: 0.09% solution given as 1 drop in affected eye BD (twice daily);
Started 1 day after cataract surgery and continued till 2 weeks after
ii. Ketorolac 0.5%
Dosage: Very potent analgesic, Efficacy comparable to morphine but
does not cause respiratory depression, hypotension or drug dependence
0.5% solution given 1-2 drops every 6 to 8 hours in affected eye
iii. Nepafenac 0.1%
Dosage: 0.1% solution given as 1 drop in affected eye TDS (thrice daily);
Started 1 day before cataract surgery and continued till 2 weeks after.

5. Cycloplegic & Mydriatic Drugs


Cycloplegic & Mydriatic Drugs
a) Parasympatho-lytics
MOA: Has both Cycloplegic and Mydriatic activity
Blockade of M3 muscarinic receptors:
i) Paralysis of Constrictor Pupillae → Passive Mydriasis
ii) Paralysis of Ciliary Muscles → Loss of Accommodation → Cycloplegia
S/E: Photophobia, Blurring of vision, Loss of accommodation
C/I: Adults with Shallow AC [Ciliary muscles relaxed → Occlude Canal of
Schlemm → Flow of Aqueous humour obstructed → ↑ IOP → Precipitation of
Acute Congestive Glaucoma]

i. Homatropine 2%
Indications: Wet retinoscopy in hypermetropic individuals between 5 and 25
years of age; Acute Anterior Uveitis, Keratitis; Accommodative Spasm;
Penalisation in Amblyopia
Dosage: 2% as eye drops given 1 drop every 10 min for 6 times.
Peak Effect: 60-90 min
Microscopy: 90 min after instillation of 1st Drop
Duration of Action: 48-72 hours
Period of Post-cycloplegic Test: After 3 days of retinoscopy
Tonus Allowance: 0.5 D

ii. Tropicamide 0.5%, 1%


Indications: Used only as mydriatic in retinoscopy; Fundoscopy
Dosage: 0.5%, 1% as eye drops given 1 drop every 15 min for 3-4 times.
Peak Effect: 20-40 min
Microscopy: 60 min after instillation of 1st Drop
Duration of Action: 4-6 hours
Period of Post-cycloplegic Test: After 1 day of retinoscopy
Tonus Allowance: 0.5 D

b) Sympatho-mimetics
i. Phenylephrine 5%, 10%
[Do not confuse Phenyl-ephrine, a selective 1-agonist used as mydriatic with
Phenyl-epinephrine (Dipivefrine), a non-selective adrenergic agonist and a
prodrug of epinephrine previously use in treatment of Glaucoma]
MOA: Sympathomimetic agent; only Mydriatic action, not cycloplegic
1-agonist → Contraction of the radial muscle fibres of Iris→ Active mydriasis
Difference from Parasympatho-lytics:
• No cycloplegia
• No loss of light reflex
• ↓ IOP due to ↓ aqueous humour formation
Indications: Wet retinoscopy in Elderly (Narrow pupil, Hazy Media);
Fundoscopy
Dosage: 5%, 10% as eye drops given 1 drop every 15 min for 3-4 times
[Alone or in Combination with Tropicamide 0.5%, 1%]
Peak Effect: 30-40 min
Microscopy: 60 min after instillation of 1st Drop
Duration of Action: 4-6 hours
Period of Post-cycloplegic Test: After 1 day of retinoscopy
Tonus Allowance: Nil
S/E: Eye Irritation, Redness; Headache; Tachyphylaxis (↑HR), ↑BP
C/I: Patient on MAO-Inhibitor [‘Cheese Reaction’ → Hypertensive Crisis]
6. Lubricating and Viscoelastic Agents
Lubricating and Viscoelastic Agents
i. Carboxy-Methyl-Cellulose (CMC) 0.5%
MOA: Contains:
• Inorganic Electrolytes (maintains ocular tonicity)
• Buffer (to adjust pH)
• Preservative (maintains solution sterility)
• Viscosity agent (Water Soluble Polymer System) – Cellulose Ester as in
Carboxy-Methyl-Cellulose (CMC)
Indications: Artificial Tear in Dry Eye; Corneal Surface irregularity; During
cataract surgery / cornea transplantation, used to protect cornea from
damage by creating a barrier; Lubricant solution for contact lens; viscous
Controlled Drug Delivery (prolongs contact time between drug & eye)
Dosage: 0.5% Eye drops; 1-2 drops given 4-6 times a day
S/E: Blurred Vision, Redness, Itching, Photophobia
C/I: Eye infection (Ulcerative, Herpes Simplex Keratitis, Fungal Infection);
Any previous HSR

ii. Hypromellose (Hydroxy-Propyl-Methyl Cellulose – HPMC) 0.5%, 1%


MOA: Contains:
• Inorganic Electrolytes (maintains ocular tonicity)
• Buffer (to adjust pH)
• Preservative (maintains solution sterility)
• Viscosity agent (Water Soluble Polymer System) – Cellulose Ester as in
Hydroxy-Propyl-Methyl-Cellulose (HPMC)
Indications: Artificial Tear in Dry Eye; Corneal Abrasion, Erosion, Dystrophies;
Controlled Drug Delivery (prolongs contact time between drug & eye); Visco-
dispersive agent during surgery (Endothelium protection > Prevention of
Anterior Chamber Collapse); Diagnostic Tests like Schirmer’s Test, TBUT
(Tear-film Break Up Time)
Dosage: Lubricant for Dry Eye or Contact Lens – 0.2 to 0.5%
Drug delivery vehicle in Glaucoma – 0.2 to 2%
Surgery – 1.4 to 3% (as Visco-elastic agent)
S/E: Blurred vision; Eye irritation, burning, stinging; Redness, itching
C/I: Eye infection; Previous HSR

iii. Sodium Hyaluronate / Hyaluronidase 0.1 to 0.3%, 1 to 1.4%, 2.3%


MOA: Contains:
• Inorganic Electrolytes (maintains ocular tonicity)
• Buffer (to adjust pH)
• Preservative (maintains solution sterility)
• Viscosity agent (Water Soluble Polymer System) – Increased viscosity
agent / Longer t1/2 Mucoadhesive as in Hyaluronidase
Indications: Dry Eye; Corneal Ulcer; Conjunctivitis; Cataract Surgery,
Refractive Surgery, Glaucoma Surgery, Corneal transplant Surgery
Dosage: 0.1% to 0.3%: Dry Eye, Corneal Ulcer, Contact Lens
1% to 1.4%: Visco-cohesive agent in surgery (Maintains Anterior Chamber
better by pushing Iris, Lens Diaphragm posteriorly)
2.3%: Visco-adaptive agent in surgery (Strikes a balance between
Endothelium and Anterior Chamber protection)
S/E: Photophobia, Eye Pain, Blurred Vision, Itching, Headache
C/I: Corneal oedema or decompensation, Infection in Eye

7. Local Anaesthesia

Local Anaesthesia
MOA: -caine: Amide group of local anaesthetics (LA)

Blocks sodium entry in Voltage-gated Na+ channels → ⨯Nerve impulse


generation, conduction
Bupivacaine also ⨯ NMDA-mediated synaptic transmission
i. Bupivacaine 0.5%
Indications: LA in cataract extraction, corneal transplantation,
trabeculectomy (glaucoma surgery); Pain relief following surgery, ocular
trauma; Chronic ocular pain (corneal neuropathy, uveitis); Strabismus
correction (by temporary paralysis of eye muscles)
Dosage: 0.5% to 0.75% in Sub-Conjunctiva / Peribulbar Space for Cataract
Extraction, Corneal Transplantation, Trabeculectomy
0.5% in Sub-conjunctiva / Sub-Tenon’s space in Ocular Pain
S/E: Dizziness, Headache, Nausea; Cardiotoxicity (Heart Block, Arrhythmia,
Cardiac Arrest); Respiratory Depression
C/I: 2°/3° Heart Block, IV Injection (too much cardiotoxic)

ii. Lignocaine 2-4%


Indications with Dosage: Corneal Anaesthesia (2% Topical drops / ointment);
Minor procedures like suturing (2% Injection in Sub-Conjunctiva); as LA
during Cataract Surgery (1% Injection Intra-cameral); Intro-ocular surgery (2%
Injection in Retro-bulbar space ← Sparingly used because of haemorrhage,
globe perforation, injury to optic nerve and muscles)
S/E: Injection site pain, Heart palpitations / arrythmias, Seizures / Convulsions
C/I: Complete Heart Block / Bradycardia; Shock / Hypovolemia, Severe Liver
Disease

iii. Proparacaine 0.5%


Indications: Topical Anaesthesia in Tonometry, Foreign Body removal;
Diagnostic Procedures like Gonioscopy, Fundoscopy (↓ Discomfort, ↑ Co-
operation); Corneal Abrasion Treatment; Ocular Trauma management; ↓Pain
during Intra-cameral Inj. (as in Macular degeneration, diabetic retinopathy)
Dosage: 0.5% to 0.75% solution as 1 to 2 drops, Injected into conjunctival sac
Action starts within 30 seconds, Effect lasts for 10 to 20 min
S/E: Photophobia; Blurred Vision; Itching; Corneal Clouding & Opacity (rare)
C/I: Premature infants; severe liver or kidney disease; History of Allergy

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