This slide has been made for medical students to know about elementary ophthalmic drugs commonly used in ophthalmic practise and asked in vivas.

1. Ocular
Therapeutics
Bipin Bista
Resident
Ophthalmology

2. Routes of administration
• Instillation into the conjunctival sac
• Subconjunctival injection
• Peribulbar injection
• Systemic administration
• Direct injection into the globe – Intracameral /
Intravitreal.

3. Topical Instillation
• Drops, ointmens, ocuserts, gels, soft contact lenses.
• Epithelium permeable to lipid soluble substance, stroma
to water soluble.
• Considerable resistance to the electrolyte flow.

4. General points
• Fat solubility
• MW below 500
• Degree of dissociation of electrolytes
• Duration of contact of drug with corneal epithelium

5. Subconjunctival Injections
• Allows free and indiscriminate transit of molecules of
considerable size.
• Useful when high dosage is required.

6. Peribulbar/Subtenon
Injection
• Short, curved needle with its bevel towards the globe is
passed through a conjunctival incision .

7. Intraocular injections
• Anterior chamber-
Intracameral
• Vitreous- Intravitreal
• To flood the ocular
tissues with antibiotics.
• Half-life in anterior
chamber is less than that
vitreous.

9. Systemic Administration
• Inflammations involving the posterior retina, optic nerve
or orbit.
• If disease spreads outside the eye.
• Orally or injections
• Barrier – blood aqueous barrier
• Large sized molecules
• Lipid solubility.

10. ANTIBIOTICS
• Many bacteriostatic , some bacteriocidal.
• Derived from fungi, bacteria or synthetic.
• Bacteriostatic : erythromycin, trimethoprim,
sulphacetamide.
• Bactericidal : penicillins, aminoglycosides,
fluoroquinolones and cephalosporins.

11. ANTIBIOTICS
Gram positive effectives Effective against both
• Penicillin G,
erythromycin, oxacillin,
vancomycin.
• Gram negative effectives
: neomycin , polymyxin B,
streptomycin.
• Gentamicin, amikacin,
ampicillin, cephalosporin,
tobramycin,
chloramphenicol,
tetracycline,
fluoroquinolones.

12. PENICILLINS
• Bactericidal
• Short half-life
• Excreted mainly by kidney, small fraction by biliary tract.
• Acts by interfering with cell wall synthesis.
• Better to be given parenterally, as these drugs get
destroyed by gastric juice.
• Look for hypersensitivity.

13. Penicillins- Groups
1. Effective against coccal and gm +ve bacilli : Penicillin V
& sodium oxacillin.
2. Penicillinase-resistant penicillins : Cloxacillin and
flucloxacillin
3. Broad spectrum penicillins : ampicillin and amoxycillin.
AMPICILLIN : 0.25 – 2 G ORAL/IM/IV, 25-50 MG/KG/DAY
for Paediatrics.

14. Cephalosporins
• Bactericidal.
• Intraocular penetration : Not Much Good.
• Nephrotoxic.
• Has better gram negative coverage.
1. First generation : cephazolin , cephalexin.
2. Second generation : cefuroxime, cefaclor.
3. Third generation : ceftazidime, cefotaxime

15. Aminoglycosides
• Streptomycin. Soframycin, tobramycin, sisomycin,
amikacin, Neomycin.
• Gram negative organisms and gram positive
staphylococci.
• Due to increasing resistance to Pseudomonas for
Gentamycin , amikacin has been recommended for
intraocular infections.
• Gentamycin – 1-1.5 mg/kg IM 8 hourly, Topically : 0.3%,
Tobra – 0.1%

16. Tetracyclines
• Smaller ability to penetrate ocular tissue.
• Most commonly used in Trachoma.
• Acne rosaecae and chronic stap. Infections.
• Doxycycline and Minocycline has better aqueous
concentrations.

17. Macrolide & Lincomycin
• Erythromycin, azithromycin, lincomycin and clindamycin.
• Azithromycin : Long-acting, 20-30 mg/kg in treatment of
Trachoma, Toxoplasmosis and Lyme disease.

18. Glycopeptides
• Vancomycin – all gm + as well as methicillin resistant
Stapylococcus aureus and Staphylococcal epidermidis.

19. Fluoroquinolones
• Bactericidal
• Derivative of nalidixic acid.
• Ciprofloxacin, ofloxacin, norfloxacin, lomefloxacin,
gatifloxacin, levofloxacin and moxifloxacin.
• Moxifloxacin achieves higher intraocular concentrations
than gatifloxacin.
• Cipro, Nor, Oflo, Lomeflo, Perflo,Gati – 0.3% 1 to 4 hrly,
• Moxifloxacin – 0.5%

20. Chloramphenicol
• Bacteriostatic
• Small molecule and lipid soluble.
• Least toxic to corneal epithelium.
• Blood dyscracias
• Gray baby syndrome.

21. Antiviral agents
• Usually pyrimidine and purine derivatives.
• Herpes simplex : Idoxuridine, Vidarabine, Trifluridine,
Acyclovir, Famiciclovir.
• Herpes zoster : Acyclovir, famiciclovir,
valaciclovir,vidarabine, sorvudine.
• CMV retinitis : Ganciclovir, Foscarnet, Zidovudine.
• Non selective : Interferons, Immunoglobulin.

22. Pyrimidine Derivatives
• Inhibits viral metabolism by substituting for thymidine in
DNA synthesis and prevents replication of virus.
• Side-effects : Follicular conjunctivitis, lacrimal punctal
stenosis and irritation with photophobia.
• Inhibits corneal stromal healing --- Never use in Post-op
keratoplasty.
• Trifluorothymidine (TF3 )- 1 % eyedrops
• IDU – 0.5 % OINT, 0.1% drops

23. Purine Derivatives
• Adenine Arabinoside
• Acyclovir
• Ganciclovir

24. Adenine Arabinoside
• Purine nucleoside
• More potent than IDU & less toxic as well.
• MOA : Metabolised to triphosphate form which inhibit
DNA polymerase, thus arrests viral DNA growth.
• 3% opht oint.

25. Acyclovir
(Acycloguanosine)
• Safest and effective agent.
• Inhibits viral DNA , preferentially entering the infected
cells.
• Uses : After penetrating keratoplasty suffering with HSV
keratitis, uveal disease, herpes zoster. 200 mg four
tablets ,5 times a day.
• 3% ophth oint five times a day,

26. Ganciclovir
• CMV RETINITIS
• 5 mg/kg bd for 2-3 weeks.

27. Anti Fungal Agents
• Polyene antifungals
• Imidazoles
• Pyridines
• Silver compounds

28. Polyene
• Mainstay
• Work by binding to the sterol groups in fungal cell
membranes .
• Nystatin – 3.5%
• Natamycin
• Amphoterecin B 0.3 %, IV-0.1mg/ml in 5% dextrose.

29. Imidazoles
• MOA : complex, change in fungal cell membranes by
blocking the production of ergosterol.
• Miconazole, Clotrimazole, Econazole, Ketoconazole,
Fluconazole, Itraconazole.
• Topical – 1 % oint,200-400 mg OD
• Fluconazole - 0.2% drops, 50-100 mg

30. ANTI INFLAMMATORY
• Corticosteroids
• Nonsteroidal Anti-Inflammatory Drugs
• Immunosuppressive & Antimitotics

31. Corticosteroids
• Compounds secreted by adrenal gland.
• Reduces inflammation by reduction of leukocytic &
plasma exudation, maintenance of cellular membrane
integrity with inhibition of tissue swelling, inhibition of
lysosome release from granulocyte, increased
stabilisation of intracellular lysosomal membranes
and suppression of circulating lymphocytes.

32. Drugs
Glucocorticoids Mineralocorticoids
• Short-acting :
Hydrocortisone (0.5 %
suspension,1.5% oint),
cortisone, prednisolone 1%,
Methylprednisolone.(0.2%
oint)
• Intermediate :
Triamcinolone,
Fluprednislone
• Long acting :
Dexamethasone,
Betamethasone
• Fludrocortisone

33. Indications
Topical Systemic
• Uveitis
• Scleritis
• Allergic conjunctivitis
• Cystoid macular oedema
• After surgeries
• Posterior uveitis
• Vogt-Koyanagi-Harada
syndrome
• Papillitis
• Retrobulbar neuritis
• Anterior ischaemic optic
neuropathy
• Malignant exophthalmos
• Orbital pseudotumors
• Corneal graft rejections.

34. Side-effects
Topical steroids Systemic
• Glaucoma
• Cataract
• Activation of infection
• Dry eye
• Ptosis
• Papilloedema
• CRVO
• Peptic ulcer
• Htn
• Osteoporosis
• DM
• Cushingoid state
• Reactivation of infections.

35. NSAIDs
• Heterogenous group of anti-
inflammatory, analgesic and
anti-pyretic compounds.
• MOA : Act by irreversibly
blocking the enzyme cyclo-
oxygenase, thus inhibiting
the prostaglandin
biosynthesis. Block other
local mediators of
inflammatory response :
polypeptides of Kinin
system, Lysosomal enzyme,
TXA2 .

36. Uses
• Episcleritis
• Scleritis
• Uveitis
• CME
• Maintaining dilation prior to surgeries.

37. Drugs
Systemic Topical Ophthalmic
• Salicylates : Aspirin
• Pyrazolone : Phenylbutazone,
aminopyrine.
• Para-aminophenol :
acetaminophen
• Indole : Indomethacin
• Priopionic acid : Ibuprofen,
naproxen, flurbiprofen
• Anthranilic acid : mefenamic
acid
• Newer : Diclofenac, ketorolac
• Indomethacin 0.1%
• Flurbiprofen- 0.3%
• Ketorolac tromethamine
0.5%
• Diclofenac sodium0.1%
• Nepafenac 0.1%
• Bromefenac 0.09%

38. Immunosuppressive &
Anti-mitotic
• Agents used to control immune-mediated inflammation or tissue
reaction.
• Uses and indications in Ophthalmology
― VKH syndrome
― Sympathetic Ophthalmia
― Behcet’s syndrome
― Serpiginous choroidopathy
― Corneal graft
― Mooren’s ulcer
― Recurrent pterygium
― Scleritis
― Grave’s Ophthalmolgy
― Ocular Myasthenia gravis

39. Drugs
• Immunomodulators : Cyclosporine, tacrolimus.
Mechanism of action : Binds to cytoplasmic receptors
termed immunophilines in T-cells, thereby selectively
inhibiting T-cell activity.
• Cytotoxic Drugs :
1. Antimetabolites : azathioprine, methotrexate
2. Alkylating agents : Cyclophosphamide

40. Antimetabolites
• MOA : Inhibits purine synthesis, which interfere with
DNA replication and RNA transcription
• Side-effects : Gastrointestinal intolerance and bone
marrow suppressions .

41. Alkylating Agents
• Cyclophosphamide :
Destroys proliferating
lymphoid cells but also
alkylate DNA.
• Side-effects : cardiac
toxicity, electrolyte
imbalance, pancytopenia
and hemorrhagic cystitis.

42. ANTI ALLERGIC AND
VASOCONSTRICTORS
• H1 receptors antagonists : Levocabastine.
• Mast cell stabilizers : Cromolyn sodium, lodoxamide,
nedocromil.
• Antihistamines with mast cell stabilizing activity : Olapatadine,
ketotifen.
• Topical NSAIDs : Flurbiprofen, ketorolac, bromfenac.
• Vasoconstrictors : Naphazoline/Pheniramine,
Naphazoline/Antazoline.
• Weak corticosteroids : Loteprednol, fluorometholone
• Oral antihistaminics : Loratidine, cetrizine, ebastine.
• Immunomodulators : Tacrolimus and cyclosporine.

43. Lubricating agents
• Cellulose esters : Methylcellulose, carboxymethyl
cellulose
• Polyvinyl alcohol : Polyvinyl alcohol
• Increased viscosity agents : Polycarbophil, dextran
• White patroleum and lanolin : Lacrilube, lacrigel

44. Intraocular Irrigating
Solutions
• Cataract surgery
• Glaucoma surgery
• Corneal surgery & anterior segment
• Vitrectomy and posterior segment surgery.

45. • Ringers solution : Sodium chloride, Potassium chloride,
calcium chloride and sodium lactate.
• pH : 7.2
• Balanced salt solution

46. Viscoelastic Substances
• Methylcellulose
• Sodium hyaluronate
• Hypromellose
• Chondroitin sulfate

47. Uses : Visco
• Cataract surgery with or without IOL implantation
 Maintenance of anterior chamber
 Protection of corneal endothelium
 Coating the IOL
 Preventing the entry of blood and fluid in the anterior
chamber.
 Retinal detachment
 Globe repair.

48. Anti-VEGF
• RANIBIZUMAB : binds to all isoforms of VEGF-A and
inhibits their biological activity.
• PPEGAPTANIB
• BAVACIZUMAB

49. Uses of anti-VEGF
• Neovascular age related macular degeneration
• Diabetic retinopathy
• Retinal vein occlusion
• Neovascular glaucoma
• Myopic CNV
• Inflammatory CNV
• Choroidal osteoma

50. Complications
• Intravitreal injections : cataract, glaucoma, vitreous
hemorrhage, endophthalmitis, retinal detachment.

51. DYES
• Fluorescein sodium
• Fluorexone
• Indocyanine green
• Rose Bengal
• Lissamine green
• Trypan Blue
• Verteporfin
• Methylene blue

52. Anti-Glaucoma Drugs
 Parasympathomimetic drugs (Miotics)
 Sympathomimetic drugs (Adrenergic agonists)
 Betablockers
 Carbonic anhydrase inhibitors
 Hyperosmotic agents
 Prostaglandins
 Calcium channel blockers

53. Parasympathomimetics
(MIOTICS)
• Direct-acting : Pilocarpine
• Indirect-acting parasympathomimetics : Physostigmine,
ectothiophate.
• Dual-acting :Carbachol
• Imitate or potentiate : acetylcholine

54. Mechanism of action
• In primary open angle glaucoma : enhance the aqueous
outflow facility.
• Achieved by changes in the Trabecular Meshwork
produced by a pull exerted on the scleral spur.
• In Primary Closed angle Glaucoma : reduce the IOP by
opening the angle. Mechanical contraction of the pupil
moves the iris away from the trabecular meshwork.

55. Side-effects
SYSTEMIC LOCAL
• Bradycardia
• Increased sweating
• Diarrhoea
• Excess salivation
• Anxiety
• Scoline apnea
• Reduced acquity
• Impairment of vision
• Contraction of visual field
• Spasm of accomodation

56. Pilocarpine
• Direct acting
sympathomimetics
• Indications : AACG,
CACG, CSACG.
• Containdications :
Inflammatory glaucoma,
malignant glaucoma and
known allergy.

57. SYMPATHOMIMETICS
• Also known as Adrenergic agonists .
• Classified as :
~ Both alpha & beta stimulators: Epinephrine.
~ Direct alpha adrenergic stimulators : Norepinephrine,
clonidine hydrochloride.
~ Indirect alpha adrenergic stimulators : Pargyline
~ Beta adrenergic stimulator : Isoproterenol.

58. MOA :
Sympathomimetics
• Increased outflow by alpha and beta stimulation.
• Decreased aqueous humour production d/t stimulation of
alpha receptors in the ciliary body.

59. Side-effects
SYMPATHOMIMETICS
Systemic Local
• Hypertension
• Headache
• Palpitation
• Tremors
• Nervousness
• Anxiety
• Burning sensation
• Reactive hyperamia
• Mydriasis
• Allergic
blepharoconjunctivitis
• Cystoid macular oedema

60. Epinephrine
• Direct acting sympathomimetics stimulates both
receptors.
• Indication : POAG, Secondary Glaucoma.

61. Brimonidine
• Selective alpha 2 adrenergic agonist and lowers IOP by
decreasing aqueous production and enhancing
uveoscleral outflow.
• Addictive effect with beta-blockers.

62. BETA BLOCKERS
• MOA : lowers IOP by blockade of beta-2 receptors in the
ciliary processes.
• Drugs : timolol, betaxolol, levobunolol, carteolol,
metipranolol.

63. Timolol
• Nonselective beta 1 & beta 2
receptor blocking agent.
• Useful in almost all glaucomas,
unless if there isnt any
systemic disease.
• Contraindication : Bronchial
asthma, emphysema, COPD,
heart blocks, congestive heart
failure or cardiomyopathy.
• Betaxolol – patients with
pulmunary disease.

64. Side-effects -Beta-blockers
Local Systemic
• Burning sensation
• Hyperaemia
• SPK
• Corneal anaesthesia
• CVS : bradycardia,
arrhythmia, heart failure
and syncope.
• Respiratory :
bronchospasm, airway
obstruction.
• CNS : depression,
anxiety, confusion,
drowsiness,
disorientation,dysarthria

65. CARBONIC ANHYDRASE
INHIBITOR (CAIs)
• Inhibit enzyme carbonic
anhydrase which reduces
the IOP by reducing
aqueous humor
formation.
• Drugs : Acetazolamide,
dorzolamide,
methazolamide,
dichlorphenamide,
Brinzolamide.

66. Side-effects
• Paresthesias
• Urinary frequencies
• Serum electrolyte imbalance
• GI symptom complex
• Sulfonamide like reactions.

67. Serum electrolyte
imbalances
• Occurs at higher doses.
1. Bicarbonate depletion : metabolic acidosis, ‘Malaise
symptom complex’ : malaise, fatigue, depression, loss
of libido, anorexia and weight loss.
2. Potassium depletion : occur with pts under
steroids,aspirin, thiazides.
3. Sodium and chloride loss.

68. Hyperosmotic agents
• Glycerol, mannitol, isosorbide and urea.
• MOA : Increase the plasma tonicity. This osmotic
gradient between blood and vitreous draws sufficient
amount of water.

69. Prostaglandin analogues
• Drugs : Latanoprost,
Bimatoprost, Travoprost.
• MOA : Ester analogue of
Prostaglandin f-2 , Increasing
uveoscleral outflow and by
causing reduction in episcleral
venous pressure
• Dose : OD, DOA : 24 hours.
• Side effects : Hyperaemia, FB
sensation, increased
pigmentation.

70. Calcium Channel Blockers
• Drugs : Nifedipine, Diltiazem, Verapamil.
• MOA : Effects on secretory ciliary epithelium.
• Given in cases where Miotics, Beta-blockers cant be
given.