This ppt explains in short about the drugs used in corneal ulcer.

1. PHARMACOTHERAPY
OF CORNEAL ULCER
Presented by-
Dr. Rajesh A Kamtane,
3rd year PG,
Dept. of Pharmacology,
MIMS

2. Ulcerative Keratitis (corneal ulcer) is seen in-
A.Infective Keratitis---Bacterial, Viral or Mycotic
corneal ulcer
B.Protozoal Keratitis---Acanthamoeba Keratitis
C.Allergic Keratitis---Phylectenular, Vernal or
Atopic Keratitis
D.Peripheral Ulcerative Keratitis---associated with
connective tissue disorders, Mooren’s Ulcer or
Rosacea Keratitis

3. E. Trophic Corneal Ulcers---Neurotrophic or
Exposure Keratopathy

4. Bacterial Corneal Ulcer
Common bacteria associated with corneal ulceration are-
--Staphylococcus aureus, Streptococcus
pneumoniae, E.coli, Proteus, Klebsiella, Pseudomonas,
N. gonorrhoea, N. meningitidis, C. diptheriae
Specific treatment-
Topical antibiotics-
Initial therapy (before C & S reports are available)
should be combination therapy to cover both gram
positive and negative organisms.

5. Any of the following 2 drugs can be instilled---
Fortified cefazolin + fortified tobramycin
or
Fortified vancomycin + one of the commercially
available fluoroquinolone eye drops (0.3 % cipro/
oflox/ gati or 0.5% moxi)

6. Frequency of instillation-
The chosen two drugs should be instilled alternately as
below—
1 hourly round the clock for first 48 hours.
2 hourly during day and 4 hourly at night till healing is
ensured.
4 hourly till healing occurs.
Once favorable response is obtained, fortified drops can
be substituted by commercially available eye drops.

7. Subsequent therapy-
No need to change initial antibiotics if response is good.
If response is poor, immediately change the antibiotics
as per C & S reports.
Systemic antibiotics-
Usually not required.
However, a cephalosporin or an aminoglycoside or oral
ciprofloxacin (750 mg BD) may be given in fulminating
cases with perforation or when sclera is also involved.

8. Non-Specific treatment:
Cycloplegic drugs.
Topical/ Systemic NSAIDs to relive pain and edema.
Vitamins (A, B- complex & C) help in early healing of
ulcer.

9. Non-Specific treatment…..
Secondary glaucoma can occur due to fibrinous exudates
blocking the angle of anterior chamber. Anti-glaucoma
drugs can be given to lower IOP (details in further slides).
Topical steroids in selected cases. E.g. marginal catarrhal
ulcer which is caused by hypersensitivity reaction to
Staphylococcal toxins (details in further slides).

10. Mycotic Corneal Ulcer
In recent years its incidence is increased due to injudicious use
of antibiotics and steroids.
Specific treatment
Topical antifungals:
Natamycin (5%), Amphotericin B and either Fluconazole
(0.2%) or miconazole or voriconazole (10% )eye drops to be
instilled one hourly round the clock, then taper slowly over 6-
8 weeks. These are effective against Aspergillus and Fusarium.
Nystatin (3.5%) eye ointment, five times a day is effective
against Candida.

11. Systemic antifungal drugs may be required for severe
cases of fungal keratitis. Tablet fluconazole or
ketoconazole may be given for 2-3 weeks.
Non-specific treatment-
NSAIDs’, cycloplegics, vitamins

12. Viral Corneal Ulcer
Herpes Simplex Keratitis
Specific treatment:
Antiviral drugs are first choice presently.
Usually after 4 days of therapy, lesion starts healing
which is completed by 10 days. After healing, taper
the drug and withdraw in 5 days.
If after 7 days of initial therapy, there is no response,
it means that virus is resistant to this drug. Hence
change the drug and / or do mechanical debridement.

13. Commonly used antiviral drugs are as follows-
Acyclovir –
1. 3% ointment, 5 times a day until ulcer heals
and then 3 times a day for 5 days.
2. It is least toxic and most commonly used
antiviral drug.
Ganciclovir -
1. 0.15% gel, 5 times a day until ulcer heals
and then 3 times a day for 5 days.
2. It is more toxic than acyclovir.

14. Triflurothymidine
1% drops, 2 hourly until ulcer heals and then 4 times a
day for 5 days.
Vidarabine
3% ointment, 5 times a day until ulcer heals and then
3 times a day for 5 days.

15. Systemic antiviral drugs for a period of 10 to 21 days
are used in recurrent and acute cases.
Tb. Acyclovir 400 mg BD/ TID
Tb. Famcyclovir 250 mg BD
Tb. Valacyclovir 500 mg BD
Non specific treatment-
Same as earlier.

16. Herpes Zoster Opthalmicus
Systemic therapy for Herpes Zoster
Oral antiviral drugs-
Tb. Acyclovir 800 mg 5 times a day for 10 days or
Tb. Valacyclovir 500 mg TID
Analgesics-
Pain during first 2 weeks of an attack is very severe and
should be treated by combination of mephenamic acid and
paracetamol or pentazocin or even pethidine (when very
severe).

17. Systemic Steroids-
They inhibit development of post herpetic neuralgia when
given in high doses. However, the risk of high doses of
steroids in elders should be considered.
They are commonly recommended in cases developing
neurological complications such as third nerve palsy and
optic neuritis.
Cimetidine 300 mg QID for 2-3 weeks reduces pain and
pruritis in acute zoster, by histamine blockade.
Amitriptyline to relieve depression in acute phase.

18. Local therapy for Herpes Zoster
1. For skin lesions-
Antibiotic- steroid ointment or lotions-- three times a day till
skin lesions heal.
2. For zoster keratitis-
• Topical steroid eye drops 4 times a day.
• Cycloplegics such as cyclopentolate eye drops or atropine
eye ointment OD.
• Topical acyclovir 3% eye ointment, 5 times a day for 2
weeks.

19. 3. For secondary infections-
Topical antibiotics
4. For secondary glaucoma-
0.5% timolol or betaxolol eye drops BD and Tb. Acetazolamide
250 mg QID.
5. For mucous plaques-
Topical mucolytics like acetyl cysteine 5 to 10%, TID.
6. For persistent epithelial defects-
Lubricating artificial tear drops.

20. Protozoal Keratitis
Acanthamoeba keratitis
Specific treatment:
Topical antiamoebic agents include-
Diamidines: propamidine isethionate
(0.1%), hexamidine (0.1%)
Biguanides: polyhexamethylene biguanide
(0.02%), chlorhexidine (0.02%)
Aminoglycosides: neomycin, paromycin
Imidazoles: clotrimazole and miconazole

21. Multiple drug therapy is required for 3-4 months for
early epithelial lesions and 6-12 months for stromal
lesions.

22. Allergic Keratitis
Local therapy
1. Vasoconstrictors like adrenaline, ephedrine and
naphazoline.
2. Topical steroids—
Their use should be minimized as much as possible,
because they frequently cause steroid induced glaucoma.
Commonly used steroids are fluorometholone, medrysone,
betamethasone or dexamethasone. First two are safest of
all these.

23. 3. Mast cell stabilizers such as sodium chromoglycate (2%)
drops 4-5 times a day.
4. Topical antihistaminics-
Azelastine eye drops
5. Acetyl cysteine (0.5%) has mucolytic properties and is
useful in treating early plaque formation.
6. Topical cyclosporine (1%) drops effective in severe
unresponsive cases.
Systemic therapy-
Oral antihistaminics and oral steroids in severe cases.

24. Peripheral ulcerative keratitis associated with
connective tissue disorders, Mooren’s Ulcer
Topical medication with antibiotics,
cycloplegics, steroids, lubricating drops.
Systemic medication includes
immunosuppresants (steroids, cyclosporine,
cyclophosphamide), doxycycline and oral
vitamin C.

25. Rosacea Keratitis
Topical treatment with steroids, but recurrences are very
common.
Systemic therapy—
Most essential and effective treatment is long course of
systemic tetracycline (250 mg QID for 3 weeks, TID for 3
weeks, BD for 3 weeks and OD for 3 months).

26. Common ocular therapeutics
Antibacterial agents
Sulphonamides:
1. Bacteriostatic.
2. Act by inhibiting folic acid synthesis in susceptible
microorganisms by competing with PABA which is
essential for bacterial cell nutrition.
3. Used in treatment of chlamydial infections.

27. Beta lactam antibiotics:
Two important groups included are penicillins and
cephalosporins.
All of them act by interfering with synthesis of bacterial cell
wall.

28. Penicillins-
Commonly used preparations are –
Benzyl penicillin, procaine penicilln, ampicillin, amoxycillin.
Methicillin, cloxacillin, flucloxacillin, carbenicillin---these are
penicillinase resistant, useful in infections caused by staph,
proteus, pseudomonas and coliform organisms.

29. Cephalosporins-
First generation (narrow spectrum)-
1. Active against gram positive cocci, hence useful against
staphylococcus.
2. Includes---cefazolin, cephradine, cephalexin, cephadroxyl
Second generation (intermediate spectrum)-
1. These have antistaphylococcal activity and are also
effective against certain gram negative organisms.
2. These include—cefuroxime, cefoxitin, cefamandole.
Third generation (wide spectrum)-
1. Mainly effective against gram negative organisms.
2. These include—cefotaxime, cefixime, cefotetan

30. Aminoglycosides-
Bactericidal.
Primarily active against gram negative organisms.
These are ototoxic and nephrotoxic.

31. Aminoglycosides……..
Commonly used preparations are—
Gentamicin-
1. Most commonly used aminoglycoside for acute infections,
broader spectrum of action, effective against
Pseudomonas aeruginosa.
2. Topically , it is used as 0.3% eye drops.
Tobramycin-
1. More active against Pseudomonas and Proteus as
compared to gentamicin.
2. Topically, it is used as 1% eye drops.

32. Aminoglycosides……
Amikacin-
It is recommended as reserve drug for hospital acquired
infections with gram negative bacilli, where gentamicin
resistance is increasing.
Neomycin and Framycetin-
1. Wide spectrum of activity.
2. Active against most gram negative and some gram positive
cocci.
3. Used only topically, due to high systemic toxicity.

33. Tetracyclines and Chloramphenicol-
1. Broad spectrum bacteriostatic agents.
2. Active against gram positive, gram negative organisms as
well as some fungi, Rickettsiae and Chlamydiae.
3. Topically used as 0.5 % eye drops.

34. Polypeptides-
1. Bactericidal.
2. Includes polymyxin B, bacitracin, colistin.
3. Polymyxin B and colistin—active against most gram
negative bacteria, notably Pseudomonas.
4. Neosporin (neomycin-polymyxin-bacitracin)—broad
spectrum antimicrobial, but has a disadvantage of high
incidence of sensitivity due to neomycin.

35. Fluoroquinolones-
1. Broad spectrum of activity against gram positive and gram
negative organisms.
2. Bactericidal drugs. Inhibit bacterial DNA synthesis.
Commonly used are—
1. First generation—cipro, norfloxacin
2. Second generation– ofloxacin, lomefloxacin, pefloxacin.
3. Third generation– sparfloxacin
4. Fourth generation—gati, moxifloxacin

36. Ocular antifungal agents
Polyene antifungals-
1. Mainstay of antifungal therapy.
2. MOA—work by binding to the sterol groups in fungal cell
membrane, making them impermeable. This leads to
lethal imbalance in cell contents.
3. These include—
Nystatin, natamycin, amphotericin B.

37. Ocular antifungal agents….
Imidazole antifungal drugs-
These include clotrimazole, econazole, fluconazole,
miconazole, itraconazole.
Other antifungals-
Flucytosine
Silver sulfadiazine—highly effective against Aspergillus
and Fusarium species.

38. Anti-glaucoma drugs for treating
secondary glaucoma
Timolol, Betaxolol-
Class---beta blockers
MOA---they block beta 2 receptors in the ciliary processess,
resulting in decreased aqueous production, thus lowering the
IOP.
These drugs should be used cautiously in patients with
bronchial asthma, emphysema, COPD, heart blocks, CCF and
cardiomyopathy.

39. Timolol, betaxolol…….
Ocular side effects-
Burning sensation, hyperemia, superficial punctate
keratopathy, corneal anesthesia.
Systemic side effects-
CVS---result from blockade of beta 1 receptors.
These include—bradycardia, arrhythmias, heart
failure, syncope.
RS---result from blockade of beta 2 receptors.
These include—brnchospasm and airway
obstruction, especially in asthmatics.
Anti-glaucoma drugs for
treating secondary
glaucoma

40. Timolol-
1. It is non selective beta 1 (cardiac) and beta 2 (smooth
muscles, respiratory tract) blocker.
2. Available as 0.25 and 0.5% eye drops.
3. Its action starts within 30 minutes, peak reaches in 2
hours and effects last up to 24 hours. Hence, used once or
twice daily.
Anti-glaucoma drugs for
treating secondary glaucoma

41. Timolol…..
4. The phenomenon of “short term escape” and “long term
drift” is seen with timolol.
“Short term escape” implies marked initial fall in IOP, followed
by a 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.
Anti-glaucoma drugs for
treating secondary
glaucoma

42. Betaxolol-
1. Is a cardioselective beta blocker, has 10 times more
affinity for beta 1 receptors than beta 2 receptors.
Hence, can be safely used in patients prone to attack of
bronchial asthma; advantage over timolol.
2. Available as 0.5 % and 0.25% suspension, is used twice
daily.
3. Action starts within 30 min, reaches peak in 2 hours and
lasts for 12 hours.
4. Slightly less effective than timolol in lowering IOP.
Anti-glaucoma drugs for
treating secondary glaucoma

43. Anti-glaucoma drugs for
treating secondary glaucomaAcetazolamide-
1. Is a carbonic anhydrase inhibitor.
2. Lowers IOP by reducing formation of aqueous humour.
3. Used as additive therapy for short term in management of
all types of acute and chronic glaucomas.
4. Side effects—paresthesias, urinary frequency, serum
electrolyte imbalance, abdominal discomfort, nausea,
diarrhoea.

44. Anti-glaucoma drugs for
treating secondary glaucomaAcetazolamide….
4. Available as tablets, capsules and injection for i.v. use.
250 mg tablet is used 6 hourly.
5. Action starts within one hour, reaches peak in 4 hours and
lasts for 6-8 hours.
Other carbonic anhydrase inhibitors—
Dorzolamide, Brinzolamide—can be used topically.

45. Anti-glaucoma drugs for
treating secondary glaucomaMannitol, Glycerol-
1. These are hyperosmotic agents, administered
systemically.
2. Used as additive therapy for rapidly lowering IOP in
emergency situations.
3. MOA– they increase the plasma tonicity. Thus, osmotic
gradient created between blood and vitreous draws
sufficient water out of the eyeball, thereby lowering IOP.

46. Anti-glaucoma drugs for
treating secondary glaucomaGlycerol-
1. Dose-1 to 1.5 gm/kg
2. Action starts in 10 minutes, peaks in 30 minutes and lasts
for about 5-6 hours.
3. It is metabolised to glucose in the body, hence repeated
use is not recommended in diabetics.

47. Anti-glaucoma drugs for
treating secondary glaucomaMannitol-
1. Dose-1-2 gm/kg
2. Administered very rapidly over 20-30 minutes.
3. Action peaks in 30 minutes and lasts for about 6 hours.
4. It doesn’t enter glucose metabolism, hence safe in
diabetics.

48. Corticosteroids
They have potent anti-inflammatory, anti-allergic and anti-
fibrotic actions.
Short acting-
Hydrocortisone, cortisone, prednisolone,
methylprednisolone, prednisone.
Intermediate acting-
Triamcinolone, fluprednisolone
Long acting-
Dexamethasone, betamethasone.

49. Corticosteroids …….
Commonly used topical preparations are cortisone
acetate, hydrocortisone, dexamethasone, betamethas
one, medryson, fluromethalone, loteprednol.
Commonly used systemic preparations are –
Prednisolone—5 / 10 mg tablet,
Dexamethasone– 0.5 mg tablet,
Betamethasone– 0.5 / 1 mg tablet.

50. Corticosteroids …….
Side effects-
Injudicious use of topical steroids can cause
glaucoma, cataract, activation of infection (if given in
herpertic, fungal or bacterial keratitis), dry eye, ptosis.
Misuse of systemic steroids can cause ocular side effects as
mentioned above and systemic side effects such as peptic
ulcer, HTN, osteoporosis, worsening of DM, cushingoid state
and reactivation of tuberculosis and other infections.

51. Non steroidal anti-inflammatory drugs
(NSAIDs)
They have anti-inflammatory, analgesic and antipyretic
actions.
MOA– act by irreversibly blocking COX enzyme, thus inhibiting
PG synthesis. Also block other local mediators of
inflammatory response.

52. Non steroidal anti-inflammatory drugs (NSAIDs)…………
Topical opthalmic NSAIDs preparations available are-
1. Indomethacin 0.1 % suspension
2. Flurbiprofen 0.3 % eye drops
3. Ketorolac 0.5 % eye drops
4. Diclofenac 0.1% eye drops
5. Bromefenac 0.09% eye drops
6. Nepafenac 0.1 % eye drops
Systemically used NSAIDs-
Paracetamol, diclofenac, acelcofenac, ketorolac, ibuprofen
flurbiprofen, naproxen, mefenamic acid, etc.

53. Cycloplegics
These are the drugs which cause paralysis of accommodation
and dilatation of the pupil.
Commonly used drug is atropine sulfate 1% eye ointment or
drops instilled 2-3 times a day.
In case of atropine allergy, other cycloplegics like 2%
homatropine or 1% cyclopentolate (short acting) eye drops
may be instilled 3-4 times/ day.
Alternatively for more cycloplegic effect, a subconjunctival
injection of 0.25 ml mydricain (mixture of
atropine, adrenaline and procaine) can be given.

54. Cycloplegics……
Mode of action of atropine-
1. Gives comfort and rest to the eye by relieving spasm of iris
sphincter and ciliary muscle.
2. Prevents formation of synechiae and may break already
formed synechiae.
3. Reduces exudation by decreasing hyperemia and vascular
permeability.
4. Increases blood supply to anterior uvea by relieving
pressure on anterior ciliary arteries. As a result more
antibodies reach the target tissue and more toxins are
absorbed.

55. Thank you