Department of optometry

Seminar on ocular antibiotics

Prepared by: Dagmawit Ayalew

4th year optometry Student

Moderator: Alemayehu
Desalegn(BSc, MSc)
DATE 05/03/2007 EC.
 Outline
• Definition
• Classification
• Mechanism of action
• Effective agents
• The therapeutic use
• Adverse effect
• Preparations
 What is antibiotic?
• Antibiotic is a chemical that is
produced by one microorganisms
and has the ability to harm other
microbes.
• The term ‘anti-infective’ covers a wide group
of agents that are effective against a variety of
infections: e.g
 viruses
 Bacteria
 fungi and protozoa
• The mechanism of action of these
agents varies greatly and, to some
extent, will depend on the organism
on which the particular agent acts.
• In the majority of cases, however, some
competitive inhibition of a biochemical
process is involved.
• As a result, the concentration level of the
antibacterial (and hence the dose) are
fundamental to the success or otherwise of
antibacterial treatments.
 classification
• Antibacterials can be divided into the following
groups:
 Beta-lactams
 Tetracyclines
 Macrolides
 Chloramphenicols
 Fluoroquinolones
 Aminoglycosides
 Sulfonamides
 Miscellaneous agents.
 1. Beta-Lactams
• These agents are so called because of the
presence of a beta lactam ring in their
chemical structure. They all produce their
effect by interfering with the synthesis of the
cell wall.
 In which, binding to certain enzymes in the
cell membrane that are responsible for the
building of the cell wall.
producing morphological changes in the
bacteria they affect. They can be divided into
two main groups: the penicillin and
cephalosporin
 penicillin
• The principal agent in this group is penicillin,
the original antibiotic. Although penicillin is still
extensively used in systemic medicine, several
synthetic derivatives have been developed with
broader spectrums (e.g. amoxicillin and
ampicillin).
• whereas others are resistant to penicillinase
(e.g. flucloxacillin). Penicillins pass across the
ocular barriers very poorly and products
containing them are rarely used in the
treatment of ocular infections.
• It can be administered locally as drop or
ointment and in deep-seated inflammation of
the orbit and lid it is given parentrally.

• e.g Ampicillin : it is broad-spectrum usually

administered orally; dosage is 0.25-2g
oral/i.m/i.v. depending upon the severity of
infection every 6 hours. paediatric dose is
25-50 mg/kg/day.
 2. Tetracyclines
• Tetracyclines are broad spectrum antibiotics.
Penetration across intact cornea is poor. Best
used for surface infections.

 Mechanism of action
:- inhibit bacterial protein synthesis.
:- bacterio static
• Specific agents:-
tetracycline, doxycycline
• Anti-microbial spectrum:- effective against
gram +ve and gram –ve bacteria
 Therapeutic use
• Superficial bacterial infection of the eye
• Mass treatment of trachoma in endemic area
• Prophylaxis of neonatal conjunctivitis
Adverse effect
• Rash, rarely stinging and burning
preparation
• Eye ointment, tetracycline hydrochloride 1%
 3. Macrolides
• Have relatively broad spectrum of anti
microbial action.
Mechanism of action
• Inhibit bacterial protein synthesis and
bacteriostatic.
Mechanism of bacterial resistance
 Decreased permeability of drug into microbe
 Modification of target size
 Hydrolysis of macrolide by bacterial enzymes

Anti microbial spectrum

• Gram +ve and gram –ve bacteria
 Erythromycin
• May have bactericidal or bacteriostatic
properties.

• Often used in the treatment of systemic

infections but for ophthalmic use, best known
for the effect on chlamydia ( 250 mg orally ) or
as (ointment 0.5%) and other organisms.
• Oral erythromycin is commonly used for
infections in many parts of the body, including
the eyelids and orbit.

• However, it is usually reserved for cases where

more effective antibiotics are contraindicated.
Adverse effects
• Irritative effects, nausea, diarrhea and gastro
intestinal upset(oral administrations)
• More serious complications such as liver
damage are rare but possible
• If taken with antihistamine could cause cardiac
toxicity.
 Azithromycin
Mechanism of action
• Inhibition of bacterial protein synthesis.
Therapeutic use
• Uncomplicated genital chlamydia infection and
trachoma.
Adverse effect
• Anorexia, dyspepsia, constipation, dizziness,
drowsiness.

Preparation
• Capsules, azithromycin 250mg 0r 500mg
• Oral suspension, azithromycin 200mg per 5ml
 4. Chloramphenicol
• The principal agent is chloramphenicol,
although another thimphenicol exists.
Mechanism of action
 Inhibit Protein synthesis
 It has bacteriostatic action
 Active agents most gram +ve and –ve,
however p.aeruginosa is resistant to this drug.
• There are many ocular patogens on which this
drug is effective e.g. E.coli, streptococci

• Topical application of chloramphenicol

solution or ointment is effective against most
bacterial infections of the external eye.
• It has been recommended for the routine
treatment of opthalmia neonatorum.

• It’s effect against chlamydiae has led to it’s use

in trachoma.

• It penetrates easily into the cell by a process of

facilitated diffusion.
 Adverse effects
• Hematopoetic abnormality bone marrow
depression(dose related toxicity), usually
discontinuing the antibiotic reverses the toxicity.

• Aplastic anemia
• Preparations:- eye drope 0.5% , eyeointment 1%.
 5. fluoroquinoiones
• Extremely effective bactericidal drugs
• Have broad spectrum activity with increased
effectiveness against gram –ve pathogens
• This group of antibiotics includes
 norfloxacin
 levofloxacin
 ciprofloxacin (0.3% solution)
 ofloxacin (eye drops 0.3%)
• Ciprofloxacin and ofloxacin have been
formulated for ophthalmic use.

• These drugs interfere with the production of

DNA by inhibiting enzyme responsible for
nucleic acid in the bacteria.
• Fluoroquinolone have several advantages over
other antimicrobials
 they have very low corneal toxicity
 they have very rapid kill rate
 they have very good corneal penetration
 Ciprofloxacin
• An ophthalmic form of ciprofloxacin has been
introduced as 0.3% solution.
• Absorption into ocular tissue is good
• It has been shown to be as effective as
tobramycin in the treatment of bacterial
conjunctivitis.
• a safe and effective treatment of bacterial
keratitis caused by a wide variety of
bacteria.

• In the treatment of bacterial conjunctivitis

ciprofloxacin has proved to be as valuable
a drug as chloramphenicol in terms of
efficacy and safety.
 ofloxacin
• Used in treatment of chlamydia conjunctivitis
(in the past)
• It is now marketed for the treatment of
external ocular infections.
• It has similar antibacterial property to
ciprofloxacin.
 Newer fluoroquinolones
• Gatifloxacin and moxifloxacin; in addition to
gram –ve, they have improved gram +ve
coverage
• Claimed to have better penetration of
- cornea
- conjunctiva
- anterior chamber
• Less tissue toxicity
 6. Aminoglycosides
• Are narrow spectrum antibiotics used
primarily against aerobic gram –ve bascilla.
• All aminoglycosides are rapidly bacteriocidal
and Inhibit protein synthesis.
• Penicillin aids the passage of aminoglycosides
into the cell. this two antibacterials should be
synergist.
specific agent:-
 gentamycin
 tobramycin
 amikacin
 Gentamycin
• Mechanism of action:
- inhibition of bacterial protein synthesis

• Therapeutic uses:
- blepharitis, bacterial conjunctivitis, systemic
infections.
- given by injection for serious systemic
infection, so should be kept for serious infections
of the eye.
• Adverse effects:
-burning, stinging, itching, dermatitis
-it is very toxic compound

• preparation:
- 0.3%gentamicin solution (as sulphate) eye drop
(more concentrated of solutions recommended for
bacterial corneal ulcer)
-0.3% ophthalmic ointment
 Tobramycin
• Marketed as 0.3% ophthalmic solution and
ointment
• It is also prepared as a topical fortified
solution
• Slightly more effective than gentamicin
• Less toxic than gentamicin
• Tobramycin is still the drug of choice for many
ocular infections.
 7. sulphonamides
• At one time they were one of the first line
treatment for bacterial conjunctivitis. they are no
longer manufactured as ophthalmic preparations
because their use has been suppressed by more
modern agents.
• Sulphacetamide sodium
• have a bacteriostatic rather than bactericidal
action.
• inhibit the growth of most gram +ve organisms
and variety of gram –ve bacteria.
• Although possessing relatively weak bactericidal
action compared to other sulphonamides, is
suitable for topical application of the eye
because of it’s acceptable PH and its solubility in
aqueous agents.
 8. Miscellaneous agents
• Are heterogeneous group of agents that are or
have been in the past formulated as topical
antibacterial agents and for ophthalmic use.
fusidic acid
• inhibiting protein synthesis although unlike
other antibiotics it does not bind to ribosomes.
• It has potent bacteriostatic or bactericidal
activity against gram +ve bacteria:- it’s effective
against staph.aureus.
• most gram –ve bacteria are resistant but it does
have some activity against gram –ve bacteria

• Lately it has become very popular for treatment

of bacterial conjunctivitis and compared with 1%
chloramphenicol ointment, applied every three
hours and produced similar beneficial effects.
• Summery
Antibiotics drugs are used in combination
with anti-viral and anti-fungal drugs for better
management.

And also used for post operation treatment

and as prophylactic treatments.
 Antibiotics
Broad spectrum Narrow spectrum
-Penicillin -Gentamicin
-Tetracycline -Tobramycin
-Erythromycin -Amikacin
-Azithromycin -Sulphacetamide sodium
-Chloramphenicol
-Ciprofloxacin
-Ofloxacin
• Reference
-ophthalmic drugs diagnostic and therapeutic
uses 5th edition
-comprehensive ophthalmology 4th edition
-clinical ocular pharmacology 5th edition
-ocular pharmacology hand out
 N …
NT IO
AT TE
U R
YO
FOR
YO U
N K
TH A
•