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Dr. Atul Kumar Anand
Senior Resident
AIIMS Patna
4 Routes of drug administration
Topical
Periocular injection
Intraocular injection
Systemic administration
Topical instillation into conjunctival sac in
the form of
(a) Eyedrops:- simplest, most
convenient & most commonly used,
(specially in daytime) drugs available for
immediate action but quickly diluted by
tears
(b)Eye ointment : increases
bioavailability of drug by increasing tissue
contact time & by preventing dilution,
however drug not available for
immediadte action & ointment blur the
vision( better for bedtime)
Gel preparations cause less blurring but
costly
Benzalkonium chloride(BKC) used as
preservative, also acts as wetting agent so
increases drug absorption
(a)Subconjunctival injection: – to
achieve higher concentration of drug &
drug which cannot penetrate cornea due to
large size can easily pass through sclera
(b)Subtenon injection:- mainly for
steroid, Anterior subtenon for severe or
resistant anterior uveitis, posterior
subtenon for intermediate & posterior
uveitis
(c)Retrobulbar injection: - used to
deliver drug for optic neuritis, papillitis & for
retrobulbar anaesthesia
(d)Peribulbar injection:- for
anaesthesia
To deliver drug in maximum concentration
at target tissue
(a)Intracameral injection:- into
anterior chamber
(b)Intravitreal injection:- into vitreous
cavity
Oral
I/V
I/M
Two group
Penicillin & Cephalosporin
MOA – act by interfering with synthesis of
bacterial cellwall
Bactericidal
Bactericidal
Excreted mainly via kidney
S/E – hypersensitivity/allergic reaction,
urticaria anaphylactic shock
In deep seated inflammation of orbit or lids
given parenterally
Example:- benzyl penicillin, procaine
penicillin, methicillin cloxacillin,
carbenicillin, ampicillin, amoxycillin
Bactrericidal
Structure & MOA similar to penicillin
S/E low, usually allergic reaction of
penicillin type
Eg. cephazolin, cephalexin, cefotaxim,
ceftazidime{intraviterially also}

Bactericidal
Not absorbed orally
Maily against gram negative
Ototoxic and nephrotoxic
Eg.streptomycin,
gentamicin[topically 0.3 %]-retinotoxic
tobramicin-more potent [1% topical]
amicakin-intravitreal along with
vancomycin in endoph, less retinotoxic

Broad spctrum, bacteriostatic
Active against both gram positive &
negative, ricketissia, clamydia (trachoma)
C/I:- child, pregnancy, lactation
Broad spctrum, bacteriostatic
Active against both gram positive &
negative, ricketissia, clamydia
Topical 0.5%
Narrow spectrum, bacteriostatic
Active against gram positive, chlamydia,
toxoplasma
Eg:- erythromycin, azithromycin
S/E:- diarrohea
Eg:-Vancomycin – bactericidal, very
effective against nearly all gram +ve &
MRSA, staph aureus, staph epidim.
Given intravitereal
DOC endophthalmitis together with
amikacin and ceftazidime
Potent, bacteriocidal broad spectrum
against gram+ve & -ve
Eg.ciprofloxacin, norfloxacin, ofloxacin,
sparfloxacin, gatifloxacin -- all 0.3%
Moxifloxacin-0.5%
Amphotericin B : fungistatic or cidal
depending on concentration
Effective in superficial infection
Effective against both yeast & filamentous
fungi
Topically 0.1 -0.25% drop or 2.5% ointment
Can be given inrtavitreal or intravenous
S/E:- kidney, bone marrow & CNS toxicity
Broad spectrum (candida, fusarium,
aspergillus)
Topical 5% suspension, hrly
Adheres well to surface of ulcer making
contact time of drug with eye greater
Fungistatic
No oral only topical
Narrow spectrum, poor penertation
Less toxic
Miconazole:- against yeast & filamentous
fungi, fungicidal
Topical 1% drop, 2% ointment
Ketoconazoles :- against candida, less for
aspergillus
Orally 200-800mg, 7days to months in
fungal endoph.& for severe corneal
infection
S/E:- liver toxicity
Fluconazole:- fungistatic, against candida,
cryptococcus
Oral 100 -200 mg
Topical 0.2%
Low S/E
Itraconazole:- similar to ketoconazole
Oral 100-400 mg
Topical 1%
Aim of treatment is lowering the IOP
Achieved by decreasing the aqueous
production or by increasing outflow of
aqueous through trabecular meshwork or
uveoscleral pathway
Parasympathomimetic drug(cholinergic
drugs) - miotics
Sympathomimetic drug(adrenergic
agonists)
Beta adrenergic blockers
Prostaglandins analogues
Carbonic anhydrase inhibitors(CAI)
Hyperosmotic agents
MOA: - in PACG constriction of pupil pulls
peripheral iris away from angle structures,
opening a functionally closed angle.
Example Pilocarpine(1%, 2%, 4%)
Carbachol
S/E:- Local:- spasm of accommodation,
iris cyst formation, frontal headache,
myopia, impairment of night vision &
generalised contraction of visual field due
to miosis
C/I:- inflammatory glaucoma, malignant
glaucoma & known allergy
Non-selective alpha & beta
agonists
Epinephrine 1%(adrenaline) twice daily
Decreases IOP by increasing rate of
aqueous outflow
S/E:- Local:- stinging, hyperaemia, CME in
aphakic eyes
C/I:- in patient with narrow anterior
chamber as it causes mydriasis
Dipivefrine 0.1% :- a prodrug, converted to
epinephrine once inside eye, 17 times
more corneal penetration but less S/E
than epinephrine
Alpha-agonist:-
Clonidine:- 0.06 to 0.125% drop 6-8 hrly
Decreases IOP by decreasing aqueous
production & to lesser extent by
increasing trabecular uveoscleral outflow
Available in europe
Apraclonidine :-1% potent ocular
hypotensive
Used prophylactically for prevention of IOP
rise following LASER trabeculoplasty, YAG
laser iridotomy & posterior capsulptony
 S/E: conjunctival blanching, follicular
conjunctivitis, dry mouth, drowsiness
 Brimonidine 0.2% drops twice or thrice
selective alpha 2 agonist, lowers IOP by
decreasing aqueous production & enhancing
uveoscleral outflow
 S/E:- similar to apraclonidine
 Neuroprotective
Lowers IOP by decreasing aqueous
production
Commonly used AGM, useful in all types of
glaucoma(congenital, primary, 2ndary)
Non-selective beta-1& beta-2 blockers:-
timolol, levobunolol, carteolol, metipranolol
have greater IOP lowering effect than beta 2
selective (cardioselective) Betaxolol but it is
safe in asthma & COPD
S/E:- dry eye, burning, hyperaemia,
bronchospasm, bradycardia depression
C/I:- COPD, asthma, heart block, CHF
Timolol Maleate 0.5% BD, tachyphylaxis
Betaxolol 0.5% BD, less effective, less
pulmonary side effect, increase perfusion
of optic nerve head
Lowers IOP by increasing uveoscleral
outflow,( lower IOP 25-30% equivalent to
Timolol)
Given Once daily(OD at HS)
Latanoprost (0.005%)
Travoprost (0.004%)
Bimatoprost (0.03%)
S/E: hyperemia, FB sensation,
pigmentation of iris
Decrease aqueous production by blocking
carbonic anhydrase enzyme
Acetazolamide potent, systemic AGM,
used for controlling very high IOP in any
glaucoma, tablet 250 mg 6 hrly, or 500mg I/V
S/E: paraesthesia of hand & feet, loss of
appetite, altered taste, potassium depletion,
diarrhoea, renal calculi SJ
syndome(sulfonamide related side effect)
Dorzolamide 2% BD or TDS, 1st topical
CAI
S/E: allergic reaction, burning
Brinzolamide 1% BD, topical CAI
Increase osmolality of serum causing water
to leave vitreous cavity, so lowering IOP,
reducing vitreous volume & deepening AC
An ideal hyperosmotic agent should be
rapidly absorbed & distributed & have a high
molecular weight so that it does not enter the
eye
Rapidally lowering IOP, used in emergenecy(
glaucoma with very high IOP)
Mannitol 20%(1-2gm/kg),
given I/V rapidlly in 20-30 minutes, does
not enter glucose metabolism, so safe in
diabetics, but given with caution in
hypertensive, pulmonary edema cardiac or
renal failure patient.
Urinary retention may occur in prostatic
hypertrophy patient
Glycerol 50%(1-1.5gm/kg) given orally
Induces nausea & vomiting, so taken
mixed with lemon juice
Metabolised to glucose in body, so less
suitable for diabetics
Urea: given I/V, lower efficacy & more
side effect, so not routinely used
For herpes simplex:- Idoxuridine, acyclovir
For herpes zoster:- acyclovir, famiciclovir
For CMV retinitis :- ganciclovir, foscarnet
Pyrimidine derivative:-
Virostatic
Against DNA virus
For dentritic ulcer 0.1% drop, 1-2 hrly
0.5% ointment,
no deep penetration(not useful in stromal
keratitis)
s/e follicular conjunctivitis, spk, punctal
stenosis
Virustatic, safe & effective in most forms of
H.simplex & zoster
3% ointement, 5 times daily in epithelial
and stromal keratitis
Oral 400 – 800 mg, 5 times day for 7-10
days
Derivative of acyclovir
Used in CMV retinitis, H.simplex 1 & 2
May be given intraviterally
Dilate pupil causing mydriasis & impair
accommodation leading to cycloplegia
Used in determining correct refraction of
eye specially in child & hypermetrops
Atropine 1% ointment, most potent,
longest acting, 7days or more, used in
child less than 5 yrs, systemic absorption
may cause facial flushing, so ointment
preferred , also used as penalisation
therapy in better eye in amblyopia
Homatropine 2% drop, less potent, effect
lasts for 4-5 days, used in treatment of
uveitis & refraction in children
Cyclopentolate 1% drop, less potent,
shorter duration of action, lasting upto 24
hrs, used for refraction
Tropicamide 0.5%, 1% drop shortest
acting, effective upto 3-4 hrs, used for
fundus examination & refraction
S/E : blurred vision & photophobia
Phenylephrine 5-10%(selective alpha 1
agonist) only mydriatics no cycloplegics
Used in combination with cyclopegics to
dilate pupil for fundus exam, retinal laser
prior to cataract surgery
S/E: stinging on application , rise in blood
pressure in predisposed individual
 Replaces aqueous component of tear
 Contain electrolytes, viscous, alkaline ph
 Eg. Hydroxypropylmethylcellulose (HPMC),
carboxymethylcellulose (CMC) ,
hydroxymethylcellulose, polyvinyl alcohol,
hyaluronic acid, chondroitin sulfate
 Preservatives are epitheliotoxic to cornea and
conjunctiva
 Benzalkonium chloride(BKC) is most
epitheliotoxic
Povidone and chlorobutanol are better
tolerated so better
Preservative free drops are best
alternative
Newer preservatives as sod.perborate and
purite disintegrate into harmless molecule
on contact with eye and exposure to light
 Viscous material that asist surgeon in different
intraocular surgery
 Properties of an ideal viscoelastic:-
 Chemically inert
 Non antigenic, non toxic, isoosmotic & sterile
 Free from particulate matter
 Optically clear
 Viscosity enough to provide sufficient space for
manipulation within eye
 Hydrophilic and dilutable properties to irrigate
material out of eye after surgery
 Protectibility to protect corneal endothelium
Types :
Cohesive & Dispersive
Cohesive mol. adhere to each other, useful
as spacers for manipulation & easy to
remove
Used for capsulorhexis & placement of IOL
Dispersive:
Coats ocular surfaces, remain in position
during irrigation
Used for protecting corneal endothelium
eg. Sod.hyaluronate 1% :- cohesive, best
but expensive
Methylcellulose :- most commonly used
Hypermellose 2%
Combination of 4% chondroitin sulphate &
3% sod.hyaluronate
Uses:-
During cataract surgery for
1.maintenantace of ant. Chamber
2.protection of corneal endothelium
3.coating the IOL
Other uses
Repair of globe in perforating injury
Glaucoma surgery
keratoplasty
S/E:-
Postop rise in iop if cosiderabl amount of
viscoelastic is left inside the ant.chamber
Ocular Pharmacology .pptx
Ocular Pharmacology .pptx
Ocular Pharmacology .pptx
Ocular Pharmacology .pptx
Ocular Pharmacology .pptx

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Ocular Pharmacology .pptx

  • 1. Dr. Atul Kumar Anand Senior Resident AIIMS Patna
  • 2. 4 Routes of drug administration Topical Periocular injection Intraocular injection Systemic administration
  • 3. Topical instillation into conjunctival sac in the form of (a) Eyedrops:- simplest, most convenient & most commonly used, (specially in daytime) drugs available for immediate action but quickly diluted by tears
  • 4. (b)Eye ointment : increases bioavailability of drug by increasing tissue contact time & by preventing dilution, however drug not available for immediadte action & ointment blur the vision( better for bedtime) Gel preparations cause less blurring but costly Benzalkonium chloride(BKC) used as preservative, also acts as wetting agent so increases drug absorption
  • 5. (a)Subconjunctival injection: – to achieve higher concentration of drug & drug which cannot penetrate cornea due to large size can easily pass through sclera (b)Subtenon injection:- mainly for steroid, Anterior subtenon for severe or resistant anterior uveitis, posterior subtenon for intermediate & posterior uveitis
  • 6. (c)Retrobulbar injection: - used to deliver drug for optic neuritis, papillitis & for retrobulbar anaesthesia (d)Peribulbar injection:- for anaesthesia
  • 7. To deliver drug in maximum concentration at target tissue (a)Intracameral injection:- into anterior chamber (b)Intravitreal injection:- into vitreous cavity
  • 9.
  • 10. Two group Penicillin & Cephalosporin MOA – act by interfering with synthesis of bacterial cellwall Bactericidal
  • 11. Bactericidal Excreted mainly via kidney S/E – hypersensitivity/allergic reaction, urticaria anaphylactic shock In deep seated inflammation of orbit or lids given parenterally Example:- benzyl penicillin, procaine penicillin, methicillin cloxacillin, carbenicillin, ampicillin, amoxycillin
  • 12. Bactrericidal Structure & MOA similar to penicillin S/E low, usually allergic reaction of penicillin type Eg. cephazolin, cephalexin, cefotaxim, ceftazidime{intraviterially also} 
  • 13. Bactericidal Not absorbed orally Maily against gram negative Ototoxic and nephrotoxic Eg.streptomycin, gentamicin[topically 0.3 %]-retinotoxic tobramicin-more potent [1% topical] amicakin-intravitreal along with vancomycin in endoph, less retinotoxic 
  • 14. Broad spctrum, bacteriostatic Active against both gram positive & negative, ricketissia, clamydia (trachoma) C/I:- child, pregnancy, lactation
  • 15. Broad spctrum, bacteriostatic Active against both gram positive & negative, ricketissia, clamydia Topical 0.5%
  • 16. Narrow spectrum, bacteriostatic Active against gram positive, chlamydia, toxoplasma Eg:- erythromycin, azithromycin S/E:- diarrohea
  • 17. Eg:-Vancomycin – bactericidal, very effective against nearly all gram +ve & MRSA, staph aureus, staph epidim. Given intravitereal DOC endophthalmitis together with amikacin and ceftazidime
  • 18. Potent, bacteriocidal broad spectrum against gram+ve & -ve Eg.ciprofloxacin, norfloxacin, ofloxacin, sparfloxacin, gatifloxacin -- all 0.3% Moxifloxacin-0.5%
  • 19.
  • 20. Amphotericin B : fungistatic or cidal depending on concentration Effective in superficial infection Effective against both yeast & filamentous fungi Topically 0.1 -0.25% drop or 2.5% ointment Can be given inrtavitreal or intravenous S/E:- kidney, bone marrow & CNS toxicity
  • 21. Broad spectrum (candida, fusarium, aspergillus) Topical 5% suspension, hrly Adheres well to surface of ulcer making contact time of drug with eye greater
  • 22. Fungistatic No oral only topical Narrow spectrum, poor penertation
  • 23. Less toxic Miconazole:- against yeast & filamentous fungi, fungicidal Topical 1% drop, 2% ointment Ketoconazoles :- against candida, less for aspergillus Orally 200-800mg, 7days to months in fungal endoph.& for severe corneal infection S/E:- liver toxicity
  • 24. Fluconazole:- fungistatic, against candida, cryptococcus Oral 100 -200 mg Topical 0.2% Low S/E Itraconazole:- similar to ketoconazole Oral 100-400 mg Topical 1%
  • 25.
  • 26. Aim of treatment is lowering the IOP Achieved by decreasing the aqueous production or by increasing outflow of aqueous through trabecular meshwork or uveoscleral pathway
  • 27. Parasympathomimetic drug(cholinergic drugs) - miotics Sympathomimetic drug(adrenergic agonists) Beta adrenergic blockers Prostaglandins analogues Carbonic anhydrase inhibitors(CAI) Hyperosmotic agents
  • 28. MOA: - in PACG constriction of pupil pulls peripheral iris away from angle structures, opening a functionally closed angle. Example Pilocarpine(1%, 2%, 4%) Carbachol S/E:- Local:- spasm of accommodation, iris cyst formation, frontal headache, myopia, impairment of night vision & generalised contraction of visual field due to miosis
  • 29. C/I:- inflammatory glaucoma, malignant glaucoma & known allergy
  • 30. Non-selective alpha & beta agonists Epinephrine 1%(adrenaline) twice daily Decreases IOP by increasing rate of aqueous outflow S/E:- Local:- stinging, hyperaemia, CME in aphakic eyes C/I:- in patient with narrow anterior chamber as it causes mydriasis
  • 31. Dipivefrine 0.1% :- a prodrug, converted to epinephrine once inside eye, 17 times more corneal penetration but less S/E than epinephrine
  • 32. Alpha-agonist:- Clonidine:- 0.06 to 0.125% drop 6-8 hrly Decreases IOP by decreasing aqueous production & to lesser extent by increasing trabecular uveoscleral outflow Available in europe Apraclonidine :-1% potent ocular hypotensive Used prophylactically for prevention of IOP rise following LASER trabeculoplasty, YAG laser iridotomy & posterior capsulptony
  • 33.  S/E: conjunctival blanching, follicular conjunctivitis, dry mouth, drowsiness  Brimonidine 0.2% drops twice or thrice selective alpha 2 agonist, lowers IOP by decreasing aqueous production & enhancing uveoscleral outflow  S/E:- similar to apraclonidine  Neuroprotective
  • 34. Lowers IOP by decreasing aqueous production Commonly used AGM, useful in all types of glaucoma(congenital, primary, 2ndary) Non-selective beta-1& beta-2 blockers:- timolol, levobunolol, carteolol, metipranolol have greater IOP lowering effect than beta 2 selective (cardioselective) Betaxolol but it is safe in asthma & COPD
  • 35. S/E:- dry eye, burning, hyperaemia, bronchospasm, bradycardia depression C/I:- COPD, asthma, heart block, CHF Timolol Maleate 0.5% BD, tachyphylaxis Betaxolol 0.5% BD, less effective, less pulmonary side effect, increase perfusion of optic nerve head
  • 36. Lowers IOP by increasing uveoscleral outflow,( lower IOP 25-30% equivalent to Timolol) Given Once daily(OD at HS) Latanoprost (0.005%) Travoprost (0.004%) Bimatoprost (0.03%) S/E: hyperemia, FB sensation, pigmentation of iris
  • 37. Decrease aqueous production by blocking carbonic anhydrase enzyme Acetazolamide potent, systemic AGM, used for controlling very high IOP in any glaucoma, tablet 250 mg 6 hrly, or 500mg I/V S/E: paraesthesia of hand & feet, loss of appetite, altered taste, potassium depletion, diarrhoea, renal calculi SJ syndome(sulfonamide related side effect)
  • 38. Dorzolamide 2% BD or TDS, 1st topical CAI S/E: allergic reaction, burning Brinzolamide 1% BD, topical CAI
  • 39. Increase osmolality of serum causing water to leave vitreous cavity, so lowering IOP, reducing vitreous volume & deepening AC An ideal hyperosmotic agent should be rapidly absorbed & distributed & have a high molecular weight so that it does not enter the eye Rapidally lowering IOP, used in emergenecy( glaucoma with very high IOP)
  • 40. Mannitol 20%(1-2gm/kg), given I/V rapidlly in 20-30 minutes, does not enter glucose metabolism, so safe in diabetics, but given with caution in hypertensive, pulmonary edema cardiac or renal failure patient. Urinary retention may occur in prostatic hypertrophy patient
  • 41. Glycerol 50%(1-1.5gm/kg) given orally Induces nausea & vomiting, so taken mixed with lemon juice Metabolised to glucose in body, so less suitable for diabetics Urea: given I/V, lower efficacy & more side effect, so not routinely used
  • 42.
  • 43. For herpes simplex:- Idoxuridine, acyclovir For herpes zoster:- acyclovir, famiciclovir For CMV retinitis :- ganciclovir, foscarnet
  • 44. Pyrimidine derivative:- Virostatic Against DNA virus For dentritic ulcer 0.1% drop, 1-2 hrly 0.5% ointment, no deep penetration(not useful in stromal keratitis) s/e follicular conjunctivitis, spk, punctal stenosis
  • 45. Virustatic, safe & effective in most forms of H.simplex & zoster 3% ointement, 5 times daily in epithelial and stromal keratitis Oral 400 – 800 mg, 5 times day for 7-10 days
  • 46. Derivative of acyclovir Used in CMV retinitis, H.simplex 1 & 2 May be given intraviterally
  • 47.
  • 48. Dilate pupil causing mydriasis & impair accommodation leading to cycloplegia Used in determining correct refraction of eye specially in child & hypermetrops Atropine 1% ointment, most potent, longest acting, 7days or more, used in child less than 5 yrs, systemic absorption may cause facial flushing, so ointment preferred , also used as penalisation therapy in better eye in amblyopia
  • 49. Homatropine 2% drop, less potent, effect lasts for 4-5 days, used in treatment of uveitis & refraction in children Cyclopentolate 1% drop, less potent, shorter duration of action, lasting upto 24 hrs, used for refraction Tropicamide 0.5%, 1% drop shortest acting, effective upto 3-4 hrs, used for fundus examination & refraction S/E : blurred vision & photophobia
  • 50. Phenylephrine 5-10%(selective alpha 1 agonist) only mydriatics no cycloplegics Used in combination with cyclopegics to dilate pupil for fundus exam, retinal laser prior to cataract surgery S/E: stinging on application , rise in blood pressure in predisposed individual
  • 51.
  • 52.  Replaces aqueous component of tear  Contain electrolytes, viscous, alkaline ph  Eg. Hydroxypropylmethylcellulose (HPMC), carboxymethylcellulose (CMC) , hydroxymethylcellulose, polyvinyl alcohol, hyaluronic acid, chondroitin sulfate  Preservatives are epitheliotoxic to cornea and conjunctiva  Benzalkonium chloride(BKC) is most epitheliotoxic
  • 53. Povidone and chlorobutanol are better tolerated so better Preservative free drops are best alternative Newer preservatives as sod.perborate and purite disintegrate into harmless molecule on contact with eye and exposure to light
  • 54.
  • 55.  Viscous material that asist surgeon in different intraocular surgery  Properties of an ideal viscoelastic:-  Chemically inert  Non antigenic, non toxic, isoosmotic & sterile  Free from particulate matter  Optically clear  Viscosity enough to provide sufficient space for manipulation within eye  Hydrophilic and dilutable properties to irrigate material out of eye after surgery  Protectibility to protect corneal endothelium
  • 56. Types : Cohesive & Dispersive Cohesive mol. adhere to each other, useful as spacers for manipulation & easy to remove Used for capsulorhexis & placement of IOL
  • 57. Dispersive: Coats ocular surfaces, remain in position during irrigation Used for protecting corneal endothelium eg. Sod.hyaluronate 1% :- cohesive, best but expensive Methylcellulose :- most commonly used Hypermellose 2% Combination of 4% chondroitin sulphate & 3% sod.hyaluronate
  • 58. Uses:- During cataract surgery for 1.maintenantace of ant. Chamber 2.protection of corneal endothelium 3.coating the IOL Other uses Repair of globe in perforating injury Glaucoma surgery keratoplasty
  • 59. S/E:- Postop rise in iop if cosiderabl amount of viscoelastic is left inside the ant.chamber