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Glaucoma
Medications
BY
Dr. Amr Mounir
Lecturer of Ophthalmology
Sohag University
Background
The aqueous humor is a transparent watery fluid
It fills both the anterior and the posterior chambers of the eye
Aqueous humor is produced by the ciliary processes
The drainage route for aqueous humor flow occurs
through two routes
1) Main route: Trabecular meshwork 90%
2) Secondary route: Uveoscleral drainage 10%
Background
α1-, α2-, β1- and β2-adrenoceptors have been located in the ciliary body.
α2- and β2-Adrenoceptors have also been located in the trabecular meshwork
- Stimulation of α2-adrenoceptors in the ciliary body,
the aqueous flow can be reduced,
while the agonist effect on the β2-adrenoceptors is
an increase in flow.
- Carbonic anhydrase isoenzyme II is found in
the ciliary body epithelium and stimulates aqueous
production
Anti glaucoma drugs classification
DRUGS THAT INCREASE AQUEOUS
OUTFLOW
DRUGS THAT REDUCE AQUEOUS
HUMOUR PRODUCTION
Nonspecific Adrenergic Agonists
:epinephrine, dipivefrin
Beta-Blockers : levobunolol, timolol, carteolol,
betaxolol
Parasympathomimetics : pilocarpine,
carbachol,
echothiophate
Alpha-2 Adrenergic Agonists : apraclonidine,
brimonidine
Prostaglandin Analogues : latanoprostCarbonic Anhydrase Inhibitors
:acetazolamide, dorzolamide
Beta-Blockers
1st line therapy for all types of glaucoma
• Good efficacy
• Minimal S/E
Mechanism of action:
Decreases aqueous humor production by blocking
beta2 receptors on ciliary epithelium
TIMOLOL:
• Most widely used ocular Antiglaucoma
• Due to its non selective beta action
Contraindicated in COPD, asthma & heart failure
• Available as 0.5 % solution & gel
S/E:-
• Systemic: Irregular heart rhythm, angina and bronchospasm
• Local:- superficial punctate keratitis, corneal
anesthesia
LEVOBUNOLOL
Levobunolol HCL Drops : Available as 0.5 – 1% solution
S/E:- the same as Timolol
BETAXOLOL
Topical β1 blocker used in
glaucoma
• lesser efficacy in reducing IOP compared to Timolol
• Additional neuroprotective effect.
CARBONIC ANHYDRASE INHIBITORS
2 types
Systemic CA inhibitors:-
Acetazolamide, Methazolamide
Topical CA inhibitors:-
Dorzolamide, Brinzolamide
Mechanism:-
• Blocks CA enzyme reversibly in ciliary body – reduces
aqueous humor production
SYSTEMIC CARBONIC ANHYDRASE
INHIBITORS
DOSAGE:-
Acetazolamide 125mg, 250mg
SIDE EFFECTS:-
High risk of systemic side effects.
Paraesthesias, Kidney stones, aplastic anemia,
Depression, Hypokalemia
TOPICAL CARBONIC ANHYDRASE
INHIBITOR
DORZOLAMIDE:-
• 1st topical CA inhibitor used
• Advantage – not absorbed systemically
• Available as 2 % solution
- local S/E includes corneal edema, allergic reaction,
burning & stinging sensation
BRINZOLAMIDE
• Available as 1% solution
• Better tolerated than dorzolamide – its pH is 7.4
PROSTAGLANDIN ANALOGUES
They include latanoprost, unoprostone,
bimatoprost, travoprost.
Mechanism:-
Decreases IOP by increasing uveoscleral
outflow
PROSTAGLANDIN ANALOGUES
LATANOPROST
• An analogue of PGF2α
• Available as 0.0005% solution, administrated at evening
• Requires refrigeration & protection from sunlight
S/E: – Conjunctival hyperemia , Iris
pigmentation, cystoid macular edema,
changes in eyelash number/color/length/thickness
BIMATOPROST:
• A synthetic prostamide analogue, administrated at evening
• Available as 0.03% solution
• Does not require refrigeration
TRAVAPROST:
• Synthetic PGF2α analogue, administrated at evening
• Available as 0.004% solution,
• Does not require refrigeration/ protection from
sunlight
ADRENERGIC AGONISTS
Includes:
• Non selective – epinephrine & dipivefrin
• Selective alpha2 agonists- Apraclonidine, Brimonidine
ALPHA2 AGONISTS:
Mechanism: Decrease aqueous humor production
APRACLONIDINE:
• Available as 0.5 – 1 %
• Short term use – Post op rise in IOP & adjuvant in
POAG
ADRENERGIC AGONISTS
BRIMONIDINE:
30 times more selective α2 agonist than Apraclonidine
Neuroprotective effect
Available as 0.2 - 0.5% ,
Uses:
- In patients with contraindications to beta
blockers,
-Short term use in post op raise in IOP
CHOLINERGIC AGONISTS
Most commonly used : Pilocarpine eye drops, gel
Mechanism:
Causes contraction of
longitudinal ciliary muscle →
trabecular outflow
Available as 0.5 to 10 % eye drops
Main indication in PACG
Side effects: Superficial punctate keratitis ,
induced myopia, increased risk of retinal
detachment & iritis
Thank you
“Alshadouf”
Mahmoud Said
1897-1964

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Glaucoma medication

  • 1. Glaucoma Medications BY Dr. Amr Mounir Lecturer of Ophthalmology Sohag University
  • 2. Background The aqueous humor is a transparent watery fluid It fills both the anterior and the posterior chambers of the eye Aqueous humor is produced by the ciliary processes The drainage route for aqueous humor flow occurs through two routes 1) Main route: Trabecular meshwork 90% 2) Secondary route: Uveoscleral drainage 10%
  • 3. Background α1-, α2-, β1- and β2-adrenoceptors have been located in the ciliary body. α2- and β2-Adrenoceptors have also been located in the trabecular meshwork - Stimulation of α2-adrenoceptors in the ciliary body, the aqueous flow can be reduced, while the agonist effect on the β2-adrenoceptors is an increase in flow. - Carbonic anhydrase isoenzyme II is found in the ciliary body epithelium and stimulates aqueous production
  • 4. Anti glaucoma drugs classification DRUGS THAT INCREASE AQUEOUS OUTFLOW DRUGS THAT REDUCE AQUEOUS HUMOUR PRODUCTION Nonspecific Adrenergic Agonists :epinephrine, dipivefrin Beta-Blockers : levobunolol, timolol, carteolol, betaxolol Parasympathomimetics : pilocarpine, carbachol, echothiophate Alpha-2 Adrenergic Agonists : apraclonidine, brimonidine Prostaglandin Analogues : latanoprostCarbonic Anhydrase Inhibitors :acetazolamide, dorzolamide
  • 5. Beta-Blockers 1st line therapy for all types of glaucoma • Good efficacy • Minimal S/E Mechanism of action: Decreases aqueous humor production by blocking beta2 receptors on ciliary epithelium
  • 6. TIMOLOL: • Most widely used ocular Antiglaucoma • Due to its non selective beta action Contraindicated in COPD, asthma & heart failure • Available as 0.5 % solution & gel S/E:- • Systemic: Irregular heart rhythm, angina and bronchospasm • Local:- superficial punctate keratitis, corneal anesthesia
  • 7. LEVOBUNOLOL Levobunolol HCL Drops : Available as 0.5 – 1% solution S/E:- the same as Timolol BETAXOLOL Topical β1 blocker used in glaucoma • lesser efficacy in reducing IOP compared to Timolol • Additional neuroprotective effect.
  • 8. CARBONIC ANHYDRASE INHIBITORS 2 types Systemic CA inhibitors:- Acetazolamide, Methazolamide Topical CA inhibitors:- Dorzolamide, Brinzolamide Mechanism:- • Blocks CA enzyme reversibly in ciliary body – reduces aqueous humor production
  • 9. SYSTEMIC CARBONIC ANHYDRASE INHIBITORS DOSAGE:- Acetazolamide 125mg, 250mg SIDE EFFECTS:- High risk of systemic side effects. Paraesthesias, Kidney stones, aplastic anemia, Depression, Hypokalemia
  • 10. TOPICAL CARBONIC ANHYDRASE INHIBITOR DORZOLAMIDE:- • 1st topical CA inhibitor used • Advantage – not absorbed systemically • Available as 2 % solution - local S/E includes corneal edema, allergic reaction, burning & stinging sensation BRINZOLAMIDE • Available as 1% solution • Better tolerated than dorzolamide – its pH is 7.4
  • 11. PROSTAGLANDIN ANALOGUES They include latanoprost, unoprostone, bimatoprost, travoprost. Mechanism:- Decreases IOP by increasing uveoscleral outflow
  • 12. PROSTAGLANDIN ANALOGUES LATANOPROST • An analogue of PGF2α • Available as 0.0005% solution, administrated at evening • Requires refrigeration & protection from sunlight S/E: – Conjunctival hyperemia , Iris pigmentation, cystoid macular edema, changes in eyelash number/color/length/thickness
  • 13. BIMATOPROST: • A synthetic prostamide analogue, administrated at evening • Available as 0.03% solution • Does not require refrigeration TRAVAPROST: • Synthetic PGF2α analogue, administrated at evening • Available as 0.004% solution, • Does not require refrigeration/ protection from sunlight
  • 14. ADRENERGIC AGONISTS Includes: • Non selective – epinephrine & dipivefrin • Selective alpha2 agonists- Apraclonidine, Brimonidine ALPHA2 AGONISTS: Mechanism: Decrease aqueous humor production APRACLONIDINE: • Available as 0.5 – 1 % • Short term use – Post op rise in IOP & adjuvant in POAG
  • 15. ADRENERGIC AGONISTS BRIMONIDINE: 30 times more selective α2 agonist than Apraclonidine Neuroprotective effect Available as 0.2 - 0.5% , Uses: - In patients with contraindications to beta blockers, -Short term use in post op raise in IOP
  • 16. CHOLINERGIC AGONISTS Most commonly used : Pilocarpine eye drops, gel Mechanism: Causes contraction of longitudinal ciliary muscle → trabecular outflow Available as 0.5 to 10 % eye drops Main indication in PACG Side effects: Superficial punctate keratitis , induced myopia, increased risk of retinal detachment & iritis