ANTI GLAUCOMA

ALPHA AGONIST

• Classifications
• 1. Both alpha and beta-receptor stimulators (epinephrine)
• 2. Direct alpha-adrenergic stimulators (norepinephrine and clonidine hydrochloride)
• 3. Indirect alpha-adrenergic stimulators (pargyline)
• 4. Beta-stimulator (isoprotereol)
 MOA

• 1. Increased aqueous outflow results by virtue of both alpha and beta-receptor stimulator
• 2. Decreased aqueous humour production occurs due to stimulation of alpha receptors in the
ciliary body
 SIDE EFFECTS

• Local SE:
• Burning sensation , Reactive hyperaemia of conjunctiva , Conjunctival pigmentation , Allergic
blepharoconjunctivitis , Mydriasis , Cystoid macular oedema (in aphakics)

• Systemic SE
• Hypertension , Tachycardia , Headache , Palpitation , Tremors , Nervousness , Anxiety
 EPINEPHRINE

• Indications:
• It is one of the standard drugs used for the management of Primary Open-Angle Glaucoma (POAG)
• It is also useful in most of the secondary glaucoma

• Contraindications:
• Absolute (none) ,
• Relative ❖ Hypersensitivity ❖ Closed-Angle Glaucoma ❖ Increased teratogenic in pregnancy
(Drug category C) ❖ Oppose action of oxytocin ❖ Delay labour
 DIPIVEFRINE
• Act as prodrug to epinephrine
• Dipivetrin converted to epinephrine = decrease aqueous production, increase outflow
• It is more lipophilic the epinephrine and thus its corneal penetration is increased by 17 times

• Indications:
• Decrease IOP
• Chronic Open-Angle Glaucoma (COAG)
• Patient not responding other anti-glaucoma

• Contraindications:
• In patient with narrow angle because dilatation pupil cause angle-closure attack
• Develop hypersensity
 CLONIDINE HYDROCHLORIDE
• It is a centrally-acting systemic antihypertensive agent
• Shown to lower the IOP by decreasing aqueous humour production by stimulation of alpha-receptors in the
ciliary body

• Indications:
• Prophylactic management of migraine or recurrent vascular headache

• Contraindications:
• Severe brady-arrhythmia - Secondary to sick-sinus syndrome - Second (2nd) degree AV block , Third (3rd)
degree AV block
 BRIMONIDINE (0.2%)
• Selective alpha-2 adrenergic agonist
• Decreasing aqueous production, enhancing blockers = lowers IOP

• Indications:
• Open-Angle Glaucoma ocular hypertension
• In patient with contraindication to beta-blocker
• Adjunctive therapy

• Contraindications:
• Hypersensitivity
• Neonates and infants
• Patient on monoamine oxidase inhibitor (MOA-i), antidepressant (affect noradrenergic trasmission)
 APRACLONIDINE

• Like brimonidine
• An extremely potent ocular hypotension drug
•
• Indications - Commonly used prophylactically for prevention of IOP elevation following laser trabeculoplasty,
YAG laser iridotomy and posterior capsulotomy

• Contraindications
• History of severe / unstable cardiovascular (CVS) disease
• With MAO-I, antidepressant
• Hypersensitivity
 BETA-BLOCKERS
• Beta-blockers reduce IOP by decreasing aqueous production, mediated by an effect on the ciliary
epithelium.
• Beta-blockers should not be instilled at bedtime as they may cause a profound drop in blood
pressure while the individual is asleep, thus reducing optic disc perfusion and potentially causing
visual field deterioration;
• However, a beta-blocker may be preferred under some circumstances such as monocular
treatment to avoid the cosmetic disadvantage of the asymmetrical periocular skin darkening
and/or conjunctival hyperaemia with prostaglandins.
• Beta-blockers are also preferred in conditions such as ocular inflammation and cystoid macular
oedema, or where there is a history of herpes simplex keratitis.
 MOA

• beta blockers in the heart helps reduced cardiac output and heart rate thus lowering the blood
pressure. However, the exact mechanism of action for beta blocker in the eye is unknown
however studies shown that it might help to redue aqueous humour production by reducing the
blood supply supplying the ciliary body.
 SIDE EFFECTS

• Ocular - Ocular side effects are few but include allergy and punctate keratitis. Granulomatous uveitis has been reported
with metipranolol
• Systemic
• ○ Bronchospasm. This may be fatal in asthma or other reversible airways disease, and it is critical to exclude a history of
asthma before prescribing a beta-blocker.
• ○ Cardiovascular. Effects include heart block, bradycardia, worsening of heart failure and hypotension, induction of the
latter by topical beta-blocker having been reported as a common cause of falls in elderly patients. A peripheral
vasoconstrictive effect means that they should be avoided or used with caution in patients with peripheral vascular disease
• ○ Unpleasant but less severe side effects include sleep disorders, reduced exercise tolerance, hallucinations, confusion,
depression, fatigue, headache, nausea, dizziness, decreased libido and dyslipidaemia.

* Systemic effects from eye drops can be reduced by occlusion of the punctum (finger pressed on the caruncle,which can be
felt as a lump at the inner canthus of the eye) or shutting the eyes for several minutes after putting in the drops. *This
reduces the lacrimal pumping mechanism and stops the eyedrops running down the lacrimal passages and being absorbed
systemically via the nasal mucosa or by inhalation directly into the lungs. This may also enhance ocular absorption of the
drugs.
 CARBONIC ANHYDRASE INHIBITORS (CAIS)

• Systemic drugs (oral): Diamox (acetazolamide) and Neptazane® (methazolamide) Topical drugs
(drops): Trusopt® (dorzolamide), Azopt® (brinzolamide) – minimal side effects

• Mode of Action : Inhibition of carbonic anhydrase enzyme (isoenzyme II) from non-pigmented
ciliary body epithelium by CAIs in local tissues reduces the formation of bicarbonate ions (HCO-
3) which decrease secretion of aqueous humour production and thus reducing fluid transport and
IOP.
 PROSTAGLANDINS

• Mode of action: Enhancement of uveoscleral aqeous outflow

• Types of prostaglandin :
• Latanoprost
• Travoprost
• Bimatoprost – have a greater IOP lowering effect than the other PG agents.
• Tafluprost – newer prostaglandin derivitative
 SIDE EFFECTS

• Ocular :
• Conjunctival hyperaemia – very common
• Eyelash lengthening, thickening, hyperpigmentation and occasionally increase in number.
• Irriversible iris hyperpigmentation.
• Hyperpigmentation of periocular skin is common but reversible.
• Preoperative use of prostaglandin agents may increase the likelihood of cystoid macular edema following cataract
surgery.
• Anterior uveitis is rare but PG should be used with caution in inflamed eyes.
• Promotion of herpetic keratitis can occur, so PG should be used with caution in patients with a history of condition

• Systemic :
• Occasional headache
• Precipitation of migraine in susceptible individuals • Malaise • Myalgia • Skin rash • Mild upper respiratory tract
symptoms
CONTRAINDICATIONS OF PROSTAGLANDINS

• Issues to consider when starting prostaglandin analogues:

• Is there active inflammation in the eye or a history of ocular inflammation?
• Is there a history of macular edema?

- The prostaglandin groups of drugs are relatively contraindicated in the presence of uveitis and are
not recommended in children with any active uveitis.