Pharmacotherapy of
Eye Conditions
Dr. Marissa Balmith
[email protected] 1
ASSESSMENT OUTCOMES
• Distinguish between open and closed-angle
glaucoma and
• Discuss the iatrogenic causes of glaucoma
• Discuss the pharmacology of drugs used for
glaucoma
• Discuss and classify the drugs used for
treating bacterial and allergic conjunctivitis
2
ANATOMY OF THE EYE
GENERAL ASPECTS
• The eye is protected by a series of barriers
• Blood-ocular barrier comprises:
• Blood-aqueous barrier
• Blood-retinal barrier
• These barriers help maintain the proper
environment for the eye by regulating the
exchange of substances between the blood
and the ocular tissues
GENERAL ASPECTS
These barriers represent:
• An opportunity for localised drug administration
• A challenge to drug delivery
• The lacrimal gland has both sympathetic and parasympathetic
innervation
MAJOR ROUTES OF OCULAR ADMINISTRATION
• Eye drops
• Rapidly eliminated from lacrimal sac (frequent administration)
• Volume of conjunctival sac less than one drop – wasteful to instil more than one drop at a
time
• Do not squeeze after administration – will eliminate fluid from sac
• More than one drug? – allow 5 mins in between to prevent overflow/dilution
MAJOR ROUTES OF OCULAR ADMINISTRATION
• Eye ointments
• Retained for longer – more sustained absorption
• S/E: blurring of vision 10 – 15 mins after application (preferred overnight or when eye is to be
covered)
• More than one product? – eye drop first; ointment 10 mins later
MAJOR ROUTES OF OCULAR ADMINISTRATION
• Subconjunctival injection (preferably by ophthalmological specialists)
• During serious intra-ocular inflammation (anti-inflammatories, glucocorticoids and mydriatics)
• High intraocular concentrations (bypasses conjunctival and corneal barriers)
• Volume usually restricted to 1 mL
PREVENTION OF MICROBIAL CONTAMINATION
• Eye preparations should be sterile when issued in patients
• May be used for one month after opening (thereafter assumed to be contaminated)
• Avoid touching eyelashes or surface of the eye with container tip
• Preparations from the same container should not be administered to different patients
• Single-dose containers preferred to multi-dose (e.g. fluorescein)
• NB: corneal abrasions are natural portals to infection
• Also note: preservatives (e.g., benzalkonium chloride) toxic to corneal epithelium and may be
absorbed by soft contact lenses)
AUTONOMIC OCULAR PHARMACOLOGY
#Parasympathetic stimulation:
• Muscarinic agonists – e.g. carbachol,
pilocarpine
• Cholinesterase inhibitors – e.g. neostigmine,
physostigmine
*Parasympathetic blockade:
• Muscarinic antagonists – e.g. atropine,
tropicamide
*Sympathetic stimulation
• e.g. phenylephrine
# Sympathetic blockade
• e.g. phentolamine
*Mydriasis
#Miosis
M3 – muscarinic receptor
DRUGS COMMONLY USED TO DILATE THE PUPIL
alpha-1 adrenergic receptors
GLAUCOMA
GLAUCOMA
• Open Angle Glaucoma
• Most frequent type of human glaucoma
• Drainage angle formed by the iris and cornea
remains open
• But other parts of the drainage system don't
drain properly
• Elevated intraocular pressure (IOP), cupping
and atrophy of the optic nerve head, and typical
visual field defects
• No specific ocular abnormalities or systemic
diseases causing the glaucoma
• Risk factors: increased IOP, advanced age,
racial background (African and Hispanic
ancestry), decreased corneal thickness, positive
family history
GLAUCOMA
• Closed angle glaucoma
• Acute Angle-Closure Glaucoma
• Sudden onset (ophthalmic emergency)
• If not properly diagnosed and treated,
progressive and permanent ocular damage
occurs in a matter of hours to days
• Sudden onset of pain, redness of the eye,
and blurred vision
• Nausea, vomiting, and profuse sweating
(may lead to improper diagnosis
• Chronic Angle-Closure Glaucoma
• Results from obstruction of the anterior
chamber angle by iris tissue, without an
obvious underlying ocular or systemic cause
IATROGENIC CAUSES OF GLAUCOMA
Class discussion:
When considering benzodiazepines, why
is it important for dentists to know that it
could cause acute angle-closure
glaucoma?
Fig. 13.5: Chapter 13;
Rang&Dale Pharmacology
GLAUCOMA TREATMENT:
PROSTAGLANDINS - TOPICAL
• Latanoprost, travoprost
• Prostaglandin F2α analogues
• First line therapy for open angle glaucoma
• Reduces intra-ocular pressure by increasing uveoscleral aqueous outflow
• Can be used in patients intolerant to β-blockers or as add on therapy when
the response to initial therapy is inadequate
• Main side-effects:
• local irritation, stinging, burning and blurred vision,
• eyelid pigmentation,
• eye lash growth,
• iris pigmentation (brown)
GLAUCOMA TREATMENT: ALPHA2-
AGONISTS - TOPICAL
• Sympathomimetic – Brimonidine, Apraclonidine - Selective α2 agonists, used
for chronic open glaucoma when other drugs are unsatisfactory
• Decrease the rate of aqueous humor production
• Alone or as adjunct to β-blocker therapy in chronic glaucoma
• Major side-effects:
• local ocular irritation
• occasional corneal staining
• Systemic S/E: dry mouth, headache, fatigue, drowsiness and allergic reactions
• Contraindicated in patients taking monoamine oxidase inhibitors (MAOIs)
• Should be used with caution in those with coronary artery disease (CAD) or
tricyclic antidepressants
GLAUCOMA TREATMENT: BETA2
ANTAGONISTS - TOPICAL
• Timolol, betaxolol, levobunolol – B2 selective antagonists
• Blocks beta-2 adrenergic receptor in the ciliary epithelium - lowers IOP by
decreasing aqueous humor production
• Main side-effects:
• Blurred vision or other change in vision
• Stinging of the eye
• Swelling, irritation or inflammation of eye or eyelid
• Systemic S/E: headaches, bradycardia, arrhythmia, bronchospasm
• Contradictions:
• Asthmatic patients (bronchoconstriction)
GLAUCOMA TREATMENT: CARBONIC
ANHYDRASE INHIBITORS - TOPICAL
• Dorzolamide
• Inhibits carbonic anhydrase enzyme on ciliary body epithelium
• Reduces the formation of bicarbonate ions
• Reduces fluid transport
• Decreases aqueous humor production - lowers intra-ocular pressure
• Used alone or as an adjunct to a β-blocker
• Systemic absorption and side effects – e.g. rashes and urolithiasis (may require
drug withdrawal)
• Adverse effects:
• local irritation of the eye and eyelid,
• stinging,
• visual blurring and
• bitter taste
GLAUCOMA TREATMENT: CARBONIC
ANHYDRASE INHIBITORS - SYSTEMIC
• Acetazolamide (Diamox) - Carbonic anhydrase inhibitor used in open angle
and closed angle glaucoma – Sulphonamide
• Competitive inhibitor of carbonic anhydrase (enzyme that converts CO2 and H2O
into H2CO3 , carbonic acid) - on ciliary body epithelium
• Reduces the formation of bicarbonate ions
• Reduces fluid transport
• Decreases the production of aqueous humor - lowers intra-ocular pressure
• Adverse effects (poorly tolerated orally):
• Paresthesia and tingling
• Nausea, vomiting and loss of taste
• Metabolic acidosis
• Polyuria due to its mild diuretic properties
• Hypersensitivity reactions
• Bone marrow suppression (rare)
CONJUNCTIVITIS –
PHARMACOTHERAPY CLASSIFICATION
Conjunctiva becomes inflamed and red
• Often starts in one eye and spreads to the other eye
• Often caused by bacteria, viruses, allergies, or foreign bodies
Assessment and management:
• viral conjunctivitis: resolves on its own - symptomatic relief
• bacterial conjunctivitis: topical antibiotic
• allergic conjunctivitis: topical antihistamine
BACTERIAL CONJUNCTIVITIS –
PHARMACOTHERAPY
ALLERGIC CONJUNCTIVITIS –
PHARMACOTHERAPY
Antihistamines and mast cell stabilisers
Indication: Allergic or seasonal conjunctivitis
• Antazoline and azelastine (S/E: ocular irritation, oedema of eyelids or
blurred vision can occur)
• Sodium chromoglicate or nedocromil – long-term treatment of allergic
conjunctivitis (S/E: local stinging)
• NSAIDs used to reduce post-operative inflammation - diclofenac,
flurbiprofen and ketorolac
Glucocorticoids
• Topical GCs should only be used under specialist supervision to treat
uveitis and scleritis
• Should never be used to treat undiagnosed red-eye as it can
aggravate infection
• Hydrocortisone, betamethasone (drops and ointment)
THANK YOU
