DRUGS ACTING ON EYE

BY MAI SAID SHOELA UNDER SUPERVISION OF PRF. DR. SAFAA EL REWANY PROFESSOR OF PHARMACOLOGY FACULTY OF MEDICINE UNIVERSITY OF ALEXANDRIA

OBJECTIVES
LIST MAIN GROUPS OF DRUGS APPLIED ON THE EYE AND THEIR CLINICAL APPLICATIONS

DISCUSS THE LOCAL EFFECTS OF AUTONOMIC DRUGS ON THEIR RECEPTOR SITES IN THE EYE WITH RELEVANCE TO THEIR CLINICAL APPLICATIONS

IDENTIFY THE LINES OF TREATMENT OF SOME EYE DISEASES AS GLAUCOMA AND CONJUNCTIVITIS

STRUCTURE OF THE EYE

ANATOMICALLY EYE COMPOSED OF

ANTERIOR CHAMBER

POSTERIOR CHAMBER

ANTERIOR CHAMBER OF EYE

INCLUDES

CORNEA

IRIS

LENS

AQUEOUS HUMOUR

THE CORNEA
CORNEAL OR CONJUNCTIVAL REFLEX
Cornea & sclera are supplied by sensory nerves When the cornea is touched, corneal reflex is initiated i.e. the eye blinks on touching the cornea with a piece of cotton

DRUGS ACTING ON CORNEA

INCLUDES
LOCAL ANAESTHETICS DIAGNOSTIC DYES

TOPICAL ANTI-INFLAMMATORY

TOPICAL ANTI-INFECTIVE DRUGS

TEAR SUBSTITUTES LUBRICATING AGENTS

LOCAL ANAESTHETIC DRUGS

INCLUDES: 1. Surface anesthesia eye drops for :
a. Tonometry: measurement of IOP b. Removal of corneal foreign bodies

2. Infiltration anesthesia :
Removal of cataracts

DIAGNOSTIC DYES
Fluorescein 1%
Used for diagnosis of corneal ulcers Denuded epithelium is stained bright green

Rose Bengal 1%
Used for diagnosis dry eye Dead cells are stained red

TOPICAL ANTIINFLAMMATORY DRUGS

INCLUDES 1. Steroidal anti-inflammatory drug

Used for inflammation of anterior segment of eye as allergic conjunctivitis

2. Non-steroidal anti-inflammatory drugs

Have anti-prostaglandins action Example: Ketophenac sodium

TOPICAL ANTI-INFECTIVE DRUGS

INCLUDES

TOPICAL ANTI-BIOTICS

TOPICAL ANTIFUNGAL

TOPICAL ANTIVIRAL AGENTS

NEOMYCIN CHLORAMPHENICOL FLUOROQUINOLONES

NYSTATIN SOLUTION

ACYCLOVIR FOR DENDRITIC CORNEAL ULCER

TEAR SUBSTITUTES AND LUBRICATING AGENTS

EXAMPLE
1. Methyl cellulose 2. Polyvinyl alcohol

USES
1. Formation of artificial tears in dry eye conditions as Sjogrens syndrome 2. Contact lens solution

THE IRIS
MUSCLES

SPHINCTER PUPILLAE MUSCLE PARASYMPATHETIC M3 RECEPTOR

DILATOR PUPILLAE MUSCLE SYMPATHETIC ALPHA 1 RECEPTOR

LIGHT REFLEX
PRINCIPLE
Narrowing of pupil (miosis) when the eye is stimulated by light This miosis is due to contraction of constrictor pupillae muscle i.e. light reflex depends on integrity of parasympathetic supply of the eye Parasympatholytics abolish light reflex

THE LENS
ACCOMODATION REFLEX

It is the ability to increases the convexity of the crystalline lense to obtain a clear image of an object at various distances This is mediated through the parasympathetically innervated ciliary muscle, whose contraction causes suspensory ligaments relaxation thus increasing the lense curvature and diopteric power leading to accomodation for near vision

THE AQUEOUS HUMOUR

It is formed of highly vascularized ciliary body processes that absorb sodium selectively via carbonic anhydrase enzyme(70%) and ATPase system The aqueous humour circulates through the pupil and is drained in the canal of Schlemm then to episcleral veins Normally there is balance between aqueous homour formation and outflow and this keeps intraocular pressure within normal range (1021mmHg)

CHANGES IN PUPIL SIZE

MIOSIS

NORMAL PUPIL

MYDRIASIS

AUTONOMIC DRUGS ACTING ON THE EYE

INCLUDES

MIOTICS

MYDRIATICS

MIOTICS
INCLUDES

PARASYMPATHO MIMETICS

SYMPATHOLYTICS

MORPHINE

AS GUANETHIDINE

BY STIMULATION OF EDINGER WESTEFAL NUCLEUS

PARASYMPATHOMIMEYICS
MECHANISM OF ACTION
They stimulate M3 receptors in ciliary muscle and constrictor pupillae muscle leading to: a. Miosis: constriction of the pupil b. Accomodation for near vision c. Reduce intraocular pressure: as when the pupil is constricted, the anterior chamber angle is widened and this facilitates the drainage through Canal of Schlemm

PARASYMOATHOMIMETICS

INCLUDES

CHOLINESTERS

CHOLINOMIMETIC ALKALOIDS

ANTICHOLINESTERASES

CHOLINOMIMETIC ALKALOIDS

Pilocarpine 2%

PARASYMATHOMIMETICS

PUPIL SIZE: MIOSIS LIGHT REFLEX: ABSENT ACCOMODATION: FOR NEAR VISION IOP: REDUCED CONJUNCTIVAL BV: CONGESTED

MYDRIATICS
CAUSE

PASSIVE MYDRIASIS

ACTIVE MYDRIASIS

PARASYMPATHO LYTICS

SYMPATHOMIMETICS

COCAINE

PARASYMPATHOLYTICS Paralysis of sphincter pupillae muscle PUPIL SIZE: LIGHT REFLEX: ACCOMODATION: IOP:
Mydriasis (Passive) ABSENT

Lost for near vision

Increased in susceptible people only

PARASYMPATHOLYTICS
INCLUDES

ATROPINE 1% LAST FOR 7-10 DAYS

ATROPINE SUBSTITUTES

HOMATROPINE 2% FOR >24 hrs

CYCLOPENTOLATE 1% for 1 day TROPICAMIDE 1% for 6hrs

PARASYMPATHOLYTICS

THERAPEUTIC USES
1. Fundus examination & diagnosis of refractory errors 2. To break recent adhesions between the iris & lens in anterior uveitis 3. Treatment of acute iritis & iridocyclitis as they relief pain resulting from cilliary muscle spasm

SYMPATHOMIMETICS
MECHANISM OF ACTION

They produce active mydriasis by sympathetic nerve fibers that are motor to radial muscle through action on 1 receptor They do not affect light reflex or accommodation

They are vasoconstrictors so the reduce vascular congestion of conjunctival BVs

EXAMPLE
Ephedrine sulphate, Phenylephrine & Dipivefrin

COCAINE
MECHANISM OF ACTION
1. It produces active mydriasis as it potentiates sympathetic response by: Decreasing re-uptake of released catecholamines 2. It preserves light reflex 3. Abolishes corneal reflex by its local anesthetic action

CONJUNCTIVITIS
INCLUDES

BACTERIAL CONJUNCTIVITIS

ALLERGIC CONJUNCTIVITIS

BACTERIAL CONJUNCTIVITIS
DEFINITION
IT IS INFLAMMATION OF THE CONJUNCTIVA ASSOCIATED WITH MUCOPURULENT DISCHARGE, REDNESS AND EYELIDS EDEMA

MANAGEMENT
INCLUDES

EYE LOTIONS

HOT FOMENTS

ASTRINGENT EYE DROPS

TOPICAL ANTIMICROBIAL AGENTS

To wash off the discharge Example: Bland eye lotions Boric acid lotion 4%

EYE LOTIONS

Are applied locally in order to relief edema and pain

HOT FOMENTS

Local eye drops every 1-2hrs/day & eye ointment at night Example: Neomycin, tobramycin

TOPICAL ANTIMICROBIAL AGENTS

ALLERGIC CONJUNCTIVITIS
DEFINITION
IT IS ACUTE ALLERGY DUE TO EXPOSURE TO ALLERGEN . THE PATIENT PRESENT WITH REDNESS OF EYES WITH ITCHING AND LACRIMATION

MANGEMENT
INCLUDES

TREATMENT OF ACUTE ATTACK

PROPHYLACTIC TREATMENT

ANTI-HISTAMINIC EYE DROPS

GLUCOCORTICOID EYE DROPS

MAST CELL STABILIZERS

ANTI-HISTAMINIC EYE DROPS

Example: Levocabastine Antazoline (+)

GLUCOCORTICOIDS EYE DROPS

Precaution: We must exclude viral dendritic ulcer & glaucoma

MAST CELL STABILIZERS

Example: Na cromoglycate

GLAUCOMA
DEFINITION
IT IS A GROUP OF DISEASES THAT HAVE IN COMMON A CHARACTERISTIC OPTIC NEUROPATHY WITH ASSOCIATED VISUAL FIELD LOSS FOR WHICH THE ELEVATED INTRAOCULAR PRESSURE IS ONE OF PRIMARY RISK FACTORS

CLASSIFICATION
INCLUDES

CLOSED-ANGLE GLAUCOMA

OPEN-ANGLE GLAUCOMA

CLOSED-ANGLE GLAUCOMA
It

is associated with a shallow anterior chamber

Acute & painful rise of IOP is often precipitated that must

be controlled on an emergency basis with drugs or prevented by iridectomy

OPEN-ANGLE GLAUCOMA
Outflow of AH through the trabecular meshwork-Schlemms canal venous system is impaired It is a chronic condition treated medically,

aiming to slow the rate of disease progression to prevent significant visual impairment

MEDICAL MANAGEMENT OF GLAUCOMA

INCLUDES

-BLOCKERS

DIURETICS

SYMPATHOMIMETICS

PROSTAGLANDIN ANALOGUES

PARASYMPATHOMIMETICS

- BLOCKERS
MECHANISM OF ACTION
Timolol blocks beta receptors on the cilliary NON-SELECTIVE processes resulting in decreasing aqueous BLOCKERS production It is treatment of choice in open-angle glaucoma
TIMOLOL MALEATE TOPICAL EYE DROPS

INCLUDES

DIURETICS
INCLUDES

HYPER CARBONIC OSMOTIC inhibit carbonic anhydrase in the ANHYDRASE They by withdrawing fluid from the eye It acts AGENTS INHIBITORS

MECHANISM OF ACTION OF MECHANISM OF ACTION OF CARBONIC ANHYDRASE AGENTS HYPEROSMOTIC INHIBITORS

cilliary body, which prevents bicarbonate and reducing vitreous volume synthesis resulting in a fall in Na transport and aqueous flow ACETAZOLAMIDE
ORAL I.V IN EMERGENCY

MANNITOL I.V

DORZOLAMIDE TOPICAL EYE DRPS

SYMPATHOMIMETICS
MECHANISM OF ACTION OF INCLUDES AND AGONISTS MECHANISM OF ACTION OF 2 AGONIST It lowers the IOP by a balance between and adrenoreceptors stimulation AND 2 1.1. It reduces VC of the cilliary BVs will mediated AH production AGONIST AGONISTS

DIPIVEFRIN HCL BRIMONIDINE TARTRATE CONTRAINDICATION TOPICAL EYE DROPS TOPICAL EYE DROPS

decrease the aqueous flow 2. It increases uveoscleral outflow (secondary 2. 2 mediated aqueous outflow 20%) pathway for effect will increase trabecular meshwork drainage Angle-closed glaucoma

PROSTAGLANDIN ANALOGUES (F2)

Latanoprost : topical eye drops

MECHANISM OF ACTION
1. It enhances the uveoscleral outflow of the aqueous 2. It increases blood flow to the optic nerve that may contribute in retinal neuroprotection

PARASYMPATHOMIMETICS
Pilocarpine HCL: topical eye drops or gel

MECHANISM OF ACTION
It increases aqueous outflow by widening of the trabecular meshwork
SIDE EFFECTS
Blurred vision and ache over the eye

DRUGS CONTRAINDICATED IN GLAUCOMA

Topical & systemic corticosteroids due to the possible increase in trabecular meshwork inducible glucocorticoid response (TIGR) gene expression as an assumed mechanism for outflow obstruction
Strong vasodilators as nitrites as they may Increase aqueous humour formation Cycloplegic drugs as atropine