Drugs and the eye

By Amos Massele

Introduction
The eye is the window of the soul The eyes are undoubtedly the most sensitive and delicate organs we possess, and perhaps the most amazing They present us with the window through which we view the world, and are responsible for four fifths(80%) of all the information our brain receives which is probably why we rely on our eyesight more than any other sense

some eye disorders

The eye works like a Camera

Innervations of the eye

Parasympathetic Sympathetic

Eye parts of pharmacological interest

The ciliary body is composed of ciliary muscles & ciliary process The ciliary body serves 2 functions - Secretion of aqueous humor - Accomodation - Parasympathetic stimulation contracts the ciliary muscles allowing the lens become convex focusing on near objects and vice versa - Contraction of ciliary muscles also widens the spaces in trabecular meshwork lowering intaocular pressure in Glaucoma

Important general pharmacokinetics of intraocular drug administration

Most drugs are delivered as drops in aqueous solution Formulations which prolong contact time include gels, ointments, solid inserts,soft contact lenses,collagen shields etc Drug penetration into the eye is approx. linearly related to the concentration of the drug Nasolacrymal drainage plays a key role in the systemic absorption of drugs administered to the eye Drugs administered by this route bypass the liver and avoid first pass effect". Ocular drugs like Beta adrenergic antagonist(

I: Drugs used to dilate the pupil(mydriatics)

Mydriasis (pupilary dilatation) required to examine the retina (fundoscopy) Two major groups of drugs are used to dilate the pupil are: (A)anticholinergics(Muscarinic antagonists/parasympatholytics) eg.tropicamide( eye drops) short acting , facilitate retinal examination (B) Sympathomimetics like adrenaline and phenylephrine EYE DROPS

 Cyclopentolate and atropine (anticholinergics)eye drops are preferred for producing cycloplegia(paralysis of the cilliary muscle) Refer to table 1& 2 below

Table 2:Drugs commonly used to dilate the pupil

Drug (I) Anticholinergics - Tropicamide - Cyclopentolate - Atropine (II)Sympathomimetics ---Adrenaline Phenylephrine receptor All are antagonists at M3 receptor, on ciliary muscle may induce blurred vision,sytemic absorption may occur -do- doall are agonist at 1 on radial muscle of iris one or two drops 1% soln. one or two drops 10% soln. systemic absorption +

Dipivefrin

one or two drops 0.3 % soln. read more on this

Table 1: receptors
Tissue - adrenergic receptor - response
Iris radial muscle Iris sphincter muscle Ciliary epithelium Ciliary muscle Lacrimal gland 1 2/2 2 1 mydriasis aqeous humour production relaxation secretion

-do Iris radial muscle Iris sphincter muscle Ciliary epithelium Ciliary muscle Lacrimal gland

Cholinergic receptor -doM3 M3 M2/M3 Miosis accommodation secretion

Nursing implications
Instruct client who has received a mydriatic to wear dark sunglasses until clear vision resumes Teach the client proper instillation

2.0 Drugs used to constrict the pupil (miotics)

Actions: exert a parasympathetic response (stimulate the parasympathetic NS) resulting in: constriction of the pupil Contraction of the accommodation muscle Decrease resistance to outflow of aqeuous humour

Drugs to treat glaucoma- drugs which constrict the pupil

Aqueous humor(AH) is produced at a rate of 2-2.5L/min & flows from posterior chamber Then flows via the trabecular meshwork into canal of Shlemm and eventually into episcleral venous plexus and eventually into systemic circulation Fluid can also flow via the ciliary muscles into suprachoroid space

Therapeutic outcomes of miotics

Decrease intraocular pressure Increase outflow of aqueous humour Of benefit in the treatment of open angle glaucoma

Nursing implications of caring for a patient on miotics

Administer at bed time to decrease blurred vision Avoid in conjuctivitis Teach client how to administer Common miotic drugs include Pilocarpine and Carbachol

3 : other drugs used to treat glaucoma

Mannitol: Osmotic diuretic Used in emergency before surgery Given IV infusion Shifts water from intracellular & transcellular compartments (including the eye) into the plasma Promotes fluid loss by its diuretic action on the kidney Its major Adverse effect is dehydration

Carbonic anhydrase inhibitors Acetazolamide Useful in acute & chronic glaucoma A competitive inhibitor of Carbonic anhydrase (CA) enzyme CA converts CO2 & H20 into H2CO3 Inhibition of this enzyme in the eye reduces aqueous humor production Revise your notes on diuretics

Acetazolamide--- Adverse effects include: - nausea,vomiting,loss of taste - Paraesthesia - Metabolic acidosis - Polyuria due to mild diuretic effect Pharmacokinetics: - Well absorbed orally - Low plasma binding - Half life is 8h eliminated by renal - A slow release preparation is available for twice daily dosing - Acetazolamide is contraindicated in renal failure,renal stones & in pregnancy

Topical agents used in glaucoma

Dorzolamide
Is a sulphonamide derivative Acts as a topical CA inhibitor
May be used alone or as adjunct to a -antagonist

like timolol May show systemic absorption with rashes, Adverse effects include local irritation to the eye with burning sensation,visual blurring etc

Latanoprost Is a PGF2 analogue

Latanoprost can be used in patients who are intolerant to antagonists like timolol It lowers intraocular pressure by increasing uveoscleral outflow

Selective 2 agonists
Brimonidin: Is recently introduced for the treatment of chronic open-angle glaucoma when other drugs do not respond adequately Is used alone or as an adjunct with blocker like timolol It decreases AH by increasing uveoscleral outflow

Selective 2 agonist --------Apraclonidine: Is a derivative of clonidine Is another selective Selective 2 agonist If formulated for ophthalmic use

Nursing implications
Carbonic anhydrase inhibitors and osmotic diuretics like mannitol are diuretics and will increase urine output Monitor electrolytes and advise patient to take early in the morning Beta blockers like timolol ,monitor heart rate Teach client how to administer

5:Drugs for eye infections

Antibacterial agents are formulated for ophthalmic use see table below: Drug broad spectrum antibiotics. Chloramphenicol Fluoroquinolones (Eg.Ciprofloxacin) Framycetin sulphate Aminoglycoside Appropriate antibiotic will depend on C/S of the eye discharge

Drugs and eye infections----- Please note that: Acute bacterial conjunctivitis is usually caused by Staphylococcal aureus or streptococcus All below drug may be applied as eye drops against (ie.Chloramphenicol,gentamicin,fusidic acid or fluoroquinolnoes(ciprofloxacin).

VI:Drugs and inflammatory disorders of the eye

Corticosteroids Topical use must be given under specialist supervision Should never be used to treat undiagnosed red eye which could be due to herpes infection which aggravates the condition and even lead to blindness. In glaucoma steroids exacerbate glaucoma Thus steroids require expertise in their use against eye disorders Preparations available include: hydrocortisone or betamethasone eye drops/ointment

6 :Drugs for inflammatory disorders of the eye

Antihistamines& Mast cell stabilizers: These are used to treat allergic or seasonal conjunctivitis Topical antihistamine preparations for ophthalmic use include: - Antazoline & levocabastine - They may cause eye irritation with edema of eyelids,blurred visison,sytemic effects may occur with drowsiness

Drugs for inflammatory disorders of the eye

Sodium chromoglycate or nedocromil eye drops are widely used in the long term treatment of allergic conjuctivitis Sodium chromogycate is very safe causing only mild stinging as its ADR Lodoxamide causes itching and lacrimation and flushing A new drug Olopatidine is another mast cell stabilizer under scrutiny

7: Local anesthetics for the eye

Amethocaine & Oxybuprocaine are widely used as topical LA Proxymetacaine is used in pediatrics as it causes less stinging Amethocaine causes profound local anesthesia and is suitable for minor surgical procedures Oxybuprocaine lignocaine plus fluorescein is used in tonometry Lignocaine adrenaline is often injected into the eyelid for minor surgery

Adverse effects on the eye of systemic drug therapy

Stevens-Johnson Syndrome involves up to 2/3 of patients Of these 1/3 may suffer permanent eye damage see table below for adverse ocular effects of drugs

Some adverse ocular effects of drugs

Drug anatomical site ADR on eye

-Anticholinergics -lacrimal apparatus - dry secretions -Cholinergic agents lacrimal apparatus- increase tear secretion -Amiodarone,amodiaquine-}- cornea microdeposits- reduced
vision Phenothiazine,gold} -do-

 Corticosteroids Anticholinergics

lenslens

- cataract formation impared { accomodation & blurred vision

Oral contraceptives

lens

lens hydration increased blurred visison

 Anticholinergics use in glaucoma - Cause increased intraocular pressure leading to reduced visual acuity - Chloroqine -optic nerve- optic atrophy - Ethambutol -do -do- Chloramphenicol - do-do- They above drugs also induce retrobulbar neuritis, optic atrophy may lead to permanent visual loss

 Digoxin

- retina - impaired yellowgreen vision

Sildenafril(Viagra) -retina- blue vision