Drugs used in ophthalmologyDrugs used in ophthalmology

lek.med. Magdalena Mazurek

Chair and Clinic of Ophthalmology with Department of Patophysilogy of Organ of Vision

How does a drug get inside the eye?How does a drug get inside the eye?

• 1. By blood

The blood-retinal barrier (BRB)

• 2. Penetrates by the cornea Mainly by epithelium and endothelium of the cornea

Route of administrationRoute of administration

• Given locally ( eye drops) – amount of drug in the anterior segment of the eye > given orally

• Given locally– achieve therapeutic levels up to the ciliary body

• Intraocular concentration :– subconjunctival injection > eye drops i ointment >

orally

Types of drugs -Types of drugs -way of administration:way of administration:

• 1. Eye drop , suspension , emulsion• 2. Ointment and gel

• 3. Inserts – i.e. Ocusert (Pilocarpine) – a drug container placed inside conjunctiva

• 4. Therapeutic Contact Lenses (‘bandage’ lenses)

Types of drugs -Types of drugs -way of administrationway of administration

• 5. Ion(t)ophoresis - technique using a small electric charge to deliver a medicine through the surface of cornea/ skin . The drug forms charged active agents ( kations, anions) which transport deaper .

• 6.Subconjunctival injection and periocular injection

• 7. Anterior chamber injection• 8. Intravitreal injection

Eye dropsEye drops

• After administration a smaller amount of drug is absorbed by the surface of the cornea, most of it reaches vascular system by the conjunctiva.

• Only 1 drop because:– Volume of the conjunctival sac = 30 μl– Volume of 1 drop = 40-70 μl

• If you administer more than one drug remember about intervals– time for penetration and absorbtion

Eye drops Eye drops

• While giving drops that have systemic effects (β-blockers, adrenaline, pilocarpine ):

– Patient should close his eyes after drug administration (it counteracts getting into the lacrimal sac by the canaliculi )

– Press in the place where lower canaliculus is located– It is possible to give the drug directly on the cornea.

OintmentsOintments

• Longer time of contact with the eyes surface

• Often given before going to sleep (overnight)

• They paste eyelashes together

• They can cause reversible loss of visual acuity

Groups of drugs:Groups of drugs:• 1. Drugs affecting the vegetative system

• 2. Drugs used in glaucoma

• 3. Anti-infectious drugs

• 4. Anti-inflammatory drugs

• 5. Anti-allergic drugs

• 6. Drugs affecting metabolism of cells and their

regeneration

• 7. Lubricant Eye Drops ( ` fake tears ` )

• 8. Anaesthetics

• 9. Disinfectant Drugs

Drugs affecting the vegetative system

SympathicomimeticsSympathicomimetics

Substance Receptors

Adrenaline α , β

Noradrenaline α , β

Fenylefryne α (non-selektive)

Brimonidyne α2

Apraklonidyne α2

SympathicomimeticsSympathicomimetics ( (mydriaticamydriatica))

• Stimulate receptor α + β:– Stimulate sympathetic nervous system– Dilate the pupil do not affect focusing

(accommodation)– Tear adhesions apart– If the angle is closing they can cause its total

closure and increased IOP

– Neosynephrin sol. 2,5% 5% 10%– Adrenaline ( 0,001%) < 1 ml

• Counter-indications :– arythmia– hypertension, high blood pressure – pheohromoctyoma– IHD– Closed angle glaucoma

Adverse effect– Anxiety, tremor– Dizziness ,headache– Tachycardia– Arythmia , acute chest pain– Allergy

Sympaticolitics (β-blockers)Sympaticolitics (β-blockers)

• ↓IOP:– ↓ production of aqueous humour by the ciliary body– affect ultrafiltration

• non-selective β-blockers (β1 + β2)– Karteolol, Timolol, Lewobunolol

• selectywne β-blockers (β1)– Betaksolol

• Glaucoma:– Open angle glaucoma– Closed angle glaucoma (with

parasympathicomimetic)– Glaucoma in aphakic eyes

Lowers elevated but also normal IOPYounger patients –stronger hypotension

β-blockery – indications β-blockery – indications

Side effects– conjunctival irritation, burning sensation, reversible

loss of visual acuity,conjunctivitis,dry eyes,ptosis, constriction of vessels

– bradycardia , arythmia, hypotension, stroke, cerebrovascular accident (CVA) , VASCULAR FAILURE

– bronchospasm (except for betaksolol), difficulty in breathing , dizziness ,headache, depression,nausea

– allergy

• Counter-indications :

– Asthma – Lung diseases– Heart/ vascular failure– II /III degree AV block– Bradycardia– Allergy

– ! Unstable diabetes !

– ! Pregnancy and Breastfeeding !

β-blockersβ-blockers

• Betaksolol (Betoptic) sol. 0,25% 0,5%

• Timolol (Oftensin, Timoptic, Cusimolol) sol. 0,25% 0,5%

• Karteolol (Arteoptic) sol. 1% 2%

• Metipranolol (Betamann) sol. 0,1% 0,3%

Parasympathicomimetic (miotics)Parasympathicomimetic (miotics)

• ↓IOP

• Dilate veins ↑aqueous outflow• Used in treatment of closed angle glaucoma

• Pilocarpine sol. ung. 1% 2% 4%• Karbachol sol. 3%

• Counter-indications:– Uveitis– Retinal Degenerative Diseases ( ↑ incidence of retinal

detachment)– Heart diseases– Asthma– Hyperthyreosis– Peptic Ulcer Disease– Parkinson's disease

ParasympathicomimeticParasympathicomimetic

• Side effects:– Headache

– Speeds up onset of cataract

– Constricts pupils poor night sight

– Posterior synechiae

– ↑ lacrimation

– Systemic effects: bradycardia, hypotension, ↑Increased urination, production of saliva

– They block the parasympathetic system– Dilate the pupil affect accommodation

– Atropine sol. 1% (children 0,25-0,5%) - 2weeks.– Homatropine sol. 1% -12 h.– Scopolamine sol. 0,25% -30 h.– Tropicamid sol. 0,5% 1% -

4 h.– Cyclopentolat sol. 0,5% 1% -

24 h.

ParasympaticolyticsParasympaticolytics ( (mydriatica et cycloplegicamydriatica et cycloplegica))

• Indications:– Helps with diagnosis (dilated pupil- fundus

examination )– Preparation for the eye surgery– In treatment of iriditis ,cyclitis– Corneal ulcers

• Counter-indications :– Closed angle glaucoma– Diseases of urinary tract and prostate with urinary

retention – Epilepsia– Allergy– < 1year old

• Parasympaticolytics can cause closure of the angle – acute glaucoma!

• gonioscopy

• If the angle is narrow :– 250 mg acetazolamide p.o. before dilation– Better use Neosynephrin

Drugs used in glaucoma

1. α2-adrenomimetics i β-adrenolitics

2. Parasympathicomimetic

3. Carbonic anhydrase inhibitors

4. Prostaglandin analogues

5. Combinated drugs

Carbonic anhydrase inhibitorsCarbonic anhydrase inhibitors

• ↓ production of aqueous

• ↑ urination (when longer used ↓K+)

• Acetazolamide - Diuramid tabl. 250 mg - Diamox inj. i.v. 500mg

• Diclofenamid (Diklofenamid) tabl. 50 mg• Dorzolamid - Trusopt sol. 2%

- Azopt sol.1%

Carbonic anhydrase inhibitorsCarbonic anhydrase inhibitors

• Counter-indications :– Renal failure, liver failure , chronic respitarory

diseases

• Side effects:– Dizziness, headache, drowsiness , depression,

dyspepsia, renal /urinary tract lithiasis , hypercaliemia i metabolic acidosis , paresthesia, itching /burning sensations of the eyes

Prostaglandin analoguesProstaglandin analogues

• ↑ Outflow of aqueous humour – Ciliary body sclera lymphatic vessels

• convenient in use – 1x day

• Latanoprost (Xalatan) sol.• Travoprost (Travatan) sol.• Bimatoprost (Lumigan) sol.

Prostaglandin analoguesProstaglandin analogues

• No systemic side effects

• Should not be combined with Pilocarpine because it blocks uveoscleral outflow

• Do not use in: allergy

• Side effects:– change of iris color (darker ↑ melanine), burning

sensation of the eyes , keratitis, palpebritis, growth of eyelashes

– rare:headache ,nausea

Combinated drugsCombinated drugs

• If monotherapy does not help

• Cosopt (Timolol + Dorzolamid) sol.

• Fotil, Timpilo (Timolol + Pilocarpina) sol.

• Normoglaucon (Metipranolol + Pilocarpina) sol.

• Xalacom (Latanoprost + Timolol) sol.

• DuoTrav (Travoprost + Timolol) sol.

Anti-infectious drugs

AntybioticsAntybiotics

• To treat infectious diseases of the eye

• Before/Postoperative prophylaxis

• Best to do antibiogram

• Used as eyedrops , ointments, injections

AntybioticsAntybiotics

• Aminoglycosides– Amikacin (Biodacin) sol.– Gentamycin 0,3% sol. ung.– Neomycyn ung.– Tobramycin (Tobrex) sol. ung.Tetracyclines– Oftalmolosa cusi tetracycline – ung.

• Chloramphnicol– Oftalmolosa cusichloramfenicol – ung.– 1% sol.Detreomycini

AntybioticsAntybiotics

• Fluoroquinolones– Ciprofloksacin (Ciloxan, Proxacin) sol.– Norfloksacin (Chibroxin) sol.– Ofloksacin (Floxal) sol. ung.

• Sulfonamids:– Sulfacetamid 10% sol.– Sulfadikramid (Irgamid) ung.

Antiviral drugs Antiviral drugs

• Herpes zoster, HSV, CMV, EBV

• NOT adenovirus infection (one of most common infections)!!!!!!

• Acylovir (Cusiviral, Virolex, Zovirax) ung. tabl.

• Vidarabine (Vira A) ung.

Anti-inflammatory drugs•SteroidsSteroids•Nonsteroidal

Hydrocortison 1 (point of reference)

Fluorometolon 1

Prednison 3,5

Prednisolon 4

Metyloprednisolon 5

Triamcinolon 5

Parametason 10

Fludrocortison 10

Deksametason 25-30

Betametason 30-40

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Steroids – local use :Steroids – local use :

• Betametason (Betnesol) sol.0,1%

• Deksametason (Dexamethason, Oftan Dexa) sol.0,1%

• Fludrocortison (Continef) ung.

• Fluorometolon (Flucon, Flarex) sol.

• Hydrocortison (Hydrocortison dispersa, Ophticor H) ung.

• Prednisolon (Prednisolonum) sol.

NSAIDsNSAIDs• General inhibition of prostanoid biosynthesis • Often used :

– Before/after surgery– Conjunctivitis, keratitis, scleritis …….– After trauma– Prevent pupil dilation during operation– When steroids can`t be used

• Diclofenac (Naclof) sol.• Flurbiprofen (Ocuflur) sol.• Indometacine (Indocollyre, Indocid) sol.

Anti-allergic drugs

Antihistamine drugsAntihistamine drugs

• Emadastine (Emadine) sol.

• Olopatadine (Opatanol) sol.

Combined :– Alergoftal (Antazoline + nafazoline) sol.– Betadrin (Difenhydramine + nafazoline) sol.– Spersallerg (Antazoline + tetryzoline) sol.

• Allergic conjunctivitis ….symptoms

Anti-allergic drugs other:Anti-allergic drugs other:

• Natrii cromoglicas (Cromohexal, Opticrom, Polcrom, Vividrin, Cusicrom) sol.

• Tilavist sol.

• Alomide sol.

Drugs affecting metabolism of cells and their regeneration

• Better corneal nutrition in dry eye syndrome, in eye burns , erosions ,corneal ulcers….– Dexpantenol (Corneregel) żel– Solcoseryl – gel

• Better metabolism of the lens and vitreous (↓ cataract onset) – Quinax sol.– Catalin sol.

Lubricant Eye Drops ( `fake tears `)

• Lacrimal sol.

• Artelac, Isopto-Tears, Methocel sol.

• Vidisic gel

• Oculotect, Vidisept sol.

• Combined :– Dacrolux sol.– Tears Naturale, Tears Naturale Free sol.– ! Better without conservants!!!!

Anaesthetics

• Given locally .• Do not use too long because they are toxic for

corneal epithelium.

– Bupivacainum inj. 0,25% 0,5%– Marcain inj. 0,25% 0,5%– Lignocainum, Lidocain, Xylocaine inj. 2% 4%– Alcaine sol.

Thanx for listening!Thanx for listening!