Common Drugs Use in Common Drugs Use in OphthalmologyOphthalmology

Rungroj Lertvithayasakul, MDRungroj Lertvithayasakul, MDVarintorn Chuckpaiwong, MDVarintorn Chuckpaiwong, MD

Department of Ophthalmology, Ramathibodi Hospital Department of Ophthalmology, Ramathibodi Hospital School of Medicine, Mahidol UniversitySchool of Medicine, Mahidol University, y, y

Route of AdministrationRoute of AdministrationRoute of AdministrationRoute of Administration

LocalLocal•• Topical Topical •• Intravitreous Intravitreous •• Subconjunctival Subconjunctival •• SubtenonSubtenon•• RetrobulbarRetrobulbar•• IntracameralIntracameral

SystemicSystemicyy

Blood aqueous barrierBlood aqueous barrierBlood retinal barrierBlood retinal barrierBlood retinal barrierBlood retinal barrier

EyedropsEyedropsEyedropsEyedrops

50 µl per drop

•• Only Only 20 20 % of the administered % of the administered drugs is retained drugs is retained

•• One drop is enough.One drop is enough.p gp g

Volume of fluid held by cul-de-sac 7 – 10 µl

Drug eliminating mechanismsDrug eliminating mechanismsDrug eliminating mechanismsDrug eliminating mechanisms

Lacrimal glandLacrimal gland

Tear production: Tear production: 11..2 2 µl /minµl /min

Turn over rate 16 % per min

Remaining 4 min : 50 %

Nasal cavityNasal cavity

10 min : 17 %

Nasal cavityNasal cavity Surface area of Surface area of 150 150 -- 200 200 cm cm 22

( ( 13 13 times of conjunctiva ) times of conjunctiva ) 200 200 times of cornea times of cornea

Drug eliminating mechanismsDrug eliminating mechanismsDrug eliminating mechanismsDrug eliminating mechanisms

If the drug is If the drug is irritating to the eyeirritating to the eye

Dilution of drugDilution of drugOverflow drainageOverflow drainagetat g to t e eyetat g to t e eye O e o d a ageO e o d a age

Improve ocular and decrease systemic Improve ocular and decrease systemic absorptionabsorption

Digital pressure at medial canthal Digital pressure at medial canthal areaarea

Keep eyes closed for Keep eyes closed for 5 5 min after min after p yp ytaking dropstaking drops

W itW it 1010 i t b t di t b t dWait Wait 10 10 minutes between dropsminutes between drops

Frequency ~ duration of actionFrequency ~ duration of action

Order of using ~ pHOrder of using ~ pH

Drug PenetrationDrug Penetration

Precorneal areaPrecorneal area

CorneaCornea

Anterior SegmentAnterior Segment

Aqueous HumorAqueous Humor

Drug PenetrationDrug PenetrationDrug PenetrationDrug Penetration

Factors that determine the amount of medication Factors that determine the amount of medication to penetrate the corneato penetrate the cornea

•• Drug concentrationDrug concentration•• ViscosityViscosity•• ViscosityViscosity•• Lipid/water solubilityLipid/water solubility

HH•• pHpH•• SurfactantsSurfactants•• Reflex tearingReflex tearing•• Preservative Preservative

FormFormFormForm

Solution and suspensionSolution and suspensionOi t tOi t tOintmentOintmentGelGel

Solution and SuspensionSolution and SuspensionSolution and SuspensionSolution and Suspension

Most commonly usedMost commonly usedyy

AdvantagesAdvantagesEasily instilledEasily instilled-- Easily instilledEasily instilled

-- Less interfere to visionLess interfere to visionFewer potential complicationsFewer potential complications-- Fewer potential complicationsFewer potential complications

DisadvantagesDisadvantagesDisadvantagesDisadvantages-- Short ocular contact timeShort ocular contact time

Imprecise and inconsistent deliveryImprecise and inconsistent delivery-- Imprecise and inconsistent delivery Imprecise and inconsistent delivery -- Frequent contaminationFrequent contamination

P ibiliti f l i j ith th d tiP ibiliti f l i j ith th d ti-- Possibilities of ocular injury with the dropper tip Possibilities of ocular injury with the dropper tip

SuspensionsSuspensionsSuspensionsSuspensions

Must be reMust be re--suspended by shaking to provide suspended by shaking to provide an accurate dosage of drugan accurate dosage of drugg gg g

OintmentOintmentOintmentOintment

Consist of petrolatum and mineral oilConsist of petrolatum and mineral oilIncrease contact timeIncrease contact timeIncrease contact timeIncrease contact timeDisturb visionDisturb vision

GelGelGelGel

PolymerPolymer--based aqueous gelsbased aqueous gels

Drug release occurs by diffusion and by erosion Drug release occurs by diffusion and by erosion

f th l ff th l fof the gel surfaceof the gel surface

Techniques of InstillationTechniques of InstillationTechniques of Instillation Techniques of Instillation

Eye ointment

Eye drop

Eye ointment

PackagingPackagingPackagingPackaging

The outer surface The outer surface dimensions of the tip dimensions of the tip

affects drop sizeaffects drop sizepp

PackagingPackagingPackagingPackaging

Standard colors for drug labeling and bottle cap Standard colors for drug labeling and bottle cap g g pg g p

YellowYellow BlueBlue B blockerB blockerYellowYellow, , BlueBlue B blockerB blockerRed Red Mydriatics and cycloplegicsMydriatics and cycloplegicsGreenGreen MioticsMioticsOrange Orange Carbonic anhydrase inhibitorsCarbonic anhydrase inhibitorsBrown or tanBrown or tan AntiAnti--infective agentsinfective agentsGrayGray NSAIDSNSAIDSGray Gray NSAIDSNSAIDSPink Pink SteroidsSteroids

Commonly used drugsCommonly used drugs

AnesthesiaAnesthesiaAnesthesiaAnesthesia

T i lT i lTopicalTopicalCornea, conjunctivaCornea, conjunctivaIrritate Irritate 15 15 secsecDuration Duration 15 15 minminFor FB removal, IOP measurement, etc.For FB removal, IOP measurement, etc.Complications : toxic to epitheliumComplications : toxic to epitheliumComplications : toxic to epitheliumComplications : toxic to epithelium

Tetracaine hydrochloride (Tetracaine)Tetracaine hydrochloride (Tetracaine) 00 55%%Tetracaine hydrochloride (Tetracaine) Tetracaine hydrochloride (Tetracaine) 00..55%%Benoxinate hydrochloride (Novesine) Benoxinate hydrochloride (Novesine) 00..44%%

AnesthesiaAnesthesiaAnesthesiaAnesthesia

LocalLocalIncluding akinesiaIncluding akinesiaggFor surgeryFor surgeryComplications: overdose systemic absorptionComplications: overdose systemic absorptionComplications: overdose, systemic absorption Complications: overdose, systemic absorption (respiratory distress, seizure) (respiratory distress, seizure)

Lidocaine hydrochloride (Xylocaine) Lidocaine hydrochloride (Xylocaine) 11--2 2 % % 11--2 2 hrhr

Bupivacaine hydrochloride (Marcaine)Bupivacaine hydrochloride (Marcaine) 00..2525--00..55% % 55--7 7 hrhr

MydriaticsMydriaticsyy

I. SympathomimeticsI. SympathomimeticsStimulate dilator muscleStimulate dilator muscleComplications: AACG, vasoconstrictionComplications: AACG, vasoconstrictionFor retinal examination surgeryFor retinal examination surgeryFor retinal examination, surgeryFor retinal examination, surgery

Phenylephrine hydrochloride (Neosynephrine)Phenylephrine hydrochloride (Neosynephrine)1010% % 22--3 3 hrhr

MydriaticsMydriaticsMydriaticsMydriatics

II Parasympatholytics / CycloplegicsII Parasympatholytics / CycloplegicsII. Parasympatholytics / CycloplegicsII. Parasympatholytics / CycloplegicsInhibit constrictor m.and ciliary m. contraction Inhibit constrictor m.and ciliary m. contraction Complications: AACG, flushingComplications: AACG, flushingFor ciliary spasm, refraction in children, retinal For ciliary spasm, refraction in children, retinal y py pexamexam

Atropine sulfate Atropine sulfate 11% % 2 2 wkwkScopolamine hydrobromide Scopolamine hydrobromide 00..2525% % 33--5 5 ddp yp yHomatropine hydrobromideHomatropine hydrobromide 11--22% % 11--3 3 ddCyclopentolate hydrochloride (Cyclogyl) Cyclopentolate hydrochloride (Cyclogyl) 11% % 24 24 hrhry p y ( y gy )y p y ( y gy ) %%Tropicamide (Mydriacyl) Tropicamide (Mydriacyl) 00..55--11% % 44--5 5 hrhr

Mydriatics and CycloplegicsMydriatics and Cycloplegics

At i lf tAt i lf tAtropine sulfate Atropine sulfate

Cyclopentolate HClCyclopentolate HClCyclopentolate HCl Cyclopentolate HCl

TropicamideTropicamideTropicamideTropicamide

Phenylephrine HClPhenylephrine HCly py p

ผปวยชายอาย 40 ป ตาขวาเคอืงเจ็บ มานาน 1 วันผูปวยชายอายุ 40 ป ตาขวาเคองเจบ มานาน 1 วน

ิ ิ ั โการวนิิจฉัยโรค

การรกัษา

ป ิ ป ป ี ี้ผูปวยหญิงอายุ 45 ป ปวดตาขวา ตาแดง มีขีตา

มานาน 3 วันมานาน 3 วน

การวนิิจฉัยโรคการวนจฉยโรค

ัการรกษา

AntibioticsAntibioticsAntibioticsAntibiotics

AntibioticsAntibioticsAntibioticsAntibiotics

ConsiderConsiderSeverity and progressionSeverity and progressionSeverity and progressionSeverity and progressionSuspected organism & SensitivitySuspected organism & SensitivityLocation & PenetrationLocation & PenetrationToxicityToxicityToxicityToxicityFrequency and concentrationFrequency and concentration

ผปวยชายอาย 18 ป เปลือกตาขวาบนเจ็บมานาน 3 วัน ู ว ุ 8 เ ล ว นเ ม น น 3 วน

การวนิิจฉัยโรคการวนจฉยโรค

ัการรกษา

Antibiotics: CombinationAntibiotics: CombinationAntibiotics: CombinationAntibiotics: Combination

Polymyxin B

Gramicidin

Neomycin

AntibioticsAntibioticsAntibioticsAntibiotics

AntibacterialAntibacterial

AntifungalAntifungal

AntiviralAntiviral

Anti parasiticAnti parasitic

ป ิ 30 ป ื ผปูวยหญง อาย ุ30 ป มาดวยอาการ เคองตาขวา

มานาน 1 เดือน

การวนิิจฉัยโรค

การรกัษาการรกษา

AntihistamineAntihistamine VasoconstrictorsVasoconstrictorsAntihistamineAntihistamine VasoconstrictorsVasoconstrictors

Pheniramine maleate

A t li HCl

Phenylephrine HCl

Naphazoline HClAntazoline HCl Tetrahydrozoline HCl

Antazoline HCl + Tetrahydrozoline HCl

Pheniramine maleate + Naphazoline HCl

ผปวยเด็กชายอาย 7 ป คันตา ตาแดง 2 ขาง มาผูปวยเดกชายอายุ 7 ป คนตา ตาแดง 2 ขาง มา

นาน 1 ป

การวนิิจฉัยโรค

การรกัษาการรกษา

M tM t ll t bilill t biliMastMast--cell stabilizercell stabilizer

Cromolyn sodiumCromolyn sodium

LodoxamideLodoxamideLodoxamideLodoxamide

Olopatadine HClOlopatadine HCl

ผปวยชาย อาย 40 ป มีเนื้อเยื่อบริเวณหัวตาซายผูปวยชาย อายุ 40 ป มเนอเยอบรเวณหวตาซาย

มานาน หลายป ซื้อยาหยอดตา dexoph ใชเปน

ประจํา

การวนิิจฉัยโรค

การรกัษา

CorticosteroidCorticosteroidCorticosteroidCorticosteroid

AntiAnti--inflammationinflammationSuppress immune system and tissue reactionSuppress immune system and tissue reactionpp ypp yPrecaution in treatment of infection especially Precaution in treatment of infection especially viral and fungal infectionviral and fungal infectionviral and fungal infectionviral and fungal infection

DexamethazoneDexamethazone 00 11%%DexamethazoneDexamethazone 00..11%%

Prednisolone acetatePrednisolone acetate 00..55%, %, 11%%

FluorometholoneFluorometholone 00..11%%

CorticosteroidsCorticosteroidsCorticosteroidsCorticosteroids

Prednisolone ( Prednisolone ( 00..55, , 11% )% )

Dexamethasone ( Dexamethasone ( 00..11%)%)

Fluorometholone ( Fluorometholone ( 00..1 1 %)%)

CorticosteroidsCorticosteroidsCorticosteroidsCorticosteroids

Side effects

G• Glaucoma

Cataract• Cataract

• Exacerbation of infectionExacerbation of infection

• Ptosis

• Scleral melting

Artificial TearArtificial TearArtificial TearArtificial Tear

SupplementSupplementIncrease contact timeIncrease contact timeFor dry eye, CL wearerFor dry eye, CL wearer

Frequency of usage ~ severityFrequency of usage ~ severityPreserve VS non preservePreserve VS non preserve

Artificial tearsArtificial tearsArtificial tearsArtificial tears

The endThe end