1: Pharmacology of drugs acting on the eye

MCQs SAQs summary

:قادة فريق علم األدوية

عبدالرحمن ذكري &لي التميمي :الشكر موصول ألعضاء الفريق املتميزين

روان سعد القحطاني

رنا باراسيجواهر اخليال

@pharma436pharma436@outlook.com

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Challengestodrugdeliverytotheeye:1)Thebloodbrainbarrier2)Theyareclearedrapidlybytearsoraqueoushumor3)HighriskofinfectionsduetoSubconjunctival&intravitrealinjections

AllmitoticdrugssuchasParasympatheticagonistcanbeusedforboth1)Openandcloseglaucoma.

Whilethemyadraticdrugssuchas(parasympatheticantagonist&sympathetic)canbeusedfor…1) Restrictiedonlyforopenglaucoma2) Fountoscopicexaminationforeyes3) Decongestionbyalpha1agonist

Latanoprost:1)TheyhavereplacedbetablockersTheyareusedtopicallyonceaday.2) ADRSheterochromiairidis&Macularedema.

SoinopenangleglaucomathefirstchoiseisLatanoprostthenBetablockers

Acutecloseglaucoma,wehavetodecreaseIOPby:1)DecreaseAqueoushumorformationà by(Carbonicanhydraseinhibitors)2)Increasetheoutflowofità by(MitoticDrugs)3)Shiftingofthefluidfromtheeyeschamberstocirculatorybloodbyà (Osmoticagents)

Anydrugscausemydriasiscannotbeusedincloseangleglaucoma1) PassiveMydriasiswithcycloplegiaà bycholinergicantagonist2) ActiveMydriasiswithoutcycloplegiaà Bynon-selectiveAdrenergicdrugsorselective

alphaagonist

Peri-ocularinjectionisaGoodroutefordrugswithlowlipidsolubility(e.g.penicillins)Peri-ocularinjectionisUsedforinfectionofanteriorsegmentandinflammationofuvea

Drugs canbedeliveredtooculartissueas:Locally(topically)orsystemically

1-Locally

injectionocular-Periinjectionocular-IntraOintmentsEyedrops

Types:- subconjunctival.- Retro-bulbar.- Peri-bulbar.- Subtenon

§ Goodfordrugswithlowlipidsolubility(e.g.penicillins)

§ Steroidandlocalanestheticscanbeappliedthisway.

§ Usedforinfectionofanteriorsegmentandinflammationofuvea

cameral:-Intra-1E.g.duringcataractsurgery.- acetylcholineor- lidocaine

- Increasesthecontacttimeofocularmedicationtoocularsurface→providingbettereffect.

- Mostcommonrouteofadministration

- Eyedropsaresalinecontainingdrops“liquid”

- hastobeusedseveraltimes.

:vitreal-Intra-2E.g.- antibiotics

àendophthalmitis- steroid

à macularedema

2-Systemically( IVorOral)

Ø Factorsinfluencingsystemicdrugpenetrationintooculartissue:• lipidsolubilityofthedrug:morepenetrationwithhighlipidsolubility• Proteinbinding:moreeffectwithlowproteinbinding(inverseproportion)• Eyeinflammation:morepenetrationwithocularinflammation.

Drugscausingcornealdeposits

depositsTheDrugs

Chromatopsia(yellowish haze)Digitalis

1- Bluishhaze. 2- LightsensitivitySildenafil

1- Pigmenteddepositsofcornea. 2- Opticneuropathy.Amiodarone,Chloroquine

Opticneuropathy.Ethambutol

Brownpigmentary.Phenothiazine

1- Cataractformation 2- IncreaseIOP 3- GlaucomaSteroids

Cholinergic agonists

Anticholinesterase)Indirectagonist(Directagonist

Drug

Reversible→1- physostigmine 2- demecariumIrreversible→1- echothiophate 2- isoflurophate

1- Methacholine 2- Acetylcholine3- Carbachol 4- Pilocarpine

Specificuses:1- Glaucoma2- Ecothiophate:Accommodative esotropia3- Physostigmine: Inliceinfestationoflashes

Specificusesoffirst threedrugs:1- Inductionofmiosisinsurgery.2- Openangleglaucoma.Specific usesofPilocarpine:1- Openangleglaucoma

indicatio

ns

Generaluses:1- Glaucoma(open&closedangle).2- Counteractactionofmydriatics.3- Tobreakiris-lensadhesions.4- Inaccommodativeesotropia (ecothiophate).

- Diminishedvision(myopia). - Headache

ADRs

Cholinergic(muscarinic)antagonists

SyntheticShortduration

NaturalLongduration

Drug

1- homatropine.2- cyclopentolate3- tropicamide

1-Atropine.2- Scopolamine (Hyoscine)

1- Topreventadhesioninuveitis&iritis.Dueitspassivemydriasis.2- Funduscopicexaminationoftheeye.&Measurementofrefractiveerror

indicatio

ns

Cycloplegia,Lossoflightreflex, sandyeye

ADRs

Glaucoma(angleclosureglaucoma)increasedI.O.PC.I

Adrenergicagonists

Selectiveα2agonistsSelectiveα1agonistsNon-selectiveagonists

Drug

ApraclonidinePhenylephrineEpinephrine (Dipivefrinisthe pro-drug)

1- Openangleglaucomatreatment2- Prophylaxis againstIOPspikingafterglaucomalaserprocedures.

1- Funduscopicexamination2- Topreventadhesioninuveitis&iritis.3- Decongestant

Openangleglaucoma.

indicatio

ns

1- Headache.2- Bradycardia.3- Hypotension.

1- Hypertension2- Reboundcongestion.

1- Headache.2- Arrhythmia.3- HypertensionAD

Rs

1- Precipitationofacuteangleclosureglaucomainpatientswithnarrowangles.

1- Inpatientswithnarrowanglesastheymayprecipitateclosedangleglaucoma.

C.I

(α1effect)→becauseitisdoingmydriasis.

Adrenergicdrugs:Betablockers

Selectiveβ1(cardio-selective)Non-selective

Drug Betaxolol1- Timolol 2-

Carteolol

- Usedintreatmentofopenangleglaucoma.

indicatio

ns

Canbeusedinpatientswithhypertension&ischemicheartdisease.

Ocularirritation.

ADRs

- Inasthmapatients.C.I

Others

Systemic Osmoticagents(Dehydratingagents)

ProstaglandinanaloguesCarbonicanhydraseinhibitors

Drug mannitolol,

Glycerol(foracuteclosuregluacoma)

latanoprost,travoprost

(topical)(oral)

Dorzolamide(preferred)

Acetazolamide

(priortoanteriorsurgicalprocedure)Usedonly inacutesituationstotemporarilyreducehighIOPuntilmoredefinitivetreatmentscanberendered.

openangleglaucoma

indicatio

ns

Diuresis,circulatoryoverload,pulmonaryedema

Heartfailure- Centralnervoussystemeffectssuchas

seizure,andcerebralhemorrhage.

Pigmentationoftheiris(heterochromiairidis),Intraocularinflammation,Macularedema.

Myopia malaise,anorexia,GIupset,headache.Metabolic

acidosis,renalstone.ADRs

Sulfaallergy, Pregnancy,Digitalisusers.C.

I

Anti-inflamatory Drugs

NSAIDsCorticosteroids

Drug

DiclofenacKetorolacFlurbiprofen

SystemicTopical

1- Prednisolone2- Cortisone

1- Prednisolone2- Dexamethasone3- Hydrocortisone

cyclooxygenaseinhibitorsinhibitingphospholipaseA2M .O .A

Postoperativeinflammation

Cystoidmacularedemaoccurringaftercataractsurgery.

Preoperativelytopreventmiosisduringcataractsurgery

1- Posterioruveitis.2- Opticneuritis.

1- Anterioruveitis.2- Severeallergicconjunctivitis.3- Scleritis.4- Preventionandsuppressionofcornealgraftrejection.5-postoperatively

indicatio

ns

- Stinging(irritation)- Sterilecornealmelt&perforation

- Glaucoma,cataract,mydriasis- Skinatrophy.- Secondaryinfection.- - Delayedwoundhealing.

ADRs

1- A20yearoldfemalewithchronicopenangleglaucoma,24weekspregnant,wasprescribedadrugthatdecreasedtheproductionofheraqueoushumor.Whichofoneofthefollowingdrugsiscontraindicatedinhercase?A- Apraclonidine. B- Tropicamide.C- Acetazolamide.D- timololAnswer:C

2- WhichoneofthefollowingisADRSofpilocarpine?A- Headache.B- Arrhythmia.C-Diminishedvision(myopia).D- Hypotension.Answer:C

3- A24yearoldmalepatientwasexperiencingminorallergichyperemiaandcongestion,andaftertakingtheprescribeddrugherealizedanincreaseinhisbloodpressure,andlaterondevelopedacuteangleclosureglaucoma.Whichismostlikelythedrugthatwasprescribed?A- Tropicamide B- Phenylephrine C- Apraclonidine D- timololAnswer:B

4- Systemicosmoticagentsareonlyusedinchroniccases?A- trueB- falseAnswer:B

5- WhichstatementistrueabouttheDiclofenac?A- ItisaCOX(cyclo-oxygenase)inhibitorB- ItisaphospholipaseA2inhibitorC- ItisusedpreoperativelytopreventmiosisduringcataractsurgeryD- ItwillcausedelayedwoundhealingbecauseoftheimmuneresponseAnswer:A

6- A53yearoldhypertensivepatientcametotheclinicandduringexaminationitwasfoundthatshehadopenangleglaucoma.Whichdrugofthefollowingistheprefered inhiscase?A- EpinephrineB- PhenylephrineC- Betaxolol D- timololAnswer:C

7- Ifanophthalmologistwantstodilatethepupilsforaneyeexamination,whichofthefollowingdrugscouldbetheoreticallyuseful?A- Acetylcholine B- Pilocarpine C- Neostigmine. D- TropicamideAnswer:D

8- Whichofthefollowingdrugsiscommonlyusedtopicallyandonceadayinthetreatmentofopenglaucoma?A- Pilocarpine B- Tropicamide C- Latanoprost D- carteololAnswer:C

9- A32yearoldfemalewithchronicopenangleglaucoma,wasprescribedadrugthatdecreasedtheproductionofheraqueoushumoraseyedrops,.Later,shedevelopconjunctivitis.Whichofoneofthefollowingroutofadministrationispreferinhercase?A- Ointment.B- PeriocularinjectionsC- Intraocularinjections.D- doesnotmaterAnswer:B

10- Whichofoneofthefollowingroutofadministrationisthebestforlowlipidsolubilitysuchaspenicillinintotheeyes?A- Ointment. B- Periocularinjections C- Intraocularinjections. D- eyedrops.Answer:B

11- InmyFunduscopicexaminationtheophthalmologistusetropicamid .WhenIleaveIcouldnotseemywatchandIdevelopedlightsensitivity.Whichoneofthefollowingdrugsshouldthedoctorsusedtocounteractthesesymptoms?A- PilocarpineB- Phenylephrine C- Apraclonidine D- timololAnswer:A

1- Givetwoexamplesofnatural drugsthatcanbeprescribedtoapatienttopreventadhesioninuveitis&iritis,andtomeasuretherefractiveerror.Naturalalkaloids:A- atropineB- Scopolamine(Hyoscine)

2- A32yearoldasthmaticpatientcametotheclinicbecauseofhypertensionandacardiovasculardisorder,andduringexaminationitwasfoundthatshehadopenangleglaucoma.Whichdrugclassiscontraindicatedandwhatisthemechanism?Betablockers,becauseoftheB2effectonthelungs(bronchospasm)andtheB1effectontheheart.

3- What’sthenameofthesurgerythattreatsemergencyacutenarrowclosedangleglaucoma?Iridectomy

4- Apatientwasprescribedprednisolonetotreathissevereallergicconjunctivitis.Mention3ADRsthathe/shemightexperience?- Glaucoma,cataract,mydriasis- Skinatrophy.- Secondaryinfection.- Delayedwoundhealing.

5- Name3drugsthatcancausecornealdeposits?Sildenafil– Ethambutol– Steroids– Phenothizines – Digitalis- AmiodaroneChloroquine

v A61yearoldfemalediagnosedwithcataractinbotheyes,After2weeksshewillhavecataractsurgery.

1- whichrouteofAdministrationisthebestforlidocaineduringthesurgery?Intracameral injectionisthebest.2-Topreventthemiosisduringthesurgery,whichdrugcanbeused?Flurbiprofen (NSAID)canbeusedpre-operavely3- Afterthesurgerythepatientmaydevelopcystoidmacularedema,whichdrugcanbeusedtominimizeit?Ketorolac(NSAID)4- Whichdrughavethehighrisktodevelopcataractassideeffect?Corticosteroidssuchasprednisolone,cortisonedexamethasoneandhydrocortisone

v A61yearoldmalediagnosedwithOpenangleglaucomainbotheyes.

1- whatarethedrugsofchoiceinhiscase?Prostaglandinsandβblockersarethemostpopular2-IfthepatienthasHypertension,whichdrugcanbeusedsafely?Betablockerssuchastimolol.3-Ifthedoctorwillprescribeoneofthefollowingdrugs(Apraclonidine/dorzolamide/latanoprost),whataretheMechanismofaction?• Apraclonidineà isaSelectiveα2agonistsà↓productionofaqueoushumor,and↑uveoscleral

outflowofaqueoushumor• Dorzolamideà isCarbonicanhydraseinhibitorsà↓productionofaqueoushumorbyblocking

carbonicanhydraseenzyme• Latanoprostà Prostaglandinanaloguesà↑uveoscleral aqueousoutflow.4-TropicamideisCholinergicantagonist,listsomeofitssideeffects?IncreaseIOPduetoitsPassiveMydriasis./cycloplegia/loselightreflex/Sandyeye.5-ListsomeeyemedicationmayleadtoincreaseinIOP?Cholinergicantagonist/corticosteroids6-Ifthepatienthashighrisktodevelopcloseangleglaucomaduetoitsnarrowangle,Listsomedrugscannotbeusedinthiscase?Epinephrine/Phenylephrine

v APatienthasglaucomadiagnosedwithAnterioruvitis.

1- whichrouteofAdministrationisthebestforeyedrugs?Peri-ocularinjection2-Listtwodrugscanbeusedinthiscase,andexplaintheirmechanismofactions?Corticosteroidssuchasprednisolone,hydrocortisoneà byinhibitingphospholipaseA2