Common Drugs Use in Ophthalmology

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The document discusses various ophthalmic drugs, their routes of administration, factors affecting drug penetration and absorption, and common preservatives used in eyedrops.

The main routes of administration discussed are local (topical) and systemic. Local routes include topical, intravitreal, subconjunctival, subtenon, retrobulbar, and intracameral administration.

Factors that determine the amount of drug penetration through the cornea include drug concentration, viscosity, lipid/water solubility, pH, surfactants, reflex tearing, and presence of preservatives.

Common Drugs Use in

Ophthalmology
Rungroj Lertvithayasakul, MD
Varintorn Chuckpaiwong, MD
Department of Ophthalmology, Ramathibodi Hospital
School of Medicine, Mahidol University

Route of Administration

Local

Topical
Intravitreous
Subconjunctival
Subtenon
Retrobulbar
Intracameral

Systemic

Blood aqueous barrier


Blood retinal barrier

Eyedrops
50 l per drop

Only 20 % of the administered


drugs is retained
One drop is enough.

Volume of fluid held by


cul-de-sac 7 10 l

Drug eliminating mechanisms


Lacrimal
Lacrimalgland
gland
Tear production: 1.2 l /min
Turn over rate 16 % per min
Remaining

4 min

: 50 %

10 min : 17 %

Nasal
Nasalcavity
cavity

Surface area of 150 - 200 cm 2


( 13 times of conjunctiva )
200 times of cornea

Drug eliminating mechanisms

If the drug is
irritating to the eye

Dilution of drug
Overflow drainage

Improve ocular and decrease systemic


absorption

Digital pressure at medial canthal


area

Keep eyes closed for 5 min after


taking drops

Wait 10 minutes between drops

Frequency ~ duration of action

Order of using ~ pH

Drug Penetration

Precorneal
Precornealarea
area

Cornea
Cornea
Anterior
AnteriorSegment
Segment

Aqueous
AqueousHumor
Humor

Drug Penetration
Factors that determine the amount of medication
to penetrate the cornea
Drug concentration
Viscosity
Lipid/water solubility
pH
Surfactants
Reflex tearing
Preservative

Form

Solution and suspension


Ointment
Gel

Solution and Suspension


Most commonly used
Advantages
- Easily instilled
- Less interfere to vision
- Fewer potential complications
Disadvantages
- Short ocular contact time
- Imprecise and inconsistent delivery
- Frequent contamination
- Possibilities of ocular injury with the dropper tip

Suspensions
Must be re-suspended by shaking to provide
an accurate dosage of drug

Ointment

Consist of petrolatum and mineral oil


Increase contact time
Disturb vision

Gel

Polymer-based aqueous gels

Drug release occurs by diffusion and by erosion


of the gel surface

Techniques of Instillation

Eye ointment

Eye drop

Eye ointment

Packaging

The outer surface


dimensions of the tip
affects drop size

Packaging
Standard colors for drug labeling and bottle cap
Yellow, Blue
Red
Green
Orange
Brown or tan
Gray
Pink

B blocker
Mydriatics and cycloplegics
Miotics
Carbonic anhydrase inhibitors
Anti-infective agents
NSAIDS
Steroids

Commonly used drugs

Anesthesia
Topical

Cornea, conjunctiva
Irritate 15 sec
Duration 15 min
For FB removal, IOP measurement, etc.
Complications : toxic to epithelium

Tetracaine hydrochloride (Tetracaine) 0.5%


Benoxinate hydrochloride (Novesine) 0.4%

Anesthesia
Local

Including akinesia
For surgery
Complications: overdose, systemic absorption
(respiratory distress, seizure)

Lidocaine hydrochloride (Xylocaine) 1-2 % 1-2 hr


Bupivacaine hydrochloride (Marcaine) 0.25-0.5%
5-7 hr

Mydriatics
I. Sympathomimetics

Stimulate dilator muscle


Complications: AACG, vasoconstriction
For retinal examination, surgery

Phenylephrine hydrochloride (Neosynephrine)


10% 2-3 hr

Mydriatics
II. Parasympatholytics / Cycloplegics

Inhibit constrictor m.and ciliary m. contraction


Complications: AACG, flushing
For ciliary spasm, refraction in children, retinal exam
Atropine sulfate 1% 2 wk
Scopolamine hydrobromide 0.25% 3-5 d
Homatropine hydrobromide 1-2% 1-3 d
Cyclopentolate hydrochloride (Cyclogyl) 1% 24 hr
Tropicamide (Mydriacyl) 0.5-1% 4-5 hr

Mydriatics and Cycloplegics

Atropine sulfate

Cyclopentolate HCl

Tropicamide

Phenylephrine HCl


40
1


45
3

Antibiotics

Antibiotics
Consider
Severity and progression
Suspected organism & Sensitivity
Location & Penetration
Toxicity
Frequency and concentration


18
3

Antibiotics: Combination

Polymyxin B
Gramicidin
Neomycin

Antibiotics

Antibacterial

Antifungal

Antiviral

Anti parasitic


30

1

Antihistamine

Vasoconstrictors
Phenylephrine HCl

Pheniramine maleate

Naphazoline HCl

Antazoline HCl

Tetrahydrozoline HCl

Antazoline HCl
+ Tetrahydrozoline HCl
Pheniramine maleate
+ Naphazoline HCl


7
2 1

Mast-cell stabilizer

Cromolyn sodium

Lodoxamide

Olopatadine HCl


40

dexoph

Corticosteroid

Anti-inflammation
Suppress immune system and tissue reaction
Precaution in treatment of infection especially
viral and fungal infection
Dexamethazone 0.1%
Prednisolone acetate 0.5%, 1%
Fluorometholone 0.1%

Corticosteroids

Prednisolone ( 0.5, 1% )

Dexamethasone ( 0.1%)

Fluorometholone ( 0.1 %)

Corticosteroids
Side effects
Glaucoma
Cataract
Exacerbation of infection
Ptosis
Scleral melting

Artificial Tear

Supplement
Increase contact time
For dry eye, CL wearer
Frequency of usage ~ severity
Preserve VS non preserve

Artificial tears

The end

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