Ophthalmic Pharmacology

Richard Alan Lewis M.D., M.S.,

PHARMACOLOGY FOPS PHARMACOKINETICS
OF Professor,
• The study of the absorption,
Departments of Ophthalmology,
OPHTHALMIC Medicine, Pediatrics, and Molecular distribution, metabolism,
AGENTS and Human Genetics and excretion of a drug or
and the National School of Tropical agent
Introduction and Review Medicine
Houston, Texas

PHARMACOKINETICS Factors Affecting Drug Penetration Factors Affecting Drug Penetration

into Ocular Tissues into Ocular Tissues
• A drug can be delivered to ocular tissue:
– Locally: • Drug concentration and solubility: The higher
the concentration the better the penetration, • Surfactants: The preservatives in ocular
• Eye drop but limited by reflex tearing. preparations alter cell membrane in the cornea
• Ointment and increase drug permeability, e.g.,
• Viscosity: Addition of methylcellulose and benzalkonium and thiomersal
• Periocular injection polyvinyl alcohol increases drug penetration by
increasing the contact time with the cornea and • pH: The normal tear pH is 7.4; if the drug pH is
• Intraocular injection
altering corneal epithelium. much different, it will cause reflex tearing.
– Systemically: • Drug tonicity: When an alkaloid drug is put in
• Lipid solubility: Because of the lipid rich
• Orally environment of the epithelial cell membranes, relatively alkaloid medium, the proportion of
the higher lipid solubility, the more the the uncharged form will increase, thus more
• IM
penetration. penetration.
• IV

FLUORESCEIN FLUORESCEIN
Chemistry Dosage
● C20H1205, brown crystal ● Adults: 500-750 mg IV
● M.W. 322.3 e.g., 3 cc 25% solution
● Peak absorption 485-500 nm. 5 cc 10% solution
● Children: 1.5-2.5 mg/kg IV
● Peak emission 520-530 nm.

Richard Alan Lewis, M.D., M.S. Nov 2013 1

Ophthalmic Pharmacology

Needle Diameter Ideal Flow through a small

FLUORESCEIN
tube varies with the 4th power
Needle Outer Diameter Inner Diameter Side Effects
of the radius (r4)
Gauge mm mm
Gauge r r4
● Skin staining: 100% (6-12 hours)
18 1.270 0.838
20 0.3015 ~0.00826 ● Aqueous staining: 100% (8-24 hours)
20 0.908 0.603
● Urine staining: 100% (24-36 hours)
21 0.819 0.514
21 0.257 ~0.00436
23 0.641 0.337 0.00826/0.00436 = 1.895
25 0.514 0.260

FLUORESCEIN ANGIOGRAPHY FLUORESCEIN ANGIOGRAPHY FLUORESCEIN

Adverse Reactions Adverse Reactions Adverse Reactions
● Local Effects
Do not change with:
Reported with: - Extravascular
- Informed consent - Intravenous
● Topical phenylephrine
- NPO state - Intra-arterial
● Venipuncture
Systemic Effects
● Fundus photography
- Premedication ●
- Mild
- Dye concentration - Moderate
- Severe

FLUORESCEIN FLUORESCEIN FLUORESCEIN

Extravasation Extravasation Intravenous
● Think prevention ● Intense local pain
● Dull ache, ipsilateral extremity
● Warm, wet compress, - Duration: 20 - 45 minutes
Chemical thrombophlebitis
30 minutes Q.I.D. - Management: self-limited Duration: 3-10 days
● Examine site at 24°, 48° reassurance
Management: self-limited
cold pack
● If avascular, refer to plastic
● Dermal necrosis
surgeon

Richard Alan Lewis, M.D., M.S. Nov 2013 2

Ophthalmic Pharmacology

FLUORESCEIN FLUORESCEIN ANGIOGRAPHY FLUORESCEIN ANGIOGRAPHY

Intra-arterial Mild Adverse Reactions Mild Adverse Reactions

● Immediate INTENSE stain of ● Nausea and vomiting < 5% ● Transient

distal extremity ● Extravasation ● Rapid and complete
● PAIN! resolution
● Sneezing
- Duration: 1-24 hours ● No treatment required
● Pruritus
- Management: Cold, Analgesia

FLUORESCEIN ANGIOGRAPHY FLUORESCEIN ANGIOGRAPHY FLUORESCEIN ANGIOGRAPHY

Moderate Adverse Reactions Moderate Adverse Reactions Severe Adverse Reactions

● Transient ● Urticaria (1.2%) • Prolonged

Medical therapy required ● Syncope (0.3%)
●
Thrombophlebitis
• Intense therapy required
● Complete, if gradual, ●

resolution with no sequelae ● Local tissue necrosis • Threat to patient safety

● Nerve palsy • Variable recovery
Overall: 1.6%

FLUORESCEIN ANGIOGRAPHY FLUORESCEIN FLUORESCEIN ANGIOGRAPHY

Severe Adverse Reactions Toxicity Death
● Respiratory (1:3,800)
- Laryngeal stridor, edema
- Bronchospasm ● Phototoxicity to skin
- Anaphylaxis
● Cardiovascular
- Circulatory shock
(1:5,300) (Premature, jaundiced infant, Death rate: 1:220,000
- Myocardial infarction, arrest UV therapy: J Peds: 1985; 107)
● Neurological (1:13,900)
- Seizure
(Overall: 1:1,900)

Richard Alan Lewis, M.D., M.S. Nov 2013 3

Ophthalmic Pharmacology
FLUORESCEIN
Precautions
• Not approved for use in pregnancy
• No evidence for teratogenicity,
embryocidicity
• Not approved for use in children
• Renal insufficiency prolongs
elimination
• Diabetics should not confuse color
with reactions for glucose
ADVERSE REACTIONS
Management
● Trained personnel
● Emergency equipment
- Airway (oral, AMBU)
- O2 (mask, prongs cylinder)
- Parenteral fluids
(I.V. stand, fluids, sets)
- B/P cuff
- Drugs
FLUORESCEIN ANGIOGRAPHY
Informed Consent
Richard Alan Lewis, M.D., M.S. Nov 2013
FLUORESCEIN
Precautions
• Does NOT cross-react with
iodinated contrast dyes
• Avoid patients with prior
serious reactions to fluorescein
• Avoid historically risky patients
FLUORESCEIN ANGIOGRAPHY
Not routinely conducted
on pregnant subjects
DRUGS for ANAPHYLACTOID
REACTIONS
Diphenhydramine (Benadryl)
25-50 mg p.o., i.m., i.v.
Tripelennamine (Pyribenzamine)
25-50 mg p.o.
Fexofenadine (Allegra)
180 mg. p.o.
FLUORESCEIN
Prophylaxis: Nausea
Metoclopramide HCl
(Reglan) 20 mg IV
5 min before F/A
MANAGEMENT
Screening
● Consent form, especially children
History of prior allergies, asthma
●
- A negative history is no
guarantee of impunity
● History of recent change in angina,
uncontrolled hypertension,
cardiac arrhythmia
Most serious reactions
occur within minutes of
injection. Severe
anaphylactoid reactions
may develop as late as
one hour after injection.
4
Ophthalmic Pharmacology

INDOCYANINE GREEN INDOCYANINE GREEN

Therefore, if there is Description Formulation
any suspicion, the Tricarbocyanine dye with •Contains 5% Nal
patient should wait peak spectral •pH 5.5 - 6.5
and be absorption at 800-810 nm,
emission at 830-840 nm, •Unstable in
observed.
in blood. aqueous solution

INDOCYANINE GREEN INDOCYANINE GREEN INDOCYANINE GREEN

Chemistry Indications Dosage

● Ophthalmic angiography • 0.5 mg/kg (<2 mg/kg)

•C43H47N2NaO6S2 ● Cardiac output
• Adults: 40 mg in 2 ml
•M.W. 774.96 ● Hepatic function, blood flow solvent with 5 cc N.S.
flush

INDOCYANINE GREEN INDOCYANINE GREEN INDOCYANINE GREEN

Pharmacology
● Bound to plasma proteins
(albumin, 95%)
● Hepatic secretion to bile
Contraindications Adverse Reactions
• Anaphylaxis, urticaria
● Diluent contains Nal reported, without
● Avoid allergy to iodides
allergy to iodides
• 2 deaths reported

Richard Alan Lewis, M.D., M.S. Nov 2013 5

Ophthalmic Pharmacology
Iodine/Iodide Allergy
• NO objective evidence
demonstrates cross-
reactivity between
allergy to shellfish and
iodine sensitivity!
J. Emerg. Med. 2010: 39 (5): 701-707
VERTEPORFIN
Indication
Light-activated drug for
photodynamic therapy of
various subretinal
neovascularizations
VERTEPORFIN
Contraindications
• Porphyria
• Liver dysfunction
• Known hypersensitivity
Richard Alan Lewis, M.D., M.S. Nov 2013
INDOCYANINE GREEN VERTEPORFIN
Pregnancy
• Trade Name: Visudyne
• Safety in pregnancy, • Formula: C41H42N4O8
nursing not established
• No animal embryocidicity, • Isomers of benzoporphorin
teratogenicity studies • Molecular Weight: 718.8
VERTEPORFIN VERTEPORFIN
Metabolism Adverse Reactions
●Skeletal: back pain, 2-15%
• Liver excretion into ● Skin: photosensitivity (5 days)
bile, feces ● GI: nausea
• Half-life 5-6 hours ● CV: syncope, hypotension,
bradycardia
VERTEPORFIN VERTEPORFIN
Other Cautions Precautions
• Photosensitization,
• Pregnancy class C
~ 5 days
• Rats: anophthalmia
• Avoid extravasation
• Avoid nursing
• Matched laser 689 nm.
6
Ophthalmic Pharmacology
VERTEPORFIN
Cautions
● Avoid other photosensitizers
(thiazides, sulfas, antidiabetics
● 83 sec. treatment, exactly 15
min. after 10 min. infusion
PEGAPTANIB
Macugen
• Mechanism: An aptamer,
modified RNA oligonucleotide,
that adopts the 3-dimensional
conformation to bind to
extracellular VEGF165 inhibiting
its binding to VEGF receptors.
PEGAPTANIB
Macugen-Safety
• Pregnancy: Not studied
• Nursing: Not studied
• Children: Not studied
• Safety or efficacy not
proven beyond 2 years
Richard Alan Lewis, M.D., M.S. Nov 2013
PEGAPTANIB
• Trade name: Macugen
• Formula:
C294H342F13N107Na28O188P28
[C2H4O]n, where n = ~900
• Molecular Wt: ~50 kD
PEGAPTANIB
Macugen
• Dose: 0.3 mg intravitreous
• Frequency: Every 6 weeks
• Half-life: ~ 10 days
• Metabolism: Degraded by
nucleases
PEGAPTANIB
Macugen
• Supplied: in a prefilled,
single use, glass syringe,
with 0.3 mg Macugen,
packaged with 30 G x ½”
BD needle
PEGAPTANIB
Macugen
• Mechanism of Action:
Selective antagonist of
Vascular Endothelial
Growth Factor (VEGF)
PEGAPTANIB
Macugen
• Indication: ‘Wet’ macular
degeneration
• Contraindications: ocular
infections;
known sensitivity
RANIBIZUMAB
• Trade name: Lucentis
• Formula: recombinant
humanized IgG1 κ
monoclonal antibody
fragment
• Molecular wt.: 48 kD
7
Ophthalmic Pharmacology

RANIBIZUMAB RANIBIZUMAB
Lucentis Lucentis
• Indication: “Wet” • Dose: 0.5 mg intravitreous
macular degeneration • Frequency: q month x 4,
• Contraindications: then q 3 months
sensitivity; active • Half-life: 7 – 12 days
ocular infections

RANIBIZUMAB RANIBIZUMAB RANIBIZUMAB

Lucentis Lucentis Lucentis
• Mechanism of action: • Cautions: • Side Effects:
Binds to all receptor Transient elevation of subconjunctival
binding sites of VEGF-A, intraocular pressure; hemorrhage, pain,
preventing interaction of endophthalmitis; v. floaters, elevated IOP,
VEGF with its receptors. thromboembolic events (<4%) intraocular inflammation

BEVACIZUMAB BEVACIZUMAB BEVACIZUMAB

• Trade name: Avastin
• Formula: complete
humanized IgG
monoclonal antibody
• Molecular wt.: 149 kD
Avastin Avastin
• Dose: 1.25 – 2.5 mg.
intravitreous • Metabolism: ? Nucleases
• Frequency: every 4 weeks • Excretion: ?
• Half-life: 20 days (11-50 d)

Richard Alan Lewis, M.D., M.S. Nov 2013 8

Ophthalmic Pharmacology

BEVACIZUMAB BEVACIZUMAB BEVACIZUMAB

Avastin Avastin Avastin
• Indications: OFF LABEL: • Side Effects: risk of
• Mechanism of Action:
“Wet” macular bleeding
Binds competitively to
degeneration; CNV, NVG, • Cost: among the most
VEGF receptors blocking
PDR, ROP, C/BRVO, expensive drugs in the
VEGF’s activity
diabetic macular edema world, widely marketed!

EYLEA: Aflibercept (EYLEA)

Mechanism Potential Risks
EYLEA
Schedule • Failure to control CNV
• Soluble
“decoy- • Endophthalmitis
receptor” of • Intravitreous injection • Retinal Detachment
both VEGF-A
and Placental • Q 4 weeks x 3; then • Transient elevation of IOP
Growth Factor • Q 8 weeks for ~1 year • ?Thromboembolism?
(PlGF)

Aflibercept (EYLEA) Routes of Administration: Routes of Administration:

• Pregnancy Class C Topical
• Most ocular medications are
• Nursing mothers? delivered topically - maximizes
• Pediatric population? anterior segment concentrations
and minimizes systemic toxicity;
• Mutagenesis? • Drug gradient from tear reservoir to
corneal and conjunctival epithelium
• Carcinogenesis? forces passive absorption.
Topical - Drops
Factors affecting absorption:
• Drug concentration (limited by
tonicity) and solubility (aqueous
solution vs. suspension)
• Viscosity (increased contact time)

Richard Alan Lewis, M.D., M.S. Nov 2013 9

Ophthalmic Pharmacology
Routes of Administration:
Topical - Drops
• Lipid solubility: lipid-rich epithelial
cell membrane vs. water-rich
stroma
• pH and ionic charge: Most eye
drops are weak bases, existing in
both charged and uncharged
forms, enhancing absorption.
Routes of Administration:
Topical - Drops
• Tissue binding: proteins in the tears
and on the ocular surface may
bind drug making the drug
unavailable or creating a slow
release reservoir. This may affect
peak effect, duration of action,
and delayed local toxicity.
Routes of Administration:
Peri-ocular Injections
• Subconjunctival, subTenon’s,
peribulbar, and retrobulbar;
• Allow drugs to bypass the
conjunctival/corneal epithelial
barrier and reach therapeutic levels
in the posterior segment;
• e.g., anesthetic agents, steroids
Richard Alan Lewis, M.D., M.S. Nov 2013
Routes of Administration:
Topical - Drops
Surfactants: preservatives are
surface-active agents that alter
cell membranes in the cornea
and bacteria, increasing drug
permeability and preventing
bacterial contamination.
Routes of Administration:
Topical - Ungt.
• Increases contact time of drug with ocular
surface;
• Mixture of petrolatum and mineral oil;
• Water-soluble drugs are insolvent in the
ointment and are present as
microcrystals.
• The surface microcrystals dissolve in the
tears; the rest are trapped until the
ointment melts.
Routes of Administration:
Intra-ocular Injections
• Allow instant drug delivery at
therapeutic concentrations to
target site;
• Intracameral, e.g., antibiotics,
viscoelastics, miochol;
• Intravitreous, e.g.,
triamcinolone, Avastin, Lucentis
Routes of Administration:
Topical - Drops
• Reflex tearing: Ocular irritation
and secondary tearing wash out
of the drug reservoir in the tears
and reduce contact time with
cornea, especially when drops
are not isotonic, have non-
physiological pH, or contain
irritants.
Routes of Administration:
Topical - Ungt.
• Only drugs with high lipid
solubility and some water
solubility will get into
both tears and corneal
epithelium.
Routes of Administration:
Systemic
• Extent of drug bound to plasma proteins
also effects access of drug into eye - only
unbound form can pass blood-ocular
barrier.
• Bolus administration exceeds the
capacity of a drug to bind to plasma
proteins and so leads to higher
intraocular drug levels than with slow IV
drip
10
Ophthalmic Pharmacology

Routes of Administration: Sustained Release Devices MYDRIASIS

Sustained Release • These devices deliver
an adequate supply
of medication at a
• Devices available for steady-state level
• e.g.,
delivery of steroids, – Ocusert delivering
pilocarpine
[G., μυδριασις]
gancyclovir within – Timoptic XE delivering
timolol Dilation of the pupil
– Ganciclovir sustained-
vitreous cavity release intraocular
device
– Collagen shields

Routes of Administration:
Topical - Drops Dilating Agents
• One drop = 50 µl • Dependent on iris
• Volume of conjunctival cul-de-sac 7-10 µl
pigmentation
• To increase drop absorption:
- wait 5-10 minutes between drops • Mechanism: Inhibition
- compress lacrimal sac of iris constrictor and
- keep lids closed for 5 minutes after ciliary muscles
instillation

MYDRIASIS CYCLOPLEGIC AGENTS

CYCLOPLEGIA
• Atropine (0.5%, 1%)
• Blockage of cholinergic [G. κυκλος = circle,
• Homatropine (1%, 5%)
stimulation to sphincter + πληγη = blow, stroke]
• Scopolamine (Hyoscine)
ms. of iris, ciliary body Paralysis of
• Cyclopentolate (0.5, 1, 2%)
• Stimulation of iris dilator accommodation
ms. • Tropicamide (0.5, 1%)
(ciliary ms.)

Richard Alan Lewis, M.D., M.S. Nov 2013 11

Ophthalmic Pharmacology

Parasympatholytic Drugs CYCLOPENTOLATE HCl CYCLOPENTOLATE HCl

Chemistry
Mydriasis Cycloplegia Duration
• Available as
ATROPINE 30 min. 60 min. 10 – 14 days
- Cyclogyl • Anticholinergic,
- Ak-Pentolate, inter alia
• Parasympatholytic
HOMATROPINE 10 – 30 min. 30 – 90 min. 2 – 4 days

• 0.5%, 1.0%, 2.0% coll.

SCOPOLAMINE 40 min. 40 min. 2 – 6 days

CYCLO- 20 – 30 min. 15 – 45 min. 12 – 24 hrs

PENTOLATE

CYCLOPENTOLATE HCl CYCLOPENTOLATE HCl CYCLOPENTOLATE HCl

Action Toxicity Side Effects
• Mydriasis • Facial flushing
• Irritation with
- Onset: 15 – 30 minutes • Wandering, irrelevant speech
concentration
- Duration: 24 hours • Disorientation, hallucinations
• ↑ IOP in open angle
• Cycloplegia • Psychosis
glaucoma
- Onset: 15 – 45 minutes • Ataxia, restlessness
• Angle closure glaucoma
- Duration: 24 hours • Grand mal seizures

CYCLOPENTOLATE HCl CYCLOPENTOLATE HCl TROPICAMIDE

Allergy Guidelines Chemistry
• Use lowest concentration
• Irritation, injection
• Avoid repetition • Anticholinergic,
• Lacrimation,
mucoid discharge • Avoid seizure-prone • Parasympatholytic
infants, elderly
• Atopic dermatitis
• Use punctal occlusion

Richard Alan Lewis, M.D., M.S. Nov 2013 12

Ophthalmic Pharmacology
TROPICAMIDE
• Available as
- Mydriacyl
- Tropicacyl, inter alia
• 0.5%, 1.0% collyrium
TROPICAMIDE
Toxicity
• Rare, due to brief action
• Cyanosis
• Muscle rigidity
• Vasomotor instability
PHENYLEPHRINE
Clinical Effects
• Rapid onset
• Virtual absence of
cycloplegia
• Accentuates effect of
mydriatic
Richard Alan Lewis, M.D., M.S. Nov 2013
TROPICAMIDE TROPICAMIDE
Action Side Effects
• Mydriasis
- Onset 15-30 min. ● Irritation on instillation
- Duration 4-6 hours ● ↑ IOP in open angle glaucoma
• Cycloplegia ● Angle closure glaucoma
- Onset 20-30 min. ● Better mydriatic than cycloplegic
- Duration 4-6 hours
PHENYLEPHRINE PHENYLEPHRINE
• Chemistry: α1 adrenergic
● Available as stimulator, agonist
- NeoSynephrine (radial iris fibers)
- Ak-Dilate • Action:
- Mydfrin - Mydriasis
- Efricel, inter alia Onset: 10-20 min.
Duration: ~ 3°
● 2.5%, 10% collyria
- Vasoconstriction
PHENYLEPHRINE PHENYLEPHRINE
Side Effects
• Other Actions:
• Irritation on instillation - Reduced aqueous inflow
- Reduced resistance to
• Angle closure glaucoma
outflow
- Stimulation of dilator ms.
13
Ophthalmic Pharmacology

PHENYLEPHRINE PHENYLEPHRINE PHENYLEPHRINE

Toxicity
• 1 gtt. 10% coll. = 3.3-6.7 mg.
• Enhanced absorption in
inflamed eyes
Toxicity
• Sudden systemic hypertension
(babies)
• Ventricular arrhythmias
• Myocardial infarction
Guidelines
• Use punctal occlusion
• Do not use in patients on
MAO inhibitors or tricyclic
antidepressants
(e.g., Parnate, Tofranil, Elavil,
Sinequan).

PHENYLEPHRINE DAPIPRAZOLE
Guidelines DAPIPRAZOLE
Trade Name [Rev-Eyes]
• Use cautiously in hypertension,
cardiac disease, aneurysm
Rev-Eyes® • C19N27N5HCl
• Use 2.5% coll. in infants,
elderly • M.W. 361.93
• Approximately gtt.1/eye/hour

DAPIPRAZOLE DAPIPRAZOLE DAPIPRAZOLE

Description Pharmacology
Now available through
selected compounding • α-adrenergic smooth
α-adrenergic muscle blocker
pharmacies
(e.g., Leitner’s Pharmacy and
blocking agent • Induces miosis by
Compounding Center, San Jose, CA dilator muscles

Richard Alan Lewis, M.D., M.S. Nov 2013 14

Ophthalmic Pharmacology

DAPIPRAZOLE DAPIPRAZOLE DAPIPRAZOLE

Pharmacology Indications Dosage
• Reconstituted as
• No action on ciliary ms. Iatrogenic mydriasis
0.5% collyrium
• Minimal effect on by adrenergic
(or parasympatholytic) • gtts ii O.U.;
sphincter ms.
agents repeat after 5 min.

DAPIPRAZOLE DAPIPRAZOLE DAPIPRAZOLE

Pregnancy
• Safety in pregnancy,
nursing not established
• Not embryocidal,
teratogenic in rats,
rabbits
Pediatrics Contraindications
• Hypersensitivity
Safety and efficacy • Strong parasympatholytic
not established agents
• Use only once/week/pt.

TOPICAL ANESTHETICS TOPICAL ANESTHETICS PROPARACAINE

• Proparacaine (Alcaine, ● Available as
• Mechanism of Action: Ophthetic, Fluoracaine, inter alia) - Ophthaine
- Reversible block, • Benoxinate (Fluress) - Aphthetic
competitive inhibition of ACh • Tetracaine - Ak-taine
- Decreased membrane
• Cocaine - Alcaine
permeability to Na+ flux
(1% - 4% as anesthetic) ● 0.5%

Richard Alan Lewis, M.D., M.S. Nov 2013 15

Ophthalmic Pharmacology
TOPICAL ANESTHETICS
• Onset: 5-30 sec.
• Duration:
- Varies with concentration,
frequency of instillation
- Generally, 20-30 min.
TOPICAL ANESTHETICS
Epithelial Toxicity
Minimal: Lidocaine (2-4%)
Maximal: Cocaine (4-20%)
PROPARACAINE
Allergy
• Rare;
• No cross-reaction with
tetracaine, benoxinate
Richard Alan Lewis, M.D., M.S. Nov 2013
TOPICAL ANESTHETICS TOPICAL ANESTHETICS
Side Effects Maximum Effective Concentrations
• Stinging on instillation Proparacaine 0.5%
• Suppression of reflex Tetracaine 1%
blinking Lidocaine 4%
• Increased corneal Cocaine 20%
permeability to drugs Benoxinate 0.4%
TOPICAL ANESTHETICS
PROPARACAINE
Toxicity
Onset: 5-20 sec.
• Epithelial punctate keratopathy
(ave. ~13 sec.)
• Retardation of epithelial healing
• Idiosyncrasy Duration : 15-25 min.
• Allergy: exfoliative dermatitis Irritation: minimal
PROPARACAINE Fluorescein – Topical
Toxicity • Available as drops or
strips
● Punctate epithelial keratopathy • Uses: stain corneal
● Stromal edema (after 5-10 min.)
defects and abrasions,
applanation tonometry,
● Suppression of reflex blink;
detecting wound leak,
NLD obstruction
drying • Caution:
• Stains soft contact lens
● Suppression of epithelial • Fluorescein drops can be
contaminated by
regeneration Pseudomonas sp.
16
Ophthalmic Pharmacology

ROSE BENGAL GLYCERIN, USP GLYCERIN

• Stains devitalized epithelium
• Uses: Severe dry eye,
herpetic keratitis
Glycerol
• Action: Osmotic agent
• Chemistry: Trihydric Alcohol
- Hydroscopic
(CH2OHCHOCH2OH)
• Colorless viscous liquid
- Deturgesces
• Miscible with H2O, EtOH
corneal edema
• Used in 50-75% conc. (aqueous) • Onset: 1-2 min.

GLYCERIN GLYCERIN GLYCERIN

Side Effects Toxicity Advantages

• Burning pain on instillation • Inexpensive

Rare, topically • Use as gonioscopic
• Transient action (topical)
lubricant

Richard Alan Lewis, M.D., M.S. Nov 2013 17