(E) Diagnostic and Therapeutic Modern Pharmacology

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OPHTHALMIC

DIAGNOSTIC
MEDICATIONS
DR.PREETI PATEL
WHICH CLASSES OF
DRUGS?
Cycloplegics

Mydriatics

Anesthetics
WHY USE DIAGNOSTICS?
Ocular media and fundus examination

Enhancing retinal photography; optical coherence


tomography

Refraction through cataracts when pupils are small

Cycloplegic refraction

Techniques where anesthesia is required


CYCLOPLEGIA

It is the paralysisof the ciliary


muscle of the eye, resulting in loss
of accommodation.
CYCLOPLEGICS
Cycloplegics work by binding to effector sites in the ciliary
muscle thereby blocking action of acetylcholine.

Pupillary dilation is an (unwanted) side effect and its


onset precedes cycloplegia.

The optometrist should ensure there are no angle


anomalies before instillation of cycloplegic drop.
CYCLOPLEGICS
Cycloplegics are most often used in children in
the presence of esotropia (eyes turns inward) or
esophoria or when latent hypermetropia is
suspected.

Another use is to impose penalization of a


dominant eye in amblyopia.
COMMON CYCLOPLEGIC
DRUGS
Atropine

Cyclopentolate

Tropicamide
ATROPINE
Atropine is a strong cycloplegic agent.

Atropine Sulphate is used 0.5% and 1% as eye


drops; and 1% eye ointment.

Muscarinic antagonist.

Peak effect of the drug is in 2-3 days.

Duration is 7-10 days.


TROPICAMIDE
Tropicamide (Midriacyl) is also a short-duration
cycloplegic available in 0.5% and 1% solutions.

For young adults 3 to 4 drops of the 1% solution,


separated by a few minutes, will bring about full
cycloplegia in about 30 minutes.

Recovery occurs within 6-8 hours.


CYCLOPENTOLATE
Short duration cycloplegic agent available in
0.5% and 1% solutions.

Cycloplegia occurs within 30 to 45 minutes and


persists for as long as 24 hours.
For children aged 6 to 16, one drop of 1%
solution
For adults one drop of 0.5% solution.
SIDE EFFECTS
Blurring of vision

Patient cannot read

Photophobia

Dry mouth

Flushing of the face

Fever
CONTRAINDICATIONS
 abnormally shallow anterior chamber

dislocation or subluxation of the


crystalline lens.
MYDRIATICS
Mydriatics dilate the pupil to facilitate a more thorough
examination of the fundus, lens periphery and vitreous.
They are mostly used on elderly patients, as older
pupils are usually smaller and lens opacities and
abnormal retinal conditions are not uncommon.
MODE OF ACTION
 The pupil dilator muscle is innervated by the
sympathetic nervous system and
sympathomimetic drugs will cause a
contraction of the dilator muscle causing
mydriasis. Sympathomimetic drugs also have
little effect on accommodation.
MYDRIATICS USES
Mydriatics are used to examine properly the ocular
media and ocular fundi

Retinoscopy through small pupil and cataract

Recent onset of floating vitreous opacities, especially if


accompanied by the symptoms of flashing light.

Fundus photography.
ANTIMUSCARIANIC
MYDRIATICS
TROPICAMIDE
1. Tropicamide is the antimuscarinic mydriatic of choice today.

2. Normally available in 0.5% and 1.0% strengths, the weaker solution is


used most often for mydriasis; the 1% strength is used for cycloplegia.

3. Tropicamide is quick in onset and short in duration (Onset in 20- 30


minutes and duration of cycloplegic effect is 6-8 hours)
All cycloplegics can be used as mydriatics but the
effect is usually too long lasting. The following
have been used in the past:
CYCLOPENTOLATE
The mydriatic concentration of cyclopentolate is 0.1%
(compared with 0.5% and 1.0% for cycloplegia).
However, this strength is no longer available and if
cyclopentolate is used as a mydriatic then significant
cycloplegia will accompany its use.
HOMATROPINE
At one time, homatropine was the principal
mydriatic. The mydriatic effect commences in
10–20 min and is maximal in 30–40 min.

Recovery takes the same time as cyclopentolate if a


miotic is not used, but it can be as prolonged as 3
day.
CONTRAINDICATIONS
Patients using pilocarpine for the treatment of glaucoma

Narrow-angle glaucoma

Abnormally shallow anterior chamber (due to the risk of angle-


closure glaucoma)

Dislocation of the crystalline, or an intraocular lens

An intraocular lens of the anterior chamber or iris-supported type.


SYMPATHOMIMETIC
MYDRIATICS
Phenylephrine is the only sympathomimetic
mydriatic in regular use. It is available in a
variety of strengths but 2.5% and 10.0% are
most often used.
PHENYLEPHRINE
Mydriasis commences in about 10 min and is maximal in 30
min; the mydriasis lasts for several hours.

There is little doubt that sympathomimetics produce less effect


on accommodation than antimuscarinics, and some authors
(Kanski 1969) suggest that phenylephrine produces mydriasis
without any cycloplegic effect at all.
ANESTHETICS
Local anaesthetics are chemical agents that
reversibly block the transmission of nerve
impulses along sensory fibres.
INDICATIONS FOR USE
Foreign body removal

Tonometry

Contact lens fitting

Gonioscopy

Certain diagnostic procedures like


Schirmer ’s test.
ANESTHETICS
Among the topical anaesthetics, the most widely used
agents are proparacaine hydrochloride 0.5% (Alcaine),
benoxinate 0.5% and tetracaine 0.5%.

 The instillation of 1 drop of these compounds renders the


corneal epithelium insensate within 15 seconds.

Reapplication will enhance the anaesthetic effect


Fluorescein dye

Corneal epithelial defects & corneal ulcers.


Applanation tonometry -Goldmann tonometer/Perkins
hand-held tonometer
Seidel's test: Concentrated fluorescein dye
Jones dye test for assessment of lacrimal passage functional
potency.
Fundus fluoroscein angiography: 10%-20% i/v
Fluorometry
Tear film break up time(TBUT)
CORNEAL EPITHELIAL DRY EYE
DEFECT

APPALANTION SEIDELS TEST POSITIVE


TONOMETER
Rose Bengal dye
Rose bengal is actually a derivative of fluorescein
Stains the devitalized cells only
Unlike fluoroscein, it’s a true histological stain which binds strongly
and selectively to cellular components
1% liquid rose bengal dye via dry impregnated paper strips

SJOGREN’S SYN-
DRY EYE KERATOCONJUNTIVITIS SICCA
Lissamine green
Stains membrane-damaged or devitalized cells- GREEN
There is no stinging or discomfort such as that associated with
rose bengal.
Stains the edges of the dendritic ulcer while fluoroscence
stains the central bed
Concentration of 1% lissamine strips.

DRY EYE DENDRITIC ULCER


OPHTHALMIC THERAPEUTIC
MEDICATION
Ocular infections
Anti bacterials Anti fungals Anti virals Anti Parasitic:
acanthamoeba

 Aminoglycosides  Polyenes- Natamycin


Acyclovir
 cephalosporins  Azoles Ampho B
Valacyclovir
 Fluoroquinolone  Polyhexamethyl
Trifluridine
 Macrolides Gancicyclovir biguanide 0.02%
 Sulfonamides Imidazole Triazole Chlorhexidine
Cidofovir
Others: Foscarnet 0.02%
Chloramphenicol  Hydrogen peroxide
Miconazole Fluconazole Benzalkonium
ketoconazole Itraconazole chloride(BKC)
voriconazole
Anti Bacterials
Anti Bacterials MOA Drugs available

Aminoglycosides Protein synthesis inhibitors Gentamycin, Tobramycin & Amikacin

Flouoroquinolones DNA gyrase inhibitors Ciprofloxacin, gati, moxi,


besifloxacin etc

Macrolides Protein synthesis Azithromycin ,


inhibitors erythromycin

Sulphonamides Anti folate antibiotics Chloramphenichol,


sulphaacetamide

Cephalosporins Cell wall synthesis inhibitors cefazoline


Aminoglycoside (cont)
Drugs Dosage Indication Side effects

Gentamycin 0.3% every four hrs Conjunctivitis, keratitis, Ocular burning & irritation,
corneal ulcers, dacrocystitis non specific conjuntivitis.
etc Pregnancy & child

Tobramycin 0.3% every four hrs Conjunctivitis, keratitis, Tearing, swelling of eye,
corneal ulcers, dacrocystitis stinging or blurred vision
etc in children

fortified Amikacin 1.25%- 2.5% Severe bacterial Ototoxicity


infection Nephrotoxicity
Eg- mycobacterium Pregnancy-D
chelonae keratitis
Fluroquinolones
Generic name formulations Toxicity Indications

Ciprofloxacin 0.3% solution Hypersensitivities Drug Conjunctivitis


0.3% ointment related corneal deposits Keratitis Corneal
ulcer blephritis
Dacrocystitis

Ofloxacin 0.3% solution Hypersensitivity Conjunctivitis Corneal


ulcers
Generic name formulations Toxicity Indications

Gatifloxacin 0.3% solution Hypersensitivity Conjunctivitis, post op


& pre op prophylaxis,
corneal pathologies etc

Moxifloxacin 0.5% solution Hypersensitivity same as above

Besifloxacin 0.6% suspension Redness, blurring of


vision, pain, irritation etc Same as above
Macrolides
MOA: Inhibits Protein synthesis by inhibiting the
translocation on 50S ribosome
Generic name formulations Toxicity Indications

Azithromycin 1% ointment Hypersensitivity Superficial infection


involving cornea and
conjunctiva

Erythromycin 0.5% ointment Hypersensitivity Superficial infection


involving cornea and
conjunctiva
Sulphonamides
MOA: These are Anti folate antibiotics which inhibit folic
acid synthesis
Generic name Formulations Dosage Indications

Chloramphenicol 0.5% solution 4-6 times daily Conjuntivitis


Keratitis

Sulfacetamide 10%, 15% and Two hourly (for Conjuntivitis, trachoma


sodium 30% w/v trachoma) and other superficial
ocular infections
Antifungal agents
Drug Administration Toxicity Indications
P Natamycin 5% suspension Hypersensitivity Yeast & fungal
O 2hourly Irritation keratitis
L Amphoteracin B 0.1-0.5% solution Hypokalemia Infusion Yeast & fungal keratitis
Y 0.8-1mg related toxicity and endophthalmitis
E subconjuctival
N 5 mcg intravitreal
S
Ketoconazole Topical 1-2% Allergic rash Yeast keratitis &
A Oral 200-600mg/d teratogenic endophthalmitis

Z
Fluconazole Topical 1-2% Oral Allergic rash Yeast keratitis &
200mg/d teratogenic endophthalmitis
O

L Itraconazole Topical 1-2% Poor penetration so Yeast & fungal keratitis


Oral 200-400 mg used in combination & endophthalmitis
E
S Voriconazole Extemporaneously No damage to the Invasive
prepared eye Aspergillosis
Antiviral agents
Generic name Route of Ocular toxicity indications
administration

Trifluridine Topical 1% Punctate keratopathy Herpes simplex


solution hypersensitivity keratitis,
keratoconjtivitis

Acyclovir Oral(200mg cap/ Herpes zooster


Gua- 800mg tab) ophthalmicus, HS
nosine iridocyclitis
nucleo
side Valacyclovir Oral (500- HS Keratitis
analog 1000mg) HZ ophthalmicus
yes Famicyclovir Intravenous HS Keratitis
intravitreal HZ ophthalmicus
Vidarabine 3% ointment Lacrimation, foreign HS Keratitis
body sensation, photo- HZ ophthalmicus ACUTE
phobia etc &RECURRENT
Anti Parasitic : Protozoal keratitis
Acanthamoeba Keratitis
Specific treatment include
Topical agents DRUGS

Diamidines Propamidine isethionate 0.1%


Hexamidine 0.1%

Biguanides Polyhexamethyl biguanide 0.02%


Chlorhexidine 0.02%

Aminoglycosides Neomycin
paromycin

Imidazoles Clotrimazole Miconazole


Drugs for CMV RETINITIS
Cytomegalovirus infection can occur in general population but CMV
retinitis occur usually with advanced immunosuppression (CD4+
cells<100/mm3)
Treatment

Anti viral agents Route Toxicity


Ganciclovir & Topically, IV, Headache, convulsion,
valganciclovir intravitreal behavioural change
Cidofovir intravitreal Vitritis, hypotony &
vision loss
Foscarnet Intravitreal, IV Headache, tremors etc
Fomiversen Intravitreal Iritis, vitritis, cataract & rise in
IOP
Ocular inflammation
Inflammation is a characteristic response of the mammalian
tissue to injury

Anti inflammatory agents:


1. Steroidal Anti Inflammatory Drugs
2. Non-Steroidal Anti Inflammatory Drugs
Corticosteroids
CLASSIFICATION

CLASSIFICATION Steroid

Short acting Hydrocortisone, cortisone, prednisolone

Intermediate acting Triamcinolone , fluprednisolone

Long acting Dexamethasone & Betamethasone


Steroidal Anti Inflammatory agents
Corticosteroids Strength (%) Indications Dosage

Prednisolone 0.125 & 1.0 Steroid responsive In tapering doses


acetate, inflammatory condition
of conjunctiva,
prednisolone cornea & ant seg of eye
soduim phophate like Uveitis, allergic
Dexamethasone 0.1 conjunctivitis, SPK, In tapering doses
episcleritis, Corneal
sodium phosphate abrasion, ocular
inflammation, corneal
Fluromethalone 0.1 injury from diff burns, In tapering doses
acetate optic neuritis etc

Loteprednol 0.5 & 0.2 In tapering doses


etabonate

Methyl 1mg/kg IV
prednisolone
Side effects of steroids
OCULAR SYSTEMIC

Glaucoma Peptic ulcer Hypertension


Cataract increases blood sugar
Activation of infection Activation of TB
Delayed wound healing Osteoporosis
Non-Steroidal Anti Inflammatory agents
NSAIDS OCULAR USES
Indomethacin To prevent miosis & CME after cataract sx
INDOLE DERIVATIV
Diclofenac Post operative inflammation
ARYL ACETIC ACID
Ketorolac Seasonal conjunctivitis, CME after cataract sx
DERIVATIVE

ARYL PROPIONOC ACID Nepafenac It’s a prodrug, 6 times faster permeation


DERIVATIVE Flurbiprofen To counter unwanted intraoperative miosis during cataract
surgery
Piroxicam Activity is comparable & tolerance is better than diclofenac
ENOLIC ACID sodium(0.1%)
DERIVATIVE

ANTI-INFLAMMATORY, ANALGESIC, ANTI-PYRETIC, FREE RADICAL


SCAVENGING ACTIVITY etc
Ocular anti Allergic drugs
Classification Drugs Allergy
Anti histamines Pheniramine, antazoline, Seasonal allergic
emedastine etc conjuntivitis(SAC) Perennial
allergic conjuntivitis(PAC)
Vernal keratoconjunctivitis
Mast cell stabilizers Cromolyn sodium, nedocromil, (VKC)
pemirolast, ketotifen Atopic kerato
conjunctivitis( AKC) Giant
Papillary conjunctivitis(GPC)
Dual action anti allergic Olapatidine,, azelatine &
drugs epinastine
NSAIDS Ketorolac
Corticosteroids Loteprednol,
fluromethalone,
dexamethasone,
prednisolone etc
ANTI GLAUCOMA DRUGS
AIM OF TREATMENT

DECREASE THE INCREASE AQUEOUS


FORMATION OF IOP DRAINAGE

-Beta blockers -Prostaglandins


-Alpha agonist -Topical miotics
-Carbonic anhydrase inhibitors
Cholinergics
MOA : stimulates the muscarinic receptors producing increased
aqueous outflow.

Indiacation : pupillary block glaucoma

Dosage : Pilocarpine 0.25%, 0.5%


one drop two to three times a day
Anti cholinergics
MOA : block the response of response of acetylcholine at the receptor

Agents :
1. Atropine
2. Cyclopentolate
3. Tropicanamide
 Not used routinely in glaucoma treatment
 Use: Inflammatory & Malignant glaucoma
Alpha adrenergics agonist
MOA: stimulate alpha 2 receptors in the ciliary epithelium and
thereby decrease the rate of aqueous production.

Agents :
1. Dipivefrin 0.1%, one drop 2-3 times a day
2. Brimonidine 0.15% one drop 2-3 times a day
Beta blockers
Mechanism of action: lower IOP by reducing aqueous formation
Also reduces ocular outflow

Non selective betablocker Selective beta 1 blockers


Timolol maleate betaxolol
Levobunolol
Metipranolol
Carteolol
20-35% fall in IOP within 1hr and last for 12
hours.
TIMOLOL 30% patients- additional
medications

Less efficacious than Timolol

BETAXOLOL Protective effect on retinal neurons


by blocking calcium channels
Adverse effects

Ocular Systemic
Stinging, redness & Bronchospasm in
dryness of eyes asthamatics & COPD
Corneal hypothesia patients
Allergic Bradycadia and accentuation
blephroconjuntivitis of heart block
Blurred vision
Prostaglandins
First line medical therapy for open angle glaucoma

PGF2 alpha analogs

Good efficacy, once daily, No systemic sideeffects

MOA: facilitate aqueous outflow through uveoscleral outflow pathway


Agents :
1. Latanoprost : 0.005% HS
2. Bimatoprost: 0.03% HS
3. Travoprost

 Adverse effects:
 Ocular irritation & pain
 Blurring of vision
 Increased iris pigmentation
 Macular edema
Immunosuppressive & Anti Mitotic
agents
 Agents commonly used
1. 5- fluorouracil
2. Mitomycin C

 Indications :
 Intermediate uveitis
 Peripheral ulcerative keratitis
 Ocular surface squamous neoplasia(OSSN)
 Trabeculectomy
 GVHD
Immunomodulators
TOPICAL CYCLOSCPORINE

-Approved for the treatment of Chronic dry eye associated with


inflammation.

Decreases inflammatory markers in lacrimal gland & increases tear


production
Angle closure glaucoma
Hypertonic Mannitol 20% IV infusion- 1.5-2 g/kg

Acetazolamide 0.5g iv followed by oral twice daily started


cncurrently

DEFINITIVE
Miotic : Pilocarpine 1-4% TREATMENT:
Surgical or Laser
Iridotomy
Timolol 0.5%

Latanoprost
Ocular Lubricants
Polymer composition of Artificial tears

Hydroxymethyl cellulose/ carboxy methyl cellulose

Carbomers (polyacrylic acid)


Hypomellose (hydroxypropylmethyl cellulose)

Liquid paraffin

Polyvinyl alcohol

Polyvinyl pyrrolidone

polycarbophil

Indications: Ocular irritation


Dry Eyes
Preservatives
Ophthalmic solutions and ointments must be sterile so wide variety of
preservatives are used for anti- microbial activity

PRESERVATIVES
Benzalkonium chloride
Chlorbutol
Phenyl mercuric nitrate
Stabilized oxychloro compound
Thiomersal
Chlorhexidine
Sorbic acid
Adverse effects of preservatives
Toxic to precorneal tear film and epithelium, thus impedes
epithelial healing and disrupting the tear film
Direct cellular damage
Reduces oxygen utilization of cornea
Hypersensitivity reaction
1. Papillary conjunctivitis
2. Punctate keratitis
3. Corneal edema

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