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M.Djamaludin,dr.,SpFK.,M.

Kes Achmad Yani School of Medicine

A.TOPICAL ANESTHETICS
The efficacy of TA is usually determined by

ability to suppress corneal sensitivity. Concentration for each drug is obtained beyond which no further increas in activity occurs

Maximum effective concentration


The concentration at which this maximum efficacy

occurs. Increasing the concentration of the anesthethic beyond the MEC serves no useful purpose but increases the risk of local and systemic toxicity.

MEC of Procaine,Tetracaine, and Cocaine are 0.5 %,

1 % and 2.0 %. In clinical practice,however,the OEC(Optimum Effective Concentration) may be less than MEC.

For instance,0.5 % tetracaine is less irritating to the

eye than the MEC 1% and thus is better suited for clinical use.
Combination of two or more local anesthetics dose

not produce and additive effect,but it dose increase the risk of side effects and so is contraindicated.

Toxicity
It is uncommon for topically applied anesthetics,

benoxinate and tetracaine,to cause mild local stingging or burning after installation.
In some patients,especially who over 50 years.......

a diffuse desquamation of corneal epithelium;Punctate keratitis

Typical manifestation of systemic intoxication


CNS :

Excitement,restlesness,headache,delirium,convulsion CVS :Rapid and irregular pulse Ocular : Dilated pupils GIT :Nausea,vomitus,abdominal pain Note:Acute systemic (10 drops of a 4% sol)

Hypersensitivity.
Ocular
Allergic episode occur mainly with use of the ester

group of anesthetics,that is,the commonly used for topical. Lidocaine,mepivacaine and bupivacaine,less frequently than with the ester other group. Systemic anaphylactic reactions topical anesthetics are extremely rare

Psychomotor Reactions.
Psychomotor reactions such as vasovagal syncope may

usually occur from anxiety related to the office visit\


Respiration and cardiovascular status should be

monitored to eliminate drug-induced anaphylaxis as a possible cause of the collapse

Prevention of Adverse Systemic Reactions


Adverse reactions to local anesthetic drugs usually

occur depend dose. Limit the dosages of drugs to those comparable with effective anesthesia without substantial risk of systemic toxicity

INDICATIONS
1.Operative
2.Remove corpus alineum

ROUTE OF ADMINITRATION
1.Injected 2.Topical

CONTRAINDICATIONS
Hypersensitivity
Liver disease Concommitans medications

Dry Eye Testing


Perporatory Ocular Injury Self Administration of Topical Anesthetics

Mechanism of pain and analgesia


Primary eye care practitioners often encounter

patients who experiencing substantial pain from an underlying ocular disease. For example patients with corneal or conjunctival foreign bodies,abrasions or traumatic hyperemia usually complain of pain as their primary complain

Cocaine
Cocaine exhibits both anesthetic and adrenergic

activity The usual concentration for ocular1 topical 1% t0 4% but the 10 % solution is often used,for the diagnosis of Horners syndrome One drop of 2 % solution produces exellent corneal anesthesia within 5 to 10 minutes

Cocaine is used as a nasal spray or in

dacryocystorhinostomy. Cocainogic due to its adrenergic effects (blocks reuptake of norephinephrine).

Cocaine contraindicated to
Systemic hypertension Retinal detachment surgery

Routine opthalmoscopy
Gonioscopy Angle close glaucoma (mydriatic effect)

Tetracaine
Ester PABA
Available 0,5

% solution

Intensity,DOA comparable with proparacaine and

benoxinate Sol. 1 % successfully to provide anesthesia during phacoemulsification cataract surgery and intraocular lens implantation

Benoxinate (Flurasafe)
It most commonly combined with sodium fluoescein 0.25 %,but recently it was combined with 0.35 % disodium flurexon Primary used for implanation tonometry. Side effects: Stingging,burning,increase or decrease corneal thickness and allergic reaction.

Proparacaine
C:0.25 % - 0.5 % solution,both with or without sodium

fluorocein The OOA,intensity,and DOA f anesthesia are similar with tetracain and benoxinate. It produce little or no discomport or irritation on instillation and therefore readily accepted by more patient. Allergic reaction: Characterized conjunctival hyperemia and edema,edematous eyelids,and lacrimation. Corneal tickness instally can occur

B.OCULAR HYPOTENSIVE DRUGS


OVERVIEW
Glaucoma can often lead to visual impairment and

even blindess. Management of these disorders is almost always directed at the existing intraocular pressure (IOP) lowering This can be accomplished eithher pharmacologically or surgically by decreasing aqueous production or by increasing aqueous outflow

Drugs classification
1.Prostaglandin Analogues
Latanoprost Travoprost Bimatoprost

Prostaglandin Combination Compunds Prostaglandin and B-blocker

2.Beta-Adrenergik Antagonist
Timolol
Levobunolol Betaxolol

Metipranolol
Carteolol

3.ADRENERGIC AGONIST
Adrenalin
Noradrenalin

Latanoprost (Xalatan)

Prostaglandin were originally discovered in the eye as mediators of the ocular inflamatory response and most of the preliminary research focused on their potensial role in uveitis and other inflamatory disease.

Latanaprost demonstrates sufficient ocular

hypotensive activity with minimal side effect. Latanaprost is an analogue of prodrug prostaglandin PGF2a-isopropyl ester.When instilled topically into human eye .Latanaprost is converted by corneal esterase into lanataprost acid, which exerts its biological activity at the FP receptor on the cilliary muscle.(FP is recepor for PGF2a).

As a selective FP receptor agonist ,latanaprost appears

to exert its ocular hypotensive effects exclusively by increasing uveoscleral outflow. In long-term clinical trial ,latanaprost has been shown to be at least as effective as timolol maleat,betablocker in reducing IOP Latanaprost should be dosed only once daily in the evening or bed time.

The additive ocular hypotensive effects achived with

combination of latanaprost and timolol are greater than than when brimonidine, dorsolamide, or pilocarpine is used with timolol. And the effect achived with miotics and pikocarpine seems to be most effective when the bed time dosed is administered 1 hour after lantanaprost Latanaprost available in concentration 0.005 % peserved with 0.02 benzalkonium chloride (BAC)

Side Effects
Iris color darkning
Increased eyelid pigmentation Ypertrichosis

Conyunctival hyperemia
Allergy

Cystolid macular edema


Anterior uveitis Punctate corneal erosions

Corneal pseudodendrites

Contraindications
Lanaprost may be relatively contraindicated in

patients with a history of uveitis or prior incisional ocular surgery. Previous episodes of herpes simplex virus keratitis Lanaprost should be used cautiously after cataract surgery in patients who have risk favouring the development of CME(Crystoid Macular Edema).

Travoprost (Travatan)

Travoprost is a PGF2a analog used for treatment of patients with open-angle glaucoma or ocular hypertension.Its mechanism of action is similar to that of latanaprost. The drugs is formulated as an aqueous solution in a concentration of 0.004 % preserved with 0.015 % BAC

Bimatoprost (Lumigan).
Bimatoprost is generally considered to be part of the

prostaglandin family of ocular hypotensive analogues. Bimatoprost is formulated as a 0.03 % solution in citrate/phosphate buffer preserved with BAC (0.005 %)

Bimatoprost dosed once daily provider lower mean


IOP than doses timolol used twice dail Side Effect. Similar to latanaprost and travoprost,bimatoprost reported to cause changes to pigmented tissues Contraindications: Similar with lanataprost

Prostaglandin combination Compounds


Prostaglandin and B-blocker
These products include a combination of latanaprost

or travanost with timolol Studies have demonstrated comparable efficacy and in the case of travoprost-timolol combination,a favorable IOP reduction product and the separate compounds administered concomitantly.

2.B-ADRENERGIC ANTAGONIST
Timolol

Given topically induced a significant and long lasting ocular hypotension.Mean decreases in IOP are approximately 25 %. The ocular hypotensive efect of timolol is greater than of pilocarpine Drug tolerance of timolol has been described

Clinical uses 1.Primary open-angle glaucoma 2.Ocular hypotension 3.Secondary glaucoma 4.Prophylactic in IOP after laser iridotomy,posterior capsulotomy,and cataract surgery Timolol is supplied as 0.25 and 0.5 % sterile ophthalmic solution of maleate salt. Given only once or twice installation

Side Effects:
CVS:

Bradycardia,conduction arrythmias, hypotension,Reynauds phenomenon,fluid retention Pulmonary :Bronchocontriction,Asthma,Dyspnea CNS: Amnesia,depression,confusion,headache,impotent, insomnia,myasthenia gravis.

GIT: Diarrhea,Nausea Dermatologic: Alopecia,Nail pigmentation Other systemic effects: Hypoglycemic

Ocular effects: Allergy:Blepharitis Dry eye Corneal anesthesia Macular edema (aphakics) Macular hemorrhage/retinal detechmaent Uveitis Cataract progression

Contraindications:
Bronchial asthma Bradycardia (pulse rate less than 60 bpm)

Severe heart block


Overt cardiac failure Hypersensitivity

Levobunolol
Similar with timolol is a noncardioselective b-blocker Clinical Uses:

IOP in ocular hypertension


Open angle glaucoma Prophylactic after cataract surgery Anterior segment laser procedure Contraindications: Broncial asthma,COPD

Betaxolol
Less potent than timolol Clinical uses:

Chronic ocular hypertension Open-angle glaucoma Side Effects: Ocular discomport with 0.25 % ,

Contraindications: Bradycardia

Severe heart block


Overt cardiac failure Hypersensitivity

Systemic Effects:

On average less effect to pulmunary function.A key clinical advantages is in the treatment of patients with coexistent open-angle glaucoma and pulmonary disease

Metipranolol

It has been used worldwide both orally in the treatment of systemic hypertension and topically for the treatment of elevated IOP Clinical Uses: Chronic treatment of IOP and open-angle glaucoma

Carteolol
Carteolol is a noncardioselective B-blocker similar to

timolol,levobunolol and metipranolol In general,carteolol 1 % demonstartes an ocular hypotensive effect similar to that of timolol maleat 0.5 % solution.

Clinical Uses
Carteolol is used for the chronic treatment of elevated

IOP in patients with ocular hypertension and openangle glaucoma. Its ocular hypotensive effects are additive to lanataprost,but its utility in IOP elevations after laserr or cataract surgery and its additivity with other ocular hypotensive agents have not been fully evaluated

Beta Blocker
CINICAL ISSUES
Best IOP control Cost

PREFERRED DRUG Avoid betaxolol Timolol Metipranolo Timolol hemihydrinante

Comfort Hypercholesterolemia COPP Pregnancy

Carteolol Carteolol Betaxolol Avoid all

3.ADRENERGIC AGONIST
Apraclonidine
Apraclonidine a relatively selective a2-adrenoceptor

agonist,was developed as a derivate of the antihypertensive agent clonidine. Clinical Uses: Prevention of post surgery Initial treatment of acute-angle glaucoma

Prevention of postcycloplegic spikes in IOP


Side Effects After topically using can occurs blanching,eyelids

retaction,and mydriasis Contraindications: Patients sensitive to clonidine and taking monoaminooxidase inhibitors

Brimonidine
Brimonidine is a relatively potent and highly selective

alfa2-adrenoceptor agonist. Brimodine,like apraclonidine is additive to other glaucoma medications Side Effects: Hyperemia,burning,stinging,blurred vision,and foreign body sensation.

Contraindications:
Patients receiving MAOI It is not contraindicated in cardiopulmonalry disease

patients but should be used with caution in patients with severe cardiovascular disease. Side effects: Sleepness,lethargy,and fatigu,young children <20 kg

4.CABONIC ANHYDRASE INHIBITORS


Mechanism of Action
Bicarbonat formation is an essential component of

aqueous production.A relatively high concentration of bicarbonate can be found in the aqueous humor.The presence of carbonic anhydrase in cilary processes can be also bedemonstrated in both humans and animals

The earliest reported ocular hypotensuive properties of

azetazolamide,a carbonic anhydrase inhibitor (CAI) demonstrated a decrease in IOP induced from inhibition of aqueous humor production. Clinical Uses: All type of glaucoma

Azetazolamide
In the treatment of all types of

glaucoma,azetazolamide is the most widely used orally administered CAI.Actazolamide tersedia dalam preparat tablet 125 dan 250 mg dan kapsul SR 500 mg (Damox). Acetazolamide is readily absorbed from gastrointestinal tract after oral administration.Acetazolamide is not metabolized dan primary excreted via urine

Clinical Uses
Oral acetazolamide is often reserved for short-term

IOP reduction only.Acetazolamide produces an additional decease in IOP when added to drug regimens including miotics,B-blockers,and prostaglandins. In acute angle-glaucoma,acetazolamide is often administered soon after the dignosis is made.

An additional clinical use of acetazolamide is unrelated to its ocular hypertension i.e for 1.Crystaloid Macular Edema 2.Retinitis pigmentosa 3Chronic intermediate uveitis (pars planitis)

Systemic Effects
Numbness,tingling of the fingers,toes and perioral

region are most common events. Malaise,fatigue,weight loss,depression, anorexia and decreased libido. Gastrointestinal symptoms: abdomnal and diarrhea.

Ocular Effects
Drug-induced transient myopia
Myopia probably results from cilliary body edema that

produces a forward displacement of the lens-iris diaphragma. The myopia subsides on reduction or discontinuation of acetazolamide therapy

Contraindications
1.Liver disease
2.Severe chronic obstructive pulmonary disease 3.Certain secondary glaucomas

4.Renal disease incuding renal stones


5.Pregnancy 6.Known hypersensitivity to sulphonamides

Pharmacokinetic Of CAI
Drug
Actz tab Actz cap

Actz iv
Mtzl Dichp

Dose 65-250 mg qid 500 mg bid 500 mg 25-100 mg bid/tid 25-50 mg bid/tid/qid

OOA -1 h 1-2 h 1 min 1h 50 min

DOA 4-6 h 10-18 4 10-14 6-12

Methazolamide
Stucturally similar with azetazolamide and designed

to decrease ionization and thereby improve intraokuler penetration. After oral administration metrazolamide is well absorbed from gastrointestinal tract.Only 55% metrazolamide binds to plasma protein compared with 90-95% azetzolamide

Clinical uses:
Methazolamide like other CAIs may be added to the

treatment of patients with primary open-angle glaucoma and secondary glaucoma when topical ocular hypotensive agents alone provide innadequate pressure control.The advantages of methazolamide are numerous enough that meny authorities believe it should be the first CAI used for sytemic glaucoma therapy.

Side Effects
Compared with azetazolamide produces less acidosis

and has less effect on urinary citrate level and less causes paresthesia but often causes more drowsiness. Skin eruption can also occur

Contraindications
Are the same as those associated with the use of

acetazolamide. Methazolamide can be used more safty in patients with history of kidney stones or renal impairment.Patients with COPD may tolerate methazolamide better than acetazolamide ,because the netabolic acidosis is less pronouced

TOPICAL CAI
Dorzolamide(Trusopt)
Dorzolamide was the first commercially available

topical CAI to show significant ocular hypotensve activity in humans. Indication:IOP,OAG SE: Local irritation (stinging,burning,blurring) Contraindication:Allergic,renal mpairment (CrCl < 30 ml/min).

Brinzolamide (Azopt)
Heterocyclic sulfonamide Indication: IOP and OAG

SE:Taste abnormalities
Contraindications:Similar with dorzolamide

Timolol 0,5% +Dorzolamide 2%


COSOPT
Twice dayly The mean reduction in IOP 22.2% - 27.4%

Clinical Advantages of Topical CAI


CAIs reduced nocturnal aqeous flow rate

by 25 %

5.CHOLINERGIC AGONIST (MYOTICS)


Direct-acting Acethylcholine Methacholine Pilocarpine Carbachol

Indirect-acting (Cholinesterase inhibitors)


Reversible

Physostigmine Neostigmine Edrophonium Demecarium Irreversible Echothiphate Diisoprophylflourophosphate

Pilocarpine
Its activity at muscarinic receptor sited on the iris sphincter ciliary muscle pilocarpine causes pupilary contriction and varying degrees of accomodative spasm depending on the patients age Clinical Uses Primary open-angle glaucoma Acute-angle closure glaucoma Many secondary glaucomas

Side Effects
Ocular Effets
Accomodatie spasm,which can last for 2 to 3 hours

after instillation of the topical solution. Systemic Effects.sis and weakneiaphore Nausea,diaphoresis,salivation,lacrimation,vomiting,an d diarrhea

Headache
Browache (Aggresive) Marked salivation

Profuse perspiration
Nausea Vomiting Bronchospasm

Pulmonary edema
Systemic hypotension Bradycardia

Generalized muscle weakness


Incread tone and motility of git

(Abdominal pain,diarrhea) Respiratory paralysis

Contraindications
Cataract (Nuclear sclerotic,an posterior

subcapsular cataract) To prevent retinal detachment,and with retinal detachment,and patients with myopia,peripheral retinal disease that predisposes the eye to the retinal detachment ,and with aphakic or pseudophakic eyes

Pilocarpine should generally be avoided in patients

with asthma or a history of asthma


Carbachol and Echothiophate Due to their side effects,these drugs are rarely used for

treatment of glaucoma

Myotics Used for Treatment of Glaucoma


Generic Name.

Pilocarpine HCl sol Pilocarpine gel Ethothiophate iodide

Trade Name. Pilopine HS gel Isopto Carbachol Phospholine iodide

Refference
Jimmy D.Barlett,Richard G.Fiscella,Siret D.Jaanus,and

Howard Barnebey in Ocular Hypotensive Drugs

/ Cendocaine gtt.opth 1-2 dd gtt 2 p.r.n.

Fl 1

-------------------

Pro:Tn Tony Sucipto Alamat: Mess Persib,Jl.Achmad Yani Bandung

Lanaprost
Timolol Cendocarpine

Dr.Ocular Jl.Retina No. 2. Tilt 08134434 Pemandangan

Baquinor 3dd gtt 2 ODS ---------------------------- Clavulanic Acid cap.500 mg 3dd 1 ---------------------------- Cendoxitrol gtt opth. 3dd gtt 2 OGDS ----------------------------

Pmd, 1 Mei 2013 Fl I

No. X

Fl I

THANK YOU

TREATMENT OF ABNORMALITAS FILM


The goal of Ocular Surface Disease (OSD) therapy are:
1.To relieve symptoms of the OSD 2.To prevent serious complications OSD

Latanaprost 0.005 %

Fl I 1dd gtt 2 h.s. -----------------------

Chondroitin sulfat (Viscoat) gtt. Fl I


1-2 dd gtt 2 ar.ocular dolens

p.r.n

The catagories treatment of dry eye


1.Tear suplementation
2.Tear conservation 3.Tear stimulation

In attempt to establish the tear film quantitavely and qualitatively. To diagnose and treat coexistent and ancillary condition that provoke or aggravate dry eye (risk faktors):Blepharitis,mebomian disease,eyelid abnormalitis

Treatment option for dry eye


Tear supplement (artificial tears): Lacrisert (Lactic

acid) Tear conservation ointment: Punctat occlusion Tear stimulation:Secretogogues,anti inflamatories/immunomodulators

Tear supplemetation
Polymer-based artificial tear are most common tear supplement product used in dry eye treatment: Ocular lubricant are used to treat: 1.Corneal abrasions 2.Ultraviolet keratitis 3.Herpes simplex keratitis 4.Herpes zoster keratitis

5.Phlyctenular disease
6.Giant pappilary conjunctivitis 7.Superior limbic keratoconjunctivitis

8.Vernal disease
9.Adenoviral infection 10.Other ocular surface condition

The ideal artificial tear


1.Produced the metabolic optic and physical

characteristic of nature tear. 2.Have a long residence time 3.Contain therapeutical additive to treat primary and secondary damage to eye Supplement of natural tear with a substanced that prolongs residence time,improve tear film break up (TBUP) and superior to tear replacement fluids of flow retention

Most artificial tear formulation are


Water based,
Polymer to enhance: Viscosity Lubricant Retention time to promote tear film

stability

Other viscosity increasing agents include:


Gelatin
Glycerin Polyethtleneglycol Poloxamer 407 Polysorbate 80

NaCl
KCl Other ions Boric acid Help to maintain tonicity and pH similar to

normal tear

1. Polysacharides and vinyl derivates


Not produce constantly 1.The substitutes shoul have properties to enhance

retention in the tear film 2.Additio of polymer to arificial tear improve : -Retention -Increase corneal surface wetability -Decrease blink friction -Minimize surface tension

Natural tear Contain:


Glycoprotein

}Decrease surface Surfactant macromol. tension

Substitutes cellulose ethers


Hydroxy ethylene celellulose
Hydroxyprophyl cellulose Methyl celluloseCarboxymethyl cellose

These colloids have been:

1. Used in artificial formulation 2.Dissolve in water to produce colories solution of varying viscocity 3.Having proper optical clarity reflective similar to cornea

VICOELASTIC AGENTS
Na hyaluronat Na chondroitin sulfate }Mucopolysach in

extrcell.matrix Such as:Vitreous,cornea,and aquous humor Used for:- Intraoocular surgery -Severe dry aye disorder Concentration: 0.1 0.5% Subjective and objective improvement (itching)

Sodium hyaluronate
Hydrophylic
High molecular weight Polysacharide polymer Reduce subjective and objective symptoms in dry eye

patients

Chondroitin sulfate
Hyaluronic acid 0.1%
Chondroitin sulfate 1% Mixture:ChS (0.38%) + HA (0.3%)

Effective in allevating symptoms of:


Itching Burning Foreign body sensation Available in as Viscoat

Polyvinil Alcohol
Enhance contact time of opthalmic

medication As wetting agent for contact lens Concentration 1.4% Has good retention time due to adsorptive properties Can be easily sterilized

VISCOSITY-ENHANCE AGENT
Other vinyl derivates
1.PVP -Non-ionic surfactant

-To increase viscosity -Concentration:3%-5% 2.HP-guar (Hydroxyprophyl guar) -High molecular weight -A gallable lubricant,to mimic the mucin layer of tears

OTHER INGREDIENTS
Electrolyt

>>NaCl

BUFFERS
Normal ph 7.5 depend on:
Bicarbonate,protein,phaosphateanion and other subtances

PRESERVATIVES
Added to opthalmic sol. To kill or inhibit growth of

moicrorganism

NUTRIENTS
Necessary for corneal and conjunctival meabolim

>>>> mucin synthesis Vit A deficiency affect a variety of epithelial-lined organ,including eye

MUCOLYTIC AGENTS
Soften mucus and make it more fluid
Acetylcystein Available as mucomyst in a 10% or 20% solution of the

sodium salt of acetylcystein

ARTIFICIAL TEAR INSERT


LACRISERT:
-Water soluble -Contain hydroxypropylcellulose

Indication:
-Blurred vision

AUTOLOGUS SERUM
A source of tear replacement in severe dry efe
Improved ocular surface staining

OINTMENT
Indicated for moderate to severe dry eye
Retain longer than other opthalmic vehicles Patient acceptance of ointment preparation highly

variable

LACRIMAL OCCLUSIVE DEVICE


Used to preserve existing tears
Absobable insert made with hydroxypropyl

cellulose,collagen and silicone Topical anesthetic may be used to minimize eyelid reaction

ADMINISTRATION OF DRUG TOPICAL EAR

ADMINISTRATION OF DRUG TOPICAL EAR

DANKE SEHR

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