Documenti di Didattica
Documenti di Professioni
Documenti di Cultura
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
occurs. Increasing the concentration of the anesthethic beyond the MEC serves no useful purpose but increases the risk of local and systemic toxicity.
1 % and 2.0 %. In clinical practice,however,the OEC(Optimum Effective Concentration) may be less than MEC.
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.......
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
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
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 contraindicated to
Systemic hypertension Retinal detachment surgery
Routine opthalmoscopy
Gonioscopy Angle close glaucoma (mydriatic effect)
Tetracaine
Ester PABA
Available 0,5
% solution
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
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
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.
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).
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.
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
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 %)
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
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.
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)
Levobunolol
Similar with timolol is a noncardioselective b-blocker Clinical Uses:
Betaxolol
Less potent than timolol Clinical uses:
Chronic ocular hypertension Open-angle glaucoma Side Effects: Ocular discomport with 0.25 % ,
Contraindications: Bradycardia
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
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
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
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
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
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
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
by 25 %
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
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
treatment of glaucoma
Refference
Jimmy D.Barlett,Richard G.Fiscella,Siret D.Jaanus,and
Fl 1
-------------------
Lanaprost
Timolol Cendocarpine
Baquinor 3dd gtt 2 ODS ---------------------------- Clavulanic Acid cap.500 mg 3dd 1 ---------------------------- Cendoxitrol gtt opth. 3dd gtt 2 OGDS ----------------------------
No. X
Fl I
THANK YOU
Latanaprost 0.005 %
p.r.n
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
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
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
stability
NaCl
KCl Other ions Boric acid Help to maintain tonicity and pH similar to
normal tear
retention in the tear film 2.Additio of polymer to arificial tear improve : -Retention -Increase corneal surface wetability -Decrease blink friction -Minimize surface tension
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%)
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
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
cellulose,collagen and silicone Topical anesthetic may be used to minimize eyelid reaction
DANKE SEHR