drugs used in ophthalmology
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Drugs used in ophthalmologyDrugs used in ophthalmology
lek.med. Magdalena Mazurek
Chair and Clinic of Ophthalmology with Department of Patophysilogy of Organ of Vision
How does a drug get inside the eye?How does a drug get inside the eye?
• 1. By blood
The blood-retinal barrier (BRB)
• 2. Penetrates by the cornea Mainly by epithelium and endothelium of the cornea
Route of administrationRoute of administration
• Given locally ( eye drops) – amount of drug in the anterior segment of the eye > given orally
• Given locally– achieve therapeutic levels up to the ciliary body
• Intraocular concentration :– subconjunctival injection > eye drops i ointment >
orally
Types of drugs -Types of drugs -way of administration:way of administration:
• 1. Eye drop , suspension , emulsion• 2. Ointment and gel
• 3. Inserts – i.e. Ocusert (Pilocarpine) – a drug container placed inside conjunctiva
• 4. Therapeutic Contact Lenses (‘bandage’ lenses)
Types of drugs -Types of drugs -way of administrationway of administration
• 5. Ion(t)ophoresis - technique using a small electric charge to deliver a medicine through the surface of cornea/ skin . The drug forms charged active agents ( kations, anions) which transport deaper .
• 6.Subconjunctival injection and periocular injection
• 7. Anterior chamber injection• 8. Intravitreal injection
Eye dropsEye drops
• After administration a smaller amount of drug is absorbed by the surface of the cornea, most of it reaches vascular system by the conjunctiva.
• Only 1 drop because:– Volume of the conjunctival sac = 30 μl– Volume of 1 drop = 40-70 μl
• If you administer more than one drug remember about intervals– time for penetration and absorbtion
Eye drops Eye drops
• While giving drops that have systemic effects (β-blockers, adrenaline, pilocarpine ):
– Patient should close his eyes after drug administration (it counteracts getting into the lacrimal sac by the canaliculi )
– Press in the place where lower canaliculus is located– It is possible to give the drug directly on the cornea.
OintmentsOintments
• Longer time of contact with the eyes surface
• Often given before going to sleep (overnight)
• They paste eyelashes together
• They can cause reversible loss of visual acuity
Groups of drugs:Groups of drugs:• 1. Drugs affecting the vegetative system
• 2. Drugs used in glaucoma
• 3. Anti-infectious drugs
• 4. Anti-inflammatory drugs
• 5. Anti-allergic drugs
• 6. Drugs affecting metabolism of cells and their
regeneration
• 7. Lubricant Eye Drops ( ` fake tears ` )
• 8. Anaesthetics
• 9. Disinfectant Drugs
Drugs affecting the vegetative system
SympathicomimeticsSympathicomimetics
Substance Receptors
Adrenaline α , β
Noradrenaline α , β
Fenylefryne α (non-selektive)
Brimonidyne α2
Apraklonidyne α2
SympathicomimeticsSympathicomimetics ( (mydriaticamydriatica))
• Stimulate receptor α + β:– Stimulate sympathetic nervous system– Dilate the pupil do not affect focusing
(accommodation)– Tear adhesions apart– If the angle is closing they can cause its total
closure and increased IOP
– Neosynephrin sol. 2,5% 5% 10%– Adrenaline ( 0,001%) < 1 ml
• Counter-indications :– arythmia– hypertension, high blood pressure – pheohromoctyoma– IHD– Closed angle glaucoma
Adverse effect– Anxiety, tremor– Dizziness ,headache– Tachycardia– Arythmia , acute chest pain– Allergy
Sympaticolitics (β-blockers)Sympaticolitics (β-blockers)
• ↓IOP:– ↓ production of aqueous humour by the ciliary body– affect ultrafiltration
• non-selective β-blockers (β1 + β2)– Karteolol, Timolol, Lewobunolol
• selectywne β-blockers (β1)– Betaksolol
• Glaucoma:– Open angle glaucoma– Closed angle glaucoma (with
parasympathicomimetic)– Glaucoma in aphakic eyes
Lowers elevated but also normal IOPYounger patients –stronger hypotension
β-blockery – indications β-blockery – indications
Side effects– conjunctival irritation, burning sensation, reversible
loss of visual acuity,conjunctivitis,dry eyes,ptosis, constriction of vessels
– bradycardia , arythmia, hypotension, stroke, cerebrovascular accident (CVA) , VASCULAR FAILURE
– bronchospasm (except for betaksolol), difficulty in breathing , dizziness ,headache, depression,nausea
– allergy
• Counter-indications :
– Asthma – Lung diseases– Heart/ vascular failure– II /III degree AV block– Bradycardia– Allergy
– ! Unstable diabetes !
– ! Pregnancy and Breastfeeding !
β-blockersβ-blockers
• Betaksolol (Betoptic) sol. 0,25% 0,5%
• Timolol (Oftensin, Timoptic, Cusimolol) sol. 0,25% 0,5%
• Karteolol (Arteoptic) sol. 1% 2%
• Metipranolol (Betamann) sol. 0,1% 0,3%
Parasympathicomimetic (miotics)Parasympathicomimetic (miotics)
• ↓IOP
• Dilate veins ↑aqueous outflow• Used in treatment of closed angle glaucoma
• Pilocarpine sol. ung. 1% 2% 4%• Karbachol sol. 3%
• Counter-indications:– Uveitis– Retinal Degenerative Diseases ( ↑ incidence of retinal
detachment)– Heart diseases– Asthma– Hyperthyreosis– Peptic Ulcer Disease– Parkinson's disease
ParasympathicomimeticParasympathicomimetic
• Side effects:– Headache
– Speeds up onset of cataract
– Constricts pupils poor night sight
– Posterior synechiae
– ↑ lacrimation
– Systemic effects: bradycardia, hypotension, ↑Increased urination, production of saliva
– They block the parasympathetic system– Dilate the pupil affect accommodation
– Atropine sol. 1% (children 0,25-0,5%) - 2weeks.– Homatropine sol. 1% -12 h.– Scopolamine sol. 0,25% -30 h.– Tropicamid sol. 0,5% 1% -
4 h.– Cyclopentolat sol. 0,5% 1% -
24 h.
ParasympaticolyticsParasympaticolytics ( (mydriatica et cycloplegicamydriatica et cycloplegica))
• Indications:– Helps with diagnosis (dilated pupil- fundus
examination )– Preparation for the eye surgery– In treatment of iriditis ,cyclitis– Corneal ulcers
• Counter-indications :– Closed angle glaucoma– Diseases of urinary tract and prostate with urinary
retention – Epilepsia– Allergy– < 1year old
• Parasympaticolytics can cause closure of the angle – acute glaucoma!
• gonioscopy
• If the angle is narrow :– 250 mg acetazolamide p.o. before dilation– Better use Neosynephrin
Drugs used in glaucoma
1. α2-adrenomimetics i β-adrenolitics
2. Parasympathicomimetic
3. Carbonic anhydrase inhibitors
4. Prostaglandin analogues
5. Combinated drugs
Carbonic anhydrase inhibitorsCarbonic anhydrase inhibitors
• ↓ production of aqueous
• ↑ urination (when longer used ↓K+)
• Acetazolamide - Diuramid tabl. 250 mg - Diamox inj. i.v. 500mg
• Diclofenamid (Diklofenamid) tabl. 50 mg• Dorzolamid - Trusopt sol. 2%
- Azopt sol.1%
Carbonic anhydrase inhibitorsCarbonic anhydrase inhibitors
• Counter-indications :– Renal failure, liver failure , chronic respitarory
diseases
• Side effects:– Dizziness, headache, drowsiness , depression,
dyspepsia, renal /urinary tract lithiasis , hypercaliemia i metabolic acidosis , paresthesia, itching /burning sensations of the eyes
Prostaglandin analoguesProstaglandin analogues
• ↑ Outflow of aqueous humour – Ciliary body sclera lymphatic vessels
• convenient in use – 1x day
• Latanoprost (Xalatan) sol.• Travoprost (Travatan) sol.• Bimatoprost (Lumigan) sol.
Prostaglandin analoguesProstaglandin analogues
• No systemic side effects
• Should not be combined with Pilocarpine because it blocks uveoscleral outflow
• Do not use in: allergy
• Side effects:– change of iris color (darker ↑ melanine), burning
sensation of the eyes , keratitis, palpebritis, growth of eyelashes
– rare:headache ,nausea
Combinated drugsCombinated drugs
• If monotherapy does not help
• Cosopt (Timolol + Dorzolamid) sol.
• Fotil, Timpilo (Timolol + Pilocarpina) sol.
• Normoglaucon (Metipranolol + Pilocarpina) sol.
• Xalacom (Latanoprost + Timolol) sol.
• DuoTrav (Travoprost + Timolol) sol.
Anti-infectious drugs
AntybioticsAntybiotics
• To treat infectious diseases of the eye
• Before/Postoperative prophylaxis
• Best to do antibiogram
• Used as eyedrops , ointments, injections
AntybioticsAntybiotics
• Aminoglycosides– Amikacin (Biodacin) sol.– Gentamycin 0,3% sol. ung.– Neomycyn ung.– Tobramycin (Tobrex) sol. ung.Tetracyclines– Oftalmolosa cusi tetracycline – ung.
• Chloramphnicol– Oftalmolosa cusichloramfenicol – ung.– 1% sol.Detreomycini
AntybioticsAntybiotics
• Fluoroquinolones– Ciprofloksacin (Ciloxan, Proxacin) sol.– Norfloksacin (Chibroxin) sol.– Ofloksacin (Floxal) sol. ung.
• Sulfonamids:– Sulfacetamid 10% sol.– Sulfadikramid (Irgamid) ung.
Antiviral drugs Antiviral drugs
• Herpes zoster, HSV, CMV, EBV
• NOT adenovirus infection (one of most common infections)!!!!!!
• Acylovir (Cusiviral, Virolex, Zovirax) ung. tabl.
• Vidarabine (Vira A) ung.
Anti-inflammatory drugs•SteroidsSteroids•Nonsteroidal
Hydrocortison 1 (point of reference)
Fluorometolon 1
Prednison 3,5
Prednisolon 4
Metyloprednisolon 5
Triamcinolon 5
Parametason 10
Fludrocortison 10
Deksametason 25-30
Betametason 30-40
Po
wer
of
the
ster
oid
s P
ow
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f th
e st
ero
ids
Steroids – local use :Steroids – local use :
• Betametason (Betnesol) sol.0,1%
• Deksametason (Dexamethason, Oftan Dexa) sol.0,1%
• Fludrocortison (Continef) ung.
• Fluorometolon (Flucon, Flarex) sol.
• Hydrocortison (Hydrocortison dispersa, Ophticor H) ung.
• Prednisolon (Prednisolonum) sol.
NSAIDsNSAIDs• General inhibition of prostanoid biosynthesis • Often used :
– Before/after surgery– Conjunctivitis, keratitis, scleritis …….– After trauma– Prevent pupil dilation during operation– When steroids can`t be used
• Diclofenac (Naclof) sol.• Flurbiprofen (Ocuflur) sol.• Indometacine (Indocollyre, Indocid) sol.
Anti-allergic drugs
Antihistamine drugsAntihistamine drugs
• Emadastine (Emadine) sol.
• Olopatadine (Opatanol) sol.
Combined :– Alergoftal (Antazoline + nafazoline) sol.– Betadrin (Difenhydramine + nafazoline) sol.– Spersallerg (Antazoline + tetryzoline) sol.
• Allergic conjunctivitis ….symptoms
Anti-allergic drugs other:Anti-allergic drugs other:
• Natrii cromoglicas (Cromohexal, Opticrom, Polcrom, Vividrin, Cusicrom) sol.
• Tilavist sol.
• Alomide sol.
Drugs affecting metabolism of cells and their regeneration
• Better corneal nutrition in dry eye syndrome, in eye burns , erosions ,corneal ulcers….– Dexpantenol (Corneregel) żel– Solcoseryl – gel
• Better metabolism of the lens and vitreous (↓ cataract onset) – Quinax sol.– Catalin sol.
Lubricant Eye Drops ( `fake tears `)
• Lacrimal sol.
• Artelac, Isopto-Tears, Methocel sol.
• Vidisic gel
• Oculotect, Vidisept sol.
• Combined :– Dacrolux sol.– Tears Naturale, Tears Naturale Free sol.– ! Better without conservants!!!!
Anaesthetics
• Given locally .• Do not use too long because they are toxic for
corneal epithelium.
– Bupivacainum inj. 0,25% 0,5%– Marcain inj. 0,25% 0,5%– Lignocainum, Lidocain, Xylocaine inj. 2% 4%– Alcaine sol.
Thanx for listening!Thanx for listening!
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