Pharmacology of the eye Synek, S. Department of Optometry and Ortoptics Medical Faculty, MU, Brno Barriers to drug delivery ´Compliance ´Poor technique ´Short residence time ´Wash out from tears Compliance ´Physical barrier: poor vision, arthritic fingers, severe kyphosis ´Cognitive: decline, poor memory ´Range of aides: memoire, gadget Local drug effectiveness ´Drug design: pH, solubility, molecular size will affect drug passage crossing cornea- it must be water and lipid soluble ´More viscous may be retained longer ´Toxicity: keratopathy punctata obr3.jpg obr 2 Rez_lid_rohovkou.gif Ways of administration ´Topically- drops or ointment ´Periocular injection- subconjunctival, subtennons ´Intravitreal injection: antiVGF, antibiotics, corticosteroids, ´Oral and intravenouos dosing: antibiotics, corticosteroids, antivirotics, antimetabolits, diuretics Aplication of drops Aplication of ointment Aplication with glass stick Rinse out Retrobulbar injection Bandage with safety shell Bandage Bandage Wet chamber Drugs ´Ophthalmic Dyes ´Anesthetic agent ´Dilating agents ´Lubricants ´Hyper osmotic agents ´Anti allergy medications ´Anti-infective agents ´Immunosuppressive agents ´Glaucoma agents Ophthalmic Dyes ´Fluorescein- stain epithelial defect, will not stain devitelized cell, stain soft contact lens, promote growth of Pseudomonas Aeruginosa, angiography ´Lissamine green-dry eye evaluation ´Rose bengal-stain devitelized cells, mucin ´Indocyanine green-angiography ´Trypan blue-stain lens capsula, epiretinal membrane Comparative staining Epithelial defect Devitelized cells Mucin Fluorescein ++ 0 + Rose bengal 0 ++ ++ Lissamine green 0 ++ + Ulcus corneae Eroze.jpg Eroze2.jpg •Fluorescein staining Bengal Rose staining DryEye-RoseBengal.gif •Dry eye Lyssamine green stain lysamine die cells.jpg •Dead cells Anesthetics agents ´Tetracain 0,5% - corneal or conjunctival foreign body, photoelectric ophthalmia, intraocular surgery ´Topical, intracameral, subconjunctival, subtenons, parabulbar Dilating drugs (mydriatics) Max. mydriasis Duration Parasympatholytica Tropicamide 0,5% 20-40 min. 4-8 hours Cyclopentolate 0,5% 30-60 min. 12-24 hours Homatropine 1% 40-60 min. 24 – 72 hours Scopolamine 0,25% 20-30 min. 3-7 days Atropine 1% 30-40 min. 7-10 days Sympathomimetica Phenylephrine 2% 20-30 min. 4-6 hours Hydroxyamphetamine 1% 25-35 min. 4-6 hours Cataract katarakta kortikalis.jpg Indication for cycloplegic refraction ´Strabismus ´Amblyopia ´Anisometropia ´Pseudomyopia ´Hyperopia with esophoria or lag of accomodation ´Unstabile end point on static retinoscopy ´Uncooperrative child Efficiency of cycloplegics ´1% atropin 100% ´1% cyclopentolate 92% ´1% tropicamide 80% ´5% homatropine 54% Ocular Side effect ´Allergic Contact dermatitis ´Angle-closure glaucoma ´Elevation of IOP with open angles Systemic side effect of atropine ´Tachycardia, dry mouth mydriasis, confusion, decreased GI motility, ataxia, hallucination, convulsion, coma New treatment modality of myopia ´0,01% atropin drops Ophthalmic lubricants ´Hydroxyethylcellulose ´Polyvinyl alcohol 1,4 – 3% ´Dextran 70% ´Hydroxypropylmethylcellulose 0,5 – 1% ´Carboxymethylcellulose ´ Ophthalmic lubricants ´Povidone ´Glycerine 1% ´Polysorbate 1% ´Polyethylen glycol 0,4% ´Propylene glycol 0,3% ´ Preservative in Ophthalmic lubricants ´Thiomersal ´EDTA ´Chlorobutanol ´Benzalkonium chloride ´Chlorobutanol ´Methylparaben ´Purite ´Polyquaternium-1 ´None Dry eye questionnaire 1.Have you ever had drops for dry eye? 2.Do you ever experience of the following eye symptomes? a.Soreness, scratchiness, dryness, grittiness, burning 3.How often do you have these symptomes? 4.Do you regard your eye as being sensitive to smoke, smog, air condition? 5. 5. 5.do you take antihistaminic, diuretics, sleeping tablets, tranquilizers , stomach medicine, high pressure medicines? 6.Do you have arthritis? 7.Are your joint fingers swollen in the morning? 8.Do you have dryness of the nose, mouth or dry cough? 9. 9.Do you have thyroid abnormality? 10.Do you ever awaken with eye irritation or excessive dried mucus in the corners of you eye? Medicaments that can affect tear quality ´Antibiotics (tetracycline) ´Antihypertensive ´Botulotoxin ´Dermatologicals (isotretinoin) ´Psychomimetics (diazepam, thioridazine) ´Topical betablockers ´Antihistamines ´Diuretics ´Long term antiperspirants Topical hyperosmotic agents ´2-5% NaCl solution ´40% glucose solution ´5% NaCl ointment ´40% glucose ointment ´ Obrázek1.jpg •Bulous keratopathy Anti-allergy medication ´Topical ´Decongestants ´Antihistamines ´Systemic antihistamines ´Sedative effects ´Antihistamine activity ´Anticholinergic activity Obrázek2.jpg •Allergic conjuctivitis Anti-infective agents ´Antibiotics ´Virostatics ´Antimycotics Absces rohovky.jpg disciformní keratitida.jpg marginální rohovkový ulcus.jpg •Deep Keratitis herpetica •Ulcus corneae •Endoftalmitis mycotica Glaucoma therapy Narrow angle Glaucoma ´Congenital ´Juvenil ´Open angle ´Close angle Acute Glaucoma Therapy ´Drops ´Laser ´Surgery (glaucoma implants) •Normal •Glaucoma excavation Drops ´Lowering intraocular pressure / miotics, alfa sympatomimetics, prostaglandins ´Lowering intraocular pressure: betablockers, inhibitors carboanhydrasis ´Osmotic agents ´Drops which raise outflow of intraocular humour, pilocarapine ´ ´ ´Lowering intraocular pressure: betablockers, inhibitors carboanhydrasis ´