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Drugs used in ophthalmology

Drugs 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 ?. 1. By blood  The blood-retinal barrier ( BRB) 2. Penetrates by the cornea

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Drugs used in ophthalmology

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  1. Drugsusedinophthalmology lek.med. Magdalena Mazurek Chair and Clinic of Ophthalmology with Department of Patophysilogy of Organ of Vision

  2. Howdoes a druggetinsidetheeye? • 1. By blood The blood-retinal barrier (BRB) • 2. Penetrates by the cornea  Mainly by epithelium and endothelium of the cornea

  3. Route 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

  4. Types of drugs -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)

  5. Types of drugs -way of administration 5.Ion(t)ophoresis- technique using a small electric charge to deliver a medicine through the surface of cornea/ skin . Thedrugformschargedactiveagents ( kations, anions) which transport deaper . 6.Subconjunctival injection and periocularinjection 7. Anteriorchamberinjection 8. Intravitrealinjection

  6. Eye 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

  7. 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.

  8. Ointments • 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

  9. 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

  10. Drugsaffectingthevegetative system

  11. Substance Receptors Adrenaline α , β Noradrenaline α , β Fenylefryne α (non-selektive) Brimonidyne α2 Apraklonidyne α2 Sympathicomimetics

  12. Sympathicomimetics (mydriatica) • 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

  13. Counter-indications : • arythmia • hypertension, high blood pressure • pheohromoctyoma • IHD • Closed angle glaucoma Adverse effect • Anxiety, tremor • Dizziness ,headache • Tachycardia • Arythmia , acute chest pain • Allergy

  14. 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

  15. β-blockery – indications • Glaucoma: • Open angle glaucoma • Closed angle glaucoma (with parasympathicomimetic) • Glaucoma in aphakic eyes Lowers elevated but also normal IOP Younger patients –stronger hypotension

  16. 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

  17. Counter-indications : • Asthma • Lung diseases • Heart/ vascular failure • II /III degree AV block • Bradycardia • Allergy • ! Unstable diabetes ! • ! Pregnancy and Breastfeeding !

  18. β-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%

  19. Parasympathicomimetic (miotics) • ↓IOP • Dilate veins  ↑aqueous outflow • Used in treatment of closed angle glaucoma • Pilocarpine sol. ung. 1% 2% 4% • Karbachol sol. 3%

  20. Parasympathicomimetic • Counter-indications: • Uveitis • Retinal Degenerative Diseases ( ↑ incidence of retinal detachment) • Heart diseases • Asthma • Hyperthyreosis • Peptic Ulcer Disease • Parkinson's disease

  21. 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

  22. Parasympaticolytics (mydriatica et cycloplegica) • 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.

  23. 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

  24. 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

  25. Drugsusedinglaucoma

  26. α2-adrenomimetics i β-adrenolitics • Parasympathicomimetic • Carbonic anhydrase inhibitors • Prostaglandin analogues • Combinated drugs

  27. Carbonicanhydraseinhibitors • ↓ 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%

  28. Carbonicanhydraseinhibitors • 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

  29. Prostaglandinanalogues • ↑ Outflow of aqueous humour • Ciliary body  sclera  lymphatic vessels • convenient in use – 1x day • Latanoprost (Xalatan) sol. • Travoprost (Travatan) sol. • Bimatoprost (Lumigan) sol.

  30. Prostaglandinanalogues • 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

  31. Combinateddrugs • 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.

  32. Anti-infectiousdrugs

  33. Antybiotics • To treat infectious diseases of the eye • Before/Postoperative prophylaxis • Best to do antibiogram • Used as eyedrops , ointments, injections

  34. Antybiotics • 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

  35. Antybiotics • Fluoroquinolones • Ciprofloksacin (Ciloxan, Proxacin) sol. • Norfloksacin (Chibroxin) sol. • Ofloksacin (Floxal) sol. ung. • Sulfonamids: • Sulfacetamid 10% sol. • Sulfadikramid (Irgamid) ung.

  36. Antiviraldrugs • Herpes zoster, HSV, CMV, EBV • NOT adenovirus infection (one of most common infections)!!!!!! • Acylovir (Cusiviral, Virolex, Zovirax) ung. tabl. • Vidarabine (Vira A) ung.

  37. Anti-inflammatorydrugs • Steroids • Nonsteroidal

  38. 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 Power of thesteroids

  39. Steroids – localuse : • 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.

  40. NSAIDs • 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.

  41. Anti-allergic drugs

  42. Antihistaminedrugs • Emadastine (Emadine) sol. • Olopatadine (Opatanol) sol. Combined : • Alergoftal (Antazoline + nafazoline) sol. • Betadrin (Difenhydramine + nafazoline) sol. • Spersallerg (Antazoline + tetryzoline) sol. • Allergic conjunctivitis ….symptoms

  43. Anti-allergicdrugsother: • Natrii cromoglicas (Cromohexal, Opticrom, Polcrom, Vividrin, Cusicrom) sol. • Tilavist sol. • Alomide sol.

  44. Drugs affecting metabolism of cells and their regeneration

  45. 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.

  46. Lubricant Eye Drops ( `fake tears `)

  47. Lacrimal sol. • Artelac, Isopto-Tears, Methocel sol. • Vidisic gel • Oculotect, Vidisept sol. • Combined : • Dacrolux sol. • Tears Naturale, Tears Naturale Free sol. • ! Better without conservants!!!!

  48. Anaesthetics

  49. 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.

  50. Thanx for listening!

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