Ocular   therapeutics
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A volatile presentation covering almost all ocular drugs,...Hope it to be useful to you all,.. Haven't presented it yet to my department

A volatile presentation covering almost all ocular drugs,...Hope it to be useful to you all,.. Haven't presented it yet to my department

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Ocular   therapeutics Ocular therapeutics Presentation Transcript

  • Ocular Therapeutics Ocular Therapeutics Dr Rajvin Samuel Ponraj
  • Pharmacodynamics
    • Study of mechanisms of drug effects
    • Receptor - special types
    • based on transduction of signal
    • Regulation of receptors – Down regulation
    • Up regulation
    • Therapeutic index
  • Pharmacokinetics
    • Quantitative study of drug movement in, through and out of the body
  • Transport across cell membrane
    • Passive transport
    • Specialized transport
    • First Pass metabolism
    • Bioavailabilty
  • Distribution
    • Barriers concerned with distribution
      • Blood aqueous barrier
      • Blood retinal barrier
      • Corneal barrier
      • Tissue binding
      • Tissue perfusion
  • Biotransformation
    • Phase 1 reactions
    • Phase 2 reactions
  • Excretion of drugs
    • Elimination kinetics - First order kinetics
    • Zero order kinetics
    • Clearance
    • Half life
  • ADVERSE DRUG EFFECTS
    • SIDE EFFECTS
    • TOXIC EFFECTS
    • INTOLERANCE
    • TERATOGENICITY
  • Routes of administration
    • Local topical
    • Periocular
    • Intraocular
    • Systemic oral
    • injection
  • Topical drug methods
    • Eye drops
    • Eye ointment
    • Gels
    • Ocuserts
    • Soft contact lens
  • Drug penetration
    • Topically : -Lipid and water solubility
    • -Contact time , viscosity ,
    • - isotonicity
    • Systemically : - Lipid solubility
    • - eye inflammation
    • - protein binding
    • -molecular weight
  • Ocular anaesthetics
    • MOA :- Reduce nerve impulse conduction by reducing membrane
    • to sodium ions.
    • Common local anaestheitics :-
    • Ester type = Tetracaine 0.5 % , propacaine 0.75 %
    • Amide type = Lidocaine 2 % , Bupivacaine 0.75 %
  • Topical anaesthetic
    • Aim :- To block nerves of superficial cornea
    • Advantages :- No needle insertion
    • No haemorrage
    • Systemic anticoagulants can use
    • Patient alert
    • Disadvantages :- No akinesia
    • Not adequate anaesthesia
    • Adv effects :- Corneal stinging ,epithelial & endothelial toxicity
    • Allergy & contact dermatitis
    • Contraindications :- Nystagmus , uncooperative patients
  • Retrobulbar block
    • Aim :- To block 3 rd cranial nerve in posterior intraconal space
    • Site of injection :- Above inferior orbital rim
    • midway of lateral canthus & temporal limbus
    • Advantages :- Excellent akinesia
    • quick onset of block
    • Disadvantages:- High complication rate
    • Complications :- Retrobulbar Haemorrhage
    • Globe perforation
    • Optic nerve contusion
    • Oculocardiac reflex
    • Respiratory depression
  •  
  • Peribulbar block
    • Aim :- To block extraconally the nerves
    • Site of injection :- midway b/w temporal limbus & lateral canthus
    • -Inferomedial to superior orbital notch
    • Advantages :- All that of retrobulbar block
    • Less complications
    • Disadvantages :- More than one injection needed
    • Only good akinesia , anesthesia
    • Longer time for anesthesia
    • Chemosis
  •  
  • Sub tenon’s block
    • At 1 or 2 ‘0’ clock positions from corneal limbus [7-8 mm away]
    • Using a 30 mm radius flexible cannula after perforating conjunctiva
    • Passed beyond equator b/w tenon’s capsule & sclera
    • Most frequent site is inferotemporal .
  • Intraocular injections
    • Intracameral or intravitreal
    • E.g.
      • Intracameral acetylcholine (miochol) during cataract surgery
      • Intravitreal antibiotics in cases of endophthalmitis
      • Intravitreal steroid in macular edema
      • Intravitreal Anti-VEGF for DR
    INTRA-OCULAR INJECTIONS
  • Mydriatics & Cycloplegics
    • Anticholinergic drugs :- Atropine 1 % - 1 week
    • Homatropine 2 % - 24 hrs
    • Cyclopentolate 1 % - 24 hrs
    • Tropicamide 0.5 % - 4 hrs
    • Indications :- corneal ulcer , uveitis , cycloplegic refraction
    • Side effects :- blurry vision , photophobia ,precipitates
    • angle closure glaucoma
    • Sympathomimetics :- Phenylephrine 5 %
    • I ndications - Along with mydriatic in Preoperative
    • cataract preparation , fundus examination
    • Side effects - Stinging , rise in Blood pressure
  • Anti glaucoma drugs
    • - B adrenergic blockers :
    • MOA - Reduce aqueous production –
    • down regulation of Adenylcyclase
    • Advan : NO pupil change, induced myopia
    • No headache, nor IOT fluctuation
    • Side eff : Stinging,burning ,allergy,..
    • Bronchospasm,Heart block
    • Timolol – Non selective 0.5 %
    • Betaxolol - B 1 selective
    • MIOTICS :
    • Pilocarpine –cholinomimetic drug
    • MOA : increases tone of ciliary muscles
    • -pull trabecular meshwork - outflow of
    • aqueous
    • Advant : Rapid but short acting
    • Disadv : IOT fluctuation ,dim visual loss
    • Side eff : Spasm of accomadation ,brow ache,
    • git disturbances
    • 0.5 % - drops , ocuserts, gel
  • Adrenergic agonists
    • Epinephrine
    • MOA - On alpha , beta receptors – reduce aqueous formation
    • increases aqueous outflow
    • Side effects : Burning , stinging , Conjunctival
    • blanching , CME , Endothelial toxicity
    • follicular conjunctivitis [0.5 -2 %]
    • tachycardia , hypertension
    • Contradicted in aphakic & Closed angle glaucoma
    • Apraclonidine
    • MOA- On alpha 1,2 receptors –reduce aqueous formation
    • Side eff : Itching ,dryness in mouth, follicular
    • conjunctivitis, mydriasis
    • Use : to reduce IOT after laser trabeculoplasty
    • [0.25 – 1 %]
    • Brimonidine – alpha 2 selective
    • Side eff :- dryness in mouth ,fall in Bp,
  • Carbonic anhydrase inhibitors
    • ACETAZOLAMIDE
    • MOA - inhibits bicarbonate ion production , osmotic gradient
    • reduce aqueous formation
    • Side effects – Paraesthesia, anorexia, malaise ,Gi irritation
    • Oral 0.25 gms BD
    • DORZOLAMIDE – 2 % DROPS
    • PROSTOGLANDINS
    • LATANOPROST
    • MOA – On prostanoid FB receptors Increase uveoscleral flow
    • & permeability of CBM
    • Side effects – eye irritation , pain, blurry vision
    • 0.005 % drops
  • Hypertonic agents
    • MOA - Raises the osmotic pressure to reduce intra ocular
    • pressure
    • Glycerol [ 10 % infusion / 1 gm /kg oral ]
    • Side effects : nauseating sweet taste ,diarrhoea,headache
    • Mannitol [ 20 % infusion ]
    • Side effects : Hypervolemia , pulmunory edema
  • Drugs during glaucoma surgery
    • ANTIFIBROBLASTIC AGENTS – 5 FU & MITOMYCIN C
    • MOA -Inhibit collagen and protein synthesis by interfering with
    • DNA transcription and replication
    • Side effects : 5 FU – keratopathy
    • Mitomycin - scleral ulcer & iritis
    • Administration : 5 FU - 50 mg/ml Sponge / sub conjunctival
    • mitomycin – 0.5 mg/ml topically
  • Antibacterials
    • PENICILLINS
    • MOA :- Bactericidal Destroys cell wall
    • [gram + , gram – cocci,spirochetes]
    • - penicillin G [1 lakh U/ml topical]
    • [0.5 M U/ ml sub conj inj ]
    • [5 M U / 4 hrs IV]
    • - Cloxacillin [penicillinase resistant]
    • [50-100 mg/kg] 6 hrly oral [staphylococci]
    • - Amoxycillin
    • [25-50 mg/kg] 6 hrly oral [ gram +,- bacteria]
    • Adverse eff :- Hypersensitivity reactions , rash ,..
  • QUINOLONES
    • MOA :- [ Bacterial ] Anti DNA gyrase – inhibits division & supercoiling
    • [gram -- bacteria , gram + bacteria ,chlamydia, mycoplasma]
    • - Ciprofloxacin :- 0.3 % topical , 500 mg BD oral , 5-10 mg/kg IV
    • 200 mg /ml intravitreal
    • Uses :- Keratoconjunctivitis, ulcers,blepharitis,
    • dacryocystitis , infectious endoophthalmitis
    • S/E :- Arthropathy in children ,GIT irritation,
    • Photosensitivity ,rash, liver damage
    • - Gatifloxacin :-
  • CEPHALOSPORINS
    • MOA :- Bactericidal – destroys cell wall
    • 1 st generation :- gram + cocci & gram – bacilli
    • Cephazolin – 0.5 – 1 g/ml 8 hrly IM /IV
    • 2000 ug Intravitreal , 100 mg S/C
    • Cefadroxil – 0.5 -1 g BD oral
    • S/E :- GIT disturbances ,hypoprothrombinemia
    • 2 nd generation :- gram – bacteria ,some anaerobes
    • Cefuroxime axetil – 250-500 mg BD oral
    • Cefoxitin – 1-2 gm 8 hrly IM/IV
    • S/E :- GIT disturbances , migraines, headache
    • 3 rd generation :- gram – bacteria
    • Cefixim – 200-400 mg bd oral
    • ceftazidim -1-2 gm 8 hrly IM/IV
    • S/E: diarrhoea , neutropenia, thrombocytopenia
    • 4 th generation :- against many bacteria ,highly resistant to
    • B –lactamases
    • Cefepime & cefpirome :- 1-2 gm 8 hrly IM/IV
    • S/E : allergic reactions , breathing difficulty,
    • swelling of face ,..
    • Uses :- along with aminoglycosides In endoophthalmitis and
    • bacterial corneal ulcers,..
  • Chloramphenicol
    • MOA :- Bacteriostatic , Inhibits Protein synthesis by binding
    • to 50 S ribosomal subunit
    • [gram +,- aerobes , chlamydia,ricketssia,mycoplasma]
    • 0.5 % ointment, 50 mg /kg 4 times oral
    • 2 mg/ml intravitreal
    • Uses :- Intraocular infections
    • Conjunctivitis
    • Side eff :- Bone marrow depression
    • Aplastic anemia , agranulocytosis
  • Tetracycline
    • MOA :- Bacteriostatic - inhibits protein synthesis by binding to
    • 30 S Ribosome
    • - 250-500 mg 4 hrly oral
    • - 1 % topical
    • Uses :- Chlamydial diseases
    • phlyctenular conjunctivitis
    • Toxoplasmosis
    • ocular rosacea
    • Side eff :- GIT disturbances
    • discolouration of teeth
    • photosensitivity , rashes
    • nephrotoxicity
  • AMINOGLYCOSIDES
    • MOA :- Bacteriocidal - inhibits protein synthesis ,binding 30 S
    • ribosome sub unit
    • [gram negative bacteria & staph aureus
    • ADR : Ototoxicity , nephrotoxicity ,corneal , retinotoxicity,..
    • Gentamycin :- 0.3 % drops, 20 mg sub conjunctival inj
    • 200 ug/ml intravitreal inj
    • Uses :- Endoophthalmitis , ocular injuries ,retained FB
    • conjunctival necrosis
    • Amikacin :- 0.3 % drops , 15 mg / kg 8 hrly IV , 0.4 mg intravitreal
    • Uses :- along vancomycin in post op endophthalmitis
    • Tobramycin :- including proteus,pseudomonas
    • 0.3 % drops , 3 - 5 mg /kg /day IV , 150-200 ug /ml
  • SULPHONAMIDES
    • MOA :- Bacteriostatic - Inhibits folate synthesis
    • [PABA folic acid ]
    • [gram - ,+ bacteria]
    • Sulfacetamide , Sulfamethoxazole , sulfadiazine
    • Topically 10% ,20 % ,30 % drops
    • Oral 2-4 gm/day TDS
    • COTRIMOXAZOLE
    • MOA :- Inhibits Dihydro folate reductase in conversion of
    • DHF THF
    • Sulfamethoxazole [400 mg ] + trimethoprim [80 mg]
    • USES :- In trachoma
    • along with pyrimethamine in toxoplasmosis
    • S/E :- GIT disturbances , Hypersensitivity reactions , urticaria ,
    • renal toxicity-crystalluria.
  • Antifungals
    • Polyene antibiotics :-
    • MOA - Selective action on ergosterol of fungal cell membrane
    • forming micropores – increase permeability
    • Amphotericin B – Against yeast ,filamental fungi [0.25 % topical ]
    • [ 0.25 mg/kg oral]
    • Nystatin - against candida [ 1 lakh u/gm oint]
    • Natamycin – against candida , aspergillus ,fusarium [ 5 % suspension]
    • Uses in keratomycosis and endophthalmitis[5-10 ug intravitreal]
    • Common side effects : allergic hypersensitivity reactions
    • Imidazoles :-
    • MOA - Block fungal cytochrome P-450 enzyme in ergosterol
    • [increase permeability tru membrane]
    • Clotrimazole :- [1 % topical]
    • Miconazole :- [ 1 % drops,2 % oint, 5-10 mg sub conj ]
    • Ketoconazole :- [200-800 mg oral daily , 0.5 mg intravitreal]
    • Uses :- candida,fungal , endoophthalmitis
    • Side effect:- liver toxicity
    • Triazoles :-
    • Fluconazole - [100-200 mg oral]
    • [0.2% topical]
    • [0.1 mg intravitreal]
    • Uses :- Candida,cryptococcus
  • Anti virals
    • PYRIMIDINE DERIVATIVES
    • Idoxuridine :- 0.1 % drops hrly / 0.5 % ointment
    • TRIFLUOROTHYMIDINE :- 1 % drops
    • MOA : By incorporation - inhibition of viral DNA synthesis
    • Uses :- Dendritic ulcer , herpes simplex keratoconjunctivitis
    • Side effects :- with corticosteroids – SPK, follicular conjunctivitis,..
  • PURINE DERIVATIVES
    • ADENINE ARABINOSIDE
    • MOA :- Blocking DNA synthesis of virus
    • Acyclovir - 3 % ointment , 400-800 mg 5 times/day a week
    • Uses :- EB virus, CMV ,Herpes zoster virus,..
    • S/E :- Allergic reactions,..
    • Valacyclovir - 1000 mg TDS
    • Famciclovir - 500 mg TDS
    • S/E :- GIT disturbances
    • Ganciclovir - 5-6 mg intravitreal inj , 5 mg IV
    • S/E :- bone marrow depression , rashes
  • Ocular antiallergics
    • MOA – Competitive antagonist of H1 receptors
    • Uses - vernal keratoconjunctivitis , Giant papillary conjunctivitis
    • Allergic conjunctivitis
    • CPM – 4 times /day topical
    • Azelastine - 2 times/day
    • Loratadine/ cetrizine – at bed time
    • Mast cell stabilizers
    • MOA – Stabilizes mast cells and prevent release of histmaine
    • Cromolyn sodium [2-4 % ] 6 hrly
    • Olapatadine [0.1 % ] 12 hrly
  • Corticosteroids
    • MOA :
    • In general : Anti inflammatory action - fibroblast formation
    • reduce capillary permeable
    • Topical steroids :
    • 1 % prednisolone
    • 0.1 % FML
    • 0.1 % dexamethasone in conjunction to
    • antibiotic
    • Uses :
    • Allergic conjunctivitis , iritis, keratitis ,episcleritis
    • Injection steroids :
    • 40 mg Triamcinolone acetate - periocular
    • 1 mg dexamethasone - intravitreal
    • Uses :
    • Endoophthalmitis, Cysotid macular edema ,…
    • Oral steroids :
    • 1 - 2 mg /kg /wt - orbital inflammation
    • post operative inflammation
    • panuveitis
    • Adverse drug reaction :
    • Prolonged use - posterior sub capsular cataract
    • glaucoma
  • NSAID
    • E.g. ketorolac 0.5 % , flurbiprofen 0.03 %,..
    • Mechanism: inactivation of cyclo-oxygenase
    • Uses: postoperatively
    • mild allergic conjunctivitis
    • episcleritis, mild uveitis, cystoid macular edema
    • Side effects: stinging , burning
  • Anti VEGF
    • MOA : Inhibits vascular EGF in retinal ischaemia
    • Uses : Diabetic retinopathy , macular edema , ROP
    • ARMD
    • - Intravitreal inj - Pegaptanib [macugen ]
    • Ranibizumab [ lucentis ]
  • Drugs for dry eye
    • Characteristics of ideal tear drops :
    • - Soothing effect
    • - proper wetting agent , viscious
    • - No epithelial toxicity
    • - Alkaline p H
    • MOA : mucomimetic - bind to corneal epithelium form
    • hydrophilic layer to stabilize tear film .
    • Hydroxy propyl methyl cellulose – 0.5 - 1 %
    • Polyvinyl alcohol -- 1.4 %
    • Carboxy methyl cellulose -- 0.5 %
  • Viscoelastics
    • Properties - optical
    • - cohesive [ space maintaining
    • tissue manipulation in surgery]
    • - dispersive [ Coating ocular surface
    • protecting corneal endothelium
    • lower surface tension]
    • - Elasticity
    • Sodium hyaluronate 1 %
    • Sodium hyaluronate 3 % & chondroitin sulphate 4 %
    • Hydroxy propyl methyl cellulose 3 %
    • Uses :-
    • - In gonioscopy
    • - in intra ocular surgeries
  • IRRIGATING SOLUTIONS
    • Characteristics of an ideal solution :
    • -- Maintain moisture of & cleanse ocular tissues
    • -- Isotonicity electrolyte and p H same as aqueous
    • -- Maintain pressure of globe
    • -- Protect delicate ocular structures
    • -- Endothelial nourishment
    • Available preparations :- Balanced salt solution[BSS]
    • BSS plus
    • Dextran containing soln
    • Glucose fortified BSS plus
    • USES :- Intraocular – in cataract surgery
    • Extraocular – FB removal,tonometry,gonioscopy
  • Ocular diagnostic drugs
    • Fluorescein dye
      • Available as drops or strips
      • Uses : stain corneal abrasions, applanation tonometry, detecting wound leak, NLD obstruction, fluorescein angiography
      • Caution:
        • stains soft contact lens
        • Fluorescein drops can be contaminated by Pseudomonas sp.
    Ocular Diagnositic Drugs
    • Rose bengal stain
      • Stains devitalized epithelium
      • Uses: severe dry eye, herpetic keratitis
  • Ocular toxicology :
    • Amiodarone :- Vortex keratopathy
    • Digitalis :- Chromatopsia [seeing yellow colour ]
    • Chloroquine :- Bull’s eye maculopathy
    • Ethambutol :- Optic neuropathy , colour vision disturbed
    • Corticosteroids :- Posterior sub capsular cataracts
    • Thioridazine :- Pigmentary retinopathy
    • Copper, Gold :- Lenticular opacities
    • Rifabutin :- Anterior uveitis
    • THANK YOU