Textbook on Clinical Ocular Pharmacology & Therapeutics SK Gupta, Renu Agarwal, Sushma Srivastava
INDEX
ABCDEFGHIKLMNOPQRSTUVWZ
Page numbers followed by f refer to figure and t refer to table.
A
Abacavir 314
Abducent nerve 24
Acanthamoeba 68, 259t, 268, 269
ACE inhibitors 310
Acetazolamide 316
Acetylcholine 210, 256
Acinetobacter species 111, 126, 131
Active transport 30f, 36
Acute angle-closure glaucoma 250
Acute conjunctivitis 111
Acute retinal necrosis 140, 141
Adenoviruses 136, 138, 143
Adenylyl cyclase-camp system 52
Adverse drug reactions 63
expected
secondary effects 63
side-effects 63
toxicity 63
unexpected
carcinogenicity 64
genetically determined 63
idiosyncratic reactions 64
immunologically mediated 63
teratogenicity 64
Age-related macular degeneration 234
laser photocoagulation in 234
nutritional agents in
lutein 235
zeaxanthin 235
photodynamic therapy in 234
verteporfin (visudyne) 234
Agonists 50, 51
Alendronate 311
Allergic conjunctivitis 187
Allopurinol 312
Alprazolam 307
Amblyopia 91
Amino acids 279
cysteine 279
taurine 279
Aminoglycosides
administration 127
adverse effects 127
bacterial resistance 126
classification 125
contraindications 128
dosage 127
therapeutic uses 127
Amiodarone 310
Amitriptyline 307
Amlodipine 310
Amorolfine 153
Amphetamine 306
Amphotericin B 146, 149, 151, 313–314
Ampicillin 314
Anidulafungin 152
Annulus of Zinn 15
Antiallergic drugs 182–192
antihistamines 184–188
mast cell stabilizers 188
Anti-angiogenic agents 235
aflibercept 235
bevacizumab 235
ranibizumab 235
Anti-glaucoma drugs
adverse effects, systemic 213
carbachol 211, 213
adverse effects 213
contraindications 213
therapeutic uses 213
ecothiophate 211, 213
adverse effects 213
contraindications 213
pilocarpine 211, 212
adverse effects 212
ocular adverse effects 212
Antihistamines 184–188
Anti-inflammatory therapy, in dry eyes 240
Antioxidants 72
Antiviral drugs 135–145, 136f
Aquaporins 10
Aqueous enhancement therapy, in dry eyes 240
Aqueous humor 13f, 23
Aqueous solutions 74
Artery
central retinal 16
ciliary 16
dorsal nasal 16
ethmoidal 16
lacrimal 16
maxillary 16
medial palpebral 16
meningeal 16
ophthalmic 3, 16
supratrochlear 16
Aspergillus niger 66
Aspergillus species 147
Aspirin 312
Atopic keratoconjunctivitis (AKC) 207
Atorvastatin 311
Atropine 90, 92
Augmentin 108
Autologous serum 243
Azathioprine 205
B
B. quintana 123
Bacillus anthracis 106, 120
Bacitracin
administration and dosage 130
contraindications of 131
in blepharitis 131
in chronic conjunctivitis 131
in corneal ulcers 131
in keratitis 131
mechanism of action of 130
Bacterial keratitis 111
Bacteroides
fragillis 111
species 108, 121
Bartonella henselae 123
Beclomethasone 312
Behçet's disease 205
Benzalkonium chloride (BAK) 66
Benzatropine 306
Beta lactam antibiotics 103
Beta-blockers 306
Betamethasone 178
Bifonazole 150
Bioadhesive hydrogels 77
Bioavailability enhancer excipients 68
BK virus 136
Blastomyces dermatitidis 147, 150
Blepharitis 111
Blepharocolysis 2
Blepharospasm 2
Blood ocular barriers 37
blood-aqueous 37
blood-retinal barriers (BRB) 37
Bordetella pertussis 123
Borrelia burgdorferi 121
Borrelia recurrentis 121
Botulinum toxin 256
Buffers 242
Bullous keratopathy 250
Busulphan 315
Butenafine 153
Butoconazole 150
C
C. pneumoniae 122
C. psittaci 122
Canal of Schlemm 11, 13
Candida spp. 66, 147–152, 154, 268
albicans 66, 268
Canis 153
Carbachol 256
Carbamazepine 308
Carbapenems 111
adverse effects of 112
in bacterial endophthalmitis 112
in prophylaxis of post-operative endophthalmitis 112
Carrier-mediated transport 29
active transport 29
facilitated diffusion 29
Caspofungin 152
Centrimonium 67
Cephalosporins 109,110t, 314
First generation 109
Fourth generation 110
Second generation 110
Third generation 110
Cevimeline 244
Chlamydia spp. 113, 122
pneumoniae 116
trachomatis 122
Chlorambucil 205
Chloramphenicol 112, 314
adverse effects 114
antibacterial spectrum 113
in corneal ulceration 114
in dacryoadenitis 114
in gonococcal conjunctivitis 114
in gonococcal corneal ulcer 114
mechanism of action 112
Chlorhexidine 68
Chloroquine 314
Chlorpheniramine 313
Cholinergic receptors 211, 211t
muscarinic 211
nicotinic 211
Cholinomimetic drugs 211
Chondroitin sulfate 242
Choroidal neovascularization 295
Ciliary body 13f
Ciliary ganglion 17, 24
Clobetasone butyrate (0.1%) 179
Clonazepam 307
Clostridia tetani 121
Clostridium
difficile 111, 122
perfringens 110
tetani 106
Clotrimazole 150
Coccidioides species 147
Codeine 307
Conjunctiva 2, 32
bulbar 32
forniceal 32
palpebral 32
Conjunctival hyperemia 199
Contact lenses 85, 265
cleaning systems 265
disinfection systems
hydrogen peroxide 268
multipurpose disinfecting solutions 268
disinfection systems of 266
enzymatic cleaners for 266
rewetting solutions for 269
storage case for 269
surfactant cleaners for 266
soft hydrogel 265
soft silicone hydrogel 265
Copper 272
deficiency 272
Corneal epithelial defects 199
Corneal herpetic lesions 139
Corneal hydrops 250
Corneal permeability coefficient 32
Corneal ulceration 111
Corneal ulcers 91, 131, 151
Corticosteroids
adverse effects 176
anti-inflammatory effect 174
classification 172
contraindications 177
immunosuppression effect 174
intraocular use 176
periocular use 175
systemic use of 176
therapeutic uses of 174
topical use of 175
Corynebacterium diphtheria 106, 121, 122
Cotton pledgets 85
Cryptococcus neoformans 147
Crystallin proteins 14
Crystalline lens 14
Cyanocobalamin (vitamin B12) 278
Cyclopentolate 92
Cyclophosphamide 205
Cycloplegia 90–91
Cyclosporin A 243
Cyclosporine 205, 316
adverse effects 207
formulations 206
mechanism of action 206f
therapeutic uses 207
Cytomegalovirus 136, 138, 139, 142, 143, 144
infections 141, 142
retinitis 142, 143, 144
D
Dacryoadenitis 111
Dacryocystitis 111
D-alanyl-D-alanine 106
Demecarium 306
Dendritic herpetic ulcer 140
Dendric ulcer 138
Desferoxamine 316
Dexamethasone 177, 312
Dexmethylphenidate 307, 316
Dextrothyroxine 311
Diabetic retinopathy 25, 230f
drugs used 232t
anti-VEGF drugs 231
bevacizumab 233
corticosteroids 233
dexamethasone 233
fluocinolone acetonide 234
pegaptanib 231
ranibizumab 231
triamcinolone acetonide 233
vitreolytic agent 234
mild NPDR 229
moderate NPDR 229
non-proliferative 229
proliferative (PDR) 229
severe NPDR 229
Diazepam 308
Didanosine 314
Difluprednate 0.05% 179
Digoxin 310
Diltiazem 310
Diphenhydramine 313
Diphenoxylate 316
Diuretics 310
Docetaxel 315
Dornase alfa 316
Dosage forms 74, 77t
Doxazosin 310
Drug absorption 30, 38
ocular 37
systemic route 36
oral 36
parenteral 36
topical route 30
transconjunctival 32
transcorneal 30
transscleral 33
Drug action
chemical reactions 55
inducing antibody formation 56
non-receptor mediated mechanisms 55
physical 56
protoplasmic poisons 56
targeting enzymes 56
Drug administration routes
intraocular 25
intracameral 25
intravitreal 25
periocular 22
peribulbar 24
retrobulbar 24
subconjunctival 22
sub-Tenon's 23
systemic 25
topical 21
Drug affinity 50
Drug effects measurement
graded dose-response curve 56
quantal dose-response curve 57
Drug safety measurement 58
Drug-drug interactions 63
Dry eyes 240
hormonal therapy in 240, 244
syndrome 207
treatment 240, 244
E
Echothiophate 306
Econazole 150
Endocytosis 30
Endophthalmitis 262
Enfuvirtide 314
Enterobacter species 108, 110, 112, 126, 129
Epidermophyton floccosum 153
Epithelial keratitis 140
Epstien barr virus 136, 139,142–144
Erythromycin 314
Escherichia coli 66, 107, 108, 112,113, 126, 129, 131
Estradiol 311
Estrogen 311
Ethambutol 314
Ethanol 308
Ethinylestradiol 311
Ethosuximide 308
Ethylene glycol dimethacrylate (EGDMA) 206
Etretinate 315
Excimer laser keratectomy 140
Extraocular irrigation 84
Eyeball injuries 5
Eyelid edema 199
F
Facilitated diffusion 29f
Fas ligands 16
Felbamate 308
Fenticonazole 150
Fluoroquinolones 103, 115- 119, 314
adverse effects 118t
contraindications 119
in acute bacterial conjunctivitis 117
in bacterial endophthalmitis 118
in bacterial keratitis 117
in blepharitis 117
in gonococcal corneal ulcer 117
in prophylaxis for post-operative endophthalmitis 118
interactions 119
Fluorometholone acetate 178
Fluvastatin 311
Folic acid (vitamin B9) 278
Fuch's endothelial dystrophy 250
Fusarium solani 268
G
Gabapentin 308
Gels 76
Gene therapy applications 292t
in corneal alkali burn 294
in corneal dystrophies 294
in corneal graft rejection 292
in corneal neovascularization 293
in corneal scarring and wound healing 293
in glaucoma 295
in ocular surface disorders 294
Genital herpes infection 141
Gentamicin 314
Glands
accessory glands of Krause 3
accessory lacrimal 3
lacrimal 3
Meibomian 1, 245
Glaucoma 14, 248, 249
Glucocorticoids 190
Gold 312
Gonococcal conjunctivitis 111
Gonococcal corneal ulceration 111
Gonococcus 109
Gramicidin 132
Granulomatosis 205
Growth factors 256
epidermal growth factor (EGF) 256
fibroblast growth factor (FGF) 257
transforming growth factors (TGFs) 257
Gypseum153
H
H. influenzae 108
H1 receptor blockers 184
adverse effects of 186t
pharmacological effects 185
anticholinergic effects 185
antiemetic effects 185
antiparkinsonian effects 185
sedation 185
topical ocular use 187
antazoline phosphate (0.5%) 187
pheniramine maleate (0.3 %) 187
pyrilamine maleate (0.1%) 187
mast cell stabilizing combinations 190, 190t
H2 receptor blockers 184t
Haemophilus influenzae 107, 108, 110, 121, 123, 126, 129
Hashish 308
Hepatitis B virus (HBV) 136
infections 136
Helicobacter pylori 107, 121, 123
Hemolytic Streptococcus 109
Hepatitis 262
Heroin 308
Herpes simplex
keratitis 137
keratoconjunctivitis 138
Herpes viruses 144
Herpes zoster 140, 141
Histamine 182
effects of 184t
Histoplasma capsulatum 147, 150
Homatropine 91
Horner's syndrome 2, 89
HSV 136, 141, 135
HSV-1 137–139, 141–144
HSV-2 137–139, 141, 143
Human immunodeficiency virus (HIV) 263
Human recombinant interferon 205
Hyaluronidase 256
Hydralazine 310
Hydrocortisone 312
Hydroxyamphetamine 90, 306
Hydroxyl ethyl methacrylate (HEMA) 206
Hydroxypropyl methylcellulose (HPMC) 255
Hyoscine 91
Hypermetropia 9
Hyperosmotic agents 246t, 247, 247f
glycerol (glycerin) 248
isosorbide 249
mannitol 248
topical 250
glycerol (glycerin) 250
hypertonic saline 250
Hyphema 199
Hypopyon 199
I
Ibuprofen 312
Indomethacin 312
Infective waste disposal 263
Infraorbital fissure 5
Infraorbital foramen 6
Infraorbital sulcus 5
Insulin 311
Interdigitalis 153
Interferons 208
adverse effects 209
mechanism of action 209
Inverse agonists 51
Ionotropic receptors (type I receptors) 52f
Iopamidol 316
Iritis 139, 140
Isocarboxazid 308
Isoniazid 314
Isosorbide 310
Isotretinoin 315
K
Keratitis 140, 131, 151
Keratoconjunctivitis 240
treatment approach 240
Ketorolac 190
Ketotifen 190
Klebsiella species 108,112, 126, 129, 131
L
Lacrimal
fossa 5
gland 3, 240, 245
papilla 3
sac 3
Lactamase inhibitor combinations 109
Lactoferrin 4
Lamivudin 314
Lamotrigine 308
L-ascorbate. See L-ascorbic acid
L-ascorbic acid 278
Laser-assisted in-situ keratomileusis (LASIK) 140
Lasik surgery 89
Leber's congenital amaurosis (LCA) 295
Leptospira species 121, 106
Leuprolide 316
Levator palpebrae muscle 1
Levetiracetam 308
Levonorgestrel 311
Levothyroxine 311
Lid scrubs 84
Linezolid 314
Lipid emulsion 243
Lipophilic drugs 31, 32
Listeria 111
Listeria species 106, 121, 122
Lithium 308
Local anesthetic
adverse effects 199
local 199
on cardiovascular system 199
on central nervous system 199
contraindications 200
injectables 196t
local infiltration 201
mechanism of action 197
peribulbar block 201
retrobulbar block 200
sub-Tenon's block 201
topical 195t, 201
Local anterior uveitis 199
Losartan 310
Loteprednol etabonate 178, 190
Lovastatin 311
LSD 308
Lutein 275
Lycopene 274f
M
M. scrofulaceum 122
Macrolides
adverse effects 124t
contraindications of 124
in bacterial conjunctivitis 123
in blephritis 123
in chronic or recurrent conjunctivitis 123
in trachoma 124
interactions of 124
mechanism of action of 122
Magnesium 272
deficiency 272
Manganese 273
deficiency 273
Marijuana 308
Mast cell stabilizers 188
adverse effects 189
cromolyn 188
disodium chromoglycate (cromolyn) 188
lodoxamide (0.1%) 189
mechanism of action 188
nedocromil sodium (2%) 189
ocular use 189
pemirolast (0.1%) 189
Measurement drug effects measurement 56
Medroxyprogesterone 311
Meibomian gland, dysfunction 2
Mescaline 308
Metabotropic receptors 53f
Methadone 308
Methotrexate 205, 315
Methyl dopa 310
Methyl phenidate 308
Methyl predinosolone 312
Methylphenidate 308
Micafungin 152
Miconazole 150–151
Microsporum
audouinii 153
canis 153
gypseum 153
Midazolam 307
Mitomycin C 257
Modified drug responses 59
acquired tolerance 60
acute tolerance 60
drug tolerance 59
natural tolerance 59
pharmacodynamic tolerance 60
pharmacokinetic tolerance 60
Molluscum contagiosum 136
Mometasone 312
Monobactams 112
Morphine 308
Mucoadhesives 69, 69t
Moraxella species 117
Muller's muscle 2, 88–89
paralysis of 2
Multiple dose administration and dosing schedule 46
Muscles
dilator pupillae 12
extraocular 15, 15f, 24
inferior oblique 1, 6, 15, 16
inferior rectus 6,15
lateral rectus 6, 15
medial rectus 6, 6f, 15
levator palpebrae superioris 1, 2, 16
superior oblique 15,6
superior rectus 15,6
Muller’s/superior tarsal 2
orbicularis oculi 1, 2
sphincter pupillae 12
superior tarsal 2
Mycobacterium spp. 117
Mycobacterium kansasii 122
Mycophenolate mofetil 205
Mycoplasma 113, 121
Mydriatics, Contradictions 88t
Mydriatics, indications 88t
Myopia 9
N
Naftifine 153
Nasolacrimal apparatus 3
Natamycin 147–149
Neisseria spp. 110,123, 130
gonorrhoea 106, 108, 110, 120, 126
meningitidis 106, 110, 126, 129
Nerves
abducent 17
frontal 6, 17
inferior ophthalmic 16
lacrimal 6, 17
maxillary 17
nasociliary 6, 17
oculomotor 2, 17, 24
ophthalmic 16, 17
optic 6, 12, 14, 17
trigeminal 2, 10
trochlear 17
zygomatic 17
Niacin 311
Niacinamide (vitamin B3) 277
Nifedipine 310
Nitrates 310
Nitroglycerine 310
Non-beta lactam antibiotics 112
in acute bacterial conjunctivitis 114
in blepharitis 114
in bacterial keratitis 114
Non-steroidal anti-inflammatory drugs (NSAIDs) 163
adverse effects 167
mechanism of action 164t
pharmacological actions 165
analgesic 166
anti-inflammatory action 166
antiplatelet action 166
therapeutic uses 166
analgesic 166
anti-inflammatory 167
antiplatelet action 167
antipyretic 167
Nonviral vectors
nanoparticles 291
hybrid metal-polymeric 291
metallic 291
polymeric 291
NSAIDs, Topical ocular use 169t
Nystatin 146–148
O
Ocular decongestants 190
adverse effects 191
naphazoline 191
oxymetazoline 191
phenylephrine 191
tetrahydrozoline 191
Ocular drug
bioavailability 38
distribution 39
elimination 41
metabolism and elimination 41
Ocular infection indications 109
Omega-3 fatty acids 240, 245
Omeprazole 313
Opioid (narcotic) analgesics 157
absorption 159
adverse effects 162
classification 159t
contraindications 162
head injury 162
impaired hepatic functions 162
impaired renal functions 162
reduced pulmonary function 162
distribution 159
mechanism of action 157
metabolism 159
pharmacological actions 160
analgesia 160
emesis 161
euphoria 160
histamine release 161
miosis 161
respiratory depression 160
sedation 160
suppression of cough reflex 161
receptor subtypes 158
dynorphins 158t
endorphin 158t
enkephalin 158t
therapeutic uses 161
acute pulmonary edema 162
analgesia 161
cough suppression 162
diarrhea 162
topical ocular use 163
Opium 308
Orbit 4
apperture 6, 7t
dimensions 5f
infection spread in 6
malignancy spread in 6
margins 5
walls 5,6t
fractures 6
inferior 6
lateral 6f
medial 6f
superior 6
Orbital apex syndrome 9
Orphenadrine 313
Oxacephems 112
Oxcarbazepine 308
Oxiconazole 150
Oxybutynin chloride 306
P
P. aeruginosa 110, 113, 116, 126
Paclitaxel 315
Palpebral fissure 89
Pantothenic acid (vitamin B5) 277
Papillary hypertrophy 199
Parabens 67
Paricalcitol 316
Parkinson's disease 2, 271
Partial agonists 51
Passive diffusion 28f, 31, 36
Pasteurella spp. 131
Penciclovir 140–141
Penetration enhancers 70
Penicillin-binding protein (PBP) 106
Penicillins
aminopenicillins 107
antipseudomonal penicillins 108
beta lactamase inhibitor combinations 108
natural penicillins 106
ophthalmic use 108
penicillin G 106
penicillin V 106
penicillinase-resistant penicillins 107
Peptococcus 121
Phagocytosis 3
Pharmacodynamics 50–64
Pharmacokinetics 28–47
acyclovir 314, 139–140
aminoglycosides 125,126
anesthetics, 195, 196, 197
azoles 150, 150t
bacitracin 130, 131
chloramphenicol 113
cidofovir 142,143
corticosteroids 172, 244
cotrimoxazole 129
disodium chromoglycate 188
echinocandins 152
famciclovir 140–141
flucytosine 148–149, 154
foscarnet 143–144
ganciclovir 141,142
griseofulvin 153
H1 receptor antagonists 185
hyperosmotic, 247, 247f
idoxuridine (IDU) 137
macrolides 122, 123
nanoparticle 296
NSAIDs 164
opioids 159
polyenes 146, 147, 147t
polymyxin B 131
terbinafine 154
tetracyclines 121
trifluridine 137
vidarabine 138
Phenobarbitone 308
Phenothiazines 308
Phenylephrine 88–90
Phenylephrine (10%), usage guidelines 90t
Phenytoin 308
Phospholipase C-inositol phosphate system 53
Physostigmine 91
Pilocarpine, contraindications 213
Pimecrolimus 208
Pinguecula 3
Pirenzepine 313
Pneumococcus 109, 117
Polyangiitis 205
Polyhexamethylenebiguanide 68
Polymeric gels 77
Polymyxin B
adverse effects 132
in blepharitis 132
in blepharoconjunctivitis 132
in conjunctivitis 132
in corneal ulcers 132
in keratitis 132
mechanism of action 131
Polyquaternium-1 67
Post-herpetic neuralgia 140
Post-operative endophthalmitis 262
Pralidoxime 306
Pravastatin 311
Prazosin 306
Prednisolone
acetate 177
sodium phosphate 177
Prednisone 312
Preservatives 65, 66t
Primidone 308
Progestogens 311
Propionibacterium 121
Proteus spp. 110, 126
mirabilis 107
Pseudomonal keratitis 111
Pseudomonas spp. 110, 111, 116
aeruginosa 66, 108, 112, 117, 126, 127, 131, 268
Psilocybin 308
Pterygium 3
Pterygopalatine ganglion 3
Ptosis 2, 89
Pupillary light reflex 19f
direct 18
indirect 18
Pyridoxine (vitamin B6) 277
Q
Quinidine 310
Quinine 314
Quinolones and fluoroquinolones 116t
first generation 116
fourth generation 116
in gonococcal conjunctivitis 117
mechanism of action 116
second generation 116
third generation 116
R
Ranitidine 313
Receptors 52
actions 55
desensitization 55
down-regulation 55
spare receptors 55
supersensitivity 55
upregulation 55
cytoplasmic receptors 54
enzyme-linked receptors 54
Retina 14
Retinal vein occlusion 235
anti-platelet therapy 236
drugs used 236
hydroxyethyl starch or dextran 236
ticlopidine 236
troxerutin 236
Retinitis 140, 142–143
Retinitis pigmentosa (RP) 295
Retinoic acid 316
Reuptake inhibitors 308
Riboflavin (vitamin B2) 276
Rickettsiae species 113, 120, 121,123
Rifabutin 314, 316
Rimexolone 178
Rofecoxib 312
Rosuvastatin 311
S
S. aureus 107, 108
S. pneumoniae 116
Salbutamol 306
Salmonella species 113, 107, 131
Sclera 11, 33
episclera 33
lamina fusca 33
stroma 33
Scleral spur 11
Scleritis 12
Scopolamine 91, 306
Secretagogues 240, 244
Selective serotonin 308
Selenium 273
Serratia spp. 126
marcescens 268
Sertaconazole 150
Shigella species 107, 113,129, 131
Sildenafil 316
Simvastatin 311
Sirolimus 205, 208
Sjogren's syndrome 244, 274
Smallpox 136
Sodium hyaluronic acid 255
Sodium perborate 68
Solifenacin succinate 306
Sorbic acid 67
Spirochetes 120
Sporothrix schenckii 147
SSRIS 308
Stabilized oxychloro complex (SOC) 68
Staphylococci 117
Staphylococcus spp. 106, 108, 111,113, 122, 130
aureus 66, 108, 129, 268
pyogenes 109
Sterilization methods 258
Streptococcus species 106,111, 120, 130
pneumoniae 129
pyogenes 129
viridans 129
Stromal keratitis 140
Subconjunctival
hemorrhage 24
injections 111
Sulconazole 150
Sulfonamides 128, 314
administration and dosage 129
adverse effects 129
local 129
systemic 130
classification 128
contraindications, 130
cotrimoxazole 129
mechanism of action 128
trimethoprim (TMP) 128
Sulfonylureas 311
Surfactants 71
Suspensions 74
Systemic drug 89
elimination half-life 43
excretion 42
first order kinetics 43
metabolism and excretion 41
mixed order kinetics 45
zero-order kinetics 44
T
Tacrolimus 205, 207
Tadalafil 316
Tamoxifen 311
Tamsulosin 306
Tarsal Meibomian glands 3
Tear film 2, 3, 240
Tenon's capsule 11f
Terazosin 310
Tetracyclines 120, 121, 244, 314
adverse effects 121
bacterial resistance of 121
blepharitis 121
classification 120, 120t
in acute conjunctivitis 121
in bacterial endophthalmitis 121
in bacterial keratitis 121
in corneal ulceration 121
in dacryoadenitis 121
in ophthalmia neonatorum 121
mechanism of action 120
TGF-B2 16
Thiabendazole 149
Thiamine 276
Thimerosal 67
Tiagabine 308
Ticarcillin disodium 108
Timentin 108
Tioconazole 150
Tolterodinet artrate 306t
Topiramate 308
Toxic anterior segment syndrome (TASS) 25
Trachoma 121
Treponema pallidum 106, 121, 123
Trichophyton
crateriform 153
gallinae 153
interdigitalis 153
megnini 153
mentagrophytes 153
rubrum 153
schoenleini 153
sulphureum 153
tonsurans 153
verrucosum 153
Trochlear fossa 5
Tropicamide 93
U
Unasyn 108
Ureaplasma 121
urealyticum 122
Uveitis 91
V
Vaccinia 138, 143
Valacyclovir 139, 140
Valdecoxib 312, 312
Valganciclovir 141–142
Valproic acid 308
Vardenafil 316
Varicella species 139
Varicella zoster virus (VZV) 135, 141–142
Vehicles 68
Vein
inferior ophthalmic 6, 16
infraorbital 16
superior ophthalmic 3, 6
Venlafaxine 308
Verapamil 310
Vernal conjunctivitis 189
Vibrio cholera 121
Vigabatrin 308
Viral vectors 287, 288f
adeno-associated virus (AAV) 288, 289, 295
recombinant 289
self-complementary 289
adenovirus (AV) 287, 295
lentivirus 290, 295
retrovirus 290
Viscosity enhancers 68
Visual pathway 18f
Vitamin A 274, 316
Vitamin B 276
Vitamin C 278
Vitamin D 275, 316
Vitamin E 276
Vitreous humor 14
Voclosporin 208
VZV 19, 138, 139, 141–143
W
Warfarin 315
Z
Zeazanthin 275
Zidovudine 314
Zinc 271
deficiency 271
toxicity 272
Zoster ophthalmicus 139
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1Textbook on Clinical Ocular Pharmacology and Therapeutics2
3Textbook on Clinical Ocular Pharmacology and Therapeutics
Editors SK Gupta PhD DSc FIPS FIACS Head, Clinical Research Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR) University of Delhi New Delhi, India Renu Agarwal PhD Faculty of Medicine Universiti Teknologi MARA Selangor, Darul Ehsan, Malaysia Sushma Srivastava PhD Department of Pharmacology Delhi Institute of Pharmaceutical Sciences and Research (DIPSAR) University of Delhi New Delhi, India
4
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Textbook on Clinical Ocular Pharmacology and Therapeutics
First Edition: 2014
9789351523413
Printed at
5Contributors
6
7Preface
The eye and the drugs used to treat ophthalmic ailments, although have been the attractive areas for scientific investigations since the ancient time; 21st century has witnessed explosive growth and development in this field. The students and practitioners are now confronted with the dilemma of how to consolidate basic concepts of pharmacology and knowledge about the newly developed drugs. This book aims to provide essential knowledge of the basic concepts of pharmacology, their application in ocular pharmacology and basic pharmacology of commonly used drugs in ophthalmology. The book also discusses the possible adverse drug reactions of systemically administered drugs. The ophthalmologists and postgraduates will find the book very useful in understanding basic pharmacology concepts, which can be utilized in therapeutics. The contents of the book are formatted in a way to provide quick to the point and easy access to the relevant matter. We believe that the subject matter in this book will be very useful for practicing ophthalmologist as a guide to answer questions that commonly arise during patient care. At the same time students find it useful to prepare for various board and certificate examinations. Although, this book can be used as quick reference, it provides enough subject matter to be used as stand-alone text without reference to larger volumes. Contents of the book have been organized with great caution; however, the feedback from the students and clinicians would be invaluable in improving the format as well as the contents of the book in future editions.
We sincerely thank all authors who have contributed immensely in putting the subject matter of this book in its current form. Without their expertise and time, this book would not be complete.
We shall feel highly rewarded if the objectives of presenting this book are fulfilled and students and practitioners can use it to their advantage in understanding the subject.
SK Gupta
Renu Agarwal
Sushma Srivastava
8
9Acknowledgments
I acknowledge the financial support from Department of Science and Technology (DST), New Delhi, for the financial assistance received under USERS project. My sincere thanks to Dr SS Kohli, Scientist F/Director, SERC division, DST, for his constant support and encouragement.
I thank all the contributors for their outstanding contributions. Despite their busy schedule and pressing commitments, they have put their best effort to give shape to this textbook.
My special thanks to my colleagues and students at Delhi Institute of Pharmaceutical Sciences and research, for their valuable help in editorial assistance, without which this task would have been meaningless.
SK Gupta
10
11DRUGS USED IN OCULAR THERAPEUTICS AT A GLANCE
Ocular therapeutics in recent years has undergone tremendous changes not only in terms of introduction of new drugs and new drug classes but also in terms of development of novel drug delivery systems. This introductory section presents a summary for quick reference to currently used drugs from different therapeutic classes. The chapters that follow this section will discuss the basic and clinical pharmacology of each of these drug classes and drugs.
Drug (generic)
Drug class
Clinical use
Trade name
Formulation
Route of administration
MYDRIATICS AND CYCLOPLEGICS
Atropine sulfate
Anticholinergic
Pupillary dilatation and cycloplegia
Atropine-care
Solution 1%
Ointment 1%
Topical
Isopto atropine
Generic
Homatropine hydrobromide
Anticholinergic
Pupillary dilatation and cycloplegia
Isopto homatropine
Solution 2%, 5%
Topical
Generic
Cyclopentolate hydrochloride
Anticholinergic
Pupillary dilatation and cycloplegia
Cyclogyl
Solution 0.5%, 1%, 2%
Topical
AK-Pentolate
Solution 1%, 2%
Generic
Solution 1%
Tropicamide
Anticholinergic
Pupillary dilatation and cycloplegia
Tropicacyl
Solution 0.5%, 1%,
Topical
Mydriacyl
Generic
Scopolamine hydrobromide
Anticholinergic
Pupillary dilatation and cycloplegia
Isopto hyoscine
Solution 0.25%
Topical
Phenylephrine hydrochloride
Sympathomimetic
Pupillary dilatation
Mydfrin
Solution 2.5%
Topical
Neo-Synephrine
Solution 2.5%
AK-Dilate
Solution 2.5%, 10%
Generic
Solution 2.5%, 10%
Hydroxyamphetamine hydrobromide/tropicamide
Sympathomimetic/ anticholinergic
Pupillary dilatation and cycloplegia
Paremyd
Solution 1%/0.25%,
Topical
Following combinations are also available in India:
Atropine sulphate 1% w/v, chloramphenicol 0.5%, dexamethasone sodium phosphate 0.1%.
Atropine sulphate 1%, prednisolone 0.25%, chlorobutanol 0.5%.
Atropine sulphate 10 mg, tetracycline 10 mg.
Cyclopentolate 1%, dexamethasone sodium phosphate 0.1%.
Cyclopentolate hydrochloride 1%, phenylephrine hydrochloride 5%.
Phenylephrine hydrochloride 5%, tropicamide 0.8%.
Homatropine hydrobromide 2%, chlorbutol 0.5%.
Tropicamide 0.8%, phenylephrine 5%.
Tropicamide 0.8%, phenylephrine hydrochloride 0.5%.
Tropicamide 0.8% w/v, phenylephrine hydrochloride 5%.
Tropicamide 1%, chlorbutol 0.5%
12
ANESTHETIC AGENTS
Lidocaine hydrochloride
Amide type of local anesthetic
Ocular surface anesthesia
Akten
Solution 3.5%
Proparacaine hydrochloride
Ester type of local anesthetic
Ocular surface anesthesia
Alcaine
Solution 0.5%
Ocu-caine
Ophthetic
Paracaine
Generic
Tetracaine hydrochloride
Ester type of local anesthetic
Ocular surface anesthesia
Generic
Solution 0.5%
Following injectable anesthetic agents are available for regional anesthesia:
  1. Bupivacaine (Amide type): 0.25–0.75%
  2. Lidocaine (Amide type): 1–2%/500 mg
  3. Mepivacaine: (Amide type): 1–2%/500 mg
  4. Prilocaine (Amide type): 1–2%/600 mg
  5. Etidocaine (Amide type): 1%
  6. Procaine (Ester type): 1–2%/500 mg
  7. Tetracaine (Ester type): 0.25%
ANTI-INFLAMMATORY AGENTS
Diclofenac sodium
NSAID
Ocular inflammation
Voltaren
Solution 0.1%
Generic
Flurbiprofen sodium
NSAID
Ocular inflammation
Ocufen
Solution 0.03%
Generic
Bromfenac
NSAID
Ocular inflammation
Bromday
Solution 0.09%
Nepafenac
NSAID
Ocular inflammation
Nevanac
Solution 0.1%
Ketorolac tromethamine
NSAID
Ocular inflammation, seasonal allergic conjunctivitis
Acular®
Solution 0.5%
Acular LS
Solution 0.4%
Acular PF (Preservative free)
Solution 0.5%
Generic
Solution 0.5%
ANTI-HISTAMINICS, DECONGESTANTS, ASTRINGENT
Olopatadine hydrochloride
Histamine H1- antagonist, Mast cell inhibitor
Seasonal allergic conjunctivitis
Patanol
Solution 0.1%
Topical
Pataday
Solution 0.2%
Epinastine hydrochloride
Histamine H1-, H2-antagonist, Mast cell inhibitor
Seasonal allergic conjunctivitis
Elestat
Solution 0.05%
Topical
Generic
Azelastin hydrochloride
Histamine H1-antagonist, Mast cell inhibitor
Seasonal allergic conjunctivitis
Optivar®
Solution 0.05%
Topical
Generic
Emedastine difumarate
Histamine H1-antagonist
Seasonal allergic conjunctivitis
Emadine®
Solution 0.05%
Topical
13
ANTI-HISTAMINICS, DECONGESTANTS, ASTRINGENT
Alcaftadine
Histamine H1-antagonist, Mast cell inhibitor
Seasonal allergic conjunctivitis
Lastacaft
Solution 0.25%
Topical
Ketotifen fumarate
Histamine H1-antagonist, Mast cell inhibitor
Seasonal allergic conjunctivitis
Alaway
Solution 0.025%
Topical
Zaditor
Generic
Naphazoline hydrochloride + antazoline phospahte
Sympathomimetic + Histamine H1-antagonist
Seasonal allergic conjunctivitis
Albalon
Solution 0.05% + 0.5%
Topical
Vasocon-A
Naphazoline hydrochloride + pheniramine maleate
Sympathomimetic + Histamine H1-antagonist
Seasonal allergic conjunctivitis, decongestant, astringent
Naphcon-A
Solution 0.025% + 0.3%
Topical
Visine-A
Opcon-A
Cromolyn sodium
Mast cell inhibitor
Seasonal allergic conjunctivitis
Crolom
Solution 4%
Topical
Generic
Nedocromil sodium
Mast cell inhibitor
Seasonal allergic conjunctivitis
Alocril
Solution 2%
Topical
Lodoxamide tromethamine
Mast cell inhibitor
Seasonal allergic conjunctivitis
Alomide
Solution 0.1%
Topical
Pemirolast potassium
Mast cell inhibitor
Seasonal allergic conjunctivitis
Alamast
Solution 0.1%
Topical
Naphazoline hydrochloride
Sympathomimetic
Decongestant
AK-Con
Solution 0.1%
Topical
Albalon
Solution 0.1%
All clear
Solution 0.012%
All clear AR
Solution 0.03%
Clear Eyes
Solution 0.012%
Generic
Phenylephrine hydrochloride
Sympathomimetic
Decongestant
AK-Nefrin
Solution 0.12%
Topical
Generic
Oxymetazoline hydrochloride
Sympathomimetic
Decongestant
Visine LR
Solution 0.025%
Topical
Tetrahydrozoline hydrochloride
Sympathomimetic
Decongestant
Murine Tear Drops
0.05%
Topical
Visine
Visine Advanced Relief
Generic
Naphazoline hydrochloride + zinc sulfate
Sympathomimetic
Decongestant, astringent
Clear Eyes ACR
0.0125%
Topical
14
ANTI-HISTAMINICS, DECONGESTANTS, ASTRINGENT
Naphazoline hydrochloride + polysorbate 80
Sympathomimetic
Decongestant, astringent
VIVA Lubricating Redness Relief
Topical
Tetrahydrozoline + zinc sulfate
Sympathomimetic
Decongestant, astringent
Visine AC
0.05%
Topical
Following combinations are available in India:
Sodium chloride 0.05%, boric acid 1.25%, chlorpheniramine maleate 0.01%, naphazoline hydrochloride 0.056%, zinc sulfate 0.012%
Diclofenac sodium 1 mg, gentamicin sulfate 3 mg/mL.
Ketorolac tromethamine 4 mg, ofloxacin 3 mg/mL.
Naphazoline 0.15%, methylcellulose 0.2%, chlorpheniramine maleate 0.01%.
Ketorolac 0.5 %, fluorometholone 0.1%.
Triamcinolone acetonide 1 mg, gramicidin 0.25 mg, neomycin sulphate 2.5 mg/g.
Ketorolac trometamol, ofloxacin.
Ketorolac trometamol 0.5%, chlorpheniramine maleate 0.2%, phenylephrine hydrochloride 0.12%.
Phenylephrine hydrochloride 0.12%, naphazoline hydrochloride 0.05%, menthol 0.005%, camphor 0.01%.
STEROIDS
Dexamethasone sodium phosphate
Glucocorticoid
Anti-inflammatory
Ocu-Dex
Solution, Ointment 0.1%, 0.5%
Topical
Maxidex
Suspension 0.1%, Ointment 0.1%, 0.5%
Fluorometholone
Glucocorticoid
Anti-inflammatory
FML SOP
Ointment 0.1%
Topical
Fluor-Op
FML
FML Forte
Generic
Suspension 0.1%
Suspension 0.1%
Suspension 0.25%
Suspension 0.1%
Flarex
Suspension 0.1%
Loteprednol etabonate
Glucocorticoid
Anti-inflammatory
Lotemax
Ointment 0.5%
Suspension 0.5%
Topical
Alrex
Suspension 0.2%
Prednisolone acetate
Glucocorticoid
Anti-inflammatory
Ecocnopred
Suspension 1%
Topical
Omnipred
Generic
Pred Forte
Pred Mild
Suspension 0.12%
Prednisolone sodium phosphate
Glucocorticoid
Anti-inflammatory
AK-Pred
Solution 1%
Topical
Generic
Solution 0.125% and 1%
Difluprednate
Glucocorticoid
Anti-inflammatory
Durezol
Emulsion 0.05%
Topical
Medrysone
Glucocorticoid
Anti-inflammatory
HMS
Suspension 1%
Topical
15
STEROIDS
Rimexolone
Glucocorticoid
Anti-inflammatory
Vexol
Suspension 1%
Topical
Fluocinolone acetonide
Glucocorticoid
Anti-inflammatory
Retisert
0.59 mg
Intraocular
Ozurdex
Glucocorticoid
Anti-inflammatory
Dexamethasone
0.70 mg
Intraocular
Triamcinolone acetonide
Glucocorticoid
Anti-inflammatory
Triesence
40 mg/mL
Intraocular
Trivaris
80 mg/mL
ANTIGLAUCOMA AGENTS
Apraclonidine hydrochloride
Sympathomimetic
Oculohypotensive
Iopidine
Solution 0.5%, 1%
Topical
Generic
Solution 0.5%
Brimonidine tartrate
Sympathomimetic
Oculohypotensive
Alphagan P
Solution 0.1%, 0.15%
Topical
Generic
Solution 0.15%, 0.2%
Dipivefrin hydrochloride
Sympathomimetic
Oculohypotensive
Propine
Solution 0.1%
Topical
Generic
Epinephrine hydrochloride
Sympathomimetic
Oculohypotensive
Generic
Solution 0.5%, 1%, 2%
Topical
Betaxolol hydrochloride
Beta-blocker
Oculohypotensive
Betoptic-S
Solution 0.25%
Topical
Generic
Solution 0.5%
Levobunolol hydrochloride
Beta-blocker
Oculohypotensive
Betagan
Solution 0.25%, 0.5%
Topical
Generic
Carteolol hydrochloride
Beta-blocker
Oculohypotensive
Generic
Solution 1%
Topical
Metipranolol
Beta-blocker
Oculohypotensive
OptiPranolol
Solution 0.3%
Topical
Generic
Timolol hemihydrate
Beta-blocker
Oculohypotensive
Betimol
Solution 0.25%, 0.5%
Topical
Timolol maleate
Beta-blocker
Oculohypotensive
Timoptic
Solution 0.25%, 0.5%
Topical
Timoptic-XE
Gel 0.25%, 0.5%
Generic
Solution and Gel 0.25%, 0.5%
Pilocarpine hydrochloride
Cholinomimetic
Oculohypotensive
Isopto carpine
Solution 1%, 2%, 4%
Topical
Pilopine-HS
Gel 4%
Generic
Solution 0.5%, 1%, 2%, 3%, 4%, 6%
16
ANTIGLAUCOMA AGENTS
Carbachol
Cholinomimetic
Oculohypotensive
Isopto carbachol
Solution 1.5%, 3%
Topical
Miostat
Solution 0.01%
Latanoprost
Prostaglandin analog
Oculohypotensive
Xalatan
Solution 0.005%
Topical
Generic
Bimatoprost
Prostaglandin analog
Oculohypotensive
Lumigan
Solution 0.01%, 0.03%
Topical
Travoprost
Prostaglandin analog
Oculohypotensive
Travatan
Solution 0.004%
Topical
Travatan-Z
Dorzolamide hydrochloride
Carbonic anhydrase inhibitor
Oculohypotensive
Trusopt
Solution 2%
Topical
Generic
Brinzolamide
Carbonic anhydrase inhibitor
Oculohypotensive
Azopt
Solution 1%
Topical
Methazolamide
Carbonic anhydrase inhibitor
Oculohypotensive
Generic
Tablets 25 mg, 50 mg
Oral
Acetazolamide
Carbonic anhydrase inhibitor
Oculohypotensive
Diamox
Tablets 125 mg, 250 mg, Capsules extended release 500 mg
Oral
Glycerine
Hyperosmotic agent
Oculohypotensive
Osmoglyn
Solution 50%
Oral
Mannitol
Hyperosmotic agent
Oculohypotensive
Osmitrol
Solution 5–20%
Intravenous
Urea
Hyperosmotic agent
Oculohypotensive
Ureaphil
Powder (4 g) to be reconstituted to 30% solution
Intravenous
Following combinations are available in India:
Brimonidine tartrate, timolol maleate.
Brimonidine tartrate 2 mg, timolol maleate 5 mg.
Timolol, bimatoprost.
Dorzolamide 2%, timolol 0.5%.
Bimatoprost 0.03%, timolol 0.5%.
Timolol maleate 0.5%, pilocarpine 2%.
Latanoprost 0.005%, timolol maleate 0.5%.
ANTIBACTERIAL AGENTS
Ciprofloxacin
Fluoroquinolone
Extraocular and intraocular infections
Ciloxan
Solution and Ointment 0.3%
Topical Intravenous: 500 mg/8 hours
Gatifloxacin
Fluoroquinolone
Extraocular and intraocular infections
Zymaxid
Solution 0.5%
Topical
Zymar
Solution 0.3%
Levofloxacin
Fluoroquinolone
Extraocular and intraocular infections
Iquix
Solution 1.5%
Topical Intravenous: 500 mg/24 hours
Quixin
Solution 0.5%
Moxifloxacin
Fluoroquinolone
Extraocular and intraocular infections
Moxeza
Solution 0.5%
Topical Intravenous: 400 mg/24 hours
Vigamox
17
ANTIBACTERIAL AGENTS
Besifloxacin
Fluoroquinolone
Extraocular and intraocular infections
Besivance
Solution 0.6%
Topical
Ofloxacin
Fluoroquinolone
Extraocular and intraocular infections
Ocuflox
Solution 0.3%
Topical
Sulfacetamide
Sulfonamide
Extraocular infections
Bleph-10
Solution 10%
Topical
Sulf-10
Solution 10%
Ointment 10%
Sulf-10 preservative free
Gentamicin sulfate
Aminoglycoside
Extraocular and intraocular infections
Genoptic
Solution 0.3%
Topical
Subconjunctival: 10–20 mg
Intravitreal: 100–200 μg
Intravenous: 3–5 mg/kg daily in 2–3 divided doses
Genoptic SOP
Ointment 0.3%
Gentak
Solution 0.3% Ointment 0.3%
Tobramycin sulfate
Aminoglycoside
Extraocular and intraocular infections
AK-Tob
Solution 0.3%
Topical
Subconjunctival: 10–20 mg
Intravitreal: 100–200 μg
Intravenous: 3–5 mg/kg daily in 2–3 divided doses
Tobrex
Solution 0.3%, Ointment 0.3%
Tobrasol
Solution 0.3%
Neomycin sulfate
Aminoglycoside
Extraocular and intraocular infections
Neomycin sulfate
Solution 0.5%
Topical
Subconjunctival: 125–250 mg
Amikacin sulfate
Aminoglycoside
Extraocular and intraocular infections
Amikin
Solution 0.3%
Topical
Subconjunctival: 25 mg
Intravitreal: 400 μg
Intravenous: 3–15 mg/kg daily in 2–3 divided doses
Kanamycin sulfate
Aminoglycoside
Extraocular and intraocular infections
Kanamycin sulfate
Solution 0.5%
Topical
Subconjunctival: 30 mg
Intravitreal: 500 μg
Ampicillin sodium
Penicillin
Intraocular infections
Topical: 50 mg/mL
Subconjunctival: 50–150 mg
Intravitreal: 5 mg
Intravenous: 4–12 g daily in 2–3 divided doses
18
ANTIBACTERIAL AGENTS
Penicillin G
Penicillin
Intraocular infections
Topical: 100,000 units/mL
Subconjunctival: 0.5–1 million units
Intravitreal: 300 units
Intravenous: 12–24 million units daily in 4–6 divided doses
Piperacillin
Penicillin
Intraocular infections
Topical: 12.5 mg/mL
Subconjunctival: 100 mg
Ticarcillin disodium
Penicillin
Intraocular infections
Topical: 6 mg/mL
Subconjunctival: 100 mg
Cefazolin sodium
Cephalosporin
Intraocular infections
Topical: 50 mg/mL
Subconjunctival: 100 mg
Intravitreal: 2250 μg
Intravenous: 2–4 g daily in 3–4 divided doses
Ceftazidime
Cephalosporin
Intraocular infections
Topical: 50 mg/mL
Subconjunctival: 100 mg
Intravitreal: 2000 μg
Intravenous: 1 g daily in 2–3 divided doses
Ceftriaxone
Cephalosporin
Intraocular infections
Topical: 50 mg/mL
Intravenous: 1–4 g daily in 1–2 divided doses
Erythromycin
Macrolide
Extraocular and intraocular infections
Topical: Ointment 0.5%, solution 50 mg/mL
Subconjunctival: 100 mg
Intravitreal: 500 μg
Azithromycin
Macrolide
Extraocular and intraocular infections
Azasite
Topical solution 1% Intravenous: 500 mg
Clarithromycin
Macrolide
Extraocular and intraocular infections
Topical: 10 mg/mL
Bacitracin zinc
Bacitracin
Extraocular and intraocular infections
Topical: 10,000 units/mL, Ointment 500 units/g
Subconjunctival: 5000 units
Polymyxin B sulfate
Polymyxin
Extraocular and intraocular infections
Topical: 10,000 units/mL, Subconjunctival: 10,000 units
Vancomycin hydrochloride
Glycopeptide
Extraocular and intraocular infections
Topical: 12.5–25 mg/mL
Subconjunctival: 25 mg
Intravitreal: 1000 μg
Intravenous: 15–30 mg/kg daily in 1–2 divided doses
Imipenem/Cilastatin sodium
Carbapenem
Extraocular and intraocular infections
Topical: 5 mg/mL
Intravenous: 2 g daily in 3–4 divided doses
Combinations of antibacterial agents
Combination
Trade name
Formulation
Bacitracin/hydrocortisone/neomycin/polymyxin
Generic
Suspension, Ointment: 400 units—1%
Polymyxin B/bacitracin Zinc
AK-Poly-Bac Generic
Ointment: 10,000–500 units/g
19
ANTIBACTERIAL AGENTS
Polymyxin B/neomycin/bacitracin
Neosporin
Generic
Solution: 10,000 units—1.75–0.025 mg/mL Ointment: 10,000 units—3.5 mg–400 units/g
Polymyxin B/neomycin/gramicidin
Neosporin
Generic
Solution: 10,000 units—1.75–0.025 mg/mL Ointment: 10,000 units—3.5 mg–400 units/g
Polymyxin B/trimethoprim
Polytrim
Generic
Solution: 10,000 units—1 mg/mL
Dexamethasone/neomycin/polymyxin B
Poly-Dex
Suspension and ointment: 0.1%—3.5 mg/mL– 10,000 units/mL
Maxitrol
Suspension and ointment: 0.1%—3.5 mg/mL–10,000 units/mL
Dexasporin
Suspension: 0.1%—3.5 mg/mL–10,000 units/mL
AK- Trol
Ointment: 0.1%—3.5 mg/mL–10,000 units/mL
Dexamethasone/tobramycin
Tobradex
Generic
Suspension and ointment: 0.1–0.3%
Fluoromethalone-sulfacetamide
FML-S
Suspension: 0.1–10%
Gentamicin–prednisolone acetate
Pred-G
Suspension: 0.3–1.0%
Ointment: 0.3–0.6%
Pred-G SOP
Loteprednol etabonate–tobramycin
Zylet
Suspension: 0.5–0.3%
Prednisolone acetate – Neomycin – Polymyxin B
Poly-Pred
Suspension: 0.5–0.35%–10,000 units/mL
Generic
Prednisolone acetate – Sulfacetamide
Blephamide
Suspension: 0.2–10%
Blephamide SOP
Ointment: 0.2–10%
Prednisolone sodium phosphate – Sulfacetamide
Vasocidin
Solution: 0.23–10%
Generic
Following combinations are also available in India:
Moxifloxacin hydrochloride 5 mg, dexamethasone phosphate 1 mg.
Chloramphenicol 5%, beclometasone dipropionate 0.025%, clotrimazole 1%, lignocaine hydrochloride 2%.
Bacitracin 500 u and polymyxin B sulfate 10,000 u.
Trimethoprim 1 mg, polymyxin B sulfate 10000 IU, polyvinyl alcohol 0.25%.
Ciprofloxacin 0.3%, dexamethasone 0.01%.
Chloramphenicol 0.2%, prednisolone acetate 0.5%.
Chloramphenicol 0.5%, dexamethasone sodium phosphate 0.1%.
Chloramphenicol 0.5 % dexamethasone 0.01 %.
Chloramphenicol 0.5%, atropine 1%, dexamethasone 0.01%,.
Neomycin 0.5%, dexamethasone 0.01%.
Neomycin sulfate 0.5%, dexamethasone sodium phosphate 0.1%.
Moxifloxacin hydrochloride 0.5%, ketorolac 0.5%
Gatifloxacin 0.3%, dexamethasone 0.1%.
Polymyxin B 5000 IU, chloramphenicol 10 mg, betamethasone 1 mg.
Ofloxacin 0.3%, prednisolone acetate 1%, benzalkonium chloride 0.05%.
Polymyxin B sulfate 5000 IU, chloramphenicol 10 mg.
Ofloxacin 0.3%, betamethasone 0.01%.
Ofloxacin 0.3%, dexamethasone 0.01%.
Chloramphenicol 0.5%, flurbiprofen sodium 0.03%.
Gatifloxacin 0.3%, dexamethasone 0.01%.
Gatifloxacin 0.3%, prednisolone acetate 1%.
Gentamycin 0.3%, dexamethasone 0.01%.
Gentamycin sulfate 0.3%, hydrocortisone acetate 1%.
Gentamicin sulfate 0.3%, betamethasone sodium phosphate 0.1%
Ofloxacin 0.3%, dexamethasone 0.1%.
Ketorolac tromethamine 5 mg, ofloxacin 3 mg/1 mL.
Tobramycin sulfate 0.3%, fluorometholone 1%.
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ANTIFUNGAL AGENTS
Amphotericin B
Ambisome (intravenous)
Topical: 0.1–0.5% solution
Subconjunctival: 0.8–1.0 mg
Intravitreal: 5 μg
Intravenous: 3–5 mg/kg/day
Natamycin
Natacyn
Topical: 5% suspension
Fluconazole
Diflucan
Oral: 150 mg single dose; 200 mg on day 1 followed by 100 mg daily; 400 mg on day 1 followed by 200 mg daily.
Intravenous: 100–400 mg daily
Itraconazole
Sporanox
Oral: 200–400 mg daily
Intravenous: 200 mg twice a day for 2 days followed by 200 mg daily for 14 days
Voriconazole
Vfend
Topical: 1% solution prepared from IV formulation.
Oral: 200 mg twice a day
Intravenous: 3–6 mg/kg every 12 hours
Clotrimazole
Oral: One troche 5 times a day
Ketoconazole
Nizrol
Oral: 200–400 mg/day
Posaconazole
Noxafil
Oral: 200 mg thrice daily; 100 mg twice on day 1 followed by 100 mg/day for 13 days; 400 mg twice a day
Anidulafungin
Eraxis
Intravenous: 100 mg/day
Caspofungin
Cancidas
Intravenous: 50 mg/day
Mycafungin
Mycamine
Intravenous: 100 mg/day
Flucytosine
Ancobon
Oral: 50–150 mg/kg daily in 4 divided doses
Griseofulvin
Oral: 500 mg/day
Oral (Ultramicrosize): 375–750 mg/day
Terbinafine
Lamisil
Oral: 250 mg/day
ANTIVIRAL AGENTS
Acyclovir sodium
Zovirax
Generic
Herpes simplex keratitis (Acute infection): Oral: 400 mg 5 times/day for 1–2 weeks
Herpes simplex keratitis (Prophylaxis): Oral: 400 mg twice/day
Herpes zoster ophthalmicus: Oral: 800 mg 5 times/day for 7–10 days
Famcyclovir
Famvir
Herpes zoster ophthalmicus: Oral: 500 mg 3 times/day for 7 days
Gencyclovir sodium
Zirgan
Herpes dendritis keratitis: Topical 0.15% gel, 5 times/day until the ulcer heals followed by 3 times a day for 7 days
Cytovene
Intravitreal: 200 μg
Intravenous: Induction—5 mg/kg administered over 1 hours, every 12 hours for 2–3 weeks; Maintenance: 5 mg/kg/day for 7 days/week or 6 mg/kg/day for 5 days/week
Vitrasert
Intravitreal insert: 4.5 mg-releases drug over 5–8 months
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ANTIVIRAL AGENTS
Valacyclovir
Valtrex
Herpes zoster ophthalmicus: Oral: 1 g thrice/day for 7 days
Valganciclovir
valcyte
CMV retinitis: Oral: Induction: 900 mg/12 hours for 21 days.
Maintenance: 900 mg/day
Cidofovir
Vistide
Intravenous: Induction—5 mg/kg administered over 1 hours once a week for 2 weeks.
Maintenance: 5 mg/kg infusion over 1 hours once every 2 weeks
Foscarnate sodium
Foscavir
Intravenous: Induction—60 mg/kg (adjusted to renal function) over 1 hour/8 hours for 2–3 weeks.
Maintenance: 90–120 mg/kg over 2 hours once daily
OFF -LABEL DRUGS USED IN OPHTHALMOLOGY
DRUGS
COMMON USES
ACTION AND DOSE
Acetylcysteine
Used in corneal conditions like burns, filamentary keratitis, keratoconjunctivitis sicca, corneal melts
Acts by inhibiting collagenase, which delays the corneal healing
Dose: Hourly in acute cases, up to 4 times/day for maintenance
Alteplase (tissue plasminogen activator)
Intraocular injection in postvitrectomy patients to treat fibrin formation, to remove fibrin membranes occluding intraocular portions of shunts
Acts as a thrombolytic agent. There is significant risk of hyphema formation
Dose: 3–6 μg postvitrectomy, 6–12 μg to remove fibrin membranes
5-Fluorouracil
Post-glaucoma filtering surgery (indicated in patients with high risk of surgical failure)
It is an antimetabolite acts by inhibiting fibroblast proliferation. Associated with risk of conjunctival wound leak, corneal epithelial defects, keratitis, hypotony, reduced visual acuity
Dose: Postoperative: Subconjunctival 5 g twice/day for 7 days followed by once daily for 7 more days
Intraoperative: 50 mg/mL solution soaked in murocell sponge for 3–5 minutes
Mitomycin C
Same as 5-Fluorouracil
Additionally has ben used to prevent recurrence after pterygium surgery and to reduced scarring after corneal surgery such as excimer laser
Its action and complications are same as 5-Fluorouracil
Dose: Intraoperative: Applied once 0.02–0.04% on a small piece of Gelfilm or Weck cell sponge
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OFF -LABEL DRUGS USE IN OPHTHALMOLOGY
Bevacizumab (Avastin)
Used in age-related macular degeneration, macular edema due to retinal vein occlusion or diabetic retinopathy.
Also used as surgical adjunct in procedures for treatment of neovascular glaucoma
Humanized monoclonal antibody. Acts by inhibiting vascular endothelial growth factor-A
Dose: 1.25 mg intravitreal
Cyclosporin (Sandimmune)
Used to prevent transplant rejection after keratoplasty
Also used to treat severe vernal conjunctivitis, ligneous conjunctivitis and noninfectious peripheral ulcerative keratitis associated with systemic autoimmune disorders
Acts as an immunosuppressant with high selectivity of T lymphocytes
Dose: 0.5–2% topical
Doxycycline and Minocycline
Used to treat ocular rosacea meibomianitis and some conditions involving corneal melting.
Tetracyclines act by inhibiting bacterial protein synthesis
Dose: 100 mg 1–2 times per day for 2–12 weeks
Source: PDR for Ophthalmic Medicines; 40th Edition, 2012; MIMS, India.