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Ocular Pharmacotherapy
José Manuel Benítez-del-Castillo, David Díaz-Valle, José Antonio Gegúndez-Fernández
CHAPTER 1:
Ophthalmic Pharmaceuticals: New Formulations
Introduction
Bioavailability of ophthalmic formulations and routes of administration
Ophthalmic topical formulations
Conventional Ophthalmic Formulations
Eyedrops
Other Topical Ophthalmic Formulations: Aqueous Suspensions, Semisolid Preparations, and Artificial Tears
Intraocular formulations
Novel formulations of ocular administration
Novel Topical Ophthalmic Formulations
Intraocular Drug Delivery Systems
CHAPTER 2:
Topical Anesthetics
History
Local anesthetics
Definition
Chemical Structure
Factors affecting the quality of the anesthesia
Anesthetic agents
Topical Anesthetic Agents
Cocaine
Tetracaine
Benoxinate or Oxybuprocaine
Proparacaine
Lidocaine
Toxicity of Topical Anesthetic Agents
Ocular Surface
Hypersensitivity
Systemic Adverse Events
Choice of types of anesthesia
General Anesthesia
Local Anesthesia
Retrobulbar Anesthesia (Intraconal)
Peribulbar Anesthesia (Extraconal)
Sub-Tenon's Anesthesia (Parabulbar)
Topical Anesthesia
CHAPTER 3:
Ocular Surface Dyes
Introduction
How to grade corneal and conjunctival staining
Fluorescein
Rose Bengal
Lissamine green
Sulforhodamine B
CHAPTER 4:
Mydriatics and Cycloplegics
Definition
Indications
Diagnostic Purposes
Surgical Purposes
Therapeutic Purposes
Contraindications cautions
Side adverse effects
Mydriatics
Cycloplegics
Atropine
Cyclopentolate
Homatropine
Scopolamine
Tropicamide
CHAPTER 5:
Commercially Available Topical Antibiotics
Introduction
Classification according to mechanism of action
Antibiotics that Act on the Bacterial Cell Membrane
Polymyxin B
Gramicidin
Antibiotics that Interfere with Bacterial Cell Wall Synthesis
β-lactams
Bacitracin
Vancomycin
Antibiotics that Affect Protein Synthesis
Aminoglycosides
Tetracyclines
Macrolides
Chloramphenicol
Antibiotics that Interfere with Folic Acid Metabolism
Sulfonamides, Pyrimethamine and Trimethoprim
Antibiotics that Interfere with Bacterial DNA Synthesis
Fluoroquinolones
CHAPTER 6:
Topical Fortified Antibiotics, Intravitreal and Subconjunctival Antibiotics
Introduction
Topical fortified antibiotics
Combination Therapy
Specific Drugs
Cotrimoxazole (Trimethoprim 16 mg/mL + Sulfamethoxazole 80 mg/mL)
Amikacin, 20–50 mg/mL
Clarithromycin, 10–40 mg/mL
Azithromycin, 2–10 mg/mL
Linezolid, 2 mg/mL
Colistin Eyedrops, 10 mg/mL
Subconjunctival route
Intrastromal and intracameral antibiotics
Intrastromal Antibiotics
Intracameral Antibiotics
Intravitreal antibiotics
Intravitreal Injection Technique
CHAPTER 7:
Systemic Antibiotics with Ophthalmic Clinical Usefulness
INTRODUCTION
BETA-LACTAMS
Penicillins
Cephalosporins
CARBAPENEMS
GLYCOPEPTIDES
Vancomycin
AMINOGLYCOSIDES
TETRACYCLINES
MACROLIDES
Erythromycin
Azithromycin
Clarithromycin
OXAZOLIDINONES
Linezolid
QUINOLONES
TREATMENT OF INFECTIOUS UVEITIS (Table 7.7)
Bartonellosis
Syphilis
Tuberculosis
Toxoplasmosis
CHAPTER 8:
Antivirals
Introduction
Antiviral drugs
Idoxuridine
Vidarabine
Trifluorothymidine
Acyclovir
Ganciclovir
Valacyclovir
Valganciclovir
Famciclovir
Foscarnet
Cidofovir
Fomivirsen
CHAPTER 9:
Antifungals
Introduction
Polyenes
Azoles
Echinocandins
Others
CHAPTER 10:
Antiparasitic Drugs
INTRODUCTION
ANTIPROTOZOAL DRUGS
Diamidines
Biguanides
Fumagillin
Pyrimethamine
ANTHELMINTIC DRUGS
Ivermectin
Diethylcarbamazine
Albendazole
COMPOUNDS AGAINST ARTHROPODS
Permethrin
TREATMENT OF PARASITIC DISEASES INVOLVING THE EYE
Protozoa
Acanthamoeba Keratitis
Ocular Microsporidiosis
Ocular Toxoplasmosis
Helminths
Loiasis
Onchocerciasis
Toxocariasis
Cysticercosis
Echinococcosis
Arthropods
Demodicosis
Phthiriasis and Pediculosis
Myiasis
CHAPTER 11:
Steroids
Introduction
Mechanism of action
Main steroids
Routes of administration in ophthalmology
Topical Administration
Periocular Administration
Subconjunctival Injection
Sub-Tenon or Orbital Floor Injection
Retrobulbar Injection
Intraocular Administration
Intravitreal Injections
Intraocular Sustained Release Devices
Systemic Administration
Oral Administration
Intravenous Administration
Side effects
Endocrinological Disorders
Musculoskeletal Disorders
Neurological Disorders
Gastrointestinal Disorders
High Blood Pressure
Dermatological Disorders
Ophthalmological Disorders
Infection Risk
Side Effects Related to the Route of Administration
Topical Administration
Periocular Administration
Intraocular Administration
CHAPTER 12:
Nonsteroidal Anti-inflammatory Drugs
Introduction
Prevention of Surgically Induced Miosis
Management of Postoperative Inflammation
Prevention and Treatment of Cystoid Macular Edema
Noninfectious Conjunctivitis
Ocular Pain
Retinal and Choroidal Diseases
Adverse effects of topical ophthalmic NSAIDs
Systemic
Local
Conclusion
CHAPTER 13:
Other Anti-inflammatory Drugs
Introduction
Essential fatty acids
Tetracycline analogs and other antibiotics
Topical calcineurin inhibitors
Cyclosporine
Tacrolimus
Pimecrolimus
Voclosporin
Other future anti-inflammatory drugs
CHAPTER 14:
Immunosuppressants
Introduction
Immunosuppressants
T-cell Inhibitors
Cyclosporine A (CsA)
Tacrolimus
Sirolimus
Antimetabolites
Methotrexate
Azathioprine
Mycophenolate Mofetil
Leflunomide
Alkylating Agents
Cyclophosphamide
Chlorambucil
Combination Therapy
CHAPTER 15:
Biologics
Introduction
Anti-TNF-α therapies
Infliximab
Adalimumab
Golimumab
Etanercept
Anti-IL-1 therapies
Canakinumab
Gevokizumab
Anakinra
Anti-IL-2 therapies
Daclizumab
Anti-IL-6 therapies
Tocilizumab
Anti-IL-17 therapies
Secukinumab
Cell therapy: rituximab
Costimulation inhibitor: abatacept
Other therapies
Interferon
Intravenous Immunoglobulins
CHAPTER 16:
Intravitreal Implants
Introduction
Intravitreal implants on the market
Vitrasert (Bausch and Lomb, Rochester, NY, USA)
Retisert (Bausch and Lomb, Rochester, NY, USA)
Ozurdex (Allergan, Inc, Irvine, CA, USA)
Iluvien (Alimera Sciences, Inc, Alpharetta, GA, USA)
Investigational implants
Summary
CHAPTER 17:
Medical Treatment of Glaucoma: Antiglaucoma Drugs
Introduction
Treatment options
Beta-blockers
Timolol Maleate
Levobunolol
Carteolol
Betaxolol
Adverse Effects of Beta-blockers
Sympathomimetics
Nonselective Agonists
Selective Agonists
Cholinergic Drugs
Carbonic Anhydrase Inhibitors
Oral
Topical
Adverse Effects
Effects on Ocular Blood Flow
Prostaglandin Analogs
Bimatoprost
Latanoprost
Travoprost
Unoprostone
Tafluprost
Adverse Effects of Prostaglandin Analogs
Hyperemia
Iris Pigmentation
Cystoid Macular Edema
Systemic Effects
Other Effects
Osmotic Agents
CHAPTER 18:
Antiangiogenics
Vessels in the developing and the adult human cornea
Corneal angiogenesis
Indications for anti(lymph)angiogenic treatment strategies in corneal and ocular surface diseases18
Anti(lymph)angiogenic treatment strategies in corneal and ocular surface diseases
Future investigations
Preclinical Models
Gene Therapy
CHAPTER 19:
Ophthalmologic Therapy with Botulinum Toxin
Introduction
Origin and Structure
History
Mechanism of action
Injection techniques
Preparing the Patient
Preparing Materials
Anesthesia
Dosage
Serotype A
Serotype B
Where and How to Inject
Extraocular Muscles
Facial Muscles
Eyelid Muscles
After Treatment Cares
Follow-up Monitoring
Therapeutic Indications
Nonophthalmological
Dermatocosmetological Applications
Around the Eye/Orbit
Blepharospasm
Lagophthalmos (Protective Ptosis, Ulcers, etc.)
Entropion
Müller's Muscle Hyperactivity in Thyroid Ophthalmopathy
Facial Wrinkles
Strabismus
Esotropias
Exotropias
Vertical Strabismus
Sensory Strabismus
Children Psychomotor Syndromes
Oculomotor Palsies
Fibrosis and Restrictive Strabismus
Nystagmus and Oscillopsia
BT as Diagnosis
Contraindications
Adverse side effects
Adverse Effects
Eyelid Ptosis
Vertical Strabismus
Diplopia and Past Pointing
Hypercorrection
Lack of Effect
Therapeutic Failure
Bruising
Ocular Puncture
Pain
Pupillary Alterations
Eye Dryness
Temporary Headache, Malaise and Mild Nausea
Generalized Effects
Presentations
CHAPTER 20:
Dietetics: Vitamins, Antioxidants and Others
Introduction
Vitamin A
Carotenoids
Lutein
Zinc
Omega-3 and omega-6 fatty acids
Curcumin
Citicoline
N-acetylcysteine
Ginkgo biloba extract
Vitamin C
Vitamin B1
Vitamin B2
Vitamin B3
Vitamin B6
Vitamin B12
Vitamin E
Selenium
L-Arginine
Coenzyme Q10
L-Carnitine
Resveratrol
CHAPTER 21:
Antiallergics
Introduction
Early- and late-phase reaction: understanding targets of treatment
Targets of Treatment: Molecules and Cells
Histamine
IgE
Leukotrienes and Prostaglandins
Cytokines
Mast Cells
Eosinophils
T-cells
Treatment of allergic eye disease
Goals of Treatment
Nonpharmacologic Treatment
Pharmacologic Treatment
First Generation of Ocular Allergy Treatment
Second Generation of Ocular Allergy Treatment
Antihistamines and Mast Cell Stabilizers
Dual Action/Multiple Action Agents: Clinical Evidence Grade B15
Nonsteroidal Anti-inflammatory Drugs: Clinical Evidence Grade D15
Leukotriene Receptor Antagonists
Oral Antihistamines: Clinical Evidence Grade C16
Topical Ophthalmic Corticosteroids: Clinical Evidence Grade C15
Calcineurin Inhibitors: Clinical Evidence Grade C15
Allergen-specific Immunotherapy: Clinical Evidence Grade A15
Additional and Future Options
Omalizumab
Selective Glucocorticoid Receptor Agonist (SEGRA)
PDE4 Inhibitors
Recombinant Antibodies
More Options in Treatment
Conclusion
CHAPTER 22:
Tear Substitutes
Introduction
Tear Substitutes
Types, characteristics and composition of tear substitutes
Viscosity
Osmolarity/Osmolality and Compatible Solutes
Electrolyte Composition
pH of Tear Substitutes
Preservatives
Inserts
Future trends in Dry Eye Disease treatment
Steroids and Nonsteroidal Anti-inflammatory Drugs
Calcineurin Inhibitors
Other Anti-inflammatory Drugs
Secretagogues
Hormones
Ocular Surface Healing Promoters
Pain Treatment
CHAPTER 23:
Surgical Use Drugs
Lidocaine
Adrenaline
Phenylephrine
Acetylcholine
Cefuroxime
Vancomycin
Intraocular irrigating solutions
Vitreous substitutes
Gases
Properties20
Classification
Perfluorocarbon Liquids
Main Features
Silicone Oils
Properties
Intraocular Toxicity of Silicones
Viscoelastics
Properties
Classification of Viscoelastics
Cohesive OVD (Healon, Healon GV, Provisc, Amvisc)
Dispersive OVD (Viscoat, Healon D, Ocucoat)
Viscoadaptive OVD (Healon 5, Micro ViscPhaco, iViscPhaco)
High-viscosity Dispersives (DisCoVisc)
Uses of Ophthalmic Viscosurgical Device
Ophthalmic Viscosurgical Device in Cataract Surgery
Alternatives Uses of OVD
Side Effects of the Use of Ophthalmic Viscosurgical Device27
Vital dyes for intraocular surgery
Dyes in Anterior Segment Surgery
Trypan Blue
Gentian Violet 0.001%
Triamcinolone Acetonide
Toluidine Blue 1%
Dyes in Posterior Segment Surgery: Chromovitrectomy
Triamcinolone Acetonide
Indocyanine Green 0.5% and Infracyanine Green 0.5%
Brilliant Blue G 0.025–0.05%
Trypan Blue
Adhesives
Cyanoacrylate
Fibrin Derivates
Tissues Adhesives Indications
OcuSeal®
CHAPTER 24:
Eyelid Hygiene Products: Treatment of Blepharitis and Meibomian Gland Dysfunction
Introduction
Ocular surface diseases associated with eyelid hygiene
Meibomian Gland Dysfunction
Dry Eye
Allergies
Anterior Blepharitis
Importance of eyelid hygiene
Eyelid hygiene products
Main components in eyelid hygiene products
Rosehip Oil
Iris Germanica
Centella Asiatica
Glycyrrhizin
Camomile
Tea Tree Oil
Glycerol
Dexpanthenol
Conclusion
CHAPTER 25:
Ocular Adverse Reactions of Systemic Drugs
Introduction
Therapeutic groups of drugs with ocular adverse effect
Antiacneic Drugs
Antiarrhythmic Drugs
Antibiotics
Antidepressants
Antiepileptic Drugs
Anti-inflammatory Drugs
Antineoplastic Drugs
Antimalarials
Bisphosphonates
Contraceptive Drugs
Corticosteroids
Erectile Dysfunction
Multiple Sclerosis
Hormones
Ocular adverse effect with other drugs
CHAPTER 26:
Ocular Adverse Events of Topical Drugs
Introduction
Contact allergic blepharoconjunctivitis
Mydriatics
Beta-blockers
Alpha-2-adrenergic Agents
Carbonic Anhydrase Inhibitors
Ketotifen
Hypertrichosis of the eyelashes
Ocular sicca disease and preservatives
Ocular surface findings
Topical Anesthetics
Mydriatics
Antibiotics
Antivirals
Steroids and Nonsteroidal Anti-inflammatory Drugs
Antiglaucoma Drugs
Uveitis
Brimonidine 0.2%
Latanoprost
Bimatoprost
Travoprost
Beta-blockers
INDEX
TOC
Index
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