Handbook of Experimental Pharmacology, Continuation of Handbuch der experimentellen Pharmakologie,, 69.
1 The History of Ophthalmic Therapeutics With 7 Figures --;References --;2 Ocular Pharmacokinetics With 20 Figures --;Abbreviations --;A. Introduction --;I. Objectives --;II. Compartments and Barriers --;III. Routes of Administration and Penetration --;1. Topical Administration --;2. Local Injection --;3. Systemic Administration --;IV. Animal Models and Human Experimentation --;1. Animal Models --;2. Human Experiments --;B. Topical Administration --;I. Factors Involved in Intraocular Penetration --;1. The Tears and Contact with Ocular Surface --;2. Corneal Penetration --;3. Conjunctiva and Sclera --;4. Intraocular Structures --;5. Metabolism of Drugs During Intraocular Penetration --;II. Compartmental Analysis --;1. Compartmentation --;2. Two-Compartment Model --;3. Tear Patterns --;4. Other Compartments --;5. Kinetics of Ocular Responses to Drugs --;6. Parameter Determination --;III. Conclusions and Recommendations --;C. Local Injections --;I. Subconjunctival --;1. Regurgitation --;2. Depot Dynamics --;3. Aqueous Humor Concentration --;4. Entry Pathways --;5. Vitreous Penetration --;6. Retrobulbar Injection --;II. Intravitreal Injection --;1. Diffusion in Vitreous --;2. Loss from the Vitreous Chamber --;3. Drug Kinetics --;4. Application to Humans --;D. Systemic Administration --;I. Intraocular Drug Penetration --;1. Structures Related to Entry from Blood --;2. The Blood-Vitreous Barrier --;3. Chemical Factors in Drug Penetration --;4. Drug Distribution in the Eye --;II. Compartmental Analysis --;1. Formulation of Aqueous Humor Dynamics --;2. One-Compartment Approximation --;3. Changes in Aqueous Concentration --;4. Kinetics of Intracameral Penetration --;5. Penetration into the Vitreous --;6. Penetration into the Cornea and Lens --;III. Conclusions and Recommendations --;E. Kinetics in Ocular Disease --;I. Inflammation and its Models --;II. Effects on Ocular Parameters --;1. Permeability --;2. Active Transport --;3. Vasomotor Effects --;III. Effects on Drug Kinetics --;1. Topical Application --;2. Systemic Penetration --;3. Periocular Injection --;4. Intravitreal Injection --;F. Conclusion --;References --;3 Biotransformation and Drug Metabolism With 25 Figures --;A. Introduction --;B. Hepatic Drug-Metabolizing Systems --;I. Microsomal Electron Transport Systems (Phase I Enzymes) --;1. Cytochrome P-450 --;2. NADPH · Cytochrome P-450 Reductase --;3. Cytochrome b5 and NADH · Cytochrome b5 Reductase --;II. Reactions Catalyzed by the Cytochrome P-450 System --;1. Oxidative Reactions --;2. Reductive Reactions --;III. Conjugation Reactions (Phase II Reactions) --;1. Glucuronidation --;2. Sulfation --;3. Acetylation --;4. Conjugation with Amino Acids --;5. Methylation --;6. Conjugation with Glutathione --;IV. Induction of Drug-Metabolizing Enzymes --;C. Ocular Drug Metabolism --;I. Aryl Hydrocarbon Hydroxylase Induction in the Eye --;II. Tissue Distribution of Drug-Metabolizing Enzymes in the Eye --;III. Drug Toxicity --;An Experimental Approach --;D. Concluding Remarks --;References --;4 Cholinergics With 11 Figures --;A. Chemistry Related to Biological Activity --;I. Cholinergic Neurotransmission --;II. Direct-Acting Agonists --;1. Muscarinic Agents --;2. Nicotinic Agents --;III. Indirect-Acting Agonists: Anticholinesterases --;1. Carbamates --;2. Organophosphorous Compounds --;B. Ocular Anatomy/Physiology Relevant to Cholinergic Mechanisms: Acute Effects of Cholinergic Drugs --;I. Lacrimation --;II. Cornea --;III. Lens --;IV. Pupillary Movement and Accommodation --;V. Aqueous Humor Formation, Removal, and Composition; Blood-Aqueous Barrier --;1. Basic Anatomy and Physiology --;2. Acute Effects of Cholinergic Drugs --;VI. Retina --;VII. Oculorotary and Respiratory Skeletal Muscles --;C. Longer-Term Effects of Cholinergic Drugs or Altered Cholinergic Neurotransmission --;I. Cholinergic Sensitivity in Ocular Smooth Muscles --;1. Physiologically and Pharmacologically Induced Alterations --;2. Disease-Induced Alterations --;3. Surgically Induced Alterations --;II. Cholinergic Toxicity --;1. Lens (Cataractogenesis) --;2. Iris/Ciliary Muscle/Trabecular Meshwork --;References --;5 a Autonomic Nervous System: Adrenergic Agonists With 21 Figures --;A. Introduction --;B. Cellular Sites and Mechanism of Adrenergic Action --;C. Modulation and Interaction of Receptor Types --;D. Sensitivity --;E. Stereoisomerism --;F. Storage, Release, and Degradation --;I. Monoamine Oxidase --;II. Catechol-O-methyltransferase --;G. Pharmacokinetics --;I. Penetration --;II. Distribution and Accumulation --;III. Duration --;IV. Action of Drugs on Intraocular Pressure --;H. Tissue Functions --;I. Lacrimal Gland --;II. Cornea and Lens --;III. Iris --;J. Blood Flow --;K. Intraocular Pressure --;L. Other Interactions --;I. Guanyl Cyclase --;II. Steroids and Adrenergics --;III. Adrenergics and Prostaglandins --;IV. Adrenergics and Ocular Pigment --;M. Retina --;References --;5b Autonomic Nervous System: Adrenergic Antagonists --;A. Introduction --;B. Beta-Adrenergic Antagonists --;I. Animal Pharmacology --;1. Intraocular Pressure --;2. Aqueous Humor Dynamics --;3. Interactions with Beta-Adrenergic Receptors in the Eye --;4. Mechanisms of Action on Intraocular Pressure --;5. Ocular Penetration and Distribution --;6. Other Ocular Pharmacology --;II. Clinical Pharmacology --;1. Intraocular Pressure --;2. Aqueous Humor Dynamics --;3. Beta-Adrenergic Receptor Blockade in the Eye --;4. Mechanisms of Action --;5. Ocular Penetration --;C. Alpha-Adrenergic Antagonists --;I. Animal Pharmacology --;1. Selective Alpha-Adrenergic Antagonists --;2. Alpha- and Beta-Adrenergic Antagonists (Labetalol) --;II. Clinical Pharmacology --;References --;6 Carbonic Anhydrase: Pharmacology of Inhibitors and Treatment of Glaucoma With 10 Figures --;A. History --;B. Pharmacology of the Clinically Used Carbonic Anhydrase Inhibitors. --;C. Physiology of Ocular Carbonic Anhydrase Inhibition --;I. Aqueous Humor Dynamics --;II. Aqueous Flow --;III. Relation to Pressure --;IV. Chemical Mechanisms of Flow --;V. Relation to Systemic Effects --;VI. Pharmacology of the Inhibitors Related to Ocular Effect and Enzyme Inhibition --;D. Clinical Uses of Carbonic Anhydrase Inhibitors --;I. Glaucoma --;II. Miscellaneous Uses and Effects --;E. Urolithiasis with Carbonic Anhydrase Inhibitors --;F. Other Toxic Effects --;G. Summary --;References --;7 Autacoids and Neuropeptides With 5 Figures --;A. Introduction --;B. Prostaglandins, Prostacyclin, Thromboxane, and Lipoxygenase Products --;I. General Background --;II. Occurrence and Biosynthesis in the Eye --;III. Elimination --;IV. Effects in the Eye --;1. Blood Flow --;2. Blood-Aqueous Barrier and Formation of Aqueous Humor --;3. Intraocular Pressure --;4. Outflow of Aqueous Humor --;5. Iridial and Ciliary Smooth Muscles --;6. Miscellaneous Effects --;V. Interaction with the Autonomic and Sensory Nervous Systems in the Eye --;VI. Pathophysiological Considerations --;1. Immediate Response to Injury of the Eye --;2. Inflammation of the Eye --;3. Other Disorders in the Eye Possibly Involving Prostaglandins --;C. Histamine --;I. General Background --;II. Occurrence and Effects in the Eye --;III. Pathophysiological Considerations --;D. 5-Hydroxytryptamine --;I. General Background --;II. Occurrence and Effects in the Eye --;E. Plasma Kinins --;I. General Background --;II. Effects in the Eye --;F. The Renin-Angiotensin System --;I. General Background --;II. Occurrence in the Eye --;G. Substance P --;I. General Background --;II. Distribution in the Eye --;III. Effects in the Eye --;1. Retina --;2. Iridial Smooth Muscles --;3. Ocular Circulation and Blood--Aqueous Barrier --;4. Intraocular Pressure --;5. Formation and Outflow of Aqueous Humor --;H. Enkephalins --;I. General Background --;II. Occurrence and Effects in the Eye --;J. Neurotensin --;K. Hypothalamic Peptides Regulating the Adenohypophysis --;I. Somatostatin --;II. Thyrotropin-Releasing Hormone --;III.
Luteinizing-Hormone-Releasing Hormone --;L. Peptide Hormones Secreted by the Neurohypophysis --;I. General Background --;II. Effects of Antidiuretic Hormone in the Eye --;III. Effects of Oxytocin in the Eye --;M. Melanocyte-Stimulating Hormones --;I. Effects in the Eye --;N. Vasoactive Intestinal Polypeptide --;I. General Background --;II. Localization and Effects in the Eye --;O. Glucagon --;P. Gastrin/Cholecystokinin --;Q. Summary --;References --;8 Vitamin A With 6 Figures --;A. Introduction --;B. Retinoid Structure --;C. Retinoid Properties --;D. Retinoid Identification --;I. Spectral Methods --;II. Fluorescence Methods --;III. Colorimetric Methods --;IV. High-Pressure Liquid Chromatography --;E. Retinoid Metabolism --;F. Retinoid Uptake --;G. Retinoid Action --;I. The Visual Process --;II. Glycoprotein Biosynthesis --;III. Hormone-like Action --;References --;9 Anti-Infective Agents --;A. Introduction --;B. Accurate Diagnosis and Drug Choice --;I. Mechanisms of Action --;II. Penetration and Absorption --;1. Protein and Tissue Binding --;2. The Blood-Aqueous Barrier --;3. Physicochemical Influences --;4. Aqueous and Uveoscleral Outflow --;III. Limiting Factors --;1. Age --;2. Renal Disease --;3. Liver Disease --;4. Enzymes --;5. Pregnancy --;6. Ocular Damage and Disease --;IV. Routes of Administration --;1. Topically Applied Antibiotic Drops --;2. Continuous Corneal Lavage with Antibiotic Solutions --;3. Subconjunctival Injections of Antibiotics --;V. Use of Antibiotics in Combination --;1. Prevention of Emergence of Drug-Resistant Mutants --;2. Treatment of Mixed Infections --;3. Initial Treatment of Vision-Threatening Infections --;4. Antibiotic Synergism and Antagonism --;VI. Adverse Drug Interactions --;C. Postoperative Intraocular Infections (Endophthalmitis) --;I. Incidence --;II. Results of Therapy --;III. Contributory Factors --;1. Sources of Infection in the Surgical Environment --;2. Ophthalmic Operative Area --;3. Influence of Host Tissue --;4. Organisms Responsible.