The treatment of mycosis with imidazole derivatives

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The treatment of mycosis with imidazole derivatives

Wolfgang P.E. Raab ; foreword by A.M. Kligman ; translated by T.C. Telger

Springer-Verlag, 1980

Other Title

Mykosebehandlung mit Imidazolderivaten

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Includes bibliographical references and index

Description and Table of Contents

Description

This is an "old-fashioned" book in the best sense of the term: It is written by one man, and it is scholarly, complete, thorough, and thoughtful. It is, in fact, a magnum opus wherein every aspect is not only touched, but handled to perfec- tion. This is a treatise that deserves careful reading by that increasing cadre of medical specialists who understand the many ways in which mycoses threaten human health and happiness, viz, the veterinarian, pharmaceutical chemist, general practitioner, pharmacologist, and entire consortium of researchers who study the biology, epidemiology, pathogenesis, and treatment of fungus infec- tions. Mycoses encompass a vast spectrum of diseases from trivial superficial skin infections (tinea versicolor), troublesome ringworm infections (the tineas of skin, hair, and nails), yeast infections (candidosis), the systemic mycosis (cryptococcosis, histoplasmosis), and even the deep-seated infections due to molds and saprophytic fungi (aspergillosis). It is precisely because of the great variety of causative organisms that the imidazoles deserve a special treatise. They provide the first class of drugs with therapeutic activity against all the important fungi which infect humans and animals. Accordingly, their medical significance is great and the possibilities endless. Morever, the imidazoles are the first effective drugs whose antimicro- bial activities extend beyond the usual designation of "broad-spectrum. " Broad-spectrum antibiotics, for example, are either antifungal or antibacterial, not both as the imidazoles are. To be sure, there have been other chemothera- peutic compounds which inhibit bacteria and fungi.

Table of Contents

1 Introduction.- 1.1 Antimicrobial Therapy.- 1.2 Microbial Diseases of the Skin and Mucous Membranes.- 1.3 Antimicrobial Drugs for Local Application.- 2 Broad-Spectrum Antimicrobials for Local Application.- 2.1 Preliminary Remarks.- 2.2 Disinf ectants and Antiseptics.- 2.3 Antibiotics.- 2.4 Chemotherapeutic Agents.- 2.5 Imidazole Derivatives with Antimicrobial Action.- 2.5.1 General.- 2.5.2 Chlormidazole.- 2.5.3 Clotrimazole.- 2.5.4 Miconazole and Isoconazole.- 2.5.5 Econazole.- 2.5.6 Ketoconazole.- 2.5.7 Assessment of Imidazole Derivatives.- 3 Econazole.- 3.1 General.- 3.2 Chemical Structure.- 3.3 Physical Properties.- 3.4 Antimicrobial Spectrum.- 3.4.1 Antifungal Activity.- 3.4.2 Antibacterial Activity.- 3.4.3 Comparison of the Antimicrobial Activity of Econazole with Other Local Therapeutic Agents.- 3.4.4 Activity Against Protozoa (Trichomonads).- 4 General Microbiology of Imidazole Derivatives for Local Application.- 4.1 Preliminary Remarks.- 4.2 Modeof Action.- 4.2.1 Morphological Findings.- 4.2.2 Biochemical Effects.- 4.2.3 Sites of Action in the Cell.- 4.3 Resistance and Tolerance.- 4.4 Interactions with Other Compounds.- 4.4.1 Preliminary Remarks.- 4.4.2 Proteins.- 4.4.3 Lipids.- 4.4.4 Glucocorticoids.- 4.4.5 Antibacterial Substances.- 4.4.6 Antimycotic Substances.- 4.4.7 Antibacterial Substances and Glucocorticoids.- 4.4.8 Conclusions.- 4.5 Bioavailability Studies.- 5 Therapeutic Use of Imidazole Derivatives in Animals (Experimental Therapy).- 5.1 Local Application.- 5.2 Systemic Application.- 6 General Pharmacology of the Imidazole Derivatives in Man and Animals.- 6.1 Pharmacologic Properties (Apart from Antimicrobial Action) ...- 6.2 Absorption, Excretion, and Metabolism in Animals.- 6.2.1 Systemic Application.- 6.2.2 Local Application to the Skin and Mucous Membranes.- 6.3 Absorption, Excretion, and Metabolism in Man.- 6.3.1 Systemic Application.- 6.3.2 Local Application to the Outer Skin.- 6.3.3 Local Application to the Vaginal Epithelium.- 6.3.4 Conclusions.- 6.4 Sensitization.- 6.4.1 Preliminary Remarks.- 6.4.2 Animal Experiments in Systemic Sensitization.- 6.4.3 Animal Experiments in Local Sensitization.- 6.4.4 Sensitization in Man.- 6.5 Anaphylactoid Activity.- 7 Toxicology of the Imidazole Derivatives.- 7.1 Preliminary Remarks.- 7.2 SystemicToxicity.- 7.3 LocalToxicity.- 7.3.1 Skin and Mucous Membrane Tolerance in Animals.- 7.3.2 Photosensitizing Reactions.- 7.3.3 Skin and Mucous Membrane Tolerance in Man.- 8 Clinical Pharmacology of Topical Antimicrobials with Special Regard to the Imidazole Derivatives.- 8.1 Preliminary Remarks.- 8.2 Physical Properties.- 8.3 SkinTolerance.- 8.4 Sensitization.- 8.5 Photosensitizing Reactions.- 8.6 Interactions with Substances on the Skin Surface.- 8.7 Penetration and Absorption.- 8.8 Systemic Administration.- 8.9 Use in Veterinary Mediane and the Food Industry.- 8.10 Special Clinical Pharmacologic Considerations in the Local Application of Antimicrobials.- 8.10.1 General.- 8.10.2 Degree and Spectrum of Activity.- 8.10.3 Resistance and Tolerance.- 8.11 Clinical Pharmacology of the Preparation.- 8.11.1 General.- 8.11.2 Interactions.- 8.11.3 Combinationof Imidazole Derivatives and Glucocortoids .....- 9 Microbial Infections in Man.- 9.1 General.- 9.2 Increase in Microbial Infections of Body Surfaces.- 9.3 Saprophytes and Parasites on Body Surf aces.- 9.4 Mixed and Double Inf ections of Body Surf aces.- 10 Mycoses.- 10.1 Etiology of Mycoses.- 10.2 The Increase in Mycoses.- 10.2.1 General.- 10.2.2 Increase in Mycoses Due to Medications.- 10.2.3 Increase in Mycoses Due to Changes in Hygienic Habits and Modes of Social Behavior.- 10.2.4 Increase in Mycoses Due to Metabolie Disturbances.- 10.2.5 Increase in Mycoses Due to Physical Influences.- 10.3 Classification of Mycoses.- 10.4 Mycoses of the Skin and Mucous Membranes.- 10.4.1 General.- 10.4.2 Diagnosis of Skin and Mucous Membrane Mycoses.- 10.5 Mycoses of the Female Genitalia.- 10.6 Systemic Mycoses.- 10.7 General Principles in the Treatment of Mycoses.- 10.7.1 Systemic Treatment.- 10.7.2 Local Antimycotics.- 10.7.3 Treatment of Mucous Membrane Mycoses.- 11 Systemic Administration of Antimycotically Active Imidazole Derivatives in Man.- 12 Local Application of Antimycotically Active Imidazole Derivatives in Man.- 12.1 Application to the Outer Skin.- 12.2 Application to the Mucous Membranes.- 13 Combined Use of Imidazole Derivatives and Glucocortoids for the Local Treatment of Skin Diseases.- 13.1 Preliminary Remarks.- 13.2 Combination of Antibiotics with Glucocortoids.- 13.3 Salicylic Acid, Haloprogin, Clioquinol, Chlorquinaldol, and Triclosan.- 13.4 Imidazole Derivatives and Glucocortoids.- 13.5 Indications for the Combined Use of Imidazole Derivatives and Glucocorticoids.- 14 Assessment of Mycoses in Various Branches of Mediane.- 14.1 Dermatology.- 14.2 Gynecology.- 14.3 Pediatrics.- 14.4 Stomatology.- 14.5 Otolaryngology.- 14.6 Otorhinolaryngology.- 14.7 Proctology.- 14.8 Urology.- 14.9 Internal Mediane.- 14.10 Orthopedics.- 14.11 Surgery, Intensive Care, Anesthesiology.- 15 Concluding Remarks.- 16 References.- 17 Subject Index.

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