|
" Antituberculosis Drugs "
K Bartmann
| Document Type
|
:
|
BL
|
| Record Number
|
:
|
738602
|
| Doc. No
|
:
|
b558515
|
| Main Entry
|
:
|
K Bartmann
|
| Title & Author
|
:
|
Antituberculosis Drugs\ K Bartmann
|
| Publication Statement
|
:
|
Berlin Springer Berlin, 2013
|
| Series Statement
|
:
|
Handbook of Experimental Pharmacology, 84
|
| Page. NO
|
:
|
XXIV, 566 Seiten in 1 Teil XXIV, 566 Seiten 68 Figuren 244 x 170 mm
|
| ISBN
|
:
|
3642728758
|
|
|
:
|
: 9783642728754
|
| Contents
|
:
|
1 Historical Introduction and Chemical Characteristics of Antituberculosis Drugs.- A. p-Aminosalicylic Acid (PAS).- B. Streptomycin (SM) - Dihydrostreptomycin (DHSM).- C. Thiosemicarbazone (TSC) [Thioacetazone, Thiacetazone, p-Aminobenzaldehyde].- D. Pyrazinamide (PZA) - Morphazinamide (MZA).- E. Isoniazid (INH).- F. Tetracyclines.- I. Oxytetracycline (Terramycin, OTC).- II. Tetracycline (TC).- G. Viomycin (VM).- H. Cycloserine (CS) - Terizidone (TZ).- I. Thioamides: Ethionamide (ETH) - Protionamide (PTH).- J. Kanamycin (KM).- K. Thiocarlide (DATC).- L. Capreomycin (CM).- M. Ethambutol (EMB).- N. Rifampicin (RMP).- References will be found on each end of Paragraphs.- 2 Experimental Evaluation of Efficacy.- A. Introduction.- B. Methods, Their Limitations, Advantages, and Disadvantages.- I. In-vitro Tests.- 1. Determination of Minimal Inhibitory Concentrations (MIC).- 2. Cross-Resistance.- 3. Type of Action.- II. Animal Experiments.- III. Cell- and Tissue Cultures.- References.- C. Drugs and Treatment Regimens.- I. p-Aminosalicylic Acid (PAS).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Cell and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- 3. Concluding Remarks.- References.- II. Streptomycin (SM) - Dihydrostreptomycin (DHSM).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance to, and Dependence on SM.- Type of Action.- Effects in Combination with Other Antituberculotics.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Continuous Monotherapy.- Intermittent Monotherapy.- SM in Combined Chemotherapy.- 3. Concluding Remarks.- References.- III. Thiosemicarbazones (TSC) [Thiacetazone, Thioacetazone].- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Combination with Other Antituberculotics.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- TSC in Combined Chemotherapy.- 3. Concluding Remarks.- References.- IV. Pyrazinamide (PZA) and Morphazinamide (MZA).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Monotherapy.- PZA in Combined Chemotherapy.- 3. Concluding Remarks.- References.- V. Isoniazid (INH).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Combination with Other Antituberculotics.- Effects in Cell- and Tissue Cultures.- Effects in Embryonated Eggs.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Efficacy in Special Animal Models.- INH in Combined Chemotherapy.- Intermittent Treatment with INH Alone and in Combination.- Treatment in Phases.- 3. Concluding Remarks.- References.- VI. Tetracyclines.- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Combination with Other Antituberculotics.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis.- 3. Concluding Remarks.- References.- VII. Viomycin (VM).- 1. Antimicrobial Spectrum in Vitro and in Vivo.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Combination with Other Antituberculotics.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis.- Monotherapy.- VM in Combined Chemotherapy.- 3. Concluding Remarks.- References.- VIII. Cycloserine (CS) and Terizidone (TZ).- 1. Cycloserine (CS).- Antimicrobial Spectrum in Vitro.- Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis.- Monotherapy.- CS in Combined Chemotherapy.- 2. Terizidone (TZ).- Activity in Experimental Tuberculosis.- Activity in Artificial Media in Vitro.- 3. Concluding Remarks.- References.- IX. Thioamides: Ethionamide (ETH), Protionamide (PTH).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Type of Action.- Bacterial Resistance.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Continuous Monotherapy.- Intermittent Monotherapy.- ETH in Combined Chemotherapy.- 3. Concluding Remarks.- References.- X. Kanamycin (KM) and Amikacin.- 1. Kanamycin - Antimicrobial Spectrum in Vitro.- 2. Kanamycin - Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis.- Monotherapy.- KM in Combined Chemotherapy.- 3. Amikacin - Antimycobacterial Activity.- 4. Concluding Remarks.- References.- XI. Thiocarlide (DATC).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis.- Monotherapy.- DATC in Combined Chemotherapy.- 3. Concluding Remarks.- References.- XII. Capreomycin (CM).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Type of Action.- Bacterial Resistance.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Monotherapy.- CM in Combined Chemotherapy.- 3. Concluding Remarks.- References.- XIII. Ethambutol (EMB).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Type of Action.- Bacterial Resistance.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Monotherapy.- EMB in Combined Chemotherapy.- 3. Concluding Remarks.- References.- XIV. Rifampicin (RMP).- 1. Antimicrobial Spectrum in Vitro.- 2. Antimycobacterial Activity.- Activity in Artificial Media in Vitro.- Bacterial Resistance.- Type of Action.- Effects in Combination with Other Antituberculotics.- Effects in Cell- and Tissue Cultures.- Activity in Experimental Tuberculosis and Development of Resistance in Vivo.- Continuous Monotherapy.- Intermittent Monotherapy.- RMP in Combined Chemotherapy (Continuous, Intermittent, in Phases).- 3. Concluding Remarks.- References.- 3 Experimental Evaluation of Chemoprophylaxis and Preventive Treatment in Animals.- A. Definitions.- B. Objectives of Laboratory Experiments.- C. Results of Animal Experiments.- I. Experiments with Monkeys.- II. Experiments with Guinea Pigs.- III. Experiments with Cattle.- D. Discussion of Experimental Data.- I. Technique of Infection.- II. Infective Dose.- III. Animal Species Differences.- IV. The Drug as Factor.- E. Preventive Treatment in Animals.- I. Experiments with Guinea Pigs.- II. Experimental Studies with Mice.- III. Mink and Rabbits.- IV. Intermittent Treatment.- V. Preventive Treatment in Cattle.- F. Immunological Questions of Chemoprophylaxis and Vaccine Prophylaxis.- Combination of Chemoprophylaxis and Immune Prophylaxis.- INH Resistant BCG.- References.- 4 Experimental and Clinical Activity of Antituberculosis Drugs and Other Antimicrobial Agents Against Mycobacteria Other than Tubercle Bacilli, Except M. Leprae.- A. Introduction.- B. Possible Reasons for the Lower Sensitivity of MOTT to many Antituberculotics Compared to M.
|
|
|
:
|
tuberculosis.- C. Efficacy of Antituberculosis Drugs and Other Antimicrobial Agents Against the Various MOTT Species.- I. Group I. Photochromogenic Mycobacteria.- 1. M. Kansasii (Yellow Bacillus, M. Luciflavum).- Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Animals.- Treatment of Infections in Man.- 2. M. Marinum (M. Balnei).- Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Animals.- Treatment of Infections in Man.- 3. M. Simiae.- Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Treatment of Infections in Man.- 4. M. Asiaticum.- Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Treatment of Infections in Man.- II. Group II. Scotochromogenic Mycobacteria.- 1. Introductory Remarks Including Types of Disease.- 2. Publications on Group II Without Identification of the Species.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Activity of Antituberculosis Drugs in Animals.- Treatment of Infections in Man.- 3. M. Flavescens.- Types of Disease and Treatment in Man.- 4. M. Gordonae.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Treatment of Infections in Man.- 5. M. Scrofulaceum (M. Marianum, M. Parafnicum).- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Treatment of Infections in Man.- 6. M. Szulgai.- Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Treatment of Infections in Man.- 7. M. Xenopi (M. Littorale, M. Xenopei).- Types of Disease.- Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Vitro.- Treatment of Infections in Man.- III. Group III.- 1. M. Avium Complex, Including M. Avium and M. Intracellulare ("Battey Bacillus").- Introductory Remarks Including Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Activity of Antituberculosis Drugs in Animals.- Treatment of Infections in Man.- 2. M. Haemophilum.- Types of Disease, Activity of Antituberculosis Drugs in Vitro, and Treatment of Infections in Man.- 3. M. Malmoense.- Types of Disease, Activity of Antituberculosis Drugs in Vitro, and Treatment of Infections in Man.- 4. M. Nonchromogenicum Complex (Including M. Nonchromogenicum, M. Terrae, M. Novum, M. Triviale).- Types of Disease, Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Vitro, and Treatment of Infections in Man.- 5. M. Ulcerans (M. Buruli).- Types of Disease.- Activity of Antituberculosis Drugs in Vitro.- Activity of Other Antimicrobial Agents in Vitro.- Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Animals.- Treatment of Infections in Man.- IV. Group IV.- 1. M. Fortuitum Complex (Including M. Fortuitum and M. Chelonei with Subspecies Abscessus).- Types of Disease.- Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Vitro and in Vivo.- Treatment of Infections in Man.- 2. M. Smegmatis.- Types of Disease.- Activity of Antituberculosis Drugs and Other Antimicrobial Agents in Vitro and in Vivo.- 3. M. Thermoresistibile.- Types of Disease, Activity of Antituberculosis Drugs, and Treatment of Infection in Man.- References.- 5 Experimental Pharmacology and Toxicology of Antituberculosis Drugs.- A. Introduction.- B. The Drugs.- I. p-Aminosalicylic Acid (PAS).- 1. Respiration, Circulation, Heart.- 2. Acute Toxicity.- 3. Subchronic and Chronic Toxicity.- References.- II. Streptomycin - Dihydrostreptomycin (SM - DHSM).- 1. Respiration, Circulation, Heart.- 2. Neuromuscular Blocking Effects of SM, DHSM, and Other Basic Antibiotics.- 3. Smooth Muscles.- 4. Ganglion Blocking Effects.- 5. Further Pharmacologic Effects.- 6. Acute Toxicity.- Attempts at Reducing the Acute Toxicity.- 7. Subchronic Toxicity.- 8. Ototoxicity of the Aminoglycoside Antibiotics.- Morphology.- Pathophysiology.- Causes: Pharmacokinetics and Biochemical Effects.- Species Related Sensitivity Differences and Differences in the Activity of the Various Antibiotics.- Attempts to Reduce Ototoxicity.- 9. Nephrotoxicity.- 10. Reproductive Toxicity.- 11. Biochemical Effects of SM.- References.- III. Thiosemicarbazone - Thiacetazone, Thioacetazone (TSC).- 1. Acute Toxicity.- 2. Subchronic and Chronic Toxicity.- 3. Liver Toxicity.- References.- IV. Pyrazinamide (PZA) and Morphazinamide (MZA).- 1. Pyrazinamide (PZA).- Respiration and Blood Pressure.- Acute and Subchronic Toxicity.- Liver Toxicity, Carcinogenicity.- References.- 2. Morphazinamide (MZA).- Acute and Subchronic Toxicity.- References.- V. Isoniazid (INH).- 1. Respiration, Circulation, Heart.- 2. Smooth Muscles.- 3. Other Pharmacological Effects.- 4. Central Stimulation Effects.- 5. INH and Vitamin B6 Metabolism.- 6. INH and the ?-Aminobutyric Acid Metabolism.- 7. Protective Action of Various Substances.- 8. Acute Toxicity.- 9. Subchronic and Chronic Toxicity.- 10. Liver Toxicity.- 11. Neurotoxic Effects.- 12. Ototoxicity.- 13. Reproductive Toxicity.- 14. Carcinogenic Effects.- 15. Cytostatic Effects.- 16. Mutagenic Effects.- 17. Lathyrogenic Activity.- References.- VI. Tetracyclines: Tetracycline, Oxytetracycline (TC, OTC).- 1. Respiration, Circulation, Heart.- 2. Neuromuscular Blocking Effects of Tetracyclines.- 3. Smooth Muscles.- 4. Acute Toxicity.- 5. Subacute Toxicity.- 6. Liver Toxicity.- 7. Nephrotoxicity.- 8. Effects on the Intestinal Epithelium.- 9. Tetracyclines and Bone Metabolism.- 10. Reproductive Toxicity.- 11. Inhibition of Protein Synthesis.- 12. Ototoxicity.- 13. Phototoxicity.- References.- VII. Viomycin (VM).- 1. Respiration, Blood Pressure.- 2. Neuromuscular Blocking Effect.- 3. Ganglion Blocking Effect.- 4. Smooth Muscles.- 5. Acute Toxicity.- 6. Subacute Toxicity.- 7. Nephrotoxicity.- 8. Ototoxicity.- References.- VIII. Cycloserine (CS) and Terizidone (TZ).- 1. d-Cycloserine (CS).- Respiration, Circulation, Heart.- Smooth Muscles.- Central Nervous Effects.- Other Pharmacological Effects.- Acute Toxicity.- Subchronic Toxicity.- Chronic Toxicity.- Nephrotoxicity, Ototoxicity.- Local Tolerability.- 2. Terizidone (TZ).- Acute Toxicity.- Subacute and Chronic Toxicity.- References.- IX. Thioamides (Ethionamide, Protionamide).- 1. Ethionamide (ETH).- Circulation, Heart.- Acute, Subchronic and Chronic Toxicity.- Reproductive Toxicity.- Carcinogenicity.- 2. Protionamide (PTH).- Acute and Subchronic Toxicity.- Reproductive Toxicity.- Carcinogenicity.- References.- X. Kanamycin (KM).- 1. Respiration, Circulation, Heart.- 2. Neuromuscular Blocking Effects.- 3. Smooth Muscles.- 4. Other Pharmacologic Effects.- 5. Acute Toxicity.- 6. Subchronic and Chronic Toxicity.- 7. Ototoxicity.- 8. Nephrotoxicity.- 9. Reproductive Toxicity.- References.- XI. Thiocarlide (DATC).- 1. Acute Toxicity.- 2. Subacute Toxicity.- 3. Chronic Toxicity.- 4. Reproductive Toxicity.- References.- XII. Capreomycin (CM).- 1. Respiration, Circulation, Heart.- 2. Acute Toxicity.- 3. Chronic Toxicity.- 4. Reproductive Toxicity.- 5. Ototoxicity.- 6. Nephrotoxicity.- References.- XIII. Ethambutol (EMB).- 1. Acute Toxicity.- 2. Chronic Toxicity.- 3. Reproductive Toxicity.- 4. Ototoxicity.- 5. Pharmacology.- References.- XIV. Rifampicin (RMP).- 1. Acute Toxicity.- 2. Subchronic Toxicity.- 3. Chronic Toxicity.- 4. Microsomal Enzyme Induction.- 5. Reproductive Toxicity.- 6. Ototoxicity.- 7. Carcinogenicity.- 8. Mutagenicity.- 9. Interactions with Other Drugs.- References.- 6 Mode of Action, Biotransformation and Pharmacokinetics of Antituberculosis Drugs in Animals and Man.- A. General Part.- I. Mode of Action of Antituberculosis Drugs.- 1. Type of Effect and Primary Site of Attack.- 2.
|
|
|
:
|
Transport of Antituberculotics to the Site of Action.- 3. Mode of Action of Antituberculosis Drugs.- Nucleic Acid and Protein Synthesis as Primary Site of Attack.- Biosynthesis of the Microbial Cell Wall as Primary Site of Attack.- II. Biotransformation.- 1. Site of the Biotransformation.- 2. Possible Reactions.- 3. Factors Influencing Biotransformation.- 4. Influence of the Inductive Effect of RMP on the Biotransformation of Other Drugs.- 5. Antituberculosis Treatment and Biotransformation.- III. Pharmacokinetics.- 1. Absorption of Antituberculosis Drugs.- 2. Factors Influencing the Absorption.- Changes in Absorption due to a Different Mode of Administration.- Influence of Structural Modifications of the Drugs.- Influence of Galenic Processing.- Influence of Food Consumption.- 3. Binding of Antituberculosis Drugs to Proteins and Blood Cells.- 4. Distribution of Antituberculosis Drugs in the Body.- 5. Excretion of Antituberculosis Drugs.- Routes of Excretion.- Influence of Age.- Influence of Kidney Function.- Influence of Liver Diseases.- 6. Factors Influencing the Pharmacokinetics of Antituberculosis Drugs.- Influence of Sex and Age.- Influence of Administration Intervals and Dose.- Influence of Combination of Antituberculosis Drugs.- 7. Serum-Concentrations of Antituberculosis Drugs as Parameter of Treatment Efficacy.- Coverage.- Half-Life.- Area Under the Curve.- IV. General Medical Relevance of the Results Obtained in the Field of Tuberculosis.- 1. Studies on the Mode of Action.- 2. Studies on Biotransformation Processes.- 3. Studies on Pharmacokinetics.- References.- B. Special Part - The Antituberculosis Drugs.- I. PAS.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- II. SM.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- III. TSC.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- IV. PZA.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- V. INH.- 1. Mode of Action.- Incorporation of INH in Mycobacteria.- Biotransformation of INH by Mycobacteria.- Uptake of INH by Resistant Mycobacteria.- Mode of Action.- 2. Biotransformation.- Biotransformation Patterns in Man and in Animals.- Biotransformation and Antituberculotic Activity.- Determination of INH and Its Biotransformation Products.- Genetically Fixed Polymorphism of INH and Other Drugs.- Possible Ways of Differentiating Between Rapid and Slow INH Biotransformation.- Biotransformation of INH Derivatives and INH Retard Preparations.- Factors Affecting Biotransformation.- Race Dependent Biotransformation.- Biotransformation in Animals.- Influence of Biotransformation on Efficacy and Side Effects.- 3. Pharmacokinetics.- References.- VI. Tetracyclines.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- VII. VM.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- VIII. CS.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- IX. ETH/PTH.- 1. Mode of Action.- 2. Biotransformation.- Possibilities of Assay of ETH, PTH and Their Biotransformation Products.- Reversible Conversion of ETH and PTH into the Corresponding Sulphoxides.- Biotransformation Products of ETH and PTH.- Biotransformation of ETH and PTH in Man and Animals.- 3. Pharmacokinetics.- References.- X. KM.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- XI. DATC.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- XII. CM.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- XIII. EMB.- 1. Mode of Action.- 2. Biotransformation.- 3. Pharmacokinetics.- References.- XIV. RMP.- 1. Mode of Action.- 2. Biotransformation.- Biotransformation Pattern in Man and in Animals.- Modification of the Biotransformation Rate by Auto-Induction.- 3. Pharmacokinetics.- References.
|
| LC Classification
|
:
|
QP905.K337 2013
|
| Added Entry
|
:
|
K Bartmann
|
| |