All new antibacterial agents which have been approved after the year 2000 have been described along with their mechanism of action, development of resistance, spectrum of activity and the stage of developmental in case of yet to be approved drugs.
This document discusses macrolide antibiotics, including their structure, examples (erythromycin, azithromycin), mechanism of action, spectrum of activity, resistance, pharmacokinetics, adverse effects, drug interactions, and contraindications. Macrolides bind to the bacterial ribosome and inhibit protein synthesis, generally being bacteriostatic. Their spectrum includes many gram-positive bacteria and some intracellular pathogens. Resistance can occur via efflux pumps or ribosomal mutations. Adverse effects include gastrointestinal issues and ototoxicity. Macrolides can interact with drugs metabolized by CYP450 enzymes.
12.COMPREHENSIVE OFANTIMICROBIAL AGENTS AND CHEMOTHERAPY ( CLASSIFICATION AND...Saminathan Kayarohanam
Antimicrobial Agents and Chemotherapy (AAC) features interdisciplinary studies that build our understanding of the underlying mechanisms and therapeutic applications of antimicrobial and antiparasitic agents and chemotherapy.
Hepatitis B is a common infectious disease caused by the hepatitis B virus (HBV) that can cause liver inflammation and disorders. A recombinant hepatitis B vaccine was developed that uses antigenic proteins from HBV produced through recombinant DNA technology rather than a weakened virus. This involves isolating the HBsAg gene from HBV, inserting it into a bacterial plasmid vector, introducing this recombinant DNA into yeast to mass produce the HBsAg protein, purifying the protein, and formulating it into a vaccine for human vaccination. The recombinant vaccine is beneficial as it stimulates protective antibodies without using a live virus.
Monoclonal antibodies (mAbs) have various applications including diagnostic, therapeutic, and catalytic uses. Diagnostically, mAbs are used in pregnancy tests, disease diagnostics, and immunohistochemistry. Therapeutically, mAbs treat cancer, transplant rejection, and autoimmune diseases by mechanisms like enhancing immune response, blocking growth signals, inhibiting angiogenesis or cytokines. Some FDA-approved mAbs for cancer include rituximab, trastuzumab, and bevacizumab. Conjugated mAbs can deliver toxins or radiation directly to tumors. mAbs also have applications in areas like organ transplantation, autoimmune diseases, and drug targeting.
Mechanism of action of major antibiotic classes including betal lactam agents, aminoglycosides, macrolides, tetracyclines, quinolons, vancomycin, oxazolidionons. Detailed review and illustrations
Nitromidazoles, nitrofurans, streptogramins DrugsAreej Abu Hanieh
This document summarizes information about various antimicrobial agents including nitroimidazoles, nitrofurans, and streptogramins. It discusses the mechanisms of action, uses, and resistance mechanisms for metronidazole, tinidazole, nitrofurantoin, furazolidone, and streptogramin A and B. It provides details on how these drugs treat various bacterial, parasitic, and protozoal infections. The synergistic activity of streptogramins A and B is highlighted when used together against multidrug-resistant bacteria like vancomycin-resistant Staphylococcus aureus and Enterococcus.
Microbial biotransformation uses microorganisms like bacteria, fungi, and actinomycetes to modify organic compounds through enzymatic reactions. Key reactions include oxidation, reduction, hydrolysis, and others. These transformations are used commercially to produce pharmaceuticals, vitamins, antibiotics, and other chemicals. For example, microbes can hydroxylate steroids through oxidation or reduce ketones and aldehydes. Biotransformation offers advantages like selectivity and mild reaction conditions compared to chemical synthesis.
Streptomycin is an antibiotic used to treat tuberculosis, endocarditis, and other bacterial infections. It works by blocking protein synthesis in bacteria, which results in death. Common side effects include dizziness, vomiting, facial numbness, fever and rash. Use during pregnancy can cause deafness in infants. It is administered via injection and is generally safe during breastfeeding but not recommended for those with myasthenia gravis due to risk of side effects like dizziness.
This document discusses macrolide antibiotics, including their structure, examples (erythromycin, azithromycin), mechanism of action, spectrum of activity, resistance, pharmacokinetics, adverse effects, drug interactions, and contraindications. Macrolides bind to the bacterial ribosome and inhibit protein synthesis, generally being bacteriostatic. Their spectrum includes many gram-positive bacteria and some intracellular pathogens. Resistance can occur via efflux pumps or ribosomal mutations. Adverse effects include gastrointestinal issues and ototoxicity. Macrolides can interact with drugs metabolized by CYP450 enzymes.
12.COMPREHENSIVE OFANTIMICROBIAL AGENTS AND CHEMOTHERAPY ( CLASSIFICATION AND...Saminathan Kayarohanam
Antimicrobial Agents and Chemotherapy (AAC) features interdisciplinary studies that build our understanding of the underlying mechanisms and therapeutic applications of antimicrobial and antiparasitic agents and chemotherapy.
Hepatitis B is a common infectious disease caused by the hepatitis B virus (HBV) that can cause liver inflammation and disorders. A recombinant hepatitis B vaccine was developed that uses antigenic proteins from HBV produced through recombinant DNA technology rather than a weakened virus. This involves isolating the HBsAg gene from HBV, inserting it into a bacterial plasmid vector, introducing this recombinant DNA into yeast to mass produce the HBsAg protein, purifying the protein, and formulating it into a vaccine for human vaccination. The recombinant vaccine is beneficial as it stimulates protective antibodies without using a live virus.
Monoclonal antibodies (mAbs) have various applications including diagnostic, therapeutic, and catalytic uses. Diagnostically, mAbs are used in pregnancy tests, disease diagnostics, and immunohistochemistry. Therapeutically, mAbs treat cancer, transplant rejection, and autoimmune diseases by mechanisms like enhancing immune response, blocking growth signals, inhibiting angiogenesis or cytokines. Some FDA-approved mAbs for cancer include rituximab, trastuzumab, and bevacizumab. Conjugated mAbs can deliver toxins or radiation directly to tumors. mAbs also have applications in areas like organ transplantation, autoimmune diseases, and drug targeting.
Mechanism of action of major antibiotic classes including betal lactam agents, aminoglycosides, macrolides, tetracyclines, quinolons, vancomycin, oxazolidionons. Detailed review and illustrations
Nitromidazoles, nitrofurans, streptogramins DrugsAreej Abu Hanieh
This document summarizes information about various antimicrobial agents including nitroimidazoles, nitrofurans, and streptogramins. It discusses the mechanisms of action, uses, and resistance mechanisms for metronidazole, tinidazole, nitrofurantoin, furazolidone, and streptogramin A and B. It provides details on how these drugs treat various bacterial, parasitic, and protozoal infections. The synergistic activity of streptogramins A and B is highlighted when used together against multidrug-resistant bacteria like vancomycin-resistant Staphylococcus aureus and Enterococcus.
Microbial biotransformation uses microorganisms like bacteria, fungi, and actinomycetes to modify organic compounds through enzymatic reactions. Key reactions include oxidation, reduction, hydrolysis, and others. These transformations are used commercially to produce pharmaceuticals, vitamins, antibiotics, and other chemicals. For example, microbes can hydroxylate steroids through oxidation or reduce ketones and aldehydes. Biotransformation offers advantages like selectivity and mild reaction conditions compared to chemical synthesis.
Streptomycin is an antibiotic used to treat tuberculosis, endocarditis, and other bacterial infections. It works by blocking protein synthesis in bacteria, which results in death. Common side effects include dizziness, vomiting, facial numbness, fever and rash. Use during pregnancy can cause deafness in infants. It is administered via injection and is generally safe during breastfeeding but not recommended for those with myasthenia gravis due to risk of side effects like dizziness.
The document discusses various classes of antimicrobial agents including their classification, mechanisms of action, spectra of activity, and examples. It covers antibiotics such as penicillin, cephalosporins, aminoglycosides, and macrolides. It also addresses antimicrobial resistance, rational antibiotic usage, and combination therapy.
- Penicillins are a major class of antibiotics that were the first discovered from the mold Penicillium. They work by inhibiting the final step of bacterial cell wall synthesis through binding to penicillin-binding proteins. This disrupts cell wall formation and causes cell lysis.
- There are different generations/classes of penicillins that vary in their spectra of activity and resistance to bacterial beta-lactamases. Oral forms are absorbed from the gastrointestinal tract while injectable forms provide more sustained drug levels. Adverse effects include hypersensitivity reactions and gastrointestinal issues.
This document discusses the structure and synthesis of bacterial cell walls. It begins by outlining the contents which include the structure of peptidoglycan, its synthesis, the role of the cytoskeleton, patterns of cell wall synthesis, and the significance of peptidoglycan cell walls. It then goes into more detail on the ultrastructure of gram positive and gram negative cell walls, the synthesis of peptidoglycan subunits, transpeptidation reactions, and how the cytoskeleton controls cell shape through cell wall synthesis. Patterns of new cell wall growth in different bacteria are also described. The conclusion emphasizes the importance of the peptidoglycan cell wall for bacterial growth, shape, and protection
Hybridoma technology is a method for producing large number of identical antibodies called monoclonal antibodies.
It was discovered by G.kohler and C.milstein in 1975. they were awarded nobel prize for physiology and medicine in 1975.
The hybrid cells are produced by fusing B- lumphocyte with myeloma cells or tumour cells.
The B-lymphocyte have the ability to produce large number of antibodies and tumour cells have indefinite growth.
This is why two cells are used for the production of hybrid cell
Aminoglycosides are a class of antibiotics that are produced by soil bacteria. They are primarily used to treat infections caused by aerobic gram-negative bacteria and some are used for mycobacterial infections. Aminoglycosides work by binding to bacterial ribosomes which interferes with protein synthesis. They have concentration-dependent bactericidal activity against many gram-negative organisms but limited activity against gram-positive bacteria. Common adverse effects include ototoxicity and nephrotoxicity. Therapeutic drug monitoring is important when using aminoglycosides to minimize toxicity risks.
This document discusses several newer antibiotics, including ceftaroline and ceftobiprole which are 5th generation cephalosporins used to treat MRSA, MSSA, and respiratory tract infections. It also mentions fidaxomicin, a novel macrolide antibiotic approved to treat C. difficile infections, with lower recurrence rates than vancomycin but a high price. Bedaquiline is an antibiotic approved for MDR-TB that inhibits mycobacterial ATP synthase and has a long half-life allowing intermittent dosing. Teixobactin is a new class of antibiotic isolated from soil that inhibits cell wall synthesis and has shown ability to kill pathogens without resistance developing.
This document discusses mechanisms of multi-drug resistance in bacteria and cancer cells. It describes how organisms can develop resistance through mutation, gene transfer, decreased membrane permeability, and efflux pumps that remove drugs from cells. Specifically, it explains that bacteria resist antibiotics via enzymatic degradation, altered target sites, and increased efflux. Cancer cells similarly resist chemotherapy through efflux pumps like P-glycoprotein and MDR proteins that transport drugs out of cells. The key mechanisms of multi-drug resistance shared by bacteria and cancer are efflux pumps and enzymatic deactivation of drugs.
The document discusses microbial biotransformation, which refers to biological processes in which microorganisms convert organic compounds into structurally modified reusable products through enzymatic reactions. It notes that biotransformation has several advantages over chemical synthesis, including specificity, mild reaction conditions, and reduced waste. Common biotransformation reactions include oxidation, reduction, hydrolysis, and isomerization. Examples of applications include producing steroids like testosterone and cortisone through microbial transformation, as well as transforming antibiotics, fatty acids, and degrading pollutants.
This document summarizes several antibiotics that inhibit bacterial cell wall synthesis including glycopeptides, lipopeptides, polypetides, fosfomycin, cycloserine, oxazolidinones, streptogramins, polymyxins, mupirocin, and fusidic acid. It provides details on their mechanisms of action, spectra of activity, uses, pharmacokinetics, and adverse effects. Key antibiotics discussed include vancomycin, telavancin, dalbavancin, oritavancin, linezolid, pristinamycin, colistin, and mupirocin.
Hybridoma technology involves fusing antibody-producing B cells (splenocytes) with myeloma cells to produce immortal hybridoma cell lines that secrete monoclonal antibodies of a single specificity. Georges Köhler and César Milstein developed the technique in 1975 and were awarded the 1984 Nobel Prize for this discovery. The process involves immunizing an animal to generate B cells that produce antibodies against the target antigen. The B cells are isolated from the spleen and fused with myeloma cells using polyethylene glycol or electrofusion. The fused cells are selected in HAT medium, which allows only hybridomas expressing the hypoxanthine-guanine phosphoribosyl transferase enzyme to survive and multiply indefinitely. The resulting stable monoclonal antibody-
Genomics and proteomics in drug discovery and developmentSuchittaU
This document discusses the role of genomics and proteomics in drug discovery and development. It explains that genomics and proteomics technologies can help identify new drug targets by comparing gene and protein expression between healthy and diseased cells. Proteomics in particular analyzes changes in protein levels and can quantify individual proteins using techniques like 2D gel electrophoresis and mass spectrometry. The integration of genomics and proteomics provides a more comprehensive understanding of biological systems and is improving the drug discovery process.
This document discusses efflux pumps in bacteria. It covers several topics:
1) Efflux pumps are membrane proteins that actively export toxins and antimicrobials from bacteria. Their overexpression is a mechanism of antimicrobial resistance.
2) Efflux pumps are classified into several families based on their structure and energy source, including ABC, MATE, MFS, SMR, and RND families.
3) Efflux pumps have natural physiological functions like exporting bile acids and fatty acids, but can also export a broad range of antimicrobials, contributing to multidrug resistance.
This document discusses superbugs and antibiotic resistance. It defines superbugs as bacteria that are resistant to multiple antibiotics. It describes the NDM-1 gene, which confers resistance to carbapenems, and notes it was first identified in India in 2010. The document outlines the main mechanisms by which bacteria develop antibiotic resistance, including drug modification, altered target sites, and efflux pumps. It lists overuse and misuse of antibiotics as key causes of rising superbug infections globally.
Antibiotics acting on cell wall 3 Carbapenems and Monobactums 03-05-2018Ravi Kant Agrawal
Carbapenems and monobactams are new classes of β-lactam antibiotics that act on cell wall synthesis. Carbapenems like imipenem and meropenem have a broad spectrum of activity against gram-positive and gram-negative bacteria. They are often used as last resort drugs for serious infections but resistance is emerging. Meropenem has advantages over imipenem like not requiring an inhibitor and being more soluble. Ertapenem also has activity against anaerobes but not pseudomonas. Monobactams have a monocyclic structure and are isolated from bacteria.
This document provides an overview of beta lactam antibiotics, including their structure, mode of action, examples, and mechanisms of resistance. It begins by discussing the bacterial cell wall structure and how beta lactams work by inhibiting cell wall synthesis. Major classes of beta lactams covered include penicillins, cephalosporins, carbapenems, and monobactams. Examples such as methicillin, amoxicillin, and imipenem are described. The document also discusses beta lactamase resistance and concludes with a brief overview of classification.
Amphotericin B is a broad-spectrum antifungal drug isolated from Streptomyces nodosus. It binds to ergosterol in fungal cell membranes, forming pores that cause leakage and cell death. Common adverse effects include infusion-related fever and chills, as well as cumulative renal toxicity. It is used for serious, life-threatening fungal infections like candidiasis, cryptococcosis, and aspergillosis.
Penicillins are a group of antibiotics that are derived from the Penicillium mold. They work by inhibiting the final step of bacterial cell wall synthesis through binding to penicillin-binding proteins. This prevents cross-linking of peptidoglycan chains, leading to cell lysis. The first penicillin discovered was penicillin G, which is acid labile and used parenterally. Semisynthetic penicillins were later developed with better stability and absorption, including penicillinase-resistant penicillins effective against Staphylococcus. Extended-spectrum penicillins like ampicillin are also active against common gram-negative bacteria.
Most antiviral drugs target viral replication by interfering with viral nucleic acid synthesis or late protein synthesis. They require conversion to active triphosphate forms by host cell kinases to inhibit viral polymerases more selectively than host polymerases. Combination antiviral therapy increases effectiveness and delays drug resistance emergence. Current HIV treatment involves two or three drugs before symptoms, often two reverse transcriptase inhibitors plus a protease inhibitor to slow viral load increases and delay resistance.
This document discusses antibiotics, including their classification, mechanisms of action, uses, and side effects. It covers several classes of antibiotics such as penicillins, cephalosporins, tetracyclines, macrolides, aminoglycosides, sulfonamides, and others. It describes how each class works, examples of drugs within the class, their indications, dosages, and potential adverse effects. The document provides a comprehensive overview of different types of antibiotics and important considerations for their use.
6.antibiotics in oral and maxillofacial surgeryTejaswini498924
This document provides an overview of antibiotics used in oral and maxillofacial surgery. It begins with a brief history of antibiotics and chemotherapy. It then classifies antibiotics based on chemical structure, mechanism of action, spectrum of activity, and type of organism targeted. The document discusses principles for choosing and administering antibiotics, including achieving sufficient concentration at the infection site. It also covers antibiotic resistance, toxicity, and failure of chemotherapy. Finally, the document provides details on common classes of antibiotics like penicillins, cephalosporins, quinolones, macrolides, tetracyclines, and aminoglycosides.
The document discusses various classes of antimicrobial agents including their classification, mechanisms of action, spectra of activity, and examples. It covers antibiotics such as penicillin, cephalosporins, aminoglycosides, and macrolides. It also addresses antimicrobial resistance, rational antibiotic usage, and combination therapy.
- Penicillins are a major class of antibiotics that were the first discovered from the mold Penicillium. They work by inhibiting the final step of bacterial cell wall synthesis through binding to penicillin-binding proteins. This disrupts cell wall formation and causes cell lysis.
- There are different generations/classes of penicillins that vary in their spectra of activity and resistance to bacterial beta-lactamases. Oral forms are absorbed from the gastrointestinal tract while injectable forms provide more sustained drug levels. Adverse effects include hypersensitivity reactions and gastrointestinal issues.
This document discusses the structure and synthesis of bacterial cell walls. It begins by outlining the contents which include the structure of peptidoglycan, its synthesis, the role of the cytoskeleton, patterns of cell wall synthesis, and the significance of peptidoglycan cell walls. It then goes into more detail on the ultrastructure of gram positive and gram negative cell walls, the synthesis of peptidoglycan subunits, transpeptidation reactions, and how the cytoskeleton controls cell shape through cell wall synthesis. Patterns of new cell wall growth in different bacteria are also described. The conclusion emphasizes the importance of the peptidoglycan cell wall for bacterial growth, shape, and protection
Hybridoma technology is a method for producing large number of identical antibodies called monoclonal antibodies.
It was discovered by G.kohler and C.milstein in 1975. they were awarded nobel prize for physiology and medicine in 1975.
The hybrid cells are produced by fusing B- lumphocyte with myeloma cells or tumour cells.
The B-lymphocyte have the ability to produce large number of antibodies and tumour cells have indefinite growth.
This is why two cells are used for the production of hybrid cell
Aminoglycosides are a class of antibiotics that are produced by soil bacteria. They are primarily used to treat infections caused by aerobic gram-negative bacteria and some are used for mycobacterial infections. Aminoglycosides work by binding to bacterial ribosomes which interferes with protein synthesis. They have concentration-dependent bactericidal activity against many gram-negative organisms but limited activity against gram-positive bacteria. Common adverse effects include ototoxicity and nephrotoxicity. Therapeutic drug monitoring is important when using aminoglycosides to minimize toxicity risks.
This document discusses several newer antibiotics, including ceftaroline and ceftobiprole which are 5th generation cephalosporins used to treat MRSA, MSSA, and respiratory tract infections. It also mentions fidaxomicin, a novel macrolide antibiotic approved to treat C. difficile infections, with lower recurrence rates than vancomycin but a high price. Bedaquiline is an antibiotic approved for MDR-TB that inhibits mycobacterial ATP synthase and has a long half-life allowing intermittent dosing. Teixobactin is a new class of antibiotic isolated from soil that inhibits cell wall synthesis and has shown ability to kill pathogens without resistance developing.
This document discusses mechanisms of multi-drug resistance in bacteria and cancer cells. It describes how organisms can develop resistance through mutation, gene transfer, decreased membrane permeability, and efflux pumps that remove drugs from cells. Specifically, it explains that bacteria resist antibiotics via enzymatic degradation, altered target sites, and increased efflux. Cancer cells similarly resist chemotherapy through efflux pumps like P-glycoprotein and MDR proteins that transport drugs out of cells. The key mechanisms of multi-drug resistance shared by bacteria and cancer are efflux pumps and enzymatic deactivation of drugs.
The document discusses microbial biotransformation, which refers to biological processes in which microorganisms convert organic compounds into structurally modified reusable products through enzymatic reactions. It notes that biotransformation has several advantages over chemical synthesis, including specificity, mild reaction conditions, and reduced waste. Common biotransformation reactions include oxidation, reduction, hydrolysis, and isomerization. Examples of applications include producing steroids like testosterone and cortisone through microbial transformation, as well as transforming antibiotics, fatty acids, and degrading pollutants.
This document summarizes several antibiotics that inhibit bacterial cell wall synthesis including glycopeptides, lipopeptides, polypetides, fosfomycin, cycloserine, oxazolidinones, streptogramins, polymyxins, mupirocin, and fusidic acid. It provides details on their mechanisms of action, spectra of activity, uses, pharmacokinetics, and adverse effects. Key antibiotics discussed include vancomycin, telavancin, dalbavancin, oritavancin, linezolid, pristinamycin, colistin, and mupirocin.
Hybridoma technology involves fusing antibody-producing B cells (splenocytes) with myeloma cells to produce immortal hybridoma cell lines that secrete monoclonal antibodies of a single specificity. Georges Köhler and César Milstein developed the technique in 1975 and were awarded the 1984 Nobel Prize for this discovery. The process involves immunizing an animal to generate B cells that produce antibodies against the target antigen. The B cells are isolated from the spleen and fused with myeloma cells using polyethylene glycol or electrofusion. The fused cells are selected in HAT medium, which allows only hybridomas expressing the hypoxanthine-guanine phosphoribosyl transferase enzyme to survive and multiply indefinitely. The resulting stable monoclonal antibody-
Genomics and proteomics in drug discovery and developmentSuchittaU
This document discusses the role of genomics and proteomics in drug discovery and development. It explains that genomics and proteomics technologies can help identify new drug targets by comparing gene and protein expression between healthy and diseased cells. Proteomics in particular analyzes changes in protein levels and can quantify individual proteins using techniques like 2D gel electrophoresis and mass spectrometry. The integration of genomics and proteomics provides a more comprehensive understanding of biological systems and is improving the drug discovery process.
This document discusses efflux pumps in bacteria. It covers several topics:
1) Efflux pumps are membrane proteins that actively export toxins and antimicrobials from bacteria. Their overexpression is a mechanism of antimicrobial resistance.
2) Efflux pumps are classified into several families based on their structure and energy source, including ABC, MATE, MFS, SMR, and RND families.
3) Efflux pumps have natural physiological functions like exporting bile acids and fatty acids, but can also export a broad range of antimicrobials, contributing to multidrug resistance.
This document discusses superbugs and antibiotic resistance. It defines superbugs as bacteria that are resistant to multiple antibiotics. It describes the NDM-1 gene, which confers resistance to carbapenems, and notes it was first identified in India in 2010. The document outlines the main mechanisms by which bacteria develop antibiotic resistance, including drug modification, altered target sites, and efflux pumps. It lists overuse and misuse of antibiotics as key causes of rising superbug infections globally.
Antibiotics acting on cell wall 3 Carbapenems and Monobactums 03-05-2018Ravi Kant Agrawal
Carbapenems and monobactams are new classes of β-lactam antibiotics that act on cell wall synthesis. Carbapenems like imipenem and meropenem have a broad spectrum of activity against gram-positive and gram-negative bacteria. They are often used as last resort drugs for serious infections but resistance is emerging. Meropenem has advantages over imipenem like not requiring an inhibitor and being more soluble. Ertapenem also has activity against anaerobes but not pseudomonas. Monobactams have a monocyclic structure and are isolated from bacteria.
This document provides an overview of beta lactam antibiotics, including their structure, mode of action, examples, and mechanisms of resistance. It begins by discussing the bacterial cell wall structure and how beta lactams work by inhibiting cell wall synthesis. Major classes of beta lactams covered include penicillins, cephalosporins, carbapenems, and monobactams. Examples such as methicillin, amoxicillin, and imipenem are described. The document also discusses beta lactamase resistance and concludes with a brief overview of classification.
Amphotericin B is a broad-spectrum antifungal drug isolated from Streptomyces nodosus. It binds to ergosterol in fungal cell membranes, forming pores that cause leakage and cell death. Common adverse effects include infusion-related fever and chills, as well as cumulative renal toxicity. It is used for serious, life-threatening fungal infections like candidiasis, cryptococcosis, and aspergillosis.
Penicillins are a group of antibiotics that are derived from the Penicillium mold. They work by inhibiting the final step of bacterial cell wall synthesis through binding to penicillin-binding proteins. This prevents cross-linking of peptidoglycan chains, leading to cell lysis. The first penicillin discovered was penicillin G, which is acid labile and used parenterally. Semisynthetic penicillins were later developed with better stability and absorption, including penicillinase-resistant penicillins effective against Staphylococcus. Extended-spectrum penicillins like ampicillin are also active against common gram-negative bacteria.
Most antiviral drugs target viral replication by interfering with viral nucleic acid synthesis or late protein synthesis. They require conversion to active triphosphate forms by host cell kinases to inhibit viral polymerases more selectively than host polymerases. Combination antiviral therapy increases effectiveness and delays drug resistance emergence. Current HIV treatment involves two or three drugs before symptoms, often two reverse transcriptase inhibitors plus a protease inhibitor to slow viral load increases and delay resistance.
This document discusses antibiotics, including their classification, mechanisms of action, uses, and side effects. It covers several classes of antibiotics such as penicillins, cephalosporins, tetracyclines, macrolides, aminoglycosides, sulfonamides, and others. It describes how each class works, examples of drugs within the class, their indications, dosages, and potential adverse effects. The document provides a comprehensive overview of different types of antibiotics and important considerations for their use.
6.antibiotics in oral and maxillofacial surgeryTejaswini498924
This document provides an overview of antibiotics used in oral and maxillofacial surgery. It begins with a brief history of antibiotics and chemotherapy. It then classifies antibiotics based on chemical structure, mechanism of action, spectrum of activity, and type of organism targeted. The document discusses principles for choosing and administering antibiotics, including achieving sufficient concentration at the infection site. It also covers antibiotic resistance, toxicity, and failure of chemotherapy. Finally, the document provides details on common classes of antibiotics like penicillins, cephalosporins, quinolones, macrolides, tetracyclines, and aminoglycosides.
Tuberculosis is completely curable disease now a days but one should follow the treatment regimens correctly .so for under graduate MBBS students it is clearly explained with animations.Hope you all this will be helpful.
ANTIBIOTICS IN ORAL & MAXILLOFACIAL SURGERYankitaraj63
This document provides an overview of antibiotics used in oral and maxillofacial surgery. It begins with an introduction to antibiotics and their history. It then discusses various ways antibiotics can be classified including by chemical structure, mechanism of action, and spectrum of activity. Key principles for choosing and administering antibiotics are outlined. Common adverse reactions and antibiotic resistance are also reviewed. The document concludes with references. It provides a comprehensive but concise review of important antibiotics and concepts related to their use in oral and maxillofacial surgery.
Beta lactams- History, Current Trend and Recent AdvancesAnkitaNegi32
This document provides an overview of beta-lactam antibiotics including their history, current trends, and recent advances. It discusses the classes of beta-lactams such as penicillin, cephalosporins, carbapenems, and monobactams. The mechanisms of action and increasing bacterial resistance are also reviewed. Recent research highlights potential new applications of beta-lactams in cancer and neurological disorders as well as development of novel agents to address resistance.
The document discusses antibiotics and analgesics. It begins by defining antibiotics as chemical substances produced by microorganisms that inhibit or kill other microorganisms. It then covers the classification, mechanisms of action, and therapeutic uses of various antibiotics like penicillin, cephalosporins, erythromycin, tetracycline, and others. It also discusses analgesic classification into opioid and non-opioid categories and pain management strategies. The document provides an overview of commonly used antibiotics and analgesics for treating odontogenic infections and dental pain.
newer antibacterials are needed because of increasing antimicrobial resistance and no progression in discovery of new drugs as we are kind of stuck with our fight against bugs
Antibiotics inhibiting protein synthesis 3 chloramphenicol and macrolides 03 ...Ravi Kant Agrawal
1. Chloramphenicol and macrolides like erythromycin inhibit protein synthesis in bacteria by binding to the 50S subunit of the bacterial ribosome, preventing proper alignment and peptide bond formation.
2. Chloramphenicol has broad-spectrum activity but is limited in clinical use due to potential bone marrow toxicity. It maintains activity against many gram-positive and gram-negative bacteria as well as some anaerobes.
3. Macrolides bind tightly to the P site of the bacterial ribosome, blocking translocation and translation. They are effective against a variety of bacteria and atypical pathogens.
The document discusses antibiotics used in dental practice. It begins with an introduction on prescribing antibiotics for odontogenic infections and issues of antibiotic resistance. It then covers definitions and classifications of antibiotics, including classifications based on susceptible organisms and mechanisms of action. The document discusses various classes of antibiotics in detail, including penicillins, cephalosporins, erythromycin, tetracyclines, clindamycin and aminoglycosides. It addresses the spectrum of activity, pharmacokinetics and therapeutic uses of antibiotics commonly prescribed for odontogenic infections.
Tuberculosis is caused by Mycobacterium tuberculosis and remains a major health problem in India with over 2 million cases annually. It is treated using a combination of anti-tubercular drugs to prevent resistance. First line drugs include isoniazid, rifampicin, pyrazinamide, and ethambutol. These are given in an initial intensive phase and then a continuation phase to fully treat the infection. Second line drugs are used when resistance develops or for intolerances. New drugs are also being developed and tested in clinical trials to improve treatment outcomes.
This document discusses anti-tubercular drugs. It begins by describing tuberculosis and its transmission. It then discusses the classification of anti-TB drugs into 1st line essential, 1st line supplemental, and 2nd line drugs. The individual drugs discussed in detail include isoniazid, rifampicin, ethambutol, pyrazinamide, and streptomycin. It covers their mechanisms of action, mechanisms of resistance, pharmacokinetics, dosages, adverse effects, and interactions. Treatment categories and regimens are also summarized.
This document provides an overview of quinolones, a class of antibacterial agents. It discusses the discovery of nalidixic acid, the first quinolone, and the subsequent development of fluoroquinolones. The mechanisms of action and mechanisms of resistance are described. Various generations of fluoroquinolones are classified and their spectra of activity, pharmacokinetics, uses, and adverse effects are summarized. Newer quinolone agents such as finalafloxacin and delafloxacin are also briefly mentioned.
This document provides an overview of antimicrobial drugs used to treat and prevent infections. It begins with objectives of reviewing key concepts of antimicrobial therapy. It then discusses mechanisms of action for different classes of antimicrobials including why antibiotics only target bacterial cells. The remainder of the document covers specific classes of antimicrobial drugs like beta-lactams, macrolides, and vancomycin. It provides details on indications, mechanisms of action, and important nursing considerations for each drug class.
This document discusses cell wall inhibitors, specifically penicillins and cephalosporins. It covers their mechanisms of action, which involve inhibiting bacterial cell wall synthesis. It describes their antimicrobial spectra against gram-positive and gram-negative bacteria. Resistance mechanisms like beta-lactamase production are also summarized. The pharmacokinetics of administration, distribution, and excretion of these drugs is covered. Finally, the document outlines some common adverse effects.
The document discusses cephalosporins, a class of beta-lactam antibiotics. It describes how cephalosporins are structurally and functionally similar to penicillins. Cephalosporins are classified into generations based on their antimicrobial spectrum, with later generations having broader coverage. The document outlines the mechanisms of action, pharmacokinetics, uses, adverse effects and contraindications of various cephalosporin antibiotics.
Glycopeptides, Lipopeptides, Lipoglycopeptides and Polymyxins Antibiotics Abdullatif Al-Rashed
1) Vancomycin and daptomycin are glycopeptides and lipopeptides respectively that are used to treat infections caused by gram-positive bacteria like MRSA. They work by inhibiting cell wall synthesis.
2) Vancomycin has side effects of fever, redness, and hearing loss while daptomycin can cause muscle damage.
3) Newer drugs like lipoglycopeptides have dual mechanisms of inhibiting cell wall synthesis and disrupting membranes. They are generally more potent than vancomycin against gram-positives.
This document discusses antimycobacterial drugs used to treat tuberculosis and other mycobacterial infections. It provides information on various first-line drugs including isoniazid, rifampin, pyrazinamide, ethambutol, and streptomycin. It notes that combinations of two or more drugs are required to treat mycobacterial infections due to slow growth and potential drug resistance. Treatment must be prolonged, typically for months to years, to eliminate both actively dividing and dormant bacteria. Second-line drugs are discussed for treatment of multi-drug resistant infections. Worldwide tuberculosis statistics and drug regimens are also summarized.
The document summarizes several classes of penicillin antibiotics including natural penicillin, beta-lactamase resistant penicillin, aminopenicillin, and macrolides. It provides information on their mechanism of action, indications, dosages, side effects, drug interactions and brands. Mechanisms generally involve inhibiting bacterial cell wall synthesis. Common indications are respiratory, skin, and ear infections. Side effects include gastrointestinal issues. Drug interactions can occur with methotrexate, oral contraceptives, and vaccines. Brand examples provided are penicillin V, cloxacillin, amoxicillin, and erythromycin.
This document discusses various antimicrobial agents used to treat different mycobacterial infections including tuberculosis, leprosy, and MAC. It provides details on the first and second line treatments for each infection, including the typical dosage of each drug. It also describes the pharmacodynamics, pharmacokinetics, mechanisms of action, resistance issues, and side effects for many of the major antimicrobial agents used, including isoniazid, rifampin, ethambutol, pyrazinamide, streptomycin, and others. Combination therapy is emphasized to reduce resistance and rapidly decrease the bacterial population for tuberculosis treatment.
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These lecture slides, by Dr Sidra Arshad, offer a simplified look into the mechanisms involved in the regulation of respiration:
Learning objectives:
1. Describe the organisation of respiratory center
2. Describe the nervous control of inspiration and respiratory rhythm
3. Describe the functions of the dorsal and respiratory groups of neurons
4. Describe the influences of the Pneumotaxic and Apneustic centers
5. Explain the role of Hering-Breur inflation reflex in regulation of inspiration
6. Explain the role of central chemoreceptors in regulation of respiration
7. Explain the role of peripheral chemoreceptors in regulation of respiration
8. Explain the regulation of respiration during exercise
9. Integrate the respiratory regulatory mechanisms
10. Describe the Cheyne-Stokes breathing
Study Resources:
1. Chapter 42, Guyton and Hall Textbook of Medical Physiology, 14th edition
2. Chapter 36, Ganong’s Review of Medical Physiology, 26th edition
3. Chapter 13, Human Physiology by Lauralee Sherwood, 9th edition
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2. INTRODUCTION
• Serious infections caused by microorganisms resistant to
commonly used antimicrobials have become a major
healthcare problem worldwide in the 21st century.
• In recent years, the number of availability of new
antimicrobials for human use across the globe has been
lower than in the recent past.
• In this presentation, all new antibacterial agents which
have been approved after the year 2000 have been
described along with their mechanism of action,
development of resistance, spectrum of activity and the
stage of developmental in case of yet to be approved
drugs.
5. Macrocyclic
antibiotic
• Fidaxomicin
• It is the first drug in this new class of
antimicrobial agents which shows narrow
spectrum of activity.
• It is active against Clostridium difficile
infection (CDI) and show limited activity
against normal intestinal flora.
• This drug acts by inhibiting the bacterial
enzyme RNA polymerase.
• It is an alternative to the currently used
treatment regimens of vancomycin and
metronidazole against CDI.
6. • In a phase III trial (n = 1000),
fidaxomicin 200 mg (twice a day) was
found to be non-inferior to
vancomycin 125 mg (four times a day)
for the treatment of initial or first
recurrences of CDI.
• Recurrence rates of CDI
with fidaxomicin were significantly
lower (13%) as compared to
vancomycin (25%).
• It is available as oral formulation with
recommended dose of 200 mg twice
daily.
7. Newer cephalosporins
Ceftaroline
• Ceftaroline fosamil is a prodrug of Ceftaroline.
• It is a novel broad-spectrum antibiotic effective against Methicillin
Resistant Staphylococcus aureus (MRSA), penicillin and cephalosporin
resistant S. pneumoniae, vancomycin-intermediate S. aureus (VISA),
and vancomycin-resistant S. aureus (VRSA).
• It is also active against many gram-negative pathogens but inactive
against extended-spectrum β-lactamase (ESBL) producing bacteria. It
has been approved for the treatment of community acquired
pneumonia (CAP).
• Ceftaroline was developed by modifying the structure of the fourth-
generation cephalosporin cefozopran.
8. • Ceftaroline acts by binding to penicillin binding proteins 1-4 (PBPs 1-4). It shows
high affinity for PBP2a present in Staphloccocus aureus, which is responsible for
methicillin resistance.
• In S. pneumonia, ceftaroline can bind to all six PBPs identified (PBP1A, 1B, 2x,
2A/B, and 3).
• Inside the blood circulation, ceftaroline fosamil (prodrug) is rapidly converted to
ceftaroline (active form) by phosphatase enzymes.
• It exhibits linear pharmacokinetics and has a serum half-life (t½) of 1.6 hr (for a
single dose) to 2.7 hr (following multiple doses).
• Volume of distribution of ceftaroline is similar to that of other parenteral
cephalosporins with plasma protein binding of 20%.
9. • Ceftaroline is metabolized by hydrolysis of its β-lactam ring which results into
the formation of an inactive, open-ring metabolite called as ceftaroline M-1.
• It has a low potential for drug interactions because of insignificant metabolism
by CYP450 enzymes.
• It is given as 600 mg intravenous dose, every 12 hourly. Dose adjustment is
required in patients with renal impairment as it is primarily eliminated by the
kidneys.
• The most common side effects observed during clinical trials were nausea,
dysgeusia and caramel-like taste disturbances, vomiting, diarhoea and headache.
10. Ceftobiprole
• It is another newer cephalosporin which has
completed its trial in 2007 and approved by FDA in
2010.
• It is the broad-spectrum antibiotic which shows
good spectrum of activity against MRSA, penicillin-
resistant S. pneumoniae, P.
aeruginosa and Enterococci. Ceftobiprole shows
strong affinity for PBP2a of MRSA and PBP2x of S.
Pneumoniae.
• It is given as 1 hr IV infusion of 500 mg every 12 hrs
for gram-positive infection and a 2 hr infusion of
500mg every 8 hrs for gram-negative. Dose
adjustment is needed in patients with renal
impairment.
• It is well tolerated with most common side effects
being nausea and dysgeusia
11. Newer
glycopeptides
• Due to emergence of vancomycin resistant
strains, interest has been focused on the
development of three newer derivatives of
glycopeptides – oritavancin, dalbavancin,
and telavancin.
• All three newer glycopeptides are much
more potent with lesser potential for
development of resistance in comparison
to vancomycin.
• They show rapid bactericidal activity
against Vancomycin
Resistant Enteroccoci (VRE) and VRSA,
unlike vancomycin which is bacteriostatic.
16. Teixobactin
• New class of antibiotic that was discovered
through the screening of uncultured bacteria
using i-Chip (isolation chip), a revolutionary
method for bacterial culture.
• In January 2015, a collaboration of four
institutes in the US and Germany together
with two pharmaceutical companies,
reported that they had isolated and
characterized a new antibiotic, killing
"without detectable resistance."[
• Teixobactin was identified as an effective
agent against Gram-positive bacteria. It
inhibits cell wall synthesis by binding to two
lipid cell wall precursors, namely lipid II
(peptidoglycan precursor) and lipid III
(teichoic acid precursor).
• In 2018 researchers synthesized the
compound and used it to treat a bacterial
17. Newer
carbapenems
• Doripenem
• It is the newer parenteral carbapenem
approved for the treatment of complicated
urinary tract infections and intra-abdominal
infections.
• The drug acts by binding to PBPs and thus
inhibiting cross-linking of the peptidoglycan
structure. The high binding affinity of
doripenem to PBP-2 and -3 may enhance its
activity against drug-resistant P. Aeruginosa.
• Thus, it is a suitable alternative to currently
available anti-pseudomonal carbapenems (i.e,
imipenem, meropenem).
• Doripenem has a unique spectrum of activity.
It shows activity against gram-positive cocci
like imipenem and activity against gram-
negative bacilli like meropenem.
18. • Recommended dose of doripenem is 500 mg
IV every 8 hr.
• The estimated elimination half-life of
doripenem is 0.95 hr, and 75% of the drug is
excreted unchanged in the urine, requiring
dosage adjustment in patients with renal
impairment.
• The most common ADRs are headache,
nausea, diarrhea, rash, and phlebitis.
Postmarketing reports have also identified
Stevens-Johnson syndrome, toxic epidermal
necrolysis, interstitial pneumonia, and
seizures as adverse drug reactions.
19. • Razupenem (PZ-601)
• It is another novel carbapenem active against multi drug-resistant gram
positive and gram-negative (ESBL producers) bacteria and is currently in
trials for cSSSI.
• further development is in doubt due to a high rate of side effects in Phase II
clinical trials.
20. Pleuromutilin
• Retapamulin
• It is a novel topical antibiotic and the
first approved member in this new
class. It is approved for the treatment
of skin and soft tissue infections caused
by S. pyogenes and S. aureus which are
resistant to the most commonly used
topical antibiotics.It is ineffective
against gram-negative organisms.
• Retapamulin is a semisynthetic
pleuromutilin derivative isolated
from Clitopilus scyphoides (an edible
mushroom).
21. • It is a protein synthesis inhibitor
which acts by binding to 50-S
subunit of bacterial ribosomes.
• Plasma protein binding of
Retapamulin is 94% and it is
metabolized mainly in liver by
CYP3A4 to numerous metabolites.
• The most common adverse effect is
pruritus at the application site.
22. Glycylcyclines
• Glycylcyclines is a new class of antimicrobials
that are chemical derivatives of minocycline
• Tigecycline
• It is the first glycylcycline approved by FDA for
cSSTIs, intra abdominal infections and CAP.
• It has been designed to overcome two
common mechanisms of tetracycline
resistance i.e. resistance mediated by
acquired efflux pumps and by ribosomal
protection.
• It acts by binding to 30-S subunit of
ribosome, thus inhibiting protein synthesis
which is 20 fold more efficient than
tetracycline.
23. • Tigecycline has a broader spectrum
of activity against aerobic and
anaerobic gram-negative and
positive pathogens. In vitro data
shows that tigecycline has very good
antibacterial activity against ESBL as
well.
• Tigecycline, formulated for
parenteral use only, is given as 100
mg loading dose followed by a
maintenance dose of 50 mg every
12 hr.
• The side effect profile includes mild
GIT disturbances like diarhoea,
nausea and vomiting.
24. Ketolides
• Ketolides are the new class of macrolides
designed particularly for the treatment of
respiratory tract pathogens that have
acquired resistance to macrolide
antibiotics.
• Telithromycin
• It is the first ketolide to enter clinical use for
the treatment of CAP, chronic bronchitis and
acute sinusitis.
• Telithromycin is a protein synthesis inhibitor
that blocks the progression of the growing
polypeptide chain by binding to 50-S subunit
of the bacterial ribosome.
25. • Telithromycin exhibits 10 times
higher affinity to the subunit 50-S
than erythromycin.
• In addition, telithromycin strongly
bind simultaneously to two
domains of 23-S RNA of the 50-S
ribosomal subunit, whereas older
macrolides bind strongly only to
one domain and weakly to the
second domain
26. • Telithromycin is more active in vitro against S. pneumoniae compared with
clarithromycin and azithromycin and maintains activity against macrolide
resistant strains (S. pneumoniae, S. pyogenes).
• Telithromycin is formulated as 400 mg tablet for oral administration. It is well
absorbed orally with 60% bioavailability.
• Approval of telithromycin was controversial due to trial irregularities, non-
inferiority study designs, and the use of foreign safety data.
• On 12 February 2007, FDA withdrew two of its indications with CAP as the only
remaining indication, with a black-box warning issued due to its safety concerns
involving hepatotoxicity, myasthenia gravis exacerbation, and visual
disturbances
27. Lipopeptides
• Daptomycin
• Daptomycin is a cyclic lipopeptide
antibiotic derived from Streptomyces
roseosporus and is the first member of
this new class of antimicrobials.
• It was approved by FDA in 2003 for the
treatment of SSTIs and approved in
2006 for the treatment of blood stream
infections.
• It shows the unique mechanism of
action by inserting its lipophilic tail
into the cell membrane of gram-
positive organisms without entering
the bacterial cytoplasm.
28. • This calcium dependent process leads to the formation of channels from
which intracellular potassium is lost disrupting the bacterial cell membrane
potential and causing cell death.
• Daptomycin is bactericidal against Methicillin resistant staphylococcus
aureus (MRSA), Methicillin-resistant Staphylococcus epidermidis and VRE
inclusive of linezolid-resistant isolates. It is inactive against gram negative
pathogens because of its inability to penetrate its outer membrane.
• It is poorly absorbed orally, thus administered by intravenous route only.
• In July 2010, a warning was issued by FDA about the potential of daptomycin
to cause life threatening complication i.e., eosinophilic pneumonia. Seven
cases of eosinophilic pneumonia were identified between 2004
and 2010
29.
30. Novel
dihydrofolate
reductase
inhibitors
• Iclaprim
• Iclaprim is a synthetic diaminopyrimidine, a
selective inhibitor of the enzyme
dihydrofolate reductase, which is similar to
trimethoprim.
• Iclaprim is particularly potent against S.
pneumoniae and S. aureus, including
trimethoprim-resistant isolates.
• In contrast to trimethoprim which is most
frequently used in combination with
sulfamethoxazole, iclaprim is being
developed for administration as a single
agent, though highly synergistic activity was
demonstrated with the sulfonamides like
sulfamethoxazole, and sulfadiazine
31. • Motif Bio submitted the NDA of iclaprim in June 2018 and about two months later
it was accepted by the FDA. The regulator also granted a priority review for the
skin disorder drug.
• The regulator indicated to the company that additional data was required in the
NDA to further asses the risk for liver toxicity prior to the drug’s approval.
• The US Food & Drug Administration (FDA) has refused to give its approval to
Motif Bio’s skin disorder drug iclaprim for the treatment of acute bacterial skin
and skin structure infections (ABSSSI).
32. Oxazolidinones
• Torezolid and radezolid are two novel
oxazolidinones being under research for
the treatment of cSSSI and uSSSI
respectively, and both have completed
phase II clinical trials.
• Their mechanism of action is similar to
linezolid i.e., to prevent the initiation of
translation of proteins by binding to the
23-S portion of the 50-S ribosomal
subunit.
• Tedizolid has been approved by the
U.S Food and Drug Administration on June
20, 2014, for the treatment of acute
bacterial Skin and skin structure
infections (ABSSSI)
33. • Radezolid (INN, codenamed RX-1741) is a novel oxazolidinone antibiotic
being developed by Melinta Therapeutics, Inc. for the treatment of bacterial
acne.
34. Target bacterial
proteins
• Antibiotics can act to target novel
bacterial proteins like inhibiting β-
ketoacyl-acyl-carrier-protein synthase
I/II enzyme required for fatty acid
biosynthesis.
• Platensimycin is one such drug in
preclinical trials which acts by blocking
these enzymes involved in the
condensation steps in fatty acid
biosynthesis.
35. Therapeutic use of
bacteriophages to
treat pathogenic
bacterial infections
• Small, acid-soluble protein (SASPs)
genes can be delivered to S. aureus via
a S. aureus-specific delivery
bacteriophage, resulting in the
production of SASPs which can bind to
and inactivate bacterial DNA.
• These proteins have been shown to be
rapidly bactericidal and active against a
range of S. aureus strains, irrespective
of existing antibiotic resistances.
36. Combination of
antibiotics with
bioenhancers
• A bioenhancer is an agent capable of enhancing
the bioavailability and efficacy of a drug with
which it is co-administered, without any
pharmacological activity of its own at the
therapeutic dose used.
• Bioenhancers can be used to increase the efficacy
of commonly used antibiotics, like combining
antibiotic tetracycline with non-antibiotic drug
loperamide tend to enhance the efficacy of
tetracycline by increasing its permeability.
• Cow urine distillate (CUD) can act as a potential
therapeutic target to enhance the activity of
antibacterial agents. CUD when combined with
rifampicin increased the activity of drug by about
5-7 times against Escherichia coli and 3-11 times
against gram-positive bacteria
37. • Engineer a prodrug that gets converted into highly potent drug within a
microbe
• Using prodrug form of a drug, which is converted into highly potent drug
within a microbe so that common resistance mechanisms could be
bypassed, can be another strategy for new drug discovery.
• Engineer hybrid antibacterial drugs for high potency against two targets
• Simultaneously two targets can be covered like Mutilin- quinolone hybrid
AM-3005 is a Type II topoisomerase inhibitor and also a protein synthesis
inhibitor.
38. Drug name Development
phase
Drug class Target Potential indication(s)?
Baxdela
(delafloxacin)
Approved
June 19, 2017
(U.S. FDA)
Fluoroquinolone Bacterial type
II topoisomeras
e
Approved for: Acute
bacterial skin and skin
structure infections;
other potential
indications:
community-acquired
bacterial pneumonia
and complicated
Vabomere
(Meropenem +
Vaborbactam)
Approved
Aug. 30, 2017
(U.S. FDA)
β-lactam
(carbapenem) +
β-lactamase
inhibitor (cyclic
boronate)
PBP; β-
lactamase
Approved for:
Complicated urinary
tract infections
including
pyelonephritis; other
potential indications:
complicated intra-
abdominal infections,
hospitalacquired
bacterial pneumonia/
ventilator-associated
bacterial pneumonia
39. Drug name Development
phase
Drug class Target Potential
indication(s)?
Taksta (fusidic
acid)
Phase 3 Fusidane Elongation
factor G
Acute bacterial skin
and skin structure
infections and
prosthetic joint
infections
Zabofloxacin Phase 3 Fluoroquinolone Bacterial type
II topoisomeras
e
Bacterial type
II topoisomerase
Sulopenem Phase 3 β-lactam
(carbapenem)
PBP Complicated and
uncomplicated urin
ary tract
infections, and
complicated intra-
abdominal
infections
40. Drug name Development
phase
Drug class Target Potential indication(s)?
Omadacycline Phase 3 Tetracycline 30S subunit
of bacterial rib
osome
Community-acquired
bacterial pneumonia,
acute bacterial skin and
skin structure infections,
urinary tract infections
Solithera
(solithromycin)
Phase 3 Macrolide 50S subunit
of bacterial rib
osome
50S subunit
of bacterial ribosome
Lefamulin (BC-
3781)
Phase 3 Pleuromutilin 50S subunit of
bacterial ribos
ome
Acute bacterial skin and
skin structure infections,6
community-acquired
bacterial pneumonia,
41. Drug name Development
phase
Drug class Target Potential
indication(s)?
Lascufloxacin
(KRP-AM1977)
Phase 3 Fluoroquinolone Bacterial type
II topoisomerase
Community-
acquired bacterial
pneumonia
Eravacycline Phase 3 Tetracycline 30S subunit
of bacterial riboso
me
Complicated
intra-abdominal
infections and
complicated
urinary tract
infections
Cadazolid Phase 3 Oxazolidinonequi
nolone hybrid
50S subunit
of bacterial riboso
me; bacterial type
II topoisomerase
C. difficile
infection
42. Drug name Development
phase
Drug class Target Potential indication(s)?
WCK 771/ WCK
234916
Phase 2 Fluoroquinolone Bacterial type
II topoisomerase
Hospital-acquired
bacterial pneumonia
Nemonoxacin Phase 2 Quinolone Bacterial type
II topoisomerase
Community-acquired
bacterial pneumonia,
diabetic foot infection,
and acute bacterial
skin and skin structure
infections
Murepavadin
(POL7080)
Phase 2 Antimicrobial
peptide
mimetic11
Ventilator-associated
bacterial pneumonia
(caused by P.
aeruginosa)
43. Drug name Development
phase
Drug class Target Potential indication(s)?
SPR994 Phase 1 β-lactam
(carbapenem)
PBP Community-acquired
bacterial pneumonia6
and complicated urinary
tract infections
MCB3837 Phase 1 Oxazolidinonequ
inolone hybrid
50S subunit
of bacterial riboso
me; bacterial type
II topoisomerase
C. difficile infection
KBP-7072 Phase 1 Tetracycline 30S subunit
of bacterial riboso
me
Community-acquired
bacterial pneumonia