Antibiotics are used to treat infections caused by bacteria. The document discusses the history and pioneers of antimicrobial therapy. It covers terminology, ideal characteristics, classification, and factors to consider when selecting antibiotics. Adverse effects like toxicity, resistance, and superinfection are also reviewed. The use of antibiotics in periodontics and ways to prevent resistance development are described.
Rational Use of Antibiotics. Infection was a major cause of morbidity and mortality, before the development of antibiotics.
The treatment of infections faced a great challenge during those periods.
Later in 1928, the discovery of Penicillin, a beta-lactam antibiotic, by Alexander Fleming opened up the golden era of antibiotics.
It marked a revolution in the treatment of infectious diseases and stimulated new efforts to synthesize newer antibiotics.
The period between the 1950s and 1970s is considered the golden era of discovery of novel antibiotic classes, with very few classes discovered since then.
1) The document discusses principles of antimicrobial therapy, including how antimicrobial drugs work by selectively killing microorganisms without harming host cells.
2) Selection of the best antimicrobial agent requires identifying the infecting organism, determining its drug susceptibility, considering the infection site and patient factors like immunity or organ function, and weighing the drug's safety, cost and ability to reach the infection site.
3) Antimicrobial therapy aims to rapidly identify pathogens, start immediate empiric treatment when needed, and later adjust therapy based on identification and susceptibility results while considering host barriers, drug properties, and toxicity risks.
1. Antibiotics are chemical substances produced by microorganisms like fungi, actinomycetes and bacteria that suppress or destroy other microorganisms.
2. Alexander Fleming discovered penicillin in 1929 after noticing that a mold growing in one of his petri dishes had prevented bacteria from growing nearby. Penicillin revolutionized medicine as the first widely used antibiotic.
3. Antibiotic resistance has become a major problem as bacteria have increasingly developed resistance, even to formerly powerful antibiotics like penicillin. Proper antibiotic stewardship including only using antibiotics when necessary and completing prescribed treatment courses can help address this growing threat.
This document discusses antibiotics used in periodontics. It defines key terms like antibiotic, antimicrobial, and provides classifications of antibiotics based on chemical structure, mechanism of action, spectrum of activity, and source. It outlines guidelines for antibiotic use in periodontal disease, including indications, choosing an antibiotic based on patient and microbe factors, dosing principles, and duration of therapy. Systemic and local antibiotic administration methods are discussed. Common antibiotics used in periodontics that have been extensively evaluated are also listed.
Antibiotic selection /certified fixed orthodontic courses by Indian dental ...Indian dental academy
This document provides information on antibiotics used for head and neck infections. It discusses the history of antibiotic discovery, classifications of antibiotics based on mechanism of action and type of organism affected, considerations for antibiotic selection such as host defenses and infection characteristics, administration principles, and potential adverse reactions. The key factors in selecting an appropriate antibiotic include the typical mixed aerobic-anaerobic oral flora, penicillin as first-line therapy, narrow-spectrum use, and parenteral administration for serious infections.
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.
This document provides an overview of antibiotics used in periodontics. It begins with an introduction to antibiotics and their historical background. It then covers classification of antimicrobial agents based on chemical structure, mechanism of action, organisms targeted, and spectrum of activity. Guidelines for antibiotic use in periodontal diseases are presented, along with the diseases where antibiotics can be used. Commonly used antibiotics like tetracycline, doxycycline, metronidazole, penicillin, and amoxicillin-clavulanate are described in detail. The document concludes with a reference to research on systemic antibiotic use in periodontics.
Rational Use of Antibiotics. Infection was a major cause of morbidity and mortality, before the development of antibiotics.
The treatment of infections faced a great challenge during those periods.
Later in 1928, the discovery of Penicillin, a beta-lactam antibiotic, by Alexander Fleming opened up the golden era of antibiotics.
It marked a revolution in the treatment of infectious diseases and stimulated new efforts to synthesize newer antibiotics.
The period between the 1950s and 1970s is considered the golden era of discovery of novel antibiotic classes, with very few classes discovered since then.
1) The document discusses principles of antimicrobial therapy, including how antimicrobial drugs work by selectively killing microorganisms without harming host cells.
2) Selection of the best antimicrobial agent requires identifying the infecting organism, determining its drug susceptibility, considering the infection site and patient factors like immunity or organ function, and weighing the drug's safety, cost and ability to reach the infection site.
3) Antimicrobial therapy aims to rapidly identify pathogens, start immediate empiric treatment when needed, and later adjust therapy based on identification and susceptibility results while considering host barriers, drug properties, and toxicity risks.
1. Antibiotics are chemical substances produced by microorganisms like fungi, actinomycetes and bacteria that suppress or destroy other microorganisms.
2. Alexander Fleming discovered penicillin in 1929 after noticing that a mold growing in one of his petri dishes had prevented bacteria from growing nearby. Penicillin revolutionized medicine as the first widely used antibiotic.
3. Antibiotic resistance has become a major problem as bacteria have increasingly developed resistance, even to formerly powerful antibiotics like penicillin. Proper antibiotic stewardship including only using antibiotics when necessary and completing prescribed treatment courses can help address this growing threat.
This document discusses antibiotics used in periodontics. It defines key terms like antibiotic, antimicrobial, and provides classifications of antibiotics based on chemical structure, mechanism of action, spectrum of activity, and source. It outlines guidelines for antibiotic use in periodontal disease, including indications, choosing an antibiotic based on patient and microbe factors, dosing principles, and duration of therapy. Systemic and local antibiotic administration methods are discussed. Common antibiotics used in periodontics that have been extensively evaluated are also listed.
Antibiotic selection /certified fixed orthodontic courses by Indian dental ...Indian dental academy
This document provides information on antibiotics used for head and neck infections. It discusses the history of antibiotic discovery, classifications of antibiotics based on mechanism of action and type of organism affected, considerations for antibiotic selection such as host defenses and infection characteristics, administration principles, and potential adverse reactions. The key factors in selecting an appropriate antibiotic include the typical mixed aerobic-anaerobic oral flora, penicillin as first-line therapy, narrow-spectrum use, and parenteral administration for serious infections.
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.
This document provides an overview of antibiotics used in periodontics. It begins with an introduction to antibiotics and their historical background. It then covers classification of antimicrobial agents based on chemical structure, mechanism of action, organisms targeted, and spectrum of activity. Guidelines for antibiotic use in periodontal diseases are presented, along with the diseases where antibiotics can be used. Commonly used antibiotics like tetracycline, doxycycline, metronidazole, penicillin, and amoxicillin-clavulanate are described in detail. The document concludes with a reference to research on systemic antibiotic use in periodontics.
this slides includes overview of antimicrobial drugs, their classifications, antimicrobial resistance, adverse effects and toxicity, choice of antimicrobial drugs and its uses
Anti-infective agents are drugs designed to selectively target and kill invading microorganisms without harming the host's cells. Paul Ehrlich was the first scientist to develop a synthetic chemical with this property in the 1920s. Anti-infectives work by interfering with microbial cell walls, protein synthesis, DNA synthesis, or cell membranes. Their goal is to reduce microbial populations to levels the immune system can handle. Microbes can develop resistance by modifying drug targets or transport mechanisms. Careful dosing and limiting inappropriate use can help prevent resistance.
This document provides an overview of different classes of antibiotics, including their mechanisms of action, uses, and side effects. It discusses beta-lactam antibiotics like penicillins and cephalosporins, as well as macrolides, fluoroquinolones, aminoglycosides, tetracyclines, chloramphenicol, glycopeptides and others. Each class is described in terms of its antimicrobial spectrum and applications for treating various bacterial infections. Potential adverse effects are also outlined for safety considerations.
The document discusses various topics related to antibiotics including their history, definitions, classifications, mechanisms of action, and guidelines for use. Some key points:
- Antibiotics are drugs produced by microorganisms that inhibit or destroy other microorganisms. They can be naturally occurring, semisynthetic, or synthetic.
- Major classifications include based on chemical structure, mechanism of action, type of organism targeted, and spectrum of activity.
- Penicillin was the first antibiotic to be used clinically in 1941. Extended-spectrum penicillins like ampicillin are broad-spectrum and cover both gram-positive and gram-negative bacteria commonly causing dental infections.
- Guidelines emphasize accurate diagnosis, appropriate antibiotic selection
This document discusses principles of antimicrobial therapy and chemotherapeutic drugs. It covers several topics including the selection and use of antimicrobial agents, factors that influence drug choice such as the infecting organism, site of infection, and patient characteristics. The document also discusses concepts like narrow versus broad spectrum antibiotics, antibiotic resistance, prophylactic use of drugs, and potential complications of therapy like hypersensitivity and superinfections. The overall goal of antimicrobial therapy is to selectively kill the infecting pathogen without harming the host. Careful consideration of many factors is needed to choose the most appropriate treatment approach.
Chemotherapy is a type of cancer treatment that uses one or more anti-cancer drugs as part of a standardized chemotherapy regimen. Chemotherapy may be given with a curative intent, or it may aim to prolong life or to reduce symptom
The document discusses anti-infective agents, which are drugs designed to selectively target and kill invading microorganisms without harming the host's cells. It provides a brief history of anti-infective development and outlines several mechanisms of action, including interfering with bacterial cell wall synthesis, protein synthesis, and DNA synthesis. The document also discusses anti-infective classification, acquiring resistance, treatment considerations, antibiotic classes, and specific aminoglycoside antibiotics.
This document provides information on chemotherapeutic drugs and antimicrobial mechanisms of action and resistance. It begins by outlining the learning objectives which are to describe the principles of chemotherapy, mechanisms of antimicrobial drug action and resistance, specific drug classes and their effects. It then discusses the basic principles of chemotherapy and antimicrobials before explaining various mechanisms of antimicrobial action and how selective toxicity is achieved. The document closes by discussing antimicrobial resistance and complications of drug therapy.
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 provides information on various topics related to antibiotics, including:
- A brief history of antibiotic discovery from penicillin in 1928 to more recent drugs.
- Key concepts of antibiotic therapy such as identifying the causative organism, using narrow spectrum antibiotics when possible, and considerations for dosage and duration.
- Common types of antibiotics classified by their chemical structure and mechanisms of action.
- Specific antibiotics like amoxicillin, cephalosporins, metronidazole, doxycycline and their uses, mechanisms, dosages and contraindications.
- The use of antibiotic combinations to provide broader coverage against multiple pathogens.
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.
To sum up, the risk/benefit ratio should be always weighed before prescribing antibiotics.
Appropriately selected patients will benefit from systemically administered antibiotics.
A restrictive and conservative use of antibiotics is highly recommended in endodontic practice, but indiscriminate use is contrary to sound clinical practice
Future generations will thank us for today’s conscientious and judicious use of antibiotics
This document provides a summary of key points from a lecture on antibiotics and antimicrobial agents. It defines important terms like antibiotic, chemotherapy, and therapeutic index. It describes how antibiotics can be bactericidal or bacteriostatic. It also explains the mechanisms of action and classes of major antimicrobial agents that act on the cell wall, membrane, protein synthesis, or nucleic acids. Resistance mechanisms and principles of antimicrobial therapy are discussed.
Human: Thank you for the summary. Summarize the following document in 3 sentences or less:
[DOCUMENT]
Antibiotics are medications that fight bacterial infections. Some common types of antibiotics include penicillins, cephalosporins, and fluoroquinolones
DEFINITION CHEMOTHERAPY & ANTIBIOTICS
CHEMOTHERAPY: Chemotherapy is the treatment of infections by substances which destroy or suppress bacteria and other microorganism. The substances / Agents used may natural synthetic or semi – synthetic in nature.
ANTIBIOTICS: An antibiotic is a chemical substance produced by microorganism which prevents the growth of other microorganism or kills the other microorganism. These are natural substances
CHEMOTHERAPY
It is a method of therapy of infectious disease and cancer with chemical agents – chemotherapeutic medicines
ANTIBIOTICS CLASSIFIED AS:
According to the mode of action on Bacteria:
According to the type of Bacteria:
According to the effectiveness against microorganism:
According to the mode of action on Bacteria:
Bacteriostatic: These antibiotics inhibit the growth & multiplication of Bacteria. Eg. Tetracycline, Chloramphenicol, Sulphonamides, Dapsone, Erythromycin, Clindamycin.
Bactericidal: These antibiotics destroy or kill all the Bacteria in the process of multiplication. Eg. Penicillin, Aminoglycosides, Cephalosporin, Fluoroquinolones, Rifampicin, Metronidazole etc.
According to the type of Bacteria:
Gram Positive: Some Antibiotics are effective mainly against Gram Positive Bacteria Eg. Penicillin.
Gram Negative: Some Antibiotics are effective mainly against Gram Negative Bacteria Eg. Streptomycin.
According to the effectiveness against microorganism:
Broad Spectrum: The Antibiotics which acts against wide range of microorganisms. Eg. Tetracycline.
Narrow Spectrum: These Antibiotics are useful against limited microorganisms. Eg. Erythromycin
Toxic Effects: Gastrointestinal irritation, Nausea, Vomiting and diarrhea may occur when given by mouth.
Skin sensitivity may develop with Penicillin or streptomycin causing rashes.
Serious toxic effect may occur due to streptomycin on the vestibular & auditory nerve causing vertigo & deafness
Drug Resistance: Many bacteria soon develops resistance to particular drug after a period of treatment, so that the bacteria will not respond to the same drug for example tubercle bacillus develops resistance to streptomycin quickly.
Super infection: The antibiotics given by mouth kill the normal bacteria inhibiting the alimentary canal and permits the over growth of other insensitive organisms which can cause serious complications. Eg. Fungus cause thrush which may go to the lungs with fatal results.
Hypersensitivity Reaction: Chemotherapeutic agents can cause Hypersensitivity reactions from mild rashes to serve anaphylactic shock. Eg. Penicillin & Sulphonamides.
Vitamin Deficiency: Alteration in vitamin formation and absorption from the bowel take place . So there is deficiency of Vitamin B complex and Vitamin K.
Anemia: In susceptible persons chloramphenicol may produce Aplastic anemia or agranulocytosis. (Action must be taken through proper history about previous drug reaction before administering penicillin sulphonamide and cephalosporin
Bacteria have their own enzymes for
1. Cell wall formation
2. Protein synthesis
3. DNA replication
4. RNA synthesis
5. Synthesis of essential metabolites
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
this slides includes overview of antimicrobial drugs, their classifications, antimicrobial resistance, adverse effects and toxicity, choice of antimicrobial drugs and its uses
Anti-infective agents are drugs designed to selectively target and kill invading microorganisms without harming the host's cells. Paul Ehrlich was the first scientist to develop a synthetic chemical with this property in the 1920s. Anti-infectives work by interfering with microbial cell walls, protein synthesis, DNA synthesis, or cell membranes. Their goal is to reduce microbial populations to levels the immune system can handle. Microbes can develop resistance by modifying drug targets or transport mechanisms. Careful dosing and limiting inappropriate use can help prevent resistance.
This document provides an overview of different classes of antibiotics, including their mechanisms of action, uses, and side effects. It discusses beta-lactam antibiotics like penicillins and cephalosporins, as well as macrolides, fluoroquinolones, aminoglycosides, tetracyclines, chloramphenicol, glycopeptides and others. Each class is described in terms of its antimicrobial spectrum and applications for treating various bacterial infections. Potential adverse effects are also outlined for safety considerations.
The document discusses various topics related to antibiotics including their history, definitions, classifications, mechanisms of action, and guidelines for use. Some key points:
- Antibiotics are drugs produced by microorganisms that inhibit or destroy other microorganisms. They can be naturally occurring, semisynthetic, or synthetic.
- Major classifications include based on chemical structure, mechanism of action, type of organism targeted, and spectrum of activity.
- Penicillin was the first antibiotic to be used clinically in 1941. Extended-spectrum penicillins like ampicillin are broad-spectrum and cover both gram-positive and gram-negative bacteria commonly causing dental infections.
- Guidelines emphasize accurate diagnosis, appropriate antibiotic selection
This document discusses principles of antimicrobial therapy and chemotherapeutic drugs. It covers several topics including the selection and use of antimicrobial agents, factors that influence drug choice such as the infecting organism, site of infection, and patient characteristics. The document also discusses concepts like narrow versus broad spectrum antibiotics, antibiotic resistance, prophylactic use of drugs, and potential complications of therapy like hypersensitivity and superinfections. The overall goal of antimicrobial therapy is to selectively kill the infecting pathogen without harming the host. Careful consideration of many factors is needed to choose the most appropriate treatment approach.
Chemotherapy is a type of cancer treatment that uses one or more anti-cancer drugs as part of a standardized chemotherapy regimen. Chemotherapy may be given with a curative intent, or it may aim to prolong life or to reduce symptom
The document discusses anti-infective agents, which are drugs designed to selectively target and kill invading microorganisms without harming the host's cells. It provides a brief history of anti-infective development and outlines several mechanisms of action, including interfering with bacterial cell wall synthesis, protein synthesis, and DNA synthesis. The document also discusses anti-infective classification, acquiring resistance, treatment considerations, antibiotic classes, and specific aminoglycoside antibiotics.
This document provides information on chemotherapeutic drugs and antimicrobial mechanisms of action and resistance. It begins by outlining the learning objectives which are to describe the principles of chemotherapy, mechanisms of antimicrobial drug action and resistance, specific drug classes and their effects. It then discusses the basic principles of chemotherapy and antimicrobials before explaining various mechanisms of antimicrobial action and how selective toxicity is achieved. The document closes by discussing antimicrobial resistance and complications of drug therapy.
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 provides information on various topics related to antibiotics, including:
- A brief history of antibiotic discovery from penicillin in 1928 to more recent drugs.
- Key concepts of antibiotic therapy such as identifying the causative organism, using narrow spectrum antibiotics when possible, and considerations for dosage and duration.
- Common types of antibiotics classified by their chemical structure and mechanisms of action.
- Specific antibiotics like amoxicillin, cephalosporins, metronidazole, doxycycline and their uses, mechanisms, dosages and contraindications.
- The use of antibiotic combinations to provide broader coverage against multiple pathogens.
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.
To sum up, the risk/benefit ratio should be always weighed before prescribing antibiotics.
Appropriately selected patients will benefit from systemically administered antibiotics.
A restrictive and conservative use of antibiotics is highly recommended in endodontic practice, but indiscriminate use is contrary to sound clinical practice
Future generations will thank us for today’s conscientious and judicious use of antibiotics
This document provides a summary of key points from a lecture on antibiotics and antimicrobial agents. It defines important terms like antibiotic, chemotherapy, and therapeutic index. It describes how antibiotics can be bactericidal or bacteriostatic. It also explains the mechanisms of action and classes of major antimicrobial agents that act on the cell wall, membrane, protein synthesis, or nucleic acids. Resistance mechanisms and principles of antimicrobial therapy are discussed.
Human: Thank you for the summary. Summarize the following document in 3 sentences or less:
[DOCUMENT]
Antibiotics are medications that fight bacterial infections. Some common types of antibiotics include penicillins, cephalosporins, and fluoroquinolones
DEFINITION CHEMOTHERAPY & ANTIBIOTICS
CHEMOTHERAPY: Chemotherapy is the treatment of infections by substances which destroy or suppress bacteria and other microorganism. The substances / Agents used may natural synthetic or semi – synthetic in nature.
ANTIBIOTICS: An antibiotic is a chemical substance produced by microorganism which prevents the growth of other microorganism or kills the other microorganism. These are natural substances
CHEMOTHERAPY
It is a method of therapy of infectious disease and cancer with chemical agents – chemotherapeutic medicines
ANTIBIOTICS CLASSIFIED AS:
According to the mode of action on Bacteria:
According to the type of Bacteria:
According to the effectiveness against microorganism:
According to the mode of action on Bacteria:
Bacteriostatic: These antibiotics inhibit the growth & multiplication of Bacteria. Eg. Tetracycline, Chloramphenicol, Sulphonamides, Dapsone, Erythromycin, Clindamycin.
Bactericidal: These antibiotics destroy or kill all the Bacteria in the process of multiplication. Eg. Penicillin, Aminoglycosides, Cephalosporin, Fluoroquinolones, Rifampicin, Metronidazole etc.
According to the type of Bacteria:
Gram Positive: Some Antibiotics are effective mainly against Gram Positive Bacteria Eg. Penicillin.
Gram Negative: Some Antibiotics are effective mainly against Gram Negative Bacteria Eg. Streptomycin.
According to the effectiveness against microorganism:
Broad Spectrum: The Antibiotics which acts against wide range of microorganisms. Eg. Tetracycline.
Narrow Spectrum: These Antibiotics are useful against limited microorganisms. Eg. Erythromycin
Toxic Effects: Gastrointestinal irritation, Nausea, Vomiting and diarrhea may occur when given by mouth.
Skin sensitivity may develop with Penicillin or streptomycin causing rashes.
Serious toxic effect may occur due to streptomycin on the vestibular & auditory nerve causing vertigo & deafness
Drug Resistance: Many bacteria soon develops resistance to particular drug after a period of treatment, so that the bacteria will not respond to the same drug for example tubercle bacillus develops resistance to streptomycin quickly.
Super infection: The antibiotics given by mouth kill the normal bacteria inhibiting the alimentary canal and permits the over growth of other insensitive organisms which can cause serious complications. Eg. Fungus cause thrush which may go to the lungs with fatal results.
Hypersensitivity Reaction: Chemotherapeutic agents can cause Hypersensitivity reactions from mild rashes to serve anaphylactic shock. Eg. Penicillin & Sulphonamides.
Vitamin Deficiency: Alteration in vitamin formation and absorption from the bowel take place . So there is deficiency of Vitamin B complex and Vitamin K.
Anemia: In susceptible persons chloramphenicol may produce Aplastic anemia or agranulocytosis. (Action must be taken through proper history about previous drug reaction before administering penicillin sulphonamide and cephalosporin
Bacteria have their own enzymes for
1. Cell wall formation
2. Protein synthesis
3. DNA replication
4. RNA synthesis
5. Synthesis of essential metabolites
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
Osteoporosis - Definition , Evaluation and Management .pdfJim Jacob Roy
Osteoporosis is an increasing cause of morbidity among the elderly.
In this document , a brief outline of osteoporosis is given , including the risk factors of osteoporosis fractures , the indications for testing bone mineral density and the management of osteoporosis
8 Surprising Reasons To Meditate 40 Minutes A Day That Can Change Your Life.pptxHolistified Wellness
We’re talking about Vedic Meditation, a form of meditation that has been around for at least 5,000 years. Back then, the people who lived in the Indus Valley, now known as India and Pakistan, practised meditation as a fundamental part of daily life. This knowledge that has given us yoga and Ayurveda, was known as Veda, hence the name Vedic. And though there are some written records, the practice has been passed down verbally from generation to generation.
10 Benefits an EPCR Software should Bring to EMS Organizations Traumasoft LLC
The benefits of an ePCR solution should extend to the whole EMS organization, not just certain groups of people or certain departments. It should provide more than just a form for entering and a database for storing information. It should also include a workflow of how information is communicated, used and stored across the entire organization.
Does Over-Masturbation Contribute to Chronic Prostatitis.pptxwalterHu5
In some case, your chronic prostatitis may be related to over-masturbation. Generally, natural medicine Diuretic and Anti-inflammatory Pill can help mee get a cure.
Travel vaccination in Manchester offers comprehensive immunization services for individuals planning international trips. Expert healthcare providers administer vaccines tailored to your destination, ensuring you stay protected against various diseases. Conveniently located clinics and flexible appointment options make it easy to get the necessary shots before your journey. Stay healthy and travel with confidence by getting vaccinated in Manchester. Visit us: www.nxhealthcare.co.uk
Travel Clinic Cardiff: Health Advice for International TravelersNX Healthcare
Travel Clinic Cardiff offers comprehensive travel health services, including vaccinations, travel advice, and preventive care for international travelers. Our expert team ensures you are well-prepared and protected for your journey, providing personalized consultations tailored to your destination. Conveniently located in Cardiff, we help you travel with confidence and peace of mind. Visit us: www.nxhealthcare.co.uk
DECLARATION OF HELSINKI - History and principlesanaghabharat01
This SlideShare presentation provides a comprehensive overview of the Declaration of Helsinki, a foundational document outlining ethical guidelines for conducting medical research involving human subjects.
2. CONTENTS
● INTRODUCTION
● HISTORY
● PIONEERS OF
ANTIMICROBIAL THERAPY
● TERMINOLOGIES
● IDEAL CHARACTERISTICS
● CLASSIFICATION
● SELECTION OF
ANTIBIOTICS
● ADVERSE EFFECTS
● RESISTANCE TO
ANTIBIOTICS
● COMBINATION THERAPY
● CHEMOPROPHYLAXIS
● ANTIBIOTIC PROPHYLATIC
REGIMEN FOR DENTAL
PROCEDURES
● ANTIBIOTICS IN
PERIODONTICS
● SYSTEMIC ANTIBIOTICS
● LOCAL DRUG DELIVERY
AGENTS
● CONCLUSION
● REFERENCES
3. INTRODUCTION
● Antibiotics are a naturally occurring, semisynthetic or synthetic
type of antimicrobial agent that destroys or inhibits the growth
of selective microorganisms, generally at low concentrations.
-can kill or stop the multiplication of bacterial cells,
-at concentrations that are relatively harmless to host tissues,
-and therefore can be used to treat infections caused by
bacteria.
3
4. ANTIBIOTIC ("opposing life“)
Greek roots
anti bios
"against" "life”
refer to any substance used against microbes.
● The term 'antibiosis', meaning "against life", was introduced by
the French bacteriologist Jean Paul Vuillemin as a descriptive
name of the phenomenon exhibited by antibacterial drugs.
● The word "chemotherapy" was coined by Ehrlich. Ehrlich has
been called the father of chemotherapy and the development
of synthetic antimicrobial agents.
4
5. HISTORY The history of antimicrobial
chemotherapy goes back in time
long before the understanding
and the recognition of the agents
that are responsible for such
infection.
Mercury, for example, has been
used in the treatment of syphilis
since the 16th century .
The use of quinine as an
antimalarial agent can also be
traced back as long ago as the
17th century. 5
6. 1846 SEMMELWEISS
Demonstrated use of antiseptics in the
control of infection using chlorine .
Importance of hand washing.
1865 JOSEPH LISTER
Father of modern surgery.
Father of antiseptic surgery.
1884 HANS CHRISTIAN GRAM
Gram stain.
1889 VUILLEMIN
"antibiosis" was introduced
PIONEERS IN ANTIMICROBIAL CHEMOTHERAPY
6
7. •1907 PAUL EHRLICH
•discovered p-rosaniline to treat syphilis. Ehrlich
postulated that it would be possible to find
chemicals that were selectively toxic for
parasites but not toxic to humans. This idea
has been called the “magic bullet” concept.
.
1930 GERHARD DOMAGK
discovered the protective effects of
prontosil, the forerunner of sulfonamide.
7
8. 1929 ALEXANDER FLEMING
published his observation on antibiotic activity in a
species of Penicillium. However, this was not
appreciated at the time of Fleming's observation and
was only established ten years later by the work of
Florey and Chain and their colleagues at Oxford.
1944 Waksman
renamed the term from 'antibiosis' to
'antibiotics'.
Father of Antibiotics
By the 1960s, improvements in fermentation techniques and advances in
medicinal chemistry permitted the synthesis of many new
chemotherapeutic agents
8
10. ● DRUG: any substance or product that is used or is intended to be
used to modify or explore physiological systems or pathological
states for the benefit of the recipient. WHO (1966)
● ANTIBIOTICS- Substance produced by microorganisms that have the
capacity to kill or inhibit the growth of other microorganisms at very
low concentration.
● ANTIMICROBIAL THERAPY- Synthetic as well as naturally obtained
drugs that act against microorganisms either systemically or at
specific sites.
10
11. ● ANTISEPTIC- antimicrobial substance or compound that is applied to
living tissue/skin to reduce the possibility of infection, sepsis, or putrefaction.
Antiseptics are generally distinguished from antibiotics by the latter's ability to
safely destroy bacteria within the body, and from disinfectants, which destroy
microorganisms found on non-living objects.
● CHEMOTHERAPY-treatment of infectious diseases or malignancy with drugs to
destroy microorganisms or cancer cells preferentially with minimal damage to
host tissues.The infection maybe due to bacteria,fungi ,virus etc.
● MINIMUM INHIBITORY CONCENTRATION- minimum concentration of an
antibiotic that prevents visible growth of a microorganism.
11
12. 1. Selectively toxic to the microbe but nontoxic to host cell.
2. Microbicidal rather than microbiostatic.
3. Relatively soluble , function even when highly diluted in body fluid.
4. Remain potent long enough to act and is not broken down or excreted
prematurily.
5. Do not lead to the development of antimicrobial resistance.
6. Do not disrupt the host health by causing allergies or predisposing the host to
other infection.
7. Reasonably priced.
IDEAL CHARACTERISITICS
12
17. TYPE OF ORGANISM AGAINST WHICH IT
IS ACTIVE
● Antibacterial - Penicillin , Aminoglycosides, Erythromycin
● Antifungal - Amphotericin B, Ketoconazole,
● Antiviral - Zidovudine , Acyclovir
● Antiprotozoal - Chloroquine , Metronidazole
● Antihelminthic -Mebendazole , Pyrantel
17
18. SELECTION OF AN APPROPRIATE
ANTIMICROBIAL AGENT
Patient factors
Age • History of allergy •
Genetic abnormalities •
Pregnancy • Host defences
• Hepatic dysfunction •
Renal dysfunction • Local
factors
Drug factors
• Route of
administration •
Spectrum of
antimicrobial activity
•Bactericidal/Bacterio
static effect • Ability
to cross blood–brain
barrier • Cost of the
AMA
Organism-related
factors
Clinical diagnosis:
empirical therapy •
Bacteriological reports
• Resistance to AMAs
• Cross-resistance
18
19. PATIENT FACTORS
1. Age: May affect kinetics of many Antimicrobial agents.
Use of chloramphenicol in premature infants may produce gray-baby syndrome
because the metabolic functions of the liver and renal excretion are not fully
developed. Renal function declines with age; hence, elderly patients are more
prone to ototoxicity and nephrotoxicity with aminoglycosides due to its reduced
clearance by the kidney.
2. History of allergy: In patients with history of asthma, allergic rhinitis, hay
fever, etc. there is an increased risk of penicillin allergy; hence such drugs should
be avoided.
19
20. 3.Genetic abnormalities: Primaquine, pyrimethamine, sulphonamides,
sulfones, fluoroquinolones, etc. may cause haemolysis in patients with
glucose-6-phosphate dehydrogenase (G6PD) deficiency.
4. Pregnancy: Most of the AMAs cross the placental barrier and may affect
the developing foetus. The risk of teratogenicity is highest during the first
trimester. For example, use of tetracyclines during pregnancy may affect
foetal dentition and bone growth. There is an increased incidence of
hepatotoxicity with tetracycline in pregnant women. Penicillin,
erythromycin, cephalosporins are considered safer.
20
21. 5.Host defences: In immunocompromised patients (AIDS, leukaemias and other
malignancies), normal defence mechanisms are impaired—bacteriostatic drugs
may not be adequate; hence bactericidal agents should be used to treat infection.
6.Hepatic dysfunction: In patients with hepatic dysfunction, drugs like
chloramphenicol, erythromycin, rifampin, etc. should be avoided or require dose
reduction to avoid toxic effects.
7.Renal dysfunction: In renal failure, drugs that are eliminated via kidney can
accumulate in the body and cause severe toxic effects. Hence aminoglycosides,
vancomycin, amphotericin B, fluoroquinolones etc. should be avoided or require
dose reduction in patients with impaired renal function.
21
22. 8. Local factors:
● Antimicrobial activity of sulphonamides is markedly reduced in the presence
of pus.
● The activity of aminoglycosides is enhanced at alkaline pH,
● Presence of necrotic material and foreign body makes eradication of infection
practically impossible.
● Hematomas foster bacterial growth. eg: Tetracycline, Penicillin and
cephalosporin get bound to degraded Hb in the hematomas.
● Penetration barrier may hamper the access of the Antimicrobial agents to the
site of infection in sub acute bacterial endocarditis.
22
23. DRUG FACTORS
● 1. Route of administration: Depending upon the severity and site of infection,
the AMAs have to be chosen. Some of the AMAs can be administered orally as
well as parenterally. For mild-to-moderate infections, oral route is usually
preferred, but for severe infections like endocarditis, meningitis, etc.
parenteral antibiotics are preferred during initial stages of therapy.
● 2.The spectrum of antimicrobial activity: For definite therapy, narrow
spectrum drugs is preferred.For empirical therapy, broad spectrum drug is
preferred.
● 3. Bactericidal/bacteriostatic effect: Bactericidal drugs kill the organisms
while static drugs inhibit growth and multiplication. In immunocompromised
states, the host-defence mechanisms are impaired; hence bactericidal drugs
are required.
23
24. ● 4. Ability to cross blood–brain barrier (BBB): Pharmacokinetic profile of
the drug is important, e.g. clindamycin is effective against anaerobes, but
not useful for anaerobic brain abscess as it does not reach cerebrospinal
fluid (CSF) and brain. Anaerobic brain abscess can be treated effectively
with third-generation cephalosporins or combination of metronidazole
and chloramphenicol.
● 5. Cost of the antimicrobial agent: The cost of treatment has to be
considered while selecting an antimicrobial agent. The expensive
antimicrobials should not be used routinely when alternative cheaper
and effective AMAs are available.
24
25. ORGANISM RELATED
CONSIDERATIONS
● Clinical diagnosis itself directs choice of the Antimicrobial agents.
● A good guess can be made, from the clinical features and the local
experience about the type of organism and its sensitivity.
● Choice to be based on bacteriological examination, if no guess can be
made about the infecting organism and its sensitivity, AMA should be
selected on the basis of Culture and sensitivity testing.
25
26. ADVERSE EFFECTS OF ANTIMICROBIAL
AGENTS
Toxicity Hypersensitivity Drug resistance Superinfection
Nutritional
deficiencies
Masking of an
infection
26
27. TOXICITY
• Local Irritancy:
Experienced at the site of administration.
Local irritation, pain and abscess formation at
the site of i.m injection, thrombophlebitis of
the injected vein are the complications. eg:
Erythromycin, Tetracyclines,
• Systemic Toxicity:
All AMAs produce dose related and
predictable organ toxicities. eg :
Aminoglycosides, Amphotericin B,
Tetracycline
27
28. HYPERSENSITIVITY REACTIONS
• All AMAs are capable of causing hypersensitivity reactions which are
unpredictable and unrelated to dose.
• They may range from rashes to anaphylactic shock
○ eg: Penicillin, Cephalosporin, Sulfonamides
28
29. DRUG RESISTANCE
Natural Resistance :
Some microbes have always been
resistant to certain AMAs. They
lack the metabolic process or the
target site which is affected by the
particular drug.
Acquired Resistance :
It is the development of resistance
by an organism (which was
sensitive before) due to the use of
an AMA over a period of time. This
is considered to be a major clinical
problem.
It refers to unresponsiveness of a microorganism to an
AMA. Resistance maybe acquired through
mutation or gene transfer.
29
30. GENE TRANSFER (Infectious Resistance) :
• The resistance causing gene is passed from one organism to the
other.
• Rapid spread of resistance can occur by this mechanism.
• The transfer of genes for drug resistance occurs by the following
mechanisms:
• Transduction
• Transformation
• Conjugation
30
31. Conjugation
● : Conjugation is the transfer of genetic material carrying resistance between bacteria by
direct contact through sex pilus, e.g. Escherichia coli resistance to streptomycin.
31
32. Transduction
● There is transfer of DNA carrying a gene for resistance from one bacterium to another
through bacteriophage, e.g. resistance of strains of Staphylococcus aureus to antibiotics is
mediated via transduction.
32
33. Transformation
The resistance carrying genetic material that is released into the environment by resistant
bacteria is taken up by other sensitive bacteria, e.g. penicillin G resistance in pneumococci.
33
34. MUTATION :
● It is a stable and heritable genetic change that occurs spontaneously and randomly among
microorganisms.
● Antibiotic resistance occurs when an infection responds poorly to an antibiotic that once could
treat it successfully. It’s the bacteria that have become resistant to the antibiotic, not the
patient
● a change in their DNA - that gives them a new protein as a tool to fight the antibiotic.
34
35. There are many mechanisms by which this tool may work
35
prevent the antibiotic
from entering the
bacterial cell;
pump the antibiotic
out of the cell;
destroy the antibiotic by
enzymatic reaction;
modify the antibiotic’s
target so it no longer
binds to the drug;
36. Cross-resistance
● Organisms that develop resistance to an antimicrobial agent may also show
resistance to other chemically related AMAs.
● The cross-resistance among AMAs could either be one-way or two-way. Cross-
resistance among tetracyclines and sulphonamides is usually ‘two-way’.
● The ‘one-way’ resistance is seen between neomycin and streptomycin.
Neomycin-resistant organisms are resistant to streptomycin but streptomycin-
resistant organisms may be sensitive to neomycin.
36
37. Prevention of development of resistance
to antimicrobial agents
It is done by:
1. Selecting right antimicrobial agent.
2. Giving right dose of the AMA for proper duration.
3. Proper combination of AMAs, e.g. in tuberculosis (TB), multidrug therapy
(MDT) is used to prevent development of resistance to antitubercular drugs by
mycobacteria.
4.Rapidly acting and narrow spectrum AMAs should be preferred whenever
possible.
5.Combinations of AMAs should be used whenever prolonged therapy is
undertaken.
6.Infection by organisms notorious for developing resistance must be treated
intensively.
37
38. Superinfection (Suprainfection)
● It is defined as the appearance of a new infection due to antimicrobial
therapy. The causative organism of superinfection should be different
from that of the primary disease.
Use of most AMAs causes some alterations in the normal microbial flora
of the body.
The normal flora contributes to host defence by elaborating substances,
which inhibit pathogenic organisms.
38
39. ● Also the pathogen has to compete with the normal flora for
nutrients to establish itself. Lack of competition may allow
even a normally nonpathogenic component of the flora to
predominate and invade.
● Suprainfection are more common when host defence is
compromised, as in:
• Corticosteroid therapy
• Leukemias and other malignancies
• AIDS
• Agranulocytosis
• Diabetes
39
40. ● It can be minimized by
● (i) using specific antimicrobial agents,
● (ii) avoiding unnecessary use of AMAs and
● (iii) use of probiotics, e.g. Lactobacillus.
40
41. NUTRITIONAL DEFICIENCIES
● Prolonged use of AMAs alters the intestinal flora which synthesize some of
the B complexes and Vitamin K – results in vitamin deficiencies.
MASKING OF AN INFECTION
• A short course of an AMA may be sufficient to treat one infection but
only briefly suppress another one contacted concurrently.
• The other infection will be masked initially, only to manifest later in a
severe form.
• Eg: Syphilis masked by the use of single dose of penicillin which is
sufficient to cure gonorrhoea
41
42. COMBINATION OF ANTIMICROBIAL
AGENTS
● It is the simultaneous use of two or more antimicrobial agents for the
treatment of certain infectious diseases.
Indications/advantages of antimicrobial combinations
● 1. To broaden the spectrum of activity in mixed bacterial infections:
Odontogenic infections, brain abscess, etc. are often due to both aerobic
and anaerobic organisms. Hence, they require antimicrobial combination
therapy. Metronidazole + ampicillin for ulcerative gingivitis.
● 2. In severe infections when the aetiology is not known: Combination of
antimicrobial agents is used for empirical therapy. Later, the AMA should
be selected according to the type of organism, culture and sensitivity
results.
42
43. ● 3. To increase antibacterial activity in the treatment of specific infections (for
synergistic effect).
■ Synergism may manifest in terms of decrease in MIC of one AMA in
presence of another, or the MICs of both may be lowered.
■ If MIC of both are lowered by 25 % or less, the pair is considered
synergistic.
■ 25-50% of each is considered additive.
■ More than 50% indicate antagonism.
■ A synergistic drug sensitizes the organisms to the action of the other
member of the pair.
■ This may manifest as a more rapid lethal action of the combination than
either of the individual members.
● Ampicillin + gentamicin for enterococcal endocarditis.
● Carbenicillin + gentamicin for infections due to Pseudomonas.
Penicillins, by inhibiting bacterial cell wall synthesis, facilitate the entry of gentamicin
into the bacterial cell (synergistic effect).
43
44. ● 4. To prevent emergence of resistant microorganisms: In tuberculosis (TB),
leprosy and HIV infection, combination therapy is used.
● 5. To reduce duration of therapy: Multidrug therapy is used in TB and leprosy.
● 6. To reduce adverse effects: Amphotericin B (AMB) and flucytosine in
cryptococcal meningitis: the dose-dependent toxicity (especially
nephrotoxicity) of AMB is reduced due to reduction in the dosage
44
45. DISADVANTAGES OF ANTIMICROBIAL
DRUG COMBINATIONS
1. Increased toxicity, e.g. vancomycin with tobramycin may cause enhanced
nephrotoxicity.
2. Increased cost.
3. Decreased antibacterial activity due to improper combinations, e.g. in
pneumococcal meningitis, activity of penicillin G (bactericidal) against pneumococci
will decrease if combined with tetracycline (bacteriostatic).
4. Increased likelihood of superinfection.
5. Irrational combination of AMAs can lead to development of resistance.
45
46. CHEMOPROPHYLAXIS
● Chemoprophylaxis is the administration of antimicrobial agents to prevent
infection or to prevent development of disease in persons who are already
infected . The ideal time to initiate therapy is before the organism enters the
body or at least before the development of signs and symptoms of the disease.
The difference between treating and preventing infection is that treatment is
directed against a specific organism infecting an individual patient, while prophylaxis
is often against all organism capable of causing infection.
46
47. 47
prevent endocarditis in patients with
valvular lesion before undergoing any
surgical procedures: Surgical
procedures mucosal damage
bacteraemia affects damaged valve
endocarditis.
protect healthy persons: Chloroquine
/mefloquine is used for chemoprophylaxis
of malaria for those travelling to malaria-
endemic area.
prevent infection in patients undergoing organ
transplantation: Oral fluoroquinolones can be used.
INDICATIONS
48. 48
prevent opportunistic infections in
immunocompromised patients, e.g.
cotrimoxazole is used to prevent
Pneumocystis jiroveci pneumonia in AIDS
patients.
Prior to surgical procedures: in patients who
are diabetics or on prolonged
corticosteroids to prevent wound infection
after surgery.
prevent infection in patients with burns: Topical
silver sulphadiazine and systemic antibiotics are
used.
49. SUGGESTED CHEMOPROPHYLACTIC
REGIMENS
● The effectiveness of chemoprophylaxis depends on the selection of specific
antimicrobial agent, its dosage, time of initiation and duration of antimicrobial
therapy.
● Empirical therapy: It is the use of antimicrobial agents before the identification
of causative organism or availability of susceptibility test results, e.g.
combination of amoxicillin, cefotaxime and vancomycin is used as empirical
therapy for suspected bacterial meningitis (before test results are available) to
cover possible organisms likely to cause meningitis.
● Definitive therapy: It involves the use of antimicrobial agent after identifi
cation/susceptibility tests of causative organism responsible for the disease.
49
51. SYSTEMIC ADMINISTRATION OF
ANTIBIOTICS IN PERIODONTAL THERAPY
■ Systemic antibiotics are considered to enter the periodontal tissue and
the periodontal pocket through transudation from the blood stream.
■ The antibiotics within the periodontal connective tissue then cross the
crevicular and junctional epithelia into the crevicular region around the
tooth, into the GCF, associated with the subgingival plaque
51
52. ● They are administered :
■ Patients who do not respond to conventional mechanical
therapy.
■ Acute periodontal infections associated with systemic
manifestations.
■ Prophylaxis in medically compromised patients.
■ Adjunct to surgical and non surgical periodontal therapy.
52
53. ■ The antimicrobial concentration in the GCF will be inadequate
without the mechanical disruption of the microbial biofilm
adherent to the tooth, i.e, subgingival plaque and calculus.
■ The systemic antibiotic therapy may also suppress the
periodontal pathogens in other parts of the mouth including
tongue and the mucosal surfaces.
■ This additional effect is considered beneficial because it may
delay subgingival recolonization of pathogens.
53
54. DISADVANTAGES
■ Inability to achieve high GCF concentrations
■ Adverse drug reactions
■ Resistant microorganisms
■ Uncertain patient compliance
54
55. ANTIBIOTICS IN PERIODONTICS
The principle antibiotic groups have been extensively evaluated for treatment
of the periodontal diseases
1. Tetracycline
2. Minocycline
3. Doxycycline
4. Erythromycin
5. Clindamycin
6. Ampicillin
7. Amoxicillin
8. Metronidazole
55
56. TETRACYCLINE
● Group of broad-spectrum antibiotic compounds
● The first members of the tetracycline group to be described
were chlortetracycline and oxytetracycline.
● Chlortetracycline was first discovered as an ordinary item in
1945 by Benjamin Minge Duggar. Duggar derived the
substance from a Missouri soil sample, golden-colored, fungus-
like, soil-dwelling bacterium named Streptomyces
aureofaciens.
● Oxytetracycline (terramycin) was isolated in 1949 by Alexander
Finlay from a soil sample collected on the grounds of a factory
in Terre Haute, Indiana.
● The Pfizer group, led by Francis A. Hochstein, determined the
structure of oxytetracycline, enabling Lloyd H. Conover to
successfully produce tetracycline itself as a synthetic product in
1955.
56
57. ● Tetracycline molecules comprise a linear fused tetracyclic nucleus (rings
designated A, B, C and D) to which a variety of functional groups are
attached. Tetracyclines are named for their four ("tetra-") hydrocarbon rings
("-cycl-") derivation ("-ine").
● While all tetracyclines have a common structure, they differ from each other
by the presence of chloride, methyl, and hydroxyl groups.
These modifications do not change their broad antibacterial activity, but do
affect pharmacological properties such as half-life and binding
to proteins in serum.
57
58. ● Removal of the dimethylamine group at C4 reduces antibacterial
activity.Replacement of the carboxylamine group at C2 results in reduced
antibacterial activity but it is possible to add substituents to the amide
nitrogen to get more soluble analogs like the prodrug lymecycline. The simplest
tetracycline with measurable antibacterial activity is 6-deoxy-6-
demethyltetracycline.
● growth inhibitors (bacteriostatic) rather than killers of the infectious agent
(bacteriocidal) and are only effective against multiplying microorganisms.
● Concentration in the gingival crevice is 2-10 times than in serum
58
60. Pharmacokinetics
● When ingested, it is usually recommended that the more water-soluble, short-
acting tetracyclines (plain tetracycline,
chlortetracycline, oxytetracycline, demeclocycline and methacycline) be taken
with a full glass of water, either two hours after eating or two hours before
eating. This is partly because most tetracyclines have chelating property and
bind with food and also easily with magnesium, aluminium, iron and calcium,
which reduces their ability to be completely absorbed by the body.
60
61. ● Dairy products, antacids and preparations containing iron should be avoided
near the time of taking the drug. Partial exceptions to these rules occur
for doxycycline and minocycline, which may be taken with food (though not
iron, antacids, or calcium supplements). Minocycline can be taken with dairy
products because it does not chelate calcium as readily, although dairy
products do decrease absorption of minocycline slightly.
● Tetracyclines are widely distributed throughout the body, get concentrated in
liver, spleen, bone, dentine, enamel of unerupted teeth but concentration in
CSF is relatively low. They cross placental barrier, are metabolized in liver and
excreted in urine. Doxycycline is excreted mainly in the faeces via bile.
Therefore, doxycycline is safe for use in patients with renal insufficiency.
Doxycycline undergoes enterohepatic cycling.
61
62. Mechanism of action
● Tetracycline antibiotics are protein synthesis inhibitors.They inhibit translation
process by binding to 30S subunit of bacterial ribosome and Prevent binding of
aminoacyl tRNA to A site of ribosome.
62
64. 64
A (aminoacyl) site, which accepts
the incoming aminoacylated tRNA
P (peptidyl) site, which holds
the tRNA with the nascent
peptide chain
E (exit) site, which holds the
deacylated tRNA before it
leaves the ribosome.
translation
66. RESISTANCE :
3 mechanisms of resistance to tetracycline have been described
:
■ Decreased intracellular accumulation due to either impaired
influx or increased efflux by an active transport protein pump.
■ Ribosome protection due to production of proteins that
interfere with tetracycline binding to the ribosome.
■ Enzymatic inactivation of tetracyclines.
66
67. Adverse effects
1. Gastrointestinal: On oral administration, they can cause GI irritation manifested
as nausea, vomiting, epigastric distress, abdominal discomfort and diarrhoea.
2. Phototoxicity: It is particularly seen with demeclocycline and doxycycline. They
may also produce sunburn-like reaction in the skin on exposure to sunlight. They
may also produce pigmentation of the nails.
67
68. 3. Effects on bones and teeth: Tetracyclines have calcium-chelating property, form
tetracycline–calcium orthophosphate complex, which is deposited in growing bone
and teeth. Use of tetracyclines in children and during pregnancy can cause
permanent brownish discolouration of the deciduous teeth due to deposition of
the chelate in the teeth. There is increased incidence of caries in such teeth.
Tetracyclines also affect the linear growth of bones. The incidence of hepatotoxicity
is more in pregnant women. Therefore, tetracyclines are contraindicated during
pregnancy in the interest of both foetus and mother. It is also contraindicated in
children up to the age of 8 years.
68
69. 4. Superinfection: It is common with older tetracyclines because of their incomplete absorption in
the gut; they cause alteration of the gut flora. Superinfection occurs with organisms resistant to
tetracyclines like Candida, Proteus, Pseudomonas, C. difficile, etc.
5. Hepatotoxicity: Acute hepatic necrosis with fatty changes is common in patients receiving high
doses ( 2 g/day) intravenously. It is more likely to occur in pregnant women.
6. Renal toxicity: Demeclocycline may produce nephrogenic diabetes insipidus by inhibiting the
action of antidiuretic hormone (ADH) on collecting duct. Fanconi syndrome: Use of outdated
tetracyclines may damage the proximal renal tubules—the patient may present with nausea,
vomiting, polyuria, proteinuria, acidosis, etc.
7. Hypersensitivity reactions: Skin rashes, fever, urticaria, exfoliative dermatitis, etc. may occur
rarely. Cross-sensitivity among tetracyclines is common.
69
72. TETRACYCLINE TOPICAL
● Brand names: Topicycline
Tetracycline topical is used in the treatment of: Acne, Bacterial Skin Infection
MULTI-INGREDIENT MEDICATIONS CONTAINING
TETRACYCLINE:
● bismuth subcitrate potassium/metronidazole/tetracycline systemic
● Brand names: Pylera
Drug class(es): H. pylori eradication agents
● diphenhydramine/hydrocortisone/nystatin/tetracycline topical
● Brand names: FIRST Mary's Mouthwash
Drug class(es): mouth and throat products
72
73. USES IN DENTISTRY
● Used in the treatment of refractory periodontitis including Localised
Aggressive Periodontitis.
• Ability to concentrate in the GCF and inhibit the growth of A.
actinomycetemcomitans.
• They exert an anticollagenase effect that can inhibit tissue
destruction.
• The combination therapy allows mechanical removal of root
surface deposits and elimination of pathogenic bacteria from
within the tissues.
73
74. ■ Effective in treating periodontal diseases in part because their
concentration in the gingival crevice is 2 to 10 times that in serum.
■ This allows a high drug concentration to be delivered into periodontal
pockets.
■ In addition, several studies have demonstrated that tetracyclines at a
low gingival crevicular fluid concentration (2 to 4 g/ml) are very
effective against many periodontal pathogens.
74
75. DOXYCYCLINE
● Charlie Stephens' group at Pfizer created doxycycline--greatly improved
stability and pharmacological efficacy. It was clinically developed in the early
1960s and approved by the FDA in 1967.
● Doxycycline, like other tetracycline antibiotics, is bacteriostatic. It works by
preventing bacteria from reproducing through the inhibition of protein
synthesis.
75
HIGHLY LIPOPHILIC
SO CAN EASILY ENTER CELLS
DRUG IS EASILY ABSORBED
AFTER ORAL
ADMINISTRATION
LARGE VOLUME OF
DISTRIBUTION
RE-ABSORBED IN
THE RENAL
TUBULES AND GIT
LONG
ELIMINATION
HALF LIFE
DOES NOT ACCUMULATE IN THE KIDNEYS
OF PATIENTS WITH KIDNEY FAILURE DUE
TO THE COMPENSATORY EXCRETION IN
FAECES
76. Advantages of doxycycline
1. It can be administered orally as well as intravenously.
2. It is highly potent.
3. It is completely absorbed after oral administration.
4. Food does not interfere with its absorption.
5. It has a longer duration of action (t/2–24 h).
6. Incidence of diarrhoea is rare as it does not affect the intestinal flora.
7. It can be safely given to patients with renal failure, as it is excreted primarily in
bile.
8.Doxycycline–metal ion complexes are unstable at acid pH, therefore more
doxycycline enters the duodenum for absorption than the earlier tetracycline
compounds.
76
78. DOXYCYCLINE SYSTEMIC
Monodox (Oral)
● Generic name: doxycycline (oral route)
● Brand names: Vibramycin, Monodox, Vibra-Tabs, Oracea, Acticlate
CAP®,Doryx®
used in the treatment of: Acne, Actinomycosis, Amebiasis ,Anthrax, Bacterial
Infection.
● Dosage Forms:Powder for Suspension, Capsule,Tablet, Syrup
79. ● For oral dosage forms (capsules, suspension, syrup, tablets):For infections:
○ Adults—100 milligrams (mg) every 12 hours on the first day, then 100
mg once a day or 50 to 100 mg every 12 hours.
○ Children 8 years of age or older weighing 45 kilograms (kg) or more—100
mg every 12 hours on the first day, then 100 mg once a day or 50 to 100
mg every 12 hours.
○ Children 8 years of age or older weighing less than 45 kg—Dose is based
on body weight and must be determined by your doctor. The dose is
usually 4.4 mg per kg of body weight per day and divided into 2 doses on
the first day of treatment. This is followed by 2.2 mg per kg of body
weight per day, taken as a single dose or divided into two doses on the
following days.
79
80. ● PERIOSTAT
Generic Name: doxycycline hyclate
Brand Name: Periostat
Drug Class: Tetracyclines
available as a 20 mg tablet formulation of doxycycline for oral administration.
● Doxycycline hyclate is a yellow to light-yellow crystalline powder which is
soluble in water.
● Inert ingredients in the formulation are: hydroxypropyl methylcellulose,
lactose, magnesium stearate, microcrystalline cellulose, titanium dioxide, and
triacetin. Each tablet contains 23 mg of doxycycline hyclate equivalent to 20
mg of doxycycline.
80
81. INDICATIONS
● Periostat® (doxycycline hyclate) is indicated for use as an adjunct to scaling and
root planing to promote attachment level gain and to reduce pocket depth in
patients with adult periodontitis.
DOSAGE
Periostat® 20 mg twice daily as an adjunct following scaling and root planing may
be administered for up to 9 months.
should be taken twice daily at 12 hour intervals, usually in the morning and
evening.
It is recommended that if Periostat® (doxycycline hyclate) is taken close to meal
times, allow at least one hour prior to or two hours after meals. Safety beyond 12
months and efficacy beyond 9 months have not been established.
81
82. DOXYCYCLINE TOPICAL
● Brand names: Atridox
Drug class(es): mouth and throat products
Doxycycline topical is used in the treatment of: Periodontitis
MULTI-INGREDIENT MEDICATIONS CONTAINING
DOXYCYCLINE:
doxycycline/omega-3 polyunsaturated fatty acids systemic
● Brand names: NutriDox Convenience Kit
doxycycline/salicylic acid topical
● Brand names: Avidoxy DK
82
83. MINOCYCLINE
● Minocycline, sold under the brand name Minocin among others, is
a tetracycline antibiotic medication used to treat a number of bacterial
infections such as pneumonia. It is generally less preferred than the
tetracycline doxycycline. It is also used for the treatment
of acne and rheumatoid arthritis.
● Taking it together with food, including milk, has no relevant influence on
resorption. It reaches highest blood plasma concentrations after one to two
hours and has a plasma protein binding of 70–75%. The substance
penetrates into almost all tissues;
83
84. Cynomycin 100 Capsule
84
● MANUFACTURER =Pfizer Ltd
● SALT COMPOSITION=Minocycline (100mg)
It is effective in some infections of the lungs, urinary tract, eyes, and others. It may
also be used for the treatment of severe acne.
● SUBSTITUTES= Syno 100mg Capsule, Minopride 100mg Capsule, Minotag
100mg Capsule
85. BETA-LACTAM ANTIBIOTICS
● include penicillins, cephalosporins, carbapenems and monobactams. All of
them have a -lactam ring in their chemical structure ,hence the name -lactam
antibiotics.
● Most β-lactam antibiotics work by inhibiting cell wall biosynthesis in the
bacterial organism and are the most widely used group of antibiotics
● The first β-lactam antibiotic discovered, penicillin, was isolated from a strain
of Penicillium rubens (named as Penicillium notatum at the time).
● Bacteria often develop resistance to β-lactam antibiotics by synthesizing a β-
lactamase, an enzyme that attacks the β-lactam ring. To overcome this
resistance, β-lactam antibiotics can be given with β-lactamase inhibitors such
as clavulanic acid.
85
86. PENICILLIN
● Penicillins are a group of antibiotics originally obtained
from Penicillium moulds, principally P. chrysogenum and P. rubens. Most
penicillins in clinical use are chemically synthesised from naturally-produced
penicillins.
● only two purified compounds are in clinical use: penicillin
G (intramuscular or intravenous use) and penicillin V (given by mouth).
● Penicillins were among the first medications to be effective against
many bacterial infections caused by staphylococci and streptococci.
86
89. MECHANISM OF ACTION:
● Interferes with the synthesis of bacterial cell wall.
The action of penicillin requires the presence of a cell
wall that contains peptidoglycans.
89
90. SYNTHESIS OF PEPTIDOGLYCAN
90
addition of 5 amino acids to N-acetyl muramic acid
Most gram positive bacteria
do not possess a periplasmic
space but have only periplasm
where metabolic digestion
occurs and new cell
peptidoglycan is attached.
91. 91
Next, N-acetyl glucosamine is added to the N-acetyl
muramic acid to form a precursor of peptidoglycan.
This peptidoglycan precursor is then transported across the cell
membrane to a cell wall acceptor in the periplasm. Once in the
periplasm, the peptidoglycan precursors bind to cell wall
acceptors, and undergo extensive crosslinking.
92. 92
Two major enzymes are involved in crosslinking: transpeptidase
and D-alanyl carboxypeptidase. These enzymes are also known as
penicillin binding proteins because of their ability to bind
penicillins and cephalosporins.
several layers of peptidoglycan are formed all of which are
crosslinked to create the cell wall. Gram positive bacteria have
many more layers than gram negative bacteria and thus have a
much thicker cell wall.
93. 93
Beta-lactam antibiotics include all penicillins and cephalosporins that
contain a chemical structure called a beta-lactam ring. This structure is
capable of binding to the enzymes that cross-link peptidoglycans. Beta-
lactams interfere with cross-linking by binding to transpeptidase and D-
alanyl carboxypeptidase enzymes, thus preventing bacterial cell wall
synthesis.
94. PENICILLIN-G (BENZYL/CRYSTALLINE
PENICILLIN)
● It is a narrow spectrum antibiotic , activity is limited to gram positive
bacteria & few others.
■ Penicillin G is acid liable- destroyed by gastric acid when given
orally.Therefore,usually given by iv route.
■ Absorption from i.m site is rapid and but painful.
■ It is distributed mainly extracellularly; reaches most body fluids but
penetration in serous cavities and CSF is poor
■ It is little metabolized because of rapid excretion
■ t1/2 of penicillin in healthy adult is 30 min.
■ Action can be prolonged by giving probenecid simultaneously.
94
95. Adverse effects
■ Penicillin G is one of the most non toxic antibiotics.
■ Local irritancy- Pain at i.m injection site, Nausea on
oral injections, Thrombophlebitis of injected veins.
■ Hypersensitivity: Rash, Itching, Urticaria, Fever,
Wheezing, Anaphylaxis
■ Superinfection: Rare because of its narrow spectrum
95
96. Jarisch – Herxheimer reaction:
acute exacerbation of signs and symptoms of syphilis during penicillin
therapy due to release of endotoxins from the dead organisms.
Penicillin injected in a syphilitic patient may produce shivering, fever,
• myalgia, exacerbation of lesion and even vascular collapse.
• This is due to the sudden release of spirochetal lytic products and lasts 12-
72 hours.
• Aspirin and sedation for relief of symptoms.
96
98. SEMISYNTHETIC PENICILLINS
■ Semisynthetic penicillins are produced by chemically
combining specific side chains.
■ This is to overcome the short comings of natural penicillin
such as:
Poor oral efficacy
Susceptibility to penicillinase
Narrow spectrum of activity
Hypersensitivity
98
101. AMPICILLIN
Ampicillin can be administered by mouth, an intramuscular injection (shot) or
by intravenous infusion.
Ampilin 250 MG Tablet
● Manufactured By :Hetero Healthcare Ltd
● Substitutes:Synthocillin 500mg Capsule,Neocillin 500mg Capsule,Ampurin
500mg Capsule,Mahacillin 500mg Capsule
● Uses : UTI , RTI, Meningits, Gonorrhoea
● Interactions : Hydrocotisone inactivates ampicillin mixed in IV
101
102. AMOXICILLIN
Amoxicillin (α-amino-p-hydroxybenzyl penicillin) is a semisynthetic derivative of
penicillin with a structure similar to ampicillin but with better absorption when taken
by mouth, thus yielding higher concentrations in blood and in urine.Amoxicillin
diffuses easily into tissues and body fluids.
Novamox 500 Capsule
● MANUFACTURER:Cipla Ltd
● SALT COMPOSITION: Amoxycillin (500mg)
● SUBSTITUTES: Moxilium 500mg Capsule,Radimox 500mg Caps
● Novamox 500 Capsule helps to eliminate a bacteria known as H. pylori in people
with peptic ulcer disease. It is a broad-spectrum antibiotic that fights and stops
the growth of many types of bacteria. This medicine is best taken with a meal to
reduce the chance of a stomach upset.
102
103. BETA – LACTAMASE INHIBITORS
• Beta-lactamases are a family of enzymes produced by many gram
positive and gram negative bacteria that inactivate the beta-
lactam antibiotics by opening the beta-lactam ring.
• They structurally resemble -lactam molecules. Beta-lactamase
inhibitors bind to lactamases and inactivate them. Coadministration of
these drugs with -lactams increases the activity of -lactams by
preventing them from enzymatic destruction.
● CLAVULANIC ACID, SULBACTAM AND TAZOBACTAM
103
104. CLAVULANIC ACID
■ Obtained from Streptomyces clavuligerus.
■ It inhibits a wide variety of beta-lactamases produced by both
gram positive and gram negative bacteria.
■ Also called ‘suicide inhibitor’ as it gets inactivated after
binding to the enzyme.
104
105. ● Uses:
• Addition of clavulanic acid reestablishes the activity of amoxicillin against
beta-lactamase producing bacteria.
• Coamoxiclav (Amoxicillin + clavulanic acid) is indicated for :
• Skin and soft tissue infections,Gonorrhoea
• Urinary, Biliary, Respiratory tract infections
• Dental infections caused by β – lactamase producing
bacteria.
• Dose: Amoxicillin 250mg + clavulanic acid 125mg tab; TDS,
severe infections 4 tabs 6 hourly.
105
106. Coamoxiclav (Amoxicillin + clavulanic acid)
• SUBSTITUTES:augmentin,moxclav,amonate
• USES:Skin and soft tissue infections,Urinary, Biliary, Respiratory
tract infections ,Gonorrhoea, Dental infections caused by β –
lactamase producing bacteria.
• Dose: Amoxicillin 250mg + clavulanic acid 125mg tab; TDS, severe
infections 4 tabs 6 hourly.
● Amoxicillin/clavulanic acid is the International Nonproprietary
Name (INN) and co-amoxiclav is the British Approved Name (BAN).
106
107. CEPHALOSPORINS
• These are group of semisynthetic antibiotics derived from
`Cephalosporin-C’ obtained from a fungus Cephalosporium.
• All cephalosporins are bactericidal and have the same mechanism of
action as penicillin.
• Penicillins are superior to these in their range of action against
periodontal pathogenic bacteria.
• Rashes, Urticaria, Fever and GI upset have been associated with
cephalosporins.
●
107
110. METRONIDAZOLE
■ Nitroimidazole compound developed in France to treat
protozoal infections
■ Bactericidal to anaerobic microoganisms .
■ Permeable through the bacterial cell wall, the drug binds DNA
and disrupts the helical structure. Breakage of the DNA
strands follows leading to cell death
■ It enters the cell by diffusion, where its nitro group is
converted into a highly reactive nitro radical which exerts
cytotoxicity.
110
111. • Plasma t1/2 is 8hrs
• Effective against A. actinomycetemcomitans when used in
combination with other antibiotics
• Also effective against anaerobes such as Porphyromonas
gingivalis and Prevotella intermedia.
Metrogyl 400 Tablet
● MANUFACTURER= J B Chemicals and Pharmaceuticals Ltd
● SALT COMPOSITION= Metronidazole (400mg)
● SUBSTITUTES= Metropen 400mg,metrogyl 400mg tab
111
112. Adverse Effects:
• Most Common=Nausea, Metallic taste, Abdominal cramps
• Less Frequent=Headache, Glossitis, Dryness of mouth and
dizziness
• Prolonged Administration=Peripheral Neuropathy and CNSa
112
113. Contraindications :
• Chronic alcoholics
• First trimester of pregnancy
• Neurological disease
• Blood dyscrasias
● Interactions:
• A Disulfiram-like intolerance to alcohol occurs in some
patients.
• Avoided for patients on anticoagulant therapy
113
114. USES IN PERIODONTICS
• It has been used to treat Gingivitis, ANUG, Chronic periodontitis,
and Aggressive periodontitis.
• Has been used in monotherapy as well as in combination with
scaling and root planing and with other antibiotics.
• A single dose of metronidazole 250 mg orally appear both in serum
and GCF in sufficient quantities to inhibit a wide range of suspected
periodontal pathogens.
114
115. ● Administered systemically 750-1000 mg/day for 2 weeks, it reduces
the growth of anaerobic flora, including spirochaetes, and decreases
the histopathologic signs of periodontitis.
● Most common regimen is 250 mg t.i.d for 8 days.
● Metronidazole used as supplement to rigorous scaling and root
planing resulted in the reduced need for surgery compared with root
planing alone.
● It offers some benefit in the treatment of refractory periodontitis,
particularly when used in combination with amoxicillin.
115
116. FLUOROQUINOLONES
● The first quinolone, nalidixic acid, is a urinary antiseptic.
● Fluoroquinolones are synthetic fl uorinated analogues of nalidixic acid. The
important fluoroquinolones are norfl oxacin, ciprofl oxacin, pefloxacin, ofl
oxacin, levofl oxacin, gemifl oxacin and moxifl oxacin.
116
118. Pharmacokinetics :
• Rapidly absorbed orally, but food delays absorption and
first pass metabolism occurs.
• The most prominent feature is High tissue penetrability,
Concentration in lung, sputum, muscle, bone, prostrate and
phagocytes exceeds that in plasma, but CSF and aqueous
levels are lower.
• It is excreted primarily in urine, both by glomerular
filtration and tubular secretion.
118
119. ● Urinary and Biliary concentrations are 10-50 fold that in plasma.
● t ½ 3 - 5 hrs
● Dose 250 - 750 mg b.i.d orally, 100 - 200 mg i.v
● Uses :
• Typhoid
• Bone & soft tissue infections
• Respiratory infections
• Urinary tract infections
• Tuberculosis
• Conjunctivitis
119
120. ● In Periodontics :
• It demonstrates minimal effect on streptococcus species, associated with
periodontal health, it may facilitate the establishment of a microflora associated
with periodontal health.
• At present ciprofloxacin is the only antibiotic in periodontal therapy to which all
strains of aggregatibacter actinomycetemcomitans are susceptible.
• It has been used in combination with metronidazole.
120
121. ● Adverse effects :
■ Gastrointestinal : Nausea, Vomiting, Bad Taste
■ CNS: Dizziness, Headache, Restlessness, Anxiety,
Insomnia, Impairment Of Concentration, Dexterity,
Tremors And Seizures (rarely)
■ Skin and Hypersensitivity: Rash, Pruritus,
Photosensitivity, Urticaria, Swelling Of Lips etc
■ Tendonitis and Tendon Rupture
■ Cartilage damage in weight bearing joints in children
121
122. MACROLIDE ANTIBIOTICS
● ERYTHROMYCIN
• Erythromycin is the first member discovered in the 1950s
• It was isolated from Streptomyces erythreus.
• Later additions - Roxithromycin, Azithromycin,
Clarithromycin
• Used as an alternative to penicillin.
122
123. MECHANISM OF ACTION :
■ Bacteriostatic at low and cidal at high concentrations.
■ They act by inhibiting protein synthesis.
■ They bind to 50S ribosomes and interferes with translocation.
■ They are active against mostly gram positive and a few gram
negative bacteria.
■ It is several fold more active in the alkaline medium, because
the nonionized form of the drug is favoured at higher pH.
123
124. Pharmacokinetics :
• It is acid labile.
• To protect it from gastric acid, it is given as enteric coated tablets,
from which absorption is incomplete and food delays absorption by
retarding gastric emptying.
• It is widely distributed in the body, enters cells and into abscesses,
crosses serous membrane and placenta, but not blood brain barrier.
• Excreted primarily in bile in the active form.
• Renal excretion minor, dose need not be altered in renal failure.
124
125. • The plasma t ½ is 1.5 hrs , but it persists longer in tissues.
• Dose: 250 - 500 mg tab 6 hourly (max. 4 g / day)
■ Children 30 - 60 mg/ kg/ day
● ERYTHROCIN, ERYSTER
• Uses :
■ Drug of choice
Atypical pneumonia
Pharyngitis
Tonsillitis
Respiratory / ENT infections
125
127. AZITHROMYCIN
• This macrolide drug has expanded spectrum, improved
pharmacokinetics, better tolerability and drug interaction
profiles.
• High activity against respiratory pathogens.
• Acid stable
• Rapid oral absorption
• Marked tissue distribution
• Intracellular penetration.
○ AZITHRAL, AZIWOK 250, 500 mg cap
127
128. ● Major advantage :
• Convenient dosing : 500 mg od for 3 days or 500 mg initial loading
dose followed by 250 mg od for 4 days
• Concentration in most tissues exceed that in plasma particularly
higher concentrations are attained in macrophages and fibroblasts.
• Slow release from intracellular sites contributes to its long terminal
t ½ > 50 hrs.
● Adverse effects:
• Mild gastric upset, Abdominal pain (less than erythromycin)
• Headache, Dizziness
128
129. CLINDAMYCIN
■ A lincosamide antibiotic similar in mechanism of action and
spectrum of activity to erythromycin, with which it exhibits
partial cross resistance.
■ Bacteriostatic drug.
■ Effective against anaerobic bacteria.
■ Used when patient allergic to penicillin.
■ Oral absorption good.
129
130. • Penetrates into most skeletal and soft tissues, but not to brain and
CSF; accumulates in neutrophils and macrophages.
• Is largely metabolized and metabolites are excreted in urine and
bile.
• t ½ is 3 hrs.
○ DALCAP, DALCIN, CLINCIN – 150, 300 mg cap. QID
• Mechanism of action :
○ Inhibits protein synthesis by binding to
50S ribosomal subunit and interferes with
translocation.
130
131. Adverse effects :
■ Rashes
■ Urticaria
■ Abdominal pain
■ Major problems – Diarrhoea and
Pseudomembranous enterocolitis
(Metronidazole alternatively Vancomycin
given to treat it )
131
132. DRUG INTERACTIONS
1. PENICILLINS :
Efficacy decreased by tetracyclines, erythromycin and cephalosporins
Potentiates anticoagulant effects of warfarin and aspirin
2. ERYTHROMYCIN :
Potentiates vasoconstrictive effects of ergot alkaloids
Potentiates toxicity of theophylline
3. TETRACYCLINES :
Potentiates anticoagulant effects of warfarin
Potentiates nephrotoxicity of diuretics
Decreases bacteriocidal effects of penicillins and ciprofloxacin
Digestive absorption inhibited by antacids, antianemics, magnesium-
containing drugs and milk product
132
133. ● 4. METRONIDAZOLE :
Potentiates anticoagulant effects of coumadin (warfarin)
Alcohol consumption and disulfiram elicit “antabuse reaction” (abdominal cramps,
nausea, vomiting, headaches, toxic psychosis)
Potentiated by chloramphenicol and cimetidine
Potentiates phenytoin and phenobarbital
● 5. CIPROFLOXACIN :
Potentiates toxicity of theophylline
Digestive absorption inhibited by antacids
Reduces metabolism of caffeine
Enhances effect of warfarin
● 6. CEPHALEXIN :
Potentiates anticoagulant effects of coumadin (warfarin) and aspirin
Bacteriocidal effects decreased by tetracyclines and erythromycin
133
135. SUBGINGIVAL METRONIDAZOLE
● Elyzo 25% Dentalgel (EDG) which is developed for use in the treatment of
periodontitis is a suspension of metronidazole benzoate (40%) in a
mixture of glyceryl mono-oleate (GMO) and triglyceride (sesame oil).
Metronidazole can be detected in the periodontal pockets 24-36 h after
application. It is applied in viscous consistency to the pocket, where it is
liquidized by the body heat and then hardens again, forming crystals in
contact with water.
● As a precursor, the preparation contains metronidazole benzoate, which
is converted into the active substance by esterases in GCF.
135
136. ● TETRACYCLINE CONTAINING FIBRES (ACTISITE)
○ Actisite® (tetracycline periodontal) periodontal fiber for periodontal
pocket placement consists of a 23 cm (9 inch) monofilament of
ethylene/vinyl acetate copolymer, 0.5 mm in diameter, containing 12.7
mg of evenly dispersed tetracycline hydrochloride, USP.Actisite®
(tetracycline periodontal) fiber provides continuous release of
tetracycline for 10 days.
136
137. SUBGINGIVAL MINOCYCLINE (ARESTIN)
● ARESTIN (minocycline hydrochloride) microspheres, 1mg is a subgingival
sustained-release product containing the antibiotic minocycline hydrochloride
incorporated into a bioresorbable polymer, Poly (glycolide-co-dl-lactide) or
PGLA, for professional subgingival administration into periodontal pockets.
Each unit-dose cartridge delivers minocycline hydrochloride equivalent to 1 mg
of minocycline free base.2% minocycline is encapsulated into bioresorbable
microspheres in a gel carrier.
137
138. DOXYCYCLINE (ATRIDOX)
● The ATRIDOX (doxycycline hyclate) ® product is a subgingival controlled-release product composed
of a two syringe mixing system.
● Syringe A contains 450 mg of the ATRIGEL® Delivery System, which is a bioabsorbable, flowable
polymeric formulation composed of 36.7% poly(DLlactide) (PLA) dissolved in 63.3% N-methyl-2-
pyrrolidone (NMP).
● Syringe B contains 50 mg of doxycycline hyclate which is equivalent to 42.5 mg doxycycline. The
constituted product is a pale yellow to yellow viscous liquid with a concentration of 10% of
doxycycline hyclate. Upon contact with the crevicular fluid, the liquid product solidifies and then
allows for controlled release of drug for a period of 7 days.
138
139. IRRIGATION WITH ANTIBIOTICS
● 10% TETRACYCLINE HCL
● As per Silverstein et al.8 when a waterpik is used to deliver tetracycline subgingivally, an
increased levels of tetracycline is obtained within gingival crevicular fluid and these levels
are more than that achieved with antibiotics administered systemically.
● Additionally, tetracycline has been shown to be efficacious against the periodontal
diseasecausing pathogenic microorganisms, by increasing the attachment of fibroblasts to
fibronectin-associated dental structures and by inhibiting the activity of collagenase.
139
140. COMMON ANTIBIOTIC THERAPIES IN THE
TREATMENT OF PERIODONTAL DISEASES
● Amoxicillin - 500 mg / t.i.d / 5 days
● Metronidazole - 400 mg / t.i.d / 8 days
● Clindamycin - 300 mg / t.i.d / 10 days
● Doxycycline or minocycline - 100 - 200 mg/ o.d /21days
● Ciprofloxacin - 500 mg / b.i.d / 8 days
● Azithromycin - 500 mg / o.d / 4 - 7 days
● Combination Therapy :
■ Metronidazole + Amoxicillin - 250 mg of each drug / t.i.d / 8
days
■ Metronidazole + Ciprofloxacin - 500 mg of each drug / b.i.d / 8 days
140
141. NECROTISING ULCERATIVE GINGIVITIS
○ Amoxicillin 500 mg every 6 hours for 10 days
● For amoxicillin sensitive patients
○ Erythromycin -500 mg every 6 hours
○ Metronidazole – 500 mg bid for 7 days
141
142. ACUTE PERICORONITIS
● Antibiotics are advised in severe cases and in patients who may have
clinical evidence of diffuse microbial infiltration of the tissue
○ Amoxcillin 500 mg + metronidazole 400mg tid for 5 days
○ Ornidazole 500 mg + ofloxacilin 200 mg bid for 5 days
142
143. ACUTE HERPETIC GINGIVOSTOMATITIS
○ Earlier consisted of palliative therapy
○ Can give antiviral therapy (acyclovir )
○ 15 mg/kg of an acyclovir suspension given five times daily for 7
days.
143
144. ACUTE PERIODONTAL ABSCESS
Amoxicillin:
■ Loading dose of 1.0 g followed by a maintenance dose of 500
mg/t.i.d. for 3 days
■ revaluation
Allergy to ß-lactam drugs
■ Azithromycin: loading dose of 1.0 g on day 1, followed by 500 mg
od for 3 days OR
■ Clindamycin: loading dose of 600 mg on day 1, followed by 300
mg/q.i.d. for 3 days
144
145. AGGRESSIVE PERIODONTITIS
○ Systemic tetracycline -250 mg qid for atleast 1 week should be
given in conjuction with mechanical debridement.
○ Doxycycline -100 mg od may be used instead of tetracycline.
145
146. FAILURES OF ANTIBIOTIC THERAPY
● Inappropriate choice
● Antibiotic resistance
microorganisms
● Low blood concentration
● Growth rate of microorganisms
● Impaired host defense
● Non compliance
● Antagonism
● Lack of penetration
● Decreased blood flow
● Local factors
● Source of infection
146
147. CONCLUSION
Antibiotics are powerful medicines that fight certain
infections and can save lives when used properly. They are
valuable and in some instances life-saving drugs. They can
only retain this position in medicine and dentistry if used
with care and prescribed appropriately.
147
148. REFERENCES :
● Essentials of medical pharmacology- K D Tripathi - 7th edition
● Carranza’s Clinical Periodontology - Newman, Takei, Klokkevold, Carranza- 10th
edition
● Antibiotic/Antimicrobial use in Dental practice - Michael Newman, Kenneth
Kornman
● Antibiotics in periodontal therapy advantages and disadvantages Slots and
Rams J Clin Periodontol l990; 17: 479-493.
● Systemic & topical antimicrobial therapy in Periodontics Periodontology 2000;
1996, vol 10
● Systemic antibiotics in the treatment of periodontal disease Periodontology
2000, Vol. 28, 2002, 106–176
148
Editor's Notes
SYRINGE USED TO INJECT MERCURY AS PART OF SYPHILIS TREATMENT
Ignaz Semmelweis was the first doctor to discover the importance for medical professionals of hand washing. In the 19th century, it was common for women to die from an illness contracted during or after childbirth, known as childbed fever.
The mouthwash Listerine was also named after Lister, in 1979 by Lawrence and Bosch, when it was marketed as a surgical antiseptic. Joseph Lister, the Man who Sterilized Surgery. Joseph Lister: father of modern surgery.
According to Glossary of Periodontal terms 2001:
Any chemical that alters the physiologic processes of living systems.
Bactericidal drug is clearly superior to the static drugs in treating patients with impaired host defence , life threatening infections, infections at less accessible sites.
genetically determined, e.g. normally,
gram-negative bacilli are not affected by penicillin G.
In acquired resistance, microbes that initially respond to an AMA later develop resistance to the same AMA by mutation or gene transfer, e.g. gonococcal resistance to penicillins.
Conjugtn--Two bacteria can pair up and connect through structures in the cell membranes and then transfer DNA from one bacterial cell to another.
The gene carrying the ‘resistance’ or ‘R’ factor is transferred only if another ‘resistance transfer factor’ (RTF) is also present.
There are several mechanisms by which an organism can develop resistance to an antimicrobial agent. The important mechanisms are:
1. Production of inactivating enzymes: For example, staphylococci, gonococci, E. coli, etc. produce beta-lactamases that can destroy some of the penicillins and cephalosporins.
2. An efflux pump mechanism: It is a mechanism that prevents the accumulation of the drug in the microorganism, e.g. resistance of gram-positive and gram-negative bacteria to tetracyclines, chloramphenicol, macrolides, etc.
3. Alteration of the binding site: For example, change in penicillin-binding proteins (PBPs) in case of certain pneumococci with decreased affi nity for penicillins.
4. Absence of metabolic pathway: For example, sulphonamide-resistant bacteria can utilize preformed folic acid without the need for the usual metabolic steps.
1. To prevent endocarditis in patients with valvular lesion before undergoing any surgical procedures: Surgical procedures mucosal damage bacteraemia affects damaged valve endocarditis.
Amoxicillin 2 g, 1 h before procedure or Cephalexin 2 g, 1 h before procedure Clindamycin 600 mg, 1 h before procedure Or Azithromycin 500 mg, 1 h before procedure • Parenteral regimens If patient is allergic to penicillin Ampicillin 2g i.m. or i.v. 30 min before procedure Or Cefazolin 1 g i.v. or i.m., 30 min before procedure Clindamycin 600 mg i.v. 1 h before procedure
form stable insoluble and unabsorbable complexes with calcium, magnesium, iron and other metal ions. Therefore, the absorption of tetracyclines is reduced by simultaneous administration with dairy products, antacids, iron, sucralfate and zinc salts.
Pseudomembranous colitis caused by C. difficile is a serious complication. It is characterized by severe diarrhoea, fever, abdominal pain and stool mixed with blood and mucus, which is treated with oral metronidazole
Requires administration of 250mg four times daily
It is inexpensive
Tetracycline works best when taken on an empty stomach 1 hour before or 2 hours after meals. If stomach upset occurs, ask your doctor if you can take this medication with food. Take each dose with a full glass of water (8 ounces or 240 milliliters) unless your doctor directs you otherwise. Do not lie down for at least 10 minutes after taking this medication. For this reason, do not take it right before bedtime.
Take this medication 2-3 hours before or after taking any products containing magnesium, aluminum, or calcium. Some examples include antacids, quinapril, certain forms of didanosine (chewable/dispersible buffered tablets or pediatric oral solution), vitamins/minerals, and sucralfate. Follow the same instructions with dairy products (such as milk, yogurt), calcium-enriched juice, bismuth subsalicylate, iron, and zinc. These products bind with tetracycline, preventing its full absorption.
Dosage is based on your medical condition and response to therapy. For use in children older than 8 years of age, the dosage is also based on weight.
For the best effect, take this antibiotic at evenly spaced times. To help you remember, take this medication at the same time(s) every day.
Continue to take this medication until the full-prescribed amount is finished even if symptoms disappear after a few days. Stopping the medication too early may allow bacteria to continue to grow, which may result in a relapse of the infection.
Inform your doctor if your condition lasts or gets worse.
How to use Vibramycin
Read the Patient Information Leaflet if available from your pharmacist before you start taking doxycycline and each time you get a refill. If you have any questions, ask your doctor or pharmacist.
This medication is best taken by mouth on an empty stomach, at least 1 hour before or 2 hours after a meal, usually 1 or 2 times daily or as directed by your doctor. Take this medication with a full glass of water (8 ounces/240 milliliters) unless directed otherwise. If stomach upset occurs, taking it with food or milk may help. However, doxycycline may not work as well if you take it with food or milk (or anything high in calcium - more details below ), so ask your doctor or pharmacist if you may take it that way. Do not lie down for at least 10 minutes after taking this medication.
Take this medication 2 to 3 hours before or after taking any products containing aluminum, calcium, iron, magnesium, zinc, or bismuth subsalicylate. Some examples include antacids, didanosine solution, quinapril, vitamins/minerals, dairy products (such as milk, yogurt), and calcium-enriched juice. These products bind with doxycycline, preventing your body from fully absorbing the drug.
When using to prevent malaria, this medication is usually taken once daily. Take the first dose of this medication 1 to 2 days before travel or as directed by your doctor. Continue to take this medication daily while in the malarious area. Upon returning home, you should keep taking this medication for 4 more weeks. If you are unable to finish this course of doxycycline, contact your doctor.
THE DOSAGE OF PERIOSTAT® (doxycycline hyclate) DIFFERS FROM THAT OF DOXYCYCLINE USED TO TREAT INFECTIONS. EXCEEDING THE RECOMMENDED DOSAGE MAY RESULT IN AN INCREASED INCIDENCE OF SIDE EFFECTS INCLUDING THE DEVELOPMENT OF RESISTANT MICROORGANISMS. Administration of adequate amounts of fluid along with the tablets is recommended to wash down the drug and reduce the risk of esophageal irritation and ulceration.
HOW SUPPLIED
Periostat® (doxycycline hyclate) (white tablet imprinted with a PS20) containing doxycycline hyclate equivalent to 20 mg doxycycline.
Effective against a broad spectrum of microorganisms in patients with adult periodontitis.
It suppresses spirochetes and motile rods as effectively as SRP, with suppression remaining evident for up to 3 months after therapy.
Can be given twice a day, thus facilitating compliance when compared with tetracycline.
Administered in a dosage of 200 mg per day for 1 week results in a reduction in total bacterial counts, complete elimination of spirochetes for periods of up to 2 months, and improvement in all clinical parameters.CYANOMYCIN 50MGMinocycline is quickly and nearly completely absorbed from the upper part of the small intestine. very high concentrations are found in the gallbladder and liver. It crosses the blood–brain barrier better than doxycycline and other tetracyclines, reaching therapeutically relevant concentrations in the cerebrospinal fluid and also in inflamed meninges.
In gram negative bacteria, the gap between the cell membrane and the cell wall is known as the periplasmic space. Penicillin can easily enter bacterial cell in case of Gram-positive species. This is because Gram-positive bacteria do not have an outer cell membrane and are simply enclosed in a thick cell wall.[43] Penicillin molecules are small enough to pass through the spaces of glycoproteins in the cell wall. For this reason Gram-positive bacteria are very susceptible to penicillin (as first evidenced by the discovery of penicillin in 1928[44])
By inhibiting cell wall synthesis, the bacterial cell is damaged. Gram positive bacteria have a high internal osmotic pressure. Without a normal, rigid cell wall, these cells burst when subjected to the low osmotic pressure of their surrounding environment. As well, the antibiotic-penicillin binding protein complex stimulates the release of autolysins that are capable of digesting the existing cell wall. Beta-lactam antibiotics are therefore considered bactericidal agents. Mechanism of bacterial resistance to penicillins Bacteria develop resistance (i) by producing -lactamases, which destroy the -lactam ring, e.g. S. aureus, E. coli, gonococci, H. infl uenzae, etc. (ii) due to altered PBPs, which have less affi nity for -lactams, e.g. S. pneumoniae (iii) due to decreased ability of the drug to penetrate to its site of action.
It differs from penicillin G, or benzylpenicillin, only by the presence of an amino group. This amino group, present on both ampicillin and amoxicillin, helps these antibiotics pass through the pores of the outer membrane of Gram-negative bacteria. , The oral form, available as capsules or oral suspensions, is not given as an initial treatment for severe infectionsbut rather as a follow-up to an IM or IV injection
Plasma t ½ is 1 hour.
Useful in the management of patients with aggressive periodontitis, both in the localized and generalized forms.
Recommended dosage is 500mg tid for 8days.
Rapid oral absorption
Plasma t ½ of 1 hr, similar to Amoxicillin.
Eliminated mainly by glomerular filtration.
USES:
1st generation compounds are used as alternative to PnG in allergic patients.
Respiratory, urinary, soft tissue infections caused by gram negative organisms.
Penicillinase producing staphylococcal infections.
Septicaemias caused by gram negative organisms.
Meningitis
Typhoid
ctisite® (tetracycline periodontal) periodontal fiber is indicated as an adjunct to scaling and root planing for reduction of pocket depth and bleeding on probing in patients with adult periodontitis.
Treatment with Actisite (tetracycline periodontal) is a component of an intervention program which includes good oral hygiene and scaling and root planing.
Effectiveness of repeated fiber applications in a site has not been studied.
The effects of Actisite (tetracycline periodontal) on bone loss, tooth mobility, or tooth loss from periodontal disease has not been established
DOSAGE AND ADMINISTRATION
Actisite (tetracycline periodontal) periodontal fiber for 10 days is indicated as an adjunct to scaling and root planing. Repeated fiber applications have not been studied. Actisite (tetracycline periodontal) fiber should be inserted into the periodontal pocket until the pocket is filled. The length of fiber used will vary with pocket depth and contour. The fiber should be placed to closely approximate the pocket anatomy and should be in contact with the base of the pocket. An appropriate cyanoacrylate adhesive should be used to help secure the fiber in the pocket.
When placed within a periodontal pocket, Actisite (tetracycline periodontal) fiber provides continuous release of tetracycline for 10 days. At the end of 10 days of treatment, all fibers must be removed. Fibers lost before 7 days should be replaced.
HOW SUPPLIED
Actisite (tetracycline periodontal) periodontal fiber is available in cartons containing 4 fibers and 10 fibers. Each individually packaged, yellow fiber is 23 cm (9 inches) long and contains 12.7 mg of Actisite (tetracycline periodontal) .
NDC 17314-4800-4 (4 Fiber carton)NDC 17314-4800-1 (10 Fiber carton)
Store at controlled room temperature 15o-30oC (59o-86oF).
CHRONIC PERIODONTITIS/ PERIODONTITIS REFRACTORY TO TREATMENT
The patients who do not respond well to conventional therapy.
Systemic antibiotic therapy is administered.
To reinforce mechanical periodontal treatment.
Support the host defence system.
Amoxicillin 250mg + Clavulanic acid 125 mg tid 14 days
Metranidazole 500 mg tid for 7 days
Clindamycin hydrochloride 150 mg qid for 7 days
Azithromycin 500 mg od for 3 days
Combination of various antibiotics