Beta lactamase inhibitors－fx
•Download as PPTX, PDF•
5 likes•5,304 views
This document discusses various beta-lactamase inhibitors that are used in combination with beta-lactam antibiotics to overcome antibiotic resistance. It describes several natural and synthetic inhibitors including clavulanic acid, tazobactam, sulbactam, oxapenems, NXL 104, BAL 30376, LK-157, BLI-489, CP3242, and SA-1-204. These inhibitors work by preventing beta-lactamase enzymes from breaking down beta-lactam antibiotics, thereby restoring the antibiotics' effectiveness against resistant bacteria. The document compares the inhibitory activities and spectra of each inhibitor.
Report
Share
Report
Share
Recommended
Cephalosporins
This document provides information on cephalosporins, a class of beta-lactam antibiotics. It discusses their development from fungi, mechanism of action similar to penicillins, and classification into 5 generations based on spectrum of activity. The first three generations are described as having activity mainly against gram-positive and some gram-negative bacteria. The fourth generation are more resistant to beta-lactamases. Adverse reactions and uses are also summarized for each generation. Other beta-lactam classes including monobactams, carbapenems, and carbacephems are introduced at the end.
Cephalosporins
Cephalosporins are a class of β-lactam antibiotics derived from fungi. They are classified into generations based on their spectrum of activity, with later generations having broader spectra. They work by binding penicillin-binding proteins. Resistance can develop via target modification or β-lactamase production. Newer generations have activity against MRSA and expanded gram-negative coverage.
Beta Lactamase Inhibitors
The presentation include pharmacology of beta lactamase inhibitors.
Contents
Introduction
Clavulanic acid
Pharmacokinetics
Clinical uses
Adverse effects
Sulbactam
Pharmacokinetics
Adverse effects
Cephalosporin
1) Cephalosporins are a class of β-lactam antibiotics that are divided into generations based on their spectrum of activity.
2) They have similar mechanisms of action and side effects as penicillins but are generally more acid stable and resistant to β-lactamase degradation.
3) Later generation cephalosporins have broader spectra of activity against gram-negative and anaerobic bacteria. Some such as ceftriaxone and cefotaxime also achieve good cerebrospinal fluid penetration.
Polypeptide antibiotics
A PowerPoint presentation on "Polypeptide antibiotics" suitable Medical and paramedical students (UG & PG), Research scholars, Faculty and others.
Calvulanic acid and analoug
Clavulanic acid is a β-lactamase inhibitor discovered from Streptomyces clavuligerus. It is used in combination with β-lactam antibiotics like amoxicillin to restore their effectiveness against β-lactamase producing bacteria. Clavulanic acid inactivates β-lactamases non-competitively but has weak antibacterial activity itself. Other β-lactamase inhibitors discussed are sulbactam, tazobactam, which have different spectrums of activity and inhibition profiles against various classes of β-lactamases. The development of β-lactamase inhibitors was an important strategy to overcome resistance arising
Monobactam
Monobactams are β-lactam compounds that contain an isolated β-lactam ring not fused to another ring, making them effective only against aerobic Gram-negative bacteria like Neisseria and Pseudomonas. Examples include aztreonam, tigemonam, nocardicin A, and tabtoxin. Potential adverse effects are skin rash, abnormal liver functions, and risk of seizures in susceptible individuals.
Carbapenems
Carbapenems are a class of beta-lactam antibiotics with a fused beta-lactam ring. They include imipenem, meropenem, ertapenem, and aztreonam (a monobactam). Carbapenems have broad spectra of activity against both gram-positive and gram-negative bacteria. Imipenem is inactivated by renal dipeptidases but combined with cilastatin. Meropenem and ertapenem are more stable. Aztreonam only covers gram-negatives but is useful in penicillin allergic patients. Carbapenems are used to treat various infections including respiratory, abdominal, skin and bone infections.
Recommended
Cephalosporins
This document provides information on cephalosporins, a class of beta-lactam antibiotics. It discusses their development from fungi, mechanism of action similar to penicillins, and classification into 5 generations based on spectrum of activity. The first three generations are described as having activity mainly against gram-positive and some gram-negative bacteria. The fourth generation are more resistant to beta-lactamases. Adverse reactions and uses are also summarized for each generation. Other beta-lactam classes including monobactams, carbapenems, and carbacephems are introduced at the end.
Cephalosporins
Cephalosporins are a class of β-lactam antibiotics derived from fungi. They are classified into generations based on their spectrum of activity, with later generations having broader spectra. They work by binding penicillin-binding proteins. Resistance can develop via target modification or β-lactamase production. Newer generations have activity against MRSA and expanded gram-negative coverage.
Beta Lactamase Inhibitors
The presentation include pharmacology of beta lactamase inhibitors.
Contents
Introduction
Clavulanic acid
Pharmacokinetics
Clinical uses
Adverse effects
Sulbactam
Pharmacokinetics
Adverse effects
Cephalosporin
1) Cephalosporins are a class of β-lactam antibiotics that are divided into generations based on their spectrum of activity.
2) They have similar mechanisms of action and side effects as penicillins but are generally more acid stable and resistant to β-lactamase degradation.
3) Later generation cephalosporins have broader spectra of activity against gram-negative and anaerobic bacteria. Some such as ceftriaxone and cefotaxime also achieve good cerebrospinal fluid penetration.
Polypeptide antibiotics
A PowerPoint presentation on "Polypeptide antibiotics" suitable Medical and paramedical students (UG & PG), Research scholars, Faculty and others.
Calvulanic acid and analoug
Clavulanic acid is a β-lactamase inhibitor discovered from Streptomyces clavuligerus. It is used in combination with β-lactam antibiotics like amoxicillin to restore their effectiveness against β-lactamase producing bacteria. Clavulanic acid inactivates β-lactamases non-competitively but has weak antibacterial activity itself. Other β-lactamase inhibitors discussed are sulbactam, tazobactam, which have different spectrums of activity and inhibition profiles against various classes of β-lactamases. The development of β-lactamase inhibitors was an important strategy to overcome resistance arising
Monobactam
Monobactams are β-lactam compounds that contain an isolated β-lactam ring not fused to another ring, making them effective only against aerobic Gram-negative bacteria like Neisseria and Pseudomonas. Examples include aztreonam, tigemonam, nocardicin A, and tabtoxin. Potential adverse effects are skin rash, abnormal liver functions, and risk of seizures in susceptible individuals.
Carbapenems
Carbapenems are a class of beta-lactam antibiotics with a fused beta-lactam ring. They include imipenem, meropenem, ertapenem, and aztreonam (a monobactam). Carbapenems have broad spectra of activity against both gram-positive and gram-negative bacteria. Imipenem is inactivated by renal dipeptidases but combined with cilastatin. Meropenem and ertapenem are more stable. Aztreonam only covers gram-negatives but is useful in penicillin allergic patients. Carbapenems are used to treat various infections including respiratory, abdominal, skin and bone infections.
Cephalosporins & other β lactam antibiotics & cell wall destructors
This document summarizes cephalosporin antibiotics and other β-lactam antibiotics. It discusses the classes of cephalosporins including their history, mechanisms of action, generations, and examples within each generation. It also describes other β-lactam antibiotics such as monobactams, carbapenems, and β-lactamase inhibitors. Additionally, it covers non-β-lactam cell wall acting antibiotics including vancomycin, daptomycin, fosfomycin, polymyxins, and cycloserine. The document provides detailed information on commonly used antibiotics in each class.
Antibiotics ppt
Antibiotics are chemical substances produced by microorganisms that can kill or inhibit the growth of other microorganisms at low concentrations. They are classified based on their mechanism of action and chemical structure. Major classes include beta-lactam antibiotics (penicillins, cephalosporins), aminoglycosides, tetracyclines, macrolides, and chloramphenicol. They work by inhibiting bacterial cell wall, membrane, or protein synthesis. Common side effects include diarrhea, rashes, and potential toxicity like kidney damage or bone marrow suppression in high doses.
Beta lactamase inhibitors
This document discusses beta lactamase inhibitors, which are used to enhance the efficacy of beta lactam antibiotics like penicillins and cephalosporins. It describes how beta lactamase enzymes produced by bacteria provide resistance to these antibiotics by breaking their beta lactam ring structure. Beta lactamase inhibitors prevent this degradation by binding to and inactivating the beta lactamase enzymes. There are two classes of inhibitors - those with a beta lactam core like clavulanic acid and those without, such as avibactam. Inhibitors are used in combination with beta lactams to treat infections that may involve beta lactamase producing bacteria.
Antibiotics acting on cell wall 3 Carbapenems and Monobactums 03-05-2018
Carbapenems and monobactams are new classes of β-lactam antibiotics that act on cell wall synthesis. Carbapenems like imipenem and meropenem have a broad spectrum of activity against gram-positive and gram-negative bacteria. They are often used as last resort drugs for serious infections but resistance is emerging. Meropenem has advantages over imipenem like not requiring an inhibitor and being more soluble. Ertapenem also has activity against anaerobes but not pseudomonas. Monobactams have a monocyclic structure and are isolated from bacteria.
Monobactam antibiotics
Monobactam Antibiotics
Introduction
Spectrum of activity
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Adverse Effect
Beta lactamase inhibitors and Monobactam
This document discusses beta lactamase inhibitors and monobactams. It describes clavulanic acid, sulbactam, and tazobactam, which are beta lactamase inhibitors used to enhance the antibiotic properties of other antibiotics by preventing microbial resistance. It also discusses the monobactams aztreonam and tigemonam, which have activity against gram-negative bacteria by binding to penicillin binding proteins, but no activity against gram-positive bacteria or anaerobes. These monobactams are used to treat various infections when patients cannot tolerate penicillins or cephalosporins.
Aminoglycosides antibiotics
Aminoglycosides are a group of natural or semi-synthetic antibiotics containing an amino sugar component and are used systemically or topically. They are derived from soil actinomycetes, not absorbed orally, and primarily target aerobic gram-negative bacteria through binding to bacterial ribosomes and inhibiting protein synthesis. Common examples include streptomycin, gentamicin, and tobramycin. While effective treatments, aminoglycosides can cause ototoxicity and nephrotoxicity.
Semisynthetic Penicillins
The presentation include semisynthetic penicillin introduction and classification.
Contents
Semisynthetic penicillins- Introduction
Classification
Acid-resistant alternative to Penicillin G
Penicillinase- resistant penicillins
Extended spectrum penicillins
Beta Lactam Antibiotics
This document provides an overview of beta lactam antibiotics, including their structure, mode of action, examples, and mechanisms of resistance. It begins by discussing the bacterial cell wall structure and how beta lactams work by inhibiting cell wall synthesis. Major classes of beta lactams covered include penicillins, cephalosporins, carbapenems, and monobactams. Examples such as methicillin, amoxicillin, and imipenem are described. The document also discusses beta lactamase resistance and concludes with a brief overview of classification.
Monobactams
Monobactams are a class of β-lactam antibiotics that contain a single β-lactam ring, unlike penicillins and cephalosporins which have the ring fused to another. Aztreonam was the first to be approved in 1986. Monobactams are effective against gram-negative bacteria and show promise in treating multi-drug resistant pathogens. They work by inhibiting cell wall synthesis through binding to penicillin-binding proteins. Side effects are generally mild but can include rashes, liver problems, and seizures in susceptible individuals.
Beta lactams antibiotics & beta lactamase inhibitors
This document provides information on beta-lactam antibiotics including penicillins, cephalosporins, and beta-lactamase inhibitors. It discusses the classes of penicillins such as phenoxymethylpenicillin, methicillin, cloxacillin, aminopenicillins, carboxypenicillins, and ureidopenicillins. It describes the structures, spectra of activity, pharmacokinetics, uses and adverse effects of various penicillin derivatives. The summary focuses on the key classes of beta-lactam antibiotics and their properties.
Aminoglycoside antibiotics
This document discusses aminoglycoside antibiotics. It describes their structure, including that they contain amino sugars linked to an aminocyclitol ring. Examples are provided such as streptomycin, kanamycin, neomycin, and gentamicin. Their broad-spectrum antibacterial activity against gram-negative bacteria is summarized. Toxicities like nephrotoxicity and ototoxicity limit their clinical use to serious infections.
Cephalosporins
A nice introduction to Cephalosporins, how they work, the different generations, spectrum, uses, side effects, pharmacokinetics and common trade names in Egyptian market.
Aminoglycosides
Aminoglycosides are a class of antibiotics that consist of amino sugars attached to a hexose ring. They are bactericidal and used to treat infections caused by aerobic gram-negative bacteria. Aminoglycosides work by binding to the 30S ribosomal subunit and inhibiting bacterial protein synthesis. They are not absorbed orally and are administered via injection or topically. Common adverse effects include ototoxicity, nephrotoxicity, and neuromuscular blockade. Aminoglycosides require monitoring due to their toxicity profile.
Cephalosporins Pharmacology
Beta lactam antibiotics cephalosporin pharmacology with mnemonics to identify the class of cephalosporin
Antimicrobial agents
This document discusses various classes of antimicrobial agents including their mechanisms of action, therapeutic uses, and side effects. It covers sulfonamides, penicillins, cephalosporins, tetracyclines, aminoglycosides, and quinolones. For each class, it provides examples of specific drugs, how they work, what types of infections they treat, and potential adverse effects. The goal is to identify the infecting organism and select the appropriate antibiotic based on its susceptibility profile.
Chloramphenicol
Chloramphenicol is an antibiotic that inhibits bacterial protein synthesis. It is effective against a variety of bacteria including H. influenzae, S. typhi, N. meningitidis, E. coli, S. pneumoniae, and V. cholerae. It is rapidly absorbed from the gastrointestinal tract and well distributed throughout the body, including into the central nervous system. Some clinical uses include treatment of typhoid fever, meningitis, and anaerobic infections, however it often has preferred alternatives due to potential side effects like aplastic anemia and grey baby syndrome. It can also interact with other drugs by inhibiting liver enzymes.
Cephalosporins
This document discusses cephalosporins, a class of beta-lactam antibiotics. It describes their history, mechanism of action, classification, uses, and adverse effects. Cephalosporins are derived from the fungus Cephalosporium and work by inhibiting bacterial cell wall synthesis. They are divided into generations based on spectrum of activity, with later generations covering more resistant organisms. Common uses include skin, respiratory, and urinary tract infections. Adverse effects can include hypersensitivity reactions and antibiotic-associated colitis. Newer agents have been developed with activity against multidrug-resistant bacteria.
1.3 penicillins, cephalosporins and cephamycins.
This document discusses the pharmacology of penicillin antibiotics. It provides an introduction to penicillin and describes its discovery, structure, mechanism of action, absorption and excretion. The document discusses bacterial resistance to penicillin through production of penicillinase enzymes. It also covers the use of penicillin in treating various bacterial infections as well as its limitations due to allergenicity and development of resistance. The intended purpose is to educate on the rational use of antimicrobial drugs like penicillin.
Aminoglycosides p pt
The document provides information about aminoglycosides, a class of antibiotics. It discusses the discovery of the first aminoglycoside streptomycin in 1944. It then summarizes that aminoglycosides are first-line therapies for infections like plague, tularemia, and tuberculosis caused by aerobic gram-negative bacteria. The document also lists some common aminoglycosides and provides brief sections on their mechanisms of action, microbial resistance, absorption, uses, and adverse effects.
SULBACTAM -BETALACTAMASE INHIBITOR,INTRODUCTION,MECHANISM OF ACTION,SAR,SYNTH...
SULBACTAM -BETALACTAMASE INHIBITOR,INTRODUCTION,MECHANISM OF ACTION,SAR,SYNTHESIS, USES.
RAVISANKAR.p
VIGNAN PHARMACY COLLEGE,VADLAMUDI,GUNTUR.
Beta lactam antibiotics
Beta lactam antibiotics include penicillins and cephalosporins. Penicillin G is a commonly used penicillin that treats streptococcal infections with doses of 0.5-5 million units given intramuscularly or intravenously for 7-10 days.
More Related Content
What's hot
Cephalosporins & other β lactam antibiotics & cell wall destructors
This document summarizes cephalosporin antibiotics and other β-lactam antibiotics. It discusses the classes of cephalosporins including their history, mechanisms of action, generations, and examples within each generation. It also describes other β-lactam antibiotics such as monobactams, carbapenems, and β-lactamase inhibitors. Additionally, it covers non-β-lactam cell wall acting antibiotics including vancomycin, daptomycin, fosfomycin, polymyxins, and cycloserine. The document provides detailed information on commonly used antibiotics in each class.
Antibiotics ppt
Antibiotics are chemical substances produced by microorganisms that can kill or inhibit the growth of other microorganisms at low concentrations. They are classified based on their mechanism of action and chemical structure. Major classes include beta-lactam antibiotics (penicillins, cephalosporins), aminoglycosides, tetracyclines, macrolides, and chloramphenicol. They work by inhibiting bacterial cell wall, membrane, or protein synthesis. Common side effects include diarrhea, rashes, and potential toxicity like kidney damage or bone marrow suppression in high doses.
Beta lactamase inhibitors
This document discusses beta lactamase inhibitors, which are used to enhance the efficacy of beta lactam antibiotics like penicillins and cephalosporins. It describes how beta lactamase enzymes produced by bacteria provide resistance to these antibiotics by breaking their beta lactam ring structure. Beta lactamase inhibitors prevent this degradation by binding to and inactivating the beta lactamase enzymes. There are two classes of inhibitors - those with a beta lactam core like clavulanic acid and those without, such as avibactam. Inhibitors are used in combination with beta lactams to treat infections that may involve beta lactamase producing bacteria.
Antibiotics acting on cell wall 3 Carbapenems and Monobactums 03-05-2018
Carbapenems and monobactams are new classes of β-lactam antibiotics that act on cell wall synthesis. Carbapenems like imipenem and meropenem have a broad spectrum of activity against gram-positive and gram-negative bacteria. They are often used as last resort drugs for serious infections but resistance is emerging. Meropenem has advantages over imipenem like not requiring an inhibitor and being more soluble. Ertapenem also has activity against anaerobes but not pseudomonas. Monobactams have a monocyclic structure and are isolated from bacteria.
Monobactam antibiotics
Monobactam Antibiotics
Introduction
Spectrum of activity
Pharmacokinetics
Pharmacodynamics
Clinical Uses
Adverse Effect
Beta lactamase inhibitors and Monobactam
This document discusses beta lactamase inhibitors and monobactams. It describes clavulanic acid, sulbactam, and tazobactam, which are beta lactamase inhibitors used to enhance the antibiotic properties of other antibiotics by preventing microbial resistance. It also discusses the monobactams aztreonam and tigemonam, which have activity against gram-negative bacteria by binding to penicillin binding proteins, but no activity against gram-positive bacteria or anaerobes. These monobactams are used to treat various infections when patients cannot tolerate penicillins or cephalosporins.
Aminoglycosides antibiotics
Aminoglycosides are a group of natural or semi-synthetic antibiotics containing an amino sugar component and are used systemically or topically. They are derived from soil actinomycetes, not absorbed orally, and primarily target aerobic gram-negative bacteria through binding to bacterial ribosomes and inhibiting protein synthesis. Common examples include streptomycin, gentamicin, and tobramycin. While effective treatments, aminoglycosides can cause ototoxicity and nephrotoxicity.
Semisynthetic Penicillins
The presentation include semisynthetic penicillin introduction and classification.
Contents
Semisynthetic penicillins- Introduction
Classification
Acid-resistant alternative to Penicillin G
Penicillinase- resistant penicillins
Extended spectrum penicillins
Beta Lactam Antibiotics
This document provides an overview of beta lactam antibiotics, including their structure, mode of action, examples, and mechanisms of resistance. It begins by discussing the bacterial cell wall structure and how beta lactams work by inhibiting cell wall synthesis. Major classes of beta lactams covered include penicillins, cephalosporins, carbapenems, and monobactams. Examples such as methicillin, amoxicillin, and imipenem are described. The document also discusses beta lactamase resistance and concludes with a brief overview of classification.
Monobactams
Monobactams are a class of β-lactam antibiotics that contain a single β-lactam ring, unlike penicillins and cephalosporins which have the ring fused to another. Aztreonam was the first to be approved in 1986. Monobactams are effective against gram-negative bacteria and show promise in treating multi-drug resistant pathogens. They work by inhibiting cell wall synthesis through binding to penicillin-binding proteins. Side effects are generally mild but can include rashes, liver problems, and seizures in susceptible individuals.
Beta lactams antibiotics & beta lactamase inhibitors
This document provides information on beta-lactam antibiotics including penicillins, cephalosporins, and beta-lactamase inhibitors. It discusses the classes of penicillins such as phenoxymethylpenicillin, methicillin, cloxacillin, aminopenicillins, carboxypenicillins, and ureidopenicillins. It describes the structures, spectra of activity, pharmacokinetics, uses and adverse effects of various penicillin derivatives. The summary focuses on the key classes of beta-lactam antibiotics and their properties.
Aminoglycoside antibiotics
This document discusses aminoglycoside antibiotics. It describes their structure, including that they contain amino sugars linked to an aminocyclitol ring. Examples are provided such as streptomycin, kanamycin, neomycin, and gentamicin. Their broad-spectrum antibacterial activity against gram-negative bacteria is summarized. Toxicities like nephrotoxicity and ototoxicity limit their clinical use to serious infections.
Cephalosporins
A nice introduction to Cephalosporins, how they work, the different generations, spectrum, uses, side effects, pharmacokinetics and common trade names in Egyptian market.
Aminoglycosides
Aminoglycosides are a class of antibiotics that consist of amino sugars attached to a hexose ring. They are bactericidal and used to treat infections caused by aerobic gram-negative bacteria. Aminoglycosides work by binding to the 30S ribosomal subunit and inhibiting bacterial protein synthesis. They are not absorbed orally and are administered via injection or topically. Common adverse effects include ototoxicity, nephrotoxicity, and neuromuscular blockade. Aminoglycosides require monitoring due to their toxicity profile.
Cephalosporins Pharmacology
Beta lactam antibiotics cephalosporin pharmacology with mnemonics to identify the class of cephalosporin
Antimicrobial agents
This document discusses various classes of antimicrobial agents including their mechanisms of action, therapeutic uses, and side effects. It covers sulfonamides, penicillins, cephalosporins, tetracyclines, aminoglycosides, and quinolones. For each class, it provides examples of specific drugs, how they work, what types of infections they treat, and potential adverse effects. The goal is to identify the infecting organism and select the appropriate antibiotic based on its susceptibility profile.
Chloramphenicol
Chloramphenicol is an antibiotic that inhibits bacterial protein synthesis. It is effective against a variety of bacteria including H. influenzae, S. typhi, N. meningitidis, E. coli, S. pneumoniae, and V. cholerae. It is rapidly absorbed from the gastrointestinal tract and well distributed throughout the body, including into the central nervous system. Some clinical uses include treatment of typhoid fever, meningitis, and anaerobic infections, however it often has preferred alternatives due to potential side effects like aplastic anemia and grey baby syndrome. It can also interact with other drugs by inhibiting liver enzymes.
Cephalosporins
This document discusses cephalosporins, a class of beta-lactam antibiotics. It describes their history, mechanism of action, classification, uses, and adverse effects. Cephalosporins are derived from the fungus Cephalosporium and work by inhibiting bacterial cell wall synthesis. They are divided into generations based on spectrum of activity, with later generations covering more resistant organisms. Common uses include skin, respiratory, and urinary tract infections. Adverse effects can include hypersensitivity reactions and antibiotic-associated colitis. Newer agents have been developed with activity against multidrug-resistant bacteria.
1.3 penicillins, cephalosporins and cephamycins.
This document discusses the pharmacology of penicillin antibiotics. It provides an introduction to penicillin and describes its discovery, structure, mechanism of action, absorption and excretion. The document discusses bacterial resistance to penicillin through production of penicillinase enzymes. It also covers the use of penicillin in treating various bacterial infections as well as its limitations due to allergenicity and development of resistance. The intended purpose is to educate on the rational use of antimicrobial drugs like penicillin.
Aminoglycosides p pt
The document provides information about aminoglycosides, a class of antibiotics. It discusses the discovery of the first aminoglycoside streptomycin in 1944. It then summarizes that aminoglycosides are first-line therapies for infections like plague, tularemia, and tuberculosis caused by aerobic gram-negative bacteria. The document also lists some common aminoglycosides and provides brief sections on their mechanisms of action, microbial resistance, absorption, uses, and adverse effects.
What's hot (20)
Cephalosporins & other β lactam antibiotics & cell wall destructors
Cephalosporins & other β lactam antibiotics & cell wall destructors
Antibiotics acting on cell wall 3 Carbapenems and Monobactums 03-05-2018
Antibiotics acting on cell wall 3 Carbapenems and Monobactums 03-05-2018
Beta lactams antibiotics & beta lactamase inhibitors
Beta lactams antibiotics & beta lactamase inhibitors
Viewers also liked
SULBACTAM -BETALACTAMASE INHIBITOR,INTRODUCTION,MECHANISM OF ACTION,SAR,SYNTH...
SULBACTAM -BETALACTAMASE INHIBITOR,INTRODUCTION,MECHANISM OF ACTION,SAR,SYNTHESIS, USES.
RAVISANKAR.p
VIGNAN PHARMACY COLLEGE,VADLAMUDI,GUNTUR.
Beta lactam antibiotics
Beta lactam antibiotics include penicillins and cephalosporins. Penicillin G is a commonly used penicillin that treats streptococcal infections with doses of 0.5-5 million units given intramuscularly or intravenously for 7-10 days.
Beta lactam antibiotics
The document discusses beta lactam antibiotics, focusing on penicillins. It describes how penicillin was discovered by Alexander Fleming and its mechanism of inhibiting cell wall synthesis. Penicillins are classified into natural and semisynthetic types, with natural penicillins having a narrower spectrum mainly against gram-positive cocci. Semisynthetic penicillins like ampicillin and amoxicillin have a broader spectrum. Beta lactamase inhibitors are also discussed which are often combined with penicillins to overcome bacterial resistance.
Piperacillin & Tazobactam
Piperacillin & tazobactam is effective against nosocomial infections caused by Staphylococcus aureus, Escherichia coli, and Pseudomonas aeruginosa. It has shown success in treating lower respiratory tract infections, intra-abdominal infections, complicated urinary tract infections, and fever in neutropenic patients. Piperacillin is an extended spectrum penicillin while tazobactam is a beta-lactamase inhibitor that protects piperacillin from degradation, allowing it to be effective against beta-lactamase producing bacteria. Clinical trials demonstrate piperacillin-tazobactam is superior to other antibiotics for various infections and has a good
Betalactams
This document summarizes the classes of β-lactam antibiotics, including their mechanisms of action, indications, and side effects. It discusses the four main classes: penicillins, cephalosporins, monobactams, and carbapenems. Each class is further broken down into generations or subtypes that have varying spectra of coverage and pharmacokinetic properties. Mnemonics are provided to help distinguish between the classes and generations.
Beta lactam antibiotics.
Beta-lactam antibiotics like penicillin have a beta-lactam ring and inhibit bacterial cell wall synthesis. Penicillin was the first antibiotic discovered in 1928 and is obtained from fungi. It is sensitive to beta-lactamase and stomach acid. Variants include methicillin, oxacillin and broad-spectrum amoxicillin. While generally safe, penicillin can cause allergic reactions treated with epinephrine, antihistamines and steroids. Therapeutic uses include streptococcal, syphilis and diphtheria infections.
3. pencillin
This document discusses various antibiotics that act on the bacterial cell wall. It begins by describing the structure and function of the bacterial cell wall and how antibiotics can disrupt it. It then lists several common antibiotics that target the cell wall, including penicillin, cephalosporins, cycloserine, bacitracin, and vancomycin. It provides details on the source and therapeutic uses of each. The remainder of the document goes into further depth about the mechanisms of action and effects of beta-lactam antibiotics like penicillin, focusing on how they inhibit cell wall synthesis and cross-linking. It describes the structures, spectra, uses and side effects of various penicillin derivatives in detail.
Beta lactam antibiotic cephalosporin
Beta Lactam Antibiotic Cephalosporin
Ref Book :Dr SK Srivastava,Dr H L Sharma and Dr KK sharma,Dr K D Tripathi, Dr Sparsh Gupta
Prof. Dr. Ravisankar
BETA-LACTAM ANTIBIOTICS
Introduction
Historical Background
Classification
PENCILLINS
Introduction
Classification
Structural Activity Relationship
Mechanism of Action
CEPHALOSPORINS
Introduction
Classification
Mechanism of Action
CARBAPENEMS
Introduction
MONOBACTAMS
Introduction
Key points
Conclcsion
6 beta lactum drugs dental
Beta lactam antibiotics like penicillins, cephalosporins, carbapenems, and monobactams contain a beta-lactam ring. They are bactericidal and work by inhibiting bacterial cell wall synthesis. Penicillins are further divided into narrow and extended spectrum types. Common side effects include hypersensitivity reactions and diarrhea. Beta lactamase inhibitors are often combined with antibiotics to overcome resistance from beta lactamase producing bacteria. Each class of beta lactam antibiotic has varying spectra of activity and therapeutic uses depending on whether they are effective against gram-positive, gram-negative, anaerobic, and multidrug resistant bacteria.
penicillins - power point - History,mechanism of action,classification,chemis...
Antibiotics - Penicillin's - power point - History, mechanism of action, classification, chemistry, SAR, Nomenclature, uses, side effects- Medicinal chemistry.
Prof. P. Ravisankar M. Pharm., Ph.D.
HOD .,
Vignan Pharmacy college
vadlamudi- Guntur-A.P, India.
banuman35@gmail.com
Phone: 0 9059994000
0 9000199106
Antibiotics
Indian Dental Academy: will be one of the most relevant and exciting training center with best faculty and flexible training programs for dental professionals who wish to advance in their dental practice,Offers certified courses in Dental implants,Orthodontics,Endodontics,Cosmetic Dentistry, Prosthetic Dentistry, Periodontics and General Dentistry.
Chopramphenicol
This document discusses the pharmacokinetics of the antibiotic chloramphenicol. It is well absorbed in the gastrointestinal tract and widely distributed throughout the body, including into the central nervous system. It is metabolized in the liver. Chloramphenicol is effective against both gram-positive and gram-negative bacteria but has more effect on gram-negatives. Its uses are now limited due to its toxicity, especially in newborn infants where it can cause a potentially fatal gray baby syndrome.
Clacef( Cefuroxime + Clavulanic Acid) presentation
This document provides information about the antibiotic Clacef® tablet, which combines cefuroxime and clavulanic acid. It discusses how antibiotics and cephalosporins work, the issues of antibiotic resistance from beta-lactamase enzymes, and how clavulanic acid helps restore the efficacy of cefuroxime by inhibiting these enzymes. The document then reviews the indications, dosage, and competition of Clacef® tablet before outlining the launch and marketing strategy to target physicians and gain market share.
LECTURES SERIES ESBLs
This document provides an overview of extended-spectrum beta-lactamases (ESBLs). It discusses the development of beta-lactam antibiotics and the emergence of antibiotic resistance. ESBLs are beta-lactamase enzymes that can hydrolyze and provide resistance to penicillins, cephalosporins, and aztreonam but not carbapenems. The major types of ESBLs are TEM, SHV, and CTX-M. Laboratories can detect ESBL production phenotypically by looking for increased antibiotic resistance or synergy between cephalosporins and clavulanic acid. Accurate detection of ESBLs is important for appropriate antibiotic treatment of
Pharmacy Industrial Report By Praveen Singh B.phrma final year
Report On Industrial Visit by
B.Pharma final year students
B.pharmacy report..
1.Brooks, Baddi, Himachal Pradesh
2. Helios-II Baddi, Himachal Pradesh
Antibiotic in endodontic
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
Introducing new generic medicine on reimbursement list and influence over HIF...
This document discusses the introduction of a generic form of amoxicillin/clavulanic acid to the Macedonian market and its impact on healthcare spending. It provides background on Macedonia's healthcare system and reimbursement process. Data shows that after the generic's introduction, spending on amoxicillin/clavulanic acid and the overall healthcare budget increased year-over-year as usage of the generic form rose significantly. The study concludes that introducing new generic medicines can lead to higher spending on the relevant drug category and impact the overall healthcare budget.
Mechanisms of Resistance to Antibiotics
1. Antimicrobial resistance arises through genetic mutations and the acquisition of resistance genes from other bacteria.
2. Resistance genes can be acquired horizontally via mobile genetic elements such as plasmids, leading to rapid spread.
3. Common resistance mechanisms include enzymatic inactivation of antibiotics, modification or protection of antibiotic targets, and efflux pumps that pump out antibiotics.
Viewers also liked (20)
SULBACTAM -BETALACTAMASE INHIBITOR,INTRODUCTION,MECHANISM OF ACTION,SAR,SYNTH...
SULBACTAM -BETALACTAMASE INHIBITOR,INTRODUCTION,MECHANISM OF ACTION,SAR,SYNTH...
penicillins - power point - History,mechanism of action,classification,chemis...
penicillins - power point - History,mechanism of action,classification,chemis...
Clacef( Cefuroxime + Clavulanic Acid) presentation
Clacef( Cefuroxime + Clavulanic Acid) presentation
Pharmacy Industrial Report By Praveen Singh B.phrma final year
Pharmacy Industrial Report By Praveen Singh B.phrma final year
Introducing new generic medicine on reimbursement list and influence over HIF...
Introducing new generic medicine on reimbursement list and influence over HIF...
Similar to Beta lactamase inhibitors－fx
Beta lactamase inhibitors
Strategies to overcome β-lactamase sensitivity, Mechanism based inhibition of Beta-lactamases, Carbapenems
BLG_fin
Beta-lactamase is an enzyme produced by bacteria that provides resistance to beta-lactam antibiotics like penicillin. It does this by hydrolyzing the beta-lactam ring structure in these antibiotics, rendering them ineffective. The document discusses the classification, mechanism of action, and applications of beta-lactamase. It describes how beta-lactamase is used to inactivate beta-lactam antibiotics in blood cultures and antibiotic assays to prevent false negative results. Protocols are provided for using beta-lactamase in blood cultures and aminoglycoside antibiotic assays.
Monobactum
Sulfazecin, SAR, Aztreonam, Structure Similarity to beta lactams, antibacterial, resistant to β-lactamases, Gram-positive or anaerobic bacteria
β- Lactam Antibiotics Renaissance
The document discusses β-lactam antibiotics, which contain a β-lactam ring and include penicillins, cephalosporins, monobactams, and carbapenems. It notes that β-lactam antibiotics are active against both gram-positive and gram-negative bacteria but that bacteria have developed resistance through β-lactamase production and other mechanisms. Newer β-lactam antibiotics combined with β-lactamase inhibitors are effective against drug-resistant pathogens. Several newer combinations of β-lactam antibiotics and inhibitors approved or in development are described.
beta lactamase inhibitors from beta lacatum antibiotics
Beta lactamase inhibitors such as clavulanic acid, sulbactam, tazobactam, and avibactam work to inhibit beta-lactamase enzymes produced by bacteria that provide resistance to beta-lactam antibiotics like penicillins. They bind to and inactivate the beta-lactamase enzymes, restoring the effectiveness of beta-lactam antibiotics. These inhibitors are often combined with antibiotics like amoxicillin, piperacillin, and ceftazidime to treat bacterial infections that have developed resistance due to beta-lactamase enzyme production. The combinations expand the antibiotic spectrum and are used for various infections including skin, respiratory, ur
Beta lactamase inhibitors
Beta lactamase inhibitors such as clavulanic acid, sulbactam, tazobactam, and avibactam work to inhibit beta-lactamase enzymes produced by bacteria that provide resistance to beta-lactam antibiotics like penicillins. They bind to and inactivate the beta-lactamase enzymes. When combined with beta-lactam antibiotics, the inhibitors can help the antibiotics overcome resistance and be effective against infections. Common combinations include amoxicillin-clavulanic acid, piperacillin-tazobactam, and ceftazidime-avibactam which are used to treat a variety of bacterial infections.
Similar to Beta lactamase inhibitors－fx (7)
beta lactamase inhibitors from beta lacatum antibiotics
beta lactamase inhibitors from beta lacatum antibiotics
More from Fei Xiang
Epigenetics and small molecule
This document summarizes recent developments in small molecule epigenetic drugs. It discusses four DNA methyltransferase (DNMT) inhibitors approved by the FDA, including Vidaza and Decitabine. It also discusses two histone deacetylase (HDAC) inhibitors approved, Vorinostat and Romidepsin. Other epigenetic targets discussed include Sirtuins, histone methyltransferases, and protein arginine methyltransferases. The document reviews the development stages of small molecules related to epigenetics and their role in disease development and progression. It provides examples of epigenetic targets disrupted in cancer and structures of common HDAC and other epigenetic inhibitors. In conclusion, it states that HDAC inhibitors
Xu wenting
This study aimed to develop folate-tethered mucoadhesive liposomes containing a polymeric drug to improve gastrointestinal absorption. The approaches tested were: 1) Increasing liposomal membrane rigidity using DSPC vs EPC liposomes, 2) Increasing mucoadhesion by coating liposomes with chitosan, and 3) Enhancing intestinal absorption through the folate transport system using folate-PEG. DSPC liposomes significantly increased drug retention in the intestinal mucosa and blood concentration compared to EPC liposomes. Chitosan coating did not increase mucoadhesion, possibly due to increased liposome size and fragility. Modification with folate did not increase intestinal absorption through the
Yuanyue
A study developed a delivery system for the anticancer drug daunorubicin using a dendrimer-drug conjugate. A poly(amidoamine) dendrimer was synthesized and conjugated to daunorubicin through a folic acid linker. Characterization with NMR, mass spectrometry, and HPLC confirmed successful synthesis. In vitro cytotoxicity tests on KB cells showed the conjugate was more effective against folate receptor-positive cancer cells than free daunorubicin. Further studies are needed to evaluate anticancer activity in enzyme-containing systems and in vivo, as well as study the kinetics of daunorubicin release from the dendrimer.
Reginal absorbtion of fexofenadin
This document summarizes a study on the regional absorption of the drug fexofenadine in the small intestine. Drug absorption is influenced by solubility, charge, metabolism, and interaction with export proteins like P-glycoprotein (Pgp). The study found that fexofenadine absorption was reduced in the distal small intestine due to higher Pgp expression levels. Pgp expression inversely correlated with absorption of fexofenadine across the intestinal epithelium. Additionally, mRNA expression of organic anion transporting polypeptides oatp1a5 and oatp2b1, which transport fexofenadine, increased along the small intestine.
Tributyrin against melanoma
Tributyrin against Melanoma is my presentation on 4/2/2011 lab meeting.
Discuss what is tributytin and melanoma
Wenting ppt
This document summarizes research on the interaction between chitosan-modified particles and mucin-coated surfaces. Chitosan-modified cubosome particles were prepared and characterized, with mean particle size increasing after chitosan modification, indicating chitosan binding to the surface. Zeta potential measurements showed the modified particles have a neutral charge at pH 7. Interactions with mucin-coated silica surfaces showed higher adsorption of modified particles at pH 4 and 6 compared to unmodified particles, due to stronger electrostatic interactions. Control experiments indicated chitosan can adsorb from solution onto silica surfaces, reducing binding of modified particles. The modified particles showed substantial irreversible adsorption to mucin surfaces.
Centrifugation sunwei 2011.3.17
Centrifugation is a process that uses centrifugal force to separate mixtures based on density. There are different types of centrifuges that vary in maximum speed and application. Desktop centrifuges have the lowest maximum speed below 3000rpm, while ultracentrifuges can reach speeds over 75,000rpm. Centrifuges consist of major components including a drive system, temperature control, vacuum system, and rotors. Common applications include sedimentation velocity, which separates based on size, shape, and density over short times, and sedimentation equilibrium, which separates based on density differences after prolonged high-speed centrifugation.
More from Fei Xiang (8)
Beta lactamase inhibitors－fx
- 2. contents Clavulanicacid: a beta-lactamase inhibitor combined with penicillin group antibiotics to overcome certain types of antibiotic resistance. Tazobactam Sulbactam Oxapenem NXL 104 BAL 30376 LK-157 BLI-489 CP3242 SA-1-204
- 3. Clavulanicacid Natural product of Streptomyces clavuligerus Prevent the destruction of substrates of enzymes Clavulanic acid + TEM-2-β-lactamases=acyl enzyme yield a transiently inhibited form act as enzyme-substrate complex
- 4. Tazobactam Inhibitory activity of CTX-M type β-lactamases: Tazobactam > clavulanic acid (10-fold) SHV-1- tazobactam complex acyclic form of tazobactam attached to Ser70 acyclic form of 5-atom vinyl carboxylic acid fragment attached to Ser130-OH in the inactive species. Acylation of Ser130Gly β-lactamase by Tazobactam inactivation proceeds independent of any additional covalent interaction
- 5. Sulbactam Clavulanicacid = Sulbactam Cephalosporinases< penicillinases or broad-spectrum β-lactamases However, the enzyme classes was not as great as observed with clavulanic acid sulbactam > cephalosporinases > clavulanicacid In extensive studies: E. coli TEM-2 β-lactamase hydrolysis of sulbactam observed Sulbactam able to inhibit the most common forms of β-lactamase not able to interact with AmpCcephalosporinase
- 6. Oxapenem Oxygen-containing ring fused to β-lactam ring found to be potent β-lactamase inhibitor but have poor stability Oxapenems reduced MICs for ceftazidime against class C hyperprodut Ceftazidime+AM-112 ->ESBL producing E. coli strains AM-114 and AM-115->class A enzymes AM-113 and AM-114->class C enzymes
- 7. NXL 104 NXL 104 and ceftazidime ->class A and class C- producing Enterobacteriaceae members MICs of ceftazidime/AVE 1330 A for Enterobacteriaceae were at least eight fold lower than those of ceftazidime alone
- 8. BAL 30376 BAL 30376 a novel beta-lactamase inhibitor a combinationofBAL 0019764 BAL 30376-f and BAL30376-v more active against MDR K.Pneumoniaecompared to Cefepime but slightly less active than imipenem. Good activity against Enterobacteriaceae non-fermentive Gram-negative bacteria
- 9. LK-157 LK-157 + cefotaxime or cefepime= activity found comparable to that of tazobactam LK-157 decreased the MICs of aztreonam, ceftazidime, and cefuroxime B. fragilis (8- to ≥128-fold) β-lactamase-producing Enterobacteriaceae members (up to ≥64-fold)
- 10. BLI-489 BLI-489 is activity against molecular class A or D enzymes Piperacillin/BLI-489 combination showed potent in vitro activity against diverse β-lactamase producers
- 11. CP3242 Metallo- β-lactamase (MBL) inhibitor and competitively inhibits both IMP-1 and VIM-2 Lowered the MICs of β-lactams against MBL-producing E. coli transformants Novel competitive MBL inhibitor can be effective against MBL-producers in combination with β-lactam antibiotics
- 12. SA-1-204 Effective against SHV producingE. coli strains piperacillin/SA-1-204 was more potent than piperacillin/ tazobactam against strains bearing blaSHV-1
- 13. Thank you for your patient Any Question
Editor's Notes
- A beta-lactamase inhibitor is a drug given in conjunction with a beta-lactam antibiotic. Although the inhibitor does not usually have significant antibiotic activity on its own,[1] it inhibits activity of beta-lactamase, a protein that confers resistance of beta-lactam antibiotics to bacteria.Beta-lactamase inhibitors in clinical use include clavulanic acid and its potassium salt (usually combined with amoxicillin or ticarcillin), sulbactam and tazobactam.