Fluoroquinolones are a class of synthetic antibacterial agents that are effective against both Gram-negative and Gram-positive bacteria. They work by inhibiting the enzymes DNA gyrase and topoisomerase IV, which prevents bacterial DNA from unwinding and duplicating. Resistance to fluoroquinolones can occur via mutations in these target enzymes or by reducing drug accumulation in bacteria through efflux pumps or changes to membrane permeability.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
International Journal of Pharmaceutical Science Invention (IJPSI) is an international journal intended for professionals and researchers in all fields of Pahrmaceutical Science. IJPSI publishes research articles and reviews within the whole field Pharmacy and Pharmaceutical Science, new teaching methods, assessment, validation and the impact of new technologies and it will continue to provide information on the latest trends and developments in this ever-expanding subject. The publications of papers are selected through double peer reviewed to ensure originality, relevance, and readability. The articles published in our journal can be accessed online.
Literature Survey Antibiotic ResistanceTuhin Samanta
Anti-toxin obstruction happens when microscopic organisms change in light of the utilization of these medications. Microscopic organisms, not people or creatures, become anti-toxin safe. These microorganisms may contaminate people and creatures, and the diseases they cause are more diligently to treat than those brought about by non-safe microscopic organisms.
The quinolones are a family of antibiotics containing a bicyclic core structure related to the compound 4-quinolone .
Since their discovery in the early 1960s, they have gained increasing importance as key therapies to treat both community-acquired and severe hospital-acquired infections.
During the 1970s–1980s, the coverage of the quinolone class was expanded by the breakthrough development of fluoroquinolones, which show a much broader spectrum of activity and improved pharmacokinetics compared to the first-generation quinolone.
Those fluoroquinolones, such as ciprofloxacin, are active against both Gram-negative and Gram-positive pathogens; importantly, they are also active against the causative agent of tuberculosis, Mycobacterium tuberculosis.
Quinolones are widely prescribed for several different types of human infections. With side effects including gastrointestinal reactions, CNS reactions, and some minor adverse effects.
DNA Gyrase Inhibitors -quinolones and Fluoroquinolones.pptxVijay Salvekar
DNA gyrase inhibitors of synthetic origin. Fluoroquinolones have been the most successful antibacterial agents targeting DNA gyrase. These compounds have been extensively explored and researched to improve spectrum of activity, potency and bacterial resistance.
To understand the mechanisms of antimicrobial action and the classification of antimicrobial drugs.
To explain the process of microbial resistance.
To understand the spread of resistant microbes.
Outlines the prevention of microbial resistance.
DNA Gyrase Inhibitors -Quinolones,Fluoroquinolones Vijay Salvekar
DNA Gyrase Inhibitors -Quinolones,Fluoroquinolones ,its Structure,Antimicrobial activity ,Mechanism of action,classifications ,Mechanisms of Resistance,Pharmacokinetics,Clinical uses,Adverse effects
Antibiotic resistance A major source of morbidity and mortality worldwide.pptxSmitha Vijayan
Antibiotic resistance is a naturally occurring process.
However, increases in antibiotic resistance are driven by a combination of germs exposed to antibiotics, and the spread of those germs and their resistance mechanisms
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Literature Survey Antibiotic ResistanceTuhin Samanta
Anti-toxin obstruction happens when microscopic organisms change in light of the utilization of these medications. Microscopic organisms, not people or creatures, become anti-toxin safe. These microorganisms may contaminate people and creatures, and the diseases they cause are more diligently to treat than those brought about by non-safe microscopic organisms.
The quinolones are a family of antibiotics containing a bicyclic core structure related to the compound 4-quinolone .
Since their discovery in the early 1960s, they have gained increasing importance as key therapies to treat both community-acquired and severe hospital-acquired infections.
During the 1970s–1980s, the coverage of the quinolone class was expanded by the breakthrough development of fluoroquinolones, which show a much broader spectrum of activity and improved pharmacokinetics compared to the first-generation quinolone.
Those fluoroquinolones, such as ciprofloxacin, are active against both Gram-negative and Gram-positive pathogens; importantly, they are also active against the causative agent of tuberculosis, Mycobacterium tuberculosis.
Quinolones are widely prescribed for several different types of human infections. With side effects including gastrointestinal reactions, CNS reactions, and some minor adverse effects.
DNA Gyrase Inhibitors -quinolones and Fluoroquinolones.pptxVijay Salvekar
DNA gyrase inhibitors of synthetic origin. Fluoroquinolones have been the most successful antibacterial agents targeting DNA gyrase. These compounds have been extensively explored and researched to improve spectrum of activity, potency and bacterial resistance.
To understand the mechanisms of antimicrobial action and the classification of antimicrobial drugs.
To explain the process of microbial resistance.
To understand the spread of resistant microbes.
Outlines the prevention of microbial resistance.
DNA Gyrase Inhibitors -Quinolones,Fluoroquinolones Vijay Salvekar
DNA Gyrase Inhibitors -Quinolones,Fluoroquinolones ,its Structure,Antimicrobial activity ,Mechanism of action,classifications ,Mechanisms of Resistance,Pharmacokinetics,Clinical uses,Adverse effects
Antibiotic resistance A major source of morbidity and mortality worldwide.pptxSmitha Vijayan
Antibiotic resistance is a naturally occurring process.
However, increases in antibiotic resistance are driven by a combination of germs exposed to antibiotics, and the spread of those germs and their resistance mechanisms
Lung Cancer: Artificial Intelligence, Synergetics, Complex System Analysis, S...Oleg Kshivets
RESULTS: Overall life span (LS) was 2252.1±1742.5 days and cumulative 5-year survival (5YS) reached 73.2%, 10 years – 64.8%, 20 years – 42.5%. 513 LCP lived more than 5 years (LS=3124.6±1525.6 days), 148 LCP – more than 10 years (LS=5054.4±1504.1 days).199 LCP died because of LC (LS=562.7±374.5 days). 5YS of LCP after bi/lobectomies was significantly superior in comparison with LCP after pneumonectomies (78.1% vs.63.7%, P=0.00001 by log-rank test). AT significantly improved 5YS (66.3% vs. 34.8%) (P=0.00000 by log-rank test) only for LCP with N1-2. Cox modeling displayed that 5YS of LCP significantly depended on: phase transition (PT) early-invasive LC in terms of synergetics, PT N0—N12, cell ratio factors (ratio between cancer cells- CC and blood cells subpopulations), G1-3, histology, glucose, AT, blood cell circuit, prothrombin index, heparin tolerance, recalcification time (P=0.000-0.038). Neural networks, genetic algorithm selection and bootstrap simulation revealed relationships between 5YS and PT early-invasive LC (rank=1), PT N0—N12 (rank=2), thrombocytes/CC (3), erythrocytes/CC (4), eosinophils/CC (5), healthy cells/CC (6), lymphocytes/CC (7), segmented neutrophils/CC (8), stick neutrophils/CC (9), monocytes/CC (10); leucocytes/CC (11). Correct prediction of 5YS was 100% by neural networks computing (area under ROC curve=1.0; error=0.0).
CONCLUSIONS: 5YS of LCP after radical procedures significantly depended on: 1) PT early-invasive cancer; 2) PT N0--N12; 3) cell ratio factors; 4) blood cell circuit; 5) biochemical factors; 6) hemostasis system; 7) AT; 8) LC characteristics; 9) LC cell dynamics; 10) surgery type: lobectomy/pneumonectomy; 11) anthropometric data. Optimal diagnosis and treatment strategies for LC are: 1) screening and early detection of LC; 2) availability of experienced thoracic surgeons because of complexity of radical procedures; 3) aggressive en block surgery and adequate lymph node dissection for completeness; 4) precise prediction; 5) adjuvant chemoimmunoradiotherapy for LCP with unfavorable prognosis.
Acute scrotum is a general term referring to an emergency condition affecting the contents or the wall of the scrotum.
There are a number of conditions that present acutely, predominantly with pain and/or swelling
A careful and detailed history and examination, and in some cases, investigations allow differentiation between these diagnoses. A prompt diagnosis is essential as the patient may require urgent surgical intervention
Testicular torsion refers to twisting of the spermatic cord, causing ischaemia of the testicle.
Testicular torsion results from inadequate fixation of the testis to the tunica vaginalis producing ischemia from reduced arterial inflow and venous outflow obstruction.
The prevalence of testicular torsion in adult patients hospitalized with acute scrotal pain is approximately 25 to 50 percent
Flu Vaccine Alert in Bangalore Karnatakaaddon Scans
As flu season approaches, health officials in Bangalore, Karnataka, are urging residents to get their flu vaccinations. The seasonal flu, while common, can lead to severe health complications, particularly for vulnerable populations such as young children, the elderly, and those with underlying health conditions.
Dr. Vidisha Kumari, a leading epidemiologist in Bangalore, emphasizes the importance of getting vaccinated. "The flu vaccine is our best defense against the influenza virus. It not only protects individuals but also helps prevent the spread of the virus in our communities," he says.
This year, the flu season is expected to coincide with a potential increase in other respiratory illnesses. The Karnataka Health Department has launched an awareness campaign highlighting the significance of flu vaccinations. They have set up multiple vaccination centers across Bangalore, making it convenient for residents to receive their shots.
To encourage widespread vaccination, the government is also collaborating with local schools, workplaces, and community centers to facilitate vaccination drives. Special attention is being given to ensuring that the vaccine is accessible to all, including marginalized communities who may have limited access to healthcare.
Residents are reminded that the flu vaccine is safe and effective. Common side effects are mild and may include soreness at the injection site, mild fever, or muscle aches. These side effects are generally short-lived and far less severe than the flu itself.
Healthcare providers are also stressing the importance of continuing COVID-19 precautions. Wearing masks, practicing good hand hygiene, and maintaining social distancing are still crucial, especially in crowded places.
Protect yourself and your loved ones by getting vaccinated. Together, we can help keep Bangalore healthy and safe this flu season. For more information on vaccination centers and schedules, residents can visit the Karnataka Health Department’s official website or follow their social media pages.
Stay informed, stay safe, and get your flu shot today!
Couples presenting to the infertility clinic- Do they really have infertility...Sujoy Dasgupta
Dr Sujoy Dasgupta presented the study on "Couples presenting to the infertility clinic- Do they really have infertility? – The unexplored stories of non-consummation" in the 13th Congress of the Asia Pacific Initiative on Reproduction (ASPIRE 2024) at Manila on 24 May, 2024.
- Video recording of this lecture in English language: https://youtu.be/lK81BzxMqdo
- Video recording of this lecture in Arabic language: https://youtu.be/Ve4P0COk9OI
- Link to download the book free: https://nephrotube.blogspot.com/p/nephrotube-nephrology-books.html
- Link to NephroTube website: www.NephroTube.com
- Link to NephroTube social media accounts: https://nephrotube.blogspot.com/p/join-nephrotube-on-social-media.html
Ethanol (CH3CH2OH), or beverage alcohol, is a two-carbon alcohol
that is rapidly distributed in the body and brain. Ethanol alters many
neurochemical systems and has rewarding and addictive properties. It
is the oldest recreational drug and likely contributes to more morbidity,
mortality, and public health costs than all illicit drugs combined. The
5th edition of the Diagnostic and Statistical Manual of Mental Disorders
(DSM-5) integrates alcohol abuse and alcohol dependence into a single
disorder called alcohol use disorder (AUD), with mild, moderate,
and severe subclassifications (American Psychiatric Association, 2013).
In the DSM-5, all types of substance abuse and dependence have been
combined into a single substance use disorder (SUD) on a continuum
from mild to severe. A diagnosis of AUD requires that at least two of
the 11 DSM-5 behaviors be present within a 12-month period (mild
AUD: 2–3 criteria; moderate AUD: 4–5 criteria; severe AUD: 6–11 criteria).
The four main behavioral effects of AUD are impaired control over
drinking, negative social consequences, risky use, and altered physiological
effects (tolerance, withdrawal). This chapter presents an overview
of the prevalence and harmful consequences of AUD in the U.S.,
the systemic nature of the disease, neurocircuitry and stages of AUD,
comorbidities, fetal alcohol spectrum disorders, genetic risk factors, and
pharmacotherapies for AUD.
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Ve...kevinkariuki227
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
TEST BANK for Operations Management, 14th Edition by William J. Stevenson, Verified Chapters 1 - 19, Complete Newest Version.pdf
Pulmonary Thromboembolism - etilogy, types, medical- Surgical and nursing man...VarunMahajani
Disruption of blood supply to lung alveoli due to blockage of one or more pulmonary blood vessels is called as Pulmonary thromboembolism. In this presentation we will discuss its causes, types and its management in depth.
Ozempic: Preoperative Management of Patients on GLP-1 Receptor Agonists Saeid Safari
Preoperative Management of Patients on GLP-1 Receptor Agonists like Ozempic and Semiglutide
ASA GUIDELINE
NYSORA Guideline
2 Case Reports of Gastric Ultrasound
Antibacterial Action Mechanism of Fluoroquinolones.pptx
1. Presentation
on
Anti-bacterial Action Mechanism of
Fluoroquinolones & Resistance Mechanism
Submitted by-
Samad Muhammad Abdus
ID-AM202318003
School of Medicine
Jeju National University
For-
Kang Hee-Kyung
Professor
School of Medicine
Jeju National University
2. Fluoroquinolones:
Fluoroquinolones are an important class of wide-spectrum synthetic antibacterial agents, which kill bacteria
and fight infections. The term quinolone refers to potent synthetic chemtherapeutic antibacterial agent.
Fluoroquinolones contain a fluorine atom in their chemical structure and are effective against both Gram-
negative and Gram-positive bacteria. They are important for treating certain bacterial infections, some of
which may be serious or life-threatening.
This group of antibiotics includes few generation, the examples are given below-
1st Generation: Nalidixic acid, Oxolinic acid, Cinoxacin, Piromidic acid, etc.
2nd Generation: Ciprofloxacin, Lomefloxacin, Norfloxacin, Ofloxacin, etc.
3rd Generation: Levofloxacin, Sparfloxacin, Temafloxacin etc.
4th Generation: Gatifloxacin, Gemifloxacin, Moxifloxacin, etc.
3. Antibacterial action mechanism of Fluoroquinolones:
The fluoroquinolones are the only direct inhibitors of DNA synthesis; by binding to the enzyme-DNA complex,
they stabilize DNA strand breaks created by DNA gyrase and topoisomerase IV. Ternary complexes of drug,
enzyme, and DNA block progress of the replication fork.
Quinolones are chemotherapeutic bactericidal drugs. They interfere with DNA replication by preventing
bacterial DNA from unwinding and duplicating. Specifically, they inhibit the ligase activity of the type II
topoisomerases, DNA gyrase and topoisomerase IV, which cut DNA to introduce supercoiling, while leaving
nuclease activity unaffected.
Inhibition of topoisomerase IV interferes with separation of replicated chromosomal DNA into the
respective daughter cells during cell division.
While all quinolones have activity at both target sites, most have higher affinity for one or the other. This
can explain differences in spectra of activity since DNA gyrase is the primary target for gram-negative
and topoisomerase IV is the primary target for gram-positive organisms.
Whether, Defloxacin has a uniquely balanced affinity for both target sites, which may contribute to its
broader spectrum of activity and reduced likelihood for induction of resistance.
5. Antibacterial action mechanism of Fluoroquinolones (continued):
Quinolones interact with both DNA gyrase, the drug's primary target, and topoisomerase IV, a similar
type II topoisomerase, in order to exert their effects. These 2 enzymes frequently have different
quinolone sensitivity ranges within a single bacterium; typically, DNA gyrase is more sensitive in Gram-
negative bacteria while topoisomerase IV is more sensitive in Gram-positive bacteria. Genetic testing
often identify the more sensitive enzyme as the main medication target, although there are reported,
poorly understood outliers.
Quinolone binding appears to cause modifications in both DNA and the topoisomerase that take place
independently from the DNA cleavage that is the hallmark of quinolone action, leading to the
development of the ternary complex of DNA, DNA gyrase, and either topoisomerase IV or DNA gyrase.
X-ray crystallographic analyses of a gyrase fragment A component has shown regions that are likely to
be quinolone binding sites, as has yeast topoisomerase IV, which has similarity to the subunits of both
DNA gyrase and topoisomerase IV. Nevertheless, to yet, no topoisomerase crystal structures with DNA
and quinolone have been published.
6. Resistance mechanism of Fluoroquinolones:
To counteract the effect of quinolones, bacteria have developed various resistance mechanisms to these
antibiotics. Bacterial resistance to quinolones is mainly based on three points:
1. Chromosomal mutations in coding genes (mutations that alter the objectives of the drug).
2. Mutations associated with the reduction of the intracytoplasmic concentration of quinolones.
3. Producing an Efflux Pump
7. Resistance mechanism of Fluoroquinolones (continued):
Resistance to fluoroquinolones mostly occurs by two mechanisms that are mutations in the both
target enzymes DNA gyrase in Gram-negative bacteria and topoisomerase IV in Gram-positive
bacteria. The second way that reduced accumulation of the fluoroquinolones can occur is through an
efflux system. Resistance is due to increased expression of chromosomal gene leading to increased
efflux of the fluoroquinolones
8. Altered target:
Mutations in the bacterial DNA gyrase and Topoisomerase IV have developed a decreased affinity for
fluoroquinolones. Resistance is frequently associated with mutations in both gyrase and topoisomerase IV.
Decreased accumulation: Reduced intracellular concentration of the drugs in the bacterial cell is linked to
two mechanisms.
One mechanism is associated with an energy-dependent efflux system in the cell membrane.
The other mechanism involves a decreased number of porins in the outer membrane of the resistant cell,
thereby impairing access of the drugs to the intracellular topoisomerases.
Resistance mechanism of Fluoroquinolones (continued):