This document discusses different classes of beta-lactam antibiotics including cephalosporins, monobactams, and carbapenems. It describes the chemistry, mechanisms of action, spectra of activity, pharmacokinetics, uses, and adverse effects of various drugs within each class. First, second, third, fourth, and fifth generation cephalosporins are compared in terms of their antimicrobial spectra and examples are provided. Monobactams such as aztreonam are noted to have activity against aerobic gram-negative rods. Carbapenems like imipenem and meropenem have broad-spectrum gram-positive and gram-negative activity including anaerobes.
Pharmacology of cephalosporins, monobactums and carbapenums including their mechanism of action, indications, adverse effects.
The various generations of cephalosporins and their spectrum of action
002. Cephalosporins for students 2023 Prof. P. Ravisankar.pdfDr. Ravi Sankar
Cephalosporins, Why Cephalosporins? Advantages of cephalosporins over penicillin, Mechanism of action of cephalosporins, Classification of cephalosporins, Structures of some important cephalosporins and cephamycins, Oximinocephalosporins, SAR of cephalosporins,Hydrolytic reactions, degradation and stability of cephalosporins, Uses of cephalosporins, Comparison between 6-APA and 7-ACA and penam and cepham.
The current slide include the pharmacology og cephalosporins.
Contents
Introduction to Cephalosporins
Classification of Cephalosporins
Cefazolin
Cephalexin
Cefuroxime
Cefuroxime axetil
Cefotaxime
Cefixime
Cefpodoxime proxetil
Cefepime
Adverse effects of Cephalosporins
Uses of Cephalosporins
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
Pharmacology of cephalosporins, monobactums and carbapenums including their mechanism of action, indications, adverse effects.
The various generations of cephalosporins and their spectrum of action
002. Cephalosporins for students 2023 Prof. P. Ravisankar.pdfDr. Ravi Sankar
Cephalosporins, Why Cephalosporins? Advantages of cephalosporins over penicillin, Mechanism of action of cephalosporins, Classification of cephalosporins, Structures of some important cephalosporins and cephamycins, Oximinocephalosporins, SAR of cephalosporins,Hydrolytic reactions, degradation and stability of cephalosporins, Uses of cephalosporins, Comparison between 6-APA and 7-ACA and penam and cepham.
The current slide include the pharmacology og cephalosporins.
Contents
Introduction to Cephalosporins
Classification of Cephalosporins
Cefazolin
Cephalexin
Cefuroxime
Cefuroxime axetil
Cefotaxime
Cefixime
Cefpodoxime proxetil
Cefepime
Adverse effects of Cephalosporins
Uses of Cephalosporins
synthetic antimicrobials having a quinolone structure that are active primarily against gram-negative bacteria, though newer fluorinated compounds also inhibit gram-positive ones.
β-lactam antibiotics are antibiotics that contain a beta-lactam ring in their chemical structure. This includes penicillin derivatives, cephalosporins and cephamycins, monobactams, carbapenems.
7-aminocephalosporanic acid has been modified by addition of different side chains to create a whole family of cephalosporin antibiotics.
these have been conventionally divided into 5 generations
Mechanism of action
All cephalosporins are bactericidal.
As penicillin it also inhibit the synthesis of bacterial cell wall and causing rapid cell lysis.
Inhibition of transpeptidation (Transpeptidase enzymes then cross-link the chains to provide strength to the cell wall and enable the bacterium to resist osmotic lysis)
Imperfect cell wall
Osmotic drive
Activation of autolysin enzymes
Lysis of bacteria
BACTERICIDAL
CLASSIFICATION
Based on
antimicrobial spectrum
Chronological sequence of development
Divided into generations.
First-generation agents
Cephalexin (O)
Cefadroxil (O)
Cefazolin (i.m, i.v)
Cefalothin (withdrawn)
Exhibit good activity against gram-positive bacteria but modest activity against gram negative organisms.
Most gram-positive cocci
Strepto,
Pneumo,
Methicillin sens. Staph. are susceptible to first-generation cephalosporins
Modest activity against E. coli, K. pneumoniae & Proteus mirabilis
Second-generation agents
Cefaclor (O)
Ceforanide
Cefuroxime (i.m , i.v)
Cefoprozil
Exhibit somewhat increased activity against gram negative organisms,
but much less active than third generation agents.
Less active against gram positive cocci & bacilli compared to first gen. drugs.
Use declined
Clinically replaced by 3rd & 4th generation drugs .
Third-generation agents
Cefotaxime
Ceftriaxone
Cefdinir
Cefibuten
Cefpodoxime
Ceftizoxime
Ceftazidime
Cefoperazone (withdrawn)
Highly augmented activity against gram-negative organisms
Less active than first generation agents against gram positive cocci & anaerobes.
All are highly resistant to β-lactamases from gram negative bacteria.
Some inhibit psuedomonas as well; ceftazidime, cefoperazone(withdrawn)
Some members of this group have enhanced ability to cross the blood-brain barrier eg. Ceftriaxone and are effective in treating meningitis caused by pneumococci, meningococci, H. influenzae and susceptible gram negative rods.
Fourth-generation agents
Cefpirome (im/iv)
Cefepime (iv)
Cefozopran (im)
Highly active against G –ve organisms
Similar to third gen drugs for g +ve bacteria
The fourth generation drugs comparable to third generation but more resistant to hydrolysis by β-lactamases.
Effective against bacterial infections resistant to earlier drugs
Fifth-generation agents
Ceftobiprole
Ceftaroline
Active against, g +ve cocci especially MRSA (Methicillin-resistant Staphylococcus aureus) It's tougher to treat than most strains of staphylococcus aureus -- or staph -- because it's resistant to some commonly used antibiotics.
penicillin resistant S. pneumoniae and enterococci
Adverse reactions
Pain after im injection
Thrombophlebitis of injected vein.
Diarrhoea more common with
oral Ceferadine
P/E Cefoperazone (Banned)
ARTIFICIAL INTELLIGENCE IN HEALTHCARE.pdfAnujkumaranit
Artificial intelligence (AI) refers to the simulation of human intelligence processes by machines, especially computer systems. It encompasses tasks such as learning, reasoning, problem-solving, perception, and language understanding. AI technologies are revolutionizing various fields, from healthcare to finance, by enabling machines to perform tasks that typically require human intelligence.
The prostate is an exocrine gland of the male mammalian reproductive system
It is a walnut-sized gland that forms part of the male reproductive system and is located in front of the rectum and just below the urinary bladder
Function is to store and secrete a clear, slightly alkaline fluid that constitutes 10-30% of the volume of the seminal fluid that along with the spermatozoa, constitutes semen
A healthy human prostate measures (4cm-vertical, by 3cm-horizontal, 2cm ant-post ).
It surrounds the urethra just below the urinary bladder. It has anterior, median, posterior and two lateral lobes
It’s work is regulated by androgens which are responsible for male sex characteristics
Generalised disease of the prostate due to hormonal derangement which leads to non malignant enlargement of the gland (increase in the number of epithelial cells and stromal tissue)to cause compression of the urethra leading to symptoms (LUTS
Recomendações da OMS sobre cuidados maternos e neonatais para uma experiência pós-natal positiva.
Em consonância com os ODS – Objetivos do Desenvolvimento Sustentável e a Estratégia Global para a Saúde das Mulheres, Crianças e Adolescentes, e aplicando uma abordagem baseada nos direitos humanos, os esforços de cuidados pós-natais devem expandir-se para além da cobertura e da simples sobrevivência, de modo a incluir cuidados de qualidade.
Estas diretrizes visam melhorar a qualidade dos cuidados pós-natais essenciais e de rotina prestados às mulheres e aos recém-nascidos, com o objetivo final de melhorar a saúde e o bem-estar materno e neonatal.
Uma “experiência pós-natal positiva” é um resultado importante para todas as mulheres que dão à luz e para os seus recém-nascidos, estabelecendo as bases para a melhoria da saúde e do bem-estar a curto e longo prazo. Uma experiência pós-natal positiva é definida como aquela em que as mulheres, pessoas que gestam, os recém-nascidos, os casais, os pais, os cuidadores e as famílias recebem informação consistente, garantia e apoio de profissionais de saúde motivados; e onde um sistema de saúde flexível e com recursos reconheça as necessidades das mulheres e dos bebês e respeite o seu contexto cultural.
Estas diretrizes consolidadas apresentam algumas recomendações novas e já bem fundamentadas sobre cuidados pós-natais de rotina para mulheres e neonatos que recebem cuidados no pós-parto em unidades de saúde ou na comunidade, independentemente dos recursos disponíveis.
É fornecido um conjunto abrangente de recomendações para cuidados durante o período puerperal, com ênfase nos cuidados essenciais que todas as mulheres e recém-nascidos devem receber, e com a devida atenção à qualidade dos cuidados; isto é, a entrega e a experiência do cuidado recebido. Estas diretrizes atualizam e ampliam as recomendações da OMS de 2014 sobre cuidados pós-natais da mãe e do recém-nascido e complementam as atuais diretrizes da OMS sobre a gestão de complicações pós-natais.
O estabelecimento da amamentação e o manejo das principais intercorrências é contemplada.
Recomendamos muito.
Vamos discutir essas recomendações no nosso curso de pós-graduação em Aleitamento no Instituto Ciclos.
Esta publicação só está disponível em inglês até o momento.
Prof. Marcus Renato de Carvalho
www.agostodourado.com
Title: Sense of Taste
Presenter: Dr. Faiza, Assistant Professor of Physiology
Qualifications:
MBBS (Best Graduate, AIMC Lahore)
FCPS Physiology
ICMT, CHPE, DHPE (STMU)
MPH (GC University, Faisalabad)
MBA (Virtual University of Pakistan)
Learning Objectives:
Describe the structure and function of taste buds.
Describe the relationship between the taste threshold and taste index of common substances.
Explain the chemical basis and signal transduction of taste perception for each type of primary taste sensation.
Recognize different abnormalities of taste perception and their causes.
Key Topics:
Significance of Taste Sensation:
Differentiation between pleasant and harmful food
Influence on behavior
Selection of food based on metabolic needs
Receptors of Taste:
Taste buds on the tongue
Influence of sense of smell, texture of food, and pain stimulation (e.g., by pepper)
Primary and Secondary Taste Sensations:
Primary taste sensations: Sweet, Sour, Salty, Bitter, Umami
Chemical basis and signal transduction mechanisms for each taste
Taste Threshold and Index:
Taste threshold values for Sweet (sucrose), Salty (NaCl), Sour (HCl), and Bitter (Quinine)
Taste index relationship: Inversely proportional to taste threshold
Taste Blindness:
Inability to taste certain substances, particularly thiourea compounds
Example: Phenylthiocarbamide
Structure and Function of Taste Buds:
Composition: Epithelial cells, Sustentacular/Supporting cells, Taste cells, Basal cells
Features: Taste pores, Taste hairs/microvilli, and Taste nerve fibers
Location of Taste Buds:
Found in papillae of the tongue (Fungiform, Circumvallate, Foliate)
Also present on the palate, tonsillar pillars, epiglottis, and proximal esophagus
Mechanism of Taste Stimulation:
Interaction of taste substances with receptors on microvilli
Signal transduction pathways for Umami, Sweet, Bitter, Sour, and Salty tastes
Taste Sensitivity and Adaptation:
Decrease in sensitivity with age
Rapid adaptation of taste sensation
Role of Saliva in Taste:
Dissolution of tastants to reach receptors
Washing away the stimulus
Taste Preferences and Aversions:
Mechanisms behind taste preference and aversion
Influence of receptors and neural pathways
Impact of Sensory Nerve Damage:
Degeneration of taste buds if the sensory nerve fiber is cut
Abnormalities of Taste Detection:
Conditions: Ageusia, Hypogeusia, Dysgeusia (parageusia)
Causes: Nerve damage, neurological disorders, infections, poor oral hygiene, adverse drug effects, deficiencies, aging, tobacco use, altered neurotransmitter levels
Neurotransmitters and Taste Threshold:
Effects of serotonin (5-HT) and norepinephrine (NE) on taste sensitivity
Supertasters:
25% of the population with heightened sensitivity to taste, especially bitterness
Increased number of fungiform papillae
Prix Galien International 2024 Forum ProgramLevi Shapiro
June 20, 2024, Prix Galien International and Jerusalem Ethics Forum in ROME. Detailed agenda including panels:
- ADVANCES IN CARDIOLOGY: A NEW PARADIGM IS COMING
- WOMEN’S HEALTH: FERTILITY PRESERVATION
- WHAT’S NEW IN THE TREATMENT OF INFECTIOUS,
ONCOLOGICAL AND INFLAMMATORY SKIN DISEASES?
- ARTIFICIAL INTELLIGENCE AND ETHICS
- GENE THERAPY
- BEYOND BORDERS: GLOBAL INITIATIVES FOR DEMOCRATIZING LIFE SCIENCE TECHNOLOGIES AND PROMOTING ACCESS TO HEALTHCARE
- ETHICAL CHALLENGES IN LIFE SCIENCES
- Prix Galien International Awards Ceremony
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2. Chemistry of Cephalosporins
• Semi-Synthetic
antibiotics derived
from
“Cephalosporium-C”
Obtained from fungus
Cephalosporium
3. • It belongs to β-lactam antibiotics
• It is similar in structure to penicillin
• β-lactam is common for both penicillin as well
as Cephalsporins
• Depending on the various substitution of
chemical group
i. Pk
ii. Anti bacterial spectrum
iii. Stability
4.
5. • Inhibit wide variety of gram(+) and gram(-)
bacteria.
• Acquired resistance is due to
a) Alteration in target protein (PBPs) reducing
affinity for the antibiotic
b) Impermeability to the antibiotic or its efflux
pump
c) Elaboration of β-lactamases which destroy
specific cephalosporins (Cephalosporinases) the
MOST COMMON MECHANISM
8. First Generation
Cephalosporins
• 1st Generation were developed in 1960s
• Highly active against gram(+) but weak against
gram(-) bacteria.
• Parenteral – Cefazolin
• Oral – Cephalexin
- Cefadroxil
9. Cefazolin
• It is the Prototype first generation that is active
against most PnG sensitive Organisms
• Streptococci
• Gonococci
• Meningiococci
• C.diptheriae
• H.Infuenzae
• Clostridia
• Actinomyces
It is the preferred parenteral
1st Generation
Cephalosporin, esp for
SURGICAL PROPHYLAXIS
11. Second Generation
Cephalosporins
• More active against gram(-) organisms with
wider coverage , inc some strains resistant to
first generation cephalosporins
• Parenteral – Cefuroxime
• Oral- Cefaclor , Cefuroxime axetil, Cefprozil
12. 2nd Gen .Parenteral – Cefuroxime
• This group of drugs is less active against gram
positive organisms than first generation
agents
• But has extended gram negative coverage.
• Cefuroxime attains higher CSF levels as
compared to other second generation
cephalosporins.
13. Spectrum
Second Gram –ve bacilli
• E. coli
• Klebsiella
• Proteus
• H. influenza
• M. catarrhalis
• Bacteroides
14. Third generation Cephalosporins
• It is active against gram(+) cocci , gram(-)
cocci, gram(-) bacilli , anaerobs
• Parentral – Cefotaxime , Ceftizoxime,
Ceftriaxone , Ceftazidime, Cefoperazone
• Oral – Cefixime , Cefpodoxime
proxetil,Cefdinir,Ceftibuten,Ceftamet pivoxil
15. 3rd generation spectrum
Gram +ve cocci
• Streptococci
• Staphylococci
Gram –ve cocci
• Gonococci
Gram –ve bacilli
• Enterobacteriaceae
• Serratia
• Pseudomonas
Anaerobes
• Bacteroides
Only ceftazidime and cefoperazone
are effective against Pseudomonas
16. • Active against gram (-) organisms resistant to
other beta lactam antibiotics.
• penetrate the blood brain barrier (except
cefoperazone and cefixime).
• Ceftazidime (maximum), ceftolozane and
cefoperazone are active against
pseudomonas.
• Ceftazidime is drug of choice for melioidiosis
(caused by Burkholderia pseudomallei).
17. • Ceftizoxime has maximum activity against
Bacteroides.
• Ceftriaxone is the first choice drug for
gonorrhoea, salmonellosis (including
typhoid), E. coli sepsis, Proteus, and empirical
therapy for bacterial meningitis.
18. Fourth Generation Cephalosporins
• These drugs possess activity against gram (-)
organisms (including pseudomonas) resistant
to 3rd generation cephalosporins.
• Their efficacy against gram positive cocci is
similar to 3rd generation compounds.
• However, these are not active against
anaerobes.
20. Newer Drugs
• Fifth generation cephalosporins
• Only Parenteral – Ceftaroline fosamil &
Ceftobiprole medocaril
• It is active against MRSA & penicillin resistance
(PBP altered)
• Ceftaroline fosamil – Prodrug
• Rapidly converted by Phosphatases to the
active Ceftaroline
21. Ceftaroline fosamil
• Inhibit wide variety of gram(+) and gram(-)
bacteria.
• MRSA
• Penicillin resistant Strep. Pneumoniae &
Enterococcus fecalis
• Ceftaroline – ability to bind to altered PBPs
expressed in theses bacteria
22. • It has high affinity for
• PBP2a (in MRSA)
• PBP2b and PBP2x (in penicillin resistant
Strep.Pneumonia)
• M.O.A- interferes with transpeptidation step
of bacterial cell wall synthesis- lethal effect
23. • Ceftaroline fosamil approved by CDSCO india in
2016 ,
• For the treatment of complicated skin and soft
tissue infection as well as community acquired
pneumonia(CAP) particularly MRSA & penicillin
resistant Strep.Pneumonia
24. Pharmacokinetics
• Most cephalosporins are excreted via kidney
through tubular secretion.
• Ceftriaxone and cefoperazone are secreted in
the bile.
• Nephrotoxicity of these drugs is increased with
loop diuretics.
25. Adverse effects
• PAIN – at the site of injection (IM) ,
Thrombophlebitis (IV)
• DIARRHOEA- due to altered Gut flora
• HYPERSENSITIVEITY REACTION – most
important adverse effect similar to penicillin
• Rashes(MC),anaphylaxis,angioedema,asthma
and urticaria
27. USES
• As alternative to penicillin for ENT,upper
respiratory and cutaneous infections
• Urinary tract infection & Soft tissue infection
• CAP,HAP
• Complicated skin and soft tissue infection due
to MRSA ( Ceftaroline fosamil)
• Septicaemias
29. Monobactams
• Monocyclic β-lactam ring
• Unique – β-lactam ring is not fused to another
ring
• Drug included in this class- Aztreonam
• Structure similarity to 3rd generation
• Spectrum of activity is similar to 3rd generation
Cephalosporins
30. Spectrum of activity
• Limited to aerobic gram negative rods
• Excellent activity against Enterobacteriaceae.
• Pseudomonas aeruginosa
• No activity against gram positive bacteria or
anaerobes
31. Pharmacokinetics
• Route – IM or IV
• Absorption – poor oral absorbtion
• Rapid and complete absorption after IM inj
• Distribution – Penetrate well into CSF
• Metabolism – Hydrolytic opening of β-lactam
ring
• Elimination – mostly unaltered
32. Pharmacodynamics
• Bactericidal activity
• M.O.A – it binds to Penicillin binding protein-3
(PPB3)
• Uses:
• Safe in patient who have allergy to penicillin
or cephalosporin
• Pneumonia
34. CARBAPENEMS
• Carbapenems are β-Lactams that contains
fused β-Lactam ring system- different from
penicillins
• Group consist of – Imipenem ,
Meropenem,Etrapenem,Faropenem,
Doripenem
35. Imipenem
• Mechanism of Action
• β – lactam antibiotics inhibit the key enzyme
in bacterial wall synthesis ( transpeptidase)
• They also appear to activate one or more cell-
wall autolytic enzymes, causing lysis of the
bacterium
37. Pharmacokinetics
• Not absorbed orally
• So, IV route is used for admistration
• The drug is hydrolyzed rapidly by
Dhydrodipeptidase I found in the brush border
of Proximal renal tuble
• Cilastatin ( reversible inhibitor of
dehydropeptidase I )
• Dose adjustment is needed in renal
insufficiency
38. Adverse effects
• Nause and Vomiting are most common
• Hypersensitivity
• Seizure – 1.5% ( if high dose is given for
patient with CNS lesion)
39. Therapeutic uses
• Urinary tract infection
• Lower respiratory infection
• Intar-abdominal infection
• Gynecological infection
• Skin and soft tissue , bone and joint infections
40. Meropenem
• Newer Carbapenem is not hydrolyzed by Renal
Peptidase
• Like Imipenem it is active against both gram(+)
& garm(-) , aerobes as well as anaerobes
• MEROPENEM is “reserve drug” for the
treatment of serious nosocomial infections like
41. • Septicaemia
• Febrile neutropenia
• Intra-abdominal infection
• Pelvic infection
• Diabetic foot
• ADVERSE EFFECTS are similar to imepenem ,
but it is less likely to cause seizure, therefore
preferred over imipenem-cilastatin.
42. Tutorial Questions
1. Cephaloxin Vs Cefadroxil.
2. Name the Cephalosporins used in PPNG (Penicilinase
producing Neisseria Gonorrhoea).
3. Ceftriaxone Vs Cefotaxime.
4. Name the Cephalosporins used in Pseudo monas infection.
5. Name the Cephalosporins used in MDR (Multi Drug Resistant)
typhoid fever ?
6. Which is highly nephrotoxic Cephalosporins.
7. Name the Cephalosporins used in menigitis caused by gram –
ve bacilli.
8. Orally active Cephalosporins.
9. 4th Generation Cephalosporins – Advantages.
10. What are the common adverse effects ?
11. What are the common uses of cephato sporins ? what are the
specific reasons for their prescription.