Overview of antimicrobial agents

Dr. Vasudha Devi

Tips
1. Know basics
A.
B.
C.
D.
E.

Name Gram +ve and ve bacteria

Identify aerobes and anaerobes
Identify intracellular organisms
List the disease caused by important ones
Generally organisms that commonly affect respiratory
tract are aerobes and those cause gynaecological and
lower abdominal infections are anaerobes
F. Gram +ve have thick cell wall: difficult for a drug to cross
this.hence generally drugs those require entry into a
cell for their action ( eg. protein synthesis inhibitors),
mainly act on G ve organisms ( have thin cell wall)
G. All cell wall synthesis inhibitors and drugs that act by
altering the permeability of cell membrane are cidal

Tips- basics
F. All protein synthesis inhibitors are static
accept aminoglycosides
Combination of protein synthesis inhibitors
may be cidal ( cotrimoxazole)
G. If a prototype drug act only on G-ve organism,
the subsequent drugs developed in that class act
on G +ve also and Vice versaexample,
ciprofloxacin acts mainly on G ve organisms,
where as other drugs ( newer) act on G +ve also.

 Drugs having low penetrability, will not act on

intracellular organisms ( like beta lactams have no
action on intracellular pathogens like ligonella,
chlamydia)
Some tables and graphs are very informative and help
you to understand this topicSelected ones are used in
this overview and underlined words are very
important.
You are not required to remember the whole
spectrum. Instead, identify the common uses (
infections) of a particular drug and remember
organism causing that infection

Clinically important bacteria

Gram +ve
Cocci
Staphylococcus
S. aureus
S. epidermidis

Streptococcus
S. pyogenes
S. viridans
S. Pneumoniae

Enterococcus
E. faecalis

Bacilli
Clostridium
C. tetani
C. perfringens
C.difficile
C. botulinum

Corynebacterim diphtheriae
Listeria monocytogenes
Bacillus anthracis

Gram -ve
Cocci

Neisseria
N.gonorrheae
N.menigitidis

Bacilli
Enterobacteriaceae
Escherichia coli
Salmonella typhi
Shigella
Klebsiella
Proteus
Helicobacter pylori
Coliforms
Pseudomonas aeruginosa
Ligionella pneumophilia
Camphylobacter
Vibrio cholerae
Haemophilus influenzae
Bordetella pertussis

others
Spirochetes
Treponema pallidum
Leptospira

Reckettsia
Chlamydiae
(intracellular)
Chlamydia trachomatis
Chlamydia pneumoniae

Mycoplasma pneumoniae
( lack cell wall)
Pnemocystis carini
(Pneumocystis jiroveci)

Diseases caused
S. aureus: abscess (furuncle, carbuncle),
endocarditis, pneumonia
S. epidermidis : skin flora; Biofilm formation on
plastic devices infection
Endocarditis
S. pyogenes: Pharyngitis, sinusitis, otitis media,
rheumatic fever, glomerulonephritis, septicemia
S. viridans: endocarditis, septicemia
S. Pneumoniae: pneumonia, meningitis, sinusitis
E. faecalis: endocarditis, UTI

C. tetani: tetanus
C. perfringens: gas gangrene
C.difficile: pseudomembranous colitis
C. botulinum: food poisoning
All are anaerobic

Corynebacterium diphtheriae (aerobic):

Diphtheria

Escherichia coli: UTI, dysentery

Salmonella typhi: typhoid, food poisoning
Shigella: gastroenteritis, dysentery
Klebsiella: UTI
Proteus: UTI
Helicobacter pylori: peptic ulcer
Coliforms
Pseudomonas aeruginosa: UTI, pneumonia, burn
infection
Vibrio cholerae: Cholera
Hemophilous influenzae: sinusitis, bronchitis,
pneumonia, meningitis

Treponema pallidum: syphilis

Leptospira : leptospirosis
Chlamydia trachomatis: sexually transmitted disease
(lymphogranuloma venereum)

Pneumocystitis carnii: pneumonia in AIDS,

lung infection in immunocompromised

Bactericidal
Penicillins
Cephalosporins
Carbapenems
Monobactams
Vancomycin
Quinolones
Aminoglycosides
Bacitracin
Colistin
Polymyxin B
Cotrimoxazole

Bacteriostatic
Tetracyclines
Sulfonamide
Trimethoprim
Macrolides
Chloramphenicol
Clinidamycin
Lincomycin
Nitrofurantoin
Linezolid
Telithromycin

Betalactams
Inhibition of transpeptidase

Accumulation of precursor cell wall units

Formation of an imperfect cell wall

Activation of cells autolytic enzymes

osmotic drive

Cell lysis

Betalactams
Have different uses
No action on those lack cell wall (mycoplasma)
No action on intracellular pathogens
(ligonella, chlamydia): cannot cross

Penicillins: remember this table (not routes

for all), you can write uses using this

Narrow spectrum penicillins

Pen V and G
Spectrum: all G +ve cocci and bacilli
Spirochetes
No action on staph (produce lactamases)
No action on G ve
lactamase resistant penicillins
Spectrum: Like Pen G + Staph

Extended spectrum penicillins

Spectrum: Pen G + some G -ve: not on Staph
Aminopenicillins:
Polar drugs: diffuse through porin channels
Hence active on G ve cocci and
bacilli (Mainly involved in RTI, UTI and GI infection)
Not on pseudomonas: No porin channel
Aminopenicillin + gentamicin: SABE caused by S.
viridance and enterococcus

Amoxicillin+ clavulanic acid:

useful in lactamase producing organisms:
Staph, Srep pneumonia, H.influenzae,
Neisseria, E.coli, proteus, Klebsiella
But not in MRSA

Ureidopenicillins and carboxypenicillins:

Spectrum: same as aminopenicillins +
pseudomonas
Use: UTI, septicemia, burn infection caused by
pseudomonas; in combination with
gentamicin
Resistance to cloxacillin/nafcillin: MRSA
due to altered PBP

Cephalosporins
Not active on enterococcus, MRSA, G +ve bacilli
1st generation: X BBB
Excreted in kidney
Sensitive to lactamase
degradation
Cocci > Bacilli ( G ve)
Cefazolin: penetrates tissues surgical prophylaxis

2nd generation
Cefuroxime cross BBB
Cefoxitin
G ve cocci and bacilli (like Amoxicillin +
clavulanic) > G +ve cocci
+
Anaerobes (Lower abdominal and gynecological
infection)
Not used much

3rd generation ( V. V. Imp)

Ceftriaxone, cefitaxime, cefixime
G ve cocci and bacilli, anaerobes > G +ve
cocci ( less than 1st generation)
All cross BBB
Highly resistant to lactamase producing G
ve bacteria

4th generation
Spectrum: same as 3rd generation for G ve
cocci and bacilli; but highly active
Not on anaerobes
Used in infection resistant to 3rd generation
hospital acquired infection

Monobactams
Betalactam
Spectrum: like aminoglycosides
Used in patients with renal impairment where
AMG cannot be used
No cross sensitivity with other betalactams

Carbapenems
Spectrum: G-ve bacilli, G +ve and anaerobes

Glycopeptides: vancomycin,
teicoplanin
Large molecules: do not penetrate into G ve
cells used in G +ve infections
Act at an earlier stage than beta-lactams: not
used in combination
iv: used in MRSA, patients allergic to betalactams, Orally: in Clostridium difficile
infection
With AMG for enterococcal endocarditis

Drugs used in MRSA

Vancomycin
Teicoplanin
Daptomycin + gentamicin
Linezolid
Quinupristin + dalfopristin

Protein synthesis inhibitors

All are bateriostatic
ACCEPT aminoglycosides
May become cidal when used in combination:
cotrimoxazole, quinupristine + dalfopristine

 Just for
understand
ing. Do not
mug up.

Aminoglycosides

Polar: Given iv or im
Do not cross BBB
Used in mainly in serious G ve infections
Remember general properties of this group

 Just for
understan
ding. Do
not mug
up.

Tetracyclines
Are active against wide variety of bacteria, but their
use is restricted due to widespread resistance
Given orally
Absorption: complete only for doxycycline and
minocycline: other drugs remain in the intestine -
problems
Well distributed and penetrates host cells to reach
intracellular organisms
Used in infection caused by mycoplasma, chlamydiae,
rickettsiae
Avoid them in pregnancy and in children < 8 years of
age

Macrolides
Erythromycin
Well distributed, penetrates host ells
Spectrum: like ampicillin Aerobic
microorganisms causing respiratory tract
infection, mycoplasma, chlamydia
Relatively free of serious toxic effects
Azithromycin
Spectrum: same as erythromycin + more activity
against H. influenza and intracellular organisms

Oxazolidinones
Linezolid
Spectrum: G +ve only, effluxed by G ve
Inhibit very first step in protein synthesis
not cross resistance with other antibiotics
In serious infections only; MRSA, VRE,

Streptogramins
Combination: Quinupristin + dalfopristin
Bactericidal
In Serious infection: MRSA

Cotrimoxazole

Sulfamethoxazole + trimethoprim
Widely distributed, reach intracellular organisms
Concentrated in prostatic fluid
Folic acid pathway inside the cell
Drug need to reach the cytoplasm
G +ve has thick cell wall difficult to cross
Hence active on G ve organisms: UTI, typhoid,
Diarrhea due to shigella & salmonella
Mainly used in G-ve infections, chlamydia,
pneumocystitis carinii pneumonia

Quinolones
Many generations available with varied
activity
Act by inhibiting DNA replication hence
need to enter the cell
Entry is easy with G ve (cocci and bacilli)
through porin channels ( no cell wall)
Low PPB good penetration to tissues
penetrates intracellular organisms

 Just
for
under
standi
ng. Do
not
mug
up.

ALL THE BEST