INTRODUCTION TO

ANTIMICROBIAL AGENTS

Dr. Shardendu K Mishra

Associate Professor
Department of Pharmacology
Ram-Eesh Institute of Vocational & Technical Education
 Antimicrobials Agents

 Definition Antibiotic is :
 A chemical substance produce by microorganism
(natural products) which has the capacity to inhibit/kill
the growth of other microbes at low concentrations. It
has a high chemotherapeutical index to reduce the
active process in organism in a diluted solution.

 Antibiotics = anti microorganisms

 Antimicrobial Agents : Substances
that inhibit the growth or kill the
microbes. It may be of natural or
synthetic origin.
 Antiseptic : chemical used/applied on living
tissue to reduce the possibility of infection.
 Disinfectants : chemicals used on non-living
things to prevent infection.
 Chemotherapy : Agents which are used to treat
specific infection or diseases without interfering
with host.
 Microbiostatic : Stop the growth of microbes
 Microbiocidal : Kills the microbes
 Minimum Inhibitory Concentration – Lowest
AMA conc. That prevents visible growth of
microbes.
 Minimum Bactericidal Concentration – Lowest
AMA conc. That kills 99.9% of the microbes.
 A small difference between MIC and MBC defines
the AMA as bactericidal.
 Post-Antibiotic Effect – PAE is the duration of
time required by microbe to show viable re-growth
following the removal of an antibiotic. Seen in
Beta Lactams, FQs, aminoglycosides.
 Classification of Antimicrobial
Agents

1. Based on chemical structures

2. Based on the sources
3. Based on mechanism of action
4. Based on spectrum of action / activity
1. Based on chemical structures
Groups of sulfonamides  Sulfamethoxazole,
sulfadiazine
Groups of Penicillin  Penicillin
G (Benzylpenicillin), Penicillin V,
Ampicillin, amoxicillin, nafcillin
Groups of cephalosporins cefalotin,
cefazolin, cefuroxime, cefotaxime, ceftriaxone.
Groups of aminoglycosides  streptomycin,
neomycin, kanamycin, gentamycin, tobramycin
Groups of nitrobenzene  chloramphenicol,
tiamphenicol
 1. Based on chemical structures
6.Groups of tetracyclines chlortetracycline,
oxytetracycline, doxycycline, minocycline HCl
7.Groups of macrolides erythromycin,
roxithromycin, azithromycin
8. Groups of polyenes  amphotericin B, nystatin
9. Groups of Lincomycins  lincomycin, clindamycin
10. Groups of polymixins  Polymyxin B, Polymyxin
E, bacitracin
11. Groups of sulfon  dapsone
1. Based on chemical structures

12.Glycopeptide derivative 
vancomycin
13.Nitrofuran analogues-
Nitrofurantoin
14.Nitroimidazoles- metronidazole
15.Groups of quinolones  nalidixic
acid, norfloxacin, ciprofloxacin,
offloxacin
16.Azole derivatives- Miconazole,
Clotrimazole, Fluconazole.
 II. Based on the sources
a. Antibiotic from microbes
§ A.B. from fungi  Penicillin from P. notatum
§ A.B. from bacteria
• A.B. from eubacteria  polymyxin from Bacillus polymyxa
• A.B. from micromonosporaceae  gentamyicin from
Micromonospora purpurea

b. Antibiotics from algae  Usnat Acid

c. Antibiotics from higher plants  Garlisina
from Allium sativum
d. Antibiotics from animals  Eritrina
from hemoglobin of cow
 III. Based on mechanism of
action
A.Inhibition of cell wall synthesis leads to the
death of the bacteria lysis (bactericidal effect) 
Penicillin, Cycloserine, Vancomycin, Bacitracin,
Cefotaxime, Ceftriaxone.
B.Disruption of cell membrane function 
Polymyxin (Polymyxin B, Polymyxin E),
Polyenes, Nystatin
C. Inhibition of protein synthesis:
 This antibiotics inhibit one of the reactions in the
process of transcription
1. Inhibition of translation process of microbes
III. Based on mechanism of
action
• Inhibit ribosome on the 30 S subunit 
Streptomycin, Tetracylines, Netilmicin, Kanamycin
• Inhibit ribosom on the 50 S subunit 
Chloramphenicol, Clyndamycin, Lincomycin
§ Inhibits the transcription process of microbes
 Rifampin, Actinomycin
D. Inhibits specific metabolic reaction
 Inhibits the enzymatic reactions 
Sulfonamides, INH, PAS, Trimethoprim
 IV. Based on spectrum of action

§ Broad spectrum: Effective to Gram+, Gram-

bacteria, Mycoplasmas, Chlamydiae,
Rickettsiae, sometimes protozoa 
Chloramphenicol, Tetracyclines
§ Narrow spectrum: Effective to Gram+ / Gram-
bacteria only  Penicillins, Cephalosporins,
Erythromycins, Polymyxins
 Mechanism of Resistance
 Bacteria produce enzymes that destroy the active drugs
such as beta-lactamases which will destroy beta-
lactams antibiotics.
 Natural resistance :
 genetic  chromosomal resistance and
extrachromosomal resistance
 non genetic
 Genetic resistance happen because of genetic
changes. Eg – Pencillin G not effective in Gram
-ve
 Non genetic resistance happen because of antibiotics
come into contact with bacteria which have active
metabolism.
 Mechanism of Resistance

 Acquired resistance  Sensitive bacteria will get

this resistance properties through plasmid which
contains resistance factors (R factors) from
resistance bacteria.
 a) Mutation – Change occur spontaneously or
randomly in the DNA.
 B) Gene Transfer – transfer of resistance
Mechanism of Resistance
1. Alteration of cell membrane permeability, such
alteration inhibit penetration of antibiotics to
bacterial cell  Staphylococcus against
tetracyclines
2. Alteration in bacterial cell, so that a big ammount of
antibiotic destroy enzymes are produced
  -lactamase against penicillins and cephalosporins
 Acetyltransferase against chloramfenicol
 Phosphorilase, acetylase and adenylase against
aminoglycosides
Mechanism of Resistance
3. Alteration of receptors usually affects
bacterial ribosomes. The mutation alters
the DNA that produces a ribosomal
protein receptor sothe a antibiotics
cannot bind to it  erythromycin receptor
in staphylococcus
4. Alteration of a metabolic pathway in bacterial cell,
to bypass a reaction inhibited by an antimicrobial
agent  dehydrofolate by trimethoprim,
sulfanomide, INH and PAS
Some approaches to solve resistance problems

1. Administration of antibiotics prescription only if the

clinical signs and tests indicated that certain
bacteria are the most probable caused of infection
2. Bacteriologic diagnosis must be sought and
susceptibility tests must be determined
3. Avoid the usage of antibiotics which have been
known resistance in one population
4. Reduce the usage of topical antibiotics, use
antiseptics instead.
5. Limit the period of consuming antibiotics
Some approaches to solve resistance problems
1. Reduce the usage of prophylactic antibiotics
2. Use narrow spectrum antibiotics
3. Always follow directions for use of antibiotics
4. Prescrible antibiotics based on clinical situation
and not on patient’s will or pharmaceutical
advertisements.

 Rational drug: drugs given after accurate

diagnosis. It will be effective with minimal side
effects.
Factors involve in the usage of AB rationally,
effectively and safely.
1. Accurate diagnosis
2. Accurate choices of antibiotics
3. Deliver accurate dose
4. Accurate dosing interval
5. Accurate examinations of patophysiologic conditions
of the patient

 Factors involve in choosing antibiotics

 Disease factors
 Drug factors
 Recipient factors
Factors involve in choosing antibiotics

1. Disease factors
 Selective for etiologic bacteria susceptibility test
 Types and doses depend on location of infection
 Enough penetrating potentials to cross :
• blood-brain barrier in
• abscess walls

§ Drugs factors  Ideal antibiotics :

 Have a narrow spectrum, affect only to etiologic bacteria

 Have a bactericidal effect, unless none is sensitive,

bacteriostatic drugs can be delivered
 Ideal antibiotics :
 Effective even in the presence of body fluids
exudate, protein or enzymes.
 Ability to reach the infected tissue, enough drug
concentration during the span of a dosing
interval in blood / infected area.
 Do not caused resistance
 Have a minimal toxic effects for the patient

 Safe for pregnancy and pediatric patients

 Low costs
 Factors involve in choosing antibiotics
3. Patient factors :
 Age
 Genetics
 Pregnancy
 Accompanying diseases
 Antibiotic prophylaxis: An antibiotic is used to
anticipate infection from certain bacteria which are
sensitive to the drug.
 Goal: To minimize the surgical wound infection, by
treating with antibiotic in lethal concentration for
microorganisms at the beginning of surgery until it
finished (done).
Sensitivity tests/resistance tests
 Qualitative :
§ Stokes method
§ Ericcson method
§ Kirby-Bauer method
§ Comparison method

§ Quantitative :
1. MIC
2. MIC plate
Qualitative

 The Kirby-Bauer Method: Commonly in

microbiology use the Kirby-Bauer Method . It
use medium of Mueller-Hinton Agar on the
susceptibility test
 Mueller-Hinton Agar
 Sensitive : clear area (zones of inhibition)
 Resistance : No zones of inhibition
 Side effects of antibiotics
§ Allergic reaction : Is a respond in sensitive
individual due to the abnormality in his immune
system  Penicillin, Sulfonamides, Streptomycin
 Mild symptoms are skin rashes and itching.

 Severe symptoms are anaphylactic shock.

 Toxic reaction : Can happen in individual depend on

the doses of drugs in the body  Hearing disorder
because of gentamycin
 Manifestation can occur :
 Temporary and permanently
 After a prolonged used / acute respond
 Antiviral Agents

1. Inhibit viruses coverage

2. Inhibit DNA and RNA synthesis in the viruses
3. Inhibit protein synthesis in the viruses
4. Inhibit specific enzymes activities in the viruses
5. Inhibit the growth of viruses
6. Promote immunity system of the body
7. Prevent virus infection to the body
 The Drugs that use :
• To inhibit viruses coverage: Amantadine, Rimantidine
• To inhibit DNA and RNA synthesis: Acyclovir,
Ganciclovir, Foscarnet, Ribavirin, Valacyclovir,
vidarabine, cidofovir
• To inhibit return transcription from nucleocid:
Zidovudine, Didanosine, Zalcitabine
• Inhibit protease enzyme Other antiviral drugs:
Idoxuridine, Trifluridine, Fluorouracil, Interferons,
Immunoglobulins
 Notes : Antiviral drugs only inhibit the early stage
of replication
 Antifungal Agents
 Fungal infection occur less frequently than bacterial or
viral infections.
 Three major groups of antifungal agents :
1. Groups of polyenes :
• Amphotericin B
• Nystatin

2. Groups of Azole Imidazoles :

• Ketoconazole
• Miconazole
• Clotrimazole
• Fluconazole
• Itraconazole
Antifungal Agents
1. Groups of Alilamin:
• Terbinafin
• Naftitin

 Other antifungal agents :

 Griseofulvin
 Flucytosine