Lec. 5 Medical Microbiology: Antibacterial Drugs

Lec.
5 Medical Microbiology
Antibacterial Drugs
Introduction .1
In the past decades, many research findings were directed towards
biomedical sciences in an attempt to give a solution to the present
health issues caused by microorganism infections.
Infectious diseases represent a considerable factor of human

morbidity and mortality for most of human existence.
The introduction of antimicrobial materials into general clinical use is

one of the most successful approaches in chemotherapy,
considerably contributing to the control of infections.
The existing antimicrobials in the clinical investigations have provided

an array of choices when treating many types of infectious diseases.
Introduction
• However, treatment options for patients are limited because the bacterial
resistance evolved more rapidly than the antibacterial drug development.
• Clinical results are reporting increasing rates of in vitro resistance among

previously susceptible organisms and the occurrence of essentially resistant
microorganisms as pathogens in immune-compromised hosts.
• To reduce the development and spread of antimicrobial resistance, the

preservation of current antimicrobials through their appropriate use becomes
mandatory.
• This motivates scientists to focus on discovery and production of new chemical

substances that destroy pathogenic microorganisms with minimal damage
to host tissues .
Definition and classification of antimicrobial
drugs
• An antibacterial drug represents a chemical substance derived

from a biological source or produced by chemical synthesis
that is able to destroy or to inhibit the development/growth of
bacteria.
Antibacterial drugs are commonly classified by considering the
following criteria:
a. Targeted pathogens: This category involves antibacterial,

antiviral, and antifungal drugs. This grouping may be further
subdivided because antibacterial drugs also include urinary
antiseptics and anti-mycobacterial drugs. Antimicrobial
drugs, especially antibacterial drugs, are strictly classified into
chemotherapeutic agents (synthetic chemicals), and
antibiotics, produced from living organisms, usually fungi.
However, 'antibiotic' is often used loosely to mean all
antibacterial drugs;
Antibacterial drugs are commonly classified by considering the
:following criteria
b. Chemical structure: Examples are penicillins and cephalosporins;
c. Source: Natural (mainly fungal sources), semi-synthetic (chemically-altered

natural compound), and synthetic (chemically designed in the lab). The “natural”
antibiotics arise from fungal sources. Organisms become resistant faster to the
natural antimicrobials because they have been pre-exposed to these
compounds in nature. Natural antibiotics are often more toxic than synthetic
ones. Semi-synthetic drugs appeared as alternative to decrease toxicity and increase
effectiveness of the first category.
Synthetic drugs have an advantage that the bacteria are not exposed to the compounds
until they are released. They are prepared to exhibit greater effectiveness and less
toxicity. There is an inverse relationship between toxicity and effectiveness starting
from natural to synthetic antibiotics.
Toxicity versus effectiveness for antimicrobial drugs
derived from different sources
d. Mechanism of action: The antibacterial drugs are designed to have a

complex mechanism of action by considering some essential factors which
render to the obtained drug-specific features. One can classify antibacterial
drugs by taking into account the following:
One can classify antibacterial drugs by taking into
:account the following
1. The effect on bacterial growth
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growth
o Bacteriostatic prevent
kill
o Bactericidal drugs
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One can classify antibacterial drugs by taking into
:account the following
2. The targeted site
a. Drugs that inhibit bacterial wall synthesis or activate enzymes that destroy the
cell wall
b. Drugs that enhance cell membrane permeability (causing leakage of intracellular

material)
c. Drugs that determine lethal inhibition of bacterial protein synthesis
d. Drugs that generate nonlethal inhibition of protein synthesis
e. Drugs that inhibit bacterial synthesis of nucleic acids
f. Antimetabolites (disruption of specific biochemical reactions---decrease in the

synthesis of essential cell constituents)
g. Inhibitors of viral enzymes

:One can classify antibacterial drugs by taking into account the following
3. The target specificity
a. The broad-spectrum drug affects a wide range of disease-causing bacteria,

including both Gram-positive and Gram-negative bacteria
b. The narrow-spectrum antibacterial drug, which acts against specific families of

bacteria.
Mode of Action
For a better understanding of the different types of antimicrobial drugs
.displays the main classes of these substances and their applications
Minimizing Toxicity
• Antibiotics act by inhibiting the basic life-sustaining processes in the
microorganism. In order to minimize toxicity, the targets of antibiotics must be
selective. However, all antibiotics are toxic to some degree. Selective toxicity
should be focused on harming the bacteria, not the host. Selection of the
appropriate antibiotic depends on the following parameters:
1. Knowledge of organism’s natural resistance
2. Pharmacological properties of the antibiotic toxicity, binding, distribution,

absorption achievable levels in blood, urine.
3. Previous experience with same species
4. Nature of patients underlying pathology

5. Patient’s immune status
The Resistance to Antimicrobial Drugs
• Evaluation of susceptibility focuses mainly on the interaction of

antimicrobial agents, the organisms, and their resistance mechanisms.
The resistance to antimicrobial drugs is based on several mechanisms,
including the following:
a. Microbes may generate drug-metabolizing enzymes (such as
penicillinase)
b. Microbes may cease active uptake of certain drugs
c. Microbial drug receptors may suffer change resulting in reduced
antibiotic binding and action
d. Microbes may produce compounds that antagonize drug actions
Spreading Resistance
• The bacteria are innately resistant to some antibiotics since they lack
a target site or are impermeable to the antibiotic.
• Resistance spreads between bacteria in three physical ways:
conjugation (by direct contact), transduction (by phages), and
transformation (uptake of free DNA). The resistance is acquired by
spontaneous mutation and conjugation. This could be the results of
two aspects as follows:
∙ Utilization of antibiotics that promote the appearance of
drug-resistant microbes
∙ Supra-infection: A new infection that occurs during the treatment of a
primary infection
Conjugation, Transduction ,
Transformation
Delaying the resistance appearance
⑤
• Delaying the appearance of resistance can be achieved
by taking into account the following solutions:
a. Use antimicrobial agents only when required

b. Utilization of narrow-spectrum antibiotics whenever
possible
c. Novel antibiotics should be kept for cases in which older

drugs are harmful or no longer effective
disadvantages of antibiotic combinations
• There are some disadvantages of antibiotic

combinations as follows:
a. Enhanced risk of toxic and allergic reactions
b. Possible antagonism of antimicrobial effects
c. Increased risk of supra-infection
d. Selection of drug-resistant bacteria
e. High costs

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Lec.

Infectious diseases represent a considerable factor of human

The introduction of antimicrobial materials into general clinical use is

The existing antimicrobials in the clinical investigations have provided

• Clinical results are reporting increasing rates of in vitro resistance among

• To reduce the development and spread of antimicrobial resistance, the

• This motivates scientists to focus on discovery and production of new chemical

• An antibacterial drug represents a chemical substance derived

a. Targeted pathogens: This category involves antibacterial,

c. Source: Natural (mainly fungal sources), semi-synthetic (chemically-altered

d. Mechanism of action: The antibacterial drugs are designed to have a

b. Drugs that enhance cell membrane permeability (causing leakage of intracellular

c. Drugs that determine lethal inhibition of bacterial protein synthesis

d. Drugs that generate nonlethal inhibition of protein synthesis

e. Drugs that inhibit bacterial synthesis of nucleic acids

f. Antimetabolites (disruption of specific biochemical reactions---decrease in the

g. Inhibitors of viral enzymes

3. The target specificity

a. The broad-spectrum drug affects a wide range of disease-causing bacteria,

b. The narrow-spectrum antibacterial drug, which acts against specific families of

2. Pharmacological properties of the antibiotic toxicity, binding, distribution,

3. Previous experience with same species

4. Nature of patients underlying pathology

• Evaluation of susceptibility focuses mainly on the interaction of

a. Use antimicrobial agents only when required

c. Novel antibiotics should be kept for cases in which older

• There are some disadvantages of antibiotic

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