Antimicrobial Drugs

Antimicrobial Drugs

Def: A substance of biological, semisynthetic or

synthetic origin of low molecular weight
(on-protein) produced by a fungus or bacterium
as secondary metabolites that inhibits or stop
growth of other microorganisms in vitro and in
vivo selectively, when it used in low
concentration
 Antimicrobial Drugs
• Chemotherapeutic agent= Antimicrobial drug

• Different types of antimicrobial drugs:

– Antibacterial drugs
– Antiviral Drugs
– Antifungal drugs
– Antiprotozoal drugs
– Anthelminthic drugs
History Of Antibiotics
 Alexander Fleming
• Working on cultures of Staphylococcus
• Contamination with mold
• Noticed colonies growing near mold
looked odd
• Found that mold was secreting substance
that was killing bacteria
Figure 20.1
 Features of Antimicrobial Drugs

• Most modern antibiotics come from species of

microorganisms that live in the soil
• To commercially produce antibiotic:
1. Select strain and grow
2. When maximum antibiotic concentration
reached, extract from medium
3. Purify
4. Chemical alter to make it more stable
 Features of Antimicrobial Drugs:
Selective Toxicity
• Cause greater harm to microorganisms than to
host
• Chemotherapeutic index= lowest dose toxic to
patient divided by dose typically used for therapy
 Features of Antimicrobial Drugs:
Antimicrobial Action
• Bacteriostatic: inhibit growth of
microorganisms

• Bactericidal: Kill microorganisms

 Features of Antimicrobial Drugs:
Spectrum of Activity
• Antimicrobial medications vary with respect to
the range of microorganisms they kill or inhibit
• Some kill only limited range : Narrow-spectrum
antimicrobial
• While others kill wide range of microorganisms:
Broad-spectrum antimicrobial
 Features of Antimicrobial Drugs:
Effects of Combining Drugs
• Combinations are sometimes used to fight
infections
• Synergistic: action of one drug enhances the
activity of another
• Antagonistic: activity of one drug interferes with
the action of another
 Features of Antimicrobial Drugs:
Adverse Effects
1. Allergic Reactions: some people develop
hypersensitivities to antimicrobials
2. Toxic Effects: some antimicrobials toxic at high
concentrations or cause adverse effects
3. Suppression of normal flora: when normal flora
killed, other pathogens may be able to grow to
high numbers
 Features of Antimicrobial Drugs:
Resistance to Antimicrobials
• Some microorganisms inherently resistant to
effects of a particular drug
• Other previously sensitive microorganisms can
develop resistance through spontaneous
mutations or acquisition of new genes
 Ideal characteristics of antibiotics
1. It must be able to reach the part of the human
body where the infection is occurring.
 Cont
2. It should not cause the development of resistant
forms of parasites.
3. It should not produce undesirable side effects in
the host such as allergic reaction, nerve damage
or irritation of the kidneys and gastrointestinal
tract
 Cont
4. It should be given orally without inactivation by
stomach acid, or by injection (parenterally) without
binding to the blood proteins
5. Finally, it should have a high level of solubility
in the body fluids and be possible to achieve
concentrations in the tissue or blood, which are
sufficiently high to inhibit or kill the infectious
agents
 Mechanisms of action of
Antibacterial Drugs
1. Inhibit cell wall synthesis
2. Inhibit protein synthesis
3. Inhibit nucleic acid synthesis
4. Injury to plasma membrane
5. Inhibit synthesis of essential metabolites
Figure 20.2