Antimicrobial Drugs

Dr. Mejbah Uddin Ahmed

Antimicrobial Agents:
Antimicrobial are the agents, they either kill or
prevent growth of micro-organisms. Two
categories:
1. Antibiotics: Antimicrobial drugs produced
from biological agents (microorganisms).
2. Synthetic drugs: Antimicrobial drugs are
synthesized in the laboratory.
Antibacterials: Relatively easy to develop and
find with low toxicity because procaryotic cells
are very different from host cells.
Antihelminthic, antiprotozoan, and antifungal
drugs: More difficult to develop because
eucaryotic cells resemble human cells.
Antivirals: Most difficult to develop because
virus reproduces using host cell enzymes and
machinery.
 Selective toxicity
A drug should selectively kill or prevent growth of a
microorganism, but not host cells.
Selective toxicity is achieved by:
 They act at specific site
 Bacterial cell wall
 Inhibition of an enzyme unique to bacteria
 Inhibition of bacterial protein synthesis
 Bacterial nucleic acid
 Selectivetoxicity is better incase of antibacterial
agents than antiviral or antifungal drug
 Classification

1. According to source of origin-

A) Antibiotics- natural products of fungi, &
bacteria which kill the microbes e.g.
Penicillins,
B) Synthetic compound- e.g. trimethoprim,
Sulfonamides.
 Classification
2. Either kill or inhibit bacteria:
A) Bactericidal- kills organisms: penicillin,
cephalosporin, aminoglycoside.
B) Bacteriostatic - Inhibit organisms from
multiplying, but does not kill: tetracycline,
chloramphenicol and erythromycin.
4. According to target site
A. Inhibition of cell wall synthesis
B. Inhibition of protein synthesis
C. Inhibition of nucleic acid synthesis
D. Inhibition of metabolic pathways
E. Interference with cell membrane integrity
 Classification
5. According to spectrum of activity:
A) Narrow spectrum: Drugs that affect only
Gram-positive organisms or only Gram-
negative organisms: Vancomycin, Nalidixic
acid.
B) Broad spectrum: Drugs that affect both
Gram-positive and Gram-negative
organisms: Tetracycline, Ciprofloxacin.
A. cell wall synthesis Inhibitors:
Beta-lactam drugs
Penicillins

Cephalosporins

Carbapenems

The others
Cycloserine

Vancomycin

bacitracin
Penicillin:
● Act by binding to Penicillin Binding Proteins.
● Inhibit transpeptidase activity & peptide cross
linking in cell wall.
● Cause the bacterial wall to weaken and take
up water and burst
B. Inhibition of protein synthesis:
♦ Irreversibly binds to 30S ribosomal
subunit:
Aminoglycoside, Tetracycline
♦ Reversibly binds to 50S ribosomal
subunit:
Chloramphenicol, Erythromycin,
clarithromycin, azithromycin
C. Inhibition of Nucleic Acid Synthesis:
Quinolones: Inhibits DNA synthesis
by affecting DNA gyrase .
Rifamycins: inhibits bacterial
DNA - dependent RNA polymerase -
blocks mRNA.
Metronidazole: Breaks the
strands of DNA
Inhibition of metabolic pathways:
Most useful are folate inhibitors: Sulfonamides
& Trimethoprim.
Pteridine + PABA + Glutamic acid
Sulfonamide dihydropteroate
synthatase
HAH2
Trimethoprim Dihydrfolate reductase

HAH4

Purine Pyrimidine Amino acids

E. Injury to cell membranes
◆ Changes in membrane permeability.
◆ Result in loss of metabolites and/or cell
lysis.
◆ Many polypeptide antibiotics.
◆ E.g.:

Polymyxin, Colistin, Daptomymycin,

miconazole, Polyenes (anti-fungal
agents)
Combinations of Drugs
 Indications

Severe and mixed infections

Prompt treatment
To delay emergence of drug resistance
To achieve bactericidal action or
synergism
 Disadvantages
 False sense of security
 High cost of treatment
 No more than effect of a single drug
 Possibility of antagonism (rarely)
 Combinations:

Sulphonamide + Trimethoprim,
β lactams + aminoglycosides
Amoxycillin + Clauvlinic acid
Anti tubercular drugs.
Safety Concerns with the Use of Antimicrobials:
♦Toxicity: Kidney, Liver damage, Bone marrow
(Chloramphenicol and aplastic anemia).
♦ Interactions with other medications
♦ Hypersensitivity reactions
♦ Fetal damage/risk to pregnant women: Tetracyclin
causes discoloration of teeth in children.
♦ Kills host’s normal beneficial flora.
♦ Antibiotic Resistance.