Chemotherapeutic

Agents
Chemotherapeutic agents (synthetic
antibiotics)
- antimicrobial agents of synthetic origin
useful in the treatment of microbial or viral
disease.
- Examples are sulfonilamides, isoniazid,
ethambutol, AZT, nalidixic acid and
chloramphenicol, etc.
 An antibiotic is an agent that either kills or
inhibits the growth of a cell (tumour, bacteria,
fungi, etc.)
 An antibacterial is an agent that either kills or
inhibits the growth of bacteria.
 What's the difference between antibacterial and
antibiotic?
 The primary difference between antibacterial
and antimicrobial substances is the types of
microorganism they act upon.
While antibacterial products prevent the
development of bacteria, antimicrobial agents
such as alcohol-based hand sanitizers prevent
the spread of bacteria, fungi, and some viruses.
Anti-infective agents:
 Anti-infectives is a general term used to
describe any medicine that is capable of
inhibiting the spread of an infectious
organism or by killing the infectious
organism outright.
 This term encompasses antibiotics,

antifungals, anthelmintics, antimalarials,

antiprotozoals, antituberculosis agents, and
antivirals.
Antibiotics:
 A substance produced by microorganisms
that in small amounts inhibits another
microorganism
 More than half of our antibiotics are

produced by bacteria
Spectrum of antimicrobial activity
 Some drugs have a narrow spectrum antibiotics
– range of different microbial types they affect
(Penicillin G) – gram positive bacteria but very
few gram negative bacteria
 Broad range of gram positive or gram negative
bacteria – broad spectrum antibiotics; have an
advantage in treating a disease but may
destroy many normal microbiota of the host
 May lead to overgrowth of pathogens 
superinfection and may be due to antibiotic-
resistant strain
Mechanism of action:
 Antimicrobial drugs are either bactericidal
(kill microbes directly) or bacteriostatic
(prevent microbes from growing)
 the host’s own defenses (phagocytosis and

antibody production) usually destroy the

microorganisms
Inhibitors of Cell Wall Synthesis
 Penicillin:
- refers to a group of over 50 chemically
related antibiotics
- have a common core structure containing a
B-lactam ring called the nucleus
- produced either naturally or
semisynthetically
- prevent cross-linking of the peptidoglycans
 interferes with the final stages of cell wall
construction (G+ bacteria)
Examples of Penicillins:
 Natural Penicillins:
> Penicillin G – narrow spectrum; DOC vs
staph, strep, spirochetes
- injected IM – rapidly excreted from the body
in 3-6h
- oral: stomach acid diminishes its
concentration
> Procaine Penicillin – up to 24 hours; conc
peak about 4 hours
 - benzathine penicillin – longer retention, 4
months but low concentration
- Penicillin V – stable in stomach acids; can
be taken orally
Disadvantages of Natural Penicillins:
1. Narrow spectrum of activity
2. Susceptibility to penicillinases (enzymes
produced by many bacteria that cleave the
B-lactam ring  also called as B-lactamases
Monobactams:
Inhibitors of Protein Synthesis
Injury to plasma membranes
Quinolones & Fluoroquionolones:
Inhibitors of Essential Metabolites
Anti-Fungal Drugs:
Antivirals for HIV/AIDS