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