Miscellaneous Antimicrobial Agents;

Disinfectants, Antiseptics, Sterilants

Professor O.G. Ademowo
Institute of Advanced Medical Research and Training
and
Department of Pharmacology and Therapeutics
University of Ibadan
13 Feb 2019
 Objectives
• Define Macrolide and DNA Gyrase
• Describe the mechanisms of action and clinical uses of
clindamycin, erythromycin, fluouroquinolones, and
vancomycin
• Describe the adverse effects of the antibiotics listed above
• Describe the pharmacologic properties of metronidazole
and bacitracin
• Describe drugs used as urinary antiseptics and their
adverse effects
• Define with examples antiseptic, sterilization, disinfectant,
and chlorine demand.
• Know the advantages and disadvantages of commonly
used antiseptics and disinfectants
Loosely, the word antimicrobial may be used to refer to antibiotics
 Definition of Terms
• Selective Toxicity: an antimicrobial drug
should be much more toxic to the ---------
causing infection than the ----------
• Antimicrobial
• Antibiotic
• Bactericidal effect: ------ the bacteria, less
dependent on ------------ for their therapeutic
effects.
• ------- effect: inhibition of growth
 Definition of Terms
• Macrolide – -------------------------.
• DNA Gyrase – --------------------------.
 Chemotherapeutic Drugs
• Anti-----------
• Anti-----------
• Anti-----------
• Anti----------
• Dis----------- and anti----------
• Anti--------
• Anti-----------
• Cancer ----------
• Immuno-----------------
 Classification of Antibiotics
• Inhibitors of -----------------
• Inhibitors of --------------------
• Inhibitors of ----------------
• Disruptors of ------------------
• ------------ agents

NB
• Each of the above categories have their -------
 Miscellaneous Antimicrobial Agents
Sub class Prototype Major variants
Macrolides ---------- --------, --------, ---------, ---------,

-------- Lincomycin ---------

Glycopeptides --------
Nitrofurans -------
Fluoroquinolones ----- --------
----- Nalidixic acid -------
------- salts Methenamine - ----------- hippurate
-------
Cycloserine --------
Others --------
----------
Pharmacologic Properties
Classes and Macrolides -
agents erythromycin
Mechanism of action -------------
Key pharmacokinetic Liver metabolism,
properties inhibits -------
increases ----------,
Excretion primarily
via -------, T1/2 - -----
Clinical uses Treatment of ------
Key adverse effects ------ irritation, -------,
-------, -------
Contraindications of note -------, existing ------
disease, concomitant
use of ------ derivatives
Formulations --------, --------, --------
Lincosamines-
clindamycin
-------------
Good ---------
absorption. High
distribution in ------ and
-------. No significant
level in ------. ---------
metabolism T1/2 – -----
-------- cocci, and ------
e.g. ------- spp
Marked ------ irritation,
-------, ---------, -------
dysfunction,
superinfection with -----
--
Hypersensitivity to the -
------ or components. ----
-----------,
---------, ----------, --------
Glycopeptides –
vancomycin
-----------------
Given -------, penetrates
most -----, eliminated ---
- in -------. Parenteral
admistration is ------
Used for serious
infections caused by ----
----- including -------
------, ------, -------, ------,
------- ,-------- may cause
diffuse flushing (--------
syndrome)
---------, previous severe
------ loss
----
Fluoroquinolones -
ciprofloxacine
--------------------
Good ------ absorption, well
distributed in -----,
elimination partly via -----
and mainly through ------
via active -------(blocked by
----------)
-------, ------ tissue, and ------
infections by
-------- organisms especially
--------, --------, --------, -------
------ irritation, -------, ------,
and -------. Superinfection
with ------ may occur. The
drug may enhance -------
toxicity
Hypersensitivity to -------.
--------, ------------,--------
 Metronidazole
MOA Bactericidal actions result from -----------, causes ----------, loss of ----
---------, and inhibition of ------------ in susceptible organisms

PK Good ---------- absorption, protein binding -------%, wide distribution into ---- and bone-----,--------
metabolism (30 – 60%), good ------ penetration especially inflamed -------, T1/2 – --------, ------ excretion,

Clinical indications An ------ agent, also Active against ----------- and -------- such as ------ and -------- spp.

Adverse effects -------- irritation, -------, ----------dysfunction, and ----------reactions with --------. ---------in some animals

Contraindications ---------- to the medication or components of ---------. ------------ dependence

Formulations ----------, -------------

 Urinary Antiseptics
Nitrofurantoin Nalidixic acid Methanamine Cycloserine
Mechanism of action Inhibits several --------- Inhibits -------- in late Hydrolysed to ------ and --------static
- systems including ---- stages of --------- ------- in ---- urine. Inhibits bacterial cell
----- interfering with -- Formaldehyde - ------ wall synthesis by ---------
---- and possibly ------ - for -------------
---

Key PK Well absorbed --------, Achieved significant ---- ------ absorption. Well absorbed, widely
protein binding --------- ---- only in the ------- Metabolism by ----------, distributed into ------
%, metabolized by ---- Protein binding ------% also 10% metabolized in including -----.
---- except -------, T1/2 – ----------hrs., ------- to active Metabolism -----, T1/2 –
T1/2- ----------, metabolism partly ------ components. T1/2 – ----- -----hrs.
excretion - --------- ---., excretion ---------. Elimination ------

Clinical indication Treatment of ----- Mainly for the treatment --------- infection -------and other ------
------ infections
Notable adverse effects -------irritation and Skin rashes, -------, ------ ------ irritation, fever, ---- Cardiac ---------
disorders, -----, ------, anaemia, weakness, -----, --- stools,
jaundice – ------ headache hypersensitivity, rash, ---
-----, headache, -----, ----

Contraindications -------, hypersensitivity ----------, ----------- Hypersensitivity, marked Hypersensitivity to the --

to --------, disorder, infants ---- yrs ------ or ------- ------ or components
impairment,
Formulations ----- ----- ------ ------
 Other Miscellaneous Antibiotics
Mechanism of action

Polymyxins: polymyxin -----, polymixin ----- Attaches to ---------- causing ----- and
-(-------) leakage of ------- contents. They act as -----
Significant ------, largely restricted to ------ ---
use

--------- Active against ------ and ------. Including ----

Topical use on ------- more common -----. Inhibits -------------. No activity against
--------------.

------------ --------- antibiotic. Inhibits ------- by binding

to the ------- sub-unit of ----------. Active
against --------- and --------. No activity
against ----------
Disinfectants, Antiseptics, and
Sterilants
-----------

-----------

-----------

-----------

-----------

-----------
Sub-class Examples Uses

Alcohols, ------, ------, ------- ---------- (alcohols), ---------- (formaldehyde), ---

aldehyde, and acid -------------- (acetic acid)
acids

Halogens --------, --------- ------------(iodine). ------------(chlorine),

halazone is used in ------ form to ------ water,
what is chlorine demand?----------
Heavy metals ---------. ------ ----------(mercuric ions), ------------- (silver
nitrate)

Chlorinated ----------, ----------- Surgical -------, irrigation of --------, antiseptic --

phenols --------
Chlorhexidine disrupts ---------, especially
those of ------, daily use may be absorbed via -
-------- causing --------- effects

Cationic --------- Antiseptics for ---------- ---------. Minimal

surfactants ------------ activity against ---------, (activity may be
antagonized by -------)
 So how do you choose
Antibiotics for use against
infections??
 Learning Pharmacology
• Other subjects too....

• Google Images
• YouTube
-----------

-----------
-----------

-----------

-----------

-----------
The WHYs Have IT.....
 Acknowledgements
• Textbook: Basic and Clinical Pharmacology,
Bertram G. Kartzung, 14th Edition
• Internet sites
• Google images