ANTIBIOTICS

DEFINITIONS OF TERMS:
CHEMOTHERAPHY - is the use of chemical
agent and the treatment of disease.
CHEMOTHERAPEUTIC AGENT - any
chemical agent use in medical practice
ANTIBIOTICS - is usually considered to be a
chemical substance made by a
microorganism that can inhibit or kill
microorganisms

ANTIBIOTICS
Naturally occuring antimicrobials
- metabolic products of bacteria and
fungi
- reduce competition for nutrients and
space
Bacteria
- Streptomyces, Bacillus
Molds
- Penincillum, Cephalosporium

MODES OF
ACTION OF
ANTIMICROBIAL
GROWTH
(ANTIBIOTICS)
Calibri Light

MIRANDA, SIENNA LAUREN GAIL

MIRABEL, GENREV ADAM

A. INHIBITION OF CELL
WALL SYSTHESIS

Beta-lactam antibiotic
penicillins, cephalosporins and
monobactams

Vanomycin and Cycloserine

disrupt cell wall formation in Gram Positive
bacteria
Bacitracin
Blocks secretion of NAG (N- acetylmuramic
acid) and NAM (N-acetyl glucosamine)
secretion from cytoplasm
Effective in treating skin infections caused
by Gram Positive bacteria
Isoniazid and ethambutol
Disrupt mycolic acid formation in
Myobacterium species

B. INHIBITION OF PROTEIN
SYNTHESIS
A. Interaction with 30S ribosomal subunit
. Aminoglycosides (gentamicin, kanamycin, tobramycin,
streptomycin)
- Isolated from genus Streptomyces
- Produced synthetically or semisynthetically
. Tetracyclines
B. Interaction with 50S ribosomal subunit
. Chloramphenicol
Broad Spectrum
antibiotics
. Macrolides

C. DISRUPTION OF
CYTOPLASMIC MEMBRANE
A. Amphotericin B, Nystatin, Polymyxin B
bind avidly to membrane sterols.
Higher affinity for ergosterol (present in fungal
membranes) than for cholesterol (in mammalian
membranes).
B. Imidazole antifungals
ketoconazole, fluconazole
inhibit 14-demethylation of lanosterol to
ergosterol (essential component of fungal
membranes).

D. INHIBITION OF
METABOLIC PATHWAY

Sulfa drugs
(sulfanilamide and
sulfamethoxazole)
are effective against
bacteria that produce
folic acid.
Inhibition of the
synthesis of folic
acid, which is
essential in nucleic
acid production, will
eventually lead to

E. INHIBITION OF NUCLEIC
ACID REPLICATION
Mode of action
of
actinomycin,
nucleotide
analogs,
fluoroquinolon
es, quinolones
and rifampin

MECHANISMS BY
WHICH MICROBES
DEVELOP
RESISTANCE TO
ANTIMICROBIAL
DRUG

A. ENZYME PRODUCTION
Some bacteria
produces enzymes
that deactivates
antimicrobial drug.
Beta-Lactamases /
Penicillinases
deactivates betalactam rings

B. ALTERATION OF CELL
MEMBRANE STRUCTURE
Pathogens alter their
cell membrane to slow
down or prevent entry of
the drug into their
cytoplasm.
Some alter the
receptors for the drug so
that it cant attach or bind
less effective.
Others pump (Efflux

C. ALTERATION OF THEIR
METABOLIC PATHWAYS
Produce more enzyme affected by the
pathway.
Sulphonamide resistant bacteria do not
require extracellular PABA, but can utilize
preformed folic acid.

Test for Efficacy of

Antimicrobial Drugs
By: Merced, Yno & Mendoza,
Patricia

Diffusion susceptibility test or the

Kirby-Bauer test
Key terms
Zone of Inhibition an area where the antibiotic inhibits
bacterial growth
Antibiotic Susceptibility- a test whether the antibiotic is
susceptible to bacteria or not
Mueller-Hinton agar- the agar used for Kirby-Bauer test

Procedure
Antimicrobial drugs are positioned the surface of
the Mueller Hinton agar (MHA)
The MHA is freshly inoculated with standardize
amount of pathogen
After incubation, look and measure the zone of
inhibition
Compared to a standard table for particular drug
and classified as: Susceptible, intermediate, or
resistant

Mueller Hinton Agar (MHA)

2.0g beef extract

17.5gcaseinhydrolysate
1.5gstarch
17.0gagar

Kirby-Bauer Test

Minimum Inhibitory
Concentration Test (MIC)

Key Terms
Minimum Inhibitory Concentrationrefers to the smallest amount of the
drug that inhibits the growth and
reproduction of a pathogen
Broth microdilution- the method used
to test MIC

Procedure
First is the antimicrobial drugs is serially diluted in broth
medium contained in tubes or wells
A standardize amount of pathogen is added to the tubes
After incubation, turbidity in tubes indicates bacterial
growth while lack of it means the pathogens were
either inhibited or killed
The lowest concentration of the drug that did not show
any turbidity is referred as the MIC against that
particular pathogen

Minimum Inhibitory Concentration

test

E-test
Combines aspects of MIC test & diffusion susceptibility test.
Processed like Kirby-Bauer test
Uses principle of a predefined antibiotic gradient on plastic
strip.
after incubation, The MIC is read

MIC value

intersectio
n of zone
of
inhibition
in e-test
strip

MBC (Minimum Bactericidal

Concentration) test

Also called MLC or Minimum Lethal Concentration Test.

kills microorganism
Refers to minimum concentration
Extension of MIC test
Samples from all the clear tubes in MIC test are inoculated
into sterile drug-free agar medium.
After incubation, growth on plates must check.
highest dilution (lowest concentration)

Undesirable Effects of
Antibiotics
Micaya, Dana Mae
Millado, Sheila Jane

Some Adverse Effects of Antibiotics

include;
Resistant Microorganisms - that survive the
effects of an antimicrobial agent, multiply and
become pre-dominant and can be transmitted
Allergic reactions hyposensitivity, hives,
anaphylactic shock
Toxic Effects toxic at high concentrations
Superinfection suppression of normal flora

Other Adverse Effects

Antibiotic-associated Diarrhea - occurs due

to eradication of the normal gut flora by the
antibiotic and results in an overgrowth of
infectious bacteria
Vaginal yeast or Oral Thrush - is also a
change in the normal flora balance in the
vagina, leading overgrowth of fungal species
Stevens Johnson Syndrome, Toxic
Epidermal Necrolysis - rare but serious
allergic reactions to substances that result in
serious skin and mucuous membrane disorders.
Phlebitis (vein inflammation) - reaction in
the injection site

Chloramphenicol
Names - Chloromycetin, Econochlor, Ocu-Chlor
Mode of Action inhibition of protein synthesis
Used for - Chloramphenicol is effective againstS.
typhi, H. influenzae,E. coli ,Neisseria
spp.,StaphylococcusandStreptococcus species,
Rickettsia, and lymphogranuloma-psittacosis group
of organisms.
Adverse Effects - headache ,
mentalconfusion,fever,rash,diarrhea, and optic
atrophy, may cause Gray syndrome and serious, fatal
blood dyscrasias, Blood dyscrasias are reductions in
blood cells leading toaplastic anemia

CEPHALOSPORINS

Names - cephalexin, cefaclor, cefuroxime, cefepime,

ceftaroline
Mode of Action interfere with cell wall synthesis
Used for against G+ (1st gen),
against G- (2nd gen),
greater activity against G- like Pseudomonas
aeruginosa & aerobic G- (3rd gen),
against both G+ and G- including P. aeruginosa (4th
gen) and
against G+ aerobic cocci including MRSA and MRSE
(5th gen)
Adverse Effects rash, diarrhea, nausea/vomiting
(rare), hypersensitivity (allergic) reactions, serum
sickness, vaginal candidiasis

CARBAPENEMS
Names meropenem, ertapenem, doripenem,
imipenem-cilastatin
Mode of Action inhibit cell wall synthesis
Used for effective against aerobic Gram+, most
aerobic Gram-, and most anaerobes, very useful in
treating bacterial infections where beta-lactamase is
produced that makes other beta-lactam antibiotics
ineffective.
Adverse Effects diarrhea, nausea/vomiting,
headache, rash, liver toxicity, eosinophilia (elevated
white blood cells), Hypersensitivity reactions reported
with meropenem, imipenem in patients with penicillin
allergy

MACROLIDES
Names erythromycin, azithromycin,
clarithromycin
Mode of Action inhibit protein synthesis
Used for bacteriostatic in lower doses an
bactericidal at higher dose, effective against
chlamydias, mycoplasmas, T. pallidum, and
Legionella spp.
Adverse Effects abdominal pain, diarrhea,
anorexia, nausea/vomiting, taste alterations
(clarithromycin), high rate of gastrointestinal
side effects

FLUORQUINOLONES
Names ciprofloxacin (Cipro), levofloxacin
(Levaquin), moxifloxacin (Avelox), ofloxacin
(Floxin)
Mode of Action inhibit DNA synthesis
Used for most commonly used (ciprofloxacin) is
effective against members of the family
Enterobacteriaceae and P. aeruginosa
Adverse Effects nausea/vomiting, diarrhea,
abdominal pain, headache, lethargy, insomnia,
photosensitivity (can be severe), moxifloxacin
associated with higher rates of side effects;
tendon rupture more common in age > 60

PENICILLIN
Names -Amoxicillin(Amoxil),
Ampicillin(Omnipen), Penicillin G(Bicillin
L-A),Penicillin V(Beepen-VK)
Mode of Action- inhibitingpenicillinbinding proteins
Used for-Natural penicillin are effective
against some Gram-positive bacteria,
some anaerobic bacteria and
spirochetes(esp. Streptococcus spp.);
Gram-negative bacteria remain
susceptible to natural penicillins.

Adverse Effectsdiarrhea that is

watery or
bloody;fever, chills,
body aches, flu
symptoms;nausea,
vomiting, stomach
pain;vaginal itching
or
discharge;Headach
e

Aminoglycosides
Names
Amikacin(Amikin),Kanamycin(Kantrex),Neom
ycin(Mycifradin)
Mode of Action-Inhibition of Protein
Synthesis
Used for-Used to treat infections of the
family Enterobacteriacase and Vibrio chlerae.
Ex:E.coli , Klebsiell, and Proteus
Adverse Effects-Hearing loss,Vision
problems,Kidney damage (nephrotoxicity)

Tetracylines
NamesDoxycycline(Doryx),Minocycline(Dynaci
n),Tetracyclin(Achromycin)
Mode of Action-protein synthesis
inhibitors
Used for-They are also effective to the
variety of bacteria including chlamydia,
mycoplasma, rickettsias, Vibrio Chlerae,
and Spirochetes

Adverse Effectssores or swelling in

your rectal or genital
area;mild nausea,
vomiting, diarrhea,
or stomach
upset;white patches
or sores inside your
mouth or on your
lips;swollen tongue,
trouble swallowing;
or.vaginal itching or

Bacitracin
Names-BACiiM ,Baci-Rx
Mode of Action-dephosphorylation
of bactoprenol
Used For- Treats staph infection
caused by bacteria called
staphylococcus.(pneumonia)
Adverse Effects- pain, burning,
neausea,vomiting, blood in the urine,
lower back pain

Vancomycin
Names-Vancocin,Vancocin HCl,
Lyphocin,Vancocin HCl Pulvules
Mode of Action- by inhibiting proper
cell wall synthesis
Used for- used to treat aninfectionof
the intestines caused byClostridium
difficile, which can cause watery or
bloodydiarrhea. It is also used to
treatstaph infectionsthat can cause
inflammation of the colon and small

 Adverse Effectsdizziness, difficulty

hearing(hearing
loss), signs of
kidney problems
(such as change in
the amount of
urine),fever, chills,
persistentdiarrhea