ANTIMICROBIAL THERAPY:

Cell Wall Inhibitors

ANA KHUSNUL FAIZAH

DEPARTEMEN FARMASI KLINIK

PRODI FARMASI FAKULTAS KEDOKTERAN
UNIVERSITAS HANG TUAH
2016

ANTIMICROBIAL THERAPY
EMPIRIC

Katzung Basic and Clinical Pharmacology 11th ed

Choice of Antimicrobial
Agent
Host factors

Katzung Basic and Clinical Pharmacology 11th ed

Monitoring Therapeutic
Response
Microbiologically

Katzung Basic and Clinical Pharmacology 11th ed

Antimicrobial Drug
Combinations
To provide broad-spectrum empiric therapy in seriously ill patients

Katzung Basic and Clinical Pharmacology 11th ed

Mechanisms of Drug Resistance

significant increase in the rate of killing

bacterial killing as the concent
Concentration-dependent
Concentration-dependent
significant increase in the rate of killing
bacterial killing as the concent
aminoglycosides

Classification of antibacterial agents

into bactericidal and bacteriostatic

Classification of antibacterial agents

according to mechanism of action

Classification of antibacterial agents

according to mechanism of action

Cell Wall Inhibitors

Structure of -Lactam Antibiotics

MECHANISM OF ACTION PENICILLIN

Resistance to penicillins and other

lactams
mechanisms:
inactivation of antibiotic by lactamase,
-Lactamase production is the most common mechanism of
resistance. Produced by Staphylococcus aureus,Haemophilus
sp, and Escherichia coli, are relatively narrow in substrate
specificity, preferring penicillins to cephalosporins.
Other lactamases, eg, AmpC lactamase produced by
Pseudomonas aeruginosa and Enterobacter sp, and
extended-spectrum lactamases (ESBLs), hydrolyze both
cephalosporins and penicillins.
Carbapenems are highly resistant to hydrolysis by
penicillinases and cephalosporinases, but they are
hydrolyzed by metallo- lactamase and carbapenemases.

 -Lactamase Inhibitor
Combinations
amoxicillin
piperacillin
ticarcillin-clavulanic
ampicillin-sulbactam

PHARMACOKINETICS
Except for oral amoxicillin,
Penicillins should be given 12 hours
before or after a meal; they should
not be given with food to minimize
binding to food proteins and acid
inactivation.

ADVERSE EFFECT OF
PENICILLIN

CEPHALOSPORINS

CARBAPENEMS AND
CARBACEPHEMS
The newest classes of -lactam
antibiotics
The first carbapenem, Imipenem is
active against most gram-positive,
gram-negative, and anaerobic bacteria.
Meropenem (Merrem) is another
carbapenem antibiotic with a broad
spectrum of activity comparable to that
of imipenem

All of the following factors influence the

penetration and concentration of an
antibacterial agent in the cerebrospinal
fluid except:
A. Lipid solubility of the drug.
B. Minimum inhibitory concentration of
the drug.
C. Protein binding of the drug.
D. Molecular weight of the drug.

Which of the following is the primary

method of -lactam resistance with
Streptococcus pneumoniae?
A. Modification of target site.
B. Decreased drug levels due to changes
in permeability.
C. Decreased drug levels due to an efflux
pump.
D. Enzymatic inactivation.

Which of the following antibiotics

exhibits concentration dependent
killing?
A. Clindamycin.
B. Linezolid.
C. Vancomycin.
D. Daptomycin.

Which of the following antibiotics

exhibits a long postantibiotic effect
that permits once-daily dosing?
A. Gentamicin.
B. Penicillin G.
C. Vancomycin.
D. Aztreonam.

Which one of the following

antibiotics is bacteriostatic :
a- Erythromycin.
b- Gentamicin.
c- Cefradin. a
d- Ampicillin.

 Which one of the following is

second generation cephalosporin
a- Cephradine.
b- Cefoperazone
c- Cefotaxime
d- Cefoxitine

 Which one of the following drugs

passes blood brain barrier
a- Cephalexin.
b- Cefaclor
c- Ceftriaxone
d- Cephradine.

General principles of anti-infective therapy

are:
a) Clinical judgment of microbiological
factors
b) Definitive identification of a bacterial
infection and the microorganisms
susceptibility
c) Optimal route of administration, dose,
dosing frequency and duration of treatment
d) All of the above

Minimal duration of antibacterial

treatment usually is:
a) Not less than 1 day
b) Not less than 5 days
c) Not less than 10-14 days
d) Not less than 3 weeks

Rational anti-microbial combination is

used to:
a) Provide synergism when
microorganisms are not effectively
eradicated with a single agent alone
b) Provide broad coverage
c) Prevent the emergence of
resistance
d) All of the above

Mechanisms of bacterial resistance to antimicrobial agents are the following, EXCEPT:

a) Active transport out of a microorganism
or/and hydrolysis of an agent via enzymes
produced by a microorganism
b) Enlarged uptake of the drug by a
microorganism
c) Modification of a drugs target
d) Reduced uptake by a microorganism

Bactericidal effect is:

a) Inhibition of bacterial cell division
b) Inhibition of young bacterial cell
growth
c) Destroying of bacterial cells
d) Formation of bacterial L-form

Which of the following antibiotics

contains a beta-lactam ring in their
chemical structure :
a) Penicillins
b) Cephalosporins
c) Carbapenems and monobactams
d) All groups

Tick the drug belonging to antibioticscarbapenems:

a) Aztreonam
b) Amoxacillin
c) Imipinem
d) Clarithromycin

Mechanism of penicillins antibacterial effect is:

a) Inhibition of transpeptidation in the
bacterial cell wall
b) Inhibition of beta-lactamase in the
bacterial cell
c) Activation of endogenous proteases, that
destroy bacterial cell wall
d) Activation of endogenous phospholipases,
which leads to alteration of cell membrane
permeability

Pick out the beta-lactamase inhibitor

for co-administration with penicillins:
a) Clavulanic acid
b) Sulbactam
c) Tazobactam
d) All of the above

Cephalosporines are drugs of choice for

treatment of:
a) Gram-positive microorganism infections
b) Gram-negative microorganism
infections
c) Gram-negative and gram-positive
microorganism infections, if penicillins
have no effect
d) Only bacteroide infections

Carbapenems are effective against:

a) Gram-positive microorganisms
b) Gram-negative microorganisms
c) Only bacteroide infections
d) Broad-spectum