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Antiobiotics

Membrane
integrity

Cell wall

B-lactam
drugs

Polypeptides
drugs

Glycopeptide
drugs

Nucleic
acid
synthesis

Protein
synthesis

Colistin
AntiTetra- Chloroam- MacroAmino
(plymixen Fungal
glycosides cycline phenicol
lides
E)
Drugs

Penicillins
imidazole

Lincosemides

Fusidic
acid

-Ketoconazole(oral)
-Clotrimazole(all
forms)
-Fluconazlo/Itraconazloe

Cephalo
sporins

Carbapenems

Monobactams

triazloe

-New/more effective/less toxic


-oral/topical for systematic
infections

polyenes

Large circular molecule consisting


of hydrophilic & hydrophobic
regions
-Skin/hair infections

Nystatin

-Oral/topical
-safe

AmphoTercin
B

-systematic infections
-IV mainly
-Toxic

Essential
metabolites
synthesis

Sulfa
-Nalidixic
Quinodrugs
acid
Rifamycin lones
-Nitro Rifampin Fluro- (sulfonafurantion
quinoloes mides)

AntiTuber
culosis
drugs

-Ex:INH+streptomycin
Ethambutol+rifampin

Cell wall

B-lactam
drugs

Penicillins

Penicillin G
Penicillin V
*A*

Ampicillin
Amoxacilllin
*B*

Cephalosporins

First
generation(1960s)
Cephradine
cephaexin
Cephalothin

Second generation
(1970s-1980s)
Cefoxitin
Cefuroxime

Polypeptide
drugs

Carbapenems

Imipenem
Entrapenem
Meropenem

-For Nosocomial
infections

Ticarcillin
carbencillin
Piperacillin
*D*

Fourth generation
(1995)
cefepime

-Mainly against gram


ve Enteric bacteria.
-used against:
E.coli/Klebsiella/entero
bacter/acinobacter/pse
udomonas aeruginosa

-polyenes
-bacteriocidal

-Broad spectrum
-for
serious/nosocomial

Third generation
(1980s-1990s)
Ceftrazidime
cefotaxime
Ceftriaxone

Aztreonam

-IV/IM

-IV/IM

-Bacetracin
-Colistin
(polymixen B)

-broad
spectrum

-peniciliinase R

Infections
Methicillin
Oxacillin
Cloxacillin
Augmentin
*C*

monobactams

-mainly against gram


ve
Bacteria
-bacteriocidal

-beaks down
phospholipids
of bacterial
cell membrane
changing
membrane
permeability.
-very
toxic( has side
effects)

-used against:

-has amino &


nitro groups

Pseudomonas
aeruginosa

-used against:

-More effective than


group
*D*

MR-pathogens
&
Acinobacter(ca
using
septicemia)
-nephrotoxic
-oral/topical
except on

Glycopeptides
drugs

Vancomysin
Teicoplanin

-used against:
*ORSA
*MRSA
*Multi Renterococci(E.fecal
is)
*but not gram Ve
bacteria.
-interfere with
enzymes
responsible for
cross linking of
peptidoglycan
layer.
-Inject able not
oral.
-useful in clinical
practice.

-originated from orange filamentous fungus


called (cephalosporium)
-used for treatment of
UT/RT/CSF/blood/intestinal/wound infections
-They cant affect Anaerobic bacteria
-They cant affect enterococcus group (UT
infecting/naturally resistant to cephalosporin's)

Fisrt generation

-similar activity to
ampicillin &
amoxicillin
-decreased usage by
time
-They have narrower
spectrum than other
drugs.

Cephalosporins

Second generation

-broad spectrum
-affect
Facultative
anaerobic
bacteria
-used especially
in surgeries

Third generation

-Mainly against
G-ve bacteria
-They are
expected to be
unavailable in the
next 5 years.

Fourth generation

-Affect mainly Gve bacteria like


pseudomonas
-used in
hospitals.

-not effective with


developing bacteria
-Broad spectrum

B lactam drugs side effects :sensitization/fever/serum sickness/penicillin


allergy/anaphylactic shock/nephritis

Penicillin
-Bactericidal
-Affect + Anaerobic/narrow
spec.
-Injected (not orally since
its inactivated by stomach
acids)
-1940-1941

*A*

*B*

*C*

-broad spectrum

Penicillin G

-Narrow
spectrum

-1965

-From organsim penicillium


notatum

(-Ve)

-Affect facultative
anaerobic bacteria
found in intestine.

Penicillin V

*D*

-mid 70s
-B lactamase
susceptible.
-For nosocomial
infections.

-Bactericidal
-Affect
+Anaerobic/narrow
spec.
*C*

-can be taken
orally (not
inactivated)
-1942-1943
-its a modified
penicillin G

Methicillin

Oxacillin

Cloxacillin

Augmentin

-first drug produced


to resist
penicillinases
-1960s
-not used any more
unstable/inactivated
at room
temperature
-has side effects
-modified to
oxacillin &

-narrow spectrum(+ve)
-used in laboratory and
Clinical Practise
-used against ampicillin
amoxicillin
Penicllin G,V resistant bacteria
-1960s

-Amoxacillin+clavulanic
acid
-Broad spectrum
-Penicillinase resistant
(due to
The presenece of
Clavulanic acid)

Protein
synthesis

-Can be inhibited by bacterial


Enzymes
-IV/acid unstable

Tuberculosis

Intestinal infection

Meningitis
sepsis

AminoGlysocides
(30s subunit)

streptomycin

Neomycin
Konamycin

Gentamycin
Tobramycin
Netilimycin
Amikacin

TetraCyclines
(30s subunit)

Doxycycline
minocycline

-Broad spectrum.
-Orally or injected
(orally more common)
-Not given to cildren
Under 8
-For Ut/Rt infections
Caused by
mycoplasma
,clamydia and
Legionella.

ChloramPhenicol
(50s subunit)

MacroLides
(5os subunit)

LincoSamides
(50s subunit)

Erythromycin
Clarithromycin
azithromycin

-For UT/RT infections like


Pneumonia & diphtheria
-For mycoplasma/clamydia/
Staphylococcus/legionella
Infections
-inhibit peptidyl
transferase activity
& translocation
of growing peptide to
Ribosome
-most applied orally/less IV

-Broad spectrum
-block peptide bond formation
-For intestinal/skin/respiratory
/CNS infections
Ie:Meningitis /septicemia/thyoid fever/
Aplastic anemia
-can cross the blood brain barrier

Fusidic acid

-applied topically
(creams/eye drops)
-for skin infections
-steroidal/prevent
t-RNA translocation
To ribosomes
-not used in system.
Infections very toxic
-metronidazol(flagyl)
is an example.

-For oral/bone infections


-promotes the growth of
colstridium Difficile
causing pseudoMembranous colitis
blood diarrhea( in colon)
-used against strpt./staphy.
infections

Anti fungal drugs: F/Cl/H/N groups.for Fungal infections caused bu yeast(candida


intestinal flora) & filamentous fungi (molds)toxic drugs

Nucleic acid
synthesis

Nalidixic acid

-affect mainly G-Ve


Bacteria in
UT.
-for UT infections
-used agains E.coli (responsible
For 70%-80% of UT
Infections)
-Acts on DNA gyrase
(type of DNA
Polymerase)

Rifamycin

quinolones

-prevent transcription
by binding to RNA
Polymerase
-Broad spectrum
-effective in killing
IC Bacteria
-used for serious infection
Meningitis /brucellosis
Not for simple RT infection
(WHO)
-Bacteria May produce enzyme
affect B Subunits in RNA
Polymerase Developing
resistance to these drugs
-less toxic then aminoglysocides.

Norfloxacin

UT/RT infections

Ciprofloxacin

UT/RT(pneumonia)/
Intestinal/blood
(septicemia)
infections

Levofloxacin

Upper RT infections