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Antiobiotics

Nucleic Essential
Membrane Protein
Cell wall acid metabolites
integrity synthesis
synthesis synthesis

Polype- Glyco-
B-lactam
ptides peptide -Nalidixic Quino- Sulfa Anti-
drugs Colistin Anti-
drugs drugs Amino Tetra- Chloroam- Macro- Linco- Fusidic acid Rifamycin lones drugs Tuber
(plymixen Fungal
glycosides cycline phenicol lides semides acid -Nitro Rifampin Fluro- (sulfona- culosis
E) Drugs
furantion quinoloes mides) drugs

Penicillins -Ex:INH+streptomycin
-Ketoconazole(oral)
imidazole Ethambutol+rifampin
-Clotrimazole(all
forms)

-Fluconazlo/Itraconazloe
Cephalo -New/more effective/less toxic
triazloe
sporins
-oral/topical  for systematic
infections
Carba-
penems
polyenes Large circular molecule consisting
of hydrophilic & hydrophobic
regions

-Skin/hair infections
Mono-
Nystatin -Oral/topical
bactams
-safe
Ampho-
Tercin -systematic infections
B
-IV mainly
-Toxic
Cell wall

B-lactam Polypeptide Glycopeptides


drugs drugs drugs

-Bacetracin
Vancomysin
Penicillins Cephalosporins Carbapenems monobactams -Colistin
Teicoplanin
(polymixen B)

-broad -used against:


First spectrum
Penicillin G generation(1960s) Imipenem *ORSA
Penicillin V Cephradine Entrapenem Aztreonam -polyenes
cephaexin
*MRSA
*A* Meropenem
Cephalothin -bacteriocidal
*Multi R-
-beaks down enterococci(E.fecal
phospholipids is)
-peniciliinase R -IV/IM of bacterial
Second generation *but not gram –Ve
cell membrane
Ampicillin (1970s-1980s) -Broad spectrum -For Nosocomial bacteria.
changing
Amoxacilllin Cefoxitin infections
Cefuroxime -IV/IM membrane -interfere with
*B* -mainly against gram – permeability. enzymes
-for
ve responsible for
serious/nosocomial -very toxic(
cross linking of
Bacteria has side
Infections peptidoglycan
effects)
Methicillin Third generation
-bacteriocidal layer.
-Mainly against gram –
Oxacillin (1980s-1990s) -has amino &
ve Enteric bacteria. -used against: -Inject able not
Cloxacillin Ceftrazidime nitro groups
oral.
Augmentin cefotaxime -used against: Pseudomonas
Ceftriaxone
-used against:
*C* E.coli/Klebsiella/entero aeruginosa -useful in clinical
bacter/acinobacter/pse MR-pathogens practice.
-More effective than
udomonas aeruginosa &
group
Acinobacter(ca
Ticarcillin *D*
Fourth generation using
carbencillin septicemia)
(1995)
Piperacillin cefepime
*D* -nephrotoxic
-oral/topical
except on
-originated from orange filamentous fungus
called (cephalosporium)
-used for treatment of
UT/RT/CSF/blood/intestinal/wound infections
-They cant affect Anaerobic bacteria
Cephalosporins
-They cant affect enterococcus group (UT
infecting/naturally resistant to cephalosporin's)

Fisrt generation Second generation Third generation Fourth generation

-similar activity to -broad spectrum -Mainly against -Affect mainly G-


ampicillin & G-ve bacteria ve bacteria like
-affect
amoxicillin pseudomonas
Facultative -They are
-decreased usage by anaerobic expected to be -used in
time bacteria unavailable in the hospitals.
next 5 years.
-They have -used especially
narrower spectrum in surgeries
than other drugs.
-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. *A* *B* *C* *D*

-Injected (not orally since


its inactivated by stomach
acids) -broad spectrum -Narrow
Penicillin G
-1940-1941 spectrum
-1965
-From organsim ”penicillium (-Ve)
-Affect facultative
notatum” anaerobic bacteria -mid 70s
Penicillin V found in intestine.
-B lactamase
susceptible.
-For nosocomial
-Bactericidal infections.
-Affect
+Anaerobic/narrow
spec.
-can be taken *C*
orally (not
inactivated)
-1942-1943
-it’s a modified
penicillin G

Methicillin
Oxacillin Cloxacillin Augmentin

-first drug produced


to resist
penicillinases
-1960s -Amoxacillin+clavulanic
-narrow spectrum(+ve)
acid
-not used any more -used in laboratory and
-Broad spectrum
-unstable Clinical Practise
-Penicillinase resistant
/inactivated at room -used against ampicillin
temperature (due to
amoxicillin
The presenece of
-has side effects Penicllin G,V resistant bacteria
Clavulanic acid)
-modified to -1960s
oxacillin &
cloxacillin
Protein
synthesis

-Can be inhibited by bacterial


Enzymes Amino- Tetra- Chloram- Macro- Linco-
-IV/acid unstable Glysocides Cyclines Phenicol Lides Samides Fusidic acid
(30s subunit) (30s subunit) (50s subunit) (5os subunit) (50s subunit)

-applied topically
Erythromycin
Doxycycline (creams/eye drops)
Tuberculosis streptomycin minocycline
Clarithromycin
-for skin infections
azithromycin
-steroidal/prevent
t-RNA translocation
To ribosomes
-Broad spectrum. -For UT/RT infections like -not used in system.
-Orally or injected Pneumonia & diphtheria Infections very toxic
Neomycin (orally more common) -For mycoplasma/clamydia/ -metronidazol(flagyl)
Intestinal infection Konamycin -Not given to cildren Staphylococcus/legionella is an example.
Under 8 Infections
-For Ut/Rt infections -inhibit peptidyl
Caused by transferase activity
mycoplasma & translocation
Meningitis Gentamycin ,clamydia and of growing peptide to
Tobramycin Legionella. Ribosome
sepsis Netilimycin -most applied orally/less IV
Amikacin

-Broad spectrum -For oral/bone infections


-block peptide bond formation -promotes the growth of
-For intestinal/skin/respiratory colstridium Difficile
/CNS infections causing pseudo-
Ie:Meningitis /septicemia/thyoid fever/ Membranous colitis
Aplastic anemia blood diarrhea( in colon)
-can cross the blood brain barrier -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 Rifamycin quinolones

-prevent transcription
-affect mainly G-Ve
by binding to RNA Norfloxacin UT/RT infections
Bacteria in
Polymerase
UT.
-Broad spectrum
-for UT infections
-effective in killing
-used agains E.coli (responsible UT/RT(pneumonia)/
IC Bacteria
For 70%-80% of UT Intestinal/blood
-used for serious infection Ciprofloxacin
Infections) (septicemia)
Meningitis /brucellosis
-Acts on DNA gyrase infections
Not for simple RT infection
(type of DNA
(WHO)
Polymerase)
-Bacteria May produce enzyme
affect B Subunits in RNA Levofloxacin
Polymerase Developing
Upper RT infections
resistance to these drugs
-less toxic then aminoglysocides.