ANTIBACTERIAL

ANTIBIOTICS
OBJECTIVES:
• To discuss the historical background
of antibiotics;
• To enumerate the requirements for
antibiotics;
• To classify the B-lactam antibiotics
and discuss their MOA;
• To classify the penicillins based on
their activities.
Historical Background
• Sir Alexander Fleming -
accidentally discovered the
antibacterial properties of
penicillin from Penicillium
notatum in 1929
• Florey & Chain - purify
penicillin and introduced it into
therapy
• Pasteur & Joubert -
discovered the anthrax bacilli
ANTIBIOTIC
• a substance produced by
microorganisms, which has the
capacity of inhibiting the growth
and even of destroying other
microorganisms (Waksman,
1942)
Requirements for Antibiotics
• It is a product of metabolism
(although it may be duplicated or
even have been anticipated by
chemical synthesis)

• It is a synthetic product produced as a

structural analog of a naturally
occurring antibiotic
• It antagonizes the growth or
survival of one or more species of
microorganisms

• It is effective in low
concentrations.
 β-LACTAM
ANTIBIOTICS
• Penicillins
• Cephalosporins
Mechanism of Action
• interfere with the last step of
bacterial cell wall synthesis
(transpeptidation or cross-
linking of peptidoglycan
chains)
PENICILLINS
• beta-lactam attached to
thiazolidine ring
• nucleus: 6-aminopenicillanic
acid
Bacterial Resistance
• Penicillinases (β-lactamases) -
enzymes that catalyze the
hydrolytic opening of the β-lactam
ring of penicillins to produce
inactive penicilloic acid (S.
aureus and most gram-negative
bacteria)
Spectrum of Activity
• Effective against gram-
positive, spirochetes and
anaerobe bacteria
• Some gram-negative bacteria
and mycoplasma are resistant
Adverse Effect
• Hypersensitivity (variety of skin
and mucous membrane
rashes to a drug fever and
anaphylaxis)
 NATURAL
PENICILLINS
PENICILLIN G
• Benzylpenicillin
• given IV/IM
• was made available in the form of
water-soluble salt of potassium,
sodium and calcium
• poorly absorbed from the intestinal
tract, oral doses must be very large
• its rapid elimination from the
bloodstream led to the
development of repository forms
• Repository Forms (IM): Pen G
Benzathine, Pen G Procaine
• DOC for many bacterial infections
(Ex: Rheumatic Heart Disease in
children and Syphilis)
Penicillin G Procaine
• Crysticillin®, Duracillin®,
Wycillin®
• mixture of penicillin with
procaine HCl
Penicillin G Benzathine
• Bicillin®, Permapen®
• gives the compound great
stability and prolonged
duration of action
Penicillin V
• Phenoxymethylpenicillin
• Pen Vee®, V-Cillin®
• acid stable thus used orally
Penicillinase-Resistant
Penicillins/
Antistaphylococcal
Penicillins: Narrow
Spectrum
METHICILLIN
• 2,6-dimethoxyphenylpenicillin
• Staphcillin®
• off the market due to high incidence of
interstitial nephritis
• absence of the benzyl methylene group of
penicillin G and the steric protection by the
2- and 6-methoxy groups makes it
resistant to penicillinase
NAFCILLIN
• 6-(2-ethoxy-1-naphthyl)penicillin sodium
• Unipen®
• acid stable enough to be used orally
• relatively small amounts are excreted
through kidneys, with the major portion
excreted in the bile
• can be given to patients with renal
problem
Isoxazoyl Penicillins
• Oxacillin
• Cloxacillin
• Dicloxacillin
OXACILLIN
• Prostaphlin®
• resistant to acid
hydrolysis thus
administered orally
CLOXACILLIN
• Tegopen®
• resembles oxacillin but oral
absorption is more
enhanced
DICLOXACILLIN
• Dynapen®, Pathocil®,
Veracillin®
• similar to cloxacillin
• enhanced stability
AMINOPENICILLINS
• have an antibacterial spectrum similar
to that of Pen G but are more
effective against gram-negative bacilli
AMPICILLIN
• Penbritn®, Polycillin®,
Omnipen®, Amcill®, Principen®
• poor GI absorption
• more frequently administered
parenterally
• not resistant to penicillinase
• used in UTI caused by E.coli or
P.mirabilis
• DOC for Haemophilus influenzae
infection
• Ampicillin + Probenecid = DOC for
gonorrhea
• oral dose should be repeated every
6 hours because its is excreted
rapidly and unchanged through the
kidneys
Prodrugs of Ampicillin
• Bacampicillin
• Cyclacillin
• Hetacillin
BACAMPICILLIN
• Spectrobid®
• has no antibacterial property
• hydrolzyed rapidly be
esterases in the plasma to
form ampicillin
AMOXICILLIN
• Amoxil®, Larotid®,
Polymox®
• better GI absorption than
ampicillin
• resistant to acid but not with
penicillinases
ANTIPSEUDOMONAL
PENICILLIN/
EXTENDED
SPECTRUM
CARBOXYPENICILLINS
• Carbenicillin
• Ticarcillin
CARBENICILLIN DISODIUM
• Geopen®, Pyopen®
• broader range of antimicrobial activity
than any other known penicillin
• not stable in acid and penicillinase
• can be used for infections caused by
gram-negative bacteria
Carbenicillin Indanyl Sodium
• Geocillin®
• provides orally active alternative for
the treatment of carbenicillin-sensitive
sytemic and urinary tract infections
caused by Pseudomonas spp, indole-
positive Proteus spp., and selected
Gram-negative bacilli
TICARCILLIN
• Ticar®
• unstable in acid thus
administered parenterally
UREIDOPENICILLINS
• Piperacillin - most potent
• Azlocillin
• Mezlocillin
MEZLOCILLIN
• Mezlin®
• recommended for the treatment of
serious infections caused by
Klebsiella spp., P. aeruginosa, H.
influenzae and anaerobic bacteria
• unstable in acid and penicillinases
PIPERACILLIN
• Pipracil®
• most active against gram-
negative bacteria
• destroyed rapidly by stomach
acid, give IV or IM
β-LACTAMASE
INHIBITORS
• structurally related to beta-lactam ring
of penicillin
• do not have significant antibacterial
activity
• "suicide substrates"
• MOA: binds to and inactivate beta-
lactamases
CLAVULANIC ACID
• an antibiotic isolated from
Streptomyces clavuligeris
• has a very weak
antibacterial activity
CO-AMOXICLAV
• combination of clavulanic acid and
amoxicillin (Augmentin®)
• intended for the treatment of skin,
respiratory, ear, and urinary tract
infections caused by β-lactamase
producing bacterial strains (S. aureus,
E.coli, K. pneumoniae, Enterobacter,
Moraxella catarrhalis, Haemophilus
ducreyi)
Ticarcillin + Clavulanate K
• Timentin®
• recommended for septicemia,
LRTI and UTI cause by β-
lactamase-producing bacteria
• also used in bone and joint
infections caused by these
organisms
SULBACTAM
• combined with ampicillin called
sultamicillin (Unasyn®)
• Recommended for the treatment of skin,
tissue, intra-abdominal, and gynecological
infections caused by β-lactamase-
producing strains of S. aureus, Klebsiella
spp., P. mirabilis, B. fragilis, Enterobacter,
and Acinetobacter spp.
TAZOBACTAM
• a more potent β-lactamase inhibitor
• combined with Piperacillin (Zosyn®,
Tazocin®)
• approved indications include
appendicitis, postpartum endometritis,
pelvic inflammation disease, skin
infections, and pneumonia caused by
β-lactamase producing bacteria
CARBAPENEMS
• differ with penicillin in that the
sulfur atom of the thiazolidine
ring has been externalized and
replaced by a carbon atom
THIENAMYCIN
• isolated from Streptomyces cattleya
• outstanding broad-spectrum
antibacterial properties in vitro against
most aerobic and anaerobic gram-
positive and gram-negative bacteria
• resistant to β-lactamases
• susceptible to acid and alkaline
hydrolysis
IMIPENEM
• retains the extraordinary spectrum of
thienamycin
• undergoes cleavage by
dihydropeptidase
• combined with Cilastatin (Primaxin),
an inhibitor of DHP-I
• Imipenem + Aminoglycoside
(Synergistic action)
MEROPENEM
• Meronem®
• a second-generation carbapenem
• has been approved for the treatment
of infections caused by multiple-
resistant bacteria and for empirical
therapy for serious infections
• exhibits greater potency against
gram-negative and anaerobic
bacteria but slightly less active
against most gram-positive
bacteria than imipenem
• not hydrolyzed by DHP-I and
beta-lactamases
• not active orally
CEPHALOSPORINS
• Beta-lactam antibiotics isolated from
Cephalosporium or prepared
semisynthetically
• Beta-lactam ring attached to
dihydrothiazine ring
• nucleus: 7-aminocephalosporanic
acid
• classified into 4 generations
Spectrum of Activity
• considered broad-spectrum
antibiotics with pattern of
effectiveness comparable to
that of ampicillin
Advantages of Cephalosporins
• resistance to inactivation by β-
lactamases
• permeability of bacterial cells
• intrinsic activity against bacterial
enzymes involved in cell wall
synthesis and cross-linking
Adverse Reactions
• Hypersensitivity
• Has cross-sensitivity reactions
with penicillins
• Disulfiram-like effect
(Cefamandole, Cefotetan,
Cefmetazole, Cefoperazone)
Generation Gram-Positive Gram-Negative

First +++ +

Second +++ ++

Third + +++

Fourth ++ ++++
First Generation
• Cefadroxil, Cephapirin, Cefalexin,
Cephradine, Cefazoline,
Cephalothin

Starts with "Cefa" or "Cepha"

except Cephradine
Second Generation
• Cefaclor, Cefoxitin, Cefonicid,
Cefuroxime, Cefamandole,
Cefpodoxime, Cefprozil,
Loracarbacef, Cefotetan

Starts with "Cef" and nothing ends with

"-ime" or "-one" except Cefuroxime,
Cefpodoxime and Loracarbacef
Third Generation
• Cefoperazone, Ceftriaxone,
Ceftibuten, Cefdinir, Cefotaxime,
Moxalactam, Ceftidoxime, Cefditoren.
Cefixime

Starts with "Cef" and ends with "-ime"

or "-one" except Ceftibuten, Cefdinir,
Moxalactam and Cefditoren
Fourth Generation
• Cefepime, Cefpirome
Fifth Generation
• Ceftabiprole
• Ceftaroline
AMINOGLYCOSIDES
• Gentamicin
• Tobramycin
• Amikacin
• Neomycin
• Kanamycin
• Streptomycin
• Streptomycin - first
aminoglycoside discovered
• obtained from Streptomyces
spp. (-mycin) and
Micromonospora spp. (-micin)
• bactericidal
• absorbed poorly after oral
administration due to its highly
POLAR structure, thus given
parenterally
• all must be given parenterally to
achieve adequate serum levels
except Neomycin (oral or topical
only)
• Synergistic with beta-lactam
antibiotics
Chemistry
• structures
consist of
amino sugars
linked
glycosidically
Mechanism of Action
• acts directly on the bacterial ribosome
to inhibit the initiation of protein
synthesis and to interfere with the
fidelity of translation of the genetic
message
• binds to the 30S ribosomal subunit to
form a complex that cannot initiate
proper amino acid polymerization
SAR
• Ring I - crucially important for
characteristic broad spectrum
antibacterial activity and the
primary target for bacterial
inactivating enzymes
• Ring II (deoxystreptamine) -
modifications of functional
groups are possible without
appreciable loss of activity in
most of the aminoglycosides
• Ring III - functional groups
appear to be somewhat less
sensitive to structural
changes than those of
either ring I or II
ADVERSE EFFECTS
• Ototoxicity (NAK)
• Nephrotoxicity (NGT)
STREPTOMYCIN
• from Streptomyces griseus
• acid hydrolysis yields streptidine
and streptobiosamine
• Streptomycin A - refers to
streptomycin
• Streptomycin B -
mannisidostreptomycin
Uses
• as an adjunct treatment for
PTB
• tx for "occupational" bacterial
infections (brucellosis,
tularemia, bubonic plague,
glanders)
• given IM
NEOMYCIN
• Mycifradin®, Neobiotic®
• from Streptomyces fradiae
• used in treating GI, dermatological
infections and acute bacterial
peritonitis
• absorbed very slightly from the
digestive tract
PARAMOMYCIN
• Humatin®
• resembles streptomycin and
neomycin in antibiotic activity
• used in GI infections caused
by Shigella & Salmonella spp.,
and EPEC
KANAMYCIN
• Kantrex®
• from Streptomyces kanamyceticus
• use is restricted to infections of the
intestinal tract and those arising from
Gram-negative bacilli that have
developed resistance to other
antibiotics
AMIKACIN
• Amikin®, Amikacide®
• semisynthetic aminoglycoside prepared
from Kanamycin
• resists attacks by most bacteria-
inactivating enzymes
• recommended for the treatment of serious
infections caused by bacterial strains
resistant to other aminoglycosides
GENTAMICIN
• Garamycin®
• obtained from Micromonospora
purpurea
• effective in the treatment of various
skin infections (can be applied
topically)
• reserved treatment for burns
complicated by pseudomonemia
• IV preparations are used for
serious systemic and
genitourinary tract infections
caused by Gram-negative
bacteria
TOBRAMYCIN
• Nebcin®
• obtained from Streptomyces
tenebrarius
• very effective against
Pseudomonas aeruginosa
(activity is twofold to fourfold than
gentamicin)
NETILMICIN
• Netromycin®
• obtained from Micromonospora
inyoensis
• used for infections caused by
Gentamicin-resistant strains
SISOMICIN
• its effectiveness against
aminoglycoside-inactivating
enzymes resemble those of
gentamicin
SPECTINOMYCIN
• Trobicin®
• isolated from Streptomyces
spectabilis
• once called actinospectocin
• administered by deep IM
injection
• MOA is the same with other
aminoglycosides antibiotic but
it doesn't cause misreading of
the messenger
• exerts a bacteriostatic action and
is inferior to other
aminoglycosides for most
systemic infections
• recommended as an alternative to
penicillin G for uncomplicated
gonorrhea
TETRACYCLINES
• broadest spectrum antibiotic
• obtained from Streptomyces
aureofaciens
• encapsulated because of their
bitterness
Mechanism of Action
• specifically inhibits bacterial
protein synthesis by binding
to the 30S ribosomal
subunit
SAR
• contain four fused rings with a system of
conjugated double bonds
Spectrum of Activity
• Gram-positive bacteria
• Gram-negative bacteria
• Spirochetes
• Mycoplasma
• Rickettsia
• Chlamydia
ADVERSE EFFECTS
• Gastric discomfort
• Deposition in bones and primary dentition
causing discoloration and hypoplasia of
the teeth
• Temporary stunting of growth
• Hepatotoxicity
• Phototoxicity (Demeclocycline)
• Vestibular problems (Minocycline)
CONTRAINDICATIONS
• Children
• Pregnant Women
• Concomitant use with antacid
and other metal-containing
drugs
TETRACYCLINE
• Achromycin®, Cyclopar®,
Panmycin®, Tetracyn®
• also available in ointments for
topical & ophthalmic use
• topical solution is used for Acne
vulgaris
CHLORTETRACYCLINE
• Aureomycin HCl®
• oral & parenteral forms are
no longer use, only the
ointment form for topical
and ophthalmic use
ROLITETRACYCLINE
• Syntetrin®
• first introduced for use by IM or IV
injection
• recommended for cases when
oral dosage forms are not
suitable, but is no longer widely
used
OXYTETRACYCLINE
• Terramycin®
• from Streptomyces rimosus
• analog of chlortetracycline
with the similar antibiotic
properties
METHACYCLINE
• Rondomycin®
• obtained from chemical
modification of oxytetracycline
• 600 mg = 1g of tetracycline
(higher potency)
• 300 mg dose lasts for 12 hours
DEMECLOCYCLINE
• Declomycin®
• obtained from a mutant
strain of S. aureofaciens
• S/E: Photosensitivity
MECLOCYCLINE
• Meclan®
• also derived from
oxytetracyline
• used only for the treatment of
acne
DOXYCYCLINE
• Vibramycin®
• preferred for uremic patients
with infections outside the
urinary tract
• also used for malaria
MINOCYCLINE
• Minocin®, Vectrin®
• the most potent tetracycline
currently used in therapy
• highly effective for Gram-positive
bacteria
• recommended for treatment of
chronic bronchitis and URTI
Newer Tetracycline
•Tigecycline
MACROLIDES
•Clarithromycin
•Azithromycin
•Roxithromycin
(Macrol)
•Erythromycin
• isolated from Actinomycetes
• Picromycin - first macrolide
identified
CHEMISTRY
• common chemical
characteristics:
- a large ketone ring
- a ketone group
- a glycosidically linked amino
sugar
MECHANISM OF ACTION
• binds selectively to a specific
site on the 50S ribosomal
subunit to prevent the
translocation step of bacterial
protein synthesis
RESISTANCE
• most of the Gram-negative
bacilli are resistant due to
the inability of macrolides to
penetrate the cell wall of
these organisms
Spectrum of Activity
• resembles Pen G but also
effective against mycoplasma,
chlamydia, campylobacter and
legionella, Neisseria and
Treponema pallidum
ADVERSE EFFECTS
• epigastric distress
• cholestatic jaundice
(estolate form of
erythromycin) - gallstone
• enzyme inhibition
ERYTHROMYCIN
• Erythrocin®, Ilotycin®
• from Streptomyces
erythraeus
• formerly Ilotycin (from Iloilo)
• alternative to penicillin
• erythromycin base is
inactivated by gastric juice
• esters of erythromycin base
(e.g. stearate, estolate &
ethylsuccinate) have improved
acid stability, and their
absorption is less altered by
food
Erythromycin Stearate
• Ethril®, Wyamycin S®,
Erypar®
• acid labile
• film coated to protect it from
acid degradation
Erythromycin Ethylsuccinate
• EES®, Pediamycin®,
EryPed®
• absorbed and hydrolyzed to
erythromycin in the plasma
Erythromycin Estolate
• Ilosone®
• acid stable
• higher incidence of
cholestatic hepatitis
Erythromycin Gluceptate
• Ilotycin Gluceptate
• intended for IV administration for the
treatment of serious infections, such
as Legionnaire's disease, or when
oral administration is not possible
• solutions are stable for 1 week if
refrigerated
Erythromycin Lactiobionate
• intended for IV administration
(after reconstitution) to achieve
high plasma levels in the
treatment of serious infection
CLARITHROMYCIN
• Biaxin®, Klaz®
• the 6-methyl ether of erythromycin
• retains antibacterial properties of
erythromycin, with markedly
increased acid stability and and oral
bioavailability
• reduced GI side effects
• more potent than erythromycin
against streptococci and
staphylococci
• may be given with or without food,
but the extended release form,
typically given once daily as a 1g
dose, should be administered with
food to improve bioavailability
• for CAP, Respiratory Tract
Infections and ulcer caused
by Helicobacter pylori
AZITHROMYCIN
• Zithromax®
• unique pharmacokinetic properties include
extensive tissue distribution and high drug
concentration within cells (including
phagocytes), resulting in much greater
concentrations of drugs in tissue or
secretions compared to simultaneous
serum concentrations
• once a day dosing
• should not be administered
with food
• the elimination half-life, 40
to 68 hours, is prolonged
because of extensive tissue
sequestration and binding
DIRITHROMYCIN
• Dynabac®
• a prodrug, releases
erythromycyclamine
• enteric-coated to protect the
drug from acid degradation
TROLEANDOMYCIN
• alternative to erythromycin for
limited indications permitting use
of an oral dosage form
• hydrolyzed in the plasma to
oleandomycin
• spectrum is inferior to
erythromycin
LINCOMYCINS
• sulfur-containing antibiotics
isolated from Streptomyces
lincolnensis
• the most active and medically
useful of the compounds
obtained from fermentation
Spectrum of Activity
• similar to macrolides
Mechanism of Action
• binds to the 50S ribosomal
subunit to inhibit protein
synthesis
• action may be bacteriostatic or
bactericidal depending on
various factors, including the
concentration of the antibiotic
LINCOMYCIN
• Lincocin®
• used for the treatment of infections
caused by Gram-positive organisms
• effective concentrations are achieved
in bone for the tx of staphylococcal
osteomyelitis but not in the CSF
• Adverse effects: severe
diarrhea and
pseudomembranous colitis
CLINDAMYCIN HCl
• Cleocin®
• semisynthetic derivative of lincomycin
• activity against staphylococci,
streptococci & pneumococci is very
high
• one of the most potent agents
available against some non-spore
forming bacteria (Bacteroides)
• Adverse Effects:
- Severe diarrhea
- Clindamycin (Lincomycin)-
associated pseudomembranous
colitis
• caused by Clostridium difficile
• can be life threatening
• reversible when the drug is
discontinued
• Tx: Vancomycin
Clindamycin Palmitate HCl
• Cleocin Pediatric®
• used in pediatrics because it is
tasteless
Clindamycin Phosphate
• Cleocin Phosphate®
• intended for parenteral (IV/IM)
administration for the treatment of
serious infections and instances
when oral administration is not
feasible
OBJECTIVES
• Identify the Polypeptide
Antibiotics and their mechanism
of action;
• Discuss the important unclassified
antibiotics including their
mechanism of action and uses;
• Enumerate the newer antibiotics.
POLYPEPTIDES
• one of the most powerful
antibiotics
• each has different mechanism
of actions
• clinical use has been limited
by their undesirable adverse
effects (renal toxicity)
VANCOMYCIN
• Vancocin®, Vancoled®
• isolate from Streptomyces orientalis
• not active against gram-negative
bacteria except Neisseria
• structure was elucidated via a
combination of NMR and x-ray
crystallography
Mechanism of Action
• Interfere with bacterial cell wall synthesis
by preventing the cell wall mucopeptide
polymer
• it does so by binding to the D-alanine-D-
alanine terminus of uridine diphosphate-N-
acetylmuramyl peptides required for
mucopeptide polymerization
• recommended for use when infection
fails to respond to treatment with
more common antibiotics or when
infection is known to be caused by
resistant strains
• effective for the treatment of
endocarditis caused by Gram-positive
bacteria
TOXICITY
TEICOPLANIN
• Teichomycin A2®, Targocid®
• mixture of 5 closely related
glycopeptides antibiotics
produced by the actinomycete
Actinoplanes teichomyceticus
• D-mannose is common to all
• advantage over vancomycin is
its longer half-life and greater
lipid solubility that makes it
penetrate more to tissues and
phagocytes
• less toxic also than
vancomycin
Mechanism of Action
• impairs bacterial cell wall
synthesis by complexing with the
terminal D-alanine-D-alanine
dipeptide of the peptidoglycan
BACITRACIN
• obtained from Bacillus subtilis
• organism had been isolated from
debrided tissue from a compound
fracture in 7-year old Margaret
Tracey, hence the name
"Bacitracin"
• heavy metals precipitate
bacitracin in the solution resulting
to inactivation
• Zn2+ is required for its activity
• MOA: bactericidal action is due to
the inhibition of mucopeptide cell
wall synthesis
• not absorbed in the GIT
• given topically for local
infections and parenterally for
serious systemic infections
POLYMYXIN B SULFATE
• Aerosporin®
• produced from Bacillus polymyxa
• active primarily against gram-
positive organisms
• mostly administered topically
Mechanism of Action
• interfere with cell membrane
function of the bacteria
COLISTIN SULFATE
• Coly-Mycin S®
• isolated from Aerobacillus
colistinus
• recommended especially for the
treatment of refractory UTI
caused by Gram-negative
organisms
COLISTIMETHATE Na
• Coly-Mycin M®
• given IM
• free from toxicity compared to
polymyxin
• used in the same conditions
mentioned for colistin
GRAMICIDIN
• obtained from Bacillus brevis
• MOA: acts as an ionophore in
bacterial cell membrane to cause
the loss of potassium ion from the
cell
• useful in Gram-negative bacterial
infections
UNCLASSIFIED
ANTIBIOTICS
CHLORAMPHENICOL
• Chloromycetin®
• isolated from Streptomyces
venezuelae
• MOA: exerts its bacteriostatic
action by a strong inhibition of
bacterial protein synthesis (50S
ribosomal subunit)
• Drug of choice for typhoid
fever
• Adverse effects:
- Gray baby syndrome
- Aplastic anemia (low WBC,
RBC & platelets)
Gray Baby Syndrome
Chloramphenicol Palmitate
• palmitic acid ester of
chloramphenicol
• tasteless prodrug intended for
pediatric use
Chloramphenicol Na Succinate
• preferred for IV
administration
NOVOBIOCIN Na
• Albamycin®
• obtained from S. spheroides & S.
niveus
• MOA: bacteriostatic; inhibits bacterial
protein and nucleic acid synthesis
• effective againts Gram-positive and
Proteus vulgaris
MUPIROCIN
• Bactroban®
• from Pseudomonas fluorescens
• MOA: inhibition of RNA and DNA
synthesis
• used topically for impetigo, eczema,
staphylococcal and beta-hemolytic
streptococcal infections
QUINUPRISTIN/DALFOPRISTIN
• Synercid®
• combination at 30:70 ratio
• from S. pristinaspiralis
• active against most Gram-(+)
organisms
• MOA: inhibits protein synthesis
through binding with the 50S
ribosomal subunit
LINEZOLID
• Zyvox®
• MOA: inhibits bacterial proteins
synthesis by binding with 30S
ribosomal subunit
• bacteriostatic agent that is active
against resistant bacterial strains
FOSFOMYCIN
• Monurol®
• a broad-spectrum bactericidal
that inactivates the first
enzyme in the bacterial cell
wall synthesis
 NEWER
ANTIBIOTICS
TIGECYCLINE
• Tygacil®
• MOA: binds to the 30S
ribosomal subunit and blocks
peptide synthesis
AZTREONAM
• a monobactam
• obtained from Chromobacterium
violaceum
• MOA: the same with penicillins
• resistant to penicillanes &
cephalosporinase
• indicated for most Gram-
negative bacteria infections
ERTRAPENEM
• Invanz®
• a carbapenem
• MOA: same with penicillins
TELITHROMYCIN
• Ketek®
• orally available macrolide
• MOA: same with macrolides
• recommended for patients 18
years of age and older
PLATENSIMYCIN
• isolate from S. platensis
• active against wide spectrum
of gram-(+) bacteria
• MOA: inhibits fatty acid
synthesis