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Penicillins Cephalosporins Monobactams Carbapenems
Penicillins Cephalosporins Monobactams Carbapenems
Penicillins Cephalosporins Monobactams Carbapenems
Penicillins
Cephalosporins
Monobactams
Carbapenems
IN H IB IT O R S O F C E L L W A L L S Y N T H E S IS
B e t a la c t a m a n t ib i o t c s O t h e r a n t ib io t ic s
P e n ic illin s C e p h a lo s p o r in s C a rb e p e n a m s M o n o b a c ta m s V a n c o m y c in
B a c i t r a c in
P e n i c i llin G 1 s t g e n e ra t io n 2 n d g e n e r a t io n I m i p e n a m s / C i la s t a t i n A z tr e o n a m
P e n i c illin V
M e t h i c i llin C e f a z o lin C e f a c lo r
O x a c i llin C e fa d r o x il C e f a m a n d o le
N a f c illin C e p h a le x in C e f o n ic id
C lo x a c i llin C e p h a lo t h in C e f a m e t a z o le
D i c lo x a c i llin C e p h r a d in e C e fo te ta n
A m p i c i llin C e p h a p i r in C e f o x it in
P ip e r a c illin C e fu r o x im e
T i c a r c i llin
C a r b e n i c i llin 3 r d g e n e r a tio n 4 th g e n e ra tio n
A m o x y c i llin
M e z lo c illin
C e f d in ir C e fe p im e
A z lo c illin
C e f ix im e
C e fo p e ra z o n e
C e fo t a x im e
C e fta z id im e
M o x a la c t a m
C e ft r ia x o n e
C e ft ib u te n
C e f tiz o x im e
Penicillins
• First antibiotic to be used clinically.
• Alexander Fleming – 1929.
6
• Moieties A and B together constitute the 6-
aminopennicillanic acid nucleus.
7
• Several types of natural penicillins
– F, G , X , & K.
– PnG (benzyl penicillin)
• Greatest antimicrobial activity
• Only natural penicillin used clinically.
• 0.6 Ug = 1 unit
• 6 Ug = 10 unit
• 6000 Ug = 10,000 units
• 6 mg = 10,000 units
• 600 mg = 10,000,00 units
Mechanism of action
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• Bacteria are surrounded by a thick cell wall
that confers stability & rigidity to their cell
structure
• Cell wall is composed of peptide chains &
glycan chains
• Extensively cross linked
• Peptidoglycan layer envelops the cell &
does not allow bacteria to swell & prevent
death due to lysis
Bacterial Cell Wall Synthesis
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• Penicillins with hydrophillic character ,
Ampicillin & amoxycillin can diffuse
through these porin channels ;
• show activity against some gram-
negative bacteria also
• but not against psuedomonas
aeruginosa because these bacteria lack
in such classical permeable porin
channels.
PENICILLINASE
PBP’s :
Penicillin
Binding
Proteins
• Natural Penicillin
• Narrow spectrum
• Primarily active against G +ve
bacteria
– Few gram negative & anaerobes
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Antibacterial spectrum :
• G +ve Cocci : streptococci are highly sensitive
• So are pneumococci
• S. aureus- >90% have acquired resistance.
• Gram +ve Bacilli : B. anthrasis, C. diphtheria, all
Clostridia, Listeria are highly sensitive.
• Gram -ve cocci:
• N. gonorrhoe (Highly resistant),
• N. meningitides are susceptible to Pn G.
• G –ve bacilli , Myco TB rickettsia, chlamydia,
protozoa, fungi & viruses are totally
unresponsive.
• Most anaerobic microorganisms including
clostridium species are highly sensitive.
• So are spirochaetes (T. pallidum,
Leptospira and others)
• Strepto
• Pneumo
• Meningo
• Anaerobes
• Spirochaetes
Pharmacokinetics:
• Acid labile -destroyed by gastric acid.
• Absorption from IM site is rapid, reaches
most body fluids
• Plasma half life is 30 minutes.
• Procaine penicillin G.
• Bezathaine penicillin G.
• Rheumatic fever
– 1.2 million units , im, once a month, lifelong
in high risk people.
• Bacterial endocarditis - caused by dental
extractions, endoscopies, catheterization,
etc. cause bacteremia which in patients
with valvular defects can cause
endocarditis.
INFECTIVE ENDOCARDITIS
• Some cases of endocarditis occur after
dental procedures.
Oxacillin
dicloxacillin
flucloxacillin are similar (not available in
India).
Methicillin:
–Highly penicillinase but not Acid resistant.
–Must be injected i.v
–MRSA have emerged in many areas
–These are insensitive to penicillinase
resistant penicillins / other B lactams &
erythromycin/ aminoglycosides/
tetracyclines etc.
–Have altered PBPs ; do not bind penicillins
–DOC Vancomycin/ linezolid/ ciprofloxacin
can also be used.
–Nephrotoxicity
Extended spectrum penicillins:
• Active against wide variety of gram –ve
bacteria as well. X Psuedomonas,
kleibseilla, proteus (lack porin channels)
Aminopenicillins :
• Amino substitution in the side chain
Ampicillin
• Active against all organisms as penicillin G + many gram
–ve bacteria(Hydrophillic; penetrate porin chanels).
– H.influenzae, E.coli, Proteus, Salmonella,
and Shigella.
– Many have developed resistance.
• Pharmacokinetics:
–oral absorption-incomplete but
adequate.
– Food interferes with absorption,
I hour before meals.(X
amoxycillin)
–primary channel kidney.
• Dose: 0.5-2gm oral/IM/IV 6 hrly.
Adverse effects :
Diarrhoea
• Unabsorbed drug irritates the lower
intestines.
• Alteration of normal bacterial flora.
Rashes
Bacampicillin
• Prodrug of ampicillin
• Completely absorbed.
– Does not disturb intestinal ecology.
– Incidence of diarrhoea is less
• Higher plasma levels are obtained.
• Better tissue penetration
Talampicillin
Pivampicillin
Hetacillin
• Are other prodrugs of ampicillin.
Amoxycillin :
Congener of ampicillin
Similar in all respects except:
Indications:
Serious infections caused by Pseudomonas or
Proteus eg.
Burns,
UTI,
Septicemia.
• Suicide inhibitors
Currently 3 ß-lactamase
inhibitors are available
B e ta la c ta m a s e In h ib ito rs
C la v u la n ic a c id S u lb a c t a m T a z o b a c ta m
–Clavulanic acid, ORAL/PARENTRAL
derived S. clavuligerus
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Endocarditis prophylaxis not recommended
• Surgical repair of
– ASD, VSD
– PDA
• Previous CABG
• MVP without valvular regurgitation.
• Physiologic, functional or innocent heart murmurs.
• Previous rheumatic fever without valvular dysfunction.
• Cardiac pacemakers (intravascular & epicardial) & implanted
defibrillators.