3656181
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Mind Map by lee fang, updated more than 1 year ago
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Created by Freddiecox96
over 9 years ago
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Copied by lee fang
over 9 years ago
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Compare and contrast the five
generations of cephalosporins
- 2nd
- Activity -Variable activity against gram
positive bacteria but increased activity
against gram negative bacteria
- Structural features and chemistry- Broader spectrum of
activity than most first generation due to greater steric
hindrance provided by the methoxy group
- Cefoxitin - Methoxy
substituent at position 7
(steric hindrance) – Urethane
group ( good metabolic
stability to esterase )
- Cefuroxime – Iminomethoxy
group at alpha position of the
acyl side chain ( Increase
resistance to B-lactamases
and mammalian esterases)
- Cefoxitin - Methoxy
substituent at position 7
(steric hindrance) – Urethane
group ( good metabolic
stability to esterase )
- Activity -Variable activity against gram
positive bacteria but increased activity
against gram negative bacteria
- 4th
- Activity- Broadest spectrum of activity, with similar
activity against gram-positive organisms as first
generation cephalosporins. Greater resistance to
beta-lactamases than the third generation
cephalosporins
- Structural feature and chemistry-
Cefepime and Cefpirome–
Zwitterionic compounds (radically
enhance the ability to penetrate
outer membrane of Gram negative
bacteria, good affinity for
transpeptidase enzyme, low affinity
for variety of B-lactamases)
- Activity- Broadest spectrum of activity, with similar
activity against gram-positive organisms as first
generation cephalosporins. Greater resistance to
beta-lactamases than the third generation
cephalosporins
- 3rd
- Activity- Broad spectrum
and the effective against
both gram positive and
gram negative bacteria.
Optimum activity is against
gram negative bacteria.
- structural features and
chemistry-Ceftazidime-
aminothiazole ring
enhances the
penetration through
lipopolysaccharide and
increase affinity for
transpeptidase
- Activity- Broad spectrum
and the effective against
both gram positive and
gram negative bacteria.
Optimum activity is against
gram negative bacteria.
- 1st
- Activity- Effective
against gram
positive bacteria
and have little
effect against
gram negative
bacteria.
- structural
features
and
chemistry
- Cephaloridine – pyridinium group at
position 3 (good leaving group, not
readily hydrolysed by esterase)
- Cephalothin- acetyoxy group at
position 3 (good leaving group but is
readily hydrolysed by esterase)
- Cefalexin – Methyl substituent at position 3 (not good
leaving group but help oral absorption) -Hydrophilic
amino group at 7-acylamino side chain (compensate
bad activity)
- Cephaloridine – pyridinium group at
position 3 (good leaving group, not
readily hydrolysed by esterase)
- Activity- Effective
against gram
positive bacteria
and have little
effect against
gram negative
bacteria.
- 5th
- Activity- Broad spectrum
activity against gram negative
bacteria such as MRSA
- structural features and
chemistry- a bicyclic ring
with four-member
β-lactam ring fused to a
six-member cephem ring
- Ceftaroline- thiazolylthio
group cause the activity
against MRSA
- Ceftaroline- thiazolylthio
group cause the activity
against MRSA
- Activity- Broad spectrum
activity against gram negative
bacteria such as MRSA
- Side effects
- 6. a) bleeding
disorders b)
Flushing,
tachycardia,
vomiting with
alcohol intake
(cefamandole,
moxalactam &
cefoperazone)
- 1. Hypersensitivity reactions
- 2. Nephrotoxicity (cephradine)
- 3. Thrombophlebitis ( i.v admin.)
- 4. Superinfections
- 5. Diahea (oral cephalosporins,
cefoperazone, ceftriaxone &
moxalactam)
- 6. a) bleeding
disorders b)
Flushing,
tachycardia,
vomiting with
alcohol intake
(cefamandole,
moxalactam &
cefoperazone)
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