Antibiotics

Antibiotics
Betalactams
Macrolides
Fluoroquinolones
Tetracyclinces
Aminoglycosides

Penicillin, Cephalosporin, Carbapenam

Glycopeptide
Polymyxins
Chloramphenicol
Interfere protein synthesis
Mechanism of antibiotics
Inhibition
Antibiotics
cell wall synthesis
Penicillin, cephalosporin, vancomycin
cell membrane
Amphotericin B, Imidazoles
function
protein synthesis
Aminoglyconsides, tetracyclines, chloramphenicol, marcolides,
lincomycins
nucleic acid
Quinolones, sulphonamides, rifampicin
synthesis
Beta lactams
Inhibit cell wall synthesis
Penicillin
Penicillins
Spectrum
Common uses
Route
Remarks
(not sole
indications)
Penicillin V
Streptococcus
pharyngitis
PO; fair
bioavailabili
S. aureus
ty
Penicillin G
Streptococcus
endocarditis
IV
short T1/2;
(aqueous)
frequent
S. aureus
dosing
Ampicillin
GPC, some GNR
upper / lower
IV, (PO)
BLI
respiratory inf.
combination
S. aueus
spectrum
Pseudomonas
Amoxicillin

Cloxacillin
(penicillinaseresistant
penicillin)
Ticarcillin

Piperacillin

PO; good
bioavailabili
ty
GPC
GNR

skin and soft

GNR
antipseudomonal

intra-abdominal;
some hospitalacquired inf.

PO, IV
(liver
metabolism
)
IV

S.
pneumoniae*
enterococcus*
listeria*
treatment of
choice for
MSSA
infection
BLI
combination
spectrum

GPC, GNR
severe infections IV
BLI
community /
combination
antihospital-acquired
spectrum
pseudomonal
B. fragilis (and some other anaerobes): resistant (unless combined with BLI, Betalactamase inhibitor)

Primarily excreted via renal route

Adverse reactions
IgE mediated (anaphylaxis 0.05%,
urticaria, angioedema; potentially
fatal do not re-challenge)
fever, rash, neutropenia
eosinophilia (may occur after
prolonged, high-dose therapy)
diarrhoea, nephritis, liver
derangement etc
Before prescribe penicillin to patient, history of adverse reactions can be asked:
1. Anaphylaxis: Any collapse, hypotension?
2. Urticaria: Any circular rash?
3. Angioedema: Any lips swelling?
In treatment of infective endocarditis, high dose is needed, adverse reactions not
likely be IgE mediated
Beta-lactam/ beta-lactamase inhibitor combinations
Clavulanate
Amoxicillin
PO, IV
Co-amoxiclav, Augmentin
Clavulanate
Ticarcillin
IV
Timentin
Sulbactam
Ampicillin
PO*, IV
Sultamicillin*, Unasyn
Sulbactam
Cefoperazone
IV
Sulperazon *
Tazobactam
Piperacillin
IV
Tazocin , Zosyn
-lactamase inhibitor (BLI):
Suicidal enzyme inhibitor
Restores activity of accompanying -lactam broader spectrum
esp. active against plasmid coded -lactamases from: MSSA, H. influenzae, M.
catarrhalis, GNRs, Bacteroides

Cephalosporins
Cephalospor Spectrum
ins
1st
generation
(e.g.

GPC
S. aureus
PRSP

Common uses
(not sole
indications)
skin and soft
tissue infections;
surgical

Route
IV1, PO2

Remarks

cefazolin1,
cephalexin2)
2nd
generation
(e.g.
cefuroxime)
3rd
generation
(e.g.
cefotaxime,
ceftriaxone3)
3rd
generation
(e.g.
ceftazidime,
cefoperazon
e4 )

prophylaxis
GNR
pseudomonas
some GPC
PRSP
GPC
PRSP
GNR
pseudomonas

intra-abdominal,
urinary infections

IV, PO (3050% bioavailability)

Severe
communityacquired
infections, CAP,
meningitis, UTI
certain hospitalacquired
infections
(susceptible
pathogen e.g.
Pseudomonas)

IV
(3,4 long halflife, 50%
biliary
excreted)
(PO=
cefixime,
cefpodoxim
e,
ceftibuten)

H. influenzae*;
communityacquired
pathogens
good CSF levels;
salmonella*;
broad-spectrum,
select drugresistant
pathogens if
used
inappropriately;
only 1 BLI comb.
available

GNR
antipseudomonal
some GPC
PRSP (S.
aureus )
4th
GNR
severe
IV
broad spectrum,
generation
community /
except for
anti(e.g.
hospital-acquired
anaerobes
pseudomonal
cefepime)
infections
GPC
PRSP, S
aureus
3rd generation has good ability to pass BBB
PRSP = Penicillin Resistant Streptococcus Pneumoniae
B. fragilis, enterococcus, listeria: resistant
Good tissue distribution (inc. CSF, for treatment of meningitis)
Primarily excreted via renal route
Adverse reactions
high urine concentration
similar to penicillins
dosage adjustment required with
cross-reaction with penicillin <8%
renal impairment (except
rash, eosinophilia, neutropenia,
3
4
ceftriaxone , cefoperazone )
diarrhoea, biliary sludge3, prolonged
PT4
Patients have penicillin allergy, still giving celphalosporins
Generally do not give beta-lactam class to patient with IgE allergy

Carbapenems
Carbapenems
Imipenem/cilast
atin,
meropenem

Spectrum
GPC, GNR,
Pseudomonas &
anaerobes

Common uses
severe hospitalacquired infections
involving drugresistant pathogens

Remarks
Always used
causes
resistant soon
HA hospital

ertapenem

No antipseudomonas
activity

(e.g. ESBL)
neutropenic fever;
life-threatening
infections

restricts using

Renal excretion
Adverse reaction:
Similar to penicillin, seizures 1-2 % in renal failure patient
Cautions in patient with renal failure
Macrolides
inhibit RNA-dependent protein synthesis
bacteriostatic
Mycoplasma, Chlamydia, Legionella, Campylobacter, streptococci, some
staphylococci
Macrolides
Spectrum
Common uses
Remarks
Erythromycin Respiratory atypical Combination
Not use as
pathogens, H.
therapy in CAP
induce
influenzae, M.
to provide
vomiting
catarrhalis
coverage for
Three
atypical
macrolides can
Enterobacteriaceae
pathogens
broaden
may be active
treatment of
spectrum by
against some GPC
nonadding
Gp A
tuberculous
penicillin
streptococcus
mycobacterium
(occasionally
infections & for
resistant), MSSA
H. pylori
for most PRSP
eradication
Clarithromyci enhanced activity
better tolerated

as
an
n
against H.
interact with
alternative in
influenzae, M.
colchicines
simple
SSTI,
catarrhalis
metabolism
e.g. penicillin
colchicines
allergy
which is fatal in
gouty arthritis
*
Azithromycin
similar; legionella
Long half-life
Other pathway
involved, safe
Not use in acute life-threatening condition
adverse reactions
GI disturbance, cholestasis, liver derangement, (hearing loss, torsade de pointes
ventricular tachycardia), -/ + hepatotoxic
drug-drug interactions* (CYP450) always check concomitant medications
Fluoroquinolones
Inhibit DNA-gyrase
Not commonly use as resistance, bacteria mutate easily by the effect of drug
When patient has respiratory symptoms, send specimen to the lab before
prescribe the drug
As fluoroquinolones suppress the s/s of TB which causes late dx & patient may
missed & die
Fluoroquinolo Spectrum
Common use
nes
Levofloxacin,
GPC (including PRSP)
respiratory, urinary
moxifloxacin,
infections, etc
GNR (enterobacteriaceae
gatifloxacin
pseudomonas)

Respiratory atypical
pathogens
MTB
Ciprofloxacin
*UTI, intra-abdominal or GI
GPC
tract infections, SSTI,
GNR
salmonellosis
more reliable antipseudomonal activity; used in
combination therapies against
pseudomonas
Issue of drug-resistance (DNA gyrase; stepwise mutations)
Caution & adverse reactions
not approved in pregnant/lactating women, or young children aged < 12 as
damaged joint & inhibit cartilage growth
skin rash, GI upset
CNS side effects
insomnia, dizziness, confusion in elderlies; rarely seizure
cardiovascular side effects
QT-prolongation / arrhythmia (with newer FQs) as hypo/ hypercalcemia
dysglycaemia (with newer FQs)
drug-drug interactions*
FDA warning: tendinitis, arthralgia, rupture tendon Achilles (esp. with prolonged
usage)
Aminoglycosides
Very potent, bactericidal
Inhibit protein synthesis
Active against gram negative bacilli, MSSA
gentamicin, netilmicin , amikacin, streptomycin, neomycin, tobramycin
Side effect: Ototoxic & Nephrotoxic (require monitoring)
Resistance due to inactivating enzymes
Glycopeptides
Bactericidal
Inhibit cell wall synthesis
Active against gram positive organisms
vancomycin, teicoplanin
Side effect: Ototoxic & nephrotoxic (require monitoring)
Red man syndrome if vancomycin is rapidly infused
Resistance: VRE, VISA, VRSA
Anti-TB drug
Given in combination for prolonged period to prevent drug resistance
1st line drugs: rifampicin, isoniazid, pyrizynamide, ethambutol, streptomycin
In uncomplicated PTB: RIP + E/S x 2/12, then RI x 4/12
Monitor compliance (DOTS), toxicity
Do not use quinolones in suspect TB case, it would cause culture ve in TB and
delay treatment
Antifungal drugs
Inhibit fungal membrane synthesis
Amphotericin B
Nystatin
Azoles
covers almost all fungi Toxic, only for topical
e.g. flucon-, itracon-,
only IV formulation,
use against yeast
ketocon-azole
renal toxic
Wide spectrum, but
usually not cover
filamentous fungi
IV, oral and topical
formulations available

Antiviral drugs
Diverse chemical groups
Current interest mainly focus on inhibition of nucleic acid metabolism
Admantanes
Amantadine, rimantadine Vs influenza A
Nucleosides
Acyclovir IV, oral, topical, Vs HSV, VZV
HAART (highly active anti-retroviral therapy) Vs HIV e.g AZT, DDI, DDC, PI