Amoxicillin+cloxacillin

Presented by:
ISHAN SHUKLA
Pharma MBA-II
KBIPER
CATEGORY
 Mechanism of
action
• Penicillins inhibit a bacterial enzyme called the transpeptidase 
enzyme  which  is  involved  in  the  synthesis  of  the  bacterial  cell 
wall
• The  ­lactam ring is involved in the mechanism of inhibition
• Penicillin becomes covalently linked to the enzyme’s active site 

O O O
H H H H H H H H H
C N C N C N
S Me S Me S Me
R R R
Enz­Nu O C HN
Nu N Me N Me Me
­H Nu­Enz
O O
Enz CO2H H CO2H CO2H

Covalent bond formed 
to transpeptidase enzyme
Irreversible inhibition
 Mechanism of action - bacterial cell wall
synthesis

NAM NAG NAM NAG NAM

L­ NAM L­
NAG NAM L­
NAG NAM
D­Glu D­Glu D­Glu
L­ L­ L­
NAM NAG NAM NAG NAM
L­Lys L­Lys L­Lys
D­Glu D­Glu D­Glu
L­ L­ L­
L­Lys L­Lys L­Lys
D­Glu D­Glu D­Glu

L­Lys L­Lys L­Lys

Bond formation
inhibited by
penicillin
Mechanism of action - bacterial cell wall
synthesis
NAM NAG NAM NAG SUGAR
BACKBONE
L­Ala L­Ala

D­Glu D­Glu

L­Lys Gly Gly Gly Gly Gly L­Lys Gly Gly Gly Gly Gly

D­Ala D­Ala

D­Ala D­Ala

PENICILLIN
TRANSPEPTIDASE
D­Alanine

NAM NAG NAM NAG SUGAR

BACKBONE
L­Ala L­Ala

D­Glu D­Glu

L­Lys Gly Gly Gly Gly Gly L­Lys Gly Gly Gly Gly Gly

D­Ala D­Ala
Cross 
Mechanism of action - bacterial cell wall
synthesis
Penicillin can be seen to mimic acyl­D­Ala­D­Ala

R R
H H
C N H H C N Me
S Me
O O H
H H
N N
Me
O O CH3
CO2H CO2H

Penicillin Acyl­D­Ala­D­Ala
INDICATION :

INFECTONS CAUSED BY SUSCOTIBLE

ORGANISMS,
UPPER AND LOWER RESPIRATORY TRACT
INFECTIONS,
GENITO URINARY.
SKIN &SOFT TISS,
BONE AND JOINT INFECTIONS,
ENT INFECTIONS ,
TYPHOID AND PARATHYROID SEPSIS ,
GONORRHOEA,
INFECTIONS CAUSED BY PENICILLI.NNASE
DOSAGE:
ORAL
ADULT: AMOXICILLIN 250 mg+CLOXACILLIN 250mg
(500 gm – 1
gm combnination)

CHILDREN: 59 mg-100mg OF COMBINATION IN 3

DIVIDED
DOSES.
PARENTRAL
ADULT: IM/IV(MORE ACUTE & SEVERE CONDITIONS.
AMOXICILLIN 250mg +CLOXACILLIN 259mg.
1-2 vials : depending upon severity.(every 6-8
hrs)
CHILDREN:IM/IV (MORE ACUTE & SEVERE CONDITIONS)
ADVERS EFFECTS:
FAILURE OF COMBINATION MAY OCCUR IF
POTENCY OF CLOXACILLIN IS REDUCED.
PRODUCTS CONT. CLOXACILLIN NOT GIVEN
WITHIV LIPIDS, BLOOD PRODUCTS,PROTEIN
HYDROLYSATE &OTHER PROTIENACEOUS
FLUIDS.
GI UPSETS,RASH,
URTICARIA,NEUTROPENIA,
NEUROTOXICITY,AGRANULOCYTOSIS,
INCREASED INCIDENCE OF PHLEBITIS WITH
Comparison:
COMPARISON:
AMPICILLIN+CLOXACILLIN
(AMPILOX) 250 mg OF EACH CAPSULE/VIAL.
VIGOROUSELY PROMOTED FOR
POSTOPERATIVE, SKIN
&TISSUE,RESPIRATORY,URINARY INFECTIONS
THE COMBINATION IS NOT SYNERGISTIC SINCE
CLOXACILLIN IS NOT ACTIVE AGAINST G-ve
BACILLI.
WHILE AMPICILLIN IS NOT ACTIVE AGAINST
STAPHYLOCCOCI
SINCE MIXEED G-ve AND STAPHYLOCCOCAL
INFECTIONS ARE UNCOMMON, ONE OF THE
COMPONENT IS USELESS BUT ADDS TO THE
COST AND ADVERS EFFECTS.
COMPARISON: CONT………..
SINCE THE AMOUNT OF DRUG WHICH IS
ACTUALLY GOING TO ACT IN ANY
INDIVIDUAL PATIENT IS HALVED(WHEN THE
COMBINATION IS USED)
EFFICACY IS REDUCED &CHANCE OF
RESISTANT INCREASED
BOTH THE DRUG ARE NINEFFECTIVE
AGAINST MRSA.
BLIND THERAPY WITH THIS COMBINATION
IS IRRATIONAL &HARMFUL.
LEADING AMOXICILLIN+CLOXACILLIN BRANDS:

NOVACLOX - CIPLA
TORMOXIN PLUS - TORRENT
TRESMOX- SARABHAI.
HIPENOX- CADILA
IMOX-CLO- IPCA
MYTIMOX- PANACEA
GARDENAL.
Other brands available.
THANK YOU