Amoxicillin

Amoxicillin+cloxacillin

Presented by: ISHAN SHUKLA Pharma MBA-II KBIPER

CATEGORY

Mechanism action

of

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 R

C

H H N

Nu Enz

O

H N

O S

C

Me Me

CO2H

­H

H H N

R Enz­Nu

O

H N H

O S

Me Me

CO2H

R

C

H H N

H

O C HN Nu­Enz

S

Me Me

CO2H

Covalent bond formed  to transpeptidase enzyme Irreversible inhibition

Mechanism of action - bacterial cell wall synthesis NAM L­ D­Glu L­Lys

NAG NAM L­ D­Glu L­Lys

Bond formation inhibited by penicillin

NAM

NAG

L­ NAG

NAM

D­Glu

NAM L­Lys L­

L­

NAG D­Glu L­Lys

NAM L­ NAG

NAM

D­Glu

L­

NAM

NAG

L­Lys

L­

D­Glu L­Lys

NAM L­

D­Glu

D­Glu

D­Glu

L­Lys

L­Lys

L­Lys

Mechanism of action - bacterial cell wall synthesis NAM NAG NAM NAG SUGAR L­Ala

L­Ala

D­Glu

D­Glu

L­Lys

Gly Gly Gly Gly Gly

L­Lys

D­Ala

D­Ala

D­Ala

D­Ala

BACKBONE

Gly Gly Gly Gly Gly

PENICILLIN

D­Alanine

NAM

NAG

TRANSPEPTIDASE

NAM

L­Ala

L­Ala

D­Glu

D­Glu

L­Lys D­Ala

Gly Gly Gly Gly Gly

Cross 

L­Lys D­Ala

NAG

Gly Gly Gly Gly Gly

SUGAR BACKBONE

Mechanism of action - bacterial cell wall synthesis Penicillin can be seen to mimic acyl­D­Ala­D­Ala R C

H N

R H

H

O O

N

S

Me Me

CO2H

Penicillin

C

H N

O O

Me H H N

H CH3 CO2H

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 TRESMOXSARABHAI. HIPENOXCADILA IMOX-CLO- IPCA MYTIMOX- PANACEA GARDENAL.

Other brands available.

THANK YOU