Cephalosporin part 1 antibiotics for bpharma 6th sem

1. Name :- Zovia Ejaz Ahmad
Rollno. :- B-VI-07

2.  INTRODUCTION
 CHEMISTRY
 MECHANISM OF ACTION
 CLASSIFICATION
 FIRST GENERATION CEPHALOSPORINS
 SECOND GENERATION CEPHALOSPORINS
 THIRD GENERATION CEPHALOSPORINS
 FOURTH GENERATION CEPHALOSPORINS
 FIFTH GENERATION CEPHALOSPORINS
 ADVERSE EFFECTS
 USES

3.  Cephalosporins are a group of semi- synthetic
antibiotic
 Derived from Cephalosporin –C , obtained
from a fungus Cephalosporium
 B- lactam antibiotic
 Wider spectrum of activity than penicillins
 Bactericidal

5. Peptidoglycan layer is
important for cell
wall structure
integrity of bacteria
Final step in synthesis
of peptidoglycan is
facilitated by PBP
Cephalosporins
competitively inhibit
PBP as it mimics the
structure of D-Ala-D-
Ala link to which PBP
bind for crosslinking
of peptidoglycan

9.  First generation cephalosporins are very
effective against gram+ve organisms.
 They are generally used in minor infections
of the skin , respiratory & urinary tract
infections.
 Examples of first generation cephalosporins
include:- Cefazolin ; Cephalexin ; Cefadroxil
; Cephradine ; Cephalothin etc.
 They were developed in 1960s

10.  SUMMARY:- Cefazolin is a broad-spectrum
cephalosporin antibiotic mainly used for the
treatment of skin bacterial infections and
other moderate to severe bacterial infections
in the lung, bone, joint, stomach, blood, heart
valve, and urinary tract.
 ANTIBACTERIAL SPECTRUM:-
 The antibacterial spectrum of cefazolin
includes streptococci , staphylococci ,
Enterobacter ,Klebsiella , E.coli etc.

11.  MECHANISM OF ACTION :-
It acts by binding to specific penicillin-binding
proteins (PBPs) located inside the bacterial cell
wall, it inhibits the third and last stage of
bacterial cell wall synthesis. Cell lysis is then
mediated by bacterial cell wall autolytic
enzymes such as autolysins.
 PHARMACOKINETICS :-
 absorption :- It is not absorbed from the GI
tract hence it must be administered
parenterally. Peak serum concentrations are
attained 1-2 hrs post IM injection

12. volume of distribution :- approx 10 L
Protein binding :- 74-86 %
metabolism :- Not metabolized
ROUTE OF ELIMINATION :-
It is excreted unchanged in the urine. In the first
six hours approximately 60% of the drug is
excreted
t1/2 (half-life) :-1.8 hr following IV
administration & 2 hr following IM administration
USES OF CEFAZOLIN :-
It is mainly used for the treatment of UTIs ;
respiratory infections; Biliary tract infections ;
Cellulitis ;infection caused by Gram +ve bacteria
(MSSA); Pneumonia ;Bacterial Endocarditis etc.

13.  Prescribed dosage of Cefazolin :-
 For infections with gram +ve bacteria :-
 1-2 weeks :- 40 mg/kg/day IV/IM divided every
12 hourly
 >7 days :- 60mg/kg/day IV/IM divided every 8
hourly
 For infants & children :- 25-150 mg /kg/day
IV/IM divided every 6-8 hourly ; do not exceed 6g
/day
 Endocarditis prophylaxis :-50 mg /kg IV/IM , 30-
60 minutes before the procedure
 NO DOSE ADJUSTMENTS REQUIRED FOR
RENALFAILURE

14.  Adverse effects of cefazolin :-
 Hypersensitivity , Anorexia , Diarrhoea,
Fever , Leukopenia ,Nausea , vomiting,oral
candidiasis etc.
 Interaction :- It shows Pharmacodynamic
synergism.
 NOTE :- Cefazolin is used as an agent of
choice for Surgical prophylaxis

15. Cephalexin is effective when given orally
Its antibacterial spectrum is same as that
of other first generation drugs.
It is less effective against penicillinase
producing staphylococci ).
It is a semisynthetic antibiotic drug
MECHANISM:- It acts by inhibiting the cell
wall synthesis by forming covalent bond
with transpeptidase.

16.  PHARMACOKINETICS :-
 Absorption :- Cefalexin is rapidly & almost
completely absorbed from GIT with oral
administration . Absorption is slightly reduced when
taken with food, it can be taken without regard for
meals. Peak levels of cefalexin occur about 1 hour of
administration.
 Volume of distribution :-5.2 -5.8 L
 Protein binding :-10-15 % bound to serum proteins
including serum albumin.
 Metabolism :- It is not metabolized in the body

17.  Route of elimination :- Cephalexin is over 90%
excreted in the urine after 6 hours by glomerular
filtration and tubular secretion , it is unchanged in
the urine.
 T1/2 :- 49 minutes in fasted state & 75 minutes when
taken with food
 USES :- It is mainly used for the treatment of
Tonsilitis ;Pyoderma ;Pyelonephritis ; Cystitis ;
Subcutaneous abcesses ; Dental infections ;
Pneumonia .
 CONTRAINDICATIONS :- Cephalexin is contraindicated
in patients with allergies

18.  PRESCRIBED DOSE :-
 For mild infection : 25-20 Po mg/kg/24 hours in 3-4
divided doses for 5-10 days
 Severe infection :- 50-100 PO mg/kg/24 hours in 3-4
divided doses for 10 days
 NO DOSE ADJUSTMENTS REQUIRED FOR RENAL
/HEPATIC FILURE
 ADVERSE EFFECT :- Pseudomembranous colitis ,
dyspepsia, nausea, vomiting, diarrhoea , rash,
urticaria, angioedema, pruritus etc.
 INTERACTION :- Decreases effect of BCG vaccine &
Typhoid vaccine

19.  Cephradine is a semi-synthetic first generation
cephalosporin , which is effective when orally
administered.
 MECHANISM OF ACTION :-It has mechanism of action
similar to that of Cefalexin . It inhibits the 3rd & last
stage of bacterial cell wall synthesis by binding to
specific penicillin binding proteins (PBPs ). Cell lysis
is then mediated by bacterial cell wall autolytic
enzymes such as the autolysins ; it could be possible
that Cephradine interferes with an autolysin inhibitor
 PHARMACOKINETICS :-
 Absorption :- It is absorbed rapidly and almost
completely when administered orally

20.  Volume of distribution :- 5L
 Protein binding :- 15 %
 Metabolism :- Not metabolized in the body
 Route of elimination :- Over 90 % of the drug is
excreted unchanged in the urine within 6 hours.
 T1/2 :- 1-2 hours
 USES :- It is used for the treatment of Bacterial-sepsis
; Bloodstream infections ; Tonsils ; Laryngitis ;
Respiratory tract infections ; UTIS etc
 CONTRAINDICATIONS :- should not be used in allergic
patients.

21. PRESCRIBED DOSE :-
For moderate infections :- 100-200 mg /day, divided
into 2-4 doses per day. The maximum dose is
400mg/day
For parenteral route :-200-400 mg /kg , divided into 4
doses by IM injection. The maximum dose is 800
mg/kg
For surgical prophylaxis :-100-200 mg before surgery
Dose for children ( susceptible infections ) :-
25-50 mg/kg/day divided into 2-4 doses
For otitis media in children :-75-100 mg/kg/day

22.  ADVERSE EFFECTS :- Diarrhoea ; Hypersensitivity
reactions such as skin rashes ; Blisters ;itching; joint
pain ; angina ; nausea ; vomiting; dizziness;
restlessness etc
 INTERACTIONS :-
 The risk of nephrotoxicity is increased when
combined with cefpirome
 It decreases the effect ,if combined with
anticoagulant drug
 If taken with alcohol ,it can show disulfiram like
reactions.

23.  Cefadroxil is an analog of Cephalexin ,it is similar to
it in many of its properties . It is generally used in
respiratory tract infections & skin infections.
 MECHANISM OF ACTION :-
 Cefadroxil is bactericidal in nature as it inhibits the
process of cross-linking in the bacterial cell wall
synthesis. It is very effective for the infections
caused by the gram +ve bacteria.
 It binds to PBP1a which leads to spheroplast
formation ultimately leading to the lysis of the
bacterial cell.

24.  PHARMACOKINETICS :-
 Absorption :-Cefadroxil is completely absorbed on
oral administration; food does not interfere with its
absorption.
 Volume of distribution :- 0.3 L/kg
 Protein binding:- About 28 % binds to plasma proteins
 Metabolism :- Not metabolized in the body
 Route of elimination :-Over 90% of the drug is
excreted unchanged in the urine within 24 hours.
 T1/2 :-1.5 hours

25.  USES OF CEFADROXIL :-
 Cefadroxil is used for the treatment of respiratory tract
infections ; Pyoderma ; Otitis media ; Pyelonephritis ;
Cystitis ; Urethritis ; Endocarditis prophylaxis
 CONTRAINDICATIONS :-
 Cefadroxil is contraindicated in patients with known
allergies to cephalosporins
 PRESCRIBED DOSAGE :-
 Oral dose :- 30 mg/kg/24 hours in 2 divided doses for 10
days . Maximum dose is 1g
 Endocarditis prophylaxis :- 50 mg/kg 1 hour before
procedure (orally )

26.  ADVERSE EFFECT :-
 Pseudomembranous colitis ,dyspepsia , nausea ,
vomiting , diarrhoea , rashes , angioedema , hepatic
dysfunction, neutropenia , agranulocytosis ,
thrombocytopenia , serum sickness , arthralgia , etc
 INTERACTIONS :-
 It competitively inhibits renal tubular secretion when
combined with Probenecid
 Dosage in renal impairment :-
 20-50 mg/kg in normal renal function
 10-20 mg/kg as in case of renal impairment

27.  Second generation Cephalosporins are more
active against some gram-negative organisms
 They are also active against some anaerobes
 They are more resistant to beta-lactamases
& H.influenzae
 Examples include:- Cefamandole,
Cefaclor,Cefoxitin etc.

28.  Cefamandole is a broad spectrum second generation
drug , it is administered parenterally. It is generally
formulated as a formate ester , cefamandole nafate.
It is no longer marketed in the U.S
 MECHANISM OF ACTION :-
 cefamandole binds to specific penicillin-binding
proteins (PBPs) located inside the bacterial cell wall,
causing the inhibition of the third and last stage of
bacterial cell wall synthesis. Cell lysis is then
mediated by bacterial cell wall autolytic enzymes
such as autolysins.

29. PHARMACOKINETICS :-
Absorption :- It is poorly absorbed in the GIT , thus it
is given parenterally . A 1g IM dose acheives a plasma
concentration of 25-30 mg/L after 1 hour
Volume of distribution :- It is widely distributed in the
body tissues
Protein binding :- 65-80 %
Elimination :- Renal excretion , a small amount is
also excreted in the bile ( 150-250 mg/L )
 t ½ :- 50 -60 minutes (less than 1 hour )

30.  USES :-
 It is widely used for the treatment of infections
caused by H . Influenzae , Enterobacter , E.coli ,
Proteus , Klebsiella etc . It is mainly used for
respiratory tract & soft tissue infections in infants &
children.
 CONTRAINDICATIONS :-
 Clinical & microbiological failure in case of meningitis
caused by H. influenzae is reported.
 Limited use to disease in which the development of
sepsis not a concern.
 The safety & efficacy of this agent is not established
for infants younger than 1 month

31.  PRESCRIBED DOSE :-
 Usual adult dose for pneumonia :-500 mg
intramuscularly or IV every 6 hours.
 Usual Adult Dose for Skin or Soft Tissue Infection :-
500 mg intramuscularly or IV every 6 hours.
 Usual Adult Dose for Urinary Tract Infection :-
 Uncomplicated: 500 mg intramuscularly or IV every 8
hours.
Complicated: 1 g intramuscularly or IV every 8 hours.
 Usual Adult Dose for Surgical Prophylaxis :-
Preoperative: 1 to 2 g IV or intramuscularly 30 to 60
minutes prior to surgical incision.

32.  Postoperative: 1 to 2 g IV or intramuscularly every 6
hours for 24 to 48 hours (72 hours for prosthetic
arthroplasty).
 Cesarean section: the initial dose may be
administered just prior to surgery or immediately
after the cord is clamped.
 Usual Pediatric Dose for Surgical Prophylaxis
 > 3 months:
50 to 100 mg/kg/day in divided doses IV or
intramuscularly 30 to 60 minutes prior to surgical
incision and every 6 hours for 24 to 48 hours.
 Renal dose adjustments are made in accordance to
creatinine clearance .

33.  ADVERSE EFFECTS :-
 Nausea and vomiting , Hypersensitivity Anaphylaxis,
maculopapular rash, urticaria, eosinophilia, and drug fever
have been reported.
 Blood Thrombocytopenia has been reported rarely.
Neutropenia has been reported, especially in long courses
of treatment.
 INTERACTIONS :-
 Nephrotoxicity has been reported following concomitant
administration of aminoglycoside antibiotics and
cephalosporins.
 As with other broad-spectrum antibiotics,
hypoprothrombinemia, with or without bleeding, has
been reported rarely, but it has been promptly
reversed by administration of vitamin K.

34.  When ingested with alcohol it shows disulfiram like
reactions , that means the concentration of
acetaldehyde rises which results in flushing ,
dizziness, nausea , vomiting , dilirium etc
 Carcinogenesis, Mutagenesis, Impairment of
Fertility Certain (beta)-lactam antibiotics containing
the N-methylthiotetrazole side chain have been
reported to cause delayed maturity of the testicular
germinal epithelium ( during spermatogenesis )

35.  Cefuroxime is a broad spectrum antibiotic , which is
administered parenterally ,Cefuroxime axetil (prodrug)
is effective orally . It is resistant to beta lactamase
enzymes
 Though it attains good conc. in the CSF it is not used in
Meningitis.
 Effective against gram –ve bacteria, Citrobacter ,
Enterobacter ,pneumonia , Gonorrhoea etc
 MECHANISM OF ACTION :- It acts by binding to specific
penicillin-binding proteins (PBPs) located inside the
bacterial cell wall, it inhibits the third and last stage of
bacterial cell wall synthesis. Cell lysis is then mediated
by bacterial cell wall autolytic enzymes such as
autolysins.

36.  PHARMACOKINETICS :-
 Absorption :-Absorbed from the gastrointestinal
tract. Absorption is greater when taken after
food (absolute bioavailability increases from 37%
to 52%).
Volume of distribution :- 11.1 -15.8 L / m(2)
Protein binding :-50% to serum protein
 Metabolism :- Body is not able to metabolize the
drug
 Elimination :- eliminated unchanged in the urine
 T1/2 :- Cefuroxime has t ½ of about 70-80 minutes

37.  USES :-
 It is used in Pharyngitis , Pneumonia , Sinusitis , Otitis
media , Skin infections , Gonorrhoea , Osteomyelitis ,
Lyme disease
 CONTRAINDICATIONS :-
 It is containdicated in patients with hypersensitivity
/allergic reactions
 PRESCRIBED DOSE :-
 < 3 months :- Safety & efficacy is not established
 >3 months – 12 years :-
 30 mg /kg/day in 12 hourly divided doses for 10 days
(Maximum is 1g /day )

38.  Alternatively , 75-150 mg/kg/day IM/IV in 8 hourly
divided doses for severe infections , do not exceed 6
g /day . Duraton varies with severity of the infection
 For >12 years :-
 250-500 mg tablet every 12 hours for 10 days.
 For infants ( less than 4 weeks ) :-
 100 -150 mg /kg /day divided 12 hourly IV
 NO hepatic dosage adjustments are recommended .
 ADVERSE EFFECTS :-
 Pseudomembranous colitis , nausea , vomiting,
diarrhoea , rashes , urticaria , amgioedem , pruritis
etc

39.  INTERACTION :-
 It increases the level of argatroban , bivalirudin
,fondaparinux by anticoagulation .

40.  Cefaclor is second generation cephalosporin
,administered orally
 It is very effective against H.influenzae , Proteus
, E.coli , Moraxella
 MECHANISM OF ACTION :-
 It acts by binding to PBP 3 , thus inhibiting the
cross-linking in the bacterial cell wall ,
ultimately causing lysis of the cell
 PHARMACOKINETICS :-

41.  Absorption :-Well absorbed after oral
administration, independent of food intake.
 Volume of distribution :- 11L
 Protein binding :- 23.5 %
 Metabolism :- No appreciable biotransformation
in liver (approximately 60% to 85% of the drug is
excreted unchanged in the urine within 8 hours).
 Elimination :- Approximately 60% to 85% of the
drug is excreted unchanged in the urine within 8
hours, the greater portion being excreted within
the first 2 hours.
 T ½ :- 1.5 hours

42.  USES :-
 Tonsilitis , Rhinosinusitis , Otitis media , External
otitis , Epiglottitis , Impetigo , Pyoderma ,
Gonococcal infections , Pyelonephritis , Cystitis
 CONTRAINDICATIONS :-
 It is contraindicated in patients with known
allergy to cephalosporins
 PRESCRIBED DOSE :-
 20 mg/kg/day in 3 divided doses . In severe
infections , dose can be doubled

43.  ADVERSE EFFECTS :-
 Serum sickness , erythema multiforme , rashes ,
arthritis , diarrhoea , nausea , vomiting , hepatitis ,
jaundice , lymphatocytosis , leukopenia ,
hyperactivity , insomnia , dizziness , hallucinations .
 INTERACTIONS :-
 Probenicid :- prolongs the serum levels by slowing the
rate of excretion by competitively inhibiting renal
tubular secretion
 Warfarin :- Prolongs anticoagulant duration

44.  Cefoxitin is more active against anaerobes & is most
active cephalosporin against B.fragilis
 It is generally used for treatment of lung abcesses , &
pelvic inflammatory disease
 MECHANISM OF ACTION :-
 Cefoxitin mainly causes inhibition of the cell wall
synthesis mainly inhibiting the cross linking of the
peptide chains.
 PHARMACOKINETICS :-
 Absorption :- The drug is well absorbed post IV/IM
infusion

45.  Distribution :- It is widely distributed throughout the
body with poor penetration
 Protein binding :- approx 30 %
 Metabolism :- Not metabolized in the body
 Elimination :- about 85 % of the drug is excreted
unchanged in the urine
 T ½ :- Half life after an IV dose is 41 -50 minutes
 USES :- It is mainly used in lung abcesses , UTIs ,
Endometritis , Gonorrhoea , Peritonitis , Influenza ,
Pelvic cellulitis etc.

46.  CONTRAINDICATIONS :-
 It is contraindicated in patients with known allergy to
cephalosporins
 PRESCRIBED DOSE :-
 Uncomplicated infections :- 1g IV in 6-8 hours ,
maximum dose is 3-4 g
 Severe infections :- 2g IV in every 6-8 hours ; 6-8
g/day is maximum dose
 If used for surgical prophylaxis :- 1-2 IV
 Renal impairment :-
 Crcl ( 30-50 Ml/min ) : 1-2 g in 8-12 hours
 Crcl (10-30 ml / min ) : 1-2 g in 12-24 hours

47.  ADVERSE EFFECTS :-
 High doses may cause CNS toxicity , pregnant women
are associated with risk of miscarriage , Diarrhoea ,
Anaemia , Eosinophilia , Leukopenia etc.
 INTERACTIONS :-
 No major drug interactions are shown by Cefoxitin

48.  Third generation cephalosporins are highly
resistant to beta-lactamases,have good
activity against gram-negative organisms &
anaerobes
 They cross the BBB , hence useful in
Meningitis
 They can be life-saving in serious gram-
negative infections & hence have replaced
 second generation agents.

49.  Cefotaxime is highly resistant to several beta-
lactamases & it has a wide gram –negative coverage.
 It crosses the BBB & has been used successfully in
the treatment of meningitis due to H.influenzae,
S.pneumoniae , meningitis
 MECHANISM OF ACTION :-
 On parenteral administration cefotaxime show
bactericidal property by inhibiting the cell wall
synthesis
 PHARMACOKINETICS :-
 Absorption :- rapidly absorbed following
intramuscular injection

50.  Distribution :- It is distributed throughout the body
 Metabolism :- approximately 20-36% of an
intravenously administered dose of 14C-cefotaxime is
excreted by the kidney as unchanged cefotaxime and
15-25% as the desacetyl derivative, the major
metabolite. The desacetyl metabolite has been
shown to contribute to the bactericidal activity. Two
other urinary metabolites (M2 and M3) account for
about 20-25%. They lack bactericidal activity.
 Elimination :- approximately 20-36% of an
intravenously administered dose of 14C-cefotaxime is
excreted by the kidney as unchanged cefotaxime and
15-25% as the desacetyl derivative, the major
metabolite.

51.  T ½ :- 60-70 minutes
 USES :- It is mainly used for the treatment of
Pneumonia , meningitis epiglottitis , pyoderma ,
pyelonephritis , subcutaneous abcess , pelvic
inflammations , peritonitis
 CONTRAINDICATIONS :- It is contraindicated in
patients with known allergy to cephalosporins
 PRESCRIBED DOSE :-
 < 12 years or <50 kg :- 50-200 mg/kg/day , IV/IM in 6-
8 hourly divided doses for 7-14 days
 For meningitis :- 250 mg/kg/day in 6-8 hourly divided
doses

52.  >12years or >50kg :-1-2 g IV/IM every 8 hours for 7-
14 days
 For meningitis :- 3g /day IV
 ADVERSE EFFECT :-
 Injection site inflammation , hypersensitivity
reactions , colitis , diarrhoea , nausea , vomiting ,
pseudomembranous colitis
 INTERACTION :- If given alongwith aminoglycoside
antibiotics , it shows increased risk of nephrotoxicity

53.  Ceftriaxone is a long-acting cephalosporin for IV / IM
administration also it is one of the most commonly
used agents for meningitis
 MECHANISM OF ACTION :-
 Ceftriaxone is bactericidal in nature as it causes
inhibition of the bacterial cell wall synthesis , mainly
by binding to PBP 3 .
 PHARMACOKINETICS :-
 Absorption :- Ceftriaxone is only given as an
injection, either intramuscularly or
intravenously.11 Ceftriaxone is less than 1%
bioavailable if given orally.3

54.  Distribution :- 5.78 to 13.5 L
 Protein binding : - Ceftriaxone is 95% protein bound
 Metabolism :- negligible
 Elimination :- about 33 % of the drug is excreted in
the urine , the remainder is eliminated by bile
secretion ( excretion by faeces )
 T ½ :- 5.8 -8.7 hours
 USES :-
 Meningitis , typhoid , pneumonia , otitis media,
pyelonephritis , pelvic infections , septicaemia ,
gonococcal infections etc

55.  CONTRAINDICATIONS :- It is contraindicated in
patients with known allergy to cephalosporins
 PRESCRIBED DOSE :-
 50-100 mg/kg/day IV divided in 12 hourly doses for
7-14 days , maximum dose is 4 g / day
 In meningitis :- 100 mg/kg/day
 ADVERSE EFFECTS :- Injection site inflammation ,
rash , pruritis , otitis media , fever , eosinophilia ,
urticaria , colitis, diarrhoea etc
 INTERACTION :- Increased nephrotoxicity if taken
with aminoglycoside antibotics

56.  Cefoperazone is particularly more effective against
Pseudomonas whereas activity against other gram –
negative bacteria is weaker
 It is not very useful for the treatment of meningitis
as it does not penetrate the BBB as freely as
compared to other 3rd generation cephalosporins
 Cefoperazone fails to inhibit beta lactamase
producing microbes
 MECHANISM OF ACTION :-
 It acts by inhibiting cell wall synthesis of bacteria by
binding to PBP3

57.  PHARMACOKINETICS :-
 Absorption :- It is well absorbed by intravenous or
intramuscular administration
 Distribution :- well distributed throughout the body
 Protein binding :- 60 -70 %
 Elimination :- It is mainly excreted by the bile
 T ½ :- 1.5 -2 hours
 USES :-
 Respiratory tract infections caused by S.
pneumoniae, H. influenzae, S. aureus
 Peritonitis and other intra-abdominal infections
caused by E. coli, P. aeruginosa, and anaerobic gram-
negative bacilli (including Bacteroides fragilis).

58.  Bacterial septicemia caused by S. pneumoniae, S.
agalactiae, S. aureus, Pseudomonas aeruginosa, E.
coli, Klebsiella spp., Klebsiella pneumoniae, Proteus
species (indole-positive and indole-
negative), Clostridium spp. and anaerobic gram-
positive cocci.
 Infections of the skin and skin structures caused by S.
aureus
 Pelvic Inflammatory Disease, Endometritis, and Other
Infections of the Female Genital Tract caused by N.
gonorrhoeae,
 Peritonitis

59.  CONTRAINDICATIONS : - It is contraindicated in
patients with hypersensitivity
 PRESCRIBED DOSE :-
 100 – 200 mg/kg/day in 2 divided doses IV/IM for 10-
14 days
 ADVERSE EFFECT :-
 Anemia , bleeding , haemolytic anemia , leukopenia ,
bone marrow depression , dizziness , fever pain,
chills , urticaria
 INTERACTIONS :-
 It produces disulfiram like reactions when taken with
alcohol

60.  It is orally effective with good activity against gram-
positive cocci , H.influenzae , gonococci , & is highly
effective against Enterobacteriaceae.
 It is mainly used in the infections of urinary , respiratory &
biliary infections
 MECHANISM OF ACTION :- It shows bactericidal activity by
causing inhibition of cross linking of peptide chains
 PHARMACOKINETICS :-
 Absorption :- With oral administration of cefixime,
about 40%-50% is absorbed whether administered
with or without food. However, time to maximal
absorption is increased approximately 0.8 hours when
administered with food.

61.  Distribution :- Cefixime has a volume of distribution
averaging 0.1 L/kg of body weight when administered
orally
 Protein binding :- 65 % cefixime is bound to serum
proteins
 Metabolism :- not metabolized in the body
 Elimination :- Approximately 50% of absorbed
cefixime is excreted unchanged in the urine in 24
hours
 T ½ :- 3-4 hours
 USES :- UTIs , Diarrhoea , Enteric fever , other garm –
ve infectionjs etc

62.  PRESCRIBED DOSE :-
 For children :- 8mg/kg/24hours orally in 1-2 divided
doses
 IN TYPHOID :- 20 mg/kg/day in 2 divided doses for 14
days
 For adolescents & adults :- 400 mg/24 hours orally in
1-2 divided doses
 ADVERSE EFFECTS :-
 Pseudomembranous colitis , nausea , vomiting,
diarrhoea , hypersensitivity , hepatic dysfunction ,
fever , thrombocytopenia , serum sickness , Stevens-
Johnsons syndrome

63.  INTERACTIONS :- No major drug or food interactions
are shown by the drug

64.  Fourth generation Cephalosporins include –
CEFPIME & CEFPIROME, active against a
variety of gram+ve & gram-ve bacteria
 More resistant to many of the Beta-
lactamases
 Both cefepime & cefpirome are administered
parenterally, half –life is about 2 hrs ,
excreted through kidneys
 Cefepime attains high concentration in CSF
while Cefpirome has good tissue
penetrability.

65.  These agents are widely used in
Specticaemia , nosocomia & other serious
infections of the skin , urinary & respiratory
tracts & infections in immunocompromised
infections
 Cefepime – DOSE:- 1-2 gm IV q 8-12hr
 Cefpirome – DOSE:-1-2 g IM/IV q 12hrs

66.  Fifth generation cephalosporins include-
Ceftaroline & Ceftobiprole
 These are anti-MRSA cephalosporins, both
drugs are also effective against penicillin-
resistant Streptococcus pneumoniae in
addition to gram-ve microbes
 Used for mainly skin & respiratory infections
 Ceftobiprole is also effective against
Pseudomonas
 DOSE:-600mg slow IV over 1 hour

67. 1.
•Hypersensitivity reactions
2.
•Nephrotoxicity
3.
•Diarrhoea

68. 4.
•Bleeding
5.
• Low WBC count
6.
• Pain

69. GRAM-VE
infections
Surgical
Prophylaxis
Gonorrhoea TYPHOID

70. Respiratory
infections
Nosocomial
infections