Student of Ayub Medical College AbbottAbad, Pakistan Email Sheralamkhan97@yahoo.com

1. Cephalosporins
By SherAlam Khan Mohmand student of Ayub Medical
college,AbbottAbad,Pakistan.
Email Sheralamkhan97@yahoo.com
Cephalosporins are bactericidal agents. Cephalosporin was isolated from fungus called
CEPHALOSPORIUM ACREMONIUM by BROTZU in from sewer water in Sardinia in 1948 in
Willium Dunn School of Pathology.The first use agent was Cephalothincephalosporin-C used
clinically in 1964.Cephalosporins are structurally related to Penicillins consists of a Beta lactum
ring attached to Dihydrothiazoilne ring.
The Cephalosporin nucleus, 7-Aminocephalosporanic acid (7-ACA) was derived from Cephalosporin-C
and proved to be analogous to the penicillin nucleus, 6-Aminopenicillanic acid.
Modification of 7-ACA side chains resulted in development of useful antibiotic agents, and the first
agent Cephalothin was launched by Eli Lilly in 1964.
These Agents are Active against
1)Gram Positive Bacteria
2)Gram Negative Bacteria
3)Some anaerobic bacteria
Mechanism of action:
Cephalosporins disrupt the Peptidoglycan layer of bacterial cell wall.
The Peptidoglycan is an important bacterial cell wall integrity.The final
transpeptidation step ithe synthesis of peptidoglycan is facilitated by
transpeptidases known as Penicillin Binding Protiens(PBP). These PBPs bind to
D-Ala-D-Ala at the end of muropeptides 9Peptidoglycan precursors) to crosslink
the peptidoglycan. So the Beta Lactumagentscompetitivel inhibit PBP crosslinking
of peptidoglycan.

2. Classification of Cephalosporins.
Cephalosporins fall in FIVE classes or Generations. Each subsequent generation of
these drugs demonstrates greater efficacy against Gram negative bacteria.
Generalization that with increasing “generation” activity in vitro against Gram
Positive Organisms decreases while activity against Gram Negative Organisms
increases.
Note: Many drugs in the same generation are not chemically related and having
different spectrum of activity. Division in generation is just for your convenience.
3rd and 4thgenrstioncephalosporins are used in hospital setting in seriously ill
patients for serious and life threatening diseases.Many of these diseases are due
to organisms residing in gastro-intestinal tract. Drugs of last resort for serious
infections due to food borne pathogens Salmonella and Shigella.
1st Generation Cephalosporins.
1) Cefacetrile
2) Cefadroxil
3) Cefalexin
4) Cefaloglycin
5) Cefalonium
6) Cefaloridine
7) Cefapirin
8) Cefalothin
9) Cefatrizine
10)
Cefazedone
11)
Cefrozadine
12)
Cefazolin
13)
Ceftezole
14)
Cefazaflur
15)
Cephradine

3. Activity of 1st generation cephalosporins.
1) Gram Positive Cocci
a)Pneumococci
b) Viridans Streptococci
c) Group-A hemolytic streptococci
d) Staphylococcus aureus
e) Streptococcus Pyogenese
f)Streptococcus Pneumoniae
2)
a)
b)
c)
d)
e)
f)
Gram Negative Bacteria
E.Coli
Klebsiella Pneumonia
Proteus Mirabilis
CorynebacteriumDiptheriae
Salmonella
Neisseria
Indications of 1st generation Cephalosporins.
1)
2)
3)
4)
5)
Nose infection
Throat infection
Chest infection
Ear infection
Urinary tract infection

4. 6)
7)
8)
9)
Gynae infection
Skin infectiom
Gum infection
Bronchitis
Contra-indications of 1st generation cephalosporins.
Avoid use in allergic persons.
Adverse effects of 1st Generation Cephalosporins.
Usually seen Adverse effects are:
diarrhea that is watery or bloody.
fever, chills, body aches, flu symptoms.
tightness in your chest.
unusual bleeding.
seizure (convulsions).
pale or yellowed skin, dark colored urine, fever, confusion or weakness.
jaundice(yellowing of the skin or eyes).
skin rash, bruising, severe tingling, numbness, pain, muscle weakness.
Sore throat, and headache with a severe blistering, peeling, and red skin rash.
Increased thirst, loss of appetite, swelling, weight gain, feeling short of breath, urinating less than usual
or not at all.
Less serious side effects of cephradine may include:
nausea, vomiting, stomach pain, mild diarrhea;
stiff or tight muscles;
joint pain;
dizziness;
feeling restless or hyperactive;
unusual or unpleasant taste in your mouth;
mild itching or skin rash; or
vaginal itching or discharge.

5. 2nd Generation Cephalosporins.
1)Cefotetan
2)Cefmetazole
3) Cefoxitin
4)Cefaclor
5) Cefonicid
6)Cefprozil
7)Cefuroxime
8)Cefuzonam
9)Cefamandole
Activity of 2nd generation cephalosporins against bacteria.
1)
2)
3)
4)
5)
6)
7)
8)
9)
Staphylococci
Streptococcus pneumonia
Moraxella catarrhalis
H.influenzae
E.Coli
Proteus Mirabilis
Klebseilla
Neisseria
Citrobacter

6. Mechanism of action of 2nd generation cephalosporins.
Mechanism of action:
Cephalosporins disrupt the Peptidoglycan layer of bacterial cell wall.
The Peptidoglycan is an important bacterial cell wall integrity.The final
transpeptidation step ithe synthesis of peptidoglycan is facilitated by
transpeptidases known as Penicillin Binding Protiens(PBP). These PBPs bind to
D-Ala-D-Ala at the end of muropeptides 9Peptidoglycan precursors) to crosslink
the peptidoglycan. So the Beta Lactumagentscompetitivel inhibit PBP crosslinking
of peptidoglycan.
Indications of 2nd generation cephalosporins.
1) Nose infection
2) Throat infection
3) Ear infection
4) U.T.I
5) Chest infection
6) Skin infection
7) Gonorrhea
8) Diverticulitis
9) Peritonitis
10) Cefoxitin and Cefotetan are used as Prophylaxis in Colorectal
surgeries, vaginal or abdominal histerectomies and appendicitis
because of activity against BacteriodFragilis.

7. Contra-indications of 2nd generation cephalosporins.
1) Use carefully in Pregnant and breast feeding women.
2) Use carefully in patients with renal failure.
3) Do not prescribe for sensitive pesrons.
Adverse Effects of 2nd generation cephalosporins.
1) Damage kidneys and liver.
2) Sleep time decrease.
3) Nausea,vomiting,diarrhea.
4) Confusion.
5) Pain in joints.
6) Temporarily decrease in White Blood Cells.
7) Generalized weakness.
8) Lightheadedness.
9) Giddiness.
10)
Prothrombin time gets increased.
11)
Fungus infection(Candidiasis)
12)
Indigestion.
13)
Sensitivity Reactions.

8. 3rd generation cephalosporins.
1) Cefixime
2) Cefdinir
3) Cefpodoxime
4) Cefteram
5) Ceftibuten
6) Cefminoxime
7) Ceftizoxime
8) Cefriaxone
9) Cefotaxime
10)
Ceftazidime
11)
Cefopirazone
Mechanism of Action of 3rd generation.
Mechanism of action:
Cephalosporins disrupt the Peptidoglycan layer of bacterial cell wall.
The Peptidoglycan is an important bacterial cell wall integrity.The final
transpeptidation step ithe synthesis of peptidoglycan is facilitated by
transpeptidases known as Penicillin Binding Protiens(PBP). These PBPs bind to
D-Ala-D-Ala at the end of muropeptides 9Peptidoglycan precursors) to crosslink
the peptidoglycan. So the Beta Lactumagentscompetitivel inhibit PBP crosslinking
of peptidoglycan.

9. Activity of 3rd generation cephalosporin against Bacteria.
1) Enterobacteriaceae
2) Pseudomonas aeruginosa
3) Hemophilus influenza
4) Neisseria
5) Nonenterococcal streptococci
6) Anaerobic gram-positive cocci.
7) Staphylococcus aureus
8) Staphylococcus epidermidis
9) Streptococcus pyogenese
10) Streptococcus pneumoniae
11) Streptococcus Group-B
12) Streptococcus viridans
13)
14)
15)
16)
17)
18)
19)
20)
21)
22)
23)
24)
25)
Moraxella catrrhalis
Neisseria gonorrheae
Neisseria meningitides
Citrobacter
Enterobacter
E.Coli
Proteus
Salmonella
Shigella
Vibrio
Pastuerella
Yersinia
Serratia

10. Indication of 3rd generation cephalosporins.
1) Sinusitis
2) Bronchitis
3) Phyrangitis
4) Tonsillitis
5) Pneumonia
6) Meningitis
7) Otitis media
8) Innfections caused by Staphylococcus aureus.
9) Gonorrhea
10)
Skin infection.
11)
Pelvic inflammatory disease.
12)
Gynae infection.
13)
Nose infection.
14)
Throat infection.
15)
Kidneys infection.
16)
Bones and joints infection.
17)
Peritonitis
18)
Septicemia
19)
Infection after surgery
20)
Gall bladder infection
Adverse effects of 3rd generation cephalosporins.
1)
2)
3)
4)
5)
Allergic reactions
Nausea,vomiting,diarrhea.
Flatulence
Anemia
Leukopenia

11. 6) Pseudomembranous colitis
7) Flushing
8) Headache
9)
10)
Giddiness
11)
Elivation of liver SGOT and SGPT
12)
Vaginitis
13)
Bronchospasm
14)
Allergic Pneumonitis
15)
Flatulence
16)
Dyspepsia
17)
Jaundice
18)
Hematuria
19)
Seizure
20)
Serum sickness
4th generation cephalosporons
1)
2)
3)
4)
5)
6)
7)
Cefepime
Cefozopran
Cefpirome
Cefquinome
Cefoselis
CefluPrenam
Cefclidine
Mechanism of Action of 4th generation.
Mechanism of action:
Cephalosporins disrupt the Peptidoglycan layer of bacterial cell wall.

12. The Peptidoglycan is an important bacterial cell wall integrity.The final
transpeptidation step ithe synthesis of peptidoglycan is facilitated by
transpeptidases known as Penicillin Binding Protiens(PBP). These PBPs bind to
D-Ala-D-Ala at the end of muropeptides 9Peptidoglycan precursors) to crosslink
the peptidoglycan. So the Beta Lactumagentscompetitivel inhibit PBP crosslinking
of peptidoglycan.
Activity of 4th generation cephalosporins against bacteria.
1) Pseudomonas auregenosa
2) Klebseilla pneumonia
3) E.Coli
4) Prteus mirabilis
5) Enterobacter Species
6) BacteroidsFragilis
7) Staphylococcus aureus.
8) Streptococcus pyogenese
9) Salmonella
10)
Citrobacter
11)
Shigella
12)
H.influenzae
13)
Streptococcus viridans
Indications of 4th generation cephalosporins.
1)
2)
3)
4)
5)
6)
7)
Otitis media
Sinusitis
Phyrangitis
Tonsillitis
Bronchitis
U.T infections
Gonorrhea

13. 8) Gynae infection
9) Infection after delivery
10)
Skin infections
11)
Intra abdominal infection (use with metronidazole)
12)
Typhoid fever
13)
Contra indications:
1) Use carefully in Pregnant Women
2) Do not use in allergic Patients
Adverse effects of 4th generation Cephalosporins.
1) Diarhea (bloody or watery)
2) Confusion
3) Hallucinations
4) Seizures
5) Fever,Chills, body aches.
6) Weakness
7) Easily bruising or bleeding.
8) Sore throat
9) Severe headache
10) Abdominal pain
11) Flatulence

14. INDICATIONS
MAXIPIME is indicated in the treatment of the following infections caused by susceptible strains of the
designated microorganisms (see alsoPRECAUTIONS: Pediatric Use and DOSAGE AND ADMINISTRATION):
Pneumonia (moderate to severe) caused by Streptococcus pneumoniae, including cases associated with
concurrent bacteremia, Pseudomonas aeruginosa, Klebsiellapneumoniae, or Enterobacter species.
Empiric Therapy for Febrile Neutropenic Patients. Cefepime as monotherapy is indicated for empiric
treatment of febrile neutropenic patients. In patients at high risk for severe infection (including patients with
a history of recent bone marrow transplantation, with hypotension at presentation, with an underlying
hematologic malignancy, or with severe or prolonged neutropenia), antimicrobial monotherapy may not be
appropriate. Insufficient data exist to support the efficacy of cefepimemonotherapy in such patients.
Uncomplicated and Complicated Urinary Tract Infections (includingpyelonephritis) caused by Escherichia
coli or Klebsiellapneumoniae, when the infection is severe, or caused by Escherichia coli,
Klebsiellapneumoniae, or Proteus mirabilis, when the infection is mild to moderate, including cases
associated with concurrent bacteremia with these microorganisms.
Uncomplicated Skin and Skin Structure Infections caused by Staphylococcus aureus (methicillin-susceptible
strains only) or Streptococcus pyogenes.
Complicated Intra-abdominal Infections (used in combination with metronidazole) caused by Escherichia
coli, viridans group streptococci,Pseudomonasaeruginosa, Klebsiellapneumoniae, Enterobacter species, or
Bacteroidesfragilis.
DOSAGE AND ADMINISTRATION
SITE AND TYPE OF INFECTION
DOSE
FREQUENCY
DURATION
(DAYS)
1 to 2 g IV
Every 12
hours
10
2 g IV
Every 8
hours
7**
Adults
Moderate to Severe Pneumonia due to S.
pneumoniae*, P.
aeruginosa, K. pneumoniae, or Enterobacter
species
Empiric therapy for febrile neutropenic patients
(See INDICATIONS AND USAGEand Clinical
Studies.)

15. Mild to Moderate Uncomplicated or
Complicated Urinary Tract Infections, including
pyelonephritis, due to E. coli, K.pneumoniae, or
P. mirabilis*
0.5 to 1 g
IV/IM***
Every 12
hours
7 to 10
Severe Uncomplicated or Complicated Urinary
Tract Infections, including pyelonephritis, due to
E. coli or K. pneumoniae*
2 g IV
Every 12
hours
10
Moderate to Severe Uncomplicated Skin and
Skin Structure Infections due to S. aureus or S.
pyogenes
2 g IV
Every 12
hours
10
Complicated Intra-abdominal Infections (used in
combination with metronidazole) caused by E.
coli, viridans group streptococci, P. aeruginosa,
K. pneumoniae, Enterobacter species, or B.
fragilis. (See Clinical Studies.)
2 g IV
Every 12
hours
7 to 10
Pediatric Patients (2 months up to 16 years)
The maximum dose for pediatric patients should not exceed the recommended adult dose. The usual
recommended dosage in pediatric patients up to 40 kg in weight for uncomplicated and complicated urinary
tract infections (including pyelonephritis), uncomplicated skin and skin structure infections, and pneumonia
is 50 mg per kg per dose, administered every 12 hours (50 mg per kg per dose, every 8 hours for febrile
neutropenic patients), for durations as given above.
*including cases associated with concurrent bacteremia **or until resolution of neutropenia. In patients
whose fever resolves but who remain neutropenic for more than 7 days, the need for continued
antimicrobial therapy should be re-evaluated frequently.
***Intramuscular route of administration is indicated only for mild to moderate, uncomplicated or
complicated UTIs due to E. coli when the intramuscular route is considered to be a more appropriate route
of drug administration.
5th Generation Cephalosporons
These agents were developed in laboratory to specifically target against resistant
strains of bacteria. In particular CEFTOBIPROLE is effective against Methicillin
Resistant Staphylococcus Aureus(MRSA).
Ceftobiprole is the only available agent of 5th generation. It has powerful
antiPseudomonal activity.
Mechanism of Action of 5th generation cephalosporins.
Same as other generations.
Activity of 5th generation cephalosporins.
1) MRSA

16. 2)
3)
4)
5)
6)
Streptococcus Pneumoniae
Pseudomonas Aeruginosa
EnteroCocci
E.Coli
Methicillin resistant Staphylococcus Epidemidis
Indication of 5th generation cephalosporins.
1)
2)
3)
4)
Hospital acquired pneumonia
Community acquired Pneumonia
Bacteremia
Chemotherapy induced Neutropenia and fever.
Adverse effects of 5th generation.
1)Nausea,vomiting,diarrhea
2)Flushing of skin
3) Weakness
4) Liver,kidneys damage
5) Indigestion