CEPHALOSPORIN

(utk 2nd and 3rd generation spectrum berbeza:reduce OR maintain +ve gram spectrum)
GENERATION 1ST 2ND 3RD 4TH 5TH

SPECTRUM - Moderate - Greater gram –ve BROAD SPECTRUM cephalosporin - EXTENDED 1. Gram +ve :
spectrum agent 1. Hemophilus with further increase in gram –ve but SPECTRUM agents - MRSA
influenza decrease again gram +ve: against gram +ve - S. pneumonia
- Treating 2. moraxella catarrhalis (same like 1st - Enterococcus
infection of: 3. Enterobacter  Gram +ve cocci (incl. Penicillin generation) and faecalis
1. Gram +ve cocci: aerogene resistance) gram -ve
4. E.coli (MAINTANCE AGAINST GRAM 2. Gram –ve
- Staphy. Aureus
5. Klebsiella +VE) similar to 3rd
(Methicillin- pneumonia - excellent against: and 4th
sensitive MSSA) 6. Proteus mirabillis  Enhance against gram –ve bacteria 1. Enterobacteriace generation
- S. epidermidis 7. Neisseria species compare 1st and 2nd: ae
(strep. group A ) (–ve cocci) 1. Enterobacctericeae (eg: E.coli, 2. Pseudomonas 3. LIMITED
- Strep. 8. B. fragilis klebsiella, proteus, Enterobacter, aeruginosa anaerobic
pneumonia Serratia, Citrobacter, Salmonella) (similar to activity
- Maintance gram +ve – often resistance ceftazidime but
- Strep. Pyogene
(similar to 1st) 2. P. mirabilis has better gram
- Anaerobic 3. Provindencia +ve activity)
streptococci - Active against anaerobic 4. H. Influenza 3. S. pneumonia
2. Poor anaerobic microbe 5. N.meningitides (similar to
3. Gram –ve 6. N. gonorrhoeae ceftriaxone)
 E. coli 1. Cephalosporin 4. Citrobacter
 Klebsiella (do not adequate anaerobic  Anti pseudomonal cephalosporin: 5. Enterobacter
coverage to be used for
 P.mirabilis
abdominal infection) 1. Pseudomonas
2. Cephamycin 2. Gram +ve
(do not have adequate gram 3. Gram –ve
+ve coverage to treat 4. Poor gram +ve cocci
respiratory infection) 5. No coccibacillus
  some anaerobic cover but not for B.
Fragilis

DOSAGE FORM - Oral agent (all 1. Cephalosporin Oral agent: 1. Cefepime 1. Ceftobiprole
have same Oral agents + broad - Cefixime (broad gram –ve with 2. Ceftolozane
efficacy) spectrum: - Cefpodoxime enhanced activity 3. Ceftaroline
1. Cephalexin - Cefaclor against pseudomonas *do not cover
(prototype, - Loracarbef Parental agent: but slightly lesser pseudomonas
help in - Cefprozil - Ceftizoxime activity against
pharyngitis) - Cefuroxime - Cefotaxime (penetrate CSF) pneumococci)
2. Cephradine *cover S.pneumoniae - Ceftriaxone 2. Cefluprenam
3. Cefadroxil *actively against penicillin-resistance 3. Cefozopran
4. Cephalothin 2. Cephamycin streptococcus pneumonia 4. Cefpirome
5. Cephapirin Parental agent + anti- - ceftazidime (antipseudomonal activity (more active against
anaerobe: and cover Pseudomonas aeruginosa) – pneumococci but lesser
- Parental agent - Cefamandole similar to aztreonam due to same pseudomonas)
1. Cefazolin - Cefotetan structure and do not cover gram +ve
(commonly - Cefoxitin bacteria)*different with other 3rd Cefepime and
used, LONG *cover B.fragilis generation. cefpirome
duration, * both active against
penetrate *2 groups in 2nd generation Cefotaxime & Ceftriaxone treat neonate nosocomial pathogen
bone well) and child meningitis, stept. Pneumonia, such as enterobacter
increase potency against penicillin and acinetobacter
resistance pneumococci. (restricted to
nosocomial sepsis)
DISEASES - Alternatives for 1. Cephalosporin - Infection involve gram –ve bacteria: - effective to treat:
4. Skin and soft - upper and lower 1. Hospital acquired infection 1. Meningitis
tissues infection respiratory tract 2. Complicated community acquired (most can across
5. Streptococcal infection: infection BBB)
pharyngitis
Eg: - community Both lead to infection: *clinical used smilar in
acquired infection 1. Respiratory tract 3rd generation
pneumonia 2. Blood
- Uncomplicated UTI 3. Intra abdominal
 (e.coli) 4. Skin
- Sinusitis 5. Soft tissue
- Otitis media 6. UTI

2. Cemphamycin: *this generation better for hospitalized pt or

- Mixed aerobic and received current antibiotics and
anaerobic infection on immunocompromised
skin and soft tissue
- Intra-abdominal
- Gynaecologic infection
- Surgical prophylaxis
- UTI (by E.coli,
klebsiella and proteus)

RESISTANCE More resistance Intermediate and high level resistance to Greater resistance than
TO BETA
LACTAMASE penicillinase check balik 3rd generation
ALLERGIC Increased cross- Cephamycin:
/ADR
reactivity in 1. Hypoprothrombinem - in renal dysfunction pt, aminoglycoside
penicillin allergic ia and bleeding (due can replace this generation (sbb gram –ve
patient compared to to disturb synthesis spectrum sama)
others of vit. K dependent
(allergic to a clotting factor
substance, however 2. Renal or hepatic
body starts to disease
develop allergic 3. Poor nutrition
towards other 4. Elderly
substance that has 5. Cancer
similarity with the 6. Alcohol intolerance-
allergen unable to break
down or metabolise
alcohol in body
(avoid alcohol after
several day stop
course)
*nosocomial infection (occur within 48 hrs hospital admission, 3 days discharge, and 30 days operation)

1. Difference between cephalosporin and cephamycins

Cephalosporin:

- Cephalosporin is extracted from FUNGUS (Cephalosporium acremonium) that contains anti bacterial properties which is containing beta-lactam
ring (like penicillin) but fused with six members dihydrothiazine.

Cephamycins:

- The first beta lactam extracted from BACTERIAL source (streptomyces clavuligerus).

2. Comparision between penicillin and cephalosporins

Similarities:

- Both contain beta lactam ring that plays role as anti-bacterial agents.
- Mechanisms of action (bind to transpeptidase (PBP) enzyme inhibit the formation of peptidoglycan in synthesis of cell wall) and resistance of
cephalosporins (inactivated by beta-lactamase) are similar to penicillin.

BROAD SPECTRUM –has activity against both gran +ve and –ve

EXTENDED SPECTRUM –had a chemical modificationwith increase gram –ve coverage. Eg:cephalosporin (1st no gram –ve)(then gram –ve
coverage increase progressively)
Penicillin: DRAW STRUCTURE:

- Has 1 side chain + beta lactam + thiazolidine ring (5 members ring)

Carbapenem

- beta lactam + cyclic 5 ring members no double bond

Cephalosporins:

- Has 2 side chains + beta lactam + dihydrothiazine ring (6 members ring)

Monobactam:

-single ring

Beta lactamase inhibitors

Class of antibiotics

1. Beta lactam 2. Glycopeptides 3. Trimethoprim

4. Aminoglycoside 5. Oxazolidinones 6. Nitrofuraton
7. Quinolone 8. Lipopeptide 9. Polymyxins
10. Macrolide 11. Streptogramims 12. Rifamycin
13. Tetracycline 14. Sulphonamide 15. Metronidazole
16. Lincosamide 17. Chloramphenicol