Pharmacology:

Antibacterial Agents Penems

With Dr. Pravin J. Shukle
Pharmacology
Penicillins

Cephalosporins
Cell wall
synthesis
inhibitors

Penems Sulfapenems

Carbapenems

Miscellaneous
Sulfapenems

Faropenem (Not available in the USA):

• Orally active unsaturated ß-lactam antibiotic

• Resistant to many different forms of extended

spectrum ß-lactamases

• Improved chemical stability

• Completed trials in tuberculosis, pulmonary

tuberculosis, and community-acquired
pneumonia
Carbapenems

Imipenem, ertapenem, meropenem

• Chemically unique, but still containing a ß-

lactam ring

• Low susceptibility to penicillinases

• Very susceptible to renal
dehydropeptidases
• Administered with cilastatin (inhibitor)
Carbapenems

Imipenem, ertapenem, meropenem

• Wide-ranging activity against:

• Gram-positive cocci

• Gram-negative rods

• Anaerobes

• Pseudomonas and Acinetobacter species

Pharmacology
Penicillins
1st generation

2nd generation
Cephalosporins
Cell wall
3rd generation
synthesis
inhibitors
4th generation
Penems
5th generation

Unclassified
Miscellaneous
First-generation Cephalosporins

Cefazolin (Ancef®), cefalexin (Keflex®), cefalotin

• Gram-positive

• Used in surgical infections

• Minimal effectiveness against gram-

negative bacteria
Pharmacology
Penicillins
1st generation

2nd generation
Cephalosporins
Cell wall
3rd generation
synthesis
inhibitors
4th generation
Penems
5th generation

Unclassified
Miscellaneous
Second-generation Cephalosporins

Cefotetan, cefuroxime, cefaclor, cefoxitin

• More active against gram-negative

• Will also work against Haemophilus

influenzae

• Has some anti-anaerobe activity

Pharmacology
Penicillins
1st generation

2nd generation
Cephalosporins
Cell wall
3rd generation
synthesis
inhibitors
4th generation
Penems
5th generation

Unclassified
Miscellaneous
Third-generation Cephalosporins

Ceftazidime, cefotaxime, ceftriaxone

• Less effective at combating gram-positive

infections compared to 1st and 2nd
generation

• Even more active against gram-negative

• Will often work against organisms that are

resistant to penicillin

• Only in serious infections

Pharmacology
Penicillins
1st generation

2nd generation
Cephalosporins
Cell wall
3rd generation
synthesis
inhibitors
4th generation
Penems
5th generation

Unclassified
Miscellaneous
Fourth-generation Cephalosporins

Cefepime

• Fourth-generation cephalosporins → zwitterions

• More resistant to ß-lactamases

• Enterobacter, Haemophilus, Neisseria

• Activity in infections caused by Pseudomonas

aeruginosa
Pharmacology
Penicillins
1st generation

2nd generation
Cephalosporins
Cell wall
3rd generation
synthesis
inhibitors
4th generation
Penems
5th generation

Unclassified
Miscellaneous
Fifth-generation Cephalosporins

Ceftaroline, ceftolozane, ceftobiprole

Not everyone accepts this nomenclature

Ceftaroline:

• MRSA coverage

Structure of ceftaroline

Edgar181, PD
Fifth-generation Cephalosporins

Ceftaroline, ceftolozane, ceftobiprole

Not everyone accepts this nomenclature

Ceftobiprole:

• Powerful antipseudomonal activity

• VRE coverage

Structure of ceftobiprole

Fuse809, PD
Fifth-generation Cephalosporins

Ceftaroline, ceftolozane, ceftobiprole

Not everyone accepts this nomenclature

Ceftolozane:

• Complicated intraabdominal infections

• Complicated urinary tract infections

• Often combined with tazobactam

Structure of ceftolozane

Edgar181, PD
Pharmacology
Penicillins
1st generation

2nd generation
Cephalosporins
Cell wall
3rd generation
synthesis
inhibitors
4th generation
Penems
5th generation

Unclassified
Miscellaneous
Unclassified Cephalosporins

Cefaparole, cefmatilen, cefsumide, cefcanel, and others

• New and have not yet been classified