1ST GENERATION

CEPHALEXIN – KEFLEX – MARK (ORAL)

CEFADROXIL – DURICEF – MARK (ORAL)
CEPHRADINE – VELOSEF – SIR NINO (ORAL AND PARENTERAL) (IM, IV)
CEFAZOLIN – KEFZOL – SIR NINO PARENTERAL (IM, IV)

2ND GENERATION
CEFACLOR – CECLOR – YAP (ORAL)
CEFPROZIL – CEFZIL – YAP
CEFOTETAN – CEFOTAN – AHLVIE
CEFOXITIN – MEFOXIN – AHLVIE (PARENTERAL)
CEFUROXIME AXITEL – ZINAT – ANGEL (ORAL)
CEFUROXIME – ZINACEF – ANGEL (PARENTERAL)

CEPHALEXIN

Cephalexin is a first-generation cephalosporin used to treat certain susceptible bacterial infections.

Brand name – CEFALEXIN EXEL
Generic Name – Cephalexin
Background - Cephalexin is the first of the first generation cephalosporins. This antibiotic contains a beta lactam and a
dihydrothiazide. Cephalexin is used to treat a number of susceptible bacterial infections through inhibition of cell wall
synthesis
Indication - Cephalexin is indicated for the treatment of certain infections caused by susceptible bacteria. These infections
include respiratory tract infections, otitis media, skin and skin structure infections, bone infections, and genitourinary tract
infections.
Pharmacodynamics - Cephalexin (also called Cefalexin) is a first-generation cephalosporin antibiotic. It is one of the most
widely prescribed antibiotics, often used for the treatment of superficial infections that result as complications of minor
wounds or lacerations. It is effective against most gram-positive bacteria through its inhibition of the cross-linking
reaction between N-acetyl muramic acid and N-acetylglucosamine in the cell wall, leading to cell lysis.
MOA - Cephalexin inhibits bacterial cell wall synthesis, leading breakdown and eventually cell death
Absorption - Well absorbed from the upper gastrointestinal tract with nearly 100% oral bioavailability. Cephalexin is not
absorbed in the stomach but is absorbed in the upper intestine.
Toxicity - Symptoms of overdose include blood in the urine, diarrhea, nausea, upper abdominal pain, and vomiting.
https://go.drugbank.com/drugs/DB00567
CEFADROXIL

Cefadroxil is a cephalosporin antibiotic used in the treatment of various bacterial infections, such as urinary tract
infections, skin and skin structure infections, and tonsillitis.
Generic Name – Cefadroxil
Background - Long-acting, broad-spectrum, water-soluble, cephalexin derivative
Indication - For the treatment of the following infections (skin, UTI, ENT) caused by; S. pneumoniae, H. influenzae,
staphylococci, S. pyogenes (group A beta-hemolytic streptococci), E. coli, P. mirabilis, Klebsiella sp, coagulase-negative
staphylococci and Streptococcus pyogenes
Pharmacodynamics - Cefadroxil, a first-generation cephalosporin antibiotic, is used to treat urinary tract infections, skin
and skin structure infections, pharyngitis, and tonsillitis.
MOA - Like all beta-lactam antibiotics, cefadroxil 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; it is possible that cefadroxil interferes with an
autolysin inhibitor.
Absorption - Cefadroxil is well absorbed on oral administration; food does not interfere with its absorption.
Toxicity - Nausea, vomiting, diarrhoea, allergic rashes may occur

https://go.drugbank.com/drugs/DB01140

CEPHRADINE

Cefradine is a first-generation cephalosporin antibiotic used in the treatment of bacterial infections of the respiratory and
urinary tracts and of the skin and soft tissues.
Generic Name – Cefradine
Brand name - Zepdril
Background - A semi-synthetic cephalosporin antibiotic.
MOA - Cefradine is a first generation cephalosporin antibiotic with a spectrum of activity similar to Cefalexin. Cefradine,
like the penicillins, is a beta-lactam antibiotic. 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; it is possible that Cefradine interferes with an autolysin inhibitor.
https://go.drugbank.com/drugs/DB01333

CEFAZOLIN
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.
Generic Name – Cefazolin BRAND NAME - Fazef
Background - A semisynthetic cephalosporin analog with broad-spectrum antibiotic action due to inhibition of bacterial
cell wall synthesis. It attains high serum levels and is excreted quickly via the urine.
Indication - Mainly used to treat bacterial infections of the skin. It can also be used to treat moderately severe bacterial
infections involving the lung, bone, joint, stomach, blood, heart valve, and urinary tract. It is clinically effective against
infections caused by staphylococci and streptococci species of Gram-positive bacteria. May be used for surgical
prophylaxis; if required metronidazole may be added to cover B. fragilis.
Pharmacodynamics - Cefazolin (also known as cefazoline or cephazolin) is a semi-synthetic first generation cephalosporin
for parenteral administration. Cefazolin has broad-spectrum antibiotic action due to inhibition of bacterial cell wall
synthesis. It attains high serum levels and is excreted quickly via the urine.
MOA - In vitro tests demonstrate that the bactericidal action of cephalosporins results from inhibition of cell wall
synthesis. 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
Absorption - Not absorbed from GI tract. Must be administered parenterally. Peak serum concentrations attained 1-2 hours
post intramuscular injection.
https://go.drugbank.com/drugs/DB01327
CEFACLOR

Cefaclor is a second generation cephalosporin used to treat a wide variety of infections in the body.
Generic Name – Cefaclor brandname - ceflor
Background - Semisynthetic, broad-spectrum antibiotic derivative of cephalexin.
Indication - For the treatment of certain infections caused by bacteria such as pneumonia and ear, lung, skin, throat, and
urinary tract infections.
Pharmacodynamics - Cefaclor is a second generation cephalosporin antibiotic with a spectrum resembling first-generation
cephalosporins. In vitro tests demonstrate that the bactericidal action of the cephalosporins results from inhibition of cell-
wall synthesis. As indicated by in vitro and in vivo clinical studies, cefaclor was shown to be effective against most strains
of Gram positive aerobes - Staphylococci (including coagulase-positive, coagulase-negative, and penicillinase-producing
strains), Streptococcus pneumoniae, Streptococcus pyogenes (group A ß-hemolytic streptococci), as well as Gram-
negative aerobes - Escherichia coli, Haemophilus influenzae (including ß-lactamase-producing ampicillin-resistant
strains), Klebsiella sp, and Proteus mirabilis.
MOA - Cefaclor, like the penicillins, is a beta-lactam antibiotic. 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. It is possible that cefaclor interferes with an
autolysin inhibitor.
Absorption - Well absorbed after oral administration, independent of food intake.
Toxicity - Symptoms of overdose include diarrhea, nausea, stomach upset, and vomiting.
https://go.drugbank.com/drugs/DB00833

CEFPROZIL

Cefprozil is a cephalosporin antibiotic used in the treatment of various bacterial infections, such as pharyngitis, tonsillitis,
otitis media, and uncomplicated skin infections.
Generic Name – Cefprozil
Background - Cefprozil is a cephalosporin antibiotic that is commonly employed to treat a variety of bacterial infections,
including those of the ear and skin, bronchitis, and others.
Indication
For the treatment of the following infections (respiratory, skin, soft tissue, UTI, ENT) caused by; S. pneumoniae, H.
influenzae, staphylococci, S. pyogenes (group A beta-hemolytic streptococci), E. coli, P. mirabilis, Klebsiella sp,
coagulase-negative staph
Pharmacodynamics
Cefprozil, a semisynthetic, second-generation cephalosporin, is used to treat otitis media, soft-tissue infections, and
respiratory tract infections.
MOA - Cefprozil, like the penicillins, is a beta-lactam antibiotic. 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; it is possible that cefprozil interferes with an
autolysin inhibitor.
Absorption - Oral bioavailability is approximately 95%
Toxicity - Single 5000 mg/kg oral doses of cefprozil caused no mortality or signs of toxicity in adult, weaning or neonatal
rats, or adult mice. A single oral dose of 3000 mg/kg caused diarrhea and loss of appetite in cynomolgus monkeys, but no
mortality.
https://go.drugbank.com/drugs/DB01150

CEFOTETAN

Cefotetan is an antibiotic medication used for the prophylaxis and treatment of various bacterial infections, including
urinary tract infections, bone and joint infection, and lower respiratory tract infections.
Generic Name - Cefotetan
Background - A semisynthetic cephamycin antibiotic that is administered intravenously or intramuscularly. The drug is
highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of both aerobic and anaerobic
gram-positive and gram-negative microorganisms.
Indication - For prophylaxis and treatment of bacterial infections.
Pharmacodynamics - Cefotetan is a semisynthetic cephamycin antibiotic that is administered intravenously or
intramuscularly. The drug is highly resistant to a broad spectrum of beta-lactamases and is active against a wide range of
both aerobic and anaerobic gram-positive and gram-negative microorganisms.
Mechanism of action - The bactericidal action of cefotetan results from inhibition of cell wall synthesis by binding and
inhibiting the bacterial penicillin binding proteins which help in the cell wall biosynthesis.

https://go.drugbank.com/drugs/DB01330

CEFOXITIN

Cefoxitin is a semi-synthetic, broad-spectrum antibiotic for parenteral administration used for the treatment of serious
bacterial infections, such as urinary tract infection, blood infection, bone and joint infection, and lower respiratory tract
infection.
Generic Name – Cefoxitin
Background - Cefoxitin is a semi-synthetic, broad-spectrum cepha antibiotic for intravenous administration. It is derived
from cephamycin C, which is produced by Streptomyces lactamdurans.
Indication - For the treatment of serious infections caused by susceptible strains microorganisms
Pharmacodynamics - Cefoxitin is a cephamycin antibiotic often grouped with the second-generation cephalosporins. It is
active against a broad range of gram-negative bacteria including anaerobes. The methoxy group in the 7a position
provides cefoxitin with a high degree of stability in the presence of beta-lactamases, both penicillinases and
cephalosporinases, of gram-negative bacteria
Mechanism of action - The bactericidal action of cefoxitin results from inhibition of cell wall synthesis.
Toxicity - The acute intravenous LD50 in the adult female mouse and rabbit was about 8.0 g/kg and greater than 1.0 g/kg,
respectively. The acute intraperitoneal LD50 in the adult rat was greater than 10.0 g/kg.
https://go.drugbank.com/drugs/DB01331

Cefuroxime

Cefuroxime is a cephalosporin indicated for the treatment of a variety of infections including acute bacterial otitis media,
several upper respiratory tract infections, skin infections, urinary tract infections, gonorrhea, early Lyme disease, and
impetigo.
Generic Name - Cefuroxime
Background - Broad-spectrum cephalosporin antibiotic resistant to beta-lactamase. It has been proposed for infections
with gram-negative and gram-positive organisms, gonorrhea, and haemophilus.
Indication - For the treatment of many different types of bacterial infections such as bronchitis, sinusitis, tonsillitis, ear
infections, skin infections, gonorrhea, and urinary tract infections.
Pharmacodynamics - Cefuroxime is a β-lactam type antibiotic. More specifically, it is a second-generation cephalosporin.
Cephalosporins work the same way as penicillins: they interfere with the peptidoglycan synthesis of the bacterial wall by
inhibiting the final transpeptidation needed for the cross-links. This effect is bactericidal. Cefuroxime is effective against
the following organisms: Aerobic Gram-positive Microorganisms: Staphylococcus aureus, Streptococcus
pneumoniae, Streptococcus pyogenes. Aerobic Gram-negative Microorganisms: Escherichia coli, Haemophilus
influenzae (including beta-lactamase-producing strains), Haemophilus parainfluenzae, Klebsiella pneumoniae, Moraxella
catarrhalis (including beta-lactamase-producing strains), Neisseria gonorrhoeae (including beta-lactamase-producing
strains). Spirochetes: Borrelia burgdorferi. Cefuroxime axetil is the prodrug
MOA - Cefuroxime, like the penicillins, is a beta-lactam antibiotic. 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; it is possible that cefuroxime interferes with an
autolysin inhibitor.
Absorption - Absorbed from the gastrointestinal tract. Absorption is greater when taken after food (absolute bioavailability
increases from 37% to 52%).
Toxicity - Allergic reactions might be expected, including rash, nasal congestion, cough, dry throat, eye irritation, or
anaphylactic shock. Overdosage of cephalosporins can cause cerebral irritation leading to convulsions
https://go.drugbank.com/drugs/DB01112