CHLORAMPHENICOL

By. •
Dr. shahid Ali •
Lecturer pharmacology •
 CHLORAMPHENICOL
Mechanism of action
Inhibits protein synthesis ( 50 s subunit )
By inhibiting peptidyl transferase
enzyme
Inhibits protein synthesis in
mitochondria of bacteria as well as
mammals
 Antibacterial activity

Gram +ve •
Gram –ve •
S. typhi •
N. Meningitidis E. coli •
S. Pneumoniae V.cholera •
Ricketsiae Anaerobes- •
clostridium &
B. fragilis •
 Chloramphenicol ( cont. )
Pharmacokinetics
Rapidly & completely absorb

Lipophilic nature can cross BBB and placenta

Metabolized by liver – glucuronidation
Well distributed, including CNS and CSF

Excreted in urine
Tubular secretion 80%
Glomerular filtration 10%
 Resistance
Plasmid mediated inactivation of
drug by acetyl transferase enzyme
Decrease permeability
 Unchanged Glomerular
8%
Filtration
90%
Chloramphenicol Glucuronide Tubular
Secretion
2% Deacetylation &
Dehalogenation

Metabolism

Excretion
 Chloramphenicol Cont. )
Clinical uses
Limited because of potential toxicities
(a plastic anaemia &circulatory collapse in
neonates)
1. Typhoid fever- s. typhi ( quinolones are preffered)
2. Meningitis – H.influenzae,N.meningitidis,S.pneumoniae
( Ceftriaxone is preffered )
3. Anaerobic infections- B. fragilis
(Metronidazole is the drug of
choice)
4. Rickettsial infections – Doxycycline is preffered
5. Bacterial conjunctivitis ( topical )
 Chloramphenicol ( cont. )
Side effects
Hypersensitivity- low incidence
May ppt hemolysis in G6PD deficient pts

GI UPSET : Irritation to GI mucosa can occur

superinfection to candida albicans can occur on
mucosa .
 BONE MARROW
DEPRESSION
Chloramphenicol can cause decrease •
maturation of red blood cell
Aplastic anemia a rare complication can •
occur it is irreversible
 GRAY BABY SYNDROME
Develop specially in neonates •
Neonates have premature liver •
Can not metabolize drug completely •
Due to deficiency of enzyme •
glucoronyltransferase
Depressed breathing cardiac collapse can •
cause cynosis
Hence term used as gray baby syndrome •
 BLOOD LEVEL OF THESE
DRUGS CAN RISE
Interaction with other drugs :
Inhibits liver microsomal enzymes
Phenytoin
Tolbutamide
Chlorpropamide
Anticoagulants