Description
- Amphenicols
- Broad spectrum antibiotics
- Bacteriostatic
- Include
- Chloramphenicol
- Thiamphenicol
- Florfenicol
• Chloramphenicol
• Mechanism of Action
• Antimicrobial Spectrum
• Pharmacokinetics
• Side effects/Adverse effects
• Administration and fate of Chloramphenicol
• Contraindications/Precautions
• Drug interactions
- Inhibits hepatic microsomal enzymes
Should not be given with beta-lactam and aminoglycoside antibiotics
• Clinical Uses
Chronic respiratory infections
Otitis externa
Typhoid in humans
Brucellosis
Bacterial meningitis
Amphenicols
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Broad spectrum antibiotics
Bacteriostatic
Include
Chloramphenicol
Thiamphenicol
Florfenicol
Chloramphenicol
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Chloramphenicol
First broadspectrum antibiotic
Bacteriostatic antibiotic
Obtained from Streptomyces venezuelae in 1947
Now manufactured synthetically
Best against anaerobic bacteria
Properties
Highly lipid soluble
Bacteriostatic
Mechanism of Action
Inhibits protein synthesis in susceptible microorganisms
Readily penetrates in bacterial cells
Inhibits bacterial peptidyltransferase
The drug binds to the bacterial 50S ribosomal subunit
and inhibits protein synthesis at the peptidyl transferase
reaction
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Mechanism of action of Chloramphenicol
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Antimicrobial Spectrum
Broad-spectrum antibiotic
Active against staphylococcus, streptococcus,
salmonella, brucella, shigella, neisseria, haemophilus,
mycoplasma, rickettsia, chlamydiae etc
Pseudomonas aeruginosa is not affected
Excellent activity against anaerobes
The drug is either bactericidal or (more commonly)
bacteriostatic, depending on the organism
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Pharmacokinetics
Highly lipid soluble
Efficiently absorbed via orally
Peak plasma conc. in 30 minutes PO
Distributed in most tissues and fluids like CSF, brain,
aqueous humour, placenta, synovial fluid
Eliminated via hepatic metabolism
Inhibit hepatic microsomal enzymes
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Administration and fate of Chloramphenicol
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Side effects/Adverse effects
Bone marrow depression
Reversible dose-dependent
Irreversible dose-independent, aplastic anemia
(Idiosyncratic)
Gray Baby Syndrome: In neonates. Drug accumulation interference with the
function of mitochondrial ribosomes
Gastrointestinal effects
Cardiovascular effects
Hypersensitive reactions
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Contraindications/Precautions
In hypersensitive patients
In hepatic and renal insufficiency
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Drug interactions
Inhibits hepatic microsomal enzymes
Should not be given with beta-lactam and
aminoglycoside antibiotics
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Inhibition of the cytochrome P450 system by chloramphenicol
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Clinical Uses
Chronic respiratory infections
Otitis externa
Typhoid in humans
Brucellosis
Bacterial meningitis
- Subject:- Pharmacology 3
- Course:- B.pharm (pharmacy),
- Semester:- 6th sem , sem :- 6
