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chloramphenicol; levomycetin; chloranfenicol; kloramfenikol (Chloromycetin, Chloroptic)
Topical agent: Tradename: Chloromycetin. Ophthalmic agent: Tradename: Chloroptic.
Indications:
1) systemic agent
a) meningitis when other agents are contraindicated
b) serious infections when other agents are inadequate or contraindicated
- gastrointestinal infections
- typhoid fever, paratyphoid fever
- postoperative infections [7]
- boutonneuse fever
- inhalation anthrax
- rickettsia infections
c) antibiotic prophylaxis during mastoidectomy
2) ophthalmic agent
a) treatment of eye infection including:
- E coli, H influenzae, M lacunata, Staphylococcus, Streptococcus, Rickettsia, Chlamydia, Mycoplasma
b) keratitis, keratoconjunctivitis
c) blepharoconjunctivitis & eyelid diseases
3) otic agent: otitis externa
Contraindications:
Caution:
1) patients with renal or hepatic impairment
2) neonates
Dosage:
1) systemic
a) meningitis: 75-100 mg/kg/day divided every 6 hours
b) other infections
- adults: 50 mg/kg/day divided every 6 hours, max: 4 g/day
- children: 50-75 mg/kg/day divided every 6 hours, max: 4 g/day
2) ophthalmic -0.5% & 1% ointment every 3-4 hours or BID-QID
Injection: sodium succinate 100 mg/mL Suspension, oral, as palmitate: 150 mg/5 mL (60 mL)
Monitor:
Therapeutic drug monitoring: Therapeutic range:
- Peak: 10-25 ug/mL
- Trough < 5 ug/mL
Antimicrobial activity:
Gram positive
- Streptococcus
- Streptococcus group A
- Streptococcus group B
- Streptococcus group C
- Streptococcus group G
- Streptococcus pneumonia
- Staphylococcus aureus (MSSA) (+/-)
Gram negative
- Neisseria gonorrhoeae
- Neisseria meningitidis [7]
- Moraxella catarrhalis
- Haemophilus influenzae
- Aeromonas
- Escherichia coli
- Klebsiella species (+/-)
- Proteus vulgaris (+/-)
- Pseudomonas cepacia
- Xanthomonas maltophilia
- Yersinia enterocolitica
- Francisella tularensis
- Brucella species
- Haemophilus ducreyi
- Vibrio vulnificus
Atypical bacteria
- Chlamydia species
- Mycoplasma pneumonia
- Rickettsia
Anaerobes
- Actinomyces
- Bacteroides fragilis
- Bacteroides melaninogenicus
- Clostridium difficile (+/-)
- Clostridium species
Adverse effects:
- uncommon (< 1%)
1) the most common offending agent in drug-induced pancytopenia
2) optic neuritis, peripheral neuropathy, nightmares, headache, rash, diarrhea, stomatitis, enterocolitis, gray baby syndrome, bone marrow suppression, aplastic anemia, nausea/vomiting
3) ocular irritation with ophthalmic agent
Drug interactions:
1) chloramphenicol inhibits metabolism of:
a) chlorpropamide
b) phenytoin
c) warfarin
2) phenobarbital & rifampin may decrease serum levels of chloramphenicol
Laboratory:
1) specimen:
a) serum, plasma (heparin, EDTA)
b) collect at trough concentration
c) centrifuge & separate from cells if not assayed immediately
2) methods: HPLC, GLC, MB, color, EIA
3) interferences: colorimetric assays may not distinguish between biologically active & inactive forms of chloramphenicol
Mechanism of action:
1) inhibits protein synthesis in bacteria & to a lesser extent in eukaryotic cells
2) acts primarily by binding reversibly to the 50S ribosomal subunit
3) can also inhibit mitochondrial protein synthesis in mammalian cells
4) mammalian erythropoietic cells appear to be particularly sensitive to chloramphenicol
Interactions
drug interactions
Related
chloramphenicol in serum/plasma
Specific
Chloramphenicol Ophthalmic; Chloromycetin Ophthalmic
General
alcohol
amide
antibacterial agent
Properties
MISC-INFO: elimination route LIVER
KIDNEY
1/2life 2-3 HOURS
12 HOURS <2-3 weeks of age>
24 HOURS <<2 weeks of age>
therapeutic-range 10-25 UG/ML
<5 UG/ML
toxic-range >25 UG/ML
protein-binding 50-60%
elimination by hemodialysis +/-
peritoneal dialysis -
pregnancy-category C
safety in lactation -
?
Database Correlations
PUBCHEM correlations
References
- The Pharmacological Basis of Therapeutics, 8th ed.
Gilman et al, eds. Permagon Press/McGraw Hill pg 1125
- The Pharmacological Basis of Therapeutics, 9th ed.
Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- Sanford Guide to antimicrobial therapy 1997
- Drug Information & Medication Formulary, Veterans Affairs,
Central California Health Care System, 1st ed., Ravnan et al
eds, 1998
- Kaiser Permanente Northern California Regional Drug
Formulary, 1998
- Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed.,
W.B. Saunders, 1995
- Deprecated Reference