
Chemical
nameD - threo - (-) - 2, 2
- Dichloro - N - (P - hydroxy - a - (hydroxymethyl) - p - nitrophenethyl]
acetamide.
CategoryAntibacterial (systemic).
Mechanism of
action
Chloramphenicol, a broad - spectrum antibiotic, is
bacteriostatic. However, it may be bactericidal in high concentrations
or when used against highly susceptible organisms. Chloramphenicol,
which is lipid soluble, diffuses through the bacterial cell membrane and
reversibly binds to the 50 S subunit of bacterial ribosomes where transfer
of amino acids to growing peptide chains is prevented (perhaps by
suppression of peptidyl transferase activity), thus inhibiting peptide
bond formation and subsequent protein synthesis.
Indications
Chloramphenicol should be reserved for serious infections
in which less toxic antibacterials are ineffective or
contraindicated. Treatment: Brain abscess - Ehrlichiosis - Meningitis -
Paratyphoid fever - Q fever - Rocky mountain spotted fever - Typhoid fever
- Typhus infections.
Precautions to
consider
Risk - benefit should be considered when the following
medical problems exist: Bone marrow depression (chloramphenicol may
cause a dose - related bone marrow depression, an idiosyncratic aplastic
anemia, and other blood dyscrasias) - Hepatic or renal function
impairment. ln patients who have had previous cytotoxic drug therapy or
radiation therapy also.
Pregnancy / Breast -
feeding
Chloramphenicol readily crosses the placenta; fetal serum
concentrations may be 30 to 80% of maternaI serum
concentrations. Although birth defects in humans have not been
documented, use is not recommended in pregnancy at term or during labor
because of potential toxicity ("gray syndrome" or bone marrow depression)
in premature or full term infants. Chloramphenicol is excreted in
breast milk in concentrations up to 25 mcg per mL. Use is not recommended
in nursing mothers because of the possibility of adverse effects,
especially bone marrow depression, in the infant.
Drug
interactions
Combinations containing any of the following
medications,depending on the amount present, may also interact with this
medication: Alfentanil - Anticonvulsants, hydantoin - Bone marrow
depressants - Radiation therapy -Antidiabetic agents - Contraceptives,
estrogen containing, oral - Clindamycin - Erythromycins - Lincomycin -
Hepatic enzyme inducers - Penicillins - Phenobarbital - Phenytoin -
Warfarin - Other medications metabolized by mixed function oxidase system
- Vitamin B12.
Side / Adverse
effects
Aplastic anemia is an idiosyncratic reaction that occurs
in 1 of every 25,000 to 40,000 courses of treatment. Those indicating
need for medical attention: Incidence less frequent: Blood
dyscrasias. Incidence rare: Gray syndrome, hypersensitivity reactions,
neurotoxic reactions, optic neuritis, peripheral neuritis.
Administration and
dosage
Capsules and oral suspension: Usual adult and adolescent
dose: Antibacterial - Oral, 12.5 mg (base) per kg of body weight every
6 hours. Usual adult prescribing limits: Up to maximum of 4 grams
(base) daily. Usual pediatric dose: Antibacterial - Premature and full
- term infants up to 2 weeks of age: Oral, 6.25 mg (base) per kg of body
weight every 6 hours. Infants 2 weeks of age and over: Oral, 12.5 mg
(base) per kg of body weight every 6 hours; or 25 mg per kg of body weight
every 12 hours.
How
supplied150 mg (base) / 5
mL, bottles of 60 mL. Oral suspension contains saccharin acid as
sweetener.
StorageCapsules: Store below 30° C, protect from
direct light and moisture. Oral suspension: Store below 30° C, protect
from light and freezing.
References1 - USP Dl Vol: 1 (1997) - Pages: 791 -
794. 2 - Drug facts and comparisons (1994). 3 - USP 23 page: 332.
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