CEBENICOL

An antibiotic first isolated from cultures of Streptomyces venezuelae in 1947 but now produced synthetically.

It has a relatively simple structure and was the first broad-spectrum antibiotic to be discovered.

It acts by interfering with bacterial protein synthesis and is mainly bacteriostatic. (From Martindale, The Extra Pharmacopoeia, 29th ed, p106) The FDA has withdrawn all oral drug products containing chloramphenicol, due to the high risk of fatal aplastic anemia associated with this specific route of administration. 6, 7.

Used in treatment of cholera, as it destroys the vibrios and decreases the diarrhea.

It is effective against tetracycline-resistant vibrios.

It is also used in eye drops or ointment to treat bacterial conjunctivitis.

Chloramphenicol is a broad-spectrum antibiotic that was derived from the bacterium Streptomyces venezuelae and is now produced synthetically.

Chloramphenicol is effective against a wide variety of microorganisms, but due to serious side-effects (e.g., damage to the bone marrow, including aplastic anemia) in humans, it is usually reserved for the treatment of serious and life-threatening infections (e.g., typhoid fever).

Chloramphenicol is bacteriostatic but may be bactericidal in high concentrations or when used against highly susceptible organisms.

Chloramphenicol stops bacterial growth by binding to the bacterial ribosome (blocking peptidyl transferase) and inhibiting protein synthesis.

Large ribosomal subunit protein uL16 (Escherichia coli (strain K12)) Inhibitor.

Rapidly and completely absorbed from gastrointestinal tract following oral administration (bioavailability 80%).

Well absorbed following intramuscular administration (bioavailability 70%).

Intraocular and some systemic absorption also occurs after topical application to the eye.

Hepatic, with 90% conjugated to inactive glucuronide.

in adults with normal hepatic and renal function is 1.5-3.5 hours.

In patients with impaired renal function half-life is 3-4 hours.

In patients with severely impaired hepatic function half-life is 4.6-11.6 hours.

Half-life in children 1 month to 16 years old is 3-6.5 hours, while half-life in infants 1-2 days old is 24 hours or longer and is highly variable, especially in low birth-weight infants.

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Oral, mouse: LD 50 = 1500 mg/kg; Oral, rat: LD 50 = 2500 mg/kg. Toxic reactions including fatalities have occurred in the premature and newborn; the signs and symptoms associated with these reactions have been referred to as the gray syndrome.

Symptoms include (in order of appearance) abdominal distension with or without emesis, progressive pallid cyanosis, vasomotor collapse frequently accompanied by irregular respiration, and death within a few hours of onset of these symptoms.

Chloramphenicol is contraindicated in individuals with a history of previous hypersensitivity and/or toxic reaction to it.

It must not be used in the treatment of trivial infections or where it is not indicated, as in colds, influenza, infections of the throat; or as a prophylactic agent to prevent bacterial infections.

Chloramphenicol Sodium Succinate for

Injection, USP is freeze-dried in the vial.

When reconstituted as directed, each vial contains a sterile solution equivalent to 100 mg of chloramphenicol per mL (1 g/10 mL).

No. 1115 63323-011-15 Available in packages of 10 vials.

Store at 20° to 25°C (68° to 77°F) .

C – Animal reproduction studies have not been conducted with chloramphenicol.

There are no adequate and well-controlled studies to establish safety of this drug in pregnancy.

It is not known whether chloramphenicol can cause fetal harm when administered to a pregnant woman.

Orally administered chloramphenicol has been shown to cross the placental barrier.

Because of potential toxic effects on the fetus See ADVERSE REACTIONS, “Gray Syndrome”, chloramphenicol should be given to a pregnant woman only if the potential benefit justifies the potential risk to the fetus.

Chloramphenicol is excreted in human milk following oral administration of the drug.

Because of the potential for serious adverse reactions in nursing infants from chloramphenicol, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother See ADVERSE REACTIONS, “Gray Syndrome”.

Precaution should be used in therapy of premature and full-term neonates and infants to avoid “gray syndrome” toxicity.

Due to immature metabolic processes in the neonate and infant, excessive blood levels may result from administration of the recommended dose.

The dosage should be adjusted accordingly or, preferable, the blood concentration should be determined at appropriate intervals See ADVERSE REACTIONS, "Gray Syndrome".

ADMINISTRATION for dosing information in the pediatric population.

Clinical studies of chloramphenicol sodium succinate did not include sufficient numbers of subjects aged and over to determine whether they respond differently from younger subjects.

Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

This drug is known to be substantially excreted by the kidney, and the risk of toxic reactions to this drug may be greater in patients with impaired renal function.

Because elderly patients are more likely to have decreased renal function, care should be taken in dose selection, and it may be useful to monitor renal function.

Each gram (10 mL of a 10% solution) of chloramphenicol sodium succinate contains approximately 52 mg (2.25 mEq) of sodium.