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Chloramphenicol

Antimicrobial Agents
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chloramphenicol palmitate (limited availability)

chloramphenicol sodium sumlinate

Brands

Chloromycetin Kapseals (chloramphenicol)

Chloromycetin Sodium Sumlinate (powder for injection)

Availability

Tablets: 100 mg, 250 mg & 500 mg chloramphenicol

Capsules: 250 mg Chloromycetin Kapseals

Injectable: 1 gram vial (100 mg/mL) Chloromycetin Sodium Sumlinate

Pharmacology

Chloramphenicol is a broad-spectrum antibiotic that acts as a bacteriostatic, but at higher concentrations can act as a bactericidal. It binds to the 50S ribosomal subunit of susceptible bacteria and prevents bacterial protein synthesis. It has activity against many Gram-negative and Gram-positive organisms. It has also shown activity against Mycoplasma.

Chlormaphenicol is rapidly absorbed following oral administration and widely distributed throughout the body, including the central nervous system, where it is able to cross the blood-brain barrier. While highest levels are found in the liver and kidney the drug tends to remain at therapeutic levels in most tissues and fluids  27.

Chloramphenicol is metabolized in the liver and eliminated by glucuronidation. It is excreted by the kidneys with only a small fraction being excreted unchanged.

Though chloramphenicol is quite effective at getting into the tissues, being able to penetrate pus to get to the bacteria, it has a short half-life which requires more frequent dosing times.
It also has the potential to accumulate at toxic levels in the newborn, and very young, due to the inability to be effectively metabolized and eliminated from the body. It is, therefore, not recommended to be given to very young animals.
Chloramphenicol is also not recommended to be given in pregnant or lactating animals due to its ability to cross the placenta and passed in breast milk.

Indications

To treat serious infections due to organisms resistant to other less toxic antibiotics, or when its penetration into the site of infection is clinically superior to other antibiotics. Those bacteria sensitive to this drug include clostridium, chlamydia, mycoplasma, salmonella.

Drug Interactions or Contraindications

Chloramphenicol is contraindicated if another drug can be used instead due to its potential to cause bone marrow depression.

Not recommended for use with Tylan, azithromycin or erythromycin, as they may be antagonistic with chloramphenicol.

Acetaminophen will elevate chloramphenicol levels.

Chloramphenicol has the potential to antagonize bactericidal activity of the penicillins and aminoglycosides.

Rifampin may decrease serum chloramphenicol levels.

Adverse Reactions

Avoid using if impaired hepatic or kidney function is present. Prolonged use may result in suprainfections.

EENT:  optic neuritis

GI:  diarrhea, disturbance of intestinal flora

Hematologic:  irreversible idiosyncratic aplastic anemia (identified in humans), dose-related bone marrow suppression with long term therapy (reversible once drug stopped). Caution is advisable when combining the use of chloramphenicol with NSAIDs or Salicylates

Hepatic: jaundice

Other:  anaphylaxis

May falsely elevate urine glucose levels.

Dosage Recommendations

(Chloramphenicol palmitate) 25-90 mg/lb , PO, q8hrs   4

or

(Chloramphenicol sodium sumlinate) 15 mg/lb to 25 mg/lb , SQ or IM, BID for 7-14 days  4

or

(Chloramphenicol palmitate) 50 mg/kg to 200 mg/kg , PO , q8hrs   1  2

or

(Chloramphenicol sodium sumlinate) 30mg/kg to 50mg/kg , SQ or IM , q12hrs   1  11

Considerations

  • Do not use for trivial infections; can be highly toxic.
  • Medication can be very bitter tasting. Mix with something sweet.
  • Due to its potential for toxicity avoid inhaling the powder when having to compound or mix this drug, and wash hands immediately following direct skin contact. Wearing gloves is advised.
  • Store capsules and tablets in tight container, away from light, at room temperature.

Posted on June 23, 2003, 14:30, Last updated on December 17, 2016, 19:00 | Antimicrobial Agents



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