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chloramphenicol (Chloramphenicol IV, Chloromycetin)

 

Classes: Antibiotics, Other

Dosing and uses of Chloramphenicol IV, Chloromycetin (chloramphenicol)

 

Adult dosage forms and strengths

injectable solution

  • 1000mg/vial

 

Serious Infections Caused by Susceptible Strains

50 mg/kg/day IV divided q6hr; in exceptional cases, patients with moderately resistant organisms or severe infections may require increased dosage up to 100 mg/kg/day; decrease these high doses as soon as possible

 

Other Indications & Uses

Use only as alternative for treatment of meningitis, typhoid, or rickettsial infection

 

Pediatric dosage forms and strengths

injectable solution

  • 1000mg/vial

 

Systemic Infections

Infants and children: As in adults; when adequate cerebrospinal fluid concentrations desired, may require up to 100 mg/kg/day; however, should reduce dose to 50 mg/kg/day as soon as possible

Infants and children with suspected immature metabolic functions: 25 mg/kg/day divided q6hr will usually produce therapeutic concentrations of the drug in the blood

 

Neonates (<28 Days Old)

Loading dose (LdD): 20 mg/kg IV once; give maintenance dose 12 hours after loading dose

Maintenance Dose

  • <7 days old: 25 mg/kg/day IV q24hr
  • >7 days old, <2000 g: 25 mg/kg/day IV q24hr
  • >7 days old, >2000 g: 50 mg/kg/day IV divided q12hr

 

Other Information

Peaks 10-20 mg/L, troughs 5-10 mg/L

 

Chloramphenicol IV, Chloromycetin (chloramphenicol) adverse (side) effects

<1%

Nightmares

Headache

Rash

Diarrhea

Stomatitis

Enterocolitis

Nausea

Vomiting

Bone marrow suppression

Aplastic anemia

Peripheral neuropathy

Optic neuritis

Gray syndrome

 

Warnings

Black box warnings

Serious and fatal blood dyscrasias, including aplastic anemia, hypoplastic anemia, thrombocytopenia, and granulocytopenia, have occurred after short-term and prolonged therapy

Monitor CBC frequently in all patients. Use only in serious infections

 

Contraindications

Hypersensitivity

Do not use oral or topical; not for use in trivial infections or for prophylaxis

Avoid during breastfeeding

 

Pregnancy and lactation

Pregnancy category: C

Lactation: enters breast milk; discontinue drug or do not nurse

 

Pregnancy categories

A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.

B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.

C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.

D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.

X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.

NA: Information not available.

 

Pharmacology of Chloramphenicol IV, Chloromycetin (chloramphenicol)

Distribution: to most tissues & body fluids; readily crosses placenta; enters breast milk CSF: blood level ratio: normal meninges: 66%; inflamed meninges: >66%

Protein Bound: 60%

 

Half-life Elimination

Normal renal function: 1.6-3.3 hr

End-stage renal disease: 3-7 hr

Cirrhosis: 10-12 hr

 

Excretion

Urine: 5-15%

Feces: 4%

 

Other Information

Metabolism: extensively hepatic (90%) to inactive metabolites, principally by glucuronidation; chloramphenicol palmitate is hydrolyzed by lipases in GI tract to the active base; chloramphenicol sodium succinate is hydrolyzed by esterases to active base

 

Mechanism of action

Inhibits bacterial protein synthesis by binding to 50S ribosomal subunit; mainly bacteriostatic

 

Administration

IV Incompatibilities

Additive: chlorpromazine, hydroxyzine, phenytion, polymyxin B sulfate, prochlorperazine, promethazine, vancomycin

Syringe: glycopyrrolate, metoclopramide

Y-site: fluconazole

 

IV Compatibilities

Solution: compatible with most common solvents

Additive (partial list): amikacin, aminophylline, ascorbic acid, CaCl2, Ca-gluconate, dimenhydrinate, dopamine, heparin, KCl, MgSO4, metronidazole, NaHCO3

Syringe: ampicillin, heparin, penicillin G sodium

Y-site: acyclovir, cyclophosphamide, enalaprilat, esmolol, foscarnet, hydromorphone, labetalol, MgSO4, meperidine, morphine, nicardipine, perphenazine, tacrolimus

 

IV Preparation

pH: 6.4-7.0

 

IV Administration:

Infuse via direct IV over 3-5 min; intermittent infusion over 30-60 min