Chloramphenicol hemisuccinate
Chloramphenicol hemisuccinate Uses, Dosage, Side Effects, Food Interaction and all others data.
Chloramphenicol hemisuccinate is an ester prodrug of chloramphenicol. Chloramphenicol is a bacteriostatic antibiotic. Use of chloramphenicol succinate and chloramphenicol has decreased due to the risk of potentially fatal blood dyscrasias.
Chloramphenicol hemisuccinate was granted FDA approval on 20 February 1959.
Chloramphenicol hemisuccinate is a prodrug of chloramphenicol, which binds to bacterial ribosomes and prevents translation. It has a narrow therapeutic index and a moderate duration of action. Patients should be counselled regarding the risk of serious fatal blood dyscrasias.
Trade Name | Chloramphenicol hemisuccinate |
Generic | Chloramphenicol succinate |
Chloramphenicol succinate Other Names | Chloramphenicol hemisuccinate |
Type | |
Formula | C15H16Cl2N2O8 |
Weight | Average: 423.202 Monoisotopic: 422.028370912 |
Protein binding | Chloramphenicol succinate is 57-92% protein bound in plasma. |
Groups | Approved |
Therapeutic Class | |
Manufacturer | |
Available Country | |
Last Updated: | September 19, 2023 at 7:00 am |
Uses
Chloramphenicol hemisuccinate is a broad-spectrum antibiotic agent used for the treatment of acute and severe infections caused by susceptible bacterial strains.
Chloramphenicol hemisuccinate is indicated to treat serious and susceptible bacterial infections where less dangerous drugs are ineffective or contraindicated.
Chloramphenicol hemisuccinate is also used to associated treatment for these conditions: Acute infection caused by Salmonella typhi, Salmonella Typhi Infection, Serious Bacterial Infection
How Chloramphenicol hemisuccinate works
Chloramphenicol hemisuccinate is hydrolyzed into the active chloramphenicol. Chloramphenicol resembles uridine-5'-phosphate. It binds to the residues A2451 and A2452 in the 23S rRNA of the 50S ribosomal subunit of E. coli, which prevents translation.
Toxicity
Patients experiencing an overdose may present with shock, cyanosis, and coma. Treat patients with symptomatic and supportive measures which may include administration of fluids, exchange transfusions, and administration of dopamine.
Food Interaction
No interactions found.Volume of Distribution
Chloramphenicol hemisuccinate has a volume of distribution of 0.2-3.1L/kg.
Elimination Route
Chloramphenicol hemisuccinate has a high degree of interpatient variability, with a Tmax of 18 minutes to 3 hours. A 1g oral chloramphenicol succinate dose every 6-8 hours reaches a mean Cmax of 11.2µg/mL with a Tmax of 1 hour.
Half Life
The half life of chloramphenicol succinate in patients with normal renal and hepatic function is 0.6-2.7h.
Clearance
Chloramphenicol hemisuccinate's total clearance is 530-540mL/min in patients with normal renal and hepatic function, and 354mL/min in patients with renal or hepatic dysfunction. Chloramphenicol hemisuccinate's renal clearance is 222-260mL/min in patients with normal renal and hepatic function, and 66mL/min in patients with renal or hepatic dysfunction.
Elimination Route
6-80% of chloramphenicol succinate is eliminated unchanged in the urine, though this is highly variable between patients. On average, 30% of chloramphenicol succinate is eliminated unchanged in the urine and 10% is eliminated as the active chloramphenicol in the urine.
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