CH3 | Protein Synthesis Inhibitors (Chloramphenicol) Flashcards
What is the chemotherapeutic spectrum of chloramephenicol?
It is a broad-spectrum antibiotic. It is restricted to life-threatening infections for which no other alternatives exist.
It is bacteriostatic, but it may exert bactericidal activity depending on the dose and organism.
What is the mechanism of action (MOA) of Chloramphenicol?
Chloramphenicol reversibly binds to the bacterial 50S ribosomal subunit and inhibits peptidyl transferase.
What effect does Chloramphenicol have on mammalian mitochondrial ribosomes?
Chloramphenicol can inhibit protein and ATP synthesis at high concentrations (resulting in bone marrow toxicity).
What is a potential side effect of high concentrations of Chloramphenicol?
Bone marrow toxicity.
Which types of organisms is Chloramphenicol effective against?
Chlamydiae, rickettsiae, spirochetes, anaerobes, aerobic and anaerobic gram-positive and gram-negative organisms.
What are the resistance mechanisms to Chloramphenicol?
Enzymatic inactivation, decreased ability to penetrate the organism, or alterations in the ribosomal binding site.
How is Chloramphenicol distributed in the body?
Widely distributed throughout the body and in the CSF.
What is the route of administration for Chloramphenicol?
Administered IV.
What happens to Chloramphenicol in the liver?
It undergoes hepatic metabolism to form an inactive glucuronide metabolite, which is then eliminated in the urine.
How is the inactive glucuronide metabolite of Chloramphenicol eliminated?
Eliminated in urine.
Is Chloramphenicol secreted in breast milk?
Yes, it is secreted in breast milk.
What are the dose-related adverse effects of Chloramphenicol?
Dose-related anemia, hemolytic anemia (in G6PD deficiency), and aplastic anemia.
What is Gray Baby Syndrome associated with Chloramphenicol?
Neonates have low capacity to glucuronidate the drug and underdeveloped renal function, leading to accumulation and interference with mitochondrial ribosomes.
What symptoms can result from Gray Baby Syndrome due to Chloramphenicol?
Poor feeding, depressed breathing, cardiovascular collapse, cyanosis, and death.
Can adults experience effects similar to Gray Baby Syndrome when taking Chloramphenicol?
Yes, adults taking high doses may experience similar effects.