CH3 | Protein Synthesis Inhibitors (Chloramphenicol) Flashcards

1
Q

What is the chemotherapeutic spectrum of chloramephenicol?

A

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.

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2
Q

What is the mechanism of action (MOA) of Chloramphenicol?

A

Chloramphenicol reversibly binds to the bacterial 50S ribosomal subunit and inhibits peptidyl transferase.

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3
Q

What effect does Chloramphenicol have on mammalian mitochondrial ribosomes?

A

Chloramphenicol can inhibit protein and ATP synthesis at high concentrations (resulting in bone marrow toxicity).

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4
Q

What is a potential side effect of high concentrations of Chloramphenicol?

A

Bone marrow toxicity.

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5
Q

Which types of organisms is Chloramphenicol effective against?

A

Chlamydiae, rickettsiae, spirochetes, anaerobes, aerobic and anaerobic gram-positive and gram-negative organisms.

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6
Q

What are the resistance mechanisms to Chloramphenicol?

A

Enzymatic inactivation, decreased ability to penetrate the organism, or alterations in the ribosomal binding site.

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7
Q

How is Chloramphenicol distributed in the body?

A

Widely distributed throughout the body and in the CSF.

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8
Q

What is the route of administration for Chloramphenicol?

A

Administered IV.

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9
Q

What happens to Chloramphenicol in the liver?

A

It undergoes hepatic metabolism to form an inactive glucuronide metabolite, which is then eliminated in the urine.

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10
Q

How is the inactive glucuronide metabolite of Chloramphenicol eliminated?

A

Eliminated in urine.

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11
Q

Is Chloramphenicol secreted in breast milk?

A

Yes, it is secreted in breast milk.

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12
Q

What are the dose-related adverse effects of Chloramphenicol?

A

Dose-related anemia, hemolytic anemia (in G6PD deficiency), and aplastic anemia.

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13
Q

What is Gray Baby Syndrome associated with Chloramphenicol?

A

Neonates have low capacity to glucuronidate the drug and underdeveloped renal function, leading to accumulation and interference with mitochondrial ribosomes.

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14
Q

What symptoms can result from Gray Baby Syndrome due to Chloramphenicol?

A

Poor feeding, depressed breathing, cardiovascular collapse, cyanosis, and death.

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15
Q

Can adults experience effects similar to Gray Baby Syndrome when taking Chloramphenicol?

A

Yes, adults taking high doses may experience similar effects.

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16
Q

How does Chloramphenicol affect drug interactions?

A

It inhibits hepatic mixed-function oxidase, leading to the accumulation of warfarin and phenytoin.