Phenicols: Chloramphenicol & Florfenicol

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Questions and Answers

Which mechanism explains how phenicols inhibit protein synthesis in both eukaryotic and prokaryotic cells?

  • Preventing transpeptidation by binding to the 30S ribosomal subunit.
  • Interfering with tRNA binding to the ribosome.
  • Inhibiting mRNA transcription.
  • Preventing transpeptidation by binding to the 50S ribosomal subunit. (correct)

Why might dosage adjustments be necessary when administering phenicols to cats?

  • Cats have increased renal clearance of the drug.
  • Cats have a genetic deficiency in glucuronidase enzymes, leading to longer drug plasma half-lives. (correct)
  • Cats have decreased drug absorption in the gastrointestinal tract.
  • Cats have increased drug metabolism due to higher liver enzyme activity.

How do phenicols affect the duration of action of other drugs administered concurrently?

  • They shorten the duration of action by accelerating renal clearance.
  • They have no effect on the duration of action of other drugs.
  • They shorten the duration of action by inducing hepatic enzymes.
  • They prolong the duration of action by acting as non-competitive microsomal enzyme inhibitors. (correct)

Which of the following is the primary reason chloramphenicol is restricted in use in food-producing animals?

<p>It causes irreversible aplastic anemia in humans. (A)</p> Signup and view all the answers

What mechanisms do bacteria use to develop resistance to phenicols?

<p>Acetylation of the phenicol and decreased membrane permeability. (D)</p> Signup and view all the answers

What is the most likely consequence of administering chloramphenicol to a patient who is not properly vaccinated?

<p>Increased risk of secondary bacterial infections due to immunosuppression. (B)</p> Signup and view all the answers

What characteristic of distribution allows phenicols to be effective in treating infections of the central nervous system (CNS) and eye?

<p>Wide distribution to tissues, including the CNS and eye. (A)</p> Signup and view all the answers

A veterinarian needs to treat bovine respiratory disease in cattle. Which phenicol is most appropriate for this condition?

<p>Florfenicol (C)</p> Signup and view all the answers

What is the primary route of metabolism for phenicols in the body?

<p>Hepatic metabolism by glucuronide conjugation (B)</p> Signup and view all the answers

A laboratory test reveals that a bacterium is resistant to tetracycline, streptomycin, and ampicillin. What can be inferred about its potential resistance to chloramphenicol?

<p>It is likely to exhibit resistance to chloramphenicol, especially if resistance mechanisms are shared. (A)</p> Signup and view all the answers

In a non-ruminant animal treated with oral chloramphenicol, what is a potential adverse effect related to the gastrointestinal system?

<p>Gastrointestinal disturbances (D)</p> Signup and view all the answers

Which of the following is a characteristic action of chloramphenicol at low concentrations?

<p>Bacteriostatic (D)</p> Signup and view all the answers

Excluding food-producing animals, what types of infections can chloramphenicol treat?

<p>Both systemic and local infections caused by anaerobes and Salmonella spp. (A)</p> Signup and view all the answers

What is the spectrum of activity of chloramphenicol?

<p>Broad: effective against Gram-positive, Gram-negative, and many anaerobes (B)</p> Signup and view all the answers

Which of the following adverse effects relates to bone marrow suppression when administering chloramphenicol?

<p>Irreversible aplastic anemia (B)</p> Signup and view all the answers

A patient is diagnosed with a Salmonella infection. Which phenicol drug would be appropriate to treat this infection?

<p>Chloramphenicol (B)</p> Signup and view all the answers

How does acetylation contribute to bacterial resistance against phenicols?

<p>It prevents the phenicol from binding to the ribosome, thus inhibiting its mechanism of action. (B)</p> Signup and view all the answers

What is a characteristic that makes Florfenicol suitable for use in cattle?

<p>It effectively bovine respiratory disease. (A)</p> Signup and view all the answers

What is the implication of decreased membrane permeability in bacteria concerning phenicol antibiotics?

<p>Reduces drug's entry into bacterial cells. (A)</p> Signup and view all the answers

Which of the following describes the distribution of phenicols within the body after administration?

<p>Widely distributed to tissues including the CNS and eye. (D)</p> Signup and view all the answers

Flashcards

Phenicols mechanism of action

Binds to the 50S ribosomal subunit, inhibiting both eukaryotic and prokaryotic protein synthesis, preventing transpeptidation.

Phenicols administration and distribution

Rapidly absorbed in the gastrointestinal tract and widely distributed, including the CNS and eye.

Phenicols in cats

Cats have a genetic deficiency in glucuronidase enzymes, which leads to longer drug plasma half-lives; dosages need adjustment.

Phenicols metabolism

Extensive hepatic metabolism via glucuronide conjugation.

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Phenicols as enzyme inhibitors

Non-competitive microsomal enzyme inhibitors, prolonging the action duration of other drugs.

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Adverse reactions to chloramphenicol

Irreversible aplastic anemia, non-regenerative anemia, and immunosuppression. GI disturbances with oral chloramphenicol in nonruminant animals

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Bacterial resistance to phenicols

Acetylation of the phenicol and decreased membrane permeability.

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Chloramphenicol's therapeutic uses

Treats both systemic and local infections caused by anaerobes + salmonella spp (resp, CNS, ocular infections).

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Chloramphenicol restrictions

Restricted in production animals because it causes irreversible aplastic anemia.

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Florfenicol use

Only used in cattle to treat bovine respiratory disease.

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Spectrum of activity of Phenicols

G+, G-, and many anaerobes; very effective against Salmonella.

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Study Notes

  • Phenicols are toxic to both humans and animals

Names

  • Chloramphenicol and Florfenicol are examples of phenicols, as indicated by the '-phenicol' suffix in their name

Mechanism of Action

  • Binding to the 50S ribosomal subunit prevents transpeptidation
  • Inhibits both eukaryotic and prokaryotic protein synthesis
  • At low concentrations, phenicols are bacteriostatic; at high concentrations, they are bactericidal

Pharmacokinetics

  • Administration allows for rapid absorption in the gastrointestinal tract
  • Distribution is wide, including the central nervous system and the eye, where it accumulates
  • Metabolism occurs through extensive hepatic glucuronide conjugation
  • Cats have a genetic deficiency in glucuronidase enzymes, resulting in longer drug plasma half-lives; dosages need adjustment
  • Phenicols function as non-competitive microsomal enzyme inhibitors, prolonging the action of other drugs

Adverse Reactions (Chloramphenicol)

  • Bone marrow suppression may cause irreversible aplastic anemia, precluding use in food animals
  • Bone marrow suppression may cause non-regenerative anemia
  • Immunosuppressant properties caution against administration close to vaccination
  • Oral chloramphenicol can cause gastrointestinal disturbances, particularly in nonruminant animals

Spectrum of Activity

  • Effective against a broad spectrum of bacteria including Gram-positive, Gram-negative, and many anaerobes, especially Salmonella

Bacterial Resistance

  • Acetylation of the phenicol prevents ribosome binding
  • Decreased membrane permeability to chloramphenicol
  • Resistance to chloramphenicol often occurs with resistance to other antibiotics, such as tetracycline, streptomycin, and ampicillin

Therapeutic Applications

  • Chloramphenicol is used to treat both systemic and local infections caused by anaerobes and Salmonella species, affecting the respiratory system, central nervous system, and eyes
  • Chloramphenicol use is restricted in production animals because it causes irreversible aplastic anemia
  • Florfenicol is exclusively used in cattle to treat bovine respiratory disease

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