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Chloramphenicol & derivates Flashcards

Quiz 1

1
Q

what type of antimicrobial interferes with bacterial protein synthesis ?

A
  1. Chloramphenicol & its derivatives
  2. Macrolides
  3. lincosamides
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2
Q

How does the antimicrobial interfere with bacterial protein synthesis ?

A

inhibits of 50s Ribosomal binders

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3
Q

what is the source for Chloramphenicol & its derivatives ?

A
  1. streptomyces venezulae

2. manufactured synthetically

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4
Q

What structures of chloramphenicol & its derivatives depend on efficiency of the drug?

A
  1. p-nitrophenol group
  2. dichloroacetyl group
  3. Alcoholic group
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5
Q

what are the general features of chloramphenicol?

A
  1. bacteriostatic
  2. lipid soluble , neutral compound
  3. antibacterial antagonism
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6
Q

what are the derivatives of chloramphenicol?

A
  1. Thiamphenicol

2. florfenicol

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7
Q

what is the mechanism of action for chloramphenicol ?

A
  1. inhibits bacterial protein synthesis
  2. permeate into bacteria & reversible binds to 50s ribosomal subunit
  3. inhibits bacterial enzyme peptide transferase
  4. inhibits peptide formation
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8
Q

What is signifiant about mammalian mitochondrial ribosome with chloramphenicol?

A

inhibits mammalian mitochondrial protein synthesis

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9
Q

What should never be done with antimicrobial the interference with bacterial protein synthesis?

A

combed together - antibacterial antagonism

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10
Q

what his the microbial susceptibility of chloramphenicol?

A

broad spectrum antibiotic

  1. gram + bacteria
  2. gram - bacteria
  3. anaerobes
  4. Mycoplasma , rickettsia
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11
Q

what are the species of gram + bacteria that can be treated with chloramphenicol ?

A
  1. staphylococci sp. ( S. aureus)

2. Streptococci (S. pyogenes)

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12
Q

what are the species of gram - bacteria that can be treated with chloramphenicol ?

A
  1. Escherichia coli
  2. bordetella bronchiseptiica
  3. Pasteurella sp.
  4. Proteus vulgaris
  5. Salmonella sp.
  6. Shigella sp.
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13
Q

what are the species off anaerobes that can be treated with chloramphenicol ?

A
  1. Actinomyces sp.
  2. clostridium sp.
  3. bactericides sp.
  4. Fusobacterium sp.
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14
Q

what is the pharmacokinetics of absorption for chloramphenicol ?

A
  1. highly lipid soluble

2. well absorbed in oral & parental route

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15
Q

What type of animal is the absorption is good & rapid ?

A
  1. monogastrics

2. preruminants

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16
Q

what type of animal is chloramphenicol inactive during absorption?

A

ruminants - ruminal microorganism

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17
Q

what is the pharmacokinetics of oral in chloramphenicol ?

A
  1. chloramphenicol base (unconjugated form)

2. chloramphenicol palmitate ( increase palatability)

18
Q

what is pharmacokinetics of parenteral in chloramphenicol succinate ?

A
  1. hydrolyses in plasma

2. rapid & complete absorption ( IM & SC)

19
Q

What type of administration for chloramphenicol ?

A
  1. oral
  2. IM
  3. SC
  4. IV
  5. otic preparation
  6. ophthalmic preparation
20
Q

what is the pharmacokinetics of distribution of chloramphenicol ?

A
  1. plasma protein binding ( 30-50%)
  2. widely distributed
  3. attains high concentration in tissue
  4. high volume distribution
21
Q

Where is chloramphenicol widely distributed in the body?

A
  1. placental barrier
  2. diffuse into milk
  3. eyes
  4. CNS
  5. heart
  6. lungs
  7. prostate
  8. salivary glands
  9. liver
  10. spleens
22
Q

Which tissue contain high concentration of chloramphenicol used for treatment of infections?

A
  1. CNS

2. Respiratory tract

23
Q

what are the pharmacokinetics of metabolism in chloramphenicol ?

A

liver

glucuronidation

24
Q

what are the metabolites of chloramphenicol

A
  1. chloramphenicol glucuroniide
25
What does metabolism of chloramphenicol depend on ?
1. age | 2. species
26
what type of animal have slow metabolism of chloramphenicol ?
young animals
27
what animals are defcient in glucuronidase enzyme causing slow metabolism of chloramphenicol ?
cats
28
what is the pharmacokinetics of excretion of chloramphenicol ?
1. urine in tubular secretion | 2. bile
29
How are chloramphenicol excreted in bile?
glucuronide conjugate excreted in biile undergo hydrolyses into active drug
30
what is the adverse effect of chloramphenicol ?
1. dose related reversible bone marrow suppression | 2. aplastic anemia
31
How is chloramphenicol a dose -related reversible bone marrow suppression ?
suppression of mitochondrial protein synthesis in bone marrow cells in host
32
What type of animals are chloramphenicol prohibited from using ?
food producing
33
What was taking out of chloramphenicol & replaced with nitrosochloramphenicol ?
para-nitro group of chloramphenicol
34
what are the type of chloramphenicol has nitros-chloramphenicol ?
1. thiamphenicol | 2. florfenicol
35
what is significant of nitrosochloramphenicol?
can't induce bone marrow toxicity
36
What type of animals are more sensitive for toxicity of chloramphenicol ?
1. young animals 2. cats 3 animal w/ impaired liver function
37
what are the clinical signs seen in adverse effects of chloramphenicol ?
1. depression 2. reduce fluid intake 3. emesis 4. diarrhea 5. dehydration 6. weight loss
38
what type of drug interaction for chloramphenicol have ?
1. inhibitor of Cytochrome P-450 drug metabolizing enzyme 2. competition for site of action with: - macrolides - chloramphenicol - lincosamides
39
what are the bacterial resistance for chloramphenicol ?
acquired plasmid -mediate resistance
40
what is resistant to enzyme inactivation in bacterial resistance of chloramphenicol ?
florfenicol
41
what is the acquired , plasmid -mediated resistance of chloramphenicol ?
due to synethesis of chloramphenicol transcetylase enzyme
42
what is thiamphenicol of chloramphenicol derivates?
1. semi- synthetic structural analog 2. para-nitro group sibstituted w/ methyl sulfonyl moiety 3. water soluble 4. metabolized to significant extent 5. excreted as active form 6. mechanism of action & antibacterial spectrum

SGU pharm II (5 decks)

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