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Pharmacology II > Lecture 21: Inhibitors of Protein Synthesis I > Flashcards

Lecture 21: Inhibitors of Protein Synthesis I Flashcards

1
Q

Aminoglycosides are poly cations and their ___is responsible for their pharmacokinetic properties

A

Polarity

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2
Q

Due to polarity of Aminoglycosides none is absorbed after ___ administration, none penetrates ___ readily

A

Oral, CSF

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3
Q

___excretes Aminoglycosides

A

Kidneys

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4
Q

What is the mechanism of action of Aminoglycosides

A

Inhibit protein synthesis by inhibiting 30s ribosomal subunit

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5
Q

Aminoglycosides treat what infections

A
  1. Gram negative enteric bacteria
  2. Suspicion of sepsis or endocarditis
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6
Q

Aminoglycosides require ___dependent active transport into bacterial cells and therefore would be ineffective against __organisms

A

Oxygen, anaerobic

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7
Q

Under aerobic conditions, aminoglycosides are bacteriocidal or bacteriostatic?

A

Bacteriocidal

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8
Q

Aminoglycosides have ___dependent killing

A

Concentration

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9
Q

Do aminoglycosides have a high or low post antibiotic effect

A

High, so antibacterial activity continues beyond the time that antibiotic is measurable

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10
Q

___dose of Aminoglycosides is better than ___dose

A

Single, large dose better than multiple small dose

(Concentration dependent killing)

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11
Q

What is the main mechanism of resistance to aminoglycosides

A

Plasmid mediated (R-Factor derived) chemical changes of enzymes that adenylate, phosphorylation or acetylate the drugs—>. Bacteria cells metabolize drug

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12
Q

What are Aminoglycosides active against

A
  1. Gram negative rods
  2. P. Aeruginosa
  3. Synergistic with beta-lactams against gram positive
  4. Gram negative infections in all species
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13
Q

Aminoglycosides can treat gram positive infections when combined with

A

Beta-lactams

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14
Q

What are the 4 examples of aminoglycosides

A
  1. Neomycin
  2. Gentamicin
  3. Amikacin
  4. Tobramycin
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15
Q

What is neomycin used for

A
  1. Labeled for cattle, sheep, goats, and birds orally for treatment of susceptible enteric infections
  2. Topically for treating skin, eye, ear infections
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16
Q

Is gentamicin a narrow or broad spectrum

A

Broad spectrum

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17
Q

What does gentamicin have activity against

A

Pseudomonas, proteus, staphylococcus, Coryne-bacterium, gram negative aerobes

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18
Q

What is gentamicin used for

A
  1. Labeled use in pigs
  2. Labeled for uterine infusion in horses
  3. Used in all species for treatment of susceptible infections of skin, respiratory tract, ear, eye, urinary tract, septicemia
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19
Q

What is amikacin labeled for

A

Dogs for susceptible UTI’s

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20
Q

Tobramycin is similar to gentamicin but has more potent ___activity and reduced ___

A

Anti-pseudomonas, Nephrotoxicity

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21
Q

T or F: tobramycin can be used in food animals

A

False

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22
Q

A dog was started on an antibiotic for systemic gram negative infection and then kidney function decreases. What antibiotic is likely?

A

Aminoglycosides

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23
Q

Macrolides are alternative agents to ___ when there is an allergy or in kidney failure

A

Penicillin

24
Q

What is the mechanism of action of macrolides

A

Inhibit protein synthesis by inhibiting 50s ribosomal subunit

25
What other antibiotic can not be given with clindamycin because there is interference and antagonistic action
Chloramphenicol with macrolides
26
What does bacterial protein synthesis start with
Formyl-methionine
27
What is the main mechanism of resistance to erythromycin
Ribosomal protection by inducible or constitutive production of methylase enzymes, mediated by expression of ermA, ermB, and ermC which modify ribosomal target and decrease drug binding
28
___rapidly destroys erythromycin base and therefore enteric coated or film coated preparations preferred
Gastric acid
29
Erythromycin passes through ___ and ___ but not into ___
Placenta, prostate fluid, not CNS
30
Erythromycin is primarily excreted in the ___
Feces
31
Only 5% of erythromycin is excreted in the __, therefore would not be good tx against ___
Urine, UTI’s
32
What is the most common adverse effect of erythromycin in large animals
Diarrhea
33
What is an adverse effect of erythromycin in foals
Hyperthermia
34
What are the adverse effects of erythromycin in small animals
Vomiting and diarrhea (motilin receptors)
35
What are the adverse effects of erythromycin in rodents and rabbits
Severe, often fatal diarrhea
36
Erythromycin increase ___, therefore can result in arrhythmias
QT interval
37
What is erythromycin used for
1. Labeled for cattle BRD 2. Used for susceptible infections in dogs, cats, ferrets and birds
38
What is tylosin used for
Labeled for cattle and swine for susceptible infections
39
What is tilmicosin used for
Labeled for cattle BRD, sheep and swine
40
What is tulathromycin used for
Single SQ injection claimed to be effective against cattle and swine respiratory infections
41
What is azithromycin used for
Susceptible infections in dogs, cats and foals
42
What is clarithromycin used for
Susceptible infections in dogs, cats, ferrets, and foals
43
What species is gamithromycin used in
Beef and non-lactating dairy cattle only
44
When can you not use gamithromycin
Female dairy cattle 20 months or older, calves for veal
45
What is gamithromycin used for
1. Treatment of BRD associated with M. Haemolytica, P. Multocida, H. Somni, M. Bovis in beef and non-lactating dairy cattle 2. Extra label to control respiratory disease in beef and non-lactating dairy cattle at high risk of BRD associated with M. Haemolytica and P. Multocida
46
What is tildipirosin used for
1. Treatment of BRD in beef and non-lactating dairy cattle associated with M, Haemloytica, P. Multocida, H. Somni 2. Extra label to control beef and non-lactating dairy cattle at risk of BRD associated with M. Haemolytica, P. Multocida, and H. Somni
47
When Tildipirosin is used in cattle intended for human consumption you must wait ___days to slaughter
21 days
48
What is the mechanism of action of lincosamides
Inhibit protein synthesis by binding 50s ribosomal subunit
49
Lincosamides have activity against what bacteria
1. Aerobic gram positive cocci 2. Anaerobic gram positive and negative bacteria 3. Many species of streptococci, staphylococci, except enterococci
50
Lincosamides is effective in combination with ___tx toxoplasmosis
Pyrimethamine
51
What is lincomycin used for
1. Approved for cats and dogs with susceptible infection 2. Used in swine to control swine dysentery 3. Tx staphylococcal, streptococcal, and mycoplasmal infection s
52
What is clindamycin used for
1. Approved in dogs and cats for periodontal disease, osteomyelitis, dermatitis and deep soft tissue infections caused by gram positive organisms 2. Used for tx toxoplasmosis in dogs and cats 3. Tx neosporosis in dogs
53
What is pirlimycin used for
Treatment of bovine mastitis
54
What species are lincosamides contraindicated in and why
Horses, rabbits, guinea pigs, hamsters because produce severe often fatal diarrhea due to altered GI flora involving C. Difficicle
55
What side effects are present in dogs, cats, cattle, and swine treated with lincosamides
NMJ blockade at high doses or used with anesthetics
56
What drug is used in combination with clindamycin to prevent C. Difficicle mediated ___ associated with clindamycin in dogs
Metronidazole, pseudomembranous colitis

Pharmacology II (36 decks)

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