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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
Q

What other antibiotic can not be given with clindamycin because there is interference and antagonistic action

A

Chloramphenicol with macrolides

26
Q

What does bacterial protein synthesis start with

A

Formyl-methionine

27
Q

What is the main mechanism of resistance to erythromycin

A

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
Q

___rapidly destroys erythromycin base and therefore enteric coated or film coated preparations preferred

A

Gastric acid

29
Q

Erythromycin passes through ___ and ___ but not into ___

A

Placenta, prostate fluid, not CNS

30
Q

Erythromycin is primarily excreted in the ___

A

Feces

31
Q

Only 5% of erythromycin is excreted in the __, therefore would not be good tx against ___

A

Urine, UTI’s

32
Q

What is the most common adverse effect of erythromycin in large animals

A

Diarrhea

33
Q

What is an adverse effect of erythromycin in foals

A

Hyperthermia

34
Q

What are the adverse effects of erythromycin in small animals

A

Vomiting and diarrhea (motilin receptors)

35
Q

What are the adverse effects of erythromycin in rodents and rabbits

A

Severe, often fatal diarrhea

36
Q

Erythromycin increase ___, therefore can result in arrhythmias

A

QT interval

37
Q

What is erythromycin used for

A
  1. Labeled for cattle BRD
  2. Used for susceptible infections in dogs, cats, ferrets and birds
38
Q

What is tylosin used for

A

Labeled for cattle and swine for susceptible infections

39
Q

What is tilmicosin used for

A

Labeled for cattle BRD, sheep and swine

40
Q

What is tulathromycin used for

A

Single SQ injection claimed to be effective against cattle and swine respiratory infections

41
Q

What is azithromycin used for

A

Susceptible infections in dogs, cats and foals

42
Q

What is clarithromycin used for

A

Susceptible infections in dogs, cats, ferrets, and foals

43
Q

What species is gamithromycin used in

A

Beef and non-lactating dairy cattle only

44
Q

When can you not use gamithromycin

A

Female dairy cattle 20 months or older, calves for veal

45
Q

What is gamithromycin used for

A
  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
Q

What is tildipirosin used for

A
  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
Q

When Tildipirosin is used in cattle intended for human consumption you must wait ___days to slaughter

A

21 days

48
Q

What is the mechanism of action of lincosamides

A

Inhibit protein synthesis by binding 50s ribosomal subunit

49
Q

Lincosamides have activity against what bacteria

A
  1. Aerobic gram positive cocci
  2. Anaerobic gram positive and negative bacteria
  3. Many species of streptococci, staphylococci, except enterococci
50
Q

Lincosamides is effective in combination with ___tx toxoplasmosis

A

Pyrimethamine

51
Q

What is lincomycin used for

A
  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
Q

What is clindamycin used for

A
  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
Q

What is pirlimycin used for

A

Treatment of bovine mastitis

54
Q

What species are lincosamides contraindicated in and why

A

Horses, rabbits, guinea pigs, hamsters because produce severe often fatal diarrhea due to altered GI flora involving C. Difficicle

55
Q

What side effects are present in dogs, cats, cattle, and swine treated with lincosamides

A

NMJ blockade at high doses or used with anesthetics

56
Q

What drug is used in combination with clindamycin to prevent C. Difficicle mediated ___ associated with clindamycin in dogs

A

Metronidazole, pseudomembranous colitis

Pharmacology II (36 decks)

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