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Pharm II > 30s binders > Flashcards

30s binders Flashcards

1
Q

What are the bacterial ribosomal subunits? Mammalian?

A

Bacterial: 50s, 30s

Mammalian: 60s/40s

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2
Q

What are the two 30s binders

A

Aminoglycosides

Tetracyclines

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3
Q

Describe aminoglycosides

A

Basic polycations

Polar organic bases

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4
Q

Are aminoglycosides static or cidal

A

Cidal

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5
Q

What do aminoglycosides target

A

Gram neg AEROBIC infections

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6
Q

Aminoglcyosides (7)

A 
TANG - KPS
Tobramycin
Amikacin
Neomycin
Gentamycin

Kanamycin
Paromomycin
Streptomycin

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7
Q

How do aminoglycosides permeate bacteria?

A
  1. Passive diffusion

2. Active transport (oxygen dependent – which is why only aerobic bacteria are susceptible)

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8
Q

What are the only protein syntethsis inhibitors that are bactericidal? Why?

A

Aminoglycosides because they cause irreversible non-functional proteins

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9
Q

Do aminoglycosides have post-antibiotic effect

A

Yes

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10
Q

Can aminoglycosides be given at long intervals

A

Yes

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11
Q

T/F - you can give aminoglycosides in a single dose

A

True

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12
Q

T/F - gentamycin can be used against anerobic bacteria

A

FALSE - NO ANEROBES!

Gentamycin CAN be used against gram + but there are better options available

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13
Q

How does environmental pH affect antibacterial activity of aminoglycosides

A

Alkaline pH —> increases antimicrobial activity

Acidic pH and Ca, Mg cations —> reduced antimicrobial activity

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14
Q

T/F - oral absorption of aminoglcyosides is good

A

False - poor, best to give parenteral

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15
Q

T/F - parenteral absorption aminoglycosides is good

A

True - 100% bioavailability IM/SC

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16
Q

T/F - aminoglycosides have high concentrations in brain, CSF…

A

False- diffusion across cell membrane is low due to poor lipid solubility

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17
Q

T/F aminoglycosides have long withdrawal period

A

True - slow depletion from tissues

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18
Q

T/F - lean, cachetic animals have increased aminoglycoside distribution

A

True - reduced protein. Can lead to toxicity

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19
Q

Where can aminoglycosides bind to, causing issues

A

Proximal tubule and cochlear tissue in inner ear

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20
Q

T/F - aminoglcyosides are excreted as active drug

A

TRUE - no biotransformation

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21
Q

What kind of toxicity (if any) can aminoglycosides have

A

Nephrotoxic due to drug sequestration in PT of kidney

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22
Q

Your patient has renal insufficiency. Are aminoglycosides safe?

A

Not really - adjust dose and give with lots of water to avoid nephrotoxicity

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23
Q

Adverse effects aminoglycosides (3)

A
  1. Nephrotoxicity: binds to basolateral membrane of PT. TUBULAR NECROSIS
  2. Ototoxicity: irreversible. Auditory (dogs), Vestibular (cats)
  3. Neuromuscular : crurare like (non-depolarizing). Rapid IV bolus = respiratory arrest
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24
Q

Resistance to aminoglycosides (3)

A
  1. Enzymatic inactivation
  2. Ribosomal alterations
  3. Reduced permeability
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25
Q

Efficacy predictor aminogycosides

A

Type 1

26
Q

Which aminoglycoside has broadest spectrum

A

Amikacin

27
Q

Which aminoglycosdie is not effective against Pseudomonas

A

Gentamycin

28
Q

Which aminoglycoside is effective against pseudomonas mediated respiratory tract infections

A

Tobramycin

29
Q

Which aminoglycoside can be absorbed orally and is added to feed/water

A

Apramycin

30
Q

What formulation are tetracyclines given in? Why?

A

Hydrochloride formulation

To stabilize proteins (denature easily)

31
Q

Natural tetracyclines

A

COT

Chlortetracycline
Oxytetraclyine
Tetraclycine

32
Q

Semi-synthetic tetracylines

A

Minocycline

Doxyclyine

33
Q

MOA tetracyclines

A

Reversibly binds to 30s ribosomal subunit

Blocks the binding of aminoacyl-tRNA to acceptor cycle on mRNA-ribosomal complex

Inhibits addition of new AAs to peptide chain

34
Q

T/F - tetracyclines are broad spectrum

A

True - highly broad spectrum

35
Q

T/F - all tetracyclines are effective against pseudomonas

A

False

36
Q

Which tetracycline is drug of choice for Chlamydia psittaci in birds

A

Doxycycline

37
Q

Which tetracycline is drug of choice for Rickettsia

A

Oxytetracycline

38
Q

A horse has equine monocytic ehrlichiosis. Which drug is effecive?

A

Oxytetracycline

39
Q

A dog has a resistant strain of Staph aureus. Can you treat with tetracyclines?

A

Yes - minocycline

40
Q

Heartworm infected dogs should be given which tetracyline? Give four reasons why

A

Doxycycline

  1. Sterilizes female worms
  2. Prevents spread of infection via mosquitos
  3. Improves efficacy of heartworm adulticide
  4. Reduces inflammation and risk of adverse reactions to Melarsomine
41
Q

Which tetracycline has complete absorption when given orally

A

Doxy

42
Q

T/F - tetracyclines have good oral absorption

A

True - can be variable

43
Q

T/F - horses and ruminants should be given tetracyclines with caution as may impair GIT microflora

A

TRUE!

44
Q

What do tetracyclines form complexes with after oral absorption

A

Divalent and trivalent calcium ions – form chelation complexes

45
Q

Which tetracycline has good parenteral absorption

A

Oxytetracycline

46
Q

Which tetracycline is given as opthalmic ointment

A

Oxytetracyline

47
Q

Which tetracylines have prolonged half-life? Why?

A

Doxy
Minocycline

80-90% plasma protein binding

48
Q

Which tetracyclines are most lipid soluble?

A

Minocycline

Doxy

49
Q

Which tetracyclines would be used for a menigeal infection?

A

Minocycline
Doxy

Because they are most lipid soluble - can penetrate brain, CSF

50
Q

What is a negative side effect of chelate complexes formed by tetracyclines

A

They can deposit at active site of ossification in bone and developing teeth of young animals

51
Q

Which tetracyclines are metabolized

A

Mino and Doxy - oxidation in the liver

52
Q

How are most tetracyclines excreted

A

Urine and feces

53
Q

T/F tetracylines undergo enterohepatic circulation

A

True

54
Q

Which is tetracyline is drug of choice for patients with impaired renal function

A

Doxycycline – excreted in bile/feces

55
Q

General adverse effects of tetracyclines

A

GIT disturbances

Hepatoxicity

Photoxicity (sits under dermis)

Renal damage

Tooth mottling

Inhibited growth of long bones in young animals

Hypersensitivity and drug fever in cats

56
Q

What is adverse effect of tetracycline in cats

A

Esophageal lesions

57
Q

Rapid IV inject of tetracycline can cause what? How can you prevent this

A

Chelating of calcium –> reduced Ca for heart contraction and collapse

Prevent by diffusing with saline

58
Q

IV injection of tetracyline can cause what in dogs

A

Anaphylactic shock

59
Q

What can doxy cause in horses

A

Fatal cardiac arrhythmias

60
Q

What can oxytetracyline cause in horses

A

Enteritis - alters commensal microflora

61
Q

Tetracyline bacterial resistance (3)

A

Impair drug permeation

Tetracycline efflux

Ribosomal alteration

62
Q

Efficacy predictor of tetracyclines

A

Type III - time dependent killing with moderate persistent effects

Pharm II (16 decks)

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