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30s binders Flashcards

(62 cards)

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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
Efficacy predictor aminogycosides
Type 1
26
Which aminoglycoside has broadest spectrum
Amikacin
27
Which aminoglycosdie is not effective against Pseudomonas
Gentamycin
28
Which aminoglycoside is effective against pseudomonas mediated respiratory tract infections
Tobramycin
29
Which aminoglycoside can be absorbed orally and is added to feed/water
Apramycin
30
What formulation are tetracyclines given in? Why?
Hydrochloride formulation To stabilize proteins (denature easily)
31
Natural tetracyclines
COT Chlortetracycline Oxytetraclyine Tetraclycine
32
Semi-synthetic tetracylines
Minocycline | Doxyclyine
33
MOA tetracyclines
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
T/F - tetracyclines are broad spectrum
True - highly broad spectrum
35
T/F - all tetracyclines are effective against pseudomonas
False
36
Which tetracycline is drug of choice for Chlamydia psittaci in birds
Doxycycline
37
Which tetracycline is drug of choice for Rickettsia
Oxytetracycline
38
A horse has equine monocytic ehrlichiosis. Which drug is effecive?
Oxytetracycline
39
A dog has a resistant strain of Staph aureus. Can you treat with tetracyclines?
Yes - minocycline
40
Heartworm infected dogs should be given which tetracyline? Give four reasons why
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
Which tetracycline has complete absorption when given orally
Doxy
42
T/F - tetracyclines have good oral absorption
True - can be variable
43
T/F - horses and ruminants should be given tetracyclines with caution as may impair GIT microflora
TRUE!
44
What do tetracyclines form complexes with after oral absorption
Divalent and trivalent calcium ions -- form chelation complexes
45
Which tetracycline has good parenteral absorption
Oxytetracycline
46
Which tetracycline is given as opthalmic ointment
Oxytetracyline
47
Which tetracylines have prolonged half-life? Why?
Doxy Minocycline 80-90% plasma protein binding
48
Which tetracyclines are most lipid soluble?
Minocycline | Doxy
49
Which tetracyclines would be used for a menigeal infection?
Minocycline Doxy Because they are most lipid soluble - can penetrate brain, CSF
50
What is a negative side effect of chelate complexes formed by tetracyclines
They can deposit at active site of ossification in bone and developing teeth of young animals
51
Which tetracyclines are metabolized
Mino and Doxy - oxidation in the liver
52
How are most tetracyclines excreted
Urine and feces
53
T/F tetracylines undergo enterohepatic circulation
True
54
Which is tetracyline is drug of choice for patients with impaired renal function
Doxycycline -- excreted in bile/feces
55
General adverse effects of tetracyclines
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
What is adverse effect of tetracycline in cats
Esophageal lesions
57
Rapid IV inject of tetracycline can cause what? How can you prevent this
Chelating of calcium --> reduced Ca for heart contraction and collapse Prevent by diffusing with saline
58
IV injection of tetracyline can cause what in dogs
Anaphylactic shock
59
What can doxy cause in horses
Fatal cardiac arrhythmias
60
What can oxytetracyline cause in horses
Enteritis - alters commensal microflora
61
Tetracyline bacterial resistance (3)
Impair drug permeation Tetracycline efflux Ribosomal alteration
62
Efficacy predictor of tetracyclines
Type III - time dependent killing with moderate persistent effects

Pharm II (16 decks)

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