Macrolides Flashcards

1
Q

What are the 14-member ring macrolides?

A

Erythromycin, Clarithromycin

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2
Q

What are the 15-member ring azalides?

A

Azithromycin, Gamithromycin

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3
Q

What is the 15-member ring triamilide?

A

Tulathromycin

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4
Q

What are the 4, 16- member rings?

A

Tylosin, Tilmicosin, Tylvalosin, Tildipirosin

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5
Q

Are these compounds acidic or basic? In what pH will they ionized?

A

Basic (7.1+)

All will ionize in acidic environment (rumen)

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6
Q

Are macrolides bacteristatic or bactericidal?

A

Normally bacteristatic but some now bactericidal

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7
Q

How do macrolides work?

A

Inhibition of protein synthesis

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8
Q

What is the spectrum of veterinary macrolides?

A

Anaerobes: +++++
Gram + aerobes: +++++
Gram - aerobes: ++

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9
Q

Are macrolides active against rhodococcus? Mycoplasma?

A

Yes

Tylosin & tulathromycin

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10
Q

Which macrolides are used for rhodococcus? What combination is regularly used?

A

Azithromycin/erythromycin-rifampin

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11
Q

Why is Tilmicosin not effective against mycoplasma?

A

Mycoplasma bovis MIC is to high & Tilmicosin is not clinically effective

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12
Q

What is another notable effect of macrolides unrelated to their antimicrobial activity?

A

Anti-inflammatory

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13
Q

Which macrolides have prokinetic effects on the GI?

A

14 (Erythromycin, clarithromycin) and 16-member rings (tylosin, tilmicosin, tylvalosin, tildipirosin)

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14
Q

Cross-resistance to other macrolides is common, what other antimicrobial is it common for bacteria to be resistant to if also resistant to a macrolide?

A

Lincosamides

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15
Q

What is the route of administration for Tilmicosin? Why?

A

SQ ONLY
IV is fatal!
IM is extremely irritating

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16
Q

Why should you never give systemic tilmicosin to swine?

A

Fatal

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17
Q

Is tilmicosin available as a top dress? Which animal(s)?

A

Yes, swine & cattle

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18
Q

Is oral tilmicosin the only way it can be delivered to swine?

A

Yes because it’s fatal

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19
Q

Tylosin is labeled for IM administration in what animal?

A

Cattle but IV and SQ use has occured

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20
Q

Tulathromycin is labeled for SQ use in what species? IM?

A

SQ in cattle

IM in swine

21
Q

Why do tissues often have higher conceontrations of macrolides than serum?

A

Macrolides concentrate in tissues

22
Q

Which cell specifically do very large amounts of macrolides accumulate in?

A

Leukocytes

23
Q

What allows macrolides to accumulate so readily in tissue?

A

High intracellular penetration

24
Q

Do macrolides reach high concentrations in CSF

A

No despite high lipid solubility

25
Q

What is the standard Vd for macrolides?

A

> 1 L/kg

26
Q

Do macrolides have good oral bioavailability?

A

Yes

27
Q

What is the primary route of elimination of macrolides?

A

Bile/hepatic

28
Q

What is the half-life of IV vs SQ tulathromycin in cattle?

A

65 IV & 92 SQ

USE SQ!

29
Q

What is the elimination half-life of azithromycin in cats/dogs?

A

30 hours (dogs 29)

30
Q

What is the Vd for azithromycin in dogs?

A

12 L/kg

31
Q

What is the oral bioavailability of azithromycin in the dog? cat?

A

100% dog

60% cat

32
Q

What is the most important concern relating to efficacy regarding serum levels?

A

Time above MIC

33
Q

What is the efficacy of azithromycin/clarithromycin most closely linked to?

A

Peak concentration

34
Q

Macrolides (specifically erythromycin) can interact with which system that changes the pharmocodynamics of other drugs? How does it change the pharmacodynamics of these drugs?

A

Cytochrome P 450

Causes decreased elimination because it is a CP450 substrate

35
Q

A low dose of what can be given to a horse to “start its gut”? Why?

A

Erythromycin because it is a prokinetic

36
Q

Rectal edema and prolapse has been associated with which macrolides in swine?

A

Tylosin & erythromycin

37
Q

Which macrolide may commonly cause GI upset in cats and dogs?

A

Erythromycin

38
Q

Why is it not advisable (generally) to use macrolides in horses or rabbits?

A

GI effects

39
Q

Erythromycin has caused death in horses due to what?

A

Clostridium difficile infection

40
Q

What is the issue with IM injection sites in food animals & macrolides?

A

Prolonged & extensive tissue blemishes because its caustic
That’s why you use it SQ

41
Q

Erythromycin can cause this in 2 - 4 month old foals?

A

hyperthermia

42
Q

Tilmicosin is fatal when given to cattle via which route?

A

IV

43
Q

Can you use Tilmicosin in goats?

A

Not a good idea, has been fatal

44
Q

At what administration of Tilmicosin IM will pigs die?

A

20 mg/kg IM

45
Q

What 2 domestic species should you never use Tilmicosin in?

A

Horses & rabbits

46
Q

Which food animals should you not use Tilmicosin in due to withdrawal time? How long is this withdrawal time?

A

Dairy cows

15 - 29 day milk residue

47
Q

Why is it not advisable to use Tilmicosin in dairy cattle?

A

There is no label for dairy cows so there is not acceptable residue level

48
Q

Why sould you not use Tlmicosin in an automatic syringe?

A

Can inject too much and kill an animal or yourself

49
Q

What is the cause of OD deaths due to Tilmicosin?

A

Cardiovascular toxicity due to Ca+ channel block