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Basic Pharmacology > Macrolides > Flashcards

Macrolides Flashcards

1
Q

what are the physicochemical properties of macrolides?

A

macrolide ring
lipid soluble
maintains activity in purulent debris

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2
Q

how well are macrolides absorbed after oral administration?

A

well absorbed: 40-90%

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3
Q

what is the distribution of macrolides?

A

concentrate intracellularly and widely distributed

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4
Q

do macrolides pass through the blood brain barrier and blood-aqueous barrier?

A

no

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5
Q

how are macrolides excreted?

A

largely through bile into fecees
enters urine in therapeutic concentrations but not major route of elimination

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6
Q

what is the mechanism of action of macrolides?

A

inhibition of protein synthesis at the 50S ribosomal subunit

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7
Q

are macrolides bacteriostatic or bactericidal?

A

mostly bacteriostatic but can be bactericidal in some cases

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8
Q

what does the DNA gyrase do?

A

unwinds DNA before replication

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9
Q

how common is cross-resistance to other macrolides and lincosamides?

A

common

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10
Q

what are some common macrolide agents?

A

erythromycin
azithromycin
clarithromycin
tylosin
tilmicosin

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11
Q

what type of inhibition is the macrolides class believed to have?

A

time-dependent

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12
Q

why is erythromycin not used in adult horses?

A

diarrhea is common in adult horsses

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13
Q

erythromycin has _________________ at low doses (sometimes used for this purpose) and often causes ________________ at antibiotic doses

A

prokinetic activity
intestinal spasms

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14
Q

what is common in dogs with erythromycin?

A

vomiting

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15
Q

what are the half-lives like of azithromycin and clarithromycin?

A

longer than erythromycin
tissue half-lives substantially exceed plasma half-lives

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16
Q

what is the best/safest drug to use for Rhodococcus equi?

A

clarithromycin
usually combined with rifampin

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17
Q

what is the feed additive of tylosin used for?

A

predominantly in food animals

18
Q

what is tylosin used for in small animals?

A

sometimes for large and small bowel diarrheas

19
Q

when is tylosin contraindicated?

A

in horses where it can cause colic and death

20
Q

who is tilmicosin cardiotoxic to?

A

ducks
goats
horses
pigs
humans

21
Q

who is tilmicosin used in?

A

cattle only
(rabbits and sheep)

22
Q

what are the long-acting repository products of tulathromycin, gamithromycin, and tidipirosin used for?

A

respiratory disease in food animals

23
Q

what is the effect of long-acting repository products of tulathromycin, gamithromycin, and tidipirosin from?

A

long half-life and distribution to tissues rather than protein binding

24
Q

who is long-acting repository products of tulathromycin, gamithromycin, and tidipirosin not for use in?

A

lactating dairy cattle: residue violations

25
Q

why are clavamox/unasyn and baytril such a popular combination?

A

complementary: together, get all four quadrants

26
Q

where do macrolides concentrate?

A

lung, prostate, milk
macrophages
other tissues

27
Q

do macrolides enter urine in therapeutic concentrations?

A

yes

28
Q

are macrolides time-dependent or concentration-dependent?

A

time-dependent inhibition

29
Q

do macrolides have a post-antibiotic effect on anything? what?

A

yes, gram positive organisms for some macrolides

30
Q

what is the four quadrant coverage of erythromycin and tylosin like?

A

E. coli: -, + for respiratory
Staphylococcus: +
Streptococcus: +
anaerobe: *

31
Q

what activity do newer macrolides have?

A

against non-enteric gram negatives

32
Q

what are some important side effects of erythromycin?

A

prokinetic at low doses
intestinal spasms at antibiotic doses
diarrhea common in adult horses
vomiting common in dogs

33
Q

how much gastrointestinal upset do azithromycin and clarithromycin cause?

A

less than erythromycin

34
Q

what is azithromycin used to treat in cats and dogs?

A

Bartonella

35
Q

what macrolides are used as a food additive?

A

tylosin
tilmicosin

36
Q

what macrolides should you not use in horses?

A

tylosin
erythromycin
tilmicosin

37
Q

what is the food additive tilmicosin used for?

A

control respiratory disease: okay for pigs via this route

38
Q

what macrolide is cardiotoxic to ducks, goats, horses, pigs, and man if injected?

A

tilmicosin

39
Q

what does the injectable formulation of tilmicosin produce for bovine respiratory disease complex?

A

3 days of effective concentrations
metaphylaxis

40
Q

what is the long-acting repository products of macrolides due to?

A

long half life and distribution to tissues

41
Q

can you use macrolides in lactating dairy cattle?

A

no- concentrates in milk

Basic Pharmacology (37 decks)

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