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Basic Pharmacology > Sulfonamides > Flashcards

Sulfonamides Flashcards

1
Q

what is the distribution of sulfonamides?

A

can penetrate intracellularly
used for systemic effect have wide distribution
can vary by agent

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2
Q

are sulfonamides used orally in ruminants for systemic effects?

A

yes

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3
Q

sulfonamides compete with ________________________________ for incorporation into the scheme for folic acid synthesis. folic acid is used for ___________________. this biological antagonism leads to decreased RNA, inhibiting protein synthesis

A

para amino benzoic acid (PABA)
purine synthesis

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4
Q

why are mammalian cells not susceptible to the mechanism of action of sulfonamides?

A

use preformed folic acid

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5
Q

why does purulent debris decrease sulfonamide activity?

A

high protein content
perhaps high para amino benzoic acid content

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6
Q

cross-resistance between sulfonamides is considered ________________

A

complete

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7
Q

what are some intermediate-acting sulfonamide agents?

A

sulfadimethoxine
sulfamethoxazole
sulfadiazine

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8
Q

what is the clinical relevance of sulfonamides?

A

too much resistance for empiric use

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9
Q

what are the selected uses for sulfonamides?

A

coccidiosis
nocardia
bovine foot rot
use in combination with other agents to enhance antimicrobial and antiprotozoal activity

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10
Q

what is a type A (1) adverse effect of sulfonamides?

A

crystalluria

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11
Q

what are some things seen in type B (2) adverse effects of sulfonamides?

A

keratoconjunctivitis sicca
IMHA/ITP
polyarthropathy
hepatotoxicity
proteinuria
cutaneous drug eruptions
hypothyroidism

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12
Q

what is the distribution of diaminopyramidines/benzylpyrimidines?

A

cross barriers well including the blood brain barrier and concentrates in prostate

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13
Q

how are diaminopyramidines/benzylpyrimidines excreted?

A

renal excretion and concentration for trimethoprim (most commonly used)

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14
Q

what is the mechanism of action of diaminopyramidines/benzylpyrimidines?

A

inhibit dihydrofolate reductase thereby interfering with purine and pyrimidine synthesis

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15
Q

why are diaminopyrimidines often combined with a sulfonamide to create a potentiated sulfa?

A

resistance development is often quick when used as a sole agent

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16
Q

what are some common potentiated sulfas?

A

trimethoprim + sulfadiazine: TMS
trimethoprim + sulfamethoxazole

17
Q

what is an important type A side effect due to the diaminopyrimidine in potentiated sulfas?

A

bone marrow suppression

18
Q

one important type B adverse effect of potentiated suflas due to the diaminopyrimidine: simultaneous injections of _____________________ and injectable TMS has caused death in horses

A

alpha-2 agonists

19
Q

which sulfonamides distribute to the CNS at effective concentrations?

A

sulfadiazine/sulfamethoxazole: sulfas used in TMS

20
Q

do sulfonamides concentrate in urine?

A

yes

21
Q

are sulfonamides bacteriostatic or bacteridicidal?

A

bacteriostatic

22
Q

what is the efficacy of sulfonamides dependent upon?

A

time above MIC

23
Q

what is an enteric sulfa agent?

A

sulfazalazine

24
Q

what are some regulatory issues with sulfonamides?

A

use of sulfonamides in lactating dairy cattle, other than those medications specifically approved for use, has been labeled as high priority by the food and drug administration

25
Q

are diaminopyrimidines/benzylpyrimidines bactericidal or bacteriostatic?

A

bactericidal in combination with sulfonamides

26
Q

what is a potentiated sulfa?

A

diaminopyrimidines combined with sulfonamides to help with resistance

27
Q

are potentiated sulfas time or concentration-dependent?

A

time-dependent
conflicting data

28
Q

what is the four quadrant coverage of potentiated sulfas?

A

E. coli: ++
Staphylococcus: ++
Streptococcus: +
anaerobe: *

29
Q

what does pyrimethamine work against?

A

Toxoplasmosis Sarcocystis (EPM)

30
Q

what microbes, outside of the four main, does TMS work against?

A

Coccidia: +
Nocardia: +
Toxoplasmosis Sarcocystis (EPM): +

31
Q

what are the type B adverse effects of potentiated sulfas due to the sulfonamides?

A

keratoconjunctivitis sicca
IMHA/ITP
polyarthropathy
hepatotoxicity
proteinuria
cutaneous drug eruptions
hypothyroidism

Basic Pharmacology (37 decks)

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