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SGU pharm II > Sulfonamides & diaminopyrimdines > Flashcards

Sulfonamides & diaminopyrimdines Flashcards

drug quiz 1

1
Q

what are the type of antibiotic that are inhibitors of folic acid synthesis ?

A
  1. sulfonamides

2. Diaminopyrimides

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2
Q

what folic acid synthesis inhibitor is a PABA structural analog & was first used a chemotherapeutic agent?

A

Sulfonamide

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3
Q

what folic acid synthesis inhibitor is a dihydrofolate reductase enzyme inhibitors?

A

diaminopyrimidine

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4
Q

What does sulfonamides inhibit?

A

dihydropteroate synathetase

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5
Q

what does diaminopyrimidines inhibit?

A

dihydrofolate reductase

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6
Q

what is sulfonamides?

A
  1. synthetic antimicrobial
  2. bacteriostatic
  3. broad spectrum
  4. weak organic acid
  5. wide range of pKa
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7
Q

What are the classification of sulfonamides?

A
  1. short-acting sulfonamides
  2. intermediate-acting sulfonamides
  3. long-acting sulfonamides
  4. Enteric sulfonamides
  5. Topical application
  6. Ophthalmic use
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8
Q

What classification of sulfonamides after one therapeutic dose the blood concentration remains above 50 µg/mL for less than 24 hrs?

A

short-acting sulfonamides

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9
Q

what are the type of short acting sulfonamides?

A
  1. sulfacetamide
  2. sulfathiazole
  3. sulfisoxazole
  4. sulfachlorpyridazine
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10
Q

What is Sulfacetamide used for ?

A
  1. neutral in pH

2. ophthalmic preparation

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11
Q

what is sulfisoxazole used for ?

A
  1. used in UTI in small animals
  2. very soluble
  3. Rapid excreted
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12
Q

what is sulfachlorpyridazine?

A
  1. used in respiratory & enteric infection in calves & swine
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13
Q

what classification of sulfonamides after one therpeutic dose the blood concentration remains above 50 µg/mL for 12-24 hrs?

A

intermediate -acting sulfonamides

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14
Q

what are type of intermediate acting sulfonamides?

A
  1. sulfamethoxazole
  2. sulfapyridine
  3. sulfamethazine/ sulfadimidine
  4. sulfadiazine
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15
Q

what is sulfamethoxazole (co-trimoxazole) used for ?

A

UTI infection in small animals

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16
Q

what is sulfapyridine/sulfamethazine ( sulfadimidine) used for ?

A
  • used in food production

- administered in drinking water & feed additive

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17
Q

what type of classification of sulfonamides after one therapeutic dose blood concentration remains above 50µg/mL for more than 24 hrs ?

A

long -acting sulfonamides

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18
Q

what are the types of long -acting sulfonamides?

A
  1. sulfadimethoxine
  2. sulfamethazine
  3. sulfaethoxypyridazine
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19
Q

what are the type of Enteric sulfonamides?

A
  1. sulfasalazine
  2. sulfaquinoxaline
  3. sulfaguanidine
  4. Phthalylsulfathiazone
  5. succinylsulfathiazole
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20
Q

what is sulfasalazine used for?

A

colitis in dogs

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21
Q

what is sulfaquinoxaline used for ?

A

coccidiosis in poultry

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22
Q

what is sulfaguanidine used for ?

A

large ruminants

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23
Q

what are the topical application of sulfonamides?

A
  1. silver sulfadiazine
  2. mafenide ( sulfamylon)
  3. sulfacetamide
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24
Q

what sulfonamide is used for ophthalmic use?

A

sulfacetamide

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25
Q

what is the spectrum of action for sulfonamides?

A
  1. Gram + aerobic bacteria
  2. Gram - aerobic bacteria
  3. Protozoa
  4. Pus/purulent tissue reduce microbial activity
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26
Q

what is sulfonamides ineffective against what type of bacteria?

A

most obligate anaerobes bacteria

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27
Q

what gram - bacteria can sulfonamide not be used on ?

A

P. aeruginosa

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28
Q

what type of protozoa can sulfonamides be used on?

A

coccidia

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29
Q

what type of spectrum of action will sulfonamide + diaminopyrimidine have ?

A

Broad spectrum of action

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30
Q

what is the pharmacokinetics of absorption in sulfonamides ?

A
  1. oral route

2. parenteral route

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31
Q

How is the pharmacokinetics of oral route of absorption for sulfonamides?

A

well absorbed except for enteric sulfonamides

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32
Q

when will there be a delay in asborption of oral sulfonamides?

A
  1. ruminants

2. monogastrics when Administered with food

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33
Q

How is the pharmacokinetics of parenteral route of absorption for sulfonamides?

A
  1. well absorbed in IM/SC

2. buffered solution

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34
Q

How is the pharmacokinetics of distribution of sulfonamides?

A
  1. widely distributed throughout the body

2. distribution of individual compounds

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35
Q

Where can sulfonamides be distributed in the body?

A
  1. synovial fluid
  2. aqueous humor
  3. cerebrospinal fluid
  4. placental transfer
  5. milk
36
Q

What does the distribution of individual sulfonamides compounds depend on?

A
  1. pKa ( high pKa= low solubility)

2. Protein binding varies from 15 %( sulfanilamide) to 90 % (sulfadimethoxine)

37
Q

what is the pharmacokinetics in metabolism of sulfonamides ?

A
  1. primarily in liver by acetylation pathway
  2. acetylated metabolites form crystalluria = less soluble
  3. Glucuronide conjugation
  4. Aromatic hydroxylation
38
Q

what animal has poor acetylation ?

39
Q

what is the pharmacokinetics in excretion of sulfonamides?

A
  1. renal excretion
40
Q

what type of renal excretions does sulfonamides use ?

A

all 3 processes

  1. glomerular filtration
  2. tubular secretion
  3. tubular reabsorption (acidic urine pH)
41
Q

What can increase the rate of elimination of sulfonamide ?

A

alkalization of urine

42
Q

How does long -acting sulfonamides difference in excretion?

A
  1. enterohepatic recycling
  2. tubular reabsorption
  3. excreted in tears/saliva/ bile/milk & sweat
43
Q

How is enteric sulfonamides excreted?

44
Q

what are the Immunological sulfonamides toxicities?

A
  1. Keratoconjunctivitis sick
  2. hepatic necrosis
  3. skin reaction
45
Q

what are the types of toxicities for sulfonamides?

A
  1. immunological

2. non-immunological

46
Q

When will you see Ketatoxonjuctivis sicca as a immunological toxicity of sulfonamide?

A

dogs weighing <12 kg

- pyridine ring induces hypersensitive Ron on lacrimal acinar cells

47
Q

When would you see hepatic necrosis as an immunological toxicity of sulfonamides ?

A
  1. induced by combination of trimethoprim + sulfadiazine & trimethoprim +sulfamethoxazole
  2. slow acetylation of sulfonamide in hepatic dogs
48
Q

when would you see skin reaction as an immunological toxicity of sulfonamides?

A

drug -induced eruption in dogs

49
Q

what are type of non immunological toxocities of sulfonamides?

A
  1. Nephrotoxicity

2. blood dycrasias

50
Q

When would you see Neprotoxicity as an non-immunological toxicity of sulfonamide?

A
  1. crystalluria
  2. hematuria
  3. renal tubular blockage
51
Q

What causes nephrotoxicity as a non-immunological toxicity of sulfonamide?

A
  1. due to low solubility & precipitation of sulfonamide metabolite in renal tubules
  2. aciduria
52
Q

What will minimizes nephrotoxicity as a non-immunological toxicity of sulfonamide?

A
  1. alkalization or urine
  2. hydration
  3. combination of sulfa drugs
53
Q

what can cause blood dycrasias as a non-immunological toxicity of sulfonamide?

A
  1. hypoprothrombinemia
  2. asplastic anemia
  3. Thrombocytopenia `
54
Q

How can sulfaquinoxaline cause blood dyscrasia as an non-immunological toxicity of sulfonamide?

A
  1. hypoprothrombinemia: inhibition of Vit. K expoxide reductase
55
Q

How can trimethoprim + sulfonamide cause blood dyscrasias as an non-immunological toxicity of sulfonamide?

A

aplastic anemia

56
Q

what type of animal is it not preferred to use sulfonamides as an antibiotic?

A

animals with pre-existing bleeding disorder

57
Q

What type of sensitivities does Doberman Pinschers have with sulfonamides?

A
  1. polyarthritis
  2. fever
  3. cutaneous
  4. cutaneous eruptions
  5. hepatitis
58
Q

what type of sensitivities do ducks have with sulfonamides?

A

Hypoglycemia

59
Q

what type of sensitivity does dogs have with sulfonamides?

A
  1. hypoglycemia

2. Iatrogenic hypothyroidism - reversible

60
Q

What type of bacterial resistance do bacteria have against Sulfonamides?

A
  1. Chromosomal mediated resistance - develops slowly
  2. plasmid mediated resistance - develops rapidly
  3. cross -resistance
61
Q

What are the consequences of bacterial resistances of sulfonamides?

A
  1. impaired drug penetration
  2. increase production of PABA
  3. sulfonamides resistant dihydropteroate synthase enzyme
62
Q

what Type II antimicrobial is lipid-soluble organic base with bacteriostatic antimicrobial properties ?

A

diaminopyrimidines

63
Q

what are the commonly used diaminopyrimidine in vet medicine?

A
  1. Ormetoprim
  2. pyrimethamine
  3. trimethoprim
  4. baquiloprim
64
Q

what is the mechanism of action for diaminopyrimidine?

A
  1. reversibly binds & inhibits dihydrofolate reductalr enzyme
  2. posses low affinity for mammalian DHF reductase enzyme
65
Q

what type of diaminopyrimidine antibiotic is specifically used for Protozoa?

A

Pyrimethamine

66
Q

what are the pharmacokinetics of diaminopyrimidines?

A
  1. well absorbed after oral/parental administration
  2. lipid solubile
  3. widely distributed
  4. penetrates blood brain barrier
  5. concentrate in prostatic fluid & milk ( ion trapping )
  6. metabolized in liver
  7. excreted in urine
67
Q

What combination of antimicrobials form potentiated sulfonamides that will have antibacterial efficacy as synergistic ?

A

sulfonamide & diaminopyrimidine (5:1 parts)

68
Q

How is the spectrum activity for potentiated sulfonamides?

A

broad spectrum antibacterial activity

69
Q

what is significant about potentiated sulfonamides spectrum activity?

A
  1. sulfonamides & trimethoprim are bacteriostatic agent alone
  2. in combination with potentiated sulfas that act as bactericidal
70
Q

what are the potentiated sulfonamides ?

A
  1. sulfadiazine + trimethoprim
  2. sulfadiazine + trimethoprim
  3. sulfadoxine + trimethoprim
  4. sulfamethoxazole + trimethoprim
  5. sulfademethoxine + ormetoprim
  6. sulfaquinoxaline + pyrimethamine
71
Q

what is sulfadiazine + trimethoprim used for ?

A
  1. Uniprim horses - oral powered

2. Duofast lactating animals - infusing intramammary

72
Q

what are potentiated sulfonamides used for ?

A
  1. urogenital infection
  2. bone infection
  3. joint infection
  4. pyoderma
  5. respiratory infection
  6. skin infection
73
Q

what is sulfadoxine +trimethoprim used for ?

A

Trivetrin : injectable

74
Q

what is sulfamethozazole + trimethoprim used for?

A
  1. Bactrim:tablets
  2. Septran
  3. Co-trim vet bolus suspension
75
Q

what is sulfadimethoxine + ormetoprim used for ?

A

primor tabs for dogs

76
Q

what potentiated sulfonamide is an anti protozoal oral suspension used in horses ?

A

rebalance = sulfadiazine & pyrimethamine

77
Q

what is the microbial susceptibility for potentiated sulfonamides?

A
  1. gram +
  2. gram -
  3. Protoza
78
Q

what are the gram + species that are susceptible to potentiated sulfonamides?

A
  1. streptococci
  2. staphylococcus
  3. Nocardia
79
Q

what are the gram - species that are susceptible to potentiated sulfonamides ?

A

Enterobacteriacease organism except P. aeruginosa

80
Q

what are the protozoa species that are susceptibility to potentiated sulfonamides ?

A
  1. coccidia

2. toxoplasma gondii

81
Q

what species of bacteria is seen in horses that is treated with sulfadiazine + pyrimethamine ?

A

Sarcocytis neurona

82
Q

what species of fungus is treated with potentiated sulfonamide Co-trimoxazole ?

A

Pneumocystis carinii = Pneumonia

83
Q

what are the pharmacokinetics for potentiated sulfonamides ?

A
  1. well absorbed orally
  2. slowly absorbed SC
  3. well distributed
  4. metabolized by liver
  5. excreted through urine
84
Q

How well is the distribution of potentiated sulfonamides ?

A
  1. penetrates CSF through inflamed meninges
  2. crosses placenta
  3. distributed into milk
85
Q

How potenaited sulfonamides metabolized ?

A
  1. sulfonamides = acetylation & conjugation w/ gluronic acid
  2. diaminopyrimidine = oxide & hydroxylated metabolites
86
Q

How is potentiated sulfonamides excreted ?

A

in urine by

  • glomerular filtration
  • tubular scretion

SGU pharm II (5 decks)

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