Sulfonamides & diaminopyrimdines Flashcards
drug quiz 1
1
Q
what are the type of antibiotic that are inhibitors of folic acid synthesis ?
A
- sulfonamides
2. Diaminopyrimides
2
Q
what folic acid synthesis inhibitor is a PABA structural analog & was first used a chemotherapeutic agent?
A
Sulfonamide
3
Q
what folic acid synthesis inhibitor is a dihydrofolate reductase enzyme inhibitors?
A
diaminopyrimidine
4
Q
What does sulfonamides inhibit?
A
dihydropteroate synathetase
5
Q
what does diaminopyrimidines inhibit?
A
dihydrofolate reductase
6
Q
what is sulfonamides?
A
- synthetic antimicrobial
- bacteriostatic
- broad spectrum
- weak organic acid
- wide range of pKa
7
Q
What are the classification of sulfonamides?
A
- short-acting sulfonamides
- intermediate-acting sulfonamides
- long-acting sulfonamides
- Enteric sulfonamides
- Topical application
- Ophthalmic use
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
9
Q
what are the type of short acting sulfonamides?
A
- sulfacetamide
- sulfathiazole
- sulfisoxazole
- sulfachlorpyridazine
10
Q
What is Sulfacetamide used for ?
A
- neutral in pH
2. ophthalmic preparation
11
Q
what is sulfisoxazole used for ?
A
- used in UTI in small animals
- very soluble
- Rapid excreted
12
Q
what is sulfachlorpyridazine?
A
- used in respiratory & enteric infection in calves & swine
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
14
Q
what are type of intermediate acting sulfonamides?
A
- sulfamethoxazole
- sulfapyridine
- sulfamethazine/ sulfadimidine
- sulfadiazine
15
Q
what is sulfamethoxazole (co-trimoxazole) used for ?
A
UTI infection in small animals
16
Q
what is sulfapyridine/sulfamethazine ( sulfadimidine) used for ?
A
- used in food production
- administered in drinking water & feed additive
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
18
Q
what are the types of long -acting sulfonamides?
A
- sulfadimethoxine
- sulfamethazine
- sulfaethoxypyridazine
19
Q
what are the type of Enteric sulfonamides?
A
- sulfasalazine
- sulfaquinoxaline
- sulfaguanidine
- Phthalylsulfathiazone
- succinylsulfathiazole
20
Q
what is sulfasalazine used for?
A
colitis in dogs
21
Q
what is sulfaquinoxaline used for ?
A
coccidiosis in poultry
22
Q
what is sulfaguanidine used for ?
A
large ruminants
23
Q
what are the topical application of sulfonamides?
A
- silver sulfadiazine
- mafenide ( sulfamylon)
- sulfacetamide
24
Q
what sulfonamide is used for ophthalmic use?
A
sulfacetamide
25
what is the spectrum of action for sulfonamides?
1. Gram + aerobic bacteria
2. Gram - aerobic bacteria
3. Protozoa
4. Pus/purulent tissue reduce microbial activity
26
what is sulfonamides ineffective against what type of bacteria?
most obligate anaerobes bacteria
27
what gram - bacteria can sulfonamide not be used on ?
P. aeruginosa
28
what type of protozoa can sulfonamides be used on?
coccidia
29
what type of spectrum of action will sulfonamide + diaminopyrimidine have ?
Broad spectrum of action
30
what is the pharmacokinetics of absorption in sulfonamides ?
1. oral route
| 2. parenteral route
31
How is the pharmacokinetics of oral route of absorption for sulfonamides?
well absorbed except for enteric sulfonamides
32
when will there be a delay in asborption of oral sulfonamides?
1. ruminants
| 2. monogastrics when Administered with food
33
How is the pharmacokinetics of parenteral route of absorption for sulfonamides?
1. well absorbed in IM/SC
| 2. buffered solution
34
How is the pharmacokinetics of distribution of sulfonamides?
1. widely distributed throughout the body
| 2. distribution of individual compounds
35
Where can sulfonamides be distributed in the body?
1. synovial fluid
2. aqueous humor
3. cerebrospinal fluid
4. placental transfer
5. milk
36
What does the distribution of individual sulfonamides compounds depend on?
1. pKa ( high pKa= low solubility)
| 2. Protein binding varies from 15 %( sulfanilamide) to 90 % (sulfadimethoxine)
37
what is the pharmacokinetics in metabolism of sulfonamides ?
1. primarily in liver by acetylation pathway
2. acetylated metabolites form crystalluria = less soluble
3. Glucuronide conjugation
4. Aromatic hydroxylation
38
what animal has poor acetylation ?
dogs
39
what is the pharmacokinetics in excretion of sulfonamides?
1. renal excretion
40
what type of renal excretions does sulfonamides use ?
all 3 processes
1. glomerular filtration
2. tubular secretion
3. tubular reabsorption (acidic urine pH)
41
What can increase the rate of elimination of sulfonamide ?
alkalization of urine
42
How does long -acting sulfonamides difference in excretion?
1. enterohepatic recycling
2. tubular reabsorption
3. excreted in tears/saliva/ bile/milk & sweat
43
How is enteric sulfonamides excreted?
feces
44
what are the Immunological sulfonamides toxicities?
1. Keratoconjunctivitis sick
2. hepatic necrosis
3. skin reaction
45
what are the types of toxicities for sulfonamides?
1. immunological
| 2. non-immunological
46
When will you see Ketatoxonjuctivis sicca as a immunological toxicity of sulfonamide?
dogs weighing <12 kg
| - pyridine ring induces hypersensitive Ron on lacrimal acinar cells
47
When would you see hepatic necrosis as an immunological toxicity of sulfonamides ?
1. induced by combination of trimethoprim + sulfadiazine & trimethoprim +sulfamethoxazole
2. slow acetylation of sulfonamide in hepatic dogs
48
when would you see skin reaction as an immunological toxicity of sulfonamides?
drug -induced eruption in dogs
49
what are type of non immunological toxocities of sulfonamides?
1. Nephrotoxicity
| 2. blood dycrasias
50
When would you see Neprotoxicity as an non-immunological toxicity of sulfonamide?
1. crystalluria
2. hematuria
3. renal tubular blockage
51
What causes nephrotoxicity as a non-immunological toxicity of sulfonamide?
1. due to low solubility & precipitation of sulfonamide metabolite in renal tubules
2. aciduria
52
What will minimizes nephrotoxicity as a non-immunological toxicity of sulfonamide?
1. alkalization or urine
2. hydration
3. combination of sulfa drugs
53
what can cause blood dycrasias as a non-immunological toxicity of sulfonamide?
1. hypoprothrombinemia
2. asplastic anemia
3. Thrombocytopenia `
54
How can sulfaquinoxaline cause blood dyscrasia as an non-immunological toxicity of sulfonamide?
1. hypoprothrombinemia: inhibition of Vit. K expoxide reductase
55
How can trimethoprim + sulfonamide cause blood dyscrasias as an non-immunological toxicity of sulfonamide?
aplastic anemia
56
what type of animal is it not preferred to use sulfonamides as an antibiotic?
animals with pre-existing bleeding disorder
57
What type of sensitivities does Doberman Pinschers have with sulfonamides?
1. polyarthritis
2. fever
3. cutaneous
4. cutaneous eruptions
5. hepatitis
58
what type of sensitivities do ducks have with sulfonamides?
Hypoglycemia
59
what type of sensitivity does dogs have with sulfonamides?
1. hypoglycemia
| 2. Iatrogenic hypothyroidism - reversible
60
What type of bacterial resistance do bacteria have against Sulfonamides?
1. Chromosomal mediated resistance - develops slowly
2. plasmid mediated resistance - develops rapidly
3. cross -resistance
61
What are the consequences of bacterial resistances of sulfonamides?
1. impaired drug penetration
2. increase production of PABA
3. sulfonamides resistant dihydropteroate synthase enzyme
62
what Type II antimicrobial is lipid-soluble organic base with bacteriostatic antimicrobial properties ?
diaminopyrimidines
63
what are the commonly used diaminopyrimidine in vet medicine?
1. Ormetoprim
2. pyrimethamine
3. trimethoprim
4. baquiloprim
64
what is the mechanism of action for diaminopyrimidine?
1. reversibly binds & inhibits dihydrofolate reductalr enzyme
2. posses low affinity for mammalian DHF reductase enzyme
65
what type of diaminopyrimidine antibiotic is specifically used for Protozoa?
Pyrimethamine
66
what are the pharmacokinetics of diaminopyrimidines?
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
What combination of antimicrobials form potentiated sulfonamides that will have antibacterial efficacy as synergistic ?
sulfonamide & diaminopyrimidine (5:1 parts)
68
How is the spectrum activity for potentiated sulfonamides?
broad spectrum antibacterial activity
69
what is significant about potentiated sulfonamides spectrum activity?
1. sulfonamides & trimethoprim are bacteriostatic agent alone
2. in combination with potentiated sulfas that act as bactericidal
70
what are the potentiated sulfonamides ?
1. sulfadiazine + trimethoprim
2. sulfadiazine + trimethoprim
3. sulfadoxine + trimethoprim
4. sulfamethoxazole + trimethoprim
5. sulfademethoxine + ormetoprim
6. sulfaquinoxaline + pyrimethamine
71
what is sulfadiazine + trimethoprim used for ?
1. Uniprim horses - oral powered
| 2. Duofast lactating animals - infusing intramammary
72
what are potentiated sulfonamides used for ?
1. urogenital infection
2. bone infection
3. joint infection
4. pyoderma
5. respiratory infection
6. skin infection
73
what is sulfadoxine +trimethoprim used for ?
Trivetrin : injectable
74
what is sulfamethozazole + trimethoprim used for?
1. Bactrim:tablets
2. Septran
3. Co-trim vet bolus suspension
75
what is sulfadimethoxine + ormetoprim used for ?
primor tabs for dogs
76
what potentiated sulfonamide is an anti protozoal oral suspension used in horses ?
rebalance = sulfadiazine & pyrimethamine
77
what is the microbial susceptibility for potentiated sulfonamides?
1. gram +
2. gram -
3. Protoza
78
what are the gram + species that are susceptible to potentiated sulfonamides?
1. streptococci
2. staphylococcus
3. Nocardia
79
what are the gram - species that are susceptible to potentiated sulfonamides ?
Enterobacteriacease organism except P. aeruginosa
80
what are the protozoa species that are susceptibility to potentiated sulfonamides ?
1. coccidia
| 2. toxoplasma gondii
81
what species of bacteria is seen in horses that is treated with sulfadiazine + pyrimethamine ?
Sarcocytis neurona
82
what species of fungus is treated with potentiated sulfonamide Co-trimoxazole ?
Pneumocystis carinii = Pneumonia
83
what are the pharmacokinetics for potentiated sulfonamides ?
1. well absorbed orally
2. slowly absorbed SC
3. well distributed
4. metabolized by liver
5. excreted through urine
84
How well is the distribution of potentiated sulfonamides ?
1. penetrates CSF through inflamed meninges
2. crosses placenta
3. distributed into milk
85
How potenaited sulfonamides metabolized ?
1. sulfonamides = acetylation & conjugation w/ gluronic acid
2. diaminopyrimidine = oxide & hydroxylated metabolites
86
How is potentiated sulfonamides excreted ?
in urine by
- glomerular filtration
- tubular scretion
