Sulfonamides, Trimethoprim and Quinolones Flashcards

1
Q

Sulfonamides tend to be much more soluble at what pH?

A

Alkaline

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2
Q

What enzyme is inhibited by sulfonamide?

A

Dihyrdopteroate synthase

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3
Q

What mechanism is used by sulfonamide for its action against susceptible microorganisms?

A

Competitive inhibition

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4
Q

What drug inhibits dihydrofolate reductase?

A

Trimethoprim or pyrimethamine

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5
Q

Combination or sulfonamide and trimethoprim provides what kind of activity against microorganisms?

A

Synergistic activity

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6
Q

How do you classify sulfonamides?

A
  1. oral, absorbable
  2. oral, non-absorbable
  3. Topical
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7
Q

How do you classify oral, absorbable sulfonamides?

A
  1. short-acting
  2. intermediate-acting
  3. long-acting
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8
Q

What is the drug of choice for Pneumocystiis Jiroveci pneumonia?

A

Trimethoprim-sulfamethoxazole

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9
Q

Sulfisoxazole and sulfamethoxazole is used almost exclusively to treat what?

A

UTI

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10
Q

What is the first line therapy for the treatment of acute toxoplasmosis?

A

Sulfadiazine in combination with pyrimethamine

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11
Q

When giving sulfadiazine with pyrimethamine, you should also administer Folinic acid. Why is that?

A

To minimize bone marrow suppression

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12
Q

What drug is used for ulcerative colitis, enteritis and other inflammatory disease?

A

Sulfasalazine

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13
Q

Mafenide acetate, a sulfonamide used topically for burn sites causes metabolilc acidosis, how?

A

Inhibition of Carbonic Anhydrase

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14
Q

What is the uncommon yet serious adverse reaction of Sulfonamides?

A

Stevens-Johnson syndrome

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15
Q

Sulfadiazine when given in large doses and when fluid intakes is poor can cause crystalluria. How do you treat crystalluria?

A

Administration of sodium bicarbonate to alkalinize the urine and fluids to increase urine flow

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16
Q

What is the mechanism of action of trimethoprim?

A

Inhibition of bacterial dihydrofolate reductase

17
Q

Is sulfonamide alone bacteriostatic or bactericidal?

A

Bacteriostatic

18
Q

Is trimethoprim-sulfonamide bacteriostatic or bactericidal?

A

Bactericidal

19
Q

What causes resistance to trimethoprim?

A
  1. Reduced cell permiability
  2. Overproduction of dihydrofolate reductase
  3. Production of an altered reductase with reduced drug binding
20
Q

Which is more lipid soluble, therefore larger volume of distribution between sulfamethoxazole and trimethoprim?

A

Trimethoprim

21
Q

Trimethoprim has more antimicrobial activity in prostatic and vaginal fluids than many other antimicrobial drugs, why?

A

Trimethorpim is a weak base and concentrates in prostatic and vaginal fluid

22
Q

What are the adverse effects of trimethoprim?

A

Megaloblastic anemia, leukopenia and granulocytopenia

23
Q

What is the mechanism of action of quinolones?

A

Inhibition of bacterial topoisomerase I (DNA gyrase) and topoisomerase IV

24
Q

Fluoroquinolones have excellent activity against what organisms?

A

Gram-negative aerobic

25
Sulfonamides are not given to patiens with G6PD deficiency, why?
Results in acute hemolysis
26
What are the drugs that interact with sulfonamides?
Warfarin and Methotrexate
27
What generation of fluoroquinolone has the highest gram, negative coverage?
2nd generation
28
When do you take fluoroquinolone?
2 before or 4 hours after taking products that contain divalent and trivalent cations
29
What is the drug of choice for prophylaxis and treatment of anthrax?
Ciprofloxacin
30
What is the serious adverse reaction of fluoroquinolones?
Tendonitis and tendon rupture
31
What are the drug interactions of fluoroquinolones?
Theophylline and other methylxanthines
32
What drug has the most activity against microorganisms associated with community-acquired pneumonia?
Levofloxacin
33
What quinolone drugs has the widest specturm of activity?
Gemifloxacin and Moxifloxacin
34
Which drug exhibits postantibiotic effects?
Fluoroquinolones
35
What is postantibiotic effect?
Bacterial growth continues to be inhibited even after the plasma concentration of the drug has fallen below the mean inhibitory concentrations
36
What is the gene in gonococci that causes resistance to quinolones?
gyrA gene