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pcol > 11 & 12 > Flashcards

11 & 12 Flashcards

1
Q

Similar to p-aminobenzoic acid
(PABA)
● Weakly acid compounds
● Modest tissue absorption

A

SULFONAMIDES

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2
Q

SULFONAMIDES excretion and metabolization sites

A

Metabolized in the liver
Excretion: urine

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2
Q

Triple Sulfa

A

Sulfisozaxole: short-acting
Sulfamethosaxole: intermediate acting
Sulfadoxine: long-acting

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3
Q

ROA SULFONAMIDES

A

Oral absorbable, Oral non-absorbable, Topical

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4
Q

Sulfonamide is a _____ inhibitor of Dihydropteroate synthase and folate production

Competitive or Selective

A

Competitive

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5
Q

SULFONAMIDES are usually given in combination with

A

Trimetophrim or Pyrimethamine

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5
Q

Sulfonamides are Bacteriostatic or Bactericidal

A

Bacteriostatic (when given alone)

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5
Q

T/F: Is sulfonamide plasmid-mediated

A

T

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6
Q

Resistance in Sulfonamide: accumulation of drug
Increase or Decrease

A

Decreased

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7
Q

Resistance in Sulfonamide: production of PABA by bacteria
Increase or Decrease

A

Increase

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8
Q

Resistance in Sulfonamide: sensitivity of
dihydropteroate synthase
Increase or Decrease

A

Decrease

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9
Q

CLINICAL APPLICATIONS:
Gram (+)
Gram (-)
Klebsiella pneumoniae
Salmonella
Shigella
Enterobacter sp.
Nocardia sp.
Chlamydia trachomatis

A

SULFONAMIDES

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10
Q

Poor against anaerobes

A

SULFONAMIDES

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11
Q

Not active against: Ricketssiae & P. aeruginosa

A

SULFONAMIDES

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12
Q

Clinical application of Oral triple sulfa, sulfisoxazole

A

Simple UTI

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13
Q

Nephrotoxicity
- Crystalluria and hematuria

A

SULFONAMIDES

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14
Q

Drug interactions with Warfarin & methotrexate

A

SULFONAMIDES

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14
Q

TOXICITY:
Hypersensitivity
- Skin rash & fever (common)
- Exfoliative dermatitis (rare)
- Polyarteritis nodosa (rare)
- Stevens-Johnson syndrome (rare)
- Cross-allergenicity

A

SULFONAMIDES

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14
Q

ROA TRIMETHOPRIM

A

PO, IV

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15
Q

Toxicity of Sulfonamide which is in the 3rd trimester of pregnancy

A

Kernicterus

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16
Q

TRIMETHOPRIM excretion site

A

Excretion: urine (unchanged)

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16
Q

Structurally similar to folic acid
● Weak base
● Trapped in acidic environments
● High conc: prostatic and vaginal fluids

A

TRIMETHOPRIM

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17
Q

TRIMETHOPRIM is a _____ inhibitor of bacterial dihydrofolate reductase

Competitive or Selective

A

Selective

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18
Q

Resistance in TRIMETHOPRIM: cell permeability

Increase or Decrease

A

Decrease

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19
Q

Resistance in TRIMETHOPRIM: production of dihydrofolate reductase

Increase or Decrease

A

Increase

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20
Q

Clinical application of Oral Trimethoprim

A

Acute UTIs

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21
Q

CLINICAL APPLICATIONS:
P. jirovecii
UTIs
Prostatitis
Shigella
Salmonella
Nontuberculous mycobacteria

A

Oral Trimethoprim-Sulfamethoxazole
(TMP-SMZ)

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22
Q

TOXICITY:
Megaloblastic anemia, Leukopenia, &
Granulocytopenia
- Supplementary folinic acid

A

TRIMETHOPRIM

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22
Q

CLINICAL APPLICATIONS:
Toxoplasmosis

A

Oral Pyrimethamine with Sulfonamide

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22
Q

CLINICAL APPLICATIONS:
Moderately severe to severe pneumocystis pneumonia

A

IV Trimethoprim-Sulfamethoxazole

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23
Q

TOXICITY:
HIV patients given ____
- Fever
- Rashes
- Leukopenia
- Diarrhea

A

TRIMETHOPRIM

24
Q

Mild elevation of blood creatinine

A

TRIMETHOPRIM

25
Q

CLINICAL APPLICATIONS:
Sinus infections caused by
- H. influenzae
- M. catarrhalis

A

TMP-SMX (TRIMETHOPRIM &
SULFAMETHOXAZOLE)

26
Q

CLINICAL APPLICATIONS:
DOC of:
- Pneumocystis pneumonia
- Toxoplasma
- Nocardiosis

A

TMP-SMX (TRIMETHOPRIM &
SULFAMETHOXAZOLE)

27
Q

Treatment of infections
- MR staphylococci
- L. monocytogenes

A

TMP-SMX (TRIMETHOPRIM &
SULFAMETHOXAZOLE)

28
Q

TOXICITY:
- Nausea
- Vomiting
- Drug fever
- Vasculitis
- Renal damage
- CNS disturbances
- HIV: Fever, Rashes, Leukopenia, Diarrhea

A

TMP-SMX (TRIMETHOPRIM &
SULFAMETHOXAZOLE)

29
Q

CLINICAL APPLICATIONS:
- Ulcerative colitis (oral)
- Rheumatoid arthritis (oral)
- Enteritis
- Other Inflammatory Bowel Diseases (IBDs)

A

SULFASALAZINE (SALICYLAZOSULFAPYRINE)

30
Q

CLINICAL APPLICATIONS:
● Opthalmic solution or
ointment
● Bacterial conjunctivitis
● Ocular infection

A

SODIUM SULFACETAMIDE

31
Q

CLINICAL APPLICATIONS:
● First line for Acute Toxoplasmosis

A

SULFADIAZINE + PYRIMETHAMINE

31
Q

CLINICAL APPLICATIONS:
● P. jirovecii pneumonia
● Toxoplasmosis
● Nocardiosis

A

SULFAMETHOXAZOLE

32
Q

CLINICAL APPLICATIONS:
● Topical
● Burn wounds
- For prevention of infection

A

SILVER SULFADIAZINE

33
Q

CLINICAL APPLICATIONS:
● Topical
● Burn wounds
- Can cause metabolic acidosis

A

MAFENIDE ACETATE

34
Q

CLINICAL APPLICATIONS:
● Marketed in some countries
● Second-line antimalarial agent

A

SULFADOXINE + PYRIMETHAMINE
(FANSINADIR / FANSIDAR)

35
Q

These were originally developed because of their gram-negative aerobic coverage (with gram+ coverage as well)

A

FLUOROQUINOLONES

36
Q

Impaired absorption when combined with antacids, divalent, and trivalent cations
(Should be taken 2h before or 4h after)

A

FLUOROQUINOLONES

37
Q

Interfere with bacterial DNA synthesis
- Topoisomerase II (relaxation)
- Topoisomerase IV (separation)

A

FLUOROQUINOLONES

38
Q

is Fluoroquinolones Bactericidal or Bacteriostatic

A

Bactericidal

39
Q

Resistant organism appears in about every 107-109:
o Staphylococci
o P. aeruginosa
o S. marcesens

A

FLUOROQUINOLONES

40
Q

Emerged rapidly for 2nd generation:
o C. jejuni and gonococci
o Gram (+) cocci (MRSA)
o Pseudomonas and Serratia

A

FLUOROQUINOLONES

41
Q

CLINICAL APPLICATIONS:
* Urogenital and gastrointestinal tract infection
* Atypical and intracellular pathogens
* Gr (+) bacteria
* Gram (-) organisms
o Gonococci
o E. coli
o K. pneumoniae
o C. jejuni
o Enterobacter
o P. aeruginosa
o Salmonella
o Shigella

A

FLUOROQUINOLONES

42
Q

CLINICAL APPLICATIONS:
Bacterial diarrhea
* Meningococcal carriers
* Prophylaxis of bacterial infections w/ neutropenia
* Effectiveness is variable due to resistance
o Respiratory tract
o Skin and soft tissue infection

A

FLUOROQUINOLONES

43
Q

TOXICITIES:
* Tendinitis and tendon rupture
* Superinfection caused by C. albicans
and streptococci
* Temporary to Permanent Peripheral
Neuropathy
* Increase levels of theophylline and
other methylxanthines

A

FLUOROQUINOLONES

44
Q

TOXICITIES:
* May damage growing cartilage and
cause arthropathy
o Not recommended but may be used
for patients below 18 years old
* Avoid in pregnancy

A

FLUOROQUINOLONES

45
Q

Which DNA gyrase inhibitors can cause photosensitivity

A

Lomefloxacin, Pefloxacin, Sparfloxacin

46
Q

Derived from nalidixic acid (earliest)
* Common pathogens that cause UTI
* Does not achieve adequate plasma levels for use in systemic infections

A

NORFLOXACIN

47
Q

Least active of the fluoroquinolones
against both gram negative and gram
positive organisms

A

NORFLOXACIN

48
Q

Synthetic fluorinated derivatives
Oral bioavailability: 70%

A

CIPROFLOXACIN

49
Q

CLINICAL APPLICATIONS:
* Gram (-): greater activity
o P. aeruginosa
* Gram (+) cocci
* Gonococcus
* Mycobacteria
* MSSA
* Atypical organisms (M. pneumoniae)

A

2nd Gen DNA gyrase inhibitors

50
Q

CLINICAL APPLICATIONS:
* N. gonorrhea (single oral doses)
- Alternative to 3rd generation cephalosporin
● Anthrax

A

CIPROFLOXACIN

51
Q

CLINICAL APPLICATIONS:
* Will eradicate accompanying organisms
like Chlamydia (7 day course)
o Urethritis

A

OFLOXACIN

52
Q

3rd GENERATION DNA gyrase inhibitors

A

LEVOFLOXACIN, GATIFLOXACIN, SPARFLOXACIN

53
Q
  • Synthetic fluorinated derivatives
  • Oral bioavailability: 95%
A

LEVOFLOXACIN

54
Q

CLINICAL APPLICATIONS:
* Slightly less active against gram (-)
* Greater activity against gram (+) cocci
* Streptococci
* S. pneumoniae
* Staphylococci
* MRSA
* MSSA
* Some strains of enterococc

A

LEVOFLOXACIN & GATIFLOXACIN

55
Q

CLINICAL APPLICATIONS:
* Community-acquired pneumonia
* Atypical pneumonia (M. pneumoniae)
* Anthrax prophylaxis

A

LEVOFLOXACIN

56
Q

CLINICAL APPLICATIONS:
* Gram (+)
o S pneumoniae
o Some staphylococci

A

GATIFLOXACIN

57
Q

CLINICAL APPLICATIONS:
* Gram (+) organisms
* Penicillin-resistant pneumococci

A

SPARFLOXACIN

58
Q
  • Enhanced activity against anaerobes
A

SPARFLOXACIN

59
Q

TOXICITIES:
QT prolongation

A

LEVOFLOXACIN

60
Q

TOXICITIES:
* QT prolongation
* Hypoglycemia when given with oral
hypoglycemic agents

A

GATIFLOXACIN

61
Q

TOXICITIES:
* Risk for cardiac arrhythmia
* Photosensitivity

A

SPARFLOXACIN

62
Q

CLINICAL APPLICATIONS:
* Gram (+)
o S pneumoniae
o Some staphylococci
* Gram (-) organisms
* Anaerobic bacteria
* Lacks appreciable activity
against:
o P. aeruginosa
* Used in meningococcal
carrier state
* Tuberculosis
* Neutropenia prophylaxis

A

MOXIFLOXACIN

63
Q

CLINICAL APPLICATIONS:
* Gram (+)
* Gram (-) organisms
* Anaerobic bacteria
* Used in meningococcal
carrier state
* Tuberculosis
* Prophylactic management:
neutropenic patients

A

TROVAFLOXACIN

64
Q

CLINICAL APPLICATIONS:
* Gram (+)
o S. pneumoniae
o Some staphylococci
● + Azithromycin
o Lower RTIs

A

GEMIFLOXACIN

65
Q

CLINICAL APPLICATIONS:
* Gram (+)
o S. pneumoniae
o Some staphylococci
o Pneumococci
o Beta-hemolytic
streptococci
o MSSA
o MRSA
* Gram (-): similar to
ciprofloxacin
o P. aeruginosa
* In vitro activity against
anaerobes but not proven

A

DELAFLOXACIN

65
Q
A
66
Q
A

pcol (8 decks)

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