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PHA6126 Pharmacology 2 Lecture > Antimetabolites > Flashcards

Antimetabolites Flashcards

1
Q

antimetabolites are divided into 2 based on their MOA

A
  1. Anti-folate drugs (sulfonamide, trimethoprim)
  2. Bacterial DNA replication inhibitors (fluoroquinolone)
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2
Q

sulfonamides inhibit _________________

A

dihydropteroate synthase, thereby inhibiting folate synthesis

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3
Q

trimethoprim is classified under

A

pyrimidine

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4
Q

sulfonamides: weak acid :: trimethoprim: ________________

A

weak base

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5
Q

what are the organisms that sulfonamide inhibits

A

gram positive, gram negative, Nocardia sp., Chlamydia trachomatis, some protozoa

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6
Q

what other organisms does sulfonamide acts against?

A

E. coli, K. pneumoniae, Salmonella, Shigella, Enterobacter

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7
Q

sulfonamide resistance

A
  1. overproduction of PABA (p-aminobenzoic acid)
  2. production of folic acid-synthesizing enzyme that has low affinity for sulfonamides
  3. impaired permeability to sulfonamides
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8
Q

types of sulfonamides

A
  1. oral absorbable (sulfisoxazole, sulfamethoxazole, sulfadiazine, sulfadoxine)
  2. oral non-absorbable
  3. topical (sodium sulfacetamide, mafenide acetate)
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9
Q

absorption site of sulfonamides

A

stomach and small intestines

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10
Q

sulfonamides are widely distributed in?

A

tissues and body fluids

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11
Q

sulfonamide protein binding

A

20% to 90%

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12
Q

a portion of sulfonamides undergo ________________ or _______________ in the liver

A

acetylation or glucuronidation

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13
Q

how are sulfonamides excreted

A

through glomerular filtration

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14
Q

oral absorbable sulfonamides

A
  1. sulfisoxazole, sulfamethoxazole
  2. sulfadiazine
  3. sulfadoxine
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15
Q

used primarily for UTI

A

sulfisoxazole, sulfamethoxazole

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16
Q

used in combination with pyrimethamine for 1st line treatment of acute toxoplasmosis

A

sulfadiazine

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17
Q

long-acting, coformulated with pyrimethamine, and is used as 2nd line treatment for malaria

A

sulfadoxine

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18
Q

oral nonabsorbable sulfonamide

A

used for ulcerative colitis, enteritis, and other IBD (inflammatory bowel disease)

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19
Q

topical sulfonamides

A
  1. sodium sulfacetamide
  2. mafenide acetate
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20
Q

ophthalmic solution or ointment for treatment of bacterial conjunctivitis

A

sodium sulfacetamide

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21
Q

for burns

A

mafenide acetate

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22
Q

pyrimidines

A
  1. trimethoprim
  2. pyrimethamine
23
Q

trimethoxybenzylpyrimidine

A

trimethoprim

24
Q

benzylpyrimidine

A

pyrimethamine

25
Q

inhibits bacterial form and prevents formation of tetrahydrofolate

A

trimethoprim

26
Q

pyrimidine (trimethoprim & pyrimethamine) resistance can result from

A
  1. reduced cell permeability
  2. overproduction of dihydrofolate reductase
  3. production of an altered reductase with reduced drug binding
27
Q

usually given orally

A

trimethoprim

28
Q

pyrimidines are well absorbed in the _______ and widely distributed in _______________

A

gut; body fluids

29
Q

T/F: trimethoprim/pyrimethamine are more lipid soluble than sulfamethoxazole

A

T

30
Q

pyrimidines are weak base concentrates in __________________ and _________________

A

prostatic fluid and vaginal fluid

31
Q

given alone in acute UTI and used for CAP

A

trimethoprim

32
Q

TMP-SMX targets what organisms

A

gram positive, gram negative, opportunistic pathogens (Pneumocystis jirovecii, T. gondii, Nocardia)

33
Q

TMP-SMX are also used for?

A

UTI, prostatitis, COPD exacerbation, acute otitis media, traveller’s diarrhea

34
Q

toxicity associated with TMP-SMX

A

hypersensitivity reactions, cross-allergy, NVD, rare granulocytopenia and thrombocytopenia, hemolysis

35
Q

group of broad spectrum antibiotic; bactericidal and inhibits bacterial DNA replication

A

fluoroquinolone

36
Q

fluoroquinolones cover what organisms

A

anaerobic and atypical organisms and some gram positive and multi-drug resistant organism

37
Q

how many fluoroquinolone generations are there?

A

4

38
Q

1st gen fluoroquinolone

A

norfloxacin

39
Q

2nd gen fluoroquinolone

A

ciprofloxacin, ofloxacin

40
Q

3rd gen fluoroquinolone

A

levofloxacin, moxifloxacin, gemifloxacin

41
Q

4th gen fluoroquinolone

A

delafloxacin

42
Q

what generation of fluoroquinolone have more gram negative activity

A

2nd generation (ciprofloxacin, ofloxacin)

43
Q

gonococcus, active against atypical bacteria (M. pneumoniae, C. pneumoniae)

A

2nd gen (ciprofloxacin, ofloxacin)

44
Q

fluoroquinoline generation that is less active against gram negative bacteria with greater activity against gram positive cocci and MRSA, anaerobes

A

3th generation (levofloxacin, moxifloxacin, gemifloxacin)

45
Q

T/F: fluoroquinolones does not have good oral bioavailability

A

F - good oral bioavailability

46
Q

fluoroquinolones have ________________ of distribution; accumulates in the ___________

A

large volume; tissues

47
Q

how are fluoroquinolones eliminated?

A

tru kidney via secretion

48
Q

fluoroquinolone that has hepatic clearance and may be used in renal failure

A

moxifloxacin

49
Q

T1/2 of fluoroquinolones

A

3-9 hrs

50
Q

primary method of fluoroquinolone elimination

A

via renal tubular secretion

51
Q

bactericidal, interferes with DNA topoisomerase with a post antibiotic effect

A

fluoroquinolone

52
Q

fluoroquinolone resistance

A
  1. decrease intracellular accumulation due to changes in porins
  2. efflux mechanisms
  3. change in sensitivity of target enzymes via point mutation
53
Q

fluoroquinolone toxicity

A

GI distress, skin rashes, headache
insomnia
phototoxicity, tendinitis, tendon rupture
not for pregnant women or growing children
newer agent: QT interval prolongation

PHA6126 Pharmacology 2 Lecture (10 decks)

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