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Antimicrobial's pharmacology > Antibacterials inhibition of nucleic acid or FAS > Flashcards

Antibacterials inhibition of nucleic acid or FAS Flashcards

1
Q

Folic acid pathway inhibitors

A

Sulfonamides
Trimethoprim

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2
Q

Nucleic acid synthesis inhibitors

A

Quinolones

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3
Q

Sulfisoxazole, sulfamethoxazole and sulfazidine are

A

Sulfonamides

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4
Q

Name the only IV sulfonamide (other two are PO)

A

Sulfamethoxazole

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5
Q

Sulfonamides have good distribution throughout

A

Body tissues, peritoneum, synovial fluid, ocular fluid, pleura

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6
Q

Why are sulfonamides effective for meningitis?

A

They cross the BBB, reaching CSF

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7
Q

By crossing the placenta, sulfonamides can cause

A

Antibacterial and toxic effects in the fetus

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8
Q

N-4 acetylated are _____ metabolites that lack ______ activity but retain ________

A

Sulfonamide
Antimicrobial
Toxicity

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9
Q

Sulfonamides MOA

A

Sulfonamides are competitive inhibitors of dihydropteroate synthase (DPT)

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10
Q

Sulfonamides incorporate ____ into DPT (folic acid precursor)

A

PABA

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11
Q

Sulfonamides bestie (more potent effects)

A

Trimethoprim

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12
Q

Sulfonamides have potent activity against

A

Haemophilus ducreyi
Nocardia spp. (AAR)
Klebsiella granulomatis
Parasites
Fungi

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13
Q

Erythromycin + sulfizoxazole

A

Otitis media in children

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14
Q

SMX has excellent activity against

A

S. aureus, epidirmidis and pyogenes

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15
Q

SMX has GOOD activity against

A

Proteus, E. coli, Klebsiella, Enterobacter, Serratia, Nocardia, Brucella

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16
Q

Systemic infections, UTIs, SHIGELLOSIS, P. jirovecii pneumonia and spora infections can be treated with

A

SMX

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17
Q

T/F Nocardia can be treated with the three sulfonamides

A

T

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18
Q

Pyrimethamine + sulfadiazine is the treatment of choice for

A

Toxoplasmosis

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19
Q

Aplastic anemia and Kernicterus are adverse effects of

A

Sulfonamides

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20
Q

Sulfonamides that induce crystalluria

A

SMX
Sulfadiazine

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21
Q

Sulfonamides mainly interact with

A

Warfarin
Sulfonylurea hypoglycemic agents
Hydantoin anticonvulsants

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22
Q

Sulfonamides and pregnancy

A

NOR

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23
Q

Sulfonamides and water intake

A

Drink more to prevent crystalluria

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24
Q

Sulfonamides resistance mechanism can come from

A

Random mutation and selection or by transfer of resistance by plasmids

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25
Q

Mechanisms of resistance of sulfonamides

A

Lower affinity of dihydropteroate synthase for sulfonamides

Decreased bacterial permeability or active efflux of the drug

An alternative metabolic pathway for synthesis of an essential metabolite

Increased production of an essential metabolite or drug antagonist

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26
Q

Derivatives of para-aminobenzenesulfonamide and are analogs of para-aminobenzoic acid

A

Sulfonamides

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27
Q

Sulfonamides are _____, so cellular and humoral mechanisms are essential for the final erradication

A

bacteriostatic

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28
Q

For nocardia treatment with sulfonamides, you should also use

A

Imipenem, amikacin, or linezolid

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29
Q

Trimethoprim is a _________ inhibitor

A

Folic acid pathway

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30
Q

Trimethoprim should be administered with

A

SMX

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31
Q

TMP rapidly enters ____ and ______

A

CSF and sputum

32
Q

Trimethoprim MOA

A

Inhibits dyhydrofolate reductase DHFR (downstream enzyme from sulfonamides target)

33
Q

Each drug alone has bacteriostatic activity, but TMP + SMX have ______ activity

A

Bactericidal

34
Q

Name urinary uses of tmx-smx

A

UTI
Prostatitis
Cystitis

35
Q

Respiratory therapeutic uses of tmx-smx

A

Outpatients with bronchitis
Maxillary sinusitis by H. influenza and s. PNEUMONIAE
P. jirovecii pneumonia

36
Q

T/F: ACUTE otitis media, shigellosis, complicated abcesses and travelers diarrhea can be treated with TMP-SMX

A

F (travelers diarrhea norrrr)

37
Q

TMP-SMX can be used as ALTERNATIVE TREATMENT FOR

A

Nocardia
Brucellosis
Stenotrophomonas

38
Q

Prophylaxis against Toxoplasma in HIV px.

39
Q

TMP ——- the toxicity of sulfonamides

40
Q

Hematological reactions caused by TMP-SMX

A

Anemia
Coag. disorders
Granulocytopenia
Purpura
Sulfhemoglobinemia

41
Q

Type of purpura in the use of TMP-SMX

A

Henoch-Schonlein

42
Q

HIV adverse effects in TMP-SMX tx.

A

Sensitivity reactions including:
Steven Johnsons syndrome
Sweet syndrome

43
Q

T/F: Jaundice, permanent renal impairment and hyperkalemia are adverse effects of TMP-SMX

44
Q

Warfarin and TMP-SMX can lead to

A

Excessive coagulation

45
Q

Methotrexate and agents that increase potasium or suppress bone marrow should be (avoided/added) when using TMP-SMX

46
Q

TMP-SMX resistance is mostly due to

A

Point mutations in genes encoding for DHFR or the acquisition of a plasmid that codes for an altered DHFR - both are associated with reduced binding of TMP

47
Q

Quinolones are

A

Nucleic acid synthesis inhibitors

48
Q

Name the 8 quinolones

A

Nalidixic Acid
Norfloxacin
Ciprofloxacin
Ofloxacin
Levofloxacin
Gatifloxacin
Moxifloxacin

49
Q

All quinolones are IV and PO administered, which is the one that is also available in opthalmic preparations?

A

Gatifloxacin

50
Q

Norfloxacin has limited use in the treatment of…

A

UTIs and GI infections

51
Q

Which quinolone has enhanced potency activity against gram-positive organisms and is not available in the US anymore

A

Gatifloxacin

52
Q

Quinolone that is very active against B. fragilis

A

Moxifloxacin

53
Q

Quinolones MOA

A

Inhibition of gyrase-mediated DNA supercoiling (bacterial growth is inhibited too)

54
Q

In gram positive bacteria, what is the quinolones main SOA?

A

Topoisomerase IV

55
Q

In gram negative bacteria, what is the main target of quinolones?

A

DNA gyrase

56
Q

Main targets of nalidixic acid (KEEPS)

A

Gram negative bacteria:
E. coli
Klebsiella spp.
Enterobacter
Proteus
Salmonella
Shigella

57
Q

Nalidixic acid is not effective against

A

P. aeruginosa
Gram-positive bacteria
Anaerobes

58
Q

Therapeutic uses of nalidixic acid

A

UTIs by Gram negative bacteria
Cystits and pyelonephritis

59
Q

—— has the same uses of nalidixic acid + traveler’s diarrhea

A

Norfloxacin

60
Q

Quinolone that has the same therapeutic uses as norfloxacin + Salmonella typhi, prophylaxis of anthrax and turalemia due to yersinia pestis

A

Ciprofloxacin

61
Q

Besides being useful in TB and Mycobacterium avium (in px with AIDS), what are the main uses of Ciprofloxacin?

A

Cystic fibrosis - Pseudomonas aeruginosa
Nosocomial pneumonia

62
Q

For cases of nosocomial pneumonia, ciprofloxacin should be combined with a

63
Q

Gatifloxacin therapeutic uses

A

Upper and lower UTIs
Cystitis and pyelonefritis
Prostatitis

64
Q

Moxifloxacin has excellent activity against…

A

S pneumoniae
H influenzae
Atypical respiratory pathogens (Bacteroidis fragillis) and intestinal anaerobes

65
Q

Moxifloxacin is mostly used for

A

CAP
Diabetic foot

66
Q

Levofloxacin therapeutic uses

A

Same as norfloxacin + chlamydial urethritis/cervicitis
+ salmonella typhi

67
Q

Nalidixic acid can cause —— in G6PD deficiency

A

Hemolytic anemia

68
Q

Tendinitis/tendon rupture
QT prolongation
CNS effects
Photosensivity are adverse effects of

A

Quinolones

69
Q

Quinolones and food

A

May delay time for peak concentrations

70
Q

When should quinolones be avoided?

A

Nursing infants
Treatment for Shiga-producing E. coli

71
Q

Cations like calcium, iron and aluminium should/shouldn’t be taken at the same time that PO quinolones BECAUSE

A

They reduce systemic bioavaliability

72
Q

In quinolones resistance, plasmids can transfer _______ chromosomal genes that encode ————–

A

Genes
DNA gyrase and topoisomerase IV

73
Q

Resistance MOA of quinolones can develop through

A

Through mutations in the bacterial chromosomal genes encoding DNA gyrase and topoisomerase IV

74
Q

Plasmids can transfer genes that encode _________ proteins or alter the quinolone

75
Q

Quinolones resistant microorganisms

A

E. coli
Pseudomonas
Staphylococci

Antimicrobial's pharmacology (7 decks)

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