Antibacterials inhibition of nucleic acid or FAS Flashcards

(75 cards)

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
Mechanisms of resistance of sulfonamides
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
26
Derivatives of para-aminobenzenesulfonamide and are analogs of para-aminobenzoic acid
Sulfonamides
27
Sulfonamides are _____, so cellular and humoral mechanisms are essential for the final erradication
bacteriostatic
28
For nocardia treatment with sulfonamides, you should also use
Imipenem, amikacin, or linezolid
29
Trimethoprim is a _________ inhibitor
Folic acid pathway
30
Trimethoprim should be administered with
SMX
31
TMP rapidly enters ____ and ______
CSF and sputum
32
Trimethoprim MOA
Inhibits dyhydrofolate reductase DHFR (downstream enzyme from sulfonamides target)
33
Each drug alone has bacteriostatic activity, but TMP + SMX have ______ activity
Bactericidal
34
Name urinary uses of tmx-smx
UTI Prostatitis Cystitis
35
Respiratory therapeutic uses of tmx-smx
Outpatients with bronchitis Maxillary sinusitis by H. influenza and s. PNEUMONIAE P. jirovecii pneumonia
36
T/F: ACUTE otitis media, shigellosis, complicated abcesses and travelers diarrhea can be treated with TMP-SMX
F (travelers diarrhea norrrr)
37
TMP-SMX can be used as ALTERNATIVE TREATMENT FOR
Nocardia Brucellosis Stenotrophomonas
38
Prophylaxis against Toxoplasma in HIV px.
TMP-SMX
39
TMP ------- the toxicity of sulfonamides
Extends
40
Hematological reactions caused by TMP-SMX
Anemia Coag. disorders Granulocytopenia Purpura Sulfhemoglobinemia
41
Type of purpura in the use of TMP-SMX
Henoch-Schonlein
42
HIV adverse effects in TMP-SMX tx.
Sensitivity reactions including: Steven Johnsons syndrome Sweet syndrome
43
T/F: Jaundice, permanent renal impairment and hyperkalemia are adverse effects of TMP-SMX
True
44
Warfarin and TMP-SMX can lead to
Excessive coagulation
45
Methotrexate and agents that increase potasium or suppress bone marrow should be (avoided/added) when using TMP-SMX
Avoided
46
TMP-SMX resistance is mostly due to
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
Quinolones are
Nucleic acid synthesis inhibitors
48
Name the 8 quinolones
Nalidixic Acid Norfloxacin Ciprofloxacin Ofloxacin Levofloxacin Gatifloxacin Moxifloxacin
49
All quinolones are IV and PO administered, which is the one that is also available in opthalmic preparations?
Gatifloxacin
50
Norfloxacin has limited use in the treatment of...
UTIs and GI infections
51
Which quinolone has enhanced potency activity against gram-positive organisms and is not available in the US anymore
Gatifloxacin
52
Quinolone that is very active against B. fragilis
Moxifloxacin
53
Quinolones MOA
Inhibition of gyrase-mediated DNA supercoiling (bacterial growth is inhibited too)
54
In gram positive bacteria, what is the quinolones main SOA?
Topoisomerase IV
55
In gram negative bacteria, what is the main target of quinolones?
DNA gyrase
56
Main targets of nalidixic acid (KEEPS)
Gram negative bacteria: E. coli Klebsiella spp. Enterobacter Proteus Salmonella Shigella
57
Nalidixic acid is not effective against
P. aeruginosa Gram-positive bacteria Anaerobes
58
Therapeutic uses of nalidixic acid
UTIs by Gram negative bacteria Cystits and pyelonephritis
59
------ has the same uses of nalidixic acid + traveler's diarrhea
Norfloxacin
60
Quinolone that has the same therapeutic uses as norfloxacin + Salmonella typhi, prophylaxis of anthrax and turalemia due to yersinia pestis
Ciprofloxacin
61
Besides being useful in TB and Mycobacterium avium (in px with AIDS), what are the main uses of Ciprofloxacin?
Cystic fibrosis - Pseudomonas aeruginosa Nosocomial pneumonia
62
For cases of nosocomial pneumonia, ciprofloxacin should be combined with a
B-lactam
63
Gatifloxacin therapeutic uses
Upper and lower UTIs Cystitis and pyelonefritis Prostatitis
64
Moxifloxacin has excellent activity against...
S pneumoniae H influenzae Atypical respiratory pathogens (Bacteroidis fragillis) and intestinal anaerobes
65
Moxifloxacin is mostly used for
CAP Diabetic foot
66
Levofloxacin therapeutic uses
Same as norfloxacin + chlamydial urethritis/cervicitis + salmonella typhi
67
Nalidixic acid can cause ------ in G6PD deficiency
Hemolytic anemia
68
Tendinitis/tendon rupture QT prolongation CNS effects Photosensivity are adverse effects of
Quinolones
69
Quinolones and food
May delay time for peak concentrations
70
When should quinolones be avoided?
Nursing infants Treatment for Shiga-producing E. coli
71
Cations like calcium, iron and aluminium should/shouldn't be taken at the same time that PO quinolones BECAUSE
They reduce systemic bioavaliability
72
In quinolones resistance, plasmids can transfer _______ chromosomal genes that encode --------------
Genes DNA gyrase and topoisomerase IV
73
Resistance MOA of quinolones can develop through
Through mutations in the bacterial chromosomal genes encoding DNA gyrase and topoisomerase IV
74
Plasmids can transfer genes that encode _________ proteins or alter the quinolone
Proteins
75
Quinolones resistant microorganisms
E. coli Pseudomonas Staphylococci