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MED ORG LEC > QUINOLONES > Flashcards

QUINOLONES Flashcards

MIDTERM QUIZ 2

1
Q

What does the quinolone antibiotics target

A

bacterial DNA gyrase and topoisomerase IV

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2
Q

what is the primary target for many gram negative bacteria

A

DNA gyrase

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3
Q

for many gram positive bacteria what is the primary target

A

topoisomerae IV

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4
Q

the quinolones inhibit what

A

gyrase-mediated DNA supercoiling

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5
Q

controls potency

A

R1

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6
Q

close to gyrase binding site

A

R2

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7
Q

controls potency, adds grampositive activity

A

R5

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8
Q

Controls gyrase and bacterial potency

A

F

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9
Q

Controls potency, spectrum and pharmacokinetics

A

R7

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10
Q

what are the drugs that are isosteric heterocyclic groupings

A

norfloxacin, ciprofloxacin, lomefloxacin

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11
Q

Naphthyridines

A

nalidixic and cinoxacin

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12
Q

two classes of quinolones

A

nalidixic acid and enoxacin

Broad spectrum fluoroquinolones

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13
Q

enumerate 4 fluoroquinolones

A

norfloxacin
ciprofloxacin
ofloxacin
levofloxacin (hemihydrate)

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14
Q
  • a yellow crystalline powder
  • soluble in water
A

norfloxacin

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15
Q

norfloxacin is effective against

A

gram negative bacteria and gram positive bacteria

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16
Q

the flouring atom in norfloxacin provides

A

increased potency against gram psotive bacteria

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17
Q

improves antipseudomonal activty

A

piperazine moiety

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18
Q

norfloxacin is also indicated for the treatment of

A

UTI

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19
Q

UTI caused by

A

E. coli
K. pneumoniae
E. cloacae
P. mirabilis
indole positive Proteus species

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20
Q

agent choice for bacterial gastroenteritis

A

ciprofloxacin

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21
Q

bacterial gastroenteritis caused by

A

gram-negative bacili like E. coli, salmonella spp., shigella spp., vibrio spp., and aeromonas hydrophilia

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22
Q

What is the chemical formula of ofloxacin

A

9-flouro - 2,3

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23
Q

Metabolized , and rapidly excreted after oral administration

A

Nalidixic acid

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24
Q

What metabolite is significantly more active than the parent compound

A

7-Hydroxymethyl metabolite

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25
Is a close congener (isostere) of oxolinic acid
cinobac
26
Appears to be more completely absorbed and less protein bound than nalidixic acid
cifloxacin
27
Activity something arrangement potency kemerut
Cyclopropane > 1,2 - diflourotoulene ~ tertiary butyl > Cyclo butyl > ethyl ## footnote O or N reduce acivity
28
Responsible for the basicity of urine
Ammonia
29
protozoans
Giardia intestinal is Trichomonas vaginalis Trypanesoma gambiense Leishmanis spp
30
Brand names for pentamidine isethionate
Nebupent, Pentam 300
31
Uses of pentamidine isethionate
Pneumonia by P. Carinii African trypanosomiasis Visceral leishmaniasis
32
For African trypanosomiasis Effective against meningoencephalitis forms
Melarsoprol
33
Melarsorol is prepared by
Reduction of a pentavalent arsanilate to the trivalent arsenoxide followed by reaction of the latter with 2,3-dimercapto-1-prpanol British anti-lewisite
34
Nitromidazole derivative tha is used for the tx of Chagas disease
Benzonidazole
35
Adverse effects of benzonidazole
Peripheral neuropathy Bone marrow depression Allergic reactions
36
Brand-name for nifurtimox
lampit
37
Nifurtimox is a
Anti bacterial Antifungal antiprotozoal
38
Use fo acute and chronic from of south American trypanosomiasis
Nifurtimox (lampit)
39
Cycle of African trypanosomiasis
Tse-tse fly entry into circulation CNS damage Transmission to other hosts
40
Drugs for gardiasis
Metronidazole Tinidazole Mepacrine albendazole
41
Brand name for metronidazole
flagyl
42
IUPAC name fr metronidazole
2-methyl-5-nitroimidazole-1-ethanol
43
Metronidazole is effective only againts
anaerobic bacteria
44
Most useful group of antiprotozoal nitroimidazole derivatives that have been synthesize \
metronidazole
45
The ability of metronidazole to act as a radiosensitizing agents is related to its
Reduction potential
46
Potential reactive intermediates of metronidazole
Nitroxide, nitroso, hydroxylamine and amine
47
Albendazole is useful for
New and Old hookworm
48
Active form albendazole
Sulfoxide conjugated
49
Increase absorption with what - Albendazole
Fatty meals
50
Drugs for trichomoniasis
Metronidazole Tinidazole
51
Antihelmitnhs drugs
Albendazole Piperazine Praziquantel Ivermectin Thiabendazole DEC (diethylcarbamazine)
52
Piperazine blocks
Ach response
53
Broad spectrum antifungal Topically for the treatment of tinea infections
clotrimazole
54
More effective against torulopsis glabrata
tioconazole
55
56
Brand name for miconazole
daktarin
57
Azole antifungals
Clotrimazole Tioconazole Miconazole Ketoconazole Itraconazole Fluconazole
58
Effective against trematodes
Praziquantel
59
Agent choice for infections caused by schistosomes, fasciolopsiasis, clonorchiasis
praziqantel
60
Blood fuke
schistosomes
61
fasciolopsiasis
Intestinal fluke
62
cloorchiasis
Chinese liver fluke
63
fasciolasis
Sheep liver fluke
64
opisthorchosis
Liver fluke
65
paragonimiasis
Lung fluke
66
Mcreases the permeability of the membranes of parasite cells for calcium ions
Praziquantel - resulting in paralysis
67
A mixture of derivatives of avermectins B1a and B1b prepared by catalytic hydrogention
ivermectin
68
Stimulate GABA = increase inhibitory effect
MOA of ivermectin
69
Treatment of Onchocerciasis
ivermectin
70
River blindness
onchocerciasis
71
Brand name for thiabendazole
Mintezol
72
Forms complex with metalions
thiabendazole
73
Block glucose uptake by the parasite leading to decrease production of energy and subsequent parasite immobilixation
albendazole
74
Albendazole is treatment for
Roundworm,pinworm, hookworm infection Alternative treatment of threadworm, filariasis Hydatid disease and cysticercosis
75
Brand name of mebendazole
vermox
76
Inhibits cell division and irreversibly blocks uptake
mebendazole
77
Effective against nematode infections
mebendazole
78
Tx for filariasis
Diethylcarbamazine citrate
79
Depolarizing neuromuscular locking agent
Pyrantel pamoate
80
Tx for infestations caused by pinworms and rundworms (ascariasis))
Pyrantel pamoate
81
Tx of asptomatic carriers of E. Hystolytica, amoebiasis acting on tissue
Diloxanide (furamide, eutamide)
82
With Ability to chelate metals
8-hydroxyquinoline
83
Used as topical antiinfectives
Solutions of acids and oxine
84
Acute and chronic amebiasis
idoquinol
85
Effective against trematodes
Praziquantel
86
Protoplasmic posions
Emetine and dehydroemetine
87
Direct amebicidial action
Emetine and dehydroemetine
88
Similar with ubiwuinone
atovaquone
89
Interfere with the function of electron transport enzymes
atovaquone
90
chelation
dimercaprol
91
Inhibits protein synthesis by preventing
Protein elongation
92
From sarcoptes scabiei
scabies
93
Agents that eliminates head/body/crab lice
Antipedicular
94
Naturally occuring ester form of Peru balsam
Benzyl benzoate
95
Halogenated carbon prepared by chlorination of benzene
lindane\ MOA Direct contact poison Fumigan effect Acts as stomachic Poison
96
Treatment of headlice (lethal action)
Permethrin
97
Two distinc populations of bacilii
M. Tuberculosis M. Leprae
98
Regiment for 3-4 drugs for 6 months to 2 years
First line treatment
99
Reserve for multidrug resistant or unresponsive infection
Secon line treatment
100
Most potent drug for MTB
isoniazid
101
Active only on the growing tubercle bacili
isoniazid
102
Coadministration odf pyridoxine prevents it
Peripheral neuritis Isoniazid + pyridoxine (b6)
103

MED ORG LEC (3 decks)

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