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PHARMACO - Macrolides Flashcards

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1
Q

 Large cyclic lactone ring structure with attached sugars

A

 Erythromycin , azithromycin, and clarithromycin

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2
Q

 Good oral bioavailability

A

Erythromycin , azithromycin, and clarithromycin

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3
Q

oral bioavailability of Erythromycin , azithromycin, and clarithromycin

A

good

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4
Q

tissue distribution of Erythromycin , azithromycin, and clarithromycin

A

wide: Distributed to most body tissues

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5
Q

macrolide whose Absorption is impeded by food

A

azithromycin

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6
Q

macrolide which is Eliminated slowly in the urine mainly as unchanged drug

A

azithromycin

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7
Q

half-life of azithromycin

A

2-4 days

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8
Q

macrolide whose levels in tissues and phagocytes are higher than in plasma

A

azithromycin

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9
Q

macrolideS whose Elimination of intact drug is rapid

A

 Erythromycin and clarithromycin

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10
Q

mode of excretion of Erythromycin

A

biliary excretion

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11
Q

mode of excretion of Hepatic metabolism and urinary excretion

A

Clarithromycin

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12
Q

half-life of Clarithromycin

A

2-5 hours

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13
Q

half-life of Erythromycin

A

2-5 hours

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14
Q

macrolide used against chlamydia

A

erythromycn

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15
Q

 Preparations erythromycin

A

Erythromycin stearate
Erythromycin lactobionate
Erythromycin estolate

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16
Q

-Best absorbed oral preparation of erythromycin

A

Erythromycin estolate

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17
Q

spectra of activity of azithromycin and clarithromycin

A

same with erythro but with GREATER activity

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18
Q

Mode of resistance of macrolides in gram +

A

 Efflux pump mechanisms

 Production of methylase that adds methyl group to the ribosomal binding site

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19
Q

Mode of resistance of macrolides to enterobacteriaceae

A

Formation of drug-metabolizing esterases

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20
Q

 Cross-resistance between individual macrolides is complete incomplete partial?

A

complete

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21
Q

if a microorganism is resistant to erythromycin, will it also be resistant to clarithromycin or azithromycin

A

yes because cross-resistance between individual macrolides is complete

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22
Q

cross-resistance with other drugs that bind to the same site occur in methylase-producing strains especially Clindamycin and streptogramins, complete incomplete partial?

A

PARTIAL

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23
Q

enzyme found in the liver

needed to metabolize other drugs

A

cytochrome P450

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24
Q

capable of inhibiting cytochrome P450

A

erythromycin

and clarithyromycin

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25
antibiotic not capable of inhibiting cytochrome P450
azithromycin
26
is erytho still commonly used?
not anymore because of azithro and clarithro
27
antibiotic that promotes the effect of other drug because it inhibits Cyt P450
erythromycin | and clarithyromycin
28
drug against  Gram (+) cocci like pneumococci (not penicillin-resistant S. pneumoniae [PRSP])  Beta-lactamase-producing staphylococci (not Methicillin-resistant S. aureus [MRSA] strains)
erythromycin
29
drug of choice for the Prophylaxis against and treatment of M. avium complex
clarithromycin
30
Component for drug regimens for ulcers caused by H. pylori
clarithromycin
31
macrolide for neisseria
azithromycin
32
 Long half-life, single dose is effective |  Urogential infections caused by C. trachomatis
azithromycin
33
 4-day course is effective for community-acquired pneumonia (CAP
azithromycin
34
``` identify which antibiotic causes this toxicity  GI irritation is common  Stimulation of motolin receptors  Skin rashes  Eosinophilia ```
macrolides
35
toxicity caused by  Erythromycin estolate
 Hypersensitivity-based acute cholestatic hepatitis
36
 Hypersensitivity-based acute cholestatic hepatitis is rare in
children
37
there is increased risk of Hypersensitivity-based acute cholestatic hepatitis
pregnant patients
38
 Inhibits several forms of cytochrome P450
Erythromycin and clarithromycin
39
 Increases the plasma levels  Anticoagulants Carbamazepine  Cisapride Digoxin  Theophylline
Erythromycin and clarithromycin
40
macrolide whose similar drug interactions of erythromycin can occur
clarithromycin
41
 Structure of lactone ring is slightly different
azithromycin
42
Drug interactions are uncommon because it Does not inhibit hepatic cytochrome P450
azithromycin
43
why are drug interactions uncommon for azithromycin
because it Does not inhibit hepatic cytochrome P450
44
prototype drug of ketolides
 Telithromycin
45
 Structurally related to macrolides
Telithromycin
46
 Same MOA as erythromycin |  Similar spectrum of antimicrobial activity
Telithromycin
47
advantage of Telithromycin over macrolides
 Some macrolide-resistant strains are susceptible to telithromycin because it binds more tightly to ribosomes
48
why are Some macrolide-resistant strains susceptible to telithromycin (2)
because it binds more tightly to ribosomes | because it is a Poor substrate for bacterial efflux pump that mediate resistance
49
dosing regimen for telithromycin
orally once daily
50
mode of elimination for telithromycin
bile and urine
51
Inhibitor of cytochrome CYP3A4 isozyme
telithromycin
52
used for CAP and other upper respiratory tract infections
telithromycin
53
drugs (2) for community acquired pneumonia
telithromycin and azithromycin
54
prototype of lincosamides
clindamycin
55
MoA of clindamycine
 Inhibit bacterial protein synthesis |  Mechanism similar to macrolides but are not chemically related
56
 Mechanism similar to macrolides but are not chemically related
clindamycin
57
 Resistance to clindamycin (2)
 Methylation of the binding site on 50S |  Enzymatic inactivation
58
 Cross-resistance with macrolides is -----
common
59
is clindamycin orally absorbed
yes
60
tissue penetration of clindamycin
good
61
mode of elimination of clindamycin
partly by metabolism and partly by biliary and renal excretion
62
clinical use of clindamycin
severe infections caused by anaerobes like bacteriodes
63
drug for severe infections caused by anaerobes like bacteriodes
clindamycin
64
 Backup drug against gram (+) cocci
clindamycin
65
 Prophylaxis for endocarditis in valvular heart disease who are allergic to penicillin
clindamycin
66
 Active against P. carinii and T. gondii
clindamycin
67
 Superinfection such as C. difficile and pseudomembranous colitis caused by clindamycin is Treated by
oral vancomycin
68
identify which antibiotic has these toxicities  GI irritation Skin rashes  Neutropenia Hepatic dysfunction
clindamycin
69
toxicities of clindamycin
 GI irritation Skin rashes |  Neutropenia Hepatic dysfunction
70
Antibiotic used for gram (-) anaerobe
clindamycin
71
 Combination of 2 streptogramins
 Quinupristin-dalfopristin
72
MoA of Quinupristin-dalfopristin
BACTERICIDAL
73
has a postantibiotic effect
Quinupristin-dalfopristin (and aminoglycosides)
74
 Duration of bacterial activity is longer than the half-lives of the 2 compounds
Postantibiotic effect of Quinupristin-dalfopristin
75
 Used for PRP, MRSA and vancomycin-resistant staphylococci (VRSA) and resistant E. faecium
Quinupristin-dalfopristin
76
 First of a new class of antibiotics
linezolid
77
a class of a new antibiotics
oxazolidinone
78
newest antibiotic in the market
linezolid
79
for Gram (+) cocci, including strains resistant to beta-lactams and vancomycin
linezolid
80
 Binds to a unique site on the 23S ribosomal RNA of 50S
linezolid
81
 No cross-resistance with other protein synthesis inhibitors
linezolid
82
does linezolid have cross-resistance with other protein synthesis inhibitors
no
83
med preparationsof linezolid
oral and parenteral forms
84
drug with RARE resistance
linezolid
85
toxicity of linezolid
 Thrombocytopenia and neutropenia occur in immunocompromised patients
86
resistance to linezolid
 Decreased affinity of the drug for its binding site
87
prototype drug of macrolides
erythromycin
88
mode of elimination of azithromycin
urinary excretion
89
a macrolide that can be given to treat chlamydia
azithromycin, erythromycin, clarithromycin
90
which drug to give between doxycycline and azithromycin for chlamydia
azithromycin because you only give 1 dose
91
causes severe epigastric pain
erythromycin
92
advantage of linezolid
no cross resistance with other protein synthesis inhibitors
93
if allergic to penicillin and cephalosporin, what drug must be given next
macrolides since they are protein synthesis inhibitors not aminoglycosides since they do not have oral preparation not chloramphenicol since they are toxic not tetracycline because not very common

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