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Botany > PHARMACO - Macrolides > Flashcards

PHARMACO - Macrolides Flashcards

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
Q

antibiotic not capable of inhibiting cytochrome P450

A

azithromycin

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26
Q

is erytho still commonly used?

A

not anymore because of azithro and clarithro

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27
Q

antibiotic that promotes the effect of other drug because it inhibits Cyt P450

A

erythromycin

and clarithyromycin

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28
Q

drug against
 Gram (+) cocci like pneumococci (not penicillin-resistant S. pneumoniae [PRSP])
 Beta-lactamase-producing staphylococci (not Methicillin-resistant S. aureus [MRSA] strains)

A

erythromycin

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29
Q

drug of choice for the Prophylaxis against and treatment of M. avium complex

A

clarithromycin

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30
Q

Component for drug regimens for ulcers caused by H. pylori

A

clarithromycin

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31
Q

macrolide for neisseria

A

azithromycin

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32
Q

 Long half-life, single dose is effective

 Urogential infections caused by C. trachomatis

A

azithromycin

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33
Q

 4-day course is effective for community-acquired pneumonia (CAP

A

azithromycin

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34
Q 
identify which antibiotic causes this toxicity
	GI irritation is common
	Stimulation of motolin receptors
	Skin rashes
	Eosinophilia
A

macrolides

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35
Q

toxicity caused by  Erythromycin estolate

A

 Hypersensitivity-based acute cholestatic hepatitis

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36
Q

 Hypersensitivity-based acute cholestatic hepatitis is rare in

A

children

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37
Q

there is increased risk of Hypersensitivity-based acute cholestatic hepatitis

A

pregnant patients

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38
Q

 Inhibits several forms of cytochrome P450

A

Erythromycin and clarithromycin

39
Q

 Increases the plasma levels
 Anticoagulants Carbamazepine
 Cisapride Digoxin
 Theophylline

A

Erythromycin and clarithromycin

40
Q

macrolide whose similar drug interactions of erythromycin can occur

A

clarithromycin

41
Q

 Structure of lactone ring is slightly different

A

azithromycin

42
Q

Drug interactions are uncommon because it Does not inhibit hepatic cytochrome P450

A

azithromycin

43
Q

why are drug interactions uncommon for azithromycin

A

because it Does not inhibit hepatic cytochrome P450

44
Q

prototype drug of ketolides

A

 Telithromycin

45
Q

 Structurally related to macrolides

A

Telithromycin

46
Q

 Same MOA as erythromycin

 Similar spectrum of antimicrobial activity

A

Telithromycin

47
Q

advantage of Telithromycin over macrolides

A

 Some macrolide-resistant strains are susceptible to telithromycin because it binds more tightly to ribosomes

48
Q

why are Some macrolide-resistant strains susceptible to telithromycin (2)

A

because it binds more tightly to ribosomes

because it is a Poor substrate for bacterial efflux pump that mediate resistance

49
Q

dosing regimen for telithromycin

A

orally once daily

50
Q

mode of elimination for telithromycin

A

bile and urine

51
Q

Inhibitor of cytochrome CYP3A4 isozyme

A

telithromycin

52
Q

used for CAP and other upper respiratory tract infections

A

telithromycin

53
Q

drugs (2) for community acquired pneumonia

A

telithromycin and azithromycin

54
Q

prototype of lincosamides

A

clindamycin

55
Q

MoA of clindamycine

A

 Inhibit bacterial protein synthesis

 Mechanism similar to macrolides but are not chemically related

56
Q

 Mechanism similar to macrolides but are not chemically related

A

clindamycin

57
Q

 Resistance to clindamycin (2)

A

 Methylation of the binding site on 50S

 Enzymatic inactivation

58
Q

 Cross-resistance with macrolides is —–

A

common

59
Q

is clindamycin orally absorbed

A

yes

60
Q

tissue penetration of clindamycin

A

good

61
Q

mode of elimination of clindamycin

A

partly by metabolism and partly by biliary and renal excretion

62
Q

clinical use of clindamycin

A

severe infections caused by anaerobes like bacteriodes

63
Q

drug for severe infections caused by anaerobes like bacteriodes

A

clindamycin

64
Q

 Backup drug against gram (+) cocci

A

clindamycin

65
Q

 Prophylaxis for endocarditis in valvular heart disease who are allergic to penicillin

A

clindamycin

66
Q

 Active against P. carinii and T. gondii

A

clindamycin

67
Q

 Superinfection such as C. difficile and pseudomembranous colitis caused by clindamycin is Treated by

A

oral vancomycin

68
Q

identify which antibiotic has these toxicities
 GI irritation Skin rashes
 Neutropenia Hepatic dysfunction

A

clindamycin

69
Q

toxicities of clindamycin

A

 GI irritation Skin rashes

 Neutropenia Hepatic dysfunction

70
Q

Antibiotic used for gram (-) anaerobe

A

clindamycin

71
Q

 Combination of 2 streptogramins

A

 Quinupristin-dalfopristin

72
Q

MoA of Quinupristin-dalfopristin

A

BACTERICIDAL

73
Q

has a postantibiotic effect

A

Quinupristin-dalfopristin (and aminoglycosides)

74
Q

 Duration of bacterial activity is longer than the half-lives of the 2 compounds

A

Postantibiotic effect of Quinupristin-dalfopristin

75
Q

 Used for PRP, MRSA and vancomycin-resistant staphylococci (VRSA) and resistant E. faecium

A

Quinupristin-dalfopristin

76
Q

 First of a new class of antibiotics

A

linezolid

77
Q

a class of a new antibiotics

A

oxazolidinone

78
Q

newest antibiotic in the market

A

linezolid

79
Q

for Gram (+) cocci, including strains resistant to beta-lactams and vancomycin

A

linezolid

80
Q

 Binds to a unique site on the 23S ribosomal RNA of 50S

A

linezolid

81
Q

 No cross-resistance with other protein synthesis inhibitors

A

linezolid

82
Q

does linezolid have cross-resistance with other protein synthesis inhibitors

A

no

83
Q

med preparationsof linezolid

A

oral and parenteral forms

84
Q

drug with RARE resistance

A

linezolid

85
Q

toxicity of linezolid

A

 Thrombocytopenia and neutropenia occur in immunocompromised patients

86
Q

resistance to linezolid

A

 Decreased affinity of the drug for its binding site

87
Q

prototype drug of macrolides

A

erythromycin

88
Q

mode of elimination of azithromycin

A

urinary excretion

89
Q

a macrolide that can be given to treat chlamydia

A

azithromycin, erythromycin, clarithromycin

90
Q

which drug to give between doxycycline and azithromycin for chlamydia

A

azithromycin because you only give 1 dose

91
Q

causes severe epigastric pain

A

erythromycin

92
Q

advantage of linezolid

A

no cross resistance with other protein synthesis inhibitors

93
Q

if allergic to penicillin and cephalosporin, what drug must be given next

A

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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