PHARMACO - Macrolides Flashcards Preview

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Flashcards in PHARMACO - Macrolides Deck (93):
1

 Large cyclic lactone ring structure with attached sugars

 Erythromycin , azithromycin, and clarithromycin

2

 Good oral bioavailability

Erythromycin , azithromycin, and clarithromycin

3

oral bioavailability of Erythromycin , azithromycin, and clarithromycin

good

4

tissue distribution of Erythromycin , azithromycin, and clarithromycin

wide: Distributed to most body tissues

5

macrolide whose Absorption is impeded by food

azithromycin

6

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

azithromycin

7

half-life of azithromycin

2-4 days

8

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

azithromycin

9

macrolideS whose Elimination of intact drug is rapid

 Erythromycin and clarithromycin

10

mode of excretion of Erythromycin

biliary excretion

11

mode of excretion of Hepatic metabolism and urinary excretion

Clarithromycin

12

half-life of Clarithromycin

2-5 hours

13

half-life of Erythromycin

2-5 hours

14

macrolide used against chlamydia

erythromycn

15

 Preparations erythromycin


Erythromycin stearate
Erythromycin lactobionate
Erythromycin estolate

16

-Best absorbed oral preparation of erythromycin

Erythromycin estolate

17

spectra of activity of azithromycin and clarithromycin

same with erythro but with GREATER activity

18

Mode of resistance of macrolides in gram +

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

19

Mode of resistance of macrolides to enterobacteriaceae

Formation of drug-metabolizing esterases

20

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

complete

21

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

yes because cross-resistance between individual macrolides is complete

22

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

PARTIAL

23

enzyme found in the liver
needed to metabolize other drugs

cytochrome P450

24

capable of inhibiting cytochrome P450

erythromycin
and clarithyromycin

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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