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