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Pharmacology 4090 > AMDs > Flashcards

AMDs Flashcards

(102 cards)

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1
Q

6 groups of AMDs

A

Beta-lactams, aminoglycosides, tetracyclines, sulfonamides, macrolides, fluoroquinolones

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2
Q

Bacteriostatic to bactericidal

A

Can become bactericidal at high enough concentrations

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3
Q

Time-dependent AMDs

A

Efficacy is associated with the length of time the drug concentration stays above the MIC

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4
Q

Concentration-dependent AMDs

A

Efficacy depends on peak concentration

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5
Q

Relationship between resistance and use

A

Positive

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6
Q

Classes of antimicrobial sensitivity

A

Good, variable, moderate, resistance

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7
Q

Are bacteria the same level of sensitivity to all drugs

A

No!

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8
Q

AMD mechanisms

A

Damage membrane s inhibit cell wall synthesis, inhibit protein synthesis, inhibit folic acid synthesis, damage DNA

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9
Q

Serial dilution

A

Keep diluting drug concentration by 50% and then seed with standard amount of bacteria → let grow and assess for cloudiness of tubes

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10
Q

MIC

A

Concentration where there’s no visible growth but some bacteria may be alive

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11
Q

MBC

A

Concentration that sterilized the tube

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12
Q

Kirby-bauer test

A

Paper discs have different drugs and are placed on bacterial lawn to see zone of inhibition

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13
Q

Culture and sensitivity testing

A

Done for life-threatening infections, but takes a long time

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14
Q

Considerations when selecting drugs

A

Bacterial sensitivity, bacteriostatic versus bactericidal, adverse effects, distribution, and cost

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15
Q

Diseases w/ special considerations

A

Osteomyelitis, foreign bodies, abscess, intracellular pathogens, obstructed areas, immunodeficiency

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16
Q

Prophylactic uses of AMDs

A

High risk of infection after trauma, immune or anatomical defects, surgery

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17
Q

AMDs during surgery

A

Want to have adequate levels at the time of incision

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18
Q

Criteria for selecting AMDs

A

Spectrum, mechanism, adverse effects, distribution and elimination, line, cost, route of admin

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19
Q

Health Canada AMD drug categories

A

1,2,3, 4

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20
Q

Category 1

A

Very high importance to human health; life and death situation

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21
Q

Category 2

A

High importance; some alternatives available;drug of choice for serious infections

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22
Q

Category 3

A

Medium importance; not preferred for serious infections

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23
Q

Category 4

A

Low importance; not used in humans

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24
Q

Beta-lactams

A

Penicillins and cephalosporins

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25
Beta-lactam ring
In beta-lactams, gives activity, susceptible to temperature changes
26
Beta-lactamases/penicillinases
Enzymes from some bacteria that destroy beta-lactams
27
Beta-lactam mechanism
Bind to and inactivate the transpeptidase enzyme that builds the cell wall → cell lysis
28
Types of penicillin
Narrow spectrum, penicillinase resistant, extended spectrum
29
Narrow-spectrum penicillin
Penicillin G
30
Penicillinase-resistant penicillin
Dicloxacillin
31
Extended spectrum penicillins
Ampicillin, amoxicillin
32
Targets of penicillin G
Gram positive aerobes, anaerobes
33
Pk of penicillin G
Not acid stable so it has to be given parenterally
34
Target of dicloxacillin
Penicillinase-producing staphylococci
35
Pk of dicloxacillin
Acid stable so it can be given orally!
36
Targets of amoxicillin
Gram positive aerobes, gram negative aerobes, and anaerobes
37
Pk of amoxicillin
Acid stable with a very high oral bioavailability
38
Potentiated penicillin
Amoxicillin plus clavulanic acid to resist penicillinases; make the penicillin second line treatment
39
Distribution of penicillins
Everywhere except CNS and prostate
40
Elimination of penicillins
Excreted unchanged in urine, mostly by active secretion
41
Resistance against penicillins
Gram-negative cell wall, acquired penicillinases
42
Adverse effects of penicillins
Hypersensitivity (don't use topically), seizures
43
Cephalosporins
Type of beta-lactam with very similar mechanism of action, distribution, elimination, and adverse effects to penicillins
44
Are cephalosporins sensitive to penicillinases?
No, but they are sensitive to beta-lactamases
45
Cephalosporin generations
1,2,3,4
46
1st generation cephalosporins spectrum and acid stability
Identical spectrum to amoxicillin, not acid stable (most)
47
3rd generation cephalosporins spectrum
Less effective against gram positive aerobes and anaerobes, but more effective against gram negative aerobes; some can readily cross the BBB
48
Aminoglycosides uses
Systemic administration for dangerous gram-negative aerobes, or topical use
49
Most commonly used aminoglycoside
Gentamicin - highly ionized so isn't absorbed orally or topically
50
Aminoglycoside mechanism of action
Irreversibly inhibit protein synthesis and cause production of wrong peptides that produce poring → lysis
51
Spectrum of aminoglycosides
Gram-negative aerobes, staph, mycoplasma
52
Types of resistance against aminoglycosides
Structural (entry requires oxygen-dependent transport so anaerobes are resistant), aminoglycosidases
53
Main adverse effects of aminoglycosides
Mephrotoxicity and ototoxicity
54
Nephrotoxicity from aminoglycosides
Every patient will have some renal damage but it usually isn't a problem unless they are dehydrated, have renal disease, or are elderly
55
Washout period
Give single dose of aminoglycosides and let concentrations fall over the day
56
Ototoxicity from aminoglycosides
Damage to cranial nerve 8 and hair cells that can cause permanent, high-frequency hearing loss but the vestibular system is okay
57
Susceptibility to ototoxicity
Inherited susceptibility for severe hearing loss, most people will just have a little
58
Tetracycline mechanism of action
Reversible inhibit bacterial protein synthesis (bacteriostatic)
59
Tetracycline spectrum
Basically all atypical bacteria
60
Atypical bacterial infections
Rickettsia, chlamydia, mycoplasma
61
Tetracycline distribution
Water-soluble don't readily enter cells or CNS, lipid-soluble (doxycycline) enters cells
62
Doxycycline
Lipid-soluble tetracycline important for intracellular pathogens
63
Tetracycline elimination
Water-soluble are excreted in urine and metabolized in liver, lipid-soluble are entirely metabolized in liver and secreted in bile
64
Resistance to tetracyclines
Efflux pump; can be overwhelmed by high topical doses
65
Adverse effects of tetracyclines
Renal damage, photosensitivity, incorporation into teeth and bones
66
What line are tetracyclines?
First!
67
Effectiveness of sulfonamides alone
Largely ineffective
68
Diaminopyrimidine inhibitors
Trimethoprim (TM)
69
Potentiated sulfonamides
Trimethoprim plus sulfonamides (TMS or co-trimoxazole)
70
Are sulfonamides bactericidal or bacteriostatic
Bactericidal
71
Mechanism of action of sulfonamides
Competitively Inhibit dihydropteroate synthetase, which helps synthesize folic acid from PABA
72
Mechanism of action of trimethoprim
Competitively inhibit dihydrofolate reductase, which helps synthesize topic acid later in the pathway
73
Why potentate sulfonamides are more effective
You competitively inhibit 2 of the enzymes in the pathway and resistance to both of these enzymes is less common
74
Why sulfonamides are ineffective with pus
Pus has a lot of PABA so they will be outcompeted
75
Spectrum of sulfonamides
Atypical bacteria; can also be used against lower UTI infections
76
Distribution of sulfonamides
To all tissues
77
Elimination of sulfonamides
Some excreted unchanged in urine, some metabolized in liver; metabolites accumulate in kidneys
78
Resistance to sulfonamides
Can acquire different dihydropteroate synthetase or dihydrofolate reductase enzymes
79
Adverse effects of sulfonamides
Hypersensitivity and renal damage
80
Most recent class of AMDs
Fluoroquinolones
81
Most common fluoroquinolone
Ciprofloxacin
82
Fluoroquinolone mechanism of action
Damage DNA by inhibiting DNA gyrases and topoisomerases
83
Spectrum of fluoroquinolones
Gram negative aerobes, staph, and some atypical (no anaerobes)
84
Pharmacokinetics of fluoroquinolones
Oral bioavailability ~100%, very long half-life, concentrates in lung, renal excretion
85
Adverse effects of fluoroquinolones
Severe cartilage damage, tendon rupture, reduction of seizure threshold, phototoxicity
86
Resistance to fluoroquinolones
Mutations in DNA gyrases and topoisomerases that stop fluoroquinolones from binding
87
Fluoroquinolone line
Only second
88
Macrolides mechanism of action
Inhibit protein synthesis reversibly
89
Pharmacokinetics of macrolides
Penetrate cells easily, concentrate in lung, older have very short half-life while newer have very long, erythromycin can inhibit p450 enzymes
90
Erythromycin
Oldest macrolide
91
Spectrum of erythromycin
Closest to broad spectrum: gram positive aerobes, anaerobes, some gram negative aerobes, some atypical
92
Spectrum of newer macrolides
Mostly gram negative aerobes, somewhat affects everything else (good for community-acquired bacterial pneumonia)
93
Macrolide resistance
Very effective macrolide efflux pump
94
Adverse effects of macrolides
Tissue irritation, vomiting because erythromycin stimulates motilin receptors
95
Divalent cations
Inhibit oral absorption of tetracyclines
96
Spectrum of chloramphenicol
Broad
97
Routes of admin of chloramphenicol
Basically all
98
Distribution of chloramphenicol
All except prostate
99
What tissue chloramphenicol penetrates best
Cornea
100
Major adverse effect of chloramphenicol
Fatal aplastic anemia
101
Mechanism of action of chloramphenicol
Inhibits protein synthesis (bacteriostatic)
102
When to use chloramphenicol
In fatal or crippling infections where there are no other options

Pharmacology 4090 (11 decks)

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