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Protein Synthesis Inhibitors Flashcards

1
Q

What are the 2 main groups of protein synthesis inhibitors?

A
  1. 30s

2. 50s

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2
Q

What are the 2 types of 30s protein synthesis inhibitors?

A
  1. Tetracyclines

2. Aminoglycosides

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3
Q

What are Macrolides?

A

50s protein synthesis inhibitors

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4
Q

T or F: The bacterial ribosome is smaller than mammalian ribosome.

A

True
Bacterial: 70s
Mammalian: 80s

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5
Q

T or F: Mitochondrial ribosomes closely resemble the bacterial ribosome.

A

True

This is important because HIGH doses may cause toxic effects

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6
Q

What is the structure of Tetracyclines?

A

4 fused rings with a system of conjugated double bonds

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7
Q

Why is the structure of tetracyclines important?

A

If you change the ring substitutions, you change the drug

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8
Q

Name the 4 Tetracycline drugs.

A
  1. Tetracycline
  2. Demecycline
  3. Doxycycline
  4. Minocycline
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9
Q

What are the short acting Tetracyclines? And how is it administered?

A

Tetracycline!

PO

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10
Q

What is Minocycline? Short acting? Long? Intermediate? How is it given?

A

Long acting

PO/IV

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11
Q

What are the long acting tetracyclines? And how are they given?

A

These are the 2nd gen:

  1. Minocycline
  2. Doxycycline

PO/IV

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12
Q

What is the intermediate acting tetracycline? How is it administered?

A

Demecycline

PO

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13
Q

What is Tetracycline–cidal or static?

A

static

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14
Q

What is the MOA of Tetracycline?

A

Drug binds to the 30s ribosomal subunit and blocks access of the tRNA to the mRNA-ribosomal complex–ultimately inhibiting protein synthesis

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15
Q

T or F: Tetracyclines are extended spectrum.

A

False: they are broad spectrum

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16
Q

Name the 7 species of bacteria that Tetracyclines are used for?

A
  1. Gram (-)= cholera
  2. Rickettsia = Rocky Mountain Spotted fever
  3. Mycoplasma
  4. Chlamydia
  5. Amoeba
  6. Spirochetes = lyme disease
  7. Bacillis Anthracis
  8. Acne: Proprionibacterium
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17
Q

Which tetracyclines have enhanced antibacterial activity? Why are they better?

A

2nd generation: (long acting)
1. Minocycline
2. Doxycycline
They penetrate the bacterial cells better.

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18
Q

What is the “R” factor referring to?

A

The Resistance factor of tetracyclines.

  1. decreased influx of drug
  2. acquisition of an energy dependent efflux pathway
  3. binding site alterations
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19
Q

In which class of Tetracyclines is cross-resistance less of an issue?

A

2nd generation

  1. Minocycline
  2. Doxycycline
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20
Q

What impairs the absorption of Tetracyclines?

A
  1. Dairy products (Ca)
  2. Antacids (Mg, Al)
  3. Fe salts
  4. Bismuth Subsalicyclate
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21
Q

If a patient needs to take Bismuth Subsalicyclate, which Tetracycline would you prefer to administer because altered absorption will be less of an issue?

A

2nd Gen TCNs:

Doxycycline and Minoxycycline

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22
Q

What kind of absorption do the tetracyclines have?

A

incomplete but adequate oral absorption

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23
Q

Once administered to the patient, where do the tetracyclines distribute in the body?

A 
Into most tissues, but concentrate into: 
Liver,
Kidney, 
Spleen, and 
Skin
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24
Q

Are tetracyclines water or lipid soluble?

A

Lipid soluble

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25
Where else do tetracyclines tend to bind/distribute in the body?
Tend to bind to: Tissue undergoing calcification, such as-- teeth and bones, and they cross the placenta to get to jr
26
All tetracyclines have inadequate penetration into the CNS EXCEPT for--?
Minoxycycline
27
Where are most tetracyclines excreted?
TCNs excreted in the bile --> from here they go to the intestine --> from which they are partially reabsorbed to the kidney
28
If a patient is taking TCNs, where in the body would you expect to see the highest concentration of TCNs?
In the liver
29
Which medical condition should TCNs be avoided with? What TCN is the exception to this?
1. Avoid TCNs in Renal failure | 2. Doxycycline: does not accumulate in the kidneys of renal failure pts
30
If a patient is being treated for H. Pylori, and you decide to place them on triple therapy using TCN and Bismuth--How should you do this?
Bismuth 4x /d + TCN 4x/d + Metronidazole 3x/d + PPI po x 2 weeks
31
What is the alternate triple therapy method for peptic ulcer disease (H. Pylori) NOT using TCNs?
PPI + Amoxicillin (PCN) + Clarithromycin (Aminoglycoside) 2x/d po All of this: x 10 d
32
Which bacillary infections are treated with TCNs?
1. Brucellosis 2. Tularemia 3. Cholera 4. Traveler's Diarrhea
33
Which Chlamydial infections are treated with TCNs?
1. Psittacosis 2. Trachoma 3. Lymphogranuloma venereum
34
What is the causative agent of lyme disease and how do you treat it?
Borrelia burgdorferi | TCNs
35
What is the common causative agent for acne and how would you treat it?
Propionibacterium acne | TCNs
36
Which Mycobacterium do you treat with TCNs?
Ureaplasma
37
Which Rickettsial diseases do you treat with TCNs?
Spotted fevers Typhus Ehrlichiosis Q fever
38
What is a common adverse effect of TCNs? How do you control it? What could this effect ultimately cause if you are not careful as a practitioner?
GI upset Take with food; NOT dairy products The pt could end up with a superinfection of Staph or C. dif
39
A patient is experiencing tooth pigmentation and enamel hypoplasia; what is the most likely causative agent?
TCNs
40
General question: What is the period of greatest danger to teeth (when the patient is pregnant)? Why does this matter?
About mid-pregnancy (4-6 mo) | If the patient has an infection, avoid giving TCNs during this this time period
41
If a pregnant patient is prescribed TCN, what is a toxic effect that could occur in the fetus?
Fetal hepatoxicity (esp if mother is experiencing pyelonephritis)
42
In which TCNs is the patient more likely to develop photoxicity?
1. Tetracycline 2. Doxycycline 3. Demecocycline
43
What other antibiotics besides TCNs have phytotoxicity as an adverse effect?
1. Sulfonamides | 2. Quinolones
44
Which TCN has vestibular disturbances?
Minoxycyline
45
Which antibiotic has an adverse effect of pseudo tumor cerebri? (benign intracranial HTN with blurred vision)
General adv effect of ALL TCNs
46
What are 2 types of superinfections a patient can get from TCN administration?
1. Vaginal candidiasis | 2. Staphylococci, C. dif
47
Which drug should you not prescribe to patient 8 years of age or younger?
TCNs
48
T or F: Pregnant and lactating women are safe to take TCNs?
NO; they are contraindicated
49
What two drugs should you instruct your patient to avoid when you prescribe them TCNs? Why?
1. Divalent 2. Trivalent The cations from the drugs can chelate the tetracyclines
50
Why should a patient avoid taking TCNs while taking birth control?
Simultaneous use of oral contraceptives with TCNs can decrease conjugated estrogen levels and thus, decreasing efficacy
51
Nephrogenic diabetes insipidus has occurred with which TCN?
Demeclocycline
52
What is the MOA of Demeclocycline?
Inhibits ADH-induced water reabsorption
53
What is Demeclocycline's one indication? (that we discussed)
Used in the treatment of SIADH
54
Name the 6 Aminoglycosides.
1. Neomycin 2. Streptomycin 3. Gentamicin 4. Tobramycin 4. Amikacin 5. Netilmycin
55
How are the Aminoglycosides administered?
IM/IV once a day dosing | EXCEPT Neomycin--Topical
56
T or F: All Aminoglycosides can be taken orally, Neomycin is especially safe.
False: NONE of the Aminoglycosides are PO | Neomycin has the highest toxic level and is restricted to topical use
57
What are the Aminoglycosides used for?
Aerobic Gram (-) bacilli but have been replaced by: 1. 3rd gen Cephs 2. Fluoroquinolones 3. Imipenem/Cilastatin
58
T or F: All Aminoglycosides share similar spectrum of activity, efficacy, toxicity, and pharmacology.
True
59
Do Aminoglycosides have good oral absorption?
No
60
Do Aminoglycosides have good CNS penetration?
No
61
Do Aminoglycosides have good excretion via the kidneys or bile?
Kidneys and yes, it is rapid
62
Are Aminoglycosides cidal or static?
cidal
63
What is the method of action of Aminoglycosides?
irreversibly to the 30s ribosomal subunit to inhibit protein synthesis
64
Would you want to use an Aminoglycoside with a PCN?
Yes; they work synergistically
65
What is the Aminoglycoside antibacterial spectrum?
Aerobic gram (-) bugs only
66
What is Streptomycin specifically used for?
TB, plague, and tularemia | + PCN or Vancomycin = strep viridans endocarditis
67
How would you treat strep viridans endocarditis?
Streptomycin + PCN or Vancomycin
68
What are some ways aerobic gram (-) bacteria become resistant to Aminoglycosides?
1. decrease the uptake of the drug via an anaerobic environment 2. altered binding site o 30S ribosome 3. Plasmid mediated enzymes such as: Acetyl- Nucleotidyl- Phospho- -transferases
69
Which Aminoglycosides are less susceptible to resistance?
Amikacin and Netilmicin
70
Which 2 Aminoglycosides have the same metabolism so bacteria might also have similar resistance mechanisms against these 2 agents?
Gentamicin | Tobramycin
71
In a patient currently taking an Aminoglycoside, where in the body would you find the highest concentration?
Renal cortex | Endolymph and perilymph of the inner ear
72
Do Aminoglycosides cross the placenta?
Yes
73
Why must you monitor the peak/trough plasma levels of Aminoglycosides?
Because of the ototoxicity that is often irreversible
74
Besides ototoxicity and nephrotoxicity, what are other adverse effects of the Aminoglycosides?
Acute neuromuscular blockade and apnea
75
Why does the neuromuscular paralysis occur with Aminoglycosides?
Probably results from a decrease of Ach release AND a decrease in postsynaptic sensitivity to the transmitter
76
A patient currently taking an aminoglycoside is experiencing neuromuscular paralysis. What should you administer to alleviate this?
Calcium glutinate | Neostigmine
77
What are the uses of Gentamicin, Tobramycin?
``` Serious gram (-) infections such as: Klebsiella Enterobacter Serratia Pseudomonas--add ticarcillin or another anti-psuedomonal ceph ```
78
Which Aminoglycoside works well with resistant bacteria in hospitals?
Amikacin
79
What other drugs should you avoid when prescribing Aminoglycosides?
1. Nephrotoxic agents 2. Neuromuscular blocking agents 3. Ethacrinyic acid (potentiates the ototoxicity)
80
If you are prescribing an Aminoglycoside and an Anti-pseudomonal PCN together, HOW should you do it?
Do not mix them together in the same injection--you will inactivate the Aminoglycoside
81
What is the first alternative agent to a patient if there is a B-Lactam allergy?
Erythromycin
82
What are the 4 types of Erythromycin and how are they administered?
1. Erythromycin PO 2. Erythromycin ethyl succinate PO 3. Pediazole (erythromycin ethyl succinate + sulfsoxazole) PO
83
What is Pediazole?
Oral | erythromycin ethyl succinate + sulfisoxazole
84
What are the 4 Macrolides?
1. Erythromycin 2. Clarithromycin 3. Azithromycin 4. Telithromycin 5. Lincomycin 6. Clindamycin 7. Chloramphenicol
85
How is Telithromycin given?
PO
86
How is Azithromycin given?
PO/IV
87
How is Clarithromycin
PO
88
What is the MOA of the Macrolides?
Bind IRREVERSIBLY to the 50s ribosome | inhibiting the translocation steps of protein synthesis
89
Are Macrolides static or cidal?
Generally Macrolides are static but at high doses, they are cidal
90
For which Macrolides is the binding site very similar?
Lincomycin Clindamycin Chloramphenicol
91
What is Erythromycin used for?
Similar to PCN G Gram (+) cocci and bacilli Mycoplasma, Legionella, and Chlamydia
92
What is Erythromycin NOT active against?
Most aerobic gram (-) bacilli
93
What is Clarithromycin used for?
``` increased activity against intracellular pathogens active against: Chlamydia Legionella Ureaplasma H. Influenza ```
94
What is Azithromycin used for?
More active against respiratory infections: H. Influenza Moraxella catarrhalis
95
This expensive drug is the preferred therapy for Chlamydia trachomatis urethritis?
Azithromycin 1gm po single dose Z-pack #6, 250 mg tabs
96
Which bacteria is Azithromycin less active against?
Staph and strep
97
What is the most common form of resistance bacteria have against Macrolides?
modification of their ribosome
98
What is a form of resistance specific to erythromycin?
Plasmid -associated erythromycin esterase
99
Which two Macrolides have cross resistance with each other?
Clarithromycin and Azithromycin
100
Which 2 Macrolides are stable to stomach acid and are absorbed well?
Clarithromycin and Azithromycin
101
Which Macrolide is destroyed by gastric acid and what is done to remedy this?
Erythromycin it is enteric coated in tablet form or there are esterified forms
102
Why should you be careful when administering erythromycin IV?
Pt can develop thrombophlebitis
103
Do Macrolides cross into the CSF?
No
104
Where in the body do Macrolides concentrate?
1. Prostatic fluid | 2. accumulates in the liver macrophages
105
Where specifically does Azithromycin concentrate in the body?
Neutrophils, macrophages, and fibroblasts
106
Which Macrolide is extensively metabolized and interferes with CYT P450?
Erythromycin
107
The oxidation of this Macrolide interferes with metabolism of theophylline and carbamazepine; what drug is it?
Clarithromycin
108
Which Macrolide does not undergo metabolism?
Azithromycin
109
How are Erythromycin and Azithromycin excreted?
In an active form in the bile
110
How is Clarithromycin excreted?
It is eliminated by the kidney as well as the liver
111
Which Macrolide should you adjust doses in a patient with compromised renal function?
Clarithromycin
112
Which Macrolide gives the patient a Metallic taste?
Clarithromycin
113
This adv effect causes poor compliance with the Macrolides--what effect?
Epigastric distress
114
This Macrolide adv effect is more prominent in the estate form of erythromycin, but can be seen with all Macrolides. What effect?
Cholestatic jaundice
115
How would you treat a patient with Cholestatic jaundice?
All sign will clear within a few days of stopping therapy
116
Which Macrolide causes the "kiss of death" = prolonging QT interval?
Azithromycin
117
Besides Azithromycin, what other drugs cause QT prolongation?
Fluoroquinolone's
118
Erythromycin and Clarithromycin inhibit the hepatic metabolism of what drugs?
1. Theophylline 2. Warfarin 3. Terfenadine 4. Astemizole 5. Carbamezapine 6. Cyclosporine
119
Macrolide increase the reabsorption of what drug?
Digoxin
120
What is the DOC for legionnaires disease?
Any Macrolide
121
What is the DOC for Mycoplasma pneumoniae?
Any of the Macrolides
122
T or F: You can give a Macrolide to treat Ureaplasma.
True
123
What is an alternative treatment for Chlamydia inf?
Any Macrolide
124
How would you treat Mycobacterium avid complex in AIDS?
With any Macrolide
125
T or F: A Macrolide cannot be used as an alternative if the patient is allergic to PCN in order to treat: Syphillis, pneumococci, etc. Eliminate Corynebacterium diphtheriae
False; Macrolides can be used
126
What is Fidaxomicin?
An oral macrolide antibiotic
127
What is Fidaxomicin used to treat?
C. dif associated diarrhea in patients older than 18 years old
128
How is Fidaxomicin absorbed?
Not very well systemically
129
How is Fidaxomicin classified?
As a Narrow spectrum antibiotic: it has little or no activity against organisms the than clostridia, so it is nice because it preserves your natural gut flora
130
Is Fidoxamin CIDAL or STATIC?
CIDAL
131
Why is vancomycin still preferred over Fidaxamicin to treat C. dif?
Because Fidaxomicin is very expensive
132
How is Chloramphenicol administered?
PO/IV
133
How is Clindamycin administered?
PO/IV
134
When would you use Chloramphenicol?
Its use is restricted to life threatening infections where nothing else works do periodic blood tests
135
What is Chloramphenicol active against?
A wide range of Gram (+) and Gram (-) Rickettsia Chlamydia
136
What is one of the most active antimicrobials against anaerobes?
Chloramphenicol
137
Is Chloramphenicol Cidal or Static?
Depends on the bug
138
What is the MOA of Chloramphenicol?
Acts primarily by binding the 50s ribosomal subunit and prevents peptide bond formation
139
Which drug also inhibits mitochondrial protein synthesis in mammalians?
Chloramphenicol
140
Does Chloramphenicol get into the brain?
Yes
141
What is Chloramphenicol converted to in the liver of newborns and preemies?
Glucuronide | They have decreased levels of glucuronyl transferase
142
Which agent will cause Grey baby syndrome? Deceased metabolism and excretion of drug baby has poor feeding, depressed breathing, cardiovascular collapse, cyanosis, and death
Chloramphenicol
143
What are some adverse effects of Chloramphenicol?
1. Bone marrow suppression (aplastic anemia) 2. Grey baby syndrome 3. GI disturbances 4. Superinfections (overgrowth of Candida) 5. Inhibits some hepatic mixed function oxidases and thus metabolism of some drugs
144
Which adverse effect of Chloramphenicol is reversible?
Aplastic anemia (bone marrow suppression)
145
Which drugs should you avoid taking with Chloramphenicol?
1. Warfarin 2. Phenytoin 3. Tolbutamide Orinase
146
Is Clindamycin STATIC or CIDAL?
STATIC
147
What is the MOA of Clindamycin?
binds to the 50s subunit
148
What is Clindamycin used to treat?
Primarily ANAEROBIC inf, esp. Bacteriodes fragilis (abdominal inf caused by trauma) It is also active against non-enterococcal gram (-) cocci very toxic--only use if this will work better than other agents
149
How is Clindamycin absorbed?
Absorbed well orally
150
Does Clindamycin get into the CSF?
No
151
What are some common adverse effects of Clindamycin?
Skin rashes Diarrhea Potentially fatal PMC (pseudomembranous colitis)--caused by a toxin secreted by clindamycin resistant strains of C. dif
152
What is potentially fatal PMC? What causes it? How do you treat it?
(pseudomembranous colitis)--caused by a toxin secreted by clindamycin resistant strains of C. dif Treat with Metronidazole or Vancomycin
153
What is the MOA of Quinupristin/Dalforpristin?
Binds to 50S
154
Is Quinupristin/Dalforpristin CIDAL or STATIC?
CIDAL
155
What do you treat with Quinupristin/Dalforpristin?
Resistant Gram (+) bugs, like MRSA, VRE (bacteriostatic)
156
How do you administer Quinupristin/Dalforpristin?
IV/IM
157
What are some adverse effects of Quinupristin/Dalforpristin?
1. Venous irritation (give through central line vs a venous line) 2. Arthralgia/Myalgia 3. Hyperbilirubinemia 4. Inhibits CYT 3A4
158
What is the MOA of Linezolid?
Binds to 50s
159
What is Linezolid used to treat?
Resistant Gram (+) bacteria reserved for: MRSA, VRSA, VRE, PCN-resis, -strept
160
What is Linezolid NOT used for?
MRSA Bacteremia
161
Is Linezolid CIDAL or STATIC?
Both
162
How do you administer Linezolid?
orally
163
What are some adverse effects of Linezolid?
1. Reversible thrombocytopenia | 2. Inhibit MAO?

Pharm Exam 4 (10 decks)

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