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PROTEIN SYNTHESIS INHIBITORS Flashcards

1
Q

Inhibitors that selectively inhibit bacterial protein synthesis

A

Protein Synthesis Inhibitors

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2
Q

Total ribosomes of Bacteria

A

70S consisting
* 50S Large Subunit
* 30S Small Subunit

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3
Q

Differences found between bacterial and mammalian protein synthesis

A
  • Ribosomal subunits
  • Chemical composition
  • Functional specificities of component nucleic acids and proteins
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4
Q

Bactericidal protein inhibitors

A
  • Oxazolidinones
  • Pleuromutilins

TIP: OP = “Out of Place ang Oxazolidinones and Pleuromutilins”

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5
Q

Broad Spectrum Protein Synthesis Inhibitors

A
  • Chloramphenicol
  • Tetracyclines
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6
Q

Moderate Spectrum

A
  • Macrolides
  • Ketolides
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7
Q

Narrow Spectrum

A
  • Lincosamides
  • Streptogramins
  • Linezolid
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8
Q

T/F

Chloramphenicol has equal bioavailability for oral and IV/IM

A

True

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9
Q

MOA of Chloramphenicol

A

Binds to the 50S subunit of bacterial ribosome

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10
Q

Chloramphenicol is bactericial for what infections

A
  • H. influenzae
  • N. meningitis
  • Bacteroides
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11
Q

T/F

Resistance of Chloramphenicol is Plasmid-Mediated

A

True

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12
Q

Enzyme that inactivates chloramphenicol

A

Chloramphenicol Acetyltransferases

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13
Q

Clinical Use of Chloramphenicol

A
  • Ricketsial Infections :Typhus
    & Rocky Mountain Spotted Fever
  • Bacterial Meningitis
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14
Q

T/F

Chloramphenicol can be used as an alternative for meningitis for patient who have major hypersensitivity to penicillin

A

True

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15
Q

T/F

Chloramphenicol can only cross the placenta and not the blood-brain barrier

A

False
Chloramphenicol readily cross the placental and blood-brain barrier

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16
Q

Chlorampheniucol is inactivated by ____ acid

a. Carbonic Acid
b. Acetic Acid
c. Glucoronic Acid
d. Citric Acid

A

Glucoronic Acid

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17
Q

Excretion of Chloramphenicol

A

Eliminated by the Urine and small amount is excreted into bile and feces

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18
Q

Notable toxicities of Chloramphenicol

A
  • Inhibition of Red Cell Matiration
  • Aplastic Anemia
  • Gray Baby Syndrome
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19
Q

Toxicity of Chloramphenicol due to lack of effective glucoronic acid conjucation for the degradation and detoxification

A

Gray Baby Syndrome

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20
Q

Chloramphenicol prolongs the effect of these drugs

PHEN TO - CH WARS

A
  • Phenytoin
  • Tolbutamide
  • Chlorpropamide
  • Warfarin
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21
Q

MOA of Tetracyclines

A

Binds reversibly to the 30S subunit of the bacterial ribosome

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22
Q

Prevents new peptide bonds
a. Tetracycline
b. Chloramphenicol

A

b. Chloramphenicol

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23
Q

Prevents new amino acids
a. Tetracycline
b. Chloramphenicol

A

a. Tetracycline

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24
Q

Antimicrobial Activity of Tetracycline

A
  • Rickettsiae
  • Chlamydiae
  • Mycoplasma
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25
Primary Use of Tetracyclines
* Mycoplasma Pneumoniae * Chlamydiae * Rickettsiae * Borrelia sp. * Vibrios * Some Spirochetes * Anaplasma phagocytophilum * Ehrlichia
26
Secondary Use of Tetracyline
* CAP * Syphilis * Chronic Bronchitis * Leptospirosis * Acne
27
Clinical Use: GI ulcers caused by H. pylori a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
b. Tetracycline
28
Clinical Use: Lyme Disease a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
a. Doxycycline
29
Clincal Use: Malaria Prophylaxis a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
a. Doxycycline
30
Clincal Use: Amoebiasis a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
a. Doxycycline
31
Clinical Use: Meningococcal Carrier State b a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
c. Minocycline
32
Clinical Use: ADH-secreting tumors a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
d. Demeclocycline
33
Clinical Use: Inhibit renal actions from ADH a. Doxycycline b. Tetracycline c. Minocycline d. Demeclocycline
d. Demeclocycline
34
Clincal Use: Coagulase Negative Staphylococus
TIGECYCLINE ERAVACYCLINE OMADACYCLINE
35
Clinical Use: MRSA & VRE
TIGECYCLINE ERAVACYCLINE OMADACYCLINE
36
Clinical Use * Streptococci * GRAM (+) RODS * Enterobacteriaceae * Acinetobacter * Rickettsiae * Chlamydiae * **Legionella pneumophila**
TIGECYCLINE ERAVACYCLINE OMADACYCLINE
37
Clinical Use: Rapidly Growing Mycobacteria --> Tuberculosis
TIGECYCLINE ERAVACYCLINE OMADACYCLINE
38
60 - 70% Bioavailability a. Tetracycline & Demeclocycline b. Doxycycline & Minocycline
a. Tetracycline & Demeclocycline
39
95 - 100% Bioavailability
b. Doxycycline & Minocycline
40
T/F Absoprtion of Tetracyclines occurs mainly in the Colon
False Upper Small Intestine
41
Tetracyclines should not be given to patients who are:
* Drinking multivitamins * Milk
42
T/F Tetracyclines cannot cross the BBB therefore cannot be used for CNS infections
True
43
Excretion of most Tetracyclines
Bile & Urine
44
Excretion of Tetracycline
Feces
45
Tetracycline eliminated by nonrenal mechanisms
Doxycycline & Tigecycline
46
Short Acting Tetracycline a. Demecycline b. Tetracycline c. Doxycycline & Minocycline
b. Tetracycline ## Footnote TT mo short eyyyyyy
47
Tetracyclines with long half-life
* Tigecycline (IV) * Eravacycline (IV) * Omadacycline (Oral & IV)
48
T/F Broad-spectrum antibiotics can usually cause bacterial infections (e.g., candidiasis and C. difficile infections) by disturbing normal gut flora due to their wide range of effectiveness
True
49
Toxicity caused by patient taking outdated tetracyclines
Fanconi Syndrome
50
Tetracyclines causes what toxicity to younger children
* Tooth enamel dysplasia * Irregularities in bone growyth * Crown deformation
51
In tetracyclines, Hepatic toxicity is usually seen in
* High doses * Pregnant patients
52
Toxicity caused by combination of Tetracycline + Diuretic
Nephrotoxicity
53
Photosensitivity is a toxicity of what tetracycline a. Doxycyline b. Democlocycline c. Minocycline d. Tigecycline
b. Democlocycline
54
54
55
Vestibular toxicity: dizziness & vertigo is caused by what tetracycline a. Doxycycline b. Minocycyline c. Both a & B d. Neither
c. Both a & B
56
Contains macrocyclic lactone ring with attached rings
Macrolides
57
57
Prototype drug of macrolides
Erythromycine
58
MOA of Macrolides
Inhibition of protein synthesis occurs via binding to the 50S subunit of bacterial ribosomes.
59
Well-known adverse effect of macrolides
Torsades de pointes Arrhythmia
60
Absoprtion of this Macrolide is impeded by food a. Erythromycin b. Azithromycin c. Clarithromycin
b. Azithromycin
61
Metabolism of Macrolides
Hepatic
62
half-life: 2 hours has the Shortest half-life a. Erythromycin b. Azithromycin c. Clarithromycin
a. Erythromycin
63
half-life: 6 hours a. Erythromycin b. Azithromycin c. Clarithromycin
b. Azithromycin
64
half-life: 2-4 days a. Erythromycin b. Azithromycin c. Clarithromycin
b. Azithromycin
65
Erythromycine is resisted by what enzyme
Enterobacteriaceae - Esterases
66
T/F Erythromycin is also resisted by modification of ribosomal binding site
True
67
68
T/F Cross-resistance occurs between erythromycin and other macrolides
True
69
Excretion of Eyrthromycine is mainly in the ____ a. Bile b. Hepatic
a. Bile
70
T/F Erythromycine is taken up by intracellular organism and is effective against polymorphnuclear leukocytes and macrophases
False Taken up by polymorphonuclear leukocytes and macrophages; o Effective against organisms that are intracellular
71
Clinical Use * Corynebacterial & Chalmydial infection * M. pneumoniae & L. pneumophilia * Staphylococci & Streptococci a. Erythromycin b. Azithromycin c. Clarithromycin
a. Erythromycin
72
Drug interaction of Eyrthromycin and Clarithromycin
* Theophylline * Warfarin * Cyclosporine * Methylprednisolone * Digoxin
72
Notable adverse reaction of Erythromycin
Acute Cholestatic Hepatitis
73
Antimicrobial activity: Tuberculosius a. Erythromycin b. Azithromycin c. Clarithromycin
c. Clarithromycin
74
Antimicrobial activity: Leprosy a. Erythromycin b. Azithromycin c. Clarithromycin
c. Clarithromycin
75
Antimicrobial activity: T. gondii a. Erythromycin b. Azithromycin c. Clarithromycin
c. Clarithromycin
75
Antimicrobial activity: H. influenzae a. Erythromycin b. Azithromycin c. Clarithromycin
c. Clarithromycin
76
Metabolized in the liver and partially eliminated in the urine a. Erythromycin b. Azithromycin c. Clarithromycin
c. Clarithromycin
77
Antimicrobial activity: M. avium complex a. Erythromycin b. Azithromycin c. Clarithromycin
b. Azithromycin
78
Penetrates into most tissues and phagocytic cells extremely well and exceeding serum concentrations is by 10 - 100 fold a. Erythromycin b. Azithromycin c. Clarithromycin
b. Azithromycin
79
Rapidly absorbed and well tolerated orally a. Erythromycin b. Azithromycin c. Clarithromycin
b. Azithromycin
80
Chlorine-substituted derivative of lincomycin
Clindamycin
81
Antimicrobial activity of Clindamycin
* Streptococci * Staphylococci * Pneumococci * Bacteroides
82
Metabolism of clindamycin
Hepatic
82
Half-life of Clindamycin
6 - 8 hrs
83
Clinical Use of Clindamycin
* Bacteroides * Fusobacterium * Prevotella * MRSA
84
Toxic Shock Syndrome is treated with
Clindamycin and Penicillin G
85
Penetrating wounds of the abdomen and gut is treated with
Clindamycine combined with aminoglycoside & cephalosphorin
86
Treatment for pneumonia in AIDS patient
Primaquine
87
Treatment for AIDS-related toxoplasmosis
Pyrimethamine
88
Toxicities caused by Clindamycin
* Neutropenia * Pseudomembranous colitis
89
Steptogramins is a combination of
* 70%: Dalfopristin (Streptogramin A) * 30%: Quinupristin (Streptogramin B)
90
Streptogramins are bactericidal except for
E. faecium
91
Antimicrobial activity of Streptogramins
* Gram (+) cocci * Multidrug-resistant strains of streptococci * Penicillin-resistant strains of S. pneumoniae * Methicillin-susceptible and resistant trains of staphylococci (MRSA) * o E. faecium
92
Resistance of Streptogramins
* Modificartion of the Quinupristin binding site * Enzymatic inactivation of Dalfopristin
93
Streptogramins is excreated mainly by
FECES
93
Clinical Use of Streptogramins
* Staphylococci (MRSA) * Vancomycin-resistant sterains of E. faecium (VRSE)
93
MOA is by binding to 23S ribosomal rna of the 50S ribosomal subunit
Linezolud
94
Notable adverse effect of Streptogramins
Arthralgia-Myalgia sYNDROME
94
Half-life of Linezolid
4 - 6 hrs
94
T/F Linezolid has 91% bioavailability
False 100% bioavailability
95
Clinical Use of Linezolid
* Vancomycine-resistant E. faecium infection * HCAP * CAP * Skin and Soft tissue infections
96
Off-label use of Linezolid
* MDR-TB: Multi-drug resistant TB * Nocardia Infections
97
Adverse Effects of Linezolid
* Thrombocytopenia * Anemia * Neutropenia * Optic and Peripheral neuropathy * Lactic Acidosis * Serotonin syndrome
98
Active moiety of the prodrug tedizolid phosphate
tedizolid
99
Antimicrobial activity of Tedizolid
* MRSA * VRE * Streptococci * Gram (+) anaerobes
100
T/F Bioavailability of Teduzolid is 100%
Fallse Bioavailability of Teduzolid is 91%
101
Clinical Use of Tidezolid
Skin and Soft tissue infection
102
Adverse Effect of Tedizolid
* Bone Marrow suppression * Serotonergic toxicity
103
MOA of Lefamulin
Binding the 50S ribosome and inhibits bacterial protein synthesis
104
Clinical Use of Lefamulin
CAP
105
Adverse Effects of Lefamulin
● Infusion-site reactions ● GI disturbances ● Congenital malformations

alien pcol (4 decks)

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