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alien pcol > PROTEIN SYNTHESIS INHIBITORS > Flashcards

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
Q

Primary Use of Tetracyclines

A
  • Mycoplasma Pneumoniae
  • Chlamydiae
  • Rickettsiae
  • Borrelia sp.
  • Vibrios
  • Some Spirochetes
  • Anaplasma phagocytophilum
  • Ehrlichia
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26
Q

Secondary Use of Tetracyline

A
  • CAP
  • Syphilis
  • Chronic Bronchitis
  • Leptospirosis
  • Acne
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27
Q

Clinical Use: GI ulcers caused by H. pylori

a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

b. Tetracycline

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28
Q

Clinical Use: Lyme Disease
a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

a. Doxycycline

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29
Q

Clincal Use: Malaria Prophylaxis
a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

a. Doxycycline

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30
Q

Clincal Use: Amoebiasis
a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

a. Doxycycline

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31
Q

Clinical Use: Meningococcal Carrier State b
a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

c. Minocycline

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32
Q

Clinical Use: ADH-secreting tumors
a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

d. Demeclocycline

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33
Q

Clinical Use: Inhibit renal actions from ADH
a. Doxycycline
b. Tetracycline
c. Minocycline
d. Demeclocycline

A

d. Demeclocycline

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34
Q

Clincal Use: Coagulase Negative Staphylococus

A

TIGECYCLINE ERAVACYCLINE OMADACYCLINE

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35
Q

Clinical Use: MRSA & VRE

A

TIGECYCLINE ERAVACYCLINE OMADACYCLINE

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36
Q

Clinical Use
* Streptococci
* GRAM (+) RODS
* Enterobacteriaceae
* Acinetobacter
* Rickettsiae
* Chlamydiae
* Legionella pneumophila

A

TIGECYCLINE ERAVACYCLINE OMADACYCLINE

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37
Q

Clinical Use: Rapidly Growing Mycobacteria –> Tuberculosis

A

TIGECYCLINE ERAVACYCLINE OMADACYCLINE

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38
Q

60 - 70% Bioavailability
a. Tetracycline & Demeclocycline
b. Doxycycline & Minocycline

A

a. Tetracycline & Demeclocycline

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39
Q

95 - 100% Bioavailability

A

b. Doxycycline & Minocycline

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40
Q

T/F Absoprtion of Tetracyclines occurs mainly in the Colon

A

False

Upper Small Intestine

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41
Q

Tetracyclines should not be given to patients who are:

A
  • Drinking multivitamins
  • Milk
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42
Q

T/F

Tetracyclines cannot cross the BBB therefore cannot be used for CNS infections

A

True

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43
Q

Excretion of most Tetracyclines

A

Bile & Urine

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44
Q

Excretion of Tetracycline

A

Feces

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45
Q

Tetracycline eliminated by nonrenal mechanisms

A

Doxycycline & Tigecycline

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46
Q

Short Acting Tetracycline
a. Demecycline
b. Tetracycline
c. Doxycycline & Minocycline

A

b. Tetracycline

TT mo short eyyyyyy

47
Q

Tetracyclines with long half-life

A
  • Tigecycline (IV)
  • Eravacycline (IV)
  • Omadacycline (Oral & IV)
48
Q

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

A

True

49
Q

Toxicity caused by patient taking outdated tetracyclines

A

Fanconi Syndrome

50
Q

Tetracyclines causes what toxicity to younger children

A
  • Tooth enamel dysplasia
  • Irregularities in bone growyth
  • Crown deformation
51
Q

In tetracyclines, Hepatic toxicity is usually seen in

A
  • High doses
  • Pregnant patients
52
Q

Toxicity caused by combination of Tetracycline + Diuretic

A

Nephrotoxicity

53
Q

Photosensitivity is a toxicity of what tetracycline

a. Doxycyline
b. Democlocycline
c. Minocycline
d. Tigecycline

A

b. Democlocycline

54
Q
A
54
Q
A
55
Q

Vestibular toxicity: dizziness & vertigo is caused by what tetracycline

a. Doxycycline
b. Minocycyline
c. Both a & B
d. Neither

A

c. Both a & B

56
Q

Contains macrocyclic lactone ring with attached rings

A

Macrolides

57
Q
A
57
Q

Prototype drug of macrolides

A

Erythromycine

58
Q

MOA of Macrolides

A

Inhibition of protein synthesis occurs via binding to the 50S subunit of bacterial ribosomes.

59
Q

Well-known adverse effect of macrolides

A

Torsades de pointes Arrhythmia

60
Q

Absoprtion of this Macrolide is impeded by food

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

b. Azithromycin

61
Q

Metabolism of Macrolides

A

Hepatic

62
Q

half-life: 2 hours
has the Shortest half-life

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

a. Erythromycin

63
Q

half-life: 6 hours
a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

b. Azithromycin

64
Q

half-life: 2-4 days
a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

b. Azithromycin

65
Q

Erythromycine is resisted by what enzyme

A

Enterobacteriaceae - Esterases

66
Q

T/F

Erythromycin is also resisted by modification of ribosomal binding site

A

True

67
Q
A
68
Q

T/F

Cross-resistance occurs between erythromycin and other macrolides

A

True

69
Q

Excretion of Eyrthromycine is mainly in the ____

a. Bile
b. Hepatic

A

a. Bile

70
Q

T/F

Erythromycine is taken up by intracellular organism and is effective against polymorphnuclear leukocytes and macrophases

A

False
Taken up by polymorphonuclear leukocytes and macrophages; o Effective against organisms that are intracellular

71
Q

Clinical Use
* Corynebacterial & Chalmydial infection
* M. pneumoniae & L. pneumophilia
* Staphylococci & Streptococci

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

a. Erythromycin

72
Q

Drug interaction of Eyrthromycin and Clarithromycin

A
  • Theophylline
  • Warfarin
  • Cyclosporine
  • Methylprednisolone
  • Digoxin
72
Q

Notable adverse reaction of Erythromycin

A

Acute Cholestatic Hepatitis

73
Q

Antimicrobial activity: Tuberculosius

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

c. Clarithromycin

74
Q

Antimicrobial activity: Leprosy
a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

c. Clarithromycin

75
Q

Antimicrobial activity: T. gondii
a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

c. Clarithromycin

75
Q

Antimicrobial activity: H. influenzae
a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

c. Clarithromycin

76
Q

Metabolized in the liver and partially eliminated in the urine

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

c. Clarithromycin

77
Q

Antimicrobial activity: M. avium complex

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

b. Azithromycin

78
Q

Penetrates into most tissues and phagocytic cells extremely well and exceeding serum concentrations is by 10 - 100 fold

a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

b. Azithromycin

79
Q

Rapidly absorbed and well tolerated orally
a. Erythromycin
b. Azithromycin
c. Clarithromycin

A

b. Azithromycin

80
Q

Chlorine-substituted derivative of lincomycin

A

Clindamycin

81
Q

Antimicrobial activity of Clindamycin

A
  • Streptococci
  • Staphylococci
  • Pneumococci
  • Bacteroides
82
Q

Metabolism of clindamycin

A

Hepatic

82
Q

Half-life of Clindamycin

A

6 - 8 hrs

83
Q

Clinical Use of Clindamycin

A
  • Bacteroides
  • Fusobacterium
  • Prevotella
  • MRSA
84
Q

Toxic Shock Syndrome is treated with

A

Clindamycin and Penicillin G

85
Q

Penetrating wounds of the abdomen and gut is treated with

A

Clindamycine combined with aminoglycoside & cephalosphorin

86
Q

Treatment for pneumonia in AIDS patient

A

Primaquine

87
Q

Treatment for AIDS-related toxoplasmosis

A

Pyrimethamine

88
Q

Toxicities caused by Clindamycin

A
  • Neutropenia
  • Pseudomembranous colitis
89
Q

Steptogramins is a combination of

A
  • 70%: Dalfopristin (Streptogramin A)
  • 30%: Quinupristin (Streptogramin B)
90
Q

Streptogramins are bactericidal except for

A

E. faecium

91
Q

Antimicrobial activity of Streptogramins

A
  • 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
Q

Resistance of Streptogramins

A
  • Modificartion of the Quinupristin binding site
  • Enzymatic inactivation of Dalfopristin
93
Q

Streptogramins is excreated mainly by

A

FECES

93
Q

Clinical Use of Streptogramins

A
  • Staphylococci (MRSA)
  • Vancomycin-resistant sterains of E. faecium (VRSE)
93
Q

MOA is by binding to 23S ribosomal rna of the 50S ribosomal subunit

A

Linezolud

94
Q

Notable adverse effect of Streptogramins

A

Arthralgia-Myalgia sYNDROME

94
Q

Half-life of Linezolid

A

4 - 6 hrs

94
Q

T/F

Linezolid has 91% bioavailability

A

False

100% bioavailability

95
Q

Clinical Use of Linezolid

A
  • Vancomycine-resistant E. faecium infection
  • HCAP
  • CAP
  • Skin and Soft tissue infections
96
Q

Off-label use of Linezolid

A
  • MDR-TB: Multi-drug resistant TB
  • Nocardia Infections
97
Q

Adverse Effects of Linezolid

A
  • Thrombocytopenia
  • Anemia
  • Neutropenia
  • Optic and Peripheral neuropathy
  • Lactic Acidosis
  • Serotonin syndrome
98
Q

Active moiety of the prodrug tedizolid phosphate

A

tedizolid

99
Q

Antimicrobial activity of Tedizolid

A
  • MRSA
  • VRE
  • Streptococci
  • Gram (+) anaerobes
100
Q

T/F

Bioavailability of Teduzolid is 100%

A

Fallse

Bioavailability of Teduzolid is 91%

101
Q

Clinical Use of Tidezolid

A

Skin and Soft tissue infection

102
Q

Adverse Effect of Tedizolid

A
  • Bone Marrow suppression
  • Serotonergic toxicity
103
Q

MOA of Lefamulin

A

Binding the 50S ribosome and inhibits bacterial protein synthesis

104
Q

Clinical Use of Lefamulin

A

CAP

105
Q

Adverse Effects of Lefamulin

A

● Infusion-site reactions
● GI disturbances
● Congenital malformations

alien pcol (4 decks)

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