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MICROPARA > M5 PART 12 > Flashcards

M5 PART 12 Flashcards

1
Q

Drugs have been used for the treatment of infectious diseases since the ____ Century (e.g., quinine and emetine)

A

17th

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2
Q

introduced Salvarsan (for syphilis)
(Arsphenamine or Compound 606)

A

PAUL ERLICH

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3
Q

Accidental discovery of Penicillin

A

ALEXANDER FLEMMING

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4
Q

/

Discovery of the sulfonamides

A

GERHARD DOGMAK

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5
Q

Penicillin has been used clinically as an antibiotic

FLOREY & CHAIN

A

1940

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6
Q

An ideal antimicrobial agent exhibits ____, which means that the drug is harmful to a pathogen without being harmful to the host.

A

SELECTIVE TOXICITY

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7
Q

antibiotics act against a limited group of bacteria

A

NARROW SPECTRUM

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8
Q

antibiotics act against a larger group of bacteria

TETRACYCLINE

A

BROAD SPECTRUM

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9
Q

Bactericidal drug ____ bacteria

A

KILL

suiCIDAL

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10
Q

Bacteriostatic drug ____ of bacteria

A

INHIBITION

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11
Q

INHIBITION OF CELL WALL SYNTHESIS

  • New peptidoglycan monomers are inserted by transglycosylase (transglycosidase)
  • The final rigidity of the cell wall is imparted by cross-linking of the peptide chains by transpeptidase enzyme
  • Penicillin-Binding Proteins (PBP) may act as transglycosylase or as transpeptidase
A

BACTERIAL CELL WALL SYNTHESIS

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12
Q

INHIBITION OF CELL WALL SYNTHESIS

BACTERIAL CELL WALL SYNTEHSIS:
New peptidoglycan monomers are inserted by ____

A

TRANSGLYCOSYLASE

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13
Q

INHIBITION OF CELL WALL SYNTHESIS

BACTERIAL CELL WALL SYNTHESIS:
The final rigidity of the cell wall is imparted by cross-linking of the peptide chains by ____ enzyme

A

TRANSPEPTIDASE

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14
Q

INHIBITION OF CELL WALL SYNTHESIS

BACTERIAL CELL WALL SYNTHESIS:
____ may act as transglycosylase or as transpeptidase

A

PENICILLIN-BINDING PROTEIN (PBP)

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15
Q

BACTERIAL CELL WALL SYNTHESIS

  • All ____ are selective inhibitors of bacterial cell wall synthesis
  • block the action of transpeptidase; no cell wall formed
A

β-lactam drugs

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16
Q

BACTERIAL CELL WALL SYNTHESIS

Destruction of bacterial ____ (destroys peptidoglycan)

A

AUTOLYSINS

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17
Q

only β-lactam drug that has one ring

A

MONOBACTAMS

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18
Q
A
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19
Q

active in non growing

A

β-lactam antibiotics

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20
Q

the only actively used monobactams

A

AZTREONAM

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21
Q

The penicillins are derived from molds of the genus

A

penicillium

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22
Q

They have the highest activity against Gram-positive organisms, spirochetes, and susceptible to β-lactamases

A

NATURAL PENICILLINS

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23
Q

NATURAL PENICILLINS

o Aqueous penicillin G (IV)
o Procaine penicillin G (IM)
o Benzathine penicillin G (IM)

A

PENICILLIN G (BENZYLPENICILLIN)

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24
Q

NATURAL PENICILLINS

phenoxymethylpenicillin

A

PENICILLIN V

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25
Q

NATURAL PENICILLINS

anesthetics combined with Pen G

A

Procaine penicillin G (IM)
Benzathine penicillin G (IM)

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26
Q

NATURAL PENICILLINS

stable in gastric acid, orally administered

A

PENICILLIN V

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27
Q

NATURAL PENICILLINS

gastric acid sensitive hence administered parenterally

A

PENICILLIN G

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28
Q
  • Antistaphylococcal penicillins
  • Lower activity against Gram-positive organisms and inactive against Gram-negative organisms.
    o Nafcillin
    o Methicillin
    o Oxacillin
    o Dicloxacillin
  • Staphylococci resistant to oxacillin and nafcillin have the mecA gene
A

β-lactamase resistant

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29
Q

β-lactamase resistant

Lower activity against Gram ____ organisms

A

positive

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29
Q
  • Extended-Spectrum Penicillins
  • They have high activity against both Gram-positive and Gram-negative organisms but are destroyed by β-lactamases
  • Ampicillin
  • Amoxicillin
A

Aminopenicillins

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29
Q

β-lactamase resistant

Staphylococci resistant to oxacillin and nafcillin have the ____ gene

A

mecA

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30
Q

β-lactamase resistant

inactive against Gram-____ organisms

A

negative

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30
Q

β-lactamase resistant drugs

A

Nafcillin
Methicillin
Oxacillin
Dicloxacillin

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31
Q

Aminopenicillins

They have high activity against ____ organisms

A

both gram-negative & gram-positive

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31
Q

Aminopenicillins

are destroyed by ____

A

β-lactamases

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32
Q

AMINOPENICILLINS

A

Ampicillin
Amoxicillin

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33
Q

MAJOR GROUPS OF CEPHALOSPORINS

Cefotaxime
Ceftizoxime
Ceftriaxone
Ceftazidime
Cefoperazone
Moxolactam
Cefixime
Cefpodoxime proxetil
Ceftibuten
Cefdinir
Cefditoren

A

THIRD GENERATION

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33
Q

Aminopenicillins + β-Lactamase Inhibitors

Ampicillin is commonly combined with what drug for β-Lactamase inhibition

A

SULBACTAM

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34
Q
  • Ampicillin + Sulbactam (Sultamicillin)
  • Amoxicillin + Clavulanic acid (Co-Amoxiclav)
A

Aminopenicillins + β-Lactamase Inhibitors

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34
Q

Aminopenicillins + β-Lactamase Inhibitors

Amoxicillin is commonly combined with what drug for β-Lactamase inhibition

A

CLAVULANIC ACID

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34
Q

Piperacillin is commonly combined with what drug for β-Lactamase inhibition

A

TAZOBACTAM

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34
Q

anti-pseudomonal
* Carbenicillin
* Ticarcillin

A

Carboxypenicillins

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34
Q

MAJOR GROUPS OF CEPHALOSPORINS

MRSA active

A

Ceftaroline
Ceftobiprole

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34
Q
  • Piperacillin (anti-pseudomonal)
  • Mezlocillin
A

Ureidopenicillins

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35
Q

Cephalosporins

Cephalosporins tend to be resistant to the

A

β-lactamases

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35
Q
  • The mechanism of action is analogous to that of penicillins
  • tend to be resistant to the** β-lactamases**
  • have been arranged into major groups, or “generations”
A

Cephalosporins

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35
Q

MAJOR GROUPS OF CEPHALOSPORINS

FIRST GENERATION

A

Cephalothin
Cephapirin
Cefazolin
Cephalexin
Cephradine
Cefadroxil

first yr students - positive (gram +)
CEPH

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35
Q

Cephalosporins

Cephalosporins have been arranged into major groups, or

A

GENERATIONS

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35
Q

Ureidopenicillins

A

Piperacillin (anti-pseudomonal)
Mezlocillin

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35
Q

Cephalosporins

The mechanism of action is analogous to that of

A

PENICILLINS

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35
Q

Carboxypenicillins

A
  • Carbenicillin
  • Ticarcillin
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35
Q

Ticarcillin is commonly combined with what drug for β-Lactamase inhibition

A

CLAVULANIC ACID

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35
Q

MAJOR GROUPS OF CEPHALOSPORINS

SECOND GENERATION

A

Cefamandole
Cefuroxime
Cefonic acid
Cefaclor
Cefoxitin
Cefotetan
Cefprozil
Cefuroxime axetil
Cefmetazole
Lorocarbef

CEF + VOWEL
equal activity = not positive, not negative

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35
Q

MAJOR GROUPS OF CEPHALOSPORINS

Cefamandole
Cefuroxime
Cefonic acid
Cefaclor
Cefoxitin
Cefotetan
Cefprozil
Cefuroxime axetil
Cefmetazole
Lorocarbef

A

SECOND GENERATION

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35
Q

MAJOR GROUPS OF CEPHALOSPORINS

Cephalothin
Cephapirin
Cefazolin
Cephalexin
Cephradine
Cefadroxil

A

FIRST GENERATION

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35
Q

MAJOR GROUPS OF CEPHALOSPORINS

only 1st gen drug administered intravenously

35
Q

MAJOR GROUPS OF CEPHALOSPORINS

the very first first generation drug

A

Cephalexin

35
Q

MAJOR GROUPS OF CEPHALOSPORINS

very first second generation drug

A

Cefuroxime

35
Q

MAJOR GROUPS OF CEPHALOSPORINS

THIRD GENERATION

A

Cefotaxime
Ceftizoxime
Ceftriaxone
Ceftazidime
Cefoperazone
Moxolactam
Cefixime
Cefpodoxime proxetil
Ceftibuten
Cefdinir
Cefditoren

CEF + CONSONANT
numbers/money
gram negative

36
Q

MAJOR GROUPS OF CEPHALOSPORINS

FOURTH GENERATION

A

Cefepime
Cefpirome

36
Q

Summary of Activity of Cephalospirins

Gram (+) cocci and PEcK (P.
mirabilis, E. coli, K. pneumoniae)

36
Q

Summary of Activity of Cephalospirins

Gram (+) cocci and HENPEcK (H. influenzae, E. aerogenes, N. gonorrhae, P. mirabilis, E. coli, K. pneumoniae)

37
Q

Summary of Activity of Cephalospirins

Gram (+) cocci and HENPPEcK (H. influenzae, E. aerogenes, N. gonorrhae, P. aeruginosa, P. mirabilis, E. coli, K. pneumoniae)

38
Q

Summary of Activity of Cephalospirins

Gram (+) cocci [MRSA] and E. coli, K. pneumoniae, P. mirabilis, and P. aeruginosa

39
Q

deactivates imipinem
inhibits cilastatin

A

RENAL DEHYDROPEPTIDASE

40
Q

RENAL DEHYDROPEPTIDASE

deactives ____

41
Q

RENAL DEHYDROPEPTIDASE

inhibits ____

A

cilastatin

42
Q

has good activity against many Gram-negative rods, Gram-positive organisms, and anaerobes.

A

Imipenem + Cilastatin

43
Q

Imipenem + Cilastatin
Meropenem
Ertapenem

A

CARBANEPAMS

44
Q
  • Aztreonam
  • It has antimicrobial activity directed primarily against the Enterobacteriaceae (Pseudomonas), including P. aeruginosa.
  • No activity against Gram-positive organisms and anaerobes
A

MONOBACTAMS

45
Q

ADVERSE EFFECTS

Hypersensitivity, Diarrhea, Nephritis, Neurotoxicity, Hematologic toxicities, Cation toxicity

A

PENICILLIN

46
Q

ADVERSE EFFECTS

Allergic manifestations

A

CEPHALOSPORINS

47
Q

ADVERSE EFFECTS

Imipenem/Cilastatin - N&V & diarrhea
Imipinem - may provoke seizures

A

CARBAPENEMS

48
Q

ADVERSE EFFECTS

Aztreonam may cause phlebitis, skin rash, and occasionally abnormal liver function tests

A

MONOBACTAM

49
Q

ADVERSE EFFECTS

fever, chills, and/or phlebitis at the infusion site
flushing (red man syndrome) and shock

A

Vancomycin

50
Q

Mode of Action of Antibiotics That Inhibit Cell Wall Synthesis

ANTIBIOTIC: VANCOMYCIN, BACITRACIN
PROCESS INTERRUPTED: ____

A

mucopeptide synthesis

50
Q

Mode of Action of Antibiotics That Inhibit Cell Wall Synthesis

ANTIBIOTIC: PENICILLIN, CEPHALOSPORINS
PROCESS INTERRUPTED: ____

A

cell wall cross-linking

51
Q

Mode of Action of Antibiotics That Inhibit Cell Wall Synthesis

ANTIBIOTIC: CYCLOSERINE
PROCESS INTERRUPTED: ____

A

synthsis of cell wall peptides

52
Q

Inhibition of Cell Membrane Function

If the functional integrity of the cytoplasmic membrane
is ____, macromolecules and ions escape from the cell, and cell damage or death ensues.

53
Q

Inhibition of Cell Membrane Function

If the functional integrity of the cytoplasmic membrane is disrupted, macromolecules and ions ____ from the cell, and cell damage or death ensues.

54
Q

Inhibition of Cell Membrane Function

  • Binds to cell membranes rich in phosphatidylethanolamine
  • Active against gram-negative rods, especially P. aeruginosa, Acinetobacter baumannii, and carbapenemase-producing Enterobacteriaceae.
  • Bactericidal
A

POLYMYXIN E (COLISTIN)

55
Q

Inhibition of Cell Membrane Function | POLYMYXIN E (COLISTIN)

binds to cell membrane rich in ____

A

phosphatidylethanolamine

56
Q

Inhibition of Cell Membrane Function

  • Induces depolarization of bacterial membrane potential resulting to release of potassium
  • This agent is given to organisms highly resistant to β-lactam agents and vancomycin.
  • Bactericidal
A

DAPTOMYCIN

56
Q

Inhibition of Cell Membrane Function | DAPTOMYCIN

Induces ____ of bacterial membrane potential resulting to release of potassium

A

depolarization

56
Q

Inhibition of Cell Membrane Function | POLYMYXIN E (COLISTIN)

active against ____

A

gram negative rods

56
Q

Inhibition of Cell Membrane Function | DAPTOMYCIN

Induces depolarization of bacterial membrane potential resulting to release of ____

57
Q

Inhibition of Cell Membrane Function | DAPTOMYCIN

This agent is given to organisms highly resistant to ____ and ____

A

β-lactam agents and vancomycin

57
Q

Amikacin
Gentamicin
Neomycin
Streptomycin
Tobramycin

A

AMINOGLYCOSIDES

57
Q

antibiotics that targets 30s ribosomes

A

Aminoglycosdies
Tetracycline
Tigecycline

buy AT 30

57
Q

blocks functioning of initiation complex & causes misreading of mRNA

A

Aminoglycosides

57
Q

antibiotics that target the 50s ribosomes

A

Chloramphenicol
Erythromycin
Linezolid
Clindamycin
Macrolides
Quinupristin / Dalfopristin

CELL at 50

58
Q

blocks tRNA binding to ribosome

A

tetracycline

58
Q

type of activity: aminoglycosides

A

bactericidal

58
Q

blocks protein translation

A

tigecycline

59
Q

mycin source

A

streptomyces

60
Q

ADVERSE EFFECTS

ototoxicity (vestibular & cochlear)
Nephrotoxicity (NTG)
Neuromuscular paralysis
Allergic reactions

A

AMINOGLYCOSIDES

61
Q

Demeclocycline
Doxycycline
Minocycline
Tetracycline

A

TETRACYCLINES

62
Q

ADVERSE EFFECTS

Gastric discomfort
Effects on calcified tissue
Fatal hepatotoxicity
Photoxicity
Vestibular problems
Pseudotumor cerebri
Superinfections
causes yellow tooth discoloration
Fancomi syndrome - acquired by taking an expired drug

A

TETRACYCLINES

63
Q

blocks peptidyltransferase

A

Chloramphenicol

64
Q

blocks translocation

A

macrolides

65
Q

causes premature release of peptide chain

A

Quinupristin / Dalfopristin

65
Q

blocks peptide bond formation

A

Clindamycin

66
Q

blocks early step in ribosome formation

67
Q

ADVERSE EFFECTS

hemolytic anemia
gray baby syndrome - cyanosis, not administered to babies
CYP450 inhibitor
rare: aplastic anemia - fatal

A

Chloramphenicol

68
Q

ADVERSE EFFECTS

epigastric distress
cholestatic jaundice - bilirubin
ototoxicity
enzyme inhibitor

A

MACROLIDES

69
Q

ADVERSE EFFECTS

Pseudomembranous colitis

A

Clindamycin

70
Q

Erythromycin
Azithromycin
Clarithromycin
Telithromycin

A

MACROLIDES

71
Q

erythromycin was named

A

Ilosone
Ilotycin

72
Q

THERAPEUTIC APPLICATIONS

some anaerobes & certain gram negative bacteria

A

STREPTOGRAMINS

72
Q

ADVERSE EFFECTS

Phlebitis
arthralgias
myalgias

A

STRETOGRAMINS
Quinupristin / Dalfopristin

73
Q

ADVERSE EFFECTS

Gastrointestinal - N&V, diarrhea

74
Q

THERAPEUTIC APPLICATIONS

Vancomycin-resistant

75
Q

THERAPEUTIC APPLICATIONS

gram positive bacterias

A

Macrolides

76
Q

THERAPEUTIC APPLICATIONS

bacteroides & other anaerobes

A

Clindamycin

77
Q

THERAPEUTIC APPLICATIONS

Salmonellae, Meningococci, H. influenzae

A

Chloramphenicol

78
Q

INHIBITION OF NUCLEIC ACID SYNTHESIS

Inhibition of bacterial DNA synthesis by blocking of DNA gyrase and topoisomerase IV

A

FLUOROQUINOLONES

79
Q

topoisomerase produced by gram negative

A

tropoisomerase II

80
Q

topoisomerase produced by gram positive

A

topoisomerase IV

81
Q

QUINOLONE | GENERATION

Nalidixic acid

82
Q

a quinolone that has no fluorine in its structure

A

nalidixic acid

83
Q

QUINOLONE | GENERATION

Ciprofloxacin
Ofloxacin
Norfloxacin

84
Q

QUINOLONE | GENERATION

Levofloxacin

85
Q

QUINOLONE | GENERATION

Moxifloxacin

86
Q

QUINOLONE | GENERATION

  • used less often today
  • have moderate gram-negative activity
  • achieve minimal serum concentrations
  • restricted to the treatment of uncomplicated urinary tract infections
86
Q

QUINOLONE | GENERATION

  • have expanded gram negative activity
  • have some activity against gram positive and atypical organisms such as Mycoplasma pneumoniae and Chlamydia pnuemoniae
87
Q

QUINOLONE | GENERATION

  • retain expanded gram negative activity
  • show improved activity against atypical organisms and specific gram positive bacteria
87
Q

QUINOLONE | GENERATION

  • shows improved gram positive coverage
  • maintains gram negative activity
  • gains anaerobic coverage
87
Q

ADVERSE EFFECTS

N&V, diarrhea
HA or dizziness
Phototoxicity - sensitivity to light
Cartilage erosion (arthropathy) - not advisable for <18 y/o, affects tendon
Contraindicated to patients with arrythmia
Drug interactions with antacids and cations

A

FLUOROQUINOLONES

88
Q

ADVERSE EFFECTS

  • Toxic effects are manifested by fever, skin rashes, gastrointestinal disturbances, depression of the bone marrow leading to anemia or agranulocytosis, hemolytic anemia, and liver and kidney function abnormalities
  • SJS - Stevens Johnson Syndrome
  • crystalluria
  • jaundice
  • kernicterus
A

SULFONAMIDES

89
Q

Drugs for Tuberculosis

  • binds to DNA-dependent RNA polymerase and thus inhibits RNA synthesis in bacteria
  • has different mechanism, targets nucleic acid synthesis
  • ADVERSE REACTION: orange color to urine, saliva, and sweat (harmless)
90
Q

Drugs for Tuberculosis

  • inhibits mycolic acid synthesis
  • targets cell wall of the MO
  • ADVERSE REACTION: Liver toxicity, Peripheral neuritis (nerves)
A

ISONIAZID

+ VIT B6

92
Q

Drugs for Tuberculosis

  • inhibits mycolic acid synthesis
  • targets the cell wall of the MO
  • ADVERSE REACTION: Hepatoxicity, N&V, hypersensitivity, hyperuricemia
A

Pyrazinamide

93
Q

Drugs for Tuberculosis

  • inhibits the synthesis of arabnogalactan
  • targets the cell wall of the MO
  • ADVERSE REACTIONS: Optic neuritis w/ blurred vision, red-green color blindness
A

Ethambutol

94
Q

o Leprosy
o SE: hemolytic anemia, gastrointestinal intolerance, fever, itching, and rashes

95
Q

o Antiprotozoal and for bacterial anaerobic infections
o SE: Stomatitis, diarrhea, and nausea

A

METRONIDAZOLE

MICROPARA (37 decks)

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