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MT 6314 - 3RD SHIFTING > BETA LACTAMS & CELL WAL SYNTHESIS INHIBITORS > Flashcards

BETA LACTAMS & CELL WAL SYNTHESIS INHIBITORS Flashcards

definition of terms, penicillins and cephalosporins

1
Q

antimicrobial drug that can eradicate an infection in the absence of host absence of host defense mechanisms

A

Bactericidal

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2
Q

Kills bacteria

A

Bactericidal

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3
Q

Does not kill bacteria

A

Bacteriostatic

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4
Q

antimicrobial drug that inhibits antimicrobial growth but requires host defense mechanism to eradicate the infection

A

Bacteriostatic

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5
Q

Slows down the proliferation of bacteria

A

Bacteriostatic

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6
Q

Lowest concentration of antimicrobial drug capable of inhibiting growth of an organism in a defined growth medium

A

Minimum inhibitory concentration (MIC)

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7
Q

Bacterial cytoplasmic membrane proteins that act as the initial receptors for penicillins and other beta-lactam antibiotics

A

Penicillin-binding proteins (PBPs)

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8
Q

More toxic to the invader than to the host; a property
of useful antimicrobial drugs

A

Selective toxicity

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9
Q

Bacterial enzymes involved in the cross-linking of linear peptidoglycan chains, the final step in cell wall synthesis

A

Transpeptidases

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10
Q

Drugs with structures containing a beta-lactam ring: includes the penicillins, cephalosporins and carbapenems.

A

Beta-lactam antibiotics

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11
Q

This ring must be intact for antimicrobial action

A

Beta-lactam antibiotics

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12
Q

T or F: Beta-lactam are bactericidal drugs?

A

T

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13
Q

Chains of polysaccharides and polypeptides that are cross-linked to form the bacterial cell wall

A

Peptidoglycan

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14
Q

Drugs that are not as important as beta-lactam drugs

A
  • Vancomycin
  • Fosfomycin
  • Bacitracin
    (VBF)
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15
Q

Major antibiotics that inhibit cell wall synthesis

A
  • Penicillins
  • Cephalosporin
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16
Q

Bacterial enzymes (penicillinases, cephalosporinases) that hydrolyze the beta-lactam ring of certain penicillins and cephalosporins; CONFER RESISTANCE

A

Beta-lactamases

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17
Q

Potent inhibitors of some bacterial beta-lactamases used in combinations to protect hydrolyzable penicillins from inactivation

A

Beta-lactam inhibitors

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18
Q

Drugs that inhibit the growth/replication, or kill microorganisms

A

Antimicrobials

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19
Q

What are the 5 subgroups of Antimicrobials

A
  • Antibacterial (Bacteria)
  • Antifungal (Fungi)
  • Antiviral (Viruses)
  • Anti-protozoal
  • Anti-parasitic (Parasite)
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20
Q

T or F:
Beta Lactams are composed of unusual 5-member ring that is common to all members

A

F, 4-member ring dapat

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21
Q

Production of antibiotic-inactivating enzymes

A

Microbial Resistance

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22
Q

What are the (3) bacterial cell wall synthesis inhibitors?

A
  • Penicillins (Narrow spectrum, Wider Spectrum)
  • Cephalosporins (Narrow spectrum, Wider Spectrum)
  • Miscellaneous (Carbapenems, Aztreonam, Vancomycin
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23
Q

T or F:

On Cephalosporins, 2nd to 4th generations are under narrow spectrum.

A

False, under siya ng WIDER SPECTRUM

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24
Q

T or F:

On Cephalosporins, 1st generation is under narrow spectrum.

A

True

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25
Q

T or F:

On Penicillins, Penicillinase Susceptible and Penicillinase resistant.

A

True

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26
Q

Changes in the structure of target receptor is called?

A

Microbial Resistance

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27
Q

Give the Pros and Cons of Penicillin Narrow Spectrum

A

Pros: effective only if bacteria is susceptible

Cons: only cover few species of bacteria

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28
Q

Give the Pros and Cons of Penicillin Wider Spectrum

A

Pros: covers more bacteria agents

Cons: can also kill normal flora which inhibits other
bacteria, has many side effects

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29
Q

Penicillin susceptible or Penicillin resistant?

Q: Can cleave/alter penicillin

A

Penicillin susceptible

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30
Q

Penicillin susceptible or Penicillin resistant?

Q: Not affected by penicillin

A

Penicillin resistant?

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31
Q

First to suggest that a Penicillium mold (now known as Penicillium chrysogenum) must secrete an antibacterial substance

A

Sir Alexander Fleming

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32
Q

First to concentrate the active substance involved, which he named penicillin, in 1928

A

Sir Alexander Fleming

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33
Q

Derivatives of 6-aminopenicillanic acid

A

Penicillin

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34
Q

The beta-lactam ring structure of Penicillin is essential for?

A

Antibacterial activity

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35
Q

The beta-lactam ring structure of Penicillin alters what?

A

Pharmacokinetics (makes it more lipophilic or hydrophilic)

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36
Q

Penicillin subclasses have additional chemical substitu- ents that confer differences in what?

A
  • Antimicrobial activity
  • Susceptibility to acid and enzymatic hydrolysis
  • Biodisposition (e.g. urine or bile)
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37
Q

What are the beta-lactam compounds?

A
  • Thiazolidine ring
  • β-lactam ring
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38
Q

What beta-lactam compound reacts with receptors?

A

Thiazolidine ring

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39
Q

What beta-lactam compound that carries a secondary amino
group (RNH–) → alters pharmacokinetics?

A

β-lactam ring

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40
Q

The pharmacokinetics of Penicillins vary on what?

A
  • Vary in their oral bioavailability (F)
  • Vary in resistance to gastric acid
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41
Q

T or F: Penicillins are polar?

A

T

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42
Q

T or F: Penicillins are metabolized extensively?

A

F, not metabolized extensively

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43
Q

Penicillins are usually excreted unchanged in urine via?

A
  • Glomerular filtration
  • Tubular excretion (inhibited by probenecid)
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44
Q

T or F: Penicillins must be given on an empty stomach?

A

T

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45
Q

Nafcillin is excreted mainly where?

A

Bile

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46
Q

T or F: Penicillins cross the blood-brain-barrier only when the meninges are inflammed?

A

T

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47
Q

T or F: Amoxicillin must be given on an empty stomach

A

F

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48
Q

Plasma half life of Penicillin vary from?

A

30 min to 1 hr

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49
Q

What are the forms of Penicillin G?

A

Procaine and benzathine
(administered itramuscularly)

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50
Q

Procaine and benzathine are administered via?

A

IM (Intramuscular)

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51
Q

Penicillins inhibit cell wall synthesis by?

A
  • BINDING of the drug to specific enzymes (penicillin-binding proteins [PBPs]) located in the bacterial cytoplasmic membrane
  • INHIBITION of the transpeptidation reaction that cross-links the linear peptidoglycan chain constituents of the cell wall
  • ACTIVATION of autolytic enzymes that cause lesions in the bacterial cell wall.
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52
Q

Enzymatic hydrolysis of the beta-lactam ring results in the _____ _____ _______?

A

loss of antibacterial activity

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53
Q

Hydrolysis of the β-lactam ring by bacterial β-lactamases

A

Resistance

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54
Q

Modification of penicillin-binding proteins [PBPs]

A

Resistance

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55
Q

Changes in membrane permeability

A

Resistance

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56
Q

In some gram-_____ _____(eg, Pseudomonas aeruginosa), changes in the porin structures in the outer cell wall membrane may contribute to resistance by impeding access of penicillins to PBPs.

A

gram-negative rods

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57
Q

Formed by most staphylococci and gram (-) organisms

A

Beta-lactamases (Penicillinases)

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58
Q

Inhibitors of Beta-lactamases (Penicillinases) are used in combination
with penicillin to prevent their inactivation in the following?

A

■ Clavulanic acid
■ Sulbactam
■ Tazobactam

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59
Q

Structural changes in target PBPs. Another mechanism of bacterial resistance is responsible for?

A
  • Methicillin resistance (in Staphylococci)
  • Penicillin G (in Pneumococci)
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60
Q

What gram-negative rod bacteria changes in the porin structures in the outer cell wall membrane may contribute to resistance by impeding access of penicillins to PBPs.

A

P. aeruginosa

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61
Q

Narrow spectrum Penicillinase susceptible agents includes?

A
  • Penicillin G
  • Penicillin V
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62
Q

Very narrow spectrum Penicillinase resistant agents includes?

A
  • Methicillin (prototype - rarely used due to nephrotoxic potential)
  • Nafcillin
  • Oxacillin
  • Cloxacillin (Dicloxacillin) - newer
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63
Q

Very-narrow-spectrum penicillinase-resistant drugs is primarily used against what bacterial infection?

A

Staphylococcus aureus

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64
Q

Very narrow spectrum Penicillinase resistant agents includes?

A
  • Ampicillin and Amoxicillin
  • Piperacillin and Ticarcillin
65
Q

Penicillin G is administered via?

A

Parenteral

66
Q

T or F: Penicillin G has a limited spectrum activity?

A

T

67
Q

Penicillin G is used for infections caused by?

A
  • Streptococci
  • Meningococci
  • Gram (+) bacilli
  • Spirochetes
68
Q

What is the causative agent of syphilis?

A

Spirochetes
(Treponema pallidum)

69
Q

What bacteria/s is/are resistant via production of beta-lactamases?

A
  • S. aureus
  • N. gonorrhoeae
70
Q

What is the drug of choice for syphilis?

A

Penicillin G

71
Q

Penicillin V is used for?

A

Oral or Oropharyngeal Infection

72
Q

Penicillin G are susceptible to?

A

Beta-lactamases

73
Q

For Pen G:
Activity against enterococci is enhanced by coadministration of ______?

A

Aminogylcosides

74
Q

Their primary use is in the treatment of known or suspected staphylococcal infections.

A

Very-narrow-spectrum penicillinase-resistant drugs

75
Q

Resistant to other members of this subgroup and often to multiple antimicrobial drugs

A

Methicillin-resistant S. aureus (MRSA)

and

S. epidermidis (MRSE)

76
Q

Since Methicillin is now rarely used, what are the alternative drugs used?

A

Oxacillin and Cloxacillin

77
Q

These drugs make up a peni- cillin subgroup that has a wider spectrum of antibacterial activity than penicillin G

A

Ampicillin and amoxicillin

78
Q

Remains susceptible to penicillinases

A

Ampicillin and amoxicillin

79
Q

Their clinical uses include indications similar to penicillin G

A

Ampicillin and amoxicillin

80
Q

In (1) e______ and l______infections, ampicillin is (2) synergistic with _____?

A

(1) enterococcal and listerial infections

(2) synergistic with aminooglycosides

81
Q

T or F: Ampicillin and amoxicillin, when used in combination with inhibitors of penicillinases (eg, clavulanic acid), their antibacterial activity is often not enhanced

A

F, their antibacterial activity is often ENHANCED

82
Q

These type of penicillin drugs have activity against several gram-negative rods
(including Pseudomonas, Klebsiella spp. & Enterobacter)

A

Piperacillin and Ticarcillin

83
Q

Piperacillin and Ticarcillin enhanced activity against gram (-) rods of which bacteria?

A

■ Pseudomonas
■ Enterobacter
■ Some cases of Klebsiella species

84
Q

T or F: Piperacillin and Ticarcillin have Synergistic action with aminoglycosides?

A

T

85
Q

T or F: Piperacillin and Ticarcillin is susceptible to penicillinases?

A

T

86
Q

Can cause interstitial nephritis more than other penicillins

A

Methicillin

87
Q

This results to cross reactivity of penicillins

A

Allergy

88
Q

Can cause maculopapular rash (not allergic)

A

Ampicillin

89
Q

Can cause neutropenia

A

Nafcillin

90
Q

caused by direct irritation or by overgrowth of gram (+) organisms or yeasts

A

Pseudomembranous colitis

91
Q

Ampicillin has been implicated?

A

Pseudomembranous colitis

92
Q

More stable to many bacterial β-lactamases

a. penicillins
b. cephalosporins
c. cefazolin
d. cefuroxime

A

b. cephalosporins

93
Q

It has a broader spectrum of activity

A

Cephalosporins

94
Q

What are the 2 sites of attachment in Cephalosporins?

A

R1 group
R2 group

95
Q

modifies pharmacokinetic profile

A

R1 group at 3 position

96
Q

alters antimicrobial activity

A

R2 group at 7 position

97
Q

Cephalosporins is a derivate of?

A

7-aminocephalosporanic acid

98
Q

T or F: Cephalosporins contains beta-lactam structure?

A

T

99
Q

Most cephalosporins are administered via ____?

A

parenteral

100
Q

T or F: Cephalosporins are also available for oral use?

A

T
(Cefdinir, Cefixime, Cephalexin)

101
Q

Cephalosporins with SIDE CHAINS undergo _____?

a. Biliary excretion
b. Renal clearance
c. Hepatic metabolism
d. Hydrolysis

A

C. Hepatic Metabolism

102
Q

Major elimination of cephalosporin is by ____?

A

renal tubular excretion (via active tubular secretion)

103
Q

How many generations of drugs are present in cephalosporins?

A

4

104
Q

In what generation of drugs does this happen?

“These drugs do not cross BBB and enter CSF even when the meninges are inflamed”

A

1st and 2nd generation drugs

105
Q

In what generation of drugs does this happen?

“These drugs are mainly excreted in the bile”

A

3rd generation drug (Cefoperazone and Ceftriaxone)

106
Q

Tor F: 1st and 2nd generation drug can be used to treat meningitis

mentioned in the recording

A

F, we cannot use 1st and 2nd generation drugs for meningitis

107
Q

T or F: Cephalosporins are bactericidal against susceptible organisms?

A

T

108
Q

T or F: Cephalosporins have a similar mechanism of action to those of penicillins?

A

T
(same sila na nag bbind with PBPs on bacterial cell membranes to inhibit bacterial cell wall synthesis)

109
Q

Cefazolin, Cephalexin, and Cefadroxil are under what generation of drugs?

A

1st generation drugs

110
Q

In 1st generation drugs, which one is the prototype?

A

Cephalexin

111
Q

In 2nd generation drugs, which one is the prototype?
(kinuha ko lang to sa recording ni sir)

A

Cefuroxime

112
Q

In 3rd generation drugs, which one is the prototype?
(kinuha ko lang to sa recording ni sir)

A

Ceftriaxone

113
Q

Cephalexin is admistered via ____?

A

Oral

114
Q

Cephalexin is under what generation of drugs?

A

1st generation drug

115
Q

Cefazolin is admistered via ____?

A

Parenteral

116
Q

Cefazolin is under what generation of drugs?

A

1st generation drug

117
Q

What drugs are mainly excreted in the bile?

A

Cefoperazone and Ceftriaxone

118
Q

T or F: Cephalosporins are more susceptible to penicillinase produced by staphylococci

A

F, less susceptible

119
Q

MRSA (Methicillin-resistant staphylococci) are also
______ to cephalosporins

a. susceptible
b. resistant

from the book

A

b. resistant

120
Q

They are active against gram-positive cocci, including staphylococci and common streptococci.

What generation of drugs is this this?

A

1st generation drugs

121
Q

1st generation of drug has MINIMAL ACTIVITY to ____?

a. gram-negative cocci
b. enterococci
c. MRSA
d. most gram-negative rods
e. all of the above

A

e. all of the above

122
Q

Cephalexin is used to treat what kind of infection?
(kinuha ko lang to sa recording ni sir)

a. Upper respiratory tract infection
b. Skin Infection
c. Both a and b
d. none of the above

A

c. both a and b

123
Q

What drug in the first-generation drug has a longer duration of action and a similar spectrum of action, compared to other first-generation drugs. It penetrates well into bone

A

Cefazolin

124
Q

Drugs in this subgroup usually have SLIGHTY LESS activity against gram-positive organisms than the first-generation drugs but have an EXTENDED gram-negative coverage.

A

2nd generation drugs

125
Q

T OR F: Anaerobic coverage is present in 2nd generation drugs?

A

T

126
Q

What drugs are under anaerobic coverage present in 2nd generation drugs?

A

Cefotetan, Cefoxitin

127
Q

What 2nd generation drugs are used to treat infection caused by anaerobic Bacteroides fragilis?

A

Cefotetan, Cefoxitin

128
Q

What 2nd generation drugs are used to treat sinus, ear, and respiratory infection caused by H. influenzae or M. catarrhalis?

A

Cefamandole, Cefuroxime, Cefaclor

129
Q

What drug in the 2nd generation crosses the blood-brain barrier, and can be used for community-acquired bronchitis or pneumonia in the elderly and for patients who are immunocompromised

A

Cefuroxime sodium

130
Q

What drug in the 2nd generation is administered twice daily? This drug is well absorbed and is active against beta-lactamase-producing organisms

A

Cefuroxime Axetil

131
Q

These drugs under 3rd generation do not penetrate the blood-brain barrier.

A

Cefoperazone and cefixime

132
Q

Ceftazidime, Cefoperazone and Cefotaxime are under what generation of drugs?

A

3rd generation

133
Q

This generation of drugs has an INCREASED activity against gram-negative organisms resistant to other beta-lactam drugs and the ABILITY TO PENETRATE the blood-brain barrier

A

3rd generation

134
Q

This drug under 3rd generation is used to treat gonococcal urethritis and it is administered via?

A

Ceftriaxone, administered via IV

135
Q

Third generation drugs are most ACTIVE against what bacterias?

A
  • Providencia
  • Serratia marcescens
  • Beta-lactamase producing strains of H. influenzae and Neisseria
136
Q

Third generation drugs are LESS ACTIVE against what bacteria?

A
  • Enterobacter strains that produce extended-spectrum beta-lactamases
137
Q

What 3rd generation drugs are currently the most active cephalosporins against penicillin-resistant pneumococci (PRSP Strains)?

A

Ceftriaxone and Cefotaxime

138
Q

This 3rd generation drug is used to treat Pseudomonas and serious infection

A

Cefoperazone, Ceftazidime

139
Q

This 3rd generation drug is used to treat B. fragilis and serious infection

A

Ceftizoxime

140
Q

What is the drug of choice for gonorrhea?

A

Ceftriaxone (parenteral) and Cefixime (oral)

141
Q

A single injection of _______ (3rd generation drug) is usually effective as a 10-day course of treatment for otitis media with AMOXICILLIN

A

Ceftriaxone

142
Q

This 3rd generation drug penetrates well into the CSF

A

Cefotaxime

143
Q

This 3rd generation drugs are administered orally once daily

A

Cefdinir, Cefixime

144
Q

This 3rd generation drug is excreted in bile and may be used in patients with renal insufficiency. It has good penetration into bone

A

Ceftriaxone

145
Q

What 4th generation drug is more resistant to beta-lactamases produced by gram-negative organisms, including Enterobacter, Haemophilus, Neisseria, and some penicillin- resistant pneumococci?

A

Cefepime

146
Q

4th generation drug that combines the gram-positive activity of first-generation agents with the wider gram-negative spectrum of third-generation cephalosporins.

A

Cefepime

147
Q

4th generation drug that has activity in infections caused by methicillin-resistant staphylococci (MRSA)

A

Ceftaroline

148
Q

4th generation drug that is active against Pseudomonas aeruginosa

A

Cefepime

149
Q

T or F: Cephalosporins can cause allergy like skin rashes to anaphylactic shock

A

T

150
Q

T or F: Complete cross-hypersensitivity exists with cephalosporins

A

T

151
Q

T or F: There is a cross-reactivity between penicillin and cephalosporins

A

T

152
Q

Give 3 OTHER adverse effects of cephalosporins

A
  • Pain at IM Injection sites
  • Phlebitis after IV injection
  • Increase nephrotoxicity of amino glycosides
153
Q

Drugs containing a methylthiotetrazole group such as ______, ______, & ______ may cause hypoprothrombinemia and disulfiram-like reactions with ethanol

A

Cefamandole, Cefoperazone, Cefotetan

154
Q

What generation of drugs is NOT useful against Enterobacter?

A

2nd and 3rd generation drugs

155
Q

What generation of drugs is USEFUL against Enterobacter infections?

A

4th generation drugs

156
Q

Cephalosporins are inactive against?

A
  • Listeria
  • Atypicals
  • Methicillin-resistant staphylococcus aureus (MRSA) - except ceftaroline
  • Enterococcus

“LAME”

157
Q

Renal adverse reaction of cephalosporins

A

Interstitial nephritis and tubular necrosis

158
Q

Hematologic adverse reaction of cephalosporins

A

Hypoprothrombinemia and bleeding disorders (Cefotetan, cefamandole, cefmetazole, and
cefoperazone)

MT 6314 - 3RD SHIFTING (3 decks)

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