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Beta lactam antibiotics Flashcards

Quiz 1

1
Q

What are the types of ß-lactam antibiotics?

A
  1. penicillin
  2. cephalosporin C
  3. carbapenems
  4. monobactams
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2
Q

what is the mechanism of action for ß-lactam antibiotics ?

A
  1. inhibits bacterial cell wall synthesis
    - binds to PBP to interfere w/ transpeptidation rxn
  2. bactericidal action
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3
Q

what enzyme does ß-lactam antiobitics inhibits ?

A

transpeptidase enzyme

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4
Q

what is the function of transpeptidase enzyme ?

A

mediates cross linking of peptidoglycan strands w/. penicillin binding proteins

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5
Q

what are the microbial resistant beta lactam antibiotic?

A
  1. production of beta lactamase enzyme
  2. permeability of cell wall
  3. reduce sensitivity of penicillin binding protein
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6
Q

What are beta -lactam antibiotic only effective against ?

A

synthesized peptioglycan

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7
Q

what are the classification for penicillin ?

A
  1. natural penicillin

2. semi-synthetic

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8
Q

what are the types of semi-synethtiec penicillins?

A
  1. penicillinase -restant penicillin
  2. broad -spectrum penicillin
  3. extended spectrum /anti-pesudomonal penicillin
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9
Q

what are the type of natural penicillin?

A
  1. penicillin G

2. penicillin V

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10
Q

what is the microbial susceptibility of natural penicillin?

A

narrow spectrum

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11
Q

How is Penicillin G administered ?

A

parenteral

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12
Q

How is penicillin V administered ?

A

orally

-acid stable

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13
Q

What species of Gram + can treated with natural penicillin G of beta lactam ?

A
  1. streptococci
  2. staphylococci
  3. Corynebacterium
  4. L.monocytogenes
  5. P.multocida
  6. haemophilus influenzar
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14
Q

what type of staphylococci can not be treated with penicillin G ?

A

non-penicillinase producing sp.

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15
Q

what types of bacteria can penicillin G treat?

A
  1. Anaerobic gram +
  2. Anaerobic gram -
  3. spirochetes
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16
Q

what species of anaerobic gram - species can be treated with penicillin G?

A
  1. clostridium
  2. fusobacterium
  3. bactericides
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17
Q

what species of spirochetes can be treated with penicillin G ?

A
  1. borrelia

2. leptospira

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18
Q

what are the dosage forms of natural penicillin ?

A
  1. Na/k salt
  2. procaine penicillin
  3. benzathine penillicin
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19
Q

what does Na/K salt natural penicillin produces what ?

A

crystalline penicillin injection

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20
Q

what does procaine penicillin produce ?

A

long acting penicillin

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21
Q

what does Benzathine penicillin produce ?

A

repository preparation ( IM/intra-mammary )

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22
Q

what semi-synthetic penicillin has good stability against bacterial beta lactase enzyme ?

A

penicillinase resistant penicillin ( isoxazolyl penicillin

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23
Q

what are the compound of penicillinase resistant penicillin has good oral absorption ?

A

acid stable

  1. cloxacillin
  2. oxacillin
  3. dicloxacillin
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24
Q

what compounds of penicillinase resistant penicillin has poor oral absorption ?

A
  1. Nafcillin

2. methicillin

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25
what is the microbial suspectiility of penicillinase resistant penicillin?
1. penicillinase producing staphylococcus sp. | 2. bacterial infection of eye
26
what bacterial species do you use penicillinase resistant penicillin ?
bovine staphylococcal mastitis
27
what type of bacterial species are penicillinase restart penicillin used for bacterial infection of the eye ?
1. staphylococcus sp. | 2. bacillus sp
28
what type of penicillinase restart penicillin is used for bacterial infection of the eye ?
benzathine cloxazillin
29
what are the types of broad spectrum penicillin ?
beta-lactamase sensitive 1. amoxicillin 2. ampicillin
30
what are the prodrug forms of ampicillin?
1. bacampicillin 2. hetacillin 3. pivampicillin 4. talampicillin
31
what is the microbial suspectibility of broad spectrum penicillin?
1. microbe susceptible to natural penicillin | 2. Entrobacteriaceae
32
what are the species of Enterobacteriaceae that broad spectrum penicillin can be treated with?
1. e.coli 2. proteus mirabilis 3. salmonella
33
what should be administered with broad spectrum penicillin?
beta lactamase inhibitors
34
what are the types of extended spectrum/anti-pseudomonal penicillin of semi-synthetic penicillin ?
1. Ticarcillin 2. Carbenicillin 3. Piperacillin 4. mezlocillin 5. azlocillin : beta-lactamase sensitive
35
what is the microbial susceptibility of extended spectrum penicillin?
broad spectrum 1. gram - aerobic & anaerobic 2. Enterobacteriaceae 3. bactericides fragilis
36
what species of gram - aerobic & anaerobic microbe can be treated with extended spectrum penicillin?
1. E.coli 2. proteus mirabilis 3. salmonella 4. Pseudomonas sp.
37
what should be administered with extended spectrum penicillin ?
beta -lactamase inhibitor
38
what is the pharmacokinetics of penicillin for absorption?
1. formulated as Na/K salt ( crystalline pencilline) | 2. administered : oral/parental/intramammary route
39
what type of penicillins are administered orally?
1. penicillinase resistant penicillin 2. pencillin V 3. aminopenicillins
40
What happen if food is given with penicillin V & penicillinase restart penicillin ?
decrease
41
what is pharmacokinetics for absorption of aminopencillin?
1. oral 2. IM 3. SC 4. suspension in oil
42
What amino penicillin is more acid stable & has complete absorption ?
amoxicillin
43
what is the oral bioavailability for amoxicillin ?
60- 70%
44
what is the oral bioavailability for amPICILLIN ?
30- 40 % | -Ester form increase bioavailability
45
How is absorption of amino penicillin administered IM/SC route ?
rapid
46
how is absorption of aminopenicillin administered in suspension in oil?
prolongs absorption for 18 hrs
47
How is absorption of berzathine penicillin G ?
prolonged for more than 7 days
48
what is the caution for procaine penicillin G?
never administered by IV route → affects cardiac conduction system
49
what is the caution for benzathine penicillin G?
repository should be administered by IM route
50
what is the distribution of penicillin ?
1. weak organic acid → ionized in plasma 2. distributed in ECF 3. low permeation to CNS 4. sufficient concentration attained in synovial fluid, skin, soft tissues ,visceral organs 5. distributed in milk of lactating animals
51
what is the distribution for semi-synthetic groups ?
permeates more through cell membrane
52
what is the percentage for cloxacillin & nafcillin?
80%
53
what is the percentage for penicillin G ?
60%
54
what is the percentage for ampicillin?
20%
55
what is the pharmacokinetics of penicillin for metabolism ?
1. only 20% of administered dose undergoes metabolism | 2. peniclloic acid metabolite → allergic rxn
56
what is the pharmacokinetics of penicillin for excretion?
1. by kidney: - glomerular filtration - proximal tubular secretion 2. interaction w/ probenecid
57
How is nafcillin excreted ?
bile
58
what are the adverse effects of penicillin Ty?
1. anaphylactic rxn 2. superinfection 3. convulsion/ataxia 4. anaphylaxis & CNS disorder 5. excitement 6. acute cardiac toxicity
59
what animals would you see convulsion/ataxia from sodium benzyl penicillin ?
dogs | cats
60
what animals would you see anaphylaxis & CNS disorders from procaine penicillin?
1. rodent 2. birds 3. snakes 4. turtles
61
what animal would you see excitement from procaine penicillin ?
horses
62
what type of penicillin can cause acute cardiac toxicity from IV administration ?
procaine /potassium penicillin salts of penicillin G & ampicillin
63
What is cehalosporin?
1. semisynthetic ß-lactams 2. more resistant to ß-lactamase 3. classified base on spectrum
64
what are the classification of cephalosporin ?
1. 1st generation 2. 2nd generation cephalosporin 3. 3rd generation cephalosporin 4. 4th generation cephalosporin
65
what are types of first generation cephalosporins ?
1. Cefadroxil 2. cephalexin 3. cafazolin 4. cephalothin 5. Cephapirin 6. cefalonium
66
what first generation cephalosporins can be given orally?
1. cefadroxil | 2. cephalexin
67
what first generation cephalosporins can be given parenterally?
1. cefazolin | 2. cepharirin
68
what first generation cephalosporin is used as a ophthalmic ointment in dogs as well as intramammary for cattle ?
Cefalonium
69
what is microbial susceptibility for first generation cephalosporins?
1. Gram + bacteria | 2. gram - bacteria
70
what are the species of gram + bacteria that is susceptible to first generation cephalosporin ?
1. corynebacteria 2. streptococci 3. staphylococci ( beta lactamase positive)
71
what are the species of gram - bacteria that is susceptible to first generation cephalosporin ?
1. E.coli 2. Klebsiella pneumonia 3. H. influenzae 4. P. mirabilis 5. Actinobacillus 6. Pasteurella 7. Salminella
72
what first generation cephalosporin is very effective in treating Salmonella ?
cefazolin
73
what are the second generation cephalosporins?
1. Cefaclor 2. Cefotetan 3. Cefoxitin 4. Cefuroxime
74
what second generation cephalosporins is given parenterally that is grouped in the cephamycin group?
1. cefotetan | 2. Cefoxitin
75
what second generation cephalosporins can be given orally ?
cefaclor
76
what 2nd generation cephalosporins can be given orally or parenterally & crosses the blood brain barrier?
Cefuroxime
77
Cefotetan & Cefoxitin treat what type of microbes?
anaerobic microbes
78
what is the microbial susceptibility for 2nd generation cephalosporins ?
1. antibacterial action gram - bacterial infection 2. anaerobic bacteria (septic peritonitis) 3. Bacteriodes fragilis ( Cefoxitin & cefotetan 4. more resistant to cephalosporinase
79
what are 3rd generation cephalosporins?
1. Cefixime 2. Cefoperazone 3. cefotaxime 4. ceftiofur 5. Ceftazidime 6. Cefovecin 7. Cefpodoxime Proxetil
80
what 3rd generation cephalosporins can be administered orally ?
1. Cefixime | 2. Cefpodoxime Proxetil
81
what 3rd generation cephalosporins can be administered parenterally?
1. cefoperazone 2. Cefotazime 3. Ceftiofur 4. Ceftazidime 5. Cefovecin
82
what 3rd generation cephalosporin is used to treat Pseudomonas sp.?
Cefoperazone
83
what 3rd generation cephalosporins is used to treat Pseudomonas species & other gram - bacteria in exotic & zoo animals?
Ceftazidime
84
what 3rd generation cephalosporins are used in dog & cats for skin/pyoderma/ UTI infections?
1. Cefotaxime | 2. Cefovecin
85
what 3rd generation cephalosporins has a long 1/2 life that can be given as a single infection to treat skin/pyoderma/UTI infections?
Cefovecin
86
what 3rd generation cephalosporin is prodrug esters that metabolism in vivo & will release active drug ?
Cefpodoxime Proxetil
87
what is the microbial susceptibility of the 3rd generation cephalosporins ?
1. most effective gram - | 2. resistant bacterial organisms to other generation cephalosporins
88
what are the species of gram - bacteria that can be treated by 3rd generation cephalosporins ?
1. E.coli 2. Enterobacter 3. Klebsiella 4. Proteus 5. Serratia 6. Pseudomonas
89
what 3rd generation cephalosporin has a broader gram + activity & active against ß-lactamase producing bacteria & anerobes ?
Ceftiofur
90
what is Ceftiofur metabolized in vivo as ?
Desfuroylceftiofur ( active )
91
what are the indications for Ceftiofur?
1. Respiratory tract infection (cattle & pigs) 2. UTI (dogs) 3. Respiratory tract infection , pleurites & peritonitis ( horses) 4. E.coli infection ( poultry)
92
what are the 4th generation Cephalosporins ?
1. Cefepime | 2. Cefquinome
93
what generation of cephalosporins is used when there is an completely resistance bacterial infection?
4th generation
94
what is microbial susceptibility for the 4th generation cephalosporins ?
1. Broad spectrum 2. more resistant to ß-lactamase 3. effective against resistant infection
95
what are the species of bacteria that 4th generation cephalosporins are used on ?
1. gram + cocci | 2. gram - bacilli & pseudomonas aeruginosa
96
what are the pharmacokinetics in absorption for cephalosporins ?
1. well absorbed orally & parentally ( IM / SC) | 2. bioavailability depends on drug & species
97
what cephalosporins have higher oral absorption ?
1. Cephalexin | 2. Cefaclor
98
what is the pharmacokinetics in distribution for cephalosporins ?
1. attains high concentr. in many areas of the body | 2. penetrates the CSF
99
Where does cephalosporins maintain high concentration in the body?
1. blood 2. urine 3. bile 4. pleural fluid 5. synovial fluid 6. pericardial fluid 7. cortical bone 8. cancellous bone
100
what 2nd generation cephalosporins penetrates the CSF ?
Cefuroxime
101
what 3rd generation cephalosporins penetrates the CSF ?
1. Ceftriaxone 2. Ceftoaxime 3. Ceftazidime 4. Ceftizoxime
102
what is the pharmacokinetics in metabolism for cephalosporins ?
liver metabolizes to form dactyl derivatives
103
what is significant about the deacetylated metabolite of cefotazime ?
1. active metabolite | 2. longer half life parent cmpd
104
what is the pharmacokinetics in excretion for cephalosporins ?
kidneys excrete by : - glomerular filtration - Proximal tubular secretion
105
what cephalosporins are not excreted by the kidneys ?
1. Ceftriaxone | 2. Cefoperazone
106
what are the side effects for cephalosporins ?
1. Local tissue rxn at injected site 2. Hypersensitivity rxn 3. GI signs : V/D in small animals
107
what are the side effects of Ceftiofur at high doses in dogs ?
1. anemia | 2. Thrombocytopenia
108
what is the side effects of Cephalothin & cefmetazole ?
decrease platelet aggregation
109
what are Betalactamase inhibitors?
1. Clavulanic acid 2. Sulbactam 3. Tazobactam
110
what is pharmacokinetics for clavulanic acid as a betalactamase inhibitor?
1. Betalactam ring in structure 2. competitive inhibitor of betalactam antibiotic 3. attaches to catalytic center of beta lactamase prevent degradation of administered penicillin
111
what are type of clavulanic acid as betalactamase inhibitors?
1. Amoxicillin + potassium clavulanate | 2. ticarcillin _potassium clavulanate
112
what is the pharmacokinetics of sulbactam as betalactamase inhibitor?
1. pencillanic acid sulfone 2. increase antimicrobial activity 3. not absorbed orally
113
what is a type of sulbactam as a betalactamase inhibitor?
1. sodium sulbactam (parenteral preparation) | 2. ampicillin (IV/IM/SC)
114
what is the pharmacokinetics of tazobactam as a betalactamase inhibitor ?
1. used in combination w/ piperacillin for IV use | 2. treat resistant Pseudomonas aeruginosa
115
what are other betalactam antibiotics ?
1. Carbapenems (penems) 2. Meropenem 3. Monobactams
116
what is a type of carbapenems used as a betalactam antibiotic ?
Imipenem
117
what is the pharmacokinetics off Imipenem?
1. stable against ß-lactamase enzyme 2. administered w/ cilastatin 3. broadest spectrum of action 4. rapid bactericidal ; post antibiotic effect
118
what is the microbial spectrum for Imipenem for other betalactam antibiotics?
1. gram - aerobic & anaerobic bacteria | 2. serious resistant infection
119
what is a type of Imipenems used ?
Imipenems + Cilastatin
120
what is the adverse effect for Imipenems + cilastatin ?
seizures
121
what is the pharmacokinetics for meropenem as betalactam antibiotic ?
1. more soluble | 2. decrease incidence of adverse rxn
122
what is the pharmacokinetics for monobactam?
1. monocyclic beta lactam antibiotic 2. gram - aerobic bacteria & pseudomonas aeurginosa 3. stable against beta lactamase hydrolysis 4. poor inducer of bet a lactamase production 5. used in PT that are allergic to penicillin

SGU pharm II (5 decks)

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