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Antibacterials I Flashcards

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1
Q

What are the examples of inhibitors of cell wall synthesis ?

A

β-lactams, cycloserine, vancomycin and bacitracin

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2
Q

What are the categories of β-lactam antibacterials?

A

Penicillins
Cephalosporins
Monobactams
Carbapenems

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3
Q

What are the two enzymatic activities of Penicillin Binding Proteins?

A

Transpeptidase: cross-links amino acid side chains
Glucosyltransferase: links subunits of glycopeptide polymer

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4
Q

What is the general structure of penicillins?

A

Penicillin nucleus
6-amino acid penicillanic acid
β-lactam nucleus

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5
Q

What is the general structure Cephalosporins?

A

Cephalosporin Nucleus
7 - amino acid cephalosporanic acid
β-lactam nucleus

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6
Q

Are β-lactams mainly bactericidal or bacteriostatic?

A

Mainly bactericidal

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7
Q

What is the mechanism of action of β-lactams?

A

Bind to specific PBP located inside bacterial cell wall

Inhibit transpeptidase

Inhibit peptidoglycan cross-link formation during cell wall synthesis

Bacterial cell wall enzymes (autolysis) cause lysis

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8
Q

What is the spectrum activity of Penicillins?

A

Gram +/-
Anaerobes

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9
Q

What is the spectrum activity of Carbapenems?

A

Broad Gram -
Anaerobes
Narrow Gram +

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10
Q

What is the spectrum of activity of Monobactams?

A

Aerobic
Gram -

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11
Q

What is the spectrum activity of Cephalosporins?

A

1st and 2nd generations: Mostly gram + and some gram -

3rd and 4th generations: Most gram -

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12
Q

What is the mechanism of bacterial resistance to penicillins and cephalosporins?

A

Inactivation of drug by β-lactamase

Altered structure of PBP

Efflux pump

Presence of permeability barrier: mainly occurs in gram - bacteria that have an outer membrane that limits penetration of hydrophilic antibiotic

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13
Q

What are β-lactamases?

A

A family of enzymes that limit the efficacy of β-lactams

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14
Q

Can the β-lactamase activity be transferred?

A

Yes, it is genetically controlled and can be transferred from one bacterium to the next (through the transfer of plasmids)

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15
Q

What are the classes of penicillins?

A

Natural Penicillin
β-lactamase resistant penicillins
Extended spectrum (β-lactamase sensitive)

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16
Q

What are the examples of natural penicillins?

A

Benzyl-penicillin & analogs

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17
Q

What are examples of extended spectrum penicillins?

A

Aminopencillins
Antipseudomonal Penicillins

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18
Q

What makes up the penicillin nucleus?

A

Thiazolidine ring and lactam ring

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19
Q

What is the chief structural requirement of the penicillin for?

A

Biological activity

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20
Q

What happens if there is metabolic transformation or chemical alteration to the penicillin nucleus?

A

Loss of all significant antibacterial activity

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21
Q

What are natural penicillins made from?

A

A fungus Penicillium Chrysogenum

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22
Q

Are natural penicillins resistant or sensitive to β-lactamases?

A

Sensitive to destruction

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23
Q

What are the pharmacokinetics of natural penicillins?

A

Penicillin G: IV or IM
Benzathine Penicillin G: IM (sustained release)!

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24
Q

What is the spectrum of activity pf natural penicillin, Penicillin G?

A

Gram +/- cocci
Gram + bacilli (non β-lactamase producing)

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25
What are the examples of non-β-lactamse producing Gram + bacilli?
Staphylococcus Streptococcus Pneumococcus Clostridium Neisseria meningitis Treponema
26
What is the pharmacokinetics of natural Penicillin, Penicillin V?
Given orally
27
What is the spectrum of activity of Penicillin V?
Same as Penicillin G but less potent Used in gonorrhoea and meningococcal meningitis
28
What are examples of β-lactamasse resistant penicillins?
Methicillin, nafcillin, oxacillin, cloxacillin, dicloxacillin, flucloxacillin
29
Which is the prototype of β-lactamase resistant penicillins?
Methicillin
30
What is the spectrum of β-lactamase resistant penicillins?
Same as Penicillin G but less potent Minimal activity against gram - infections
31
When are β-lactamase resistant penicillins used?
Mainly with β-lactamase -producing staphylococcus like MSSA
32
What are the different examples of extended spectrum penicillins?
Aminopenicillins Antipsuedomnal penicillins
33
What are the examples of aminopenicillins?
Ampicillin and Amoxicillin
34
What is the pharmacokinetics of Ampicillin?
Given orally or IV
35
What is the pharmacokinetics of Amoxicillin?
Given orally
36
What is the pharmacokinetics of Aminopenicillins?
Same as Penicillin G and have improved activity against Gram - Less potent than Penicillin G
37
What happens if you add β-lactamase inhibitor?
Further extends spectrum
38
What are the combinations of aminopenicillins and β-lactamase inhibitor?
Amoxicillin/ Clavulanate Ampicillin/Sulbactam
39
What are the examples of antipseudomonal penicillins ?
Carbepenicillin Ticarcillin Piparacellin
40
What is the spectrum of the antipseudomonal penicillins?
Same as aminopenicillins plus activity against pseudomonas, proteus, and klabsiella
41
What are the generalised pharmacokinetics of Penicillins?
Orally or Parenterally Widely distributed; exhibit 45 to 68% protein-binding mainly to albumin Penetrate inflamed meninges and reach CSF Eliminated via kidneys --> tubular secretion
42
What are the adverse effects of penicillins?
Hypersensitivity reactions GI disturbances Cross-sensitivity to other penicillins or cephalosporins
43
What are some examples of therapeutic use of Penicillins?
Meningitis Listeriosis Endocarditi Anaerobic LRTI URTI Anthrax Gonorrhoea Syphilis
44
What are examples of the β-lactamase inhibitor?
Clavulanic acid Tazobactam Sulbactam
45
Mechanism of action of β-lactamase inhibitor?
Resemble β-lactams in structure, No significant antibacterial activity Inhibit many β-lactamases
46
What is Augmentin?
Combination of β-lactamase inhibitor with hydrolazable β-lactams Amoxicillin + Clavulanic Acid
47
What do the side chain modifications of the cephem nucleus confer?
Improved spectrum Pharmacokinetic advantages Additional side-effects
48
What are the similarities between penicillins and cephalosporins?
Similar to penicillins chemically, in MOA and toxicity
49
What are the differences between Penicillins and cephalosporins?
Cephalosporins are more stable than penicillins to β-lactamases Broader spectrum than penicillins
50
How many generations of cephalosporins are there?
4 + 1 generations
51
What are the examples of first generation cephalosporins?
Cephadroxin Cephalexin Cafzolin
52
What are examples of the second generation cephalosporins?
Cefuroxime Cefaclor Cefprozil Cefoxitin Cefofetan
53
What are examples of the third generation of cephalosporins?
Cefotaxime Ceftriaxone Cefdinir Cefixime
54
What are examples of the fourth generation of cephalosporins?
Cefepime Cefpirome
55
What are the examples of advanced generation?
Ceftaroline Ceftobiprole
56
What is the spectrum of activity as the generations of cephalosporins progress?
Gram + activity becomes less, Gram - increases
57
Which cephalosporin generation covers pseudomonas?
4th generation
58
Which cephalosporin generation covers MRSA?
5th generation
59
What is the spectrum of generation 1 cephalosporins?
Really good against Gram +, moderate activity against Gram - Does not penetrate CSF
60
What are some Gram - bacteria that are covered by first generation cephalosporins?
E.coli, Proteus Mirabilis K. pneumonia
61
Clinical use of first generation cephalosporins?
Skin and soft tissue infections, serious infections due to MSSA Perioperative surgical prophylaxis
62
What is the spectrum of activity for 2nd generation cephalosporins?
Slightly less active against gram +, better activity against Gram - Do not penetrate CSF
63
What are the Gram - bacteria targeted by 2nd generation cephalospsorin?
Hemophilus E. coli Enterobacter Klabsiella Neisseria
64
Clinical use of 2nd generation cephalosporins?
Perioperative surgical prophylaxis Management of URTI, urinary tract, bone & soft tissue infections
65
What is the spectrum of third generation cephalosporins?
Less potent against gram + and better activity against gram -
66
What are some gram - bacteria that are targeted with 3rd generation cephalosporins?
Pseudomonas aeruginosa Enteribacter Salmonella
67
What are the pharmacokinetics of 3rd generation cephalosporins?
Most penetrate CSF
68
Clinical use of 3rd generation cephalosporins?
Serious hospital-acquired gram - infection, LRTI, UTI, meningitis, Lyme disease
69
What are some Gram - organisms that are targeted by 4th generation cephalosporins?
Pseudomonas aeruginosa Enteribacter S. aerus S. pneumoniae Hemophilus Neisseria
70
What are the pharmacokinetics of 4th generation cephalosporins?
Excellent penetration into CSF
71
What are the PK of 4th generation cephalosporins?
Stable to hydrolysis by many β-lactamases
72
What is the spectrum of advanced generation cephalosporins?
Broad gram + Strong activity against gram -
73
What are the bacteria targeted by advanced generation cephalosporins?
Excellent activity against MRSA, MSSA, H. Influenza, Proteus, E. coli Klabsiella Serratia
74
What are clinical uses of advanced generation of cephalosporins?
Treatment of complicated skin and skin structure infections and CAP
75
What are the adverse effects of Cephalosporins?
GI disturbances Hypersensitivity reactions Nephrotoxicity Intolerance to alcohol Bleeding disorders
76
Which kind of cephalosporin is not nephrotoxic?
Cefotaxime
77
What are the two kinds of β-lactams that are resistant to β - lactamases?
Monobactams Carbapenems
78
What is an example of monobactams?
Aztreonam
79
What are monbactams?
Synthetic Bacteriocidal
80
Which group confers the activity of aztreonam?
SUlfonic acid
81
What are examples of carbapenems?
Imipenem Doripenem Ertapenem Meropenem
82
Spectrum of activity of carbapenems?
Broadest spectrum of activity
83
Antibacterial spectrum of aztreonam?
Different to the other β-lactams Spectrum limited to gram (-) aerobic bacteria No gram + or anaerobic activity
84
Which drug group does the spectrum of monobactams resemble?
Aminoglycosides
85
Which bacteria are targeted by monobactams?
Enterobacteriaceae and P. aeruginosa
86
What would monobactams be used as an alternative of and why?
As an alternative to aminoglycosides because they have similar spectrum but monobactams are less nephrotoxic
87
Clinical use of monobactams?
Skin and soft tissue infections UTI RTI Intra-abdominal infections Postoperative infections Gynecologic infections
88
Are monobactams indicated for meningitis?
No
89
What is another reason for the use of monobactams for patients that cannot take penicillin?
They do not tend to have a reaction to monobactams even if they are allergic to both penicillins and cephalosporins
90
Spectrum of activity of carbapenems?
Active against a wide range of gram + and gram - organisms Highly active against Enterobactericeae
91
What are the traits that carbapenems have that make them effective antibiotics?
Efficient penetration through bacterial cell wall Exceptional stability against β-lactamases Affinity for all PBP (widest spectrum)
92
What is Imipenem rapidly metabolised by?
Dehydropeptidase 1
93
Where is dehydropeptidase 1 found?
Renal tubular border
94
What do the imipenem metabolites cause?
Nephrotoxicity (toxicity to proximal tubule)
95
What is cilastatin?
Reversible, competitive inhibitor of DHP 1 enzyme --> no imipenem metabolites --> no nephrotoxicity
96
Does cilastatin have any antibacterial activity?
No
97
What are the therapeutic uses of Imipenem - Cilastatin combination?
UTI Nosocomial LRTI Intra-abdominal and gynaecological infections Skin, soft tissues, bone and joint infections Meningitis Peritonitis
98
Which drug exactly would be used for the treatment of meningitis?
Meropenem
99
What are the PK of the imipenem-cilastatin combination?
IV When given with cilastatin, about 70% of imipenem can be excreted unchanged in the urine
100
What are the adverse effects of Imipenem - Cilastatin combination?
GI disturbances Seizures (rarely) Hypersensitivity reaction if allergic to other β-lactams
101
Why does meropenem not require co-administration with cilastatin?
It is not sensitive to renal dehydropeptidase 1 like imipenem is
102
What is the spectrum of activity of Meropenem?
Similar to imipenem, but also targets some imipenem-resistant bacteria Less activity against gram + cocci
103
What is an imipenem-resistant bacteria that is targeted by meropenem?
Pseudomonas aeruginosa
104
Compared to imipenem is meropenem nephrotoxic?
No, not sensitive to DHP 1
105
Compared to imipenem is meropenem more or less likely to cause seizures?
Less likely
106
What is Vancomycin?
A glycopeptide
107
Is Vancomycin bactericidal or bacteriostatic?
Bacteriocidal
108
What is the mechanism of action of Vancomycin?
High affinity binding to d-alanyl-d-alanine (terminus of peptidoglycan precursors) Prevents transpeptidase action on NAM & NAG Disrupt polymerization and cross-linking
109
What is another function of Vancomycin?
Inhibits transglycosylase
110
What is the spectrum of Vancomycin?
Mainly against Gram + bacteria NOT effect against most gram - bacteria
111
What are some bacteria that are targeted by Vancomycin?
Strep Staph (MRSA) Enterococcus Pneumococcus Listeria Corynebacteriu Bacilus Clostridium Difficile
112
What are the PK of Vancomycin?
Poorly absorbed after oral Given IV 30% of Vancomycin is plasma bound, appears in body fluids Renal excretion Slow CSF penetration
113
What are the adverse effects of Vancomycin?
Nephrotoxicity Ototoxicity Rapid IV transfusion = erythematous reaction --> Red man syndrome Hypersensitive reactions
114
What are the therapeutic uses of Vancomycin?
Skin and soft tissue, bone and joint infections RTI CNS infections (Community and hospital-acquired meningitis) Endocarditis Vascular Catheter Infections Psudomembranous Colitis
115
When can Vancomycin be given orally?
If it is for C. difficile

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