Antio Flashcards

1
Q

What are most antibiotics derived from?

A

→natural products by fermentation

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2
Q

Why are antibiotics chemically modified?

A

→pharmacological properties ie can they survive in the stomach
→antimicrobial effect

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3
Q

What is an example of totally synthetic antibiotics?

A

→sulphonamides

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4
Q

What are natural products of fungi and bacteria derived from?

A

→- soil dwellers natural antagonism and selective advantage

→kill or inhibit the growth of other microorganisms

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5
Q

Why is there selective toxicity?

A

→Due to the differences in structure and metabolic pathways between host and pathogen

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6
Q

Why is selective toxicity difficult in viruses?

A

→intracellular

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7
Q

What are the principles of selective toxicity?

A

→Due to the differences in structure and metabolic pathways between host and pathogen
→Harm microorganisms, not the host
→Target in microbe, not host (if possible)
→Difficult for viruses (intracellular), fungi and parasites
→Variation between microbes
→effect on commensals

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8
Q

What is therapeutic margin?

A

→active dose (MIC) versus toxic effect

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9
Q

What types of drugs have narrow therapeutic margins?

A

→toxic drugs

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10
Q

Why is microbial antagonism important?

A

→Maintains flora

→Limits growth of competitors and pathogens

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11
Q

What happens with loss of flora?

A

→bacterial or pathogen overgrowth

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12
Q

Example of a disease cause by loss of flora

A

→Antibiotic Associated Colitis

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13
Q

Which bacteria can cause pseudomembranous colitis?

A

Clostridioides difficile

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14
Q

Which antibiotics most commonly cause colitis?

A

→Fluoroquinolones
→clindamycin,
→broad-spectrum lactams

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15
Q

What conditions cause immunosuppression?

A

→cancer chemotherapy,
→transplantations,
→myeloma,
→leukaemias,

→HIV with low CD4

→Neutropenics,
→asplenics,
→renal disease,
diabetes

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16
Q

How are antibiotics classified?

A

→Type of activity

→Structure

→ Target site for activity

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17
Q

What are bactericidal antibiotics?

A

→Kill bacteria

→Used when the host defense mechanisms are impaired

→Required in endocarditis, kidney infection

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18
Q

Describe bacteriostatic antibiotics

A

→Inhibit bacteria eg tetracyclin

→Used when the host defense mechanisms are intact

→Used in many infectious diseases

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19
Q

What might a bacteriostatic antibiotic become if dose is increased?

A

→bactericidal if dose is increased

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20
Q

Examples of broad spectrum antibiotics

A

→Cefotaxime

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21
Q

Example of narrow spectrum antibiotics

A

→Penicillin G

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22
Q

What are cephalosporins now most effective against?

A

→gram negatives

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23
Q

What are basic penicillin active against?

A

→streptococci,
→pneumococci,
→meningococci,
→treopnemes

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24
Q

Which bacteria are resistant against basic penicilin?

A

→Staphylococcus aureus

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25
What type of natural substance does penicilin have?
→Beta-lactams
26
What are anti-staphylococcal penicillin?
→narrow spectrum, →G+ves, →beta-lactamase resistant
27
Compare Pen G and Pen V?
Pen G →not acid stable →i/v or i/m →good for some G-ves as well as G+ves Pen V →oral (more acid stable than penG) →less active v G-ves, → same activity with G+ves as PenG
28
What are broader spectrum penicillins?
→Spectrum of activity is similar to basic penicillins but also includes some Gram-negative organsims and also enterococci
29
What are anti-pseudomonal penicillin?
→extended spectrum beta-lactam antibiotic →also G+ve, G-ve, anaerobes
30
Example of anti-pseudomonal penicillin
→piperacillin
31
What are beta-lactam/lactamase inhibitors?
→Spectrum like amoxicillin plus activity against some Gram-negatives and Staph aureus
32
What are pseudomonal?
→a major cause of lung infections in people with cystic fibrosis. →thrive in moist environments and equipment
33
What are the molecular structure classifications of antibiotics?
``` →nalidixic acid →ciprofloxacin →erythromycin →tetracycline →vancomycin →streptomycin(aminoglycosides) ```
34
What are beta lactams?
Structural mimics of natural substrates for enzymes
35
Why are beta-lactams important?
→Without B lactam there will be no antimicrobial property →stop bacterial growth by inhibiting PBPs that are indispensable for the cross-linking process during cell wall biosynthesis
36
Which bacteria have beta lactams?
→penicillin
37
What are carbepenams?
→effective antibiotic agents commonly used for the treatment of severe or resistant bacteria
38
What are the modes of actions of bacteria?
``` →cell wall synthesis →DNA →folic acid →metabolism →cell membrane →protein sythesis- 50S and 30S →DNA and RNA processing- Gyrase, DNA-directed RNA polymerase ```
39
Is tetracycline -cidal or static?
→static
40
How do antibiotics reach membrane of gram negatives?
→porins in outer membrane mediate the passive diffusion of antibiotics
41
What are the sites of action of inhibitors of bacterial cell wall synthesis?
→cytoplasm- synthesis of cell wall precursors →cytoplasmic membrane- synthesis of cell wall subunits →cell wall- new wall unit attachment
42
What are D-alanines?
→incorporated by PBPs into peptidoglycan
43
How does cycloserine inhibit bacteria cell wall synthesis?
→inhibits incorporation of alanine into cell wall precursor
44
How does vancomycin inhibit bacteria cell wall syntesis?
→bind to terminal D-ala D-ala residues to prevent incorporation of subunit into peptidoglycan
45
How does bacitracin inhibit bacteria cell wall synthesis?
→prevents dephosphorylation of phospholipid carrier which prevents regeneration of carrier to continue synthesis
46
How do penicillin and cephalosporins inhibit bacteria cell wall synthesis?
→inhibit enzymes which catalyse cross linking
47
Which bacteria is resistant against penicillin?
→mycoplasma pneumoniae | →have sterol packed cell membrane
48
What type of antibiotic are folic acid synthesis inhibitors?
→bactericidal | →broad spectrum
49
What are the targets of folic acid synthesis inhibitors?
→PABA | →dihydrofolate reductase- human DHFR is less inhibited hence selective toxicity
50
How do aminoglycosides inhibit protein sythesis?
→Binding fmet t-RNA Initiation complex formation | →streptomycin
51
How does gentamycin inhibit protein synthesis?
→Translocation of fmet t-RNA | to P site
52
How does tetracycline inhibit protein synthesis?
→Competition with new Aminoacyl t-RNA at the A site
53
How does chloramphenicol inhibit protein synthesis?
→Blocks formation of peptide bond peptidyl transferase | →Bind to 50S ribosome
54
How do erythromycin and fusidic acid inhibit protein sythesis?
→Block translocation of peptidyl t-RNA
55
What 2 infections can antibiotics be used prophylaxis?
→meningitis | →tuberculosis
56
How is antibiotic given in a meningitis case?
→i/m injection
57
Which conditions are antibiotics given topically?
→conjunctivitis →antiseptic creams →burns
58
What does minimum inhibition concentration depend on?
``` →age →weight →renal and liver function →severity of infection →susceptibility of the organism →properties of the antibiotic ```
59
What are the two pharmacodynamic properties of antibiotics killing activity?
→time-dependence | →concentration-dependence = max or area above MIC
60
Why are antibiotic combinations used?
→life-threatening infections e.g. endocarditis, septicaemia →Polymicrobial infections →Less toxic doses →synergy eg. penicillin and gentamicin →reduce antibiotic resistance e.g. Tuberculosis