Clinical Uses of Antibiotics Flashcards

1
Q

how are most penicillins administered

A

IM or IV

not very soluble or stable in stomach acid

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2
Q

what does the R-group of a penicillin determine

A

selectivity, solubility, stability, bioavailability, beta-lactamase resistance

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3
Q

what penicillins are beta-lactamase sensitive

A

benzylpenicillin, phenoxymethylpenicillin

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4
Q

what penicillins are beta-lactamase resistant

A

flucloxacillin, temocillin

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5
Q

what are some broad spectrum penicillins

A

ampicillin, amoxicillin, co-amoxiclav

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6
Q

what penicillins are anti-pseudomonal

A

piperacillin

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7
Q

what are the pharmacokinetics of benzylpenicillin

A

IM or IV slow infusion, high blood conc achieved rapidly, non-toxic, good diffusion into body and tissues, low CSF levels, long post-antibiotic effect, rapid excretion in urine

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8
Q

how to maintain benzylpenicillin blood levels

A

administer large doses

frequent dosing

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9
Q

what is benzylpenicillin used for

A

mild to moderate throat infections, otitis media, cellulitis, pneumonia, endocarditis, meningitis

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10
Q

what causes meningitis

A

neisseria meningitis, stapholococcus pneumoniae, haemophilus influenzae

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11
Q

what are the pharmacokinetics of amoxicillin

A

70-90% absorption, peak blood conc after 90 min, good CSF levels in meningitis, mainly excreted in urine

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12
Q

what are the clinical uses of amoxicillin

A

RTIs, oral infections, otitis media, sinusitis, UTIs, GI, listerial meningitis

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13
Q

what are the side effects of amoxicillin

A

hypersensitivity, neurotoxicity, renal failure, diarrhoes and pseudomembranous colitis (c. diff)

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14
Q

what is the origin of cephalosporins

A

isolated from cephalosporium acremonium

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15
Q

what are the properties of cephalosporins

A

resistant to beta lactamases, originally active against gram positive bacteria, risk of c.diff

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16
Q

what is the cephalosporin activity aainst gram positive bacteria

A

affinity for PBPs, resistant to beta lactamases

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17
Q

what is the cephalosporin activity against gram negative bacteria

A

penetration through outer membrane

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18
Q

what are second generation cephalosporins

A

active against gram positive and some gram negatives
more resistance to beta lactams
used for severe infections

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19
Q

what are third generation cephalosporins

A

broad spectrum, increased activity and increased resistance to beta lactamases
active against pseudonomas

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20
Q

what are carbapenems

A

inhibitors of cell wall synthesis

highly resistant to beta lactamases, broad spectrum activity

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21
Q

what are glycopeptides

A

inhibitors of cell wall synthesis

only active against gram positive (too large to pass through membrane of gram negative)

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22
Q

what are some examples of glycopeptides

A

vancomycin, teicoplanin

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23
Q

what is vancomycin used for

A
systemic infections (IV)
orally (c.diff)
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24
Q

what is teicoplanin used for

A

IM or IV injection for systemic infections

also for infection from b-lactam resistant organisms (MRSA)

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25
Q

what are some features of vancomycin and teicoplanin

A

penetrate CSF, excreted by kidney, cannot be absorbed through the gut, can be used orally for c.diff

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26
Q

what are the side effects of vancomycin and teicoplanin

A

pain at injection site, renal toxicity, ototoxicity, blood disorders, anaphylactoid reactions

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27
Q

what antimicrobials affect bacterial membranes

A

polymyxin (colistin) - active on gram negative bacteria (disrupt membrane and cause leakage of cytoplasm)

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28
Q

what are polymyxins used for

A

IV for resistant gram negative infections, nebulised or DPI for p.aeruginosa in GF patients

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29
Q

what are the side effects of polymyxins

A

highly neurotoxic and nephrotxic

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30
Q

what antimicrobials affect bacterial membranes

A

lipopeptides like daptomycin

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31
Q

how does daptomycin (lipopeptide) work

A

active on gram positive bacteria
rapid depolarisation of cytoplasmic membrane resulting in loss of function due to leakage of ions and depolarisation of cell

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32
Q

what are the uses of lipopeptides

A

IV for skin and soft tissue infections, endocarditis caused by resistant gram positives (MRSA)

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33
Q

what are some side effects of lipopeptides

A

nephrotoxicity, myopathy, peripheral neuropathy, colitis

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34
Q

what are examples of metabolic inhibitors of nucleic acid synthesis

A

sulphonamides, trimethoprim

sulfonamides more selective than trimethoprim

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35
Q

where do sulphonamides act

A

on para-amino benzoic acid conversion to dihydropteroic acid in nucleic acid synthesis

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36
Q

where does trimethoprim work

A

on dihydrofolic acid in nucleic acid synthesis

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37
Q

what are the uses of sulphonamides

A

limited uses

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38
Q

what are the uses for trimethoprim

A

UTI and acne

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39
Q

what are the side effects of trimethoprim

A

(rare) GI tract, allergy, myelosuppression

avoid in 1st trimester pregnancy

40
Q

what are examples of fluoroquinolones

A

ciprofloxacin, levofloxacin, moxifloxacin, ofloxacin

41
Q

what is ciprofloxacin

A

flouroquinolone

synthetic, broad spectrum, bacterialcidal, inhibit DNA gyrase and IV topisomerase

42
Q

what are the uses of ciprofloxacin

A

active against gram negative bacteria and intracellular pathogens like chlamydia, myobacteria
limited use with streptococci and enterococci

43
Q

what are the side effects of ciprofloxacin

A

GI, CNS, tendon damage, photosensitiviy, renal impairment

interacts with a lot of CYP enzymes

44
Q

what is a dietary caution with ciprofloxacin

A

avoid dairy as they contain a lot of cations

avoid iron tablets as they can affect absorption

45
Q

what is an example of a RNA polymerase inhibitor

A

rifamycin

e.g.rifampicin

46
Q

what is rifampicin

A

semi-synthetic bactericidal antibiotic

penetrates deep into bone

47
Q

what are the uses for rifampicin

A

TB, meningitis prophylaxis, infections of joints, endocarditis

48
Q

what are dietary cautions for rifampicin

A

avoid dairy or taking iron tablets at the same time

can turn urine red

49
Q

what are the side effects of rifampicin

A

hepatotoxicity, fever/rash, GI, orange-red colour to secretions
can increase metabolism of other drugs

50
Q

what is an example of a DNA inhibitor

A

nitromidazoles

e.g. metronidazole

51
Q

what are the uses of metronidazole

A

anaerobic infections, genital tract infections, SSTIs where anaerobes are suspected, abdominal and dental infections

52
Q

what are the side effects of metronidazole

A

GIT, candida infections, CNS, hypersensitivity, red/brown urine

53
Q

how does nitrofurantoin work

A

its active metabolites target DNA synthesis, RNA synthesis, protein synthesis, aerobic energyy metabolism, cell wall synthesis
it accumulates in the bladder and cannot be used on patients with a catheter

54
Q

what are the uses for nitrofurantoin

A

treating non-catheterised UTI caused by gram positive and gram negative aerobic bacteria

55
Q

summary of agents for cell wall synthesis

A

glycopeptides

56
Q

summary for agents for cell membrane

A

polymyxin

daptomycin

57
Q

summary of agents for nucleic acids

A

sulphonamides/trimethorpim, fluoroquinolones, rifamycin, metronidazole, nitrofurantoin

58
Q

what are some examples of aminoglycosides

A

gentamicin, amikacin, tobramycin, streptomycin

59
Q

what is gentamicin used for

A

serious infections caused by aerobic bacteria
active against gram negatives like pseudonomas
active against gram positives like staphylococci

60
Q

what are the pharmacokinetics of aminoglycosides

A

Iv, IM or topically for wounds, oral for gut contamination as it is not absorbed, short half life, crosses placenta, prro penetration, renal excretion

61
Q

what are the side effects of aminoglycosides

A

nephrotoxicity (reversible, caused by the drug accumulating in proximal tubule)
ototoxicity (irriversible, drug accumulates in fluid-filled inner ear and damages hair cells)

62
Q

what are examples of tetracyclines

A

coxycycline, minocycline, oxytetracycline

63
Q

what are tetracyclines used for

A

acne, RTIs, chlamydia, SSTIs

64
Q

what are the pharmacokinetics of tetracyclines

A

high absorption but decreased by cations, well distributed (inclusing foetus), accumulation and excretion in bile

65
Q

what are the side effects of tetracyclines

A

GI, deposition in forming bone/teeth, lover damage, vertigo, photosensitivity

66
Q

what are the side effects of doxycycline

A

incorporation into tissues that are calcifying at time of administration (staining of teeth)
photosensitivity from aromatic rings absorbing light energy, producing reactive O2 intermediates which can damage cell membranes

67
Q

what are macrolides

A

alternatives to penicillin for trating infections caused by streptococci

68
Q

what are examples of macrolides

A

erythromycin, azithromycin, clarithromycin

69
Q

what is the mode of action of erythromycin

A

bind 23S rNA in 50S subunit, decreasing translocation and release of tRNA

70
Q

what are the pharmacokinetics of erythromycin

A

oral or IV, acid labile, rapidly absorbed and well distributed, metabolised in liver and excreted in bile

71
Q

what are the side effects of erythromycin

A

GI, cholestatic jaundice, reversible ototoxicity, allergic reactions, cardiac arrhythmia

72
Q

what is am example of a lincosamide

A

clindamycin

73
Q

what is clindamycin used for

A

staphylococcal bone and joint infections, RTs, peritonitis, scepticaemia

74
Q

what is an example of oxazolidinones

A

linezolid

75
Q

how is linezolid used

A

infection cause by resistant gram positive bacteria (MRSA) and vancomycin resistant enterococci
no major side effects - rarely used

76
Q

what is fusidic acid

A

narrow spectrum for staphylococcal infections

77
Q

how does fusidic acid work

A

affects EF-G which supplies energy for translocation stage of protein synthesis

78
Q

what is fusidic acid used for

A

topical for skin and eye infections

oral or IV for osteomyelitis and endocarditis

79
Q

what is the mode of action for chloramphenicol

A

binds to 50s subunit and prevents peptide bond formation

80
Q

what are the pharmacokinetics of chloramphenicol

A

topical/oral/IV, penetrates all tissues including the brain, metabolised in the liver and renally excreted

81
Q

what are the side effects of chloramphenicol

A

bone marrow suppression, GI, peripheral or optic neuritis, aplastic anaemia

82
Q

what is aplastic anaemia

A

bone marrow stem cells die - normal haemopoietic cells are absent and the space is filled by adipose tissue
rare but fatal
caused by chloramphenicol

83
Q

summary of antibacterials which inhibit protein synthesis

A

aminoglycosides/oxazolidinones, tetracyclines, macrolides/lincosamides, fusidic acid, chloramphenicol

84
Q

what is the definition of surgical site infection (superficial)

A

occurs 30 days postoperatively and involves skin or subcutaneous tissue of the the incision and drainage/symptom of infection/culture

85
Q

what is the definition of surgical site infection (deep)

A

30 days postoperatively or within one year if an implant is left in place, infection involves deep soft tissues and pt has drainage/fever/localised pain and tenderness/abcess

86
Q

what is the definition of surgical site infection (organ)

A

part of the body opened during operative procedure, pt has drainage/infective organisms/abcess

87
Q

what are the meausres that can prevent surgical site infection

A

theatre airflow and workflow, skin prep, bowel prep, implants/foreign meterials containing antimicrobials, screening, prophylaxis

88
Q

what is a clean degree of contamination

A

no inflammation, respiratory/GI tract not entered

89
Q

what is clean-contaminated degree of contamination

A

respiratory/GI tracts entered without spillage

90
Q

what is contaminated degree of contamination

A

accute inflammation without pus, visible wound contamination

91
Q

what is dirty degree of contamination

A

presence of pus, compound/open injuries more than four hours old

92
Q

what is the duration of antibiotic prophylaxis recommended for a clean-contaminated proceedure

A

one dose

93
Q

what is the duration of antibiotic prophylaxis recommended for a contaminated proceedure

A

5-7 days of treatment

94
Q

when is non-surgical prophylaxis given

A

recurrent infections, endocarditis, high risk contacts (HIV, meningitis, influenza), immunosuppressed (chemotherapy)

95
Q

what is asplenia

A

removal of spleen after it ruptures
spleen stores white blood cells so pts now have higher risk of infection
prophylaxis recommended